TW200823188A - Certain chemical entities, compositions, and methods - Google Patents

Certain chemical entities, compositions, and methods Download PDF

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TW200823188A
TW200823188A TW096128145A TW96128145A TW200823188A TW 200823188 A TW200823188 A TW 200823188A TW 096128145 A TW096128145 A TW 096128145A TW 96128145 A TW96128145 A TW 96128145A TW 200823188 A TW200823188 A TW 200823188A
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ethyl
optionally substituted
amino
methyl
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TW096128145A
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Xiangping Qian
Jeffrey T Finer
Pu-Ping Lu
Chihyan Grace Chuang
Bradley P Morgan
Morgans, Jr
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Cytokinetics Inc
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Abstract

Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.

Description

200823188 九、發明說明： 本申凊案係申請2006年8月1曰申請之美國臨時專 利申請案第60/834,903號、2006年8月1日申請之美國臨 時專利申請案第60/835,183號、2006年8月1日申請之美 國臨時專利申請案第6〇/835,01〇號、2006年8月1日申請 之美國臨時專利申請案第60/834,904號、2006年8月1曰 申請之美國臨時專利申請案第60/834,901號及2006年8 月2曰申請之美國臨時專利申請案第6〇/835,236號之利 益，其全面係以引用之方式併入本文中。 【發明所屬之技術領域】 本發明係提供特定經取代雜環，包括調節平滑肌肌凝 蛋白及/或非肌肉肌凝蛋白之化學品，治療與平滑肌肌凝蛋 白及/或非肌肉肌凝蛋白相關疾病和症狀之化學品、醫藥組 合物及方法。 【先前技術】 肌凝蛋白係存在所有的肌肉及非肌肉細胞中。在人類 細胞十種不同種類的肌凝蛋白中，肌凝蛋白被認為是骨 絡肌、心臟及平滑肌收縮的主要形式。肌凝蛋白亦為存 在於非肌肉·肌凝蛋白之同質物，亦稱為細胞質肌凝蛋白。 非肌肉肌凝蛋白係無所不在地存在於真核細胞中，其中平 滑肌肌凝蛋白一般係存在於平滑肌細胞中。 肌凝蛋白-II在胺基酸組成及整體結構上明顯地與其 他9種不同的肌凝蛋白不同。肌凝蛋白_π係由二種藉由長 5 200823188 的α-螺旋捲曲-捲曲尾薄連結在一起，稱為次斷片_丨或幻 之球狀頭部區域所組成。依照蛋白質水解之狀況，肌凝蛋 白之蛋白質水解產生S1或重酶解肌球蛋白（HMM，一種帶 有截尾之二頭形式）。S1含有ATP酶及與肌動蛋白結合之 分子特性。在活體外S1已顯示能充分移動肌動蛋白絲， 且因而似乎為分子之運動區域。 雖然各種組織之肌凝蛋白_n同質物具有許多不同的 生物特性，但其分享與二對輕鏈（約20及17kDa)非共價連 結之二條重鏈二聚體（約2〇〇kDa)之相同的基本分子結 構。此二個球狀胺基端頭部係藉由二個羧基端心螺旋捲曲 的捲型形成一個尾部綁在一起。此尾部，咸信係與肌凝蛋 白分子組合成絲有關，然而頭部則被認為具有肌動蛋白活 化的Mg2+-ATP酶活性。各肌凝蛋白頭部可由三個蛋白酶 敏感區域分成約25、50及20 kDa之胜肽。此胺基酸端25 1^1^-50 1^^連結處較靠近^1>結合區，然而此肌動蛋白 結合區係接近50 kDa - 20 kDa連接處。 S1係由球狀肌動蛋白區及稱為催化區之核苷結合區 所組成。此區域係在其羧基端與具有二條約2〇kDa輕鏈各 自將其包覆之α-螺旋相連。此S1之輕鏈結合區稱為桿臂。 依仃程W過渡至行程後階段，咸信此桿臂係經由一約9〇 度的角約在靠近核絲合位置之催化區域之支點游移。此 「動力行程」係由ATP水解所驅動。 肌凝蛋白分子之另一端點為涉及肌凝蛋白分子自我 組合成雙極粗絲之α-螺旋捲曲的捲區尾部。這些粗絲交叉 6 200823188 在較細的肌動蛋⑽間4在肌肉收軸間二鋪系相互 擦身而過。此絲系滑動機制被認為與肌凝蛋白頭部中構象 改變有關’造成料ATP水狀沿_細的肌動蛋白 絲走動。當非肌肉肌凝蛋白以類似的方式作用時，已了解 其係以比平滑肌肌凝蛋白更低的速度來滑動。 、人類平滑肌肌凝蛋白之完整的cDNA已有描述。人類 平滑肌，凝蛋白之序列與人類心臟催化S1區域之肌凝蛋 白有52/〇相同性。參見，例如pCT公開案第w〇 〇3/14323 號。 10 【發明内容】 種選自式X化合物及其醫藥上 本發明係提供至少一 可接受鹽類之化學品 15 其中200823188 IX. INSTRUCTIONS: This application is filed in the US Provisional Patent Application No. 60/834,903, filed on August 1, 2006, and U.S. Provisional Patent Application No. 60/835,183, filed on August 1, 2006, U.S. Provisional Patent Application No. 6/835,01, filed on August 1, 2006, and U.S. Provisional Patent Application No. 60/834,904, filed on August 1, 2006, filed on August 1, 2006 U.S. Provisional Patent Application Serial No. 60/834,901, the entire disclosure of which is incorporated herein by reference. TECHNICAL FIELD OF THE INVENTION The present invention provides specific substituted heterocycles, including chemicals that modulate smooth muscle myosin and/or non-muscle myosin, and are associated with smooth muscle myosin and/or non-muscle myosin. Chemicals, pharmaceutical compositions and methods for diseases and conditions. [Prior Art] Myosin is present in all muscle and non-muscle cells. Among the ten different types of myosin in human cells, myosin is considered to be the main form of contraction of the osseous muscle, heart and smooth muscle. Myosin is also a homologue of non-muscle and myosin, also known as cytoplasmic myosin. Non-muscle myosin is ubiquitously present in eukaryotic cells, and smooth muscle myosin is generally present in smooth muscle cells. Myosin-II is distinctly different from the other nine different myosin proteins in the amino acid composition and overall structure. The myosin _π system is composed of two α-helical coil-curled tails of length 5 200823188, which are called sub-slices _ 丨 or phantom globular head regions. According to the state of proteolysis, the protein of myosin is hydrolyzed to produce S1 or heavy enzymatic myosin (HMM, a form with two truncated ends). S1 contains ATPase and molecular properties associated with actin. It has been shown in vitro that S1 can fully move the actin filaments and thus appears to be the region of motion of the molecules. Although myosin_n homogens of various tissues have many different biological properties, they share two heavy chain dimers (about 2〇〇kDa) that are non-covalently linked to two pairs of light chains (about 20 and 17 kDa). The same basic molecular structure. The two globular amine-terminated heads are tied together by a two-carboxy-core-coiled coiled form. In this tail, the Xianxin line is related to the combination of the muscle gelatin molecules, but the head is considered to have the actin-activated Mg2+-ATPase activity. Each myosin head can be divided into approximately 25, 50 and 20 kDa peptides by three protease sensitive regions. The amino acid end 25 1^1^-50 1^^ junction is closer to the ^1> binding region, however the actin binding region is close to the 50 kDa - 20 kDa junction. S1 is composed of a globular actin region and a nucleoside-binding region called a catalytic region. This region is linked at its carboxy terminus to the alpha-helix which has its two coated 2〇kDa light chains. The light chain binding region of this S1 is referred to as a lever arm. Depending on the transition from the process W to the post-stroke phase, it is believed that the arm is moved about a fulcrum of the catalytic region near the core-bonding position by an angle of about 9 degrees. This "power stroke" is driven by ATP hydrolysis. The other end of the myosin molecule is the tail of the volume involving the myosin molecule self-assembling the alpha-helical curl of the bipolar filament. These thick crosses 6 200823188 Between the thin muscles (10) 4 in the muscle retraction between the two lines. This silk-sliding mechanism is thought to be associated with a conformational change in the myosin head, causing the ATP water to move along the fine actin filaments. When non-muscle myosin acts in a similar manner, it is known to slide at a lower rate than smooth muscle myosin. The complete cDNA of human smooth muscle myosin has been described. The human smooth muscle, the sequence of the gelatin protein is 52/〇 identical to the human heart catalyzing the muscle glycoprotein in the S1 region. See, for example, pCT Publication No. W〇 〇 3/14323. 10 SUMMARY OF THE INVENTION The present invention is directed to a compound of formula X and a pharmaceutical thereof. The present invention provides at least one acceptable salt chemical 15

W係選自N及CR6，且W2係選自N及CR4，其限 制條件1為及W2二者不可皆為N ; /、 R及R係獨立地選自氫、氰基、鹵基、羥基、疊氮 土#肖基、4醯基、亞磺醯基、硫烷基、視需要經取代之 烷氧基、視需要經取代之醯氧基、視需要經取代之胺基羰 7 20 200823188 基氧基、視需要經取代之芳基氧基、視需要經取代之雜芳 基氧基、視需要經取代之雜環烷基氧基、視需要經取代之 烷氧基羰基、視需要經取代之烷基、視需要經取代之婦 基、視需要經取代之炔基、視需要經取代之芳基氧基、視 需要經取代之方基、視需要經取代之雜芳基、視需要纟<τ<取 代之雜環烧基、視需要經取代之胺基、視需要經取代之酉蠢 基、視需要經取代之胺基羰基及視需要經取代之 carbaminodoyl ； Z1係選自氫、視需要經取代之芳基、視需要經取代 之雜芳基、視需要經取代之環烷基、視需要經取代之雜環 烧基、氰基、視需要經取代之烧基、視需要經取代之醯基、 視需要經取代之烷氧基羰基、視需要經取代之胺基、視需 要經取代之胺基獄基、視需要經取代之甲脒基、視需要經 取代之烷氧基、視需要經取代之芳基氧基、視需要經取代 之雜芳基氧基、視需要經取代之雜環烷基氧基、視需要經 取代之烯基、視需要經取代之炔基、磺醯基、亞磺醯基及 硫烧基； z係遠自鼠、視需要經取代之曱肺基、魏基、視需 要經取代之烷氧基羰基、視需要經取代之醯基、視需要經 取代之_基、視需要經取代之烧基、視需要經取代之雜環 烧基、視需要經取代之雜芳基及視需要經取代之胺基幾 基； z3係選自氫、齒素及視需要經取代之烷基； R3係選自氩及視需要經取代之烷基；及 8 200823188 R6係選自氫、視需要經取代之醯基、視需要經取代 之烷基、氰基、鹵基、疊氮基、視需要經取代之胺基、視 需要經取代之烷氧基羰基、視需要經取代之胺基羰基、磺 醯基、亞磺醯基及硫烷基。 亦提供包含至少一種如本文所述之化學品與至少一 種選自載劑、佐劑及賦形劑之醫藥上可接受媒劑之醫藥組 合物。 10 15 20 t ’、仏治療一或多種與平滑肌肌凝蛋白或非肌肉肌 本文所述化學品盘至少、=化學ασ ’或包含至少一種 藥上=接受媒狀醫自載劑、佐劑及賦形劑之醫 說明將能^及具體實施例’熟習本項技術者由下列詳細 如本說明書中戶. 下列字詞或片語通常非内文中另有指出範圍，否則 如文中所用望具有下列所說明之意義。 其每次出現時之定義係與二他次以上時’ 二有所指干。 =腺苷酸5，-三磷酸 PIPES ATP DTT BSA nadh DL_W is selected from N and CR6, and W2 is selected from N and CR4, and both of the constraints 1 and W2 are not N; /, R and R are independently selected from hydrogen, cyano, halo, hydroxy. , azide soil #肖基, 4-mercapto, sulfinyl, sulfhydryl, optionally substituted alkoxy, optionally substituted methoxy, optionally substituted aminocarbonyl 7 20 200823188 Alkoxy group, optionally substituted aryloxy group, optionally substituted heteroaryloxy group, optionally substituted heterocycloalkyloxy group, optionally substituted alkoxycarbonyl group, optionally Substituted alkyl group, optionally substituted methoxy group, optionally substituted alkynyl group, optionally substituted aryloxy group, optionally substituted aryl group, optionally substituted heteroaryl group, optionally纟<τ<substituted heterocycloalkyl, optionally substituted amino group, optionally substituted oxime, optionally substituted aminocarbonyl, and optionally substituted carbaminodoyl; Z1 is selected from hydrogen , optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally taken a heterocyclic alkyl group, a cyano group, an optionally substituted alkyl group, an optionally substituted fluorenyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted amino group, or an optionally substituted amino group. Prison base, optionally substituted formazan group, optionally substituted alkoxy group, optionally substituted aryloxy group, optionally substituted heteroaryloxy group, optionally substituted heterocycloalkane Alkoxy group, optionally substituted alkenyl group, optionally substituted alkynyl group, sulfonyl group, sulfinyl group and thiol group; z system far from mouse, optionally substituted silicyl group, Weiji a substituted alkoxycarbonyl group, optionally substituted fluorenyl group, optionally substituted yl group, optionally substituted alkyl group, optionally substituted heterocyclic alkyl group, optionally substituted a heteroaryl group and an optionally substituted amino group; z3 is selected from the group consisting of hydrogen, dentate and optionally substituted alkyl; R3 is selected from argon and optionally substituted alkyl; and 8 200823188 R6 An alkyl group selected from the group consisting of hydrogen, optionally substituted, alkyl, cyano, halo, or Group, the optionally substituted amino group, the optionally substituted alkoxycarbonyl group, an optionally substituted amino group of the carbonyl group, sulfo acyl, sulfinyl group and sulfanyl. Pharmaceutical compositions comprising at least one chemical as described herein and at least one pharmaceutically acceptable vehicle selected from the group consisting of carriers, adjuvants and excipients are also provided. 10 15 20 t ', 仏 treatment of one or more of the smooth muscle myosin or non-muscle muscles described herein at least, = chemical ασ ' or contains at least one drug = accept the media from the drug, adjuvant and The medical instructions for the excipients will be able to and the specific examples of those skilled in the art are as follows. The following words or phrases are usually not specified in the text, otherwise the following is expected as the text The meaning of the description. The definition of each occurrence is related to two times. = adenosine 5,-triphosphate PIPES ATP DTT BSA nadh DL_

Ail 蘇糖醇 牛血清白蛋白 菸鹼醯胺腺嘌呤二核苷 9 200823188 PEP =磷酸烯醇丙酮酸 EGTA -乙二醇-雙(2_胺基乙基醚)-N，N，N’，N’-四乙酸Ail threitol bovine serum albumin nicotine indoleamine adenine dinucleoside 9 200823188 PEP = phosphoenolpyruvate EGTA-ethylene glycol-bis(2-aminoethyl ether)-N,N,N', N'-tetraacetic acid

Ac =乙醯基 APCI =大氣壓化學電離Ac = ethyl sulfhydryl APCI = atmospheric pressure chemical ionization

Atm =大氣壓Atm = atmospheric pressure

Boc 二第二丁氧基幾基 c- =環 CBZ =苄氧基羰基=苯甲基氧基羰基 CDI =羰基二咪唑 10 15 DCM =二氯甲烷=申曱基氯=CH2C12 DIAD =疊氮二羧酸二異丙酯 DIE A = DIPEA二N，N-二異丙基乙基胺 DMAP = 4-(二甲基胺基)吡啶 DMF = N，N-二曱基曱醯胺 DMSO =二甲基亞砜 (DPPF)PdCl2二[1，Γ -雙(二苯基膦基)二茂鐵]二氯鈀(II)Boc di-butoxyl group c- = ring CBZ = benzyloxycarbonyl = benzyloxycarbonyl CDI = carbonyl diimidazole 10 15 DCM = dichloromethane = decyl chloride = CH2C12 DIAD = azide dicarboxylic acid Diisopropyl ester DIE A = DIPEA di N,N-diisopropylethylamine DMAP = 4-(dimethylamino)pyridine DMF = N,N-didecylguanamine DMSO = dimethyl Sulfone (DPPF) PdCl2 bis[1,Γ-bis(diphenylphosphino)ferrocene]dichloropalladium(II)

Et = 乙基Et = ethyl

EtOAc 1=1 乙酸乙酯EtOAc 1 = 1 ethyl acetate

EtOH = 乙醇 g = 克 GC = 氣體層析 Η或hr = 小時 HATU 二 0-(7-氮雜苯并三唑-1·基)-Ν，Ν，Ν,Ν’-四曱基 六磷酸錁 10 20 200823188 HBTU = O·(苯并三唑-1-基)-N，N，N，N’-四曱基六磷酸 - - 錁 _ HOBT = 1-羥基苯并三唑 HPLC = 南壓液相層分析 5 1- = 異 kg 或 Kg = 公斤 L或1 = 公升 LC/MS = LCMS =液相層析-質譜 LDA = 二異丙基醯胺鋰 ίο LRMS = 低解晰質譜 m/z = 質量對電核比率 Me = 曱基 NMP = N-曱基-2-吡咯酮 NMR - 核磁共振 15 MPLC = 中壓液相層析 min = 分鐘 mL 二 毫升 MW = 微波 n- 二 正- 20 Ph = 苯基 (Ph3P)4Pd=肆(三苯基膦)鈀(0) (Ph3P)2PdCl2 -二氯雙(三苯基膦)鈀(II) RP-HPLC 二逆相南壓液相層析 Rt 或 RT = 室溫 11 200823188 ^ sec- =第二 > tert- =第三 四丁基氟化銨 TBS 5 TES TMS TFA THF TLC !〇 UV Vol TBDMS =四丁基二曱基石夕烧 三乙基矽烷基或三乙基矽烷 三曱基矽烷基或三甲基矽烷 三氟乙酸 四氳呋喃 薄層層析 紫外線 mL/g或L/Kg之體積當望*或除非另有說明否則 為限制試劑 ' 不是在字母間或符號間之破折號(“_“)係用來指出取 代基之連接點。例如_c〇nh2係經由碳原子來連結。 「視需要(optional或optionally)」係指隨後所述的事 件或情況可能發生或可能不發生，且該說明包括其中事件 或情況發生之例子及其中事件或情況不發生之例子。例 如，「視需要經取代之烧基」涵蓋如下所定義之「燒基 及「經取代烷基」。熟習本項技術者應了解，所指的任^ 含有一或多個取代基之基團並不希望導入任何立體上不 切實際，合成上不可行及/或本質上不穩定之取代或取代 模式。 本文所用之術ATP轉」係指能水解Ατρ之酵素。 ΑΤΡ酶包括包含分子馬達例如肌凝蛋白之蛋白質。 12 200823188 「烷基」包含具有所指碳原子數之直鏈和支鍵，通常 從1至20個碳原子，例如1至8個峻原子，如1至6個 碳原子。例如CrC6烷基包含從1至6個碳原子之直連和 支鏈烷基二者。烷基基團之實例包括曱基、乙基、丙基、 異丙基、正丁基、第二丁基、第三丁基、戊基、2-戊基、 異戊基、新戊基、己基、2-己基、3-己基、3-甲基戊基及 其類似物。伸烧基為另一種烧基之子基，係指與烧基相同 的殘基，但具有二個連接點。伸烷基基團通常會具有從2 至20個碳原子，例如2至8個碳原子，如從2至6個碳 原子。例如，CG伸烷基係指一共價鍵，而Ci伸烷基為伸 甲基基團。當具有一特定數目碳原子之烷基殘基經命名 後’係希望涵蓋所有具有該等碳原子數之幾何組合；因 此’例如「丁基」係指包括正丁基、第二丁基、異丁基及 第三丁基；「丙基」包括正丙基及異丙基。「低碳烷基」係 指具有一至四個碳之垸基基團。 「稀基」係指不飽和支鏈或直鏈烷基基團，其具有至 少一個藉由從原烯基之單一碳原子上移除一個氫原子所 衍生之碳-碳雙鍵。此基團之雙鍵可為順式或反式構形。 典型的烯基基團包括(但不限於）乙稀基；丙稀基例如丙小 烯-1-基、丙-1-稀：基、丙_2_烯小基(稀丙基）、丙_2_烯士 基、環丙-1-烯-1-基；環丙_2-烯基；丁烯基例如丁 烯小基、丁小烯么基、2_甲基-丙+嫦小基、丁 _2鲁卜 基、丁-2-烯-1-基、丁_2_烯_2_基、丁_i，3_二烯-卜基、丁4,3-一烯-2-基、裱丁-1_烯_1_基、環丁_丨·烯_3_基、環丁 13 200823188 j-i-基；及其類似物。在料實施例中，烯基 攸2至20個碳原子，右甘 y 图/、有 子。 十在其他實施例中係從2至6個碳原 5 15 ，「块基」係指讀和支鏈或直麟基基®，其具有至 少一個藉由從原炊其夕留 /、百至 之π #夹@、土早—碳原子上移除一個氫原子所 :生之奴，缝。典型的块基基團包括(但不限 基；丙炔翻如w基n炔·ιυ炔基例Γ 丁-^1-基、丁小快_3_基、丁冬炔小基；及其類似物。 在4寸定貫施例中，炔基基團具有從2至2〇個碳原子，而 在其他貝施例中係從3至6個碳原子。 壞烷基」係指非芳香碳環，通常具有從3至7個環 碳原子。此環可為飽和或具有一或多個碳_碳雙鍵。環烷 基基團之實例包括環丙基、環丁基、環戊基、環戊烯基、 環己基及環己烯基，以及橋連和籠形飽和環基團例如正葙 烷。 「烧氧基」係指經由一氧橋連結所指碳原子數目之烷 基基團，例如曱氧基、乙氧基、丙氧基、異丙氧基、正丁 氧基、第二丁氧基、第三丁氧基、戊基氧基、2-戊基氧基、 異戊基氧基、新戊基氧基、己基氧基、2-己基氧基、3-己 基氧基、3-甲基戊基氧基及其類似物。烧氧基基團通常具 有經由氧橋連結從1至7個碳原子。「低碳烷氧基」係指 具有一至四個碳之烷氧基基團。 術語「曱脒基」係指-C(=NH)-NH2基團。術語「經取 代曱脒基」係指化學式-C(=NR’)-NR”R”，其中各R”基團 14 200823188 係獨立地選自氫、視需要經取代之烧基、視需要經取代之 烷氧基、視需要經取代之胺基羰基、視需要經取代之芳 基、視需要經取代之雜芳基、視需要經取代之雜環基、醯 基、烷氧基羰基、硫烷基、亞磺醯基及磺醯基，而R，係選 自氫、氰基、視需要經取代之烷基、視需要經取代之烷氧 基、視需要經取代之胺基羰基、視需要經取代之芳基、 ^經取代之雜芳基、視f要經取代之雜環基、酿^、燒 氧基縣、硫烧基、亞續醯基及續醯基 ϋ ^ 少-個R，或R，，基團不為氫。 市仏件為至 「早及二_炫基甲醯胺」包括式-(C=〇)NRaRh之其 ^，其巾Ra及Rb_立地選自氫 ^ 基團，「:其:制^ 侧(二^ ^ 土 7 ，（方基）_C(〇)-;(雜芳其 15 基)-c(〇)-基團，其中該基團係;及（雜環燒 結，且其中烧基、環烧基、芳基月匕基與原結構連 文中所述。醯基基團具有所指馬方土及雜環烧基係如 係包括在碳原子數中。例如反原子數，而氧基團之碳 CH3(〇〇)_之乙醯基基團。，C2醯基基團為具有式 「「甲醯基」係指-C(〇)H基圏。 「羧基（carboxy)」及/或「 -C(0)0H基團。 缓基（carboxyl)」係指 「烷氧基羰基」係指經 基)(〇〇)-之基團，其中該烷 1基奴連接之式（烷氧 土基團具有所指數目之碳 20 200823188 原子。因此，CrQ烷氧基羰基基團為一具有從1至6個 碳原子，經由其氧與羰基連結阜連結之烷氧基基團。 「胺基」係指-NH2基團。 「單-及二-(烷基)胺基」包括二級和三級烷基胺基基 5 團，其中烷基基團係如上所定義且具有所指數目之碳原 子。The point of attachment of the烷基胺基基團之連結點 係在氮上。單-及二-(烷基）胺基基團之實例包括乙基胺 基、二甲基胺基及甲基-丙基-胺基。 術語「胺基幾基」係指-C0NRbRc基團，其中Rb係選 10 自Η、視需要經取代之CrC6烧基、視需要經取代之環烧 基、視需要經取代之雜環烷基、視需要經取代之芳基及視 需要經取代之雜芳基；而Rc係獨立地選自氫及視需要經 取代之CrC4炫基；或Rb及與其相鍵結之氮共同形成 一視需要經取代之5-至7-員含氮之雜環烷基，其視需要在 15 雜環烷基環中包括1或2個選自〇、N及S之額外的雜原 子；其中各經取代之基團係獨立地經一或多個獨立地由下 列選出之取代基取代：CrC4烷基、芳基、雜芳基、芳基 -C1-C4少元基-、雜方基-C1-C4烧基-、Ci_C4 1¾基烧基、-〇cllec 烷基、-0CrC4烷基苯基、-CrC4烷基-OH、-OCrC4鹵基 20 烷基、鹵基、-OH、-NH2、-CrC4 烷基-丽2、-N(CVc4 烷 基)(CrC4 烧基）、-NH(CrC4 烧基）、-WCrQ *完基)(crc4 文元基本基）、-NH(Ci_C4纟元基苯基）、氰基、确基、氧基(如 作為環烷基、雜環烷基或雜芳基之取代基）、_c〇2H、 -C(0)0CrC4 烷基、C〇N(CrC4 烷基）(CrC4 烷基）、 16 200823188 -CONH(CrC4 烷基）、-CONH2、-NHC(0)(CrC4 烷基）、 -NHC(〇)(苯基）、，N(CrC4 烷基）C(0)(CrC4 烷基 乂、 -N(CrC4 烷基)C(0)(苯基）、_C(0)CrC4 烷基、_c(o)crc4 烷基苯基、-C(0)CrC4鹵基烷基' -〇c(〇)CrC4烷基、… S〇2(CrC4 炫基）、-S〇2(苯基）、_S〇2(CrC4 g 基烧基）、 -S02NH2、_S02NH(CrC4 烷基）、_S〇2NH(苯基）、 -NHS〇2(CrC4 烷基）、-NHS〇2(苯基)及-NHS〇2(CrC4 卣基 烷基）。 ^ 「芳基」包括： 6-員碳環芳香環，例如苯； ’例如萘、氫茚及 雙環系，其中至少有一個環為芳香碳環 四氫萘；以及 ，、T至^、有 一π -V々，自、吸银，例如苐。 15 20 例如’芳基包括6-員芳香碳環與含有一或多個選 Ν、〇及S雜原子之5-至7_員雜環烷其护细』y 雙環系其巾财其卜健料香^ 烧基環上。由經取代苯衍生物二成之二^ 基及在裱原子上具有三價者係稱為經取只 三價之碳原子移除一個氳，名稱末土。猎由從 自單價多環煙基之二價基，係二為亞^ 對應的單價基之名稱上來命名，例如，^(_ldene)」加到 蔡基基團係稱為亞萘基。然而，點之 面不與雜芳基重複，其分別定義如下=讀在任何方 芳香碳環與芳香雜環烷基環稠合， 右或多個 所生成的環系為雜芳 17 200823188 基，而非如文中所定義之芳基。 術語「芳基氧基」係指-〇-芳基基團。 $語「芳烷基」係指-烷基_芳基基團。 「甲脉基」係指_C(=NH)-NH2基團。 代氫=、視需要經取代之烧基、視需要經取 ^之衣絲、視需要經取代之芳基、視需要經 基及視需要經取代之雜環絲；❿Rf =方 白·与、H A J八汉κ係獨立地選 10 15 、·虱、視萬要經取代之烷基、視需要經取代之 視需要經取狀絲、視需要經取代之雜綠及視需"^經 取代之雜環烷基，但其限制條件為Re、1^及R9至少有二 個不為氫’且其中經取代之烧基、環燒基、芳基環烧 ，及雜芳基係分別指絲、魏基、芳基、雜環烧基及ς 芳基其中-或多個(例如至高5個，例如至高3個）氫經獨 立地由下列選出之取代基取代： R、-OR、視需要經取代之胺基（包括_NRCc〇Rb、 -NRcC02Ra、_NRec〇NRbRC、_NRbc(NRC)NRbRC、 -NRbC(NCN)NRbRc 及 _NrS〇2Ra)、鹵基、氰基、硝基、氧 基(作為環烷基、雜環烷基及雜芳基之取代基）、視需要經 取代之醯基(例如CORb)、視需要經取代之烷氧基羰基(例 如-C〇2Rb)、胺基幾基(例如 CONRbRc)、_〇c〇Rb、-OC〇2Ra、 -OCONRbRe、-OP(〇)(ORb)ORc、硫烷基(例如 SRb)、亞磺 醯基(例如-SORa)及石黃醯基(例如_s〇2Ra &_s〇2NRbRc)， 其中Ra係選自視需要經取代之C!_C6烷基、視需要經取代 20 200823188 之芳基及視需要經取代之雜芳基，EtOH = ethanol g = gram GC = gas chromatography hr or hr = hour HATU dioxo 0-(7-azabenzotriazol-1·yl)-Ν,Ν,Ν,Ν'-tetramethylene hexaphosphate 10 20 200823188 HBTU = O·(benzotriazol-1-yl)-N,N,N,N'-tetradecylhexaphosphate- - 锞_ HOBT = 1-hydroxybenzotriazole HPLC = South Pressure Phase analysis 5 1- = isokg or Kg = kg L or 1 = liter LC/MS = LCMS = liquid chromatography-mass spectrometry LDA = lithium diisopropyl guanamine ίο LRMS = low resolution mass spectrum m/z = Mass to Electron Nucleus Ratio Me = 曱-based NMP = N-mercapto-2-pyrrolidone NMR - NMR 15 MPLC = Medium Pressure Liquid Chromatography min = min mL 2 ml MW = Microwave n- 二正 - 20 Ph = Phenyl (Ph3P)4Pd=肆(triphenylphosphine)palladium(0)(Ph3P)2PdCl2-dichlorobis(triphenylphosphine)palladium(II) RP-HPLC two reversed phase south pressure liquid chromatography Rt or RT = room temperature 11 200823188 ^ sec- = second > tert- = third tetrabutylammonium fluoride TBS 5 TES TMS TFA THF TLC !〇UV Vol TBDMS = tetrabutyl bismuth sulphate triethyl decane Or triethyl decane tridecyl decyl or trimethyl decane trifluoroacetic acid tetrahydrofuran Layer chromatography UV mL / g or L / Kg of volume when looking * unless otherwise stated or otherwise, as limiting reagent 'is not (' _ ") is used to indicate the connection point of the substituents dashes between the letters or between symbols. For example, _c〇nh2 is linked via a carbon atom. "Optional or optional" means that the event or circumstance described below may or may not occur, and the description includes examples in which the event or circumstance occurs and instances in which the event or circumstance does not occur. For example, "the base to be substituted as needed" encompasses "alkyl and "substituted alkyl" as defined below. Those skilled in the art will appreciate that the reference to a group containing one or more substituents is not intended to introduce any sterically impractical, synthetically infeasible and/or substantially unstable substitution or substitution pattern. . As used herein, "ATP trans" refers to an enzyme that hydrolyzes Ατρ. Chymase includes a protein comprising a molecular motor such as myosin. 12 200823188 "Alkyl" embraces straight and branched bonds having the indicated number of carbon atoms, usually from 1 to 20 carbon atoms, for example from 1 to 8 such as from 1 to 6 carbon atoms. For example, a CrC6 alkyl group contains both straight and branched alkyl groups of from 1 to 6 carbon atoms. Examples of alkyl groups include mercapto, ethyl, propyl, isopropyl, n-butyl, t-butyl, t-butyl, pentyl, 2-pentyl, isopentyl, neopentyl, Hexyl, 2-hexyl, 3-hexyl, 3-methylpentyl and the like. The extension group is a subunit of another alkyl group and refers to the same residue as the base, but has two attachment points. The alkylene group will typically have from 2 to 20 carbon atoms, such as from 2 to 8 carbon atoms, such as from 2 to 6 carbon atoms. For example, CG alkyl refers to a covalent bond and Ci alkyl has a methyl group. When an alkyl residue having a specified number of carbon atoms is named, it is intended to encompass all geometric combinations having the number of such carbon atoms; thus, for example, "butyl" is meant to include n-butyl, second butyl, iso Butyl and tert-butyl; "propyl" includes n-propyl and isopropyl. "Lower alkyl" means an fluorenyl group having one to four carbons. "Thin base" means an unsaturated branched or straight chain alkyl group having at least one carbon-carbon double bond derived by the removal of one hydrogen atom from a single carbon atom of the original alkenyl group. The double bond of this group can be in a cis or trans configuration. Typical alkenyl groups include, but are not limited to, ethylenyl; propyl groups such as propylene small-1-yl, prop-1-enyl: propyl-2-phenylene (dilyl), propyl _2_ethenyl, cycloprop-1-en-1-yl; cycloprop-2-enyl; butenyl group such as butenyl, butylenyl, 2-methyl-propene Base, butyl 2 ububyl, but-2-en-1-yl, but-2-en-2-yl, butyl-i, 3-diene-buyl, butane 4,3-alene-2 - ketone, ketone-1 - ene-1-yl, cyclobutyl hydrazine -3-yl, cycline 13 200823188 ji-yl; and analogs thereof. In the examples, the alkenyl group is 2 to 20 carbon atoms, and the right is y. In other embodiments, from 2 to 6 carbon atoms, 5 15 , "block base" refers to read and branched or straight Lin base ®, which has at least one by leaving from the original π #夹@,土早—The removal of a hydrogen atom from a carbon atom: a slave of life, a seam. Typical radical groups include (but are not limited to; propynes such as w-based n-alkyne-methane-alkynyl) ---l-yl, butyl _3_yl, butyryne small group; and the like In a 4-inch example, an alkynyl group has from 2 to 2 carbon atoms, while in other shell examples it has from 3 to 6 carbon atoms. A bad alkyl group refers to a non-aromatic carbon. The ring typically has from 3 to 7 ring carbon atoms. The ring may be saturated or have one or more carbon-carbon double bonds. Examples of cycloalkyl groups include cyclopropyl, cyclobutyl, cyclopentyl, Cyclopentenyl, cyclohexyl and cyclohexenyl, and bridged and caged saturated cyclic groups such as n-decane. "Alkoxy" means an alkyl group having the number of carbon atoms bonded via an oxygen bridge. , for example, an oxiranyloxy group, an ethoxy group, a propoxy group, an isopropoxy group, a n-butoxy group, a second butoxy group, a third butoxy group, a pentyloxy group, a 2-pentyloxy group, an isopenic group Alkoxy, neopentyloxy, hexyloxy, 2-hexyloxy, 3-hexyloxy, 3-methylpentyloxy and the like. The alkoxy groups typically have linkage via an oxygen bridge From 1 to 7 carbon atoms. "Lower alkoxy "Alkyloxy group having one to four carbons. The term "mercapto" refers to a -C(=NH)-NH2 group. The term "substituted thiol" refers to the formula -C(=NR ')-NR"R", wherein each R" group 14 200823188 is independently selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted aminocarbonyl, optionally A substituted aryl group, optionally substituted heteroaryl group, optionally substituted heterocyclic group, fluorenyl group, alkoxycarbonyl group, sulfanyl group, sulfinyl group and sulfonyl group, and R, An alkyl group selected from the group consisting of hydrogen, cyano, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted aminocarbonyl, optionally substituted aryl, ^substituted heteroaryl, f. The substituted heterocyclic group, the aryl group, the oxyalkyl group, the thiol group, the hydrazine group, and the hydrazine group ϋ are less than one R, or R, and the group is not hydrogen. To "early and bis-methyl carbamide" includes the formula -(C=〇)NRaRh, its towel Ra and Rb_ are selected from the group consisting of hydrogen^, ": its: system side (two ^ ^ Soil 7 , (square base) _C (〇)-; a 15()-c(〇)- group in which the group is; and (heterocycle sintered, and wherein the alkyl group, the cycloalkyl group, the aryl fluorenyl group and the original structure are described in the text. Amidino group Having the indicated horseshoe and the heterocyclic alkyl group are, for example, included in the number of carbon atoms, such as a counter atomic number, and the carbon group of the oxygen group CH3(〇〇)_, an alkyl group. The group has the formula ""carboyl group" refers to the -C(〇)H group. "carboxy" and/or "-C(0)0H group. "carboxy" means "alkane" "Alkoxycarbonyl" refers to a radical of the radical (〇〇)- wherein the alkane 1 is bonded to the formula (the alkoxylate group has the indicated number of carbons 20 200823188 atoms). Thus, the CrQ alkoxycarbonyl group is an alkoxy group having from 1 to 6 carbon atoms via which the oxygen and the carbonyl group are bonded to each other. "Amine" refers to a -NH2 group. "Mono- and di-(alkyl)amino" includes both secondary and tertiary alkylamino-5 groups wherein the alkyl group is as defined above and has the indicated number of carbon atoms. The point of attachment of the alkylamino group is attached to the nitrogen. Examples of the mono- and di-(alkyl)amino group include an ethylamino group, a dimethylamino group, and a methyl-propyl-amino group. The term "amino" refers to a -C0NRbRc group wherein Rb is selected from the group consisting of, optionally substituted, CrC6 alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, Optionally substituted aryl and optionally substituted heteroaryl; and Rc is independently selected from hydrogen and optionally substituted CrC4 leuco; or Rb and its bonded nitrogen form a desired Substituted 5- to 7-membered nitrogen-containing heterocycloalkyl, which optionally includes 1 or 2 additional heteroatoms selected from the group consisting of ruthenium, N and S in the 15 heterocycloalkyl ring; The groups are independently substituted by one or more substituents independently selected from the group consisting of: CrC4 alkyl, aryl, heteroaryl, aryl-C1-C4 oligo-, heteroaryl-C1-C4 Base-, Ci_C4 13⁄4 base, -〇cllec alkyl, -0CrC4 alkylphenyl, -CrC4 alkyl-OH, -OCrC4 halo 20 alkyl, halo, -OH, -NH2, -CrC4 alkyl - Li 2, -N (CVc4 alkyl) (CrC4 alkyl), -NH (CrC4 alkyl), -WCrQ * complete) (crc4 phenobase), -NH (Ci_C4 fluorenyl phenyl), Cyano, acetyl, oxy (eg as cycloalkyl) a substituent of a heterocycloalkyl or heteroaryl group), _c〇2H, -C(0)0CrC4 alkyl, C〇N(CrC4 alkyl)(CrC4 alkyl), 16 200823188 -CONH(CrC4 alkyl), -CONH2, -NHC(0)(CrC4 alkyl), -NHC(〇)(phenyl), N(CrC4 alkyl)C(0)(CrC4 alkyl fluorene, -N(CrC4 alkyl)C( 0) (phenyl), _C(0)CrC4 alkyl, _c(o)crc4 alkylphenyl, -C(0)CrC4 haloalkyl'-〇c(〇)CrC4 alkyl,... S〇2 (CrC4 炫), -S〇2 (phenyl), _S〇2 (CrC4 g based alkyl), -S02NH2, _S02NH(CrC4 alkyl), _S〇2NH(phenyl), -NHS〇2 (CrC4 Alkyl), -NHS〇2 (phenyl) and -NHS〇2 (CrC4 mercaptoalkyl). ^ "Aryl" includes: 6-membered carbocyclic aromatic ring, such as benzene; 'eg naphthalene, hydroquinone and a bicyclic ring system in which at least one ring is an aromatic carbocyclic tetrahydronaphthalene; and, T to ^, a π-V 々, self-, silver-absorbing, such as ruthenium. 15 20 For example, 'aryl group includes 6-member aromatic carbocyclic ring And 5- to 7-membered heterocycloalkanes containing one or more selected hydrazine, hydrazine and S heteroatoms, which are protected by a y-bicyclic ring, which is derived from substituted benzene. Object Group, and bis ^ into those having a trivalent atomic system mounted on only referred to via the taking of a trivalent carbon atoms removing a heavy atmosphere, the end of the name of the soil. Hunting is named from the name of the monovalent group corresponding to the monovalent polycyclic nicotine group, and the second is the subunit of the subunit, for example, ^(_ldene) is added to the Caiqui group called naphthylene. However, the faces of the dots are not repeated with heteroaryl groups, which are respectively defined as follows = read at any of the aromatic carbon rings fused to the aromatic heterocycloalkyl ring, and the right or more of the resulting ring system is heteroaryl 17 200823188, and An aryl group other than as defined herein. The term "aryloxy" refers to a -〇-aryl group. The term "aralkyl" refers to an -alkyl-aryl group. "A group" refers to a _C(=NH)-NH2 group. Substituting hydrogen =, if necessary, substituted base, if necessary, by taking the silk, optionally substituted aryl, optionally via, and optionally substituted heterocyclic filament; ❿Rf = square white · and The HAJ Bahan κ series independently selects 10 15 , · 虱, depending on the alkyl group to be replaced, if necessary, it needs to be replaced by the silk, if necessary, replaced by green and as needed a heterocycloalkyl group, but the limitation is that at least two of Re, 1 and R9 are not hydrogen' and wherein the substituted alkyl, cycloalkyl, aryl ring, and heteroaryl are respectively referred to , Wei, aryl, heterocycloalkyl and fluorene wherein one or more (for example up to 5, for example up to 3) hydrogen are independently substituted by the substituents selected below: R, -OR, as needed Substituted amine groups (including _NRCc〇Rb, -NRcC02Ra, _NRec〇NRbRC, _NRbc(NRC)NRbRC, -NRbC(NCN)NRbRc and _NrS〇2Ra), halo, cyano, nitro, oxy ( a substituent which is a cycloalkyl group, a heterocycloalkyl group and a heteroaryl group, an optionally substituted thiol group (for example, CORb), an optionally substituted alkoxycarbonyl group (for example, -C〇2Rb), Amino groups (eg, CONRbRc), _〇c〇Rb, -OC〇2Ra, -OCONRbRe, -OP(〇)(ORb)ORc, sulfanyl (eg, SRb), sulfinyl (eg, -SORa) And a sulphate group (for example, _s〇2Ra &_s〇2NRbRc), wherein Ra is selected from a C?_C6 alkyl group which is optionally substituted, an optionally substituted aryl group of 20 200823188 and optionally substituted heteroaryl group ,

Rb係選自Η、視需要經取代之Ci_C6絲、視需要經取代 之方基及視需要經取代之雜芳基；以及Rb is selected from the group consisting of hydrazine, a Ci_C6 filament which is optionally substituted, a substituted radical, and optionally substituted heteroaryl;

Re係獨立地選自氫及視需要經取代之Ci_C4烷基；或 5 RK於其相連結之Μ彡成—視需要經取代之雜環烧基 基團；且 其中各視需要經取代之基團為未取代或獨立地經一或多 個，例如一、二或三個獨立地由下列選出之取代基取代： CrC4烧基、芳基、雜芳基、芳基-crc4烷基-、雜芳基-Q-C4 10 烧基-、C1-C4鹵炫基、-〇CrC4烧基、_〇(^_〇：4烧基苯基、Re is independently selected from the group consisting of hydrogen and optionally substituted Ci_C4 alkyl; or 5 RK is bonded to the optionally substituted heterocycloalkyl group; and wherein each substituent is optionally substituted The group is unsubstituted or independently substituted with one or more, for example one, two or three substituents independently selected from the group consisting of: CrC4 alkyl, aryl, heteroaryl, aryl-crc4 alkyl-, hetero aryl-Q-C4 10 alkyl group, C1-C4 halogen group, -〇CrC4 alkyl group, _〇(^_〇: 4-alkylphenyl group,

-Crc4烧基-OH、-OCrC4鹵烧基、齒基、_〇H、-NH2、-CiA 烷基-NH2、-NCCrQ烷基)(CrC4烷基）、-NH(CrC4烷基）、 -N(CrC4烧基)（CrQ烧基苯基）、_NH(CrC4烧基苯基）、氰 基、硝基、氧基(作為環烷基、雜環烷基或雜芳基之取代 15 基）、-C02H、-C(0)0CrC4烧基、-CON(CrC4烷基XCVQ 烷基）、-CONHCCrQ烷基）、-CONH2、-NHC(0)(CrC4烷 基）、-NHC(0)(苯基）、-N(CrC4烷基)C(0)(CrC4烷基）、 -N(CrC4烷基)C(0)(苯基）、-C(0)CrC4烷基、-cccocvcu 苯基、-c(o)crc4鹵烷基、-〇C(0)CrC4烷基、-S02(crc4 20 烷基）、_S02(苯基）、-S02(CrC4 鹵烷基）、-S02NH2、 -S02NH(CrC4烷基）、-S02NH(苯基）、-NHS02(CrC4烷 基）、-NHS02(苯基)及-NHS02(CrC4鹵烷基）。 術語「鹵基」包括氟基、氯基、溴基及碘基，而術語 「鹵素」包括氟、氯、溴及破。 19 200823188 鹵燒基」係指具有特定數目碳 之鹵素取 氟甲基、 ❹個，高至最大容許自 i燒基之貫例包括(但不限於)三氟曱基、二 2-氟乙基及五氟乙基。 雜方基」包括： 5二員芳香單環’其含有-或多個例如!至4個，或# 只施例中1至3個選自N、〇及8之 戍在4寸 碳者； 以原子’其餘環原子為 雙環雜魏基環，其含有—❹個例如…個 ，例中1至3個選㈣、◦及s之雜原子，其餘環原 且^至少有—個雜員子係存在於芳香環上者；及* 絲環，其含有一或多個例如出個，或在特定 15 20 :='至4個選自心_之雜原子，其餘環原子為碳 且/、中至シ有一個雜員子係存在於芳香環上者。 I如’ 4芳基包括5_至7_員雜環烧基芳香環與5_至 7員環烷基或‘環烷基環稠合。就此等稠合， 環系其中僅其中-個環含有一或多個雜原子，其連 ^任何-個環上。在雜芳基基團中當8及〇之總數超過i 時，這些雜原子並不相互相鄰。在特定實施例中，雜芳基 基團中s及0原子之總數不超過2。在特定實施例中，芳 香雜環中S及0原子之總數不超過i。雜芳基基團基之實 例包括（但不限於)(係由指定第i優先之連接位置來編 號)2-吡啶基、3-吡啶基、4-吡啶基、2,3_吡畊基、3,4_吡畊 基、2,4+定基、3,5啶基、2,3_π比唑啉基、2,4_味唑基、 20 200823188 唉^主琳基、σ号唾琳基、π塞σ坐琳基、σ塞二唾琳基、四°坐基、 基、苯并噻吩基、呋喃基、苯并呋喃基、苯并咪唑啉 0 ^呷哚啉基、嗒畊基、三唑基、喹啉基、吡唑基及5,6,7,8_ 末=異°圭琳基。藉由從三價之原子移除一個氫原子，名稱 將「為「基(-yl)」，衍生自單價雜芳基之二價基，係藉由 你u亞基(_idene)」加到對應的單價基之名稱上來命名， 其 ▼有一個連結點之吡啶基團係稱為吡啶亞基。雜芳 &不包括或不與文帽定叙絲、賴基或雜環燒基重 10 15 20 經取代雜芳基亦包括經—或多個氧化物取 取代之環系，例如吡啶基队氧化物。 #壤烧基」係指帶有3至7個環原子之非 =其除了 Μ個獨立地選自氧、硫及氮之雜原子，以及 =少其中一個前述雜原子之組合外，係含有至少2個 該環可為飽和或具有—至多個碳·碳雙鍵。適人 2壞烧基基團之實例包括，例如(係由指定第 ”來編號）2·蛛定基、2,4__㈣基、2,3: 基、2♦定基、定基、定基及&底 = ^琳基基團’包括2驾基及3·嗎似(其中係指^ :、弟丄優先所編#。。、峰代雜環絲亦包括經」二 氧基(=0)或氧化物（-〇·)取代美 或夕们 Ν-氧化物、嗎淋基_Ν_氧化物=卜氧基二塞嗎定基 二氧基-1-噻嗎啉基。 ’、、基及U- 「雜環烧基」亦包括雙環系，其巾—個非芳香環通常 21 200823188-Crc4 alkyl-OH, -OCrC4 halogen group, dentate group, _〇H, -NH2, -CiA alkyl-NH2, -NCCrQ alkyl) (CrC4 alkyl), -NH(CrC4 alkyl), - N(CrC4 alkyl) (CrQ alkylphenyl), _NH(CrC4 alkylphenyl), cyano, nitro, oxy (substituted as a cycloalkyl, heterocycloalkyl or heteroaryl group 15) , -C02H, -C(0)0CrC4 alkyl, -CON(CrC4 alkyl XCVQ alkyl), -CONHCCrQ alkyl), -CONH2, -NHC(0)(CrC4 alkyl), -NHC(0)( Phenyl), -N(CrC4 alkyl)C(0)(CrC4 alkyl), -N(CrC4 alkyl)C(0)(phenyl), -C(0)CrC4 alkyl, -cccocvcu phenyl , -c(o)crc4haloalkyl, -〇C(0)CrC4 alkyl, -S02(crc4 20 alkyl), _S02(phenyl), -S02(CrC4 haloalkyl), -S02NH2, -S02NH (CrC4 alkyl), -S02NH (phenyl), -NHS02 (CrC4 alkyl), -NHS02 (phenyl), and -NHS02 (CrC4 haloalkyl). The term "halo" includes fluoro, chloro, bromo and iodo, and the term "halogen" includes fluoro, chloro, bromo and ruthenium. 19 200823188 "haloalkyl" means a halogen having a specified number of carbons, fluoromethyl, fluorene, and up to a maximum allowable range of n-alkyl groups including, but not limited to, trifluoromethyl, di-2-fluoroethyl And pentafluoroethyl. "Heterinary group" includes: 5 two-membered aromatic single ring 'which contains - or a plurality of, for example, ~ to four, or # only one to three of the examples are selected from N, 〇 and 8 in 4 inch carbon; The remaining ring atoms of the atom are bicyclic hetero-Weiyl rings, which contain - for example, one, for example, one to three (four), ◦ and s heteroatoms, and the remaining ring atoms and at least one heterogeneous sub-system exist. And on the aromatic ring; and * a silk ring containing one or more, for example, one or a specific 15 20 :=' to 4 hetero atoms selected from the heart, the remaining ring atoms are carbon and /, medium to There is a heterosexual child who is present on the aromatic ring. I, such as the '4 aryl group, includes a 5- to 7-membered heterocyclic alkyl aromatic ring fused to a 5- to 7-membered cycloalkyl or a 'cycloalkyl ring. In the case of such condensing, only one of the rings of the ring system contains one or more heteroatoms which are attached to any ring. In the heteroaryl group, when the total number of 8 and oxime exceeds i, these heteroatoms are not adjacent to each other. In a particular embodiment, the total number of s and 0 atoms in the heteroaryl group does not exceed two. In a particular embodiment, the total number of S and 0 atoms in the aromatic heterocycle does not exceed i. Examples of heteroaryl group include, but are not limited to, (numbered by the position assigned to the i-th preferred) 2-pyridyl, 3-pyridyl, 4-pyridyl, 2,3-pyrroxy, 3,4_pyrrolidine, 2,4+-fixing, 3,5-pyridyl, 2,3_π-pyrazolyl, 2,4-oxazolyl, 20 200823188 唉^main Linji, σ 唾 琳 基, π 塞 坐 坐 基 、 σ σ 坐 坐 σ σ σ σ σ σ σ σ 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 四 坐 坐Azolyl, quinolyl, pyrazolyl and 5,6,7,8-end = iso-gurin. By removing a hydrogen atom from a trivalent atom, the name will be "base (-yl)", derived from the divalent group of the monovalent heteroaryl, added to your corresponding subunit (_idene). The name of the monovalent group is named above, and the pyridyl group whose ▼ has a linking point is called a pyridyl subunit. Heteroaryl & does not include or does not bear with a cap, a lysine or a heterocycloalkyl group. The substituted heteroaryl group also includes a ring system substituted with one or more oxides, such as a pyridyl group. Oxide. #地烧基" means a non-contained atom having 3 to 7 ring atoms; in addition to a hetero atom independently selected from oxygen, sulfur and nitrogen, and a combination of one of the aforementioned heteroatoms, at least Two of the rings may be saturated or have - to multiple carbon-carbon double bonds. Examples of suitable human 2 base groups include, for example, (numbered by the designated number) 2. spider base, 2,4__(tetra)yl, 2,3: base, 2♦ base, base, base and & ^Linki group 'includes 2 drivers and 3 · like (in which refers to ^:, sister-in-law preferred edited #.., peak generation heterocyclic wire also includes "dioxy (=0) or oxide (-〇·) Substituting mei or xi Ν-oxide, 淋 基 Ν 氧化物 氧化物 氧化物 = = = = = = = = = 卜 卜 卜 氧化物 氧化物 氧化物 ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' ' 氧化物 氧化物 氧化物"Heterocyclic alkyl" also includes bicyclic rings, which are non-aromatic rings usually 21 200823188

St二二;個^原子’其除了 M個獨立地選自氧、硫及 二及包含至少其中一個前述雜原子之組合 ’、3 少2個碳原子；而另一個環通常具有3至7 個環原子，視需要合右^ 1#从 原子且不為料^有侧·^自氧、硫及氮之雜 如本文所用，「調節」係指相對於缺乏化學品之存在 下’以改變活性作為對文中所述之化： fmr為增加活性或降低活性，亦可能係因為化 a物與目‘物之直接相互作用，或因為化合物與一或多個 ，他依序影響目標物活性之因子的交互作用。例如，化學 品之存在可能’例如#由直接與目標物結合、藉由（直接 或間接）造成另-因子增加或降低目標物活性或藉由（直 接或間接)增加或降低存在細胞或生物體之目標物數量來 增加或降低目標物活性。 15 20 術語「硫院基」係包括下列基團：_s_(視需要經取代 之(C，-C6)烧基）、_s_(視需要經取代之芳基）、_s_(視需要經 取代之雜芳基)及-s_(視需要經取代之雜環烧基）。因此， 硫燒基包括crc6烷基硫烷基。 術語「亞俩基」係包括下列基團：_s(〇)·(視需要經 代之(CrC6)烧基）、_S(〇)_視需要經取代之芳基）、_s(〇)_ =需要經取代之雜芳基）、___(視需要經取^之雜環烧 土），及4(〇)_(視需要經取代之胺基）。 術語「績醯基」係包括下列基團：,2)_(視需要經 代之（crC6)烷基）、_s(〇2)-視需要經取代之芳基）、 22 200823188 娜2)_視需要經取代之雜芳基）、_s(〇2)_(視需要經 雜環烧基）、-_)-(視需要經取代之烧氧基）、_s(〇2H見· 要經取代之芳基氧基）、都士視需要經取代之雜芳基^ 基）、_s(〇2m視需要經取代之雜環基氧基）；及_8 5 需要經取代之胺基）。 如本文所用，術語「經取代」係指任何在所指的原子 或基團上之-或多個氫經由下列所指的基團中所選出者 取代，但其限制條件為不能超過該指定原子之正常價數。 當取代基為氧基時(亦即，，則取代原子上的2個氯。取 0 代基及或魏基之化合僅在此等化合產生穩定的化合物 或有用的合成中間物時才為容許的。穩定的化合物或穩定 的結構係指化合物足以從化學反應中堅定地留下分離 出，並隨後調配成具有最少實際用途之藥劑。除非另以說 明，否則取代基命名係併入核心結構。例如，應了解，當 ;(環烷基)烷基列出作為可能的取代基時，此取代基與核心 結構之連結點係在烧基部分。 如術浯「經取代」烷基、環烷基、芳基、雜環烷基及雜 芳基，除非另有定義，否則係指烷基、環烷基、芳基、雜 裱烷基及雜芳基其中一或多個（例如至高5個，例如至高3 個）氫經獨立地由下列選出之取代基取代·· -R、_OR、視需要經取代之胺基（包括-NRec〇Rb、 -NRcC02Ra > -NRcC〇NRbRc ^ -NRbC(NRc)NRbRc > -NRbC(NCN)NRbRc及视別奶、齒基、氰基、硝基、氧 基(作為環烷基、雜環烷基及雜芳基之取代基）、視需要經 23 200823188 取代之醯基例如-CORb)、視需要經取代之烷氧基羰基（例 如-C02R )、胺基幾基(例如c〇NRbRe)、_〇c〇Rb、_〇c〇2Ra、 -〇CONRbRe、_〇P(〇)(ORb)〇RC、硫烷基(例如SRb)、亞磺醯 基(例如-SORa)及磺醯基(例如_S〇2Ra& _s〇2NRbR')， 其中Ra係選自視需要經取代之CrC6烷基、視需要經取代 之環烷基、視需要經取代之雜環烷基、視需要經取代之稀 基、視需要經取代之炔基、視需要經取代之芳基及視需要 經取代之雜芳基；St 二 二; a ^ atom 'in addition to M independently selected from oxygen, sulfur and two and comprising at least one of the aforementioned combinations of hetero atoms ', 3 less than 2 carbon atoms; and the other ring usually has 3 to 7 Ring atom, if necessary, right ^ 1# from atom and not material ^ has side · ^ from oxygen, sulfur and nitrogen as used herein, "regulation" refers to the change in activity relative to the absence of chemicals As described in the text: fmr is to increase the activity or reduce the activity, may also be due to the direct interaction of the a substance with the object, or because the compound and one or more, he factors affect the activity of the target Interaction. For example, the presence of a chemical may be 'for example, by directly binding to a target, by (directly or indirectly) causing another factor to increase or decrease the activity of the target or by (directly or indirectly) increasing or decreasing the presence of a cell or organism. The number of targets to increase or decrease the activity of the target. 15 20 The term "sulphur-based" includes the following groups: _s_ (optionally substituted (C,-C6) alkyl), _s_ (optionally substituted aryl), _s_ (optionally substituted) Aryl) and -s_ (heterocyclic alkyl optionally substituted). Thus, sulfur-containing groups include crc6 alkylsulfanyl groups. The term "subunit" includes the following groups: _s(〇)·(optionally replaced (CrC6)), _S(〇)_optionally substituted aryl), _s(〇)_ = A substituted heteroaryl group is required, ___ (heterocyclic charcoal which is taken as needed), and 4 (〇)_ (an amine group which is optionally substituted). The term "performance base" includes the following groups: 2) _ (optionally substituted (crC6) alkyl), _s (〇2) - optionally substituted aryl), 22 200823188 na 2) _ If necessary, substituted heteroaryl), _s(〇2)_ (optionally substituted with a heterocyclic group), -_)- (optionally substituted alkoxy group), _s (〇2H see · to be substituted The aryloxy group, the disulfide is required to be substituted with a heteroaryl group, _s (〇2m is optionally substituted with a heterocyclic oxy group); and _8 5 requires a substituted amino group). As used herein, the term "substituted" means that any or a plurality of hydrogens on the indicated atom or group are substituted by a selected one of the groups indicated below, but the limitation is that the specified atom cannot be exceeded. The normal price. When the substituent is an oxy group (that is, it replaces two chlorines on the atom. The combination of the 0 and / or the wei group is only acceptable if these compounds are combined to produce a stable compound or a useful synthetic intermediate. A stable compound or stable structure means that the compound is sufficiently separated from the chemical reaction to be firmly separated and subsequently formulated into the agent with the least practical use. Unless otherwise stated, the substituent nomenclature is incorporated into the core structure. For example, it is understood that when a (cycloalkyl)alkyl group is listed as a possible substituent, the point of attachment of the substituent to the core structure is in the alkyl group. For example, "substituted" alkyl, naphthenic Alkyl, aryl, heterocycloalkyl and heteroaryl, unless otherwise defined, means one or more of alkyl, cycloalkyl, aryl, heteroalkyl and heteroaryl (eg up to 5) For example, up to three hydrogens are independently substituted by the substituents selected below: -R, _OR, optionally substituted amine groups (including -NRec〇Rb, -NRcC02Ra > -NRcC〇NRbRc ^ -NRbC( NRc)NRbRc > -NRbC(NCN)NRbRc and parenteral milk, dentate base, cyano group a nitro group, an oxy group (as a substituent of a cycloalkyl group, a heterocycloalkyl group and a heteroaryl group), an optionally substituted thiol group such as -CORb), and optionally substituted alkoxycarbonyl group (for example - C02R ), amino group (for example, c〇NRbRe), _〇c〇Rb, _〇c〇2Ra, -〇CONRbRe, _〇P(〇)(ORb)〇RC, sulfanyl group (for example, SRb), a sulfinyl group (for example, -SORa) and a sulfonyl group (for example, _S〇2Ra& _s〇2NRbR'), wherein the Ra is selected from the group consisting of an optionally substituted CrC6 alkyl group, optionally substituted cycloalkyl group, A substituted heterocycloalkyl group, an optionally substituted dilute group, an optionally substituted alkynyl group, an optionally substituted aryl group, and optionally a substituted heteroaryl group are required;

Rb係選自氫、視需要經取代2CrC6烷基、視需要經取代 之環烷基、視需要經取代之雜環烷基、視需要經取代之芳 基及視需要經取代之雜芳基；及 RC係獨立地選自氫及視需要經取代之Ci_C4烷基；或 R及Re與其相連結之氮形成一視需要經取代之雜環烷基 基團；及 其中各視需要經取代之基團為未取代或獨立地經一或多 個，例如一、二或三個獨立地由下列選出之取代基取代： CrC4烷基、芳基、雜芳基、芳基-Crc4烷基_、雜芳基-Ci-C4 烧基·、CrC4 i基烷基、-0Ci-c4烷基、-〇Ci_c4烷基苯基、 -CrQ 烷基_〇H、_〇CKC4 鹵基烷基、鹵基、-Of!、-NH2、 -Q-q 烧基-NH2、-N(CrC4 烷基)(CrC4 烷基）、-NH(C「C4 烧基）、-N(CrC4烷基)(CVC4烷基苯基）、-NH(CrC4烷基 苯基）、氰基、硝基、氧基(作為環烷基、雜環烷基及雜芳 基之取代基）、-C02H、-C(〇)〇CrC4 烷基、-C0N(CrC4 烷 基）(CrC4 烷基）、-coNIKCi-Q 烷基）、-C0NH2、 24 200823188 -NHC(0)(CrC4 烷基）、-NHC(0)(苯基）、-N(CVC4 燒 基）qOXCVCl· 烷基）、NiCVQ 烷基）C(0)(苯基）、 -ccokvq 烷基、-c(o)crc4 烷基苯基、-c(o)crc4 4基 烷基、-oc(o)crc4 烷基、-so2(crc4 烷基）、-so2(笨基）、 麵鹵基烧基）、-S02NH2、-SC^NHCCVQ 烧基）、 -S02NH(苯基）、-NHS02(CrC4 烷基）、-NHS02(苯基）及 -NHSC^CrQ鹵基烷基）。 術語「經取代之醯基」係指（經取代烷基)-C(0)_基團； (經取代環烷基)-c(0)-;(經取代芳基)-C(0)-;(經取代雜芳 基)_c(0)_ ;及(經取代雜環烷基)-C(0)-，其中該基團係經 由幾基功能基與原結構連結，且其中經取代烧基、環燒 基、芳基、雜芳基及雜環烷基分別係指烷基、環烷基、芳 基、雜方基及雜J辰烧基其中一或多個（例如至高5個，例如 至高3個）氫經獨立地由下列選出之取代基取代： -Ra、-ORb、視需要經取代之胺基（包括-NRcC0Rb、 -NReC02Ra、-NRoC0NRbRc、-NRbC(NRc)NRbRc、 -NRbC(NCN)NRbRi_NRcs〇2Ra)、鹵基、氰基、硝基、氧 基(作為環烷基、雜環烷基及雜芳基之取代基）、視需要經 取代之酿基(例如-CORb)、視需要經取代之烷氧基羰基(例 如-C〇2Rb)、胺基幾基（例如 _c〇NRbRe)、_〇c〇Rb、 •C^02Ra、_〇C〇NRbRe、_〇p(〇)(〇Rb)〇Re、硫烷基（例如 SR)、亞磺醯基（例如_S〇Ra)及磺醯基（例如-S〇2Ra及 _S02NRbRc)， 其中^係選自視需要經取代之crc6烷基、視需要經取代之 25 200823188 稀基、視f要娜代之祕m錄狀 經取代之㈣基；.Rb is selected from the group consisting of hydrogen, optionally substituted 2CrC6 alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, and optionally substituted heteroaryl; And the RC is independently selected from the group consisting of hydrogen and optionally substituted Ci_C4 alkyl; or R and Re are bonded to the nitrogen to form a heterocycloalkyl group which is optionally substituted; and each of the optionally substituted groups The group is unsubstituted or independently substituted with one or more, for example one, two or three substituents independently selected from the group consisting of: CrC4 alkyl, aryl, heteroaryl, aryl-Crc4 alkyl _, hetero aryl-Ci-C4 alkyl group, CrC4 i-alkyl group, -0Ci-c4 alkyl group, -〇Ci_c4 alkylphenyl group, -CrQ alkyl group 〇H, 〇 〇CKC4 haloalkyl group, halogen group, -Of!, -NH2, -Qq alkyl-NH2, -N(CrC4 alkyl) (CrC4 alkyl), -NH (C "C4 alkyl", -N(CrC4 alkyl) (CVC4 alkylphenyl) , -NH(CrC4 alkylphenyl), cyano, nitro, oxy (substituent as cycloalkyl, heterocycloalkyl and heteroaryl), -C02H, -C(〇)〇CrC4 alkane Base, -C0N (CrC4 alkyl) (CrC4 alkyl), -coNIKCi-Q alkane Base), -C0NH2, 24 200823188 -NHC(0)(CrC4 alkyl), -NHC(0)(phenyl), -N(CVC4 alkyl)qOXCVCl·alkyl), NiCVQ alkyl)C(0) (phenyl), -ccokvq alkyl, -c(o)crc4 alkylphenyl, -c(o)crc4 4 alkyl, -oc(o)crc4 alkyl, -so2(crc4 alkyl), - So2 (stupyl), face haloalkyl), -S02NH2, -SC^NHCCVQ alkyl, -S02NH(phenyl), -NHS02(CrC4 alkyl), -NHS02(phenyl), and -NHSC^CrQ Haloalkyl). The term "substituted thiol" refers to a (substituted alkyl)-C(0)- group; (substituted cycloalkyl)-c(0)-; (substituted aryl) )-C(0)-;(substituted heteroaryl)-c(0)_; and (substituted heterocycloalkyl)-C(0)-, wherein the group is via a functional group and a primary structure Linked, and wherein the substituted alkyl, cycloalkyl, aryl, heteroaryl and heterocycloalkyl are respectively one or more of alkyl, cycloalkyl, aryl, heteroaryl and hetero-alkyl Hydrogens (for example up to 5, for example up to 3) are independently substituted by the substituents selected below: -Ra, -ORb, optionally substituted amines (including -NRcC0Rb, -NReC02Ra, -NRoC) 0NRbRc, -NRbC(NRc)NRbRc, -NRbC(NCN)NRbRi_NRcs〇2Ra), halo, cyano, nitro, oxy (substituent as cycloalkyl, heterocycloalkyl and heteroaryl), A substituted aryl group (e.g., -CORb), an optionally substituted alkoxycarbonyl group (e.g., -C〇2Rb), an amino group (e.g., _c〇NRbRe), _〇c〇Rb, • C^ are required. 02Ra, _〇C〇NRbRe, _〇p(〇)(〇Rb)〇Re, sulfiliary alkyl (for example, SR), sulfinyl (for example, _S〇Ra), and sulfonyl (for example, -S〇2Ra) And _S02NRbRc), wherein ^ is selected from the optionally substituted crc6 alkyl group, if necessary, substituted 25 200823188 dilute base, according to the secret of the Na Na's secret m recorded replacement (four) base;

Rb係選自H、視需要經取代之crc6録、視需要經取代之 5 10 15 環烧基、視需要經取代之雜狀基、㈣要經取代之芳美、 及視需要經取代之雜芳基；及 土 係獨。立地選自氫及視需要經取代之Ci_Q烷基；或 R及Re與其相連結之氮形成一視需要經取代之雜環烷基基 團；及 土土 其中各視需要經取代之基團為未取代或獨立地經一或多 個，例如一、二或三個獨立地由下列選出之取代基取代·· CrC4烷基、芳基、雜芳基、芳基_Ci_c4烷基_、雜芳基_Ci_C4 烷基-、CrC4鹵基烷基、-〇crc4烷基、-OCrCt烷基苯基、 -CrC4 烧基-〇H、-OCrC4 鹵基烷基、!g 基、_〇H、一NIV-CrQ 烧基-NH2、-N(CrC4 烷基)(CrC4 烷基）、-NH(CrC4 烷基)， -N(CrC4烧基)(CrC4烷基苯基）、_NH(CrC4烷基苯基）、氰 基、确基、氧基(作為ί辰烧基、雜環炫基及雜芳基之取代 基）、-co2h、_c(o)ocrc4烷基、-CON(CrC4烷基)(crc4 烷基）、_CONH(CrC4烷基）、-CONH2、-NHC(0)(CrC4烷 基）、-NHC(0)(本基）、-N(Ci_C4烧基）C(0)(Ci_C4烧基）、 -N(CrC4烷基)C(0)(苯基）、-c(0)crc4烷基、-c(o)crc4 烷基苯基、-c(o)crc4鹵基烷基、-oc(o)crc4烷基、 -so2(crc4烷基）、-so2(苯基）、_so2(crc4鹵基烷基）、 -S02NH2、-S02NH(CrC4 烷基）、-S02NH(苯基）、 -NHS02(CrC4 烷基）、-NHS〇2(苯基)及-NHS〇2(CrC4 鹵基烷 26 20 200823188 基）。 術語「經取代之烷氧基」係指其中烷基取代基經取代 之烷氧基（亦即-0_(經取代烷基))其中「經取代烷基」係指 烷基其中一或多個（例如至高5個，例如至高3個）氫經獨立 地由下列選出之取代基取代： -R、-OR、視需要經取代之胺基（包括_NRCc〇Rb、 -NR C02Ra、-NReCONRbRe、-NRbc(NRC)NRbRC、 -NRbC(NCN)NRbRe及视cs〇2Ra)、鹵基、氛基、硝基、氧 基(作為環烷基、雜環烷基及雜芳基之取代基）、視需要經 10 15 取代之醯&基（例如-CORb)、視需要經取代之烷氧基羰基 (如-C02R )、胺基羰基(如_c〇NRbRC)、_〇c〇Rb、、 OCONR R、、硫烧基(如 sRb)、亞續酿 基(例如-SOR )及確醯基(例如_s〇2Ri_S(^NRbRC)， 其中Ra係選自視需要經取代之c i _ c 6烧基、視需要經取代 之婦基、視需要經取代之炔基、視需要經取代之芳基及視 需要經取代之雜芳基； ^係選自H、視需要經取代之心心烧基、視需要經取代之 祕基、視需要經取代之雜環烧基、視需要經取代之芳基 及視需要經取代之雜芳基；及 R:係獨。立地選自氫及視需要經取代院基；或 R及R與其減結之氮形成—視需要經取代之雜 基團；及 其中各視需要録代之基團為未取代錢立地經一或多 .口例如、一或二個獨立地由下列選出之取代基取代： 27 20 200823188Rb is selected from the group consisting of H, optionally substituted crc6, optionally substituted 5 10 15 cycloalkyl, optionally substituted heterobasic, (d) substituted, aromatic, and optionally substituted. Base; and soil system alone. The site is selected from the group consisting of hydrogen and optionally substituted Ci_Q alkyl; or R and Re are bonded to the nitrogen to form a heterocycloalkyl group which is optionally substituted; and the earthy soil is optionally substituted with a group Unsubstituted or independently substituted by one or more, for example one, two or three, independently selected from the following substituents: CrC4 alkyl, aryl, heteroaryl, aryl_Ci_c4 alkyl _, heteroaryl _Ci_C4 alkyl-, CrC4 haloalkyl, - 〇crc4 alkyl, -OCrCt alkylphenyl, -CrC4 alkyl-hydrazine H, -OCrC4 haloalkyl, !g base, _〇H, one NIV-CrQ alkyl-NH2, -N(CrC4 alkyl) (CrC4 alkyl), -NH(CrC4 alkyl), -N(CrC4 alkyl) (CrC4 alkylphenyl), _NH(CrC4 alkylbenzene , cyano, decyl, oxy (substituent as octanoyl, heterocyclic and heteroaryl), -co2h, _c(o)ocrc4 alkyl, -CON(CrC4 alkyl) Crc4 alkyl), _CONH(CrC4 alkyl), -CONH2, -NHC(0)(CrC4 alkyl), -NHC(0)(local), -N(Ci_C4 alkyl)C(0)(Ci_C4 , -N(CrC4 alkyl)C(0)(phenyl), -c(0)crc4alkyl, -c(o)crc4 alkylphenyl, -c(o)crc4haloalkyl, - Oc(o)crc4 alkyl, -so2(crc4 alkyl), -so2(phenyl), _so2(crc4haloalkyl), -S02NH2, -S02NH(CrC4 alkyl), -S02NH(phenyl), -NHS02 (CrC4 alkyl), -NHS〇2 (phenyl) and -NHS〇2 (CrC4 haloalkane 26 20 200823188). The term "substituted alkoxy" refers to an alkoxy group in which an alkyl substituent is substituted (ie, -0-(substituted alkyl)) wherein "substituted alkyl" refers to one or more alkyl groups. (for example up to 5, for example up to 3) Hydrogen is independently substituted with the substituents selected below: -R, -OR, optionally substituted amine groups (including _NRCc〇Rb, -NR C02Ra, -NReCONRbRe, -NRbc(NRC)NRbRC, -NRbC(NCN)NRbRe and cfs2Ra), a halogen group, an aryl group, a nitro group, an oxy group (as a substituent of a cycloalkyl group, a heterocycloalkyl group and a heteroaryl group), An alkoxycarbonyl group (e.g., -C02R), an aminocarbonyl group (e.g., _c〇NRbRC), _〇c〇Rb, OCONR R, a sulphur-burning group (such as sRb), a sub-continuous base (such as -SOR), and a thiol group (for example, _s〇2Ri_S(^NRbRC), wherein Ra is selected from ci _ c 6 as desired. a base group, a substituted base group, an optionally substituted alkynyl group, an optionally substituted aryl group, and an optionally substituted heteroaryl group as required; ^ is selected from H, optionally substituted core group As needed a substituent, a substituted heterocyclic alkyl group, an optionally substituted aryl group, and optionally a substituted heteroaryl group; and R: a system. The site is selected from the group consisting of hydrogen and, if desired, a substituted base; Or R and R and its reduced nitrogen form - optionally substituted hetero-group; and each of the groups as required to be substituted is unsubstituted, one or more, for example, one or two independently Substituted by the following selected substituents: 27 20 200823188

CrC4烷基、芳基、雜芳基、芳基_Cl_c4烷基_、雜芳基_Crc4 烷基-、CrC4鹵基烷基、-〇crC4烷基、-ocrc4烷基苯基、 -Crc4 烷基-OH、-OCrC4 鹵基烷基、_ 基、_〇H、_NH2、 -CrC4 烷基-NH2、-N(CrC4 烷基)(c，-C4 烷基）、-NH(CrC4 烧基）、-N(CrC4烷基)(CrC4烷基苯基）、_NH(CrC4烷基 苯基）、氰基、硝基、氧基(作為環烷基、雜環烷基及雜芳 基之取代基）、_co2h、-C(0)〇CrC4 烷基、-CON(CrC4 烷基）(CrC4 烷基）、_CONH(CrC4 烷基）、-CONH2、 -丽C(0)(CrC4 烷基）、-NHC(0)(苯基）、-N(CrC4 烷 基）C(〇)(CrC4 烷基）、-N(CrC4 烷基）C(0)(苯基）、 -c(o)crc4 烷基、-c(o)crc4 烷基苯基、-c(0)crc4 鹵基 烧基、-oc(o)crc4 烷基、-S02(crc4 烷基）、-S02(苯基）、 -SOXCVQ 鹵基烷基）、_S02NH2-S02NH(CrC4 烷基）、 -S02NH(苯基）、-NHS02(CrC4 烷基）、-NHS02(苯基）及 -NHS〇2(CrC4鹵基烷基）。在某些實施例中，經取代烷氧 基基團為「多烧氧基」或_〇_(視需要經取代之伸烧基)_(視 需要經取代之烷氧基），並包括例如-OCH2CH2OCH3之基 團，及甘油醚之殘基例如聚乙二醇和_〇(CH2CH20)xCH3， 其中X為2-20之整數，例如2-10，及例如2-5。另外的經 取代烷氧基基團為羥基烷氧基或-〇CH2(CH2)yOH，其中y 為M0之整數，例如1_4。 術語「經取代烷氧基羰基」係指（經取代烷基)-〇-C(0)-基團’其中該基團係經由羰基功能基與原結構連結，且其 中經取代係指烷基其中一或多個（例如至高5個，例如至高3 28 200823188 個）氫經獨立地由下列選出之取代基取代：-Ra、-ORb、視 需要經取代之胺基（包括-NReCORb、-NRcC02Ra、 -NRcCONRbRc、-NRbC(NRc)NRbRc、-NRbC(NCN)NRbRc及 -NRcS02Ra)、鹵基、氰基、確基、氧基(作為環烧基、雜環 烷基及雜芳基之取代基）、視需要經取代之醯基（例如 -CORb)、視需要經取代之烷氧基羰基(例如-C〇2Rb)、胺基 羰基(例如-CONRbRc)、-〇CORb、-〇〇〇2Ra、-〇CONRbRc、 -〇P(0)(ORb)ORe、硫烷基(例如SRb)、亞磺醯基(例如·s〇Ra) 及石黃醯基(例如-S02Ra及-S02NRbRc)， 其中Ra係選自視需要經取代之CrC6烷基、視需要經取代 之烯基、視需要經取代之炔基、視需要經取代之芳基及 視需要經取代之雜芳基；CrC4 alkyl, aryl, heteroaryl, aryl_Cl_c4 alkyl, heteroaryl-Crc4 alkyl-, CrC4 haloalkyl, -〇crC4 alkyl, -ocrc4 alkylphenyl, -Crc4 alkane -OH, -OCrC4 haloalkyl, _ group, _〇H, _NH2, -CrC4 alkyl-NH2, -N(CrC4 alkyl)(c,-C4 alkyl), -NH(CrC4 alkyl) , -N(CrC4 alkyl)(CrC4 alkylphenyl), _NH(CrC4 alkylphenyl), cyano, nitro, oxy (substituent as cycloalkyl, heterocycloalkyl and heteroaryl) ), _co2h, -C(0)〇CrC4 alkyl, -CON(CrC4 alkyl)(CrC4 alkyl), _CONH(CrC4 alkyl), -CONH2, -Li C(0)(CrC4 alkyl), - NHC(0)(phenyl), -N(CrC4 alkyl)C(〇)(CrC4 alkyl), -N(CrC4 alkyl)C(0)(phenyl), -c(o)crc4 alkyl , -c(o)crc4 alkylphenyl, -c(0)crc4 haloalkyl, -oc(o)crc4 alkyl, -S02(crc4 alkyl), -S02(phenyl), -SOXCVQ halo Alkyl), _S02NH2-S02NH(CrC4 alkyl), -S02NH(phenyl), -NHS02 (CrC4 alkyl), -NHS02 (phenyl), and -NHS〇2 (CrC4 haloalkyl). In certain embodiments, the substituted alkoxy group is "polyalkyloxy" or _〇_ (optionally substituted alkyl) - (optionally substituted alkoxy), and includes, for example a group of -OCH2CH2OCH3, and a residue of a glyceryl ether such as polyethylene glycol and 〇(CH2CH20)xCH3, wherein X is an integer from 2 to 20, for example 2 to 10, and for example 2 to 5. The additional substituted alkoxy group is hydroxyalkoxy or -〇CH2(CH2)yOH, wherein y is an integer of M0, such as 1-4. The term "substituted alkoxycarbonyl" means a (substituted alkyl)-fluorene-C(0)- group, wherein the group is bonded to the original structure via a carbonyl functional group, and wherein the substituted group means an alkyl group. One or more (eg, up to 5, for example, up to 3 28 200823188) hydrogen are independently substituted with the substituents selected below: -Ra, -ORb, optionally substituted amine groups (including -NReCORb, -NRcC02Ra) -NRcCONRbRc, -NRbC(NRc)NRbRc, -NRbC(NCN)NRbRc and -NRcS02Ra), halo, cyano, decyl, oxy (substituent as cycloalkyl, heterocycloalkyl and heteroaryl) a substituted thiol group (e.g., -CORb), an optionally substituted alkoxycarbonyl group (e.g., -C〇2Rb), an amine carbonyl group (e.g., -CONRbRc), -〇CORb, -〇〇〇2Ra , -〇CONRbRc, -〇P(0)(ORb)ORe, sulfanyl (e.g., SRb), sulfinyl (e.g., s〇Ra), and sulphate (e.g., -S02Ra and -S02NRbRc), wherein Ra is a selected from the group consisting of a substituted CrC6 alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted aryl group, and optionally a substituted heteroaryl group;

Rb，選自H、視需要經取代之Ci_c6烷基、視需要經取代 之環烷基、視需要經取代之雜環烷基、視需要經取代之芳 基及視需要經取代之雜芳基；及 系獨立地選自氫及視需要經取代之Ci_C4烧基；或 =及R與其相連結之氮形成_視需要經取代之雜環烧基 基團；及 其中各視需要㈣代之基團為未取代或獨立地經一或多 例如―、二或三個獨立地由下列選出之取代基取代： 院基、芳基、雜芳基、芳基<vc4燒基-、雜芳基-Cl_C4 ，基-、㈣^紐基、0Ci_C4絲、.0^4絲苯基、 rC4 烷基-OH、-0CrC4 i 基燒基、_ 基、_〇H、-Nh2、 rC4 烧基顧2、_N(CVC道基)(CVC4 烧基）、·ΝΗ(α4 29 200823188 烷基）、-N(CKC4烷基)(CrC4烷基苯基）、-NH(CrC4烷基 苯基)·、氰基、硝基、氧基(作為環烷基、雜環烷基及雜芳 基之取代基）、_C02H、_C(0)0CrC4 烷基、_CON(CrC4 烷基)(CrC4 烷基）、-CONH(CrC4 烷基）、-CONH2、 -NHC(0)(CrC4 烷基）、_NHC(0)(苯基）、-N(CrC4 垸 基）C(0)(CrC4 烷基）、-N(CrC4 烷基）C(0)(苯基）、 -c(o)crc4 烷基、-c(o)crc4 烷基苯基、-c(o)crc4 鹵基 烷基、_OC(0)CrC4 烷基、-S02(CrC4 烷基）、_so2(苯基）、 -S〇2(CrC4 鹵基烧基）、_s〇2NH2、_S〇2NH(CrC4 烷基）、 _S02NH(苯基）、_NHS02(CrC4 烷基）、_NHS02(苯基）及 -NHS02(CrC4 ifi 基烷基）。 術語「經取代胺基」係指基團，其中 R係選自：羥基、視需要經取代之烧氧基、視需要經取代 之烧基、視需要經取代之環烷基、視需要經取代之醯基、 視需要經取代之甲脒基、胺基羰基、視需要經取代之芳 基、視需要經取代之雜芳基、視需要經取代之雜環烧基、 視舄要經取代之燒氧基幾基、亞石黃酸基及石黃醯基，且其中 R係選自··視需要經取代之烷基、視需要經取代之環烷基、 視需要經取代之芳基、視需要經取代之雜芳基及視需要經 取代之雜環烷基，而其中經取代烷基、環烷基、芳基、雜 環烷基及雜芳基分別係指烷基、環烷基、芳基、雜環烷基 及雜芳基其令一或多個（例如至高5個，例如至高3個）氫原 子經獨立地由下列選出之取代基取代：_Ra、_〇Rb、視需要 經取代之胺基（包括小RcC〇Rb、_NRcc〇2Ra、 30 200823188 -NRcCONRbRc、-NRbC(NR、)NRbRe、-NRbC(NCN)NRbRe及 -NReS〇2Ra)、鹵基、氰基、硝基、氧基(作為環烷基、雜環 烷基及雜芳基之取代基）、視需要經取代之醯基（例如 -CORb)、視需要經取代之烷氧基羰基(例如_c〇2Rb)、胺基 5 羰基(例如 CONRbRc)、_〇CORb、_〇C02Ra、_OCONRbRc、 -0P(0)(0Rb)0Re、硫烷基(例如SR)、亞磺醯基(例如_s〇Ra) 及石黃醯基(例如_S02Ra及-S02NRbRe)， 其中Ra係選自視需要經取代iCl_C6烷基、視需要經取代 之稀基、視需要經取代之炔基、視需要經取代之芳基及視 ίο 需要經取代之雜芳基；Rb, selected from H, optionally substituted Ci_c6 alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl and optionally substituted heteroaryl And are independently selected from hydrogen and optionally substituted Ci_C4 alkyl; or = and R and its associated nitrogen are formed - optionally substituted heterocycloalkyl groups; and each of them is optionally substituted (four) The group is unsubstituted or independently substituted with one or more substituents such as ", two or three independently selected from the following: aryl, aryl, heteroaryl, aryl < vc4 alkyl-, heteroaryl -Cl_C4, ke-, (4)^NZ, 0Ci_C4, .0^4 phenyl, rC4 alkyl-OH, -0CrC4 i group, _ group, _〇H, -Nh2, rC4 , _N (CVC) (CVC4 alkyl), ΝΗ (α4 29 200823188 alkyl), -N (CKC4 alkyl) (CrC4 alkylphenyl), -NH (CrC4 alkylphenyl), cyanide Base, nitro, oxy (substituent as cycloalkyl, heterocycloalkyl and heteroaryl), _C02H, _C(0)0CrC4 alkyl, _CON(CrC4 alkyl)(CrC4 alkyl), -CONH (CrC4 alkyl), -CONH2, -NHC(0) (CrC4 alkane ), _NHC(0)(phenyl), -N(CrC4 fluorenyl)C(0)(CrC4 alkyl), -N(CrC4 alkyl)C(0)(phenyl), -c(o)crc4 Alkyl, -c(o)crc4 alkylphenyl, -c(o)crc4 haloalkyl, _OC(0)CrC4 alkyl, -S02(CrC4 alkyl), _so2(phenyl), -S〇 2 (CrC4 haloalkyl), _s〇2NH2, _S〇2NH (CrC4 alkyl), _S02NH (phenyl), _NHS02 (CrC4 alkyl), _NHS02 (phenyl) and -NHS02 (CrC4 ifi alkyl) . The term "substituted amino group" refers to a group wherein R is selected from the group consisting of: a hydroxyl group, an optionally substituted alkoxy group, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, optionally substituted. Anthracenyl, optionally substituted formazanyl, aminocarbonyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, orthoquinone substituted An alkoxy group, a sulphate group, and a sulphate group, wherein R is selected from the group consisting of an alkyl group which is optionally substituted, a cycloalkyl group which is optionally substituted, an optionally substituted aryl group, if necessary Substituted heteroaryl and optionally substituted heterocycloalkyl, wherein substituted alkyl, cycloalkyl, aryl, heterocycloalkyl and heteroaryl are respectively alkyl, cycloalkyl, aryl a heterocyclic alkyl group and a heteroaryl group such that one or more (e.g., up to 5, for example, up to 3) hydrogen atoms are independently substituted with a substituent selected from the group consisting of: _Ra, _〇Rb, optionally substituted Amino groups (including small RcC〇Rb, _NRcc〇2Ra, 30 200823188 -NRcCONRbRc, -NRbC(NR,)NRbRe, -NRbC(N CN) NRbRe and -NReS〇2Ra), halo, cyano, nitro, oxy (substituent as cycloalkyl, heterocycloalkyl and heteroaryl), optionally substituted thiol (eg - CORb), optionally substituted alkoxycarbonyl (eg _c〇2Rb), amine 5 carbonyl (eg CONRbRc), _〇CORb, _〇C02Ra, _OCONRbRc, -0P(0)(0Rb)0Re, sulfur An alkyl group (e.g., SR), a sulfinyl group (e.g., _s〇Ra), and a sulphate group (e.g., _S02Ra and -S02NRbRe), wherein the Ra is selected from the group consisting of an optionally substituted iCl_C6 alkyl group, optionally substituted. a substituted alkynyl group, an optionally substituted aryl group, and a substituted heteroaryl group as needed;

Rb係選自H、視需要經取代iCl_C6烷基、視需要經取代之 環烧基、視需要經取代之雜環烷基、視需要經取代之芳基 及視需要經取代之雜芳基；及Rb is selected from H, optionally substituted iCl_C6 alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, and optionally substituted heteroaryl; and

Re係獨立地選自氫及視需要經取代之CrC4烷基；或 15 “及與其相連結之氮形成一視需要經取代之雜環烷基 基團；及 其中各視需要經取代之基團為未取代或獨立地經一或多 個，例如一、二或三個獨立地由下列選出之取代基取代： Q-C4烷基、芳基、雜芳基、芳基-CrC4烷基_、雜芳基_Ci_C4 2〇 烧基-、CrC4幽基烷基、_0CkC4烷基、-〇CrC4烷基苯基、 _CrC4 烷基-OH、-〇CrC4 鹵基烷基、鹵基、·〇ϋ、-NH2、 烧基-NH2、-N(CrC4 烷基)(Cl_C4 烷基）、_NH(CrC4 烷基）、 -NA-Q烧基)(CVC4烧基苯基）、_nh(Ci_C4烧基苯基）、 氰基、硝基、氧基(作為環烷基、雜環烷基及雜芳基之取 31 200823188 5 10 15 20 代基）、-CO2H、-C(0)0Ci_C4 烧基、_CON(Ci_C4 烧基XC1-C4 烷基）、-CQNH(CrC4烷基）、_CONH2、-NHC(0)(CrC4烷 基）、-NHC(0)(苯基）、_N(CrC4 烷基)C(0)(CrC4 烷基）、 -N(CrC4 烷基)C(0)(苯基）、-C(0)CrC4 烷基、-C(0)CrC4 烷基苯基、-C(0)CrC4鹵基烷基、_〇c(〇)CrC4烷基、-SOdCi-C4 烧基）、-S〇2(苯基）、-S02(CrC4 ή 基烧基）、 -S02NH2、-S02NH(CrC4 烷基）、-S〇2NH(苯基）、 -NHS02(CrC4 烷基）、_NHS02(苯基)及-NHS02(CrC4 鹵基 烷基）；及 其中視需要經取代之醯基、視需要經取代之烷氧基羰基、 亞磺醯基及磺醯基係如文中所定義。 術语「經取代胺基」亦指各如上所述_NHRd及NRdRd 基團之N -氧化物。N -氧化物可藉由將對應的胺基基團與例 如過氧化氳或間氯過氧苯甲酸作用來製備。熟習本項技術 者熟悉進行此N-氧化作用之反應條件。 式X化合物包括（但不限於）式乂化合物之光學異構 物、外消旋物及其其他的混合物。在此等情況下，單二鏡 像異構物或非對映異構物，亦即光學活性形式，可藉由= 對稱合成或藉由外消旋物之解晰來製得。外消旋物 可例如藉由習㈣方法，如在拆分劑之存在下結晶或使= 例如對掌高壓液相層析(肌c)管柱層析來進行。此外， 式X化合物包括帶有碳-碳雙鍵之厶及£_型 ^ 子，本發明之化學品包括此化合物之所有互變異構形 32 200823188 式0 .本發明化學品包括（但不限於)式x化合物及其所有氰 藥上可接受形式。本文所述之化學品之醫藥上可接受形式 包括醫藥上可接受鹽類、溶劑化物、結晶形式（包括多晶 5 形物及晶籠化合物）、螯合物、非共價複合物、前藥及其 混合物。在特定實施例中，本文所述之化學品為醫藥上可 接受鹽之形式。因此，術語「化學品（chemical entity及 chemical entities)」亦包括醫藥上可接受鹽類、溶劑化物、 螯合物、非共價複合物、前藥及其混合物。 10 「醫藥上可接受鹽類」包括（但不限於）無機酸之鹽 類，例如鹽酸鹽、磷酸鹽、二磷酸鹽、溴酸鹽、硫酸鹽、 亞磺酸鹽、硝酸鹽及其類似物；以及有機之鹽類，例如蘋 果酸鹽、馬來酸鹽、延湖索酸鹽、酒石酸鹽、琥轴酸鹽、 檸檬酸鹽、乳酸鹽、曱磺酸鹽、對甲苯磺酸鹽、2-羥基乙 15 磺酸鹽、苯甲酸鹽、水揚酸鹽、硬脂酸鹽及烷酸鹽例如乙 酸鹽、HOOC-(CH2)n-COOH其中n為〇-4及其類似鹽類。同 樣地，醫藥上可接受陽離子包括（但不限於)鈉、鉀、I弓、 鋁、鋰及銨。 此外，若得到式X化合物為一酸加成鹽，則游離鹼可 20 藉由將酸鹽溶液鹼化來製得。反之，若產物為游離鹼，一 種加成鹽’特別疋醫樂上可接雙加成鹽，可藉由將游離驗 溶於適合的有機溶劑中並將此溶液與酸作用，根據習用的 由驗化合物製備酸加成鹽之製程來產生。熟習本項技術者 應了解各種可用於製備無毒的醫藥上可接受加成鹽之合 33 200823188 成方法。 如上所述，前藥亦在化學·品之範圍内，例如式X化人 物之酯或醯胺衍生物。術語「前藥」包括任何當投予病串 後，例如依前藥之代謝作用會變為式X化合物之化學品。 前藥之實例包括（但不限於)在式X化合物中功能基團（例 如醇或胺基團）之乙酸鹽、甲酸鹽、磷酸鹽和苯甲酸職 類似衍生物。 術語「溶劑化物」係指藉由溶劑與化合物之交化 所形成的化學品。適合的溶劑化物為醫藥上可接A作用 化物，例如水合物，包括單水合物及半水人物又之心劑 術語「螯合物」係指化合物對金屬離子在二點 更多）之配位所形成之化學品。 ”（或 術語「非共價複合物」係指藉由化合物 之交互作用所形成之化學品，其中共僧綠、 似刀子 15 分子間形成。例如，複合作用可經由范德瓦^化合物及 der Waals interaction)、氫鍵及靜電作 / y、斤作用（van 來產生。 ’、稱為離子鍵結） 術語「活性劑」係指具有生物活性之化風 實施例中，「活性劑」為具有醫藥用途之學品。在特定 性劑可為抗癌治療劑。 5物。例如活 「顯著的」係指在標準的統計顯著性^ 例如學生T-試驗其中ρ<0·05，任何統計上，签數試驗中， 改變。 口 _著的可偵測之 術語，文中所述之化學品之 34 治療上有致量 j 係指 20 200823188 有效量，當投予人類或非人類病患時，提供了治療上的利 益例如減缓症狀或預防疾病。 「治療(Treatment或treating)」係指對病患疾病之任何 治療，包括： a) 預防疾病，亦即使疾病臨床症狀不發生； b) 抑制疾病； c) 減緩或阻止臨床症狀之發展；及/或 d) 解除疾病，亦即，使臨床症狀消退。 貓及狗。 「病患」係指雜’例如其已為麵為治療、觀察或 實驗對象之哺⑽物。本文所述之方法可祕人類治療及 獸醫上應用。在某些實_中，病患為哺乳動物；在某些 實施例中’病患為人類；及在某些實施例中，病患係選自 可接受鹽類之化學品 本發明係提供至少-種選自式X化合物及其醫藥上Re is independently selected from the group consisting of hydrogen and optionally substituted CrC4 alkyl; or 15" and the nitrogen to which it is attached forms a heterocycloalkyl group which is optionally substituted; and each of the groups which are optionally substituted Substituted unsubstituted or independently by one or more, for example one, two or three, independently selected from the following substituents: Q-C4 alkyl, aryl, heteroaryl, aryl-CrC4 alkyl _, Heteroaryl_Ci_C4 2 mercapto-, CrC4 decylalkyl, _0CkC4 alkyl, -〇CrC4 alkylphenyl, _CrC4 alkyl-OH, -〇CrC4 haloalkyl, halo, oxime, -NH2, alkyl-NH2, -N(CrC4 alkyl) (Cl_C4 alkyl), _NH(CrC4 alkyl), -NA-Q alkyl (CVC4 alkyl), _nh (Ci_C4 alkylphenyl) ), cyano, nitro, oxy (as cycloalkyl, heterocycloalkyl and heteroaryl) 31 200823188 5 10 15 20 alkenyl), -CO2H, -C(0)0Ci_C4 alkyl, _CON( Ci_C4 alkyl group XC1-C4 alkyl), -CQNH(CrC4 alkyl), _CONH2, -NHC(0)(CrC4 alkyl), -NHC(0)(phenyl), _N(CrC4 alkyl)C(0 )(CrC4 alkyl), -N(CrC4 alkyl)C(0)(phenyl), -C(0)CrC4 alkyl, -C(0)CrC4 alkyl Phenyl, -C(0)CrC4 haloalkyl, 〇〇c(〇)CrC4 alkyl, -SOdCi-C4 alkyl), -S〇2(phenyl), -S02(CrC4 fluorenyl) -S02NH2, -S02NH(CrC4 alkyl), -S〇2NH(phenyl), -NHS02(CrC4 alkyl), _NHS02(phenyl), and -NHS02(CrC4 haloalkyl); Substituted thiol, optionally substituted alkoxycarbonyl, sulfinyl and sulfonyl are as defined herein. The term "substituted amino" also refers to each of the _NHRd and NRdRd groups as described above. N-oxide. The N-oxide can be prepared by reacting the corresponding amine group with, for example, ruthenium peroxide or m-chloroperoxybenzoic acid. Those skilled in the art are familiar with the reaction conditions for carrying out this N-oxidation. Compounds of formula X include, but are not limited to, optical isomers of the formula oxime compounds, racemates, and other mixtures thereof. In such cases, a single dichroic isomer or diastereomer, i.e., an optically active form, can be prepared by = symmetric synthesis or by resolution of the racemate. The racemate can be carried out, for example, by the method of (4), for example, by crystallization in the presence of a resolving agent or by, for example, high pressure liquid chromatography (muscle c) column chromatography. In addition, the compound of formula X includes a hydrazine having a carbon-carbon double bond and a steroid, and the chemical of the present invention includes all tautomeric forms of the compound. 32 200823188 Formula 0. The chemical of the present invention includes (but is not limited to a compound of formula x and all its cyanide acceptable forms. The pharmaceutically acceptable forms of the chemicals described herein include pharmaceutically acceptable salts, solvates, crystalline forms (including polymorphs and caged compounds), chelates, non-covalent complexes, prodrugs And mixtures thereof. In a particular embodiment, the chemical described herein is in the form of a pharmaceutically acceptable salt. Therefore, the term "chemical entities and chemical entities" also includes pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs and mixtures thereof. 10 "Pharmaceutically acceptable salts" include, but are not limited to, mineral acid salts such as hydrochlorides, phosphates, diphosphates, bromates, sulfates, sulfinates, nitrates and the like. And organic salts such as malate, maleate, sulphate, tartrate, succinate, citrate, lactate, sulfonate, p-toluenesulfonate, 2-hydroxyethyl 15 sulfonate, benzoate, salicylate, stearate and alkanoate such as acetate, HOOC-(CH2)n-COOH wherein n is 〇-4 and the like . Likewise, pharmaceutically acceptable cations include, but are not limited to, sodium, potassium, I bow, aluminum, lithium, and ammonium. Further, if the compound of the formula X is obtained as an acid addition salt, the free base can be obtained by basifying the acid salt solution. On the other hand, if the product is a free base, an addition salt can be combined with a double addition salt, which can be dissolved in a suitable organic solvent by a free test and the solution is reacted with an acid. The process for preparing an acid addition salt of a compound is produced. Those skilled in the art will be aware of a variety of methods that can be used to prepare non-toxic pharmaceutically acceptable addition salts. As mentioned above, prodrugs are also within the scope of chemicals, such as esters or guanamine derivatives of formula X. The term "prodrug" includes any chemical that, when administered to a diseased string, such as a compound of formula X, depends on the metabolism of the prodrug. Examples of prodrugs include, but are not limited to, acetate, formate, phosphate and benzoic acid similar derivatives of functional groups (e.g., alcohol or amine groups) in the compound of formula X. The term "solvate" refers to a chemical formed by the crosslinking of a solvent with a compound. Suitable solvates are pharmaceutically acceptable A-acting compounds, such as hydrates, including monohydrates and semi-hydrated formulas. The term "chelate" refers to the coordination of a compound to a metal ion at two points. The chemicals formed. (or the term "non-covalent complex" refers to a chemical formed by the interaction of compounds, in which a total of green, like a knife 15 is formed. For example, the complex action can be via van der Waals compound and der Waals interaction), hydrogen bonding and electrostatic action / y, jin effect (van to produce. ', called ionic bonding) The term "active agent" refers to the biologically active chemical embodiment, the "active agent" has Academic use for medical purposes. The specific agent may be an anticancer therapeutic agent. 5 things. For example, live "significant" refers to the statistical significance of the standard ^ such as the student T-test where ρ < 0·05, in any statistically, the number of trials, changes. Detectable terminology, the chemical described in the article 34 therapeutically effective, refers to 20 200823188 effective amount, when administered to human or non-human patients, provides therapeutic benefits such as mitigation Symptoms or prevent disease. "Treatment or treating" means any treatment of a disease in a patient, including: a) preventing the disease, even if the clinical symptoms of the disease do not occur; b) inhibiting the disease; c) slowing or preventing the development of clinical symptoms; Or d) relieve the disease, that is, cause the clinical symptoms to subside. Cats and dogs. "Patient" means a substance (10) which has been treated as a treatment, observation or subject. The methods described herein are useful for human therapy and veterinary applications. In some embodiments, the patient is a mammal; in some embodiments, the patient is a human; and in certain embodiments, the patient is selected from a chemical that is acceptable for the present invention. - a compound selected from the group X compound and its medicine

式X 其中 而~2係選自N及CR4,其限制條 W1係選自N及CR6， 件為W1及W2兩者不能皆為N ; 卣基、羥基、疊氮基、 R1及R4係獨立地選自氫、氰基、 35 200823188 確基、續醒基、亞續醯基、硫烧基、 基、視需要經取代之醯氧基、視需要經取代:胺 f、視j要經取代之芳基氧基、視需要經取代之ς“ 其羿其、目币Γ 視需要經取代之烧氧 基叛基、視品要經取代之烷基、視需 10 15 之炔基、視需要經取代之芳基氧基、^要Ξ =方基、視需要經取代之雜衫、視需要經取代之雜 壤烧基、視需要經取代之胺基、視需要經取代之醯基、視 需要經取代之胺基縣及視需要經取代之e論min〇d_ ; /係選自氫、視需要經取代之芳基、視需要經取代之 雜方基、視需要餘代之環錄、視需要經取代之雜環烧 基、氛基、視需要經取代之烧基、視需要經取代之酿基、 視需要經取代之烷氧基羰基、視需要經取代之胺基、視需 要經取代之胺基羰基、視需要經取代之曱脒基、視需要經 取代之院氧基、視需要經取代之芳基氧基、視需要經取代 之雜芳基氧基、視需要經取代之雜環烷基氧基、視需要經 取代之烯基、視需要經取代之炔基、磺醯基、亞磺醯基及 硫烷基； Z2係選自氫、視需要經取代之曱脒基、羧基、視需要 經取代之烷氧基羰基、視需要經取代之醯基、視需要經 取代之烯基、視需要經取代之烷基、視需要經取代之雜環 烷基、視需要經取代之雜芳基及視需要經取代之胺基羰 基； Z3係選自氫、_素及視需要經取代之烧基； 36 20 200823188 R3係選自氫及視需要經取代之烧基；及 R6係選自氳、視需要經取代之醯基、視需要經取代 之烷基、氰基、鹵基、疊氮基、視需要經取代之胺基、視 需要經取代之院氧基幾基、視需要經取代之胺基幾基、磺 醯基、亞磺醯基及硫烷基。 在有些式X化合物之實施例中，W1為N，而W2為 CR4。在有些式X化合物之實施例中，wi為cr6而w2 為N 〇 本發明係提供至少一種選自式I化合物及其醫藥上可 接受鹽類之化學品Wherein ~2 is selected from N and CR4, and the restriction strip W1 is selected from N and CR6, and both W1 and W2 are not N; thiol, hydroxyl, azide, R1 and R4 are independent Is selected from the group consisting of hydrogen, cyano, 35 200823188, singular, sulphonyl, thiol, thiol, optionally substituted methoxy, substituted as needed: amine f, visual j to be substituted The aryloxy group, if necessary, is substituted by the oxime group, the alkyl group which is substituted according to the need, the alkyl group to be substituted, the alkynyl group as required, and 10 as needed. Substituted aryloxy group, oxime = square group, optionally substituted shawl, optionally substituted heterologous base, optionally substituted amine group, optionally substituted thiol, visually A substituted amine base and, if necessary, substituted e, min〇d_; / selected from hydrogen, optionally substituted aryl, optionally substituted heteroaryl, optionally recycled a substituted heterocyclic alkyl group, an aryl group, an optionally substituted alkyl group, an optionally substituted aryl group, an optionally substituted alkoxycarbonyl group, optionally taken Amino group, optionally substituted aminocarbonyl group, optionally substituted thiol group, optionally substituted oxy group, optionally substituted aryloxy group, optionally substituted heteroaryloxy group a substituted heterocycloalkyloxy group, optionally substituted alkenyl group, optionally substituted alkynyl group, sulfonyl group, sulfinyl group and sulfanyl group; Z2 is selected from hydrogen, A substituted thiol group, a carboxyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted thiol group, an optionally substituted alkenyl group, an optionally substituted alkyl group, optionally substituted a cycloalkyl group, optionally substituted heteroaryl, and optionally substituted aminocarbonyl; Z3 is selected from the group consisting of hydrogen, _ and optionally substituted alkyl; 36 20 200823188 R3 is selected from hydrogen and optionally Substituted alkyl; and R6 is selected from the group consisting of hydrazine, optionally substituted thiol, optionally substituted alkyl, cyano, halo, azide, optionally substituted amine, optionally Substituting an alkoxy group, an optionally substituted amino group, a sulfonyl group, a sulfinyl group, and In some embodiments of the compound of formula X, W1 is N and W2 is CR4. In some embodiments of the compound of formula X, wi is cr6 and w2 is N 〇 the invention provides at least one selected from Compound I and its pharmaceutically acceptable salts

R及R4係獨立地選自氫、氰基、鹵基、羥基、疊氮 基二硝基、磺醯基、亞磺醯基、硫烷基、視需要經取代之 烷，基、視需要經取代之醯氧基、視需要經取代之胺基羰 基，基、視需要經取代之芳基氧基、視需要經取代之雜芳 基氧基、視需要經取代之雜環烷基氧基、視需要經取代之 烷氧基羰基、視需要經取代之烷基、視需要經取代之烯 $、視需要經取代之炔基、視需要經取代之芳基氧基、視 而要、、二取代之芳基、視需要經取代之雜芳基、視需要經取 37 200823188 雜環烧基、視需要經取代之胺基、視需要經取代之酸基、 視需要經取代之胺基羰基及視需要經取代之 carbaminodoyl ； Z係選自視需要經取代之芳基及視需要經取代之雜 芳基； … 2 / z係選自氳、視需要經取代之甲肺基、羧基、視需要 經取代之烷氧基羰基、視需要經取代之醯基、視需要經 取代之烯基、視需要經取代之烷基、視需要經取代之雜環 10 15 烷基、視需要經取代之雜芳基及視需要經取代之胺基羰 基； Z3係選自氫及視需要經取代之烧基；及 R3係選自氫及視需要經取代之烷基。 在式I化合物之特定實施例中，Z1為視需要經取 芳基。 、、二代之 在式I化合物之特定實施例中，z1為視需要經 Z為視需要經取代之 在式I化合物之特定實施例中 烧基。 在式I化合物之特定實施例中，z3係選自视需要麫 代之芳烷基及視需要經取代之雜芳烷基。 、、二取 本發明係提供至少一種選自式合物及其較雜 接受鹽類之化學品 /、Μ W上可 38 20 200823188R and R4 are independently selected from the group consisting of hydrogen, cyano, halo, hydroxy, azidodinitro, sulfonyl, sulfinyl, sulfanyl, optionally substituted alkane, radical, optionally a substituted methoxy group, an optionally substituted aminocarbonyl group, a substituted aryloxy group, an optionally substituted heteroaryloxy group, an optionally substituted heterocycloalkyloxy group, Optionally substituted alkoxycarbonyl, optionally substituted alkyl, optionally substituted alkene, optionally substituted alkynyl, optionally substituted aryloxy, optionally, and Substituted aryl, optionally substituted heteroaryl, optionally taken 37 200823188 heterocycloalkyl, optionally substituted amine, optionally substituted acid, optionally substituted aminocarbonyl and Carbidodoyl substituted as needed; Z is selected from the optionally substituted aryl and optionally substituted heteroaryl; ... 2 / z is selected from the group consisting of hydrazine, optionally substituted methyl lung, carboxyl, as needed Substituted alkoxycarbonyl, optionally substituted thiol, optionally substituted alkene , optionally substituted alkyl, optionally substituted heterocyclic 10 15 alkyl, optionally substituted heteroaryl, and optionally substituted aminocarbonyl; Z 3 is selected from hydrogen and optionally substituted An alkyl group; and R3 is selected from the group consisting of hydrogen and optionally substituted alkyl. In a particular embodiment of the compound of formula I, Z1 is an aryl group optionally taken. And, in a particular embodiment of the compound of formula I, z1 is optionally substituted in the particular embodiment of the compound of formula I via Z as desired. In a particular embodiment of the compound of formula I, z3 is selected from the group consisting of aralkyl groups as desired and heteroarylalkyl groups optionally substituted. The present invention provides at least one chemical selected from the group consisting of the formula and its more acceptable salts. /, Μ W can be 38 20 200823188

式II 其中 R1及R4係獨立地選自氫、視需要經取代之醯基、視 需要經取代之烧基、氰基、鹵基、豐氮基、視需要經取代 之胺基、視需要經取代之烷氧基羰基、視需要經取代之胺 基幾基、磺醯基、亞續醯基及硫炫基； Z1為視需要經取代之芳基； Z2係選自虱、視需要經取代之曱肺基、叛基、視需要 經取代之燒氧基幾基、視需要經取代之醯基、視需要經取 代之蛾基、視需要經取代之烧基及視需要經取代之胺基幾 基； Z3係選自視需要經取代之芳烷基及視需要經取代之 雜芳嫁基，及 R3係選自氫及視需要經取代之烷基。 在式Π化合物之特定實施例中，Z2係選自羧基、視需 要經取代之烷氧基羰基、視需要經取代之醯基、視需要經 取代之烯基及視需要經取代之烷基。在特定實施例中，Z2 係選自羧基、視需要經取代之哌啶基羰基、視需要經取代 之批咬基縣、視需要娜狀低碳絲、視需要經取代 39 200823188 之低碳烯基及低碳烧氧基幾基。在式Η化合物之特定實施 例中，Ζ2係選自（2-(Ν-乙醯基胺基曱基冰啶小基)羰基；(厶 胺基甲基哌啶-1-基）羰基；1-羥基冬胺基_乙基；孓(（甲基 石黃酿胺基）甲基)哌啶-1-基羰基；2-(曱基胺基羰基）乙烯基； 5 2十比咬基曱基三唑-5-基；胺基曱基；羧基；甲氣 基裁基；吡啶-2-基羰基；吡啶冬基羰基；及吡啶_4-基幾 基。 犬 在式II化合物之特定實施例中，R3係選自氳及視需要 經取代之低碳烧基。在式II化合物之特定實施例中，在式 10 11化合物之特定實施例中，R3係選自氫及低碳烷基。在式 II化合物之特定實施例中，R3係選自氳及甲基。在式 合物之特定實施例中，R3為氫。 在式II化合物之特定實施例中，R4係選自氳、氰基、 鹵基、疊氮基、視需要經取代之胺基羰基及視需要經取代 15 之烷基。在式II化合物之特定實施例中，R4係選自氫、氰 基、氯、溴、氟、疊氮基、視需要經取代之烷基胺基羰基 及視需要經取代之甲基。在式II化合物之特定實施例中， R係選自氫、氰基、氯、溴、疊氮基、吼咬_3_基曱基胺基 羰基、胺基甲基及羥基曱基。在式II化合物之特定實施例 20 中’ R4為氫。 在式II化合物之特定實施例中，z2為-C(0)-NR2R5， 其中R2係選自視需要經取代之烷基及視需要經取代之環 烷基；而R5係選自氫及視需要經取代之烷基。 在式II化合物之特定實施例中，R2係選自視需要經取 200823188 代之曱基、視需要經取代之乙基、視需要經取代之丙 視需要經取代之丁基、視需要經取代之戊基、视需f、 代之己基、視品要經取代之環丙基、視需要經取代之产、 基及視給要經取代之環己基，其中各視需要經取代之^、 5 係視需要經一、二或三個由下列選出之基團取代：视二團 經取代之芳基、視需要經取代之雜芳基、視需要經取二= 雜環烷基、視需要經取代之環烷基、視需要經取代之胺= 羰基、視需要經取代之胺基、羥基、羧基、視需要經 之烷氧基羰基及視需要經取代之烷氧基。 10 在式11化合物之特定實施例中，R2係選自甲基及乙 基’其中甲基及乙基基團係視需要經一或二個由下列選出 之基團取代：視需要經取代之芳基、視需要經取代之雜芳 基、視需要經取代之雜環烷基、視需要經取代之環燒基、 視需要經取代之胺基羰基、視需要經取代之胺基、經基、 15 羧基、視需要經取代之炫氧基幾基及視需要經取代之烧氧 基0 在式II化合物之特定實施例中，R2係選自（1_(2_胺基乙 基)-1Η-σ比ΰ坐-3-基）甲基；（1-(甲基石黃驢基)派u定基）甲基； (1-乙酸基11 底17定-3-基）曱基；（1-乙酸基。比略咬-2-基）甲基； 2〇 (1Η-咪唑-2-基）曱基；（1Η-吡唑-3-基）曱基；甲基_1H4b 嗤-3-基）甲基，（1-曱基比嗤-5-基）甲基；（2-(胺基-幾基) 乙基胺基)羰基曱基；（2-(胺基曱基户比啶-3-基）曱基；（2-(羧 基）乙基胺基)羰基曱基；（2-(二曱基胺基）乙基胺基)羰基甲 基；（2-(羥基）乙基胺基)幾基曱基；（2_(曱基胺基）乙基胺基) 200823188 羰基曱基；〇(Ν·甲基-Ν·(第三丁氧基羰基)_胺基）乙基胺基) 獄基甲基；（2-氧基娘唆-3-基甲基；（3-(二甲基胺基）丙基胺 基)羰基甲基；（3-(羥基）乙基胺基)羰基曱基；（3-(第三丁氧 基羰基胺基）丙基胺基)羰基曱基；（4-(胺基曱基)吼啶_2_基） 曱基；（5-(胺基曱基)吼啶-2_基曱基；（6-((1,3-二氧基異吲 哚啉-2-基）曱基)吼啶-2-基曱基；（6-(2-胺基乙基胺基)吼啶 -2-基）甲基；（6-(3-胺基丙基胺基)吡啶-2-基）甲基；（6-(胺基 甲基)吡啶-2-基）甲基；（6-(羥基曱基）吡啶基）曱基；（6_ 溴吼啶-2-基）曱基；（曱基磺醯胺基)羰基曱基；（η比啶基） 乙基胺基；1-(2-(第三丁氧基羰基胺基）乙基)―沿^比唑各 基甲基；1-(2-(第三丁氧基羰基胺基）乙基)_1H_吡唑基曱 基；1-(胺基羰基)-2·(胺基)_乙_1·基；1_(胺基羰基)各(胺基)_ 丙基；Η胺基羰基)-4_(胺基)-丁基；1_(胺基羰基)冰(苯曱 基氧基羰基胺基)-戊基；1_(胺基羰基)_5_(胺基)_戊基；1兴胺 基羰基）乙-1-基；1-(羧基)-2-(胺基)-乙-1-基；1_(二曱基胺 基幾基)_2_(胺基)_乙-1_基；1_(羥基)_2_(胺基羰基曱基胺基） 乙小基；1-(經基)-2-(乙氧基羰基甲基胺基）乙小基；卜(羥 基)-2十比啶_2_基曱基胺基）乙+基；丨_(曱氧基羰基)_2-(胺 基)-乙-1-基；1-(甲氧基羰基)_2_(第三丁氧基羰基胺基)_乙 -1-基；1-(甲氧基羰基）乙-丨_基；1_(曱基胺基羰基>2_(胺基> 乙-1-基(2 occ) ; 1-(甲基胺基羰基）乙_丨_基；^胺基羰基-2-私基-乙小基；1-曱氧基羰基_2-經基乙小基；2-(2_胺基乙 氧基）乙基；2-(2-胺基乙基)-u比啶_6_基曱基；2-(2-胺基乙基 胺基）乙基；2-(3-氟苯基）乙基；2-(3-甲氧基羰基）乙基； 42 200823188 2-(6-(胺基甲基）吼啶-2-基）乙基；2-(乙醯基胺基）乙基； 2-(胺基）乙基·;2-(胺基羰基)_2-(乙醯基胺基)_乙_丨_基(胺 基幾基)_2_(胺基)-乙小基；2_(胺基幾基）乙基；2_(胺基甲 基)°比咬-5-基曱基；2-(叛基)-2-(胺基)-乙_ι_基；2_(-甲美 胺基）乙基；2-(二曱基胺基羰基)-2-(胺基)-乙-l基；2_(乙1 氧基羰基）乙基；2-(曱氧基羰基)-2-(乙醯基胺基基； 2-（甲氧基羰基)-2-(胺基)-乙_1_基；2-(曱氧基羰基胺基）乙 基’ 2-(甲基胺基）乙基，2-(甲基胺基祿基)-2-(乙酿基胺基)_ 乙-1-基；2-(曱基胺基羰基)-2-(胺基)-乙小基；2_(曱基磺醯 胺基）乙基；2-(甲基氧基羰基)-2-(胺基)-乙-1-基；2-(Ν-(定 三丁氧基羰基)-Ν-(甲基)-胺基）乙基；2-(哌畊-1-基）乙基； 2十比畊-2-基）乙基；2-(吼啶-2-基）乙基；2十比啶-3-基）乙基； 2-(第三丁氧基羰基胺基曱基)吡啶基甲基；2-(第三丁氧 基幾基胺基甲基)。比咬-6-基甲基；2-(三氟曱基)-ϋ比咬-6-基 甲基；2-胺基吡啶-3-基甲基；2-胺基吡啶-5-基甲基；2-氯 11比啶-5-基甲基；2-氰基吡啶-5-基甲基；2-羥基-3-胺基-丙 小基；2-羥基乙基；2-甲氧基乙小基；2-甲氧基吡啶-3_基 甲基；2-甲氧基吡啶-5-基甲基；2-甲基吡啶各基甲基；2-甲基吼啶-5-基甲基；2-甲基吡啶_6_基甲基；3-(2-胺基乙基） 壤已基）甲基；3-(4-甲基哌畊基）丙基；3-(胺基)-3-(甲基 胺基幾基）丙-1-基；3-(胺基羰基）丙基；3-(胺基曱基）苯曱 基；3-(胺基甲基）π比啶_2_基甲基；3_(甲氧基羰基）丙基； 3_(甲基胺基羰基）丙基；3-(三氟甲基)_π比啶-2-基曱基；3,4-一氟苯甲基；3-胺基甲基吡啶基曱基；3_胺基丙基；3- 43 200823188 ;3-甲氧基丙Wherein R 1 and R 4 are independently selected from the group consisting of hydrogen, optionally substituted fluorenyl, optionally substituted alkyl, cyano, halo, azide, optionally substituted amine, optionally a substituted alkoxycarbonyl group, optionally substituted amino group, sulfonyl group, sulfhydryl group and thiodyl group; Z1 is an optionally substituted aryl group; Z2 is selected from hydrazine, optionally substituted A lung-based, rebel-based, optionally substituted alkoxy group, optionally substituted sulfhydryl group, optionally substituted moth group, optionally substituted alkyl group, and optionally substituted amine group a Z3 group selected from the group consisting of an optionally substituted aralkyl group and an optionally substituted heteroaryl group, and the R3 group is selected from the group consisting of hydrogen and optionally substituted alkyl groups. In a particular embodiment of the hydrazine compound, Z2 is selected from the group consisting of a carboxy group, an alkoxycarbonyl group optionally substituted, an optionally substituted thiol group, an optionally substituted alkenyl group, and an optionally substituted alkyl group. In a particular embodiment, Z2 is selected from the group consisting of a carboxy group, a substituted piperidinylcarbonyl group, a substituted bite base as desired, a naphthalene low carbon wire, optionally substituted 39 200823188, a lower olefin. Base and low carbon alkoxy groups. In a particular embodiment of the hydrazine compound, hydrazine 2 is selected from the group consisting of (2-(indolylaminomethylhydrazinyl) carbonyl; (decylaminomethylpiperidin-1-yl)carbonyl; -hydroxybutyryl-ethyl; hydrazine ((methyl sulphate) methyl) piperidin-1-ylcarbonyl; 2-(decylaminocarbonyl)vinyl; 5 2 decyl Triazol-5-yl; amino fluorenyl; carboxy; methyl-based cleavage; pyridin-2-ylcarbonyl; pyridylcarbonyl; and pyridine-4-yl-based. Specific implementation of canine compounds of formula II In one embodiment, R3 is selected from the group consisting of hydrazine and optionally substituted lower carbon alkyl groups. In a particular embodiment of the compound of formula II, in a particular embodiment of the compound of formula 1011, R3 is selected from the group consisting of hydrogen and lower alkyl. In a particular embodiment of the compound of Formula II, R3 is selected from the group consisting of hydrazine and methyl. In a particular embodiment of the Formula, R3 is hydrogen. In a particular embodiment of the compound of Formula II, R4 is selected from the group consisting of hydrazine, a cyano group, a halogen group, an azido group, an optionally substituted aminocarbonyl group, and optionally an alkyl group substituted by 15. In a specific embodiment of the compound of formula II, R4 is selected from the group consisting of hydrogen, cyano, chlorine, and bromine. Fluorine a nitrogen-based, optionally substituted alkylaminocarbonyl group and optionally substituted methyl group. In a particular embodiment of the compound of formula II, R is selected from the group consisting of hydrogen, cyano, chloro, bromo, azide, hydrazine Biting _3_ylmercaptoalkylcarbonyl, aminomethyl and hydroxyindenyl. In a particular embodiment 20 of the compound of formula II, 'R4 is hydrogen. In a particular embodiment of the compound of formula II, z2 is -C( 0) -NR2R5, wherein R2 is selected from optionally substituted alkyl and optionally substituted cycloalkyl; and R5 is selected from hydrogen and optionally substituted alkyl. Specific examples of compounds of formula II Wherein R2 is selected from the group consisting of a thiol group as required by the formula 200823188, an ethyl group which may be substituted as required, a substituted butyl group which is optionally substituted, a pentyl group which is optionally substituted, and an optional f. Substituting the cyclopropyl group, the cyclopropyl group to be substituted, the cyclohexyl group to be substituted as needed, and the cyclohexyl group to be substituted as required, wherein each of the two is required to be replaced by one or two Three are replaced by the following selected groups: the aryl group substituted by the two groups, the heteroaryl group substituted as needed, as needed Taking biscycloalkyl, optionally substituted cycloalkyl, optionally substituted amine = carbonyl, optionally substituted amine, hydroxy, carboxy, optionally alkoxycarbonyl and optionally Substituted alkoxy. In a particular embodiment of the compound of formula 11, R2 is selected from the group consisting of methyl and ethyl' wherein the methyl and ethyl groups are optionally substituted by one or two of the groups selected below. : optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, optionally substituted cycloalkyl, optionally substituted aminocarbonyl, optionally substituted Amino group, transadolyl group, 15 carboxy group, optionally substituted methoxyl group and optionally substituted alkoxy group 0. In a specific embodiment of the compound of formula II, R2 is selected from (1_(2_amine) Benzyl)-1Η-σ ratio ΰ-3-yl)methyl; (1-(methyl sulphate) phenyl) methyl; (1-acetic acid 11 phenyl 17 -3-yl) ) fluorenyl; (1-acetic acid group. Tetidine-2-yl)methyl; 2〇(1Η-imidazol-2-yl)indenyl; (1Η-pyrazol-3-yl)indolyl; methyl_1H4b indol-3-yl)methyl (1-(indolylpyridin-5-yl)methyl; (2-(amino-hexyl)ethylamino)carbonylindenyl; (2-(aminopurinyl)pyridin-3-yl (2-(carboxy)ethylamino)carbonylcarbonyl; (2-(didecylamino)ethylamino)carbonylmethyl; (2-(hydroxy)ethylamino) (2_(nonylamino)ethylamino) 200823188 carbonyl fluorenyl; hydrazine (Ν·methyl-Ν·(t-butoxycarbonyl)-amino)ethylamino) Methyl; (2-oxanthene-3-ylmethyl; (3-(dimethylamino)propylamino)carbonylmethyl; (3-(hydroxy)ethylamino)carbonyl fluorenyl (3-(t-butoxycarbonylamino)propylamino)carbonylcarbonyl; (4-(aminoalkyl)acridin-2-yl) fluorenyl; (5-(amino fluorenyl) Acridine-2_ylindenyl; (6-((1,3-dioxyisoindol-2-yl)indolyl)acridin-2-ylindenyl; (6-(2-amine) (ethylamino) acridine-2-yl)methyl; (6-(3-aminopropylamino)pyridin-2-yl)methyl; (6-(amino) (6-(hydroxyindenyl)pyridyl)indenyl; (6-bromopyridin-2-yl)indenyl; (fluorenylsulfonylamino)carbonylindenyl; (n-pyridyl) ethylamino; 1-(2-(t-butoxycarbonylamino)ethyl)--[i-[3-(t-butoxy) Carbonylamino)ethyl)_1H-pyrazolylfluorenyl; 1-(aminocarbonyl)-2.(amino)-ethyl}yl; 1-(aminocarbonyl) each (amino)-propyl ; amidinocarbonyl)-4-(amino)-butyl; 1-(aminocarbonyl) ice (benzoyloxycarbonylamino)-pentyl; 1-(aminocarbonyl)_5-(amino)-pentyl 1; (amino)carbonyl)ethyl-1-yl; 1-(carboxy)-2-(amino)-eth-1-yl; 1-(didecylamino)-2-(amino)-B -1_yl; 1_(hydroxy)_2_(aminocarbonylcarbonylamino) ethyl small group; 1-(radio)-2-(ethoxycarbonylmethylamino)ethyl small group; -2 decapyridin-2-ylhydrazino)ethylidene; 丨-(decyloxycarbonyl)_2-(amino)-eth-1-yl; 1-(methoxycarbonyl)_2_(第Tributoxycarbonylamino)-ethyl-1-yl; 1-(methoxycarbonyl)ethyl-indole-yl; 1-(decylaminocarbonyl)>2_(amino> ethyl-1-yl ( 2 occ) ; 1-(methylaminocarbonyl)ethyl 丨 丨 基 ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ ^ (2-aminoethyloxy)ethyl; 2-(2-aminoethyl)-u-pyridyl-6-ylindenyl; 2-(2-aminoethylamino)ethyl; 2- (3-fluorophenyl)ethyl; 2-(3-methoxycarbonyl)ethyl; 42 200823188 2-(6-(Aminomethyl)acridin-2-yl)ethyl; 2-(B 2-mercaptoamino)ethyl; 2-(amino)ethyl·; 2-(aminocarbonyl)_2-(ethinylamino)-ethylidene-yl (amino)-2-(amino) )-B-yl; 2-((amino)ethyl; 2-(aminomethyl) ° ratio -5-ylindenyl; 2-(inferior)-2-(amino)-ethyl 2-(2-methylamido)ethyl; 2-(didecylaminocarbonyl)-2-(amino)-ethyl-1-yl; 2-(ethyloxycarbonyl)ethyl; (曱oxycarbonyl)-2-(ethinylamino); 2-(methoxycarbonyl)-2-(amino)-ethyl-1-yl; 2-(decyloxycarbonylamino) '2-(Methylamino)ethyl, 2-(methylaminoethyl)-2-(ethylamino)-ethyl-1-yl; 2-(decylaminocarbonyl)- 2-(Amino)-ethyl small group; 2_(indolylsulfonylamino)ethyl; 2-(methyloxy 2-carbonyl(2-(amino)-amino)-yl; 1-yl)ethyl; 2 decyl-2-yl)ethyl; 2-(acridin-2-yl)ethyl; 2 decapyridin-3-yl)ethyl; 2-(third Oxycarbonylaminoalkylmercapto)pyridylmethyl; 2-(t-butoxymethylaminomethyl). Than 6-ylmethyl; 2-(trifluoromethyl)-indole ratio bit-6-ylmethyl; 2-aminopyridin-3-ylmethyl; 2-aminopyridine-5-yl 2-chloro 11-pyridin-5-ylmethyl; 2-cyanopyridin-5-ylmethyl; 2-hydroxy-3-amino-propanyl; 2-hydroxyethyl; 2-methoxy Ethyl bromide; 2-methoxypyridin-3-ylmethyl; 2-methoxypyridin-5-ylmethyl; 2-methylpyridylmethyl; 2-methylacridine-5- Methyl group; 2-methylpyridine-6-ylmethyl; 3-(2-aminoethyl) hexyl)methyl; 3-(4-methylpipedyl)propyl; 3-( Amino)-3-(methylaminomethyl)propan-1-yl; 3-(aminocarbonyl)propyl; 3-(aminoindenyl)phenylhydrazine; 3-(aminomethyl)比Biidine-2-ylmethyl; 3-(methoxycarbonyl)propyl; 3-(methylaminocarbonyl)propyl; 3-(trifluoromethyl)-π-pyridin-2-ylindenyl; , 4-fluorofluoromethyl; 3-aminomethylpyridinyl sulfhydryl; 3-aminopropyl; 3-43 200823188; 3-methoxypropane

胺甲醯基環戊基；3-羧基丙基；3_羥基丙基,· 基；4_(胺基甲基比啶_2_基甲基；t(N此二 啶-3-基甲基；4-(第三丁氧基羰基胺基)_嗎 苯甲基；4_甲基胺基吼咬各基甲基；4_甲基苯甲基；4_嗎 啉基吡啶-3-基甲基；4_哌畊基吡啶-3_基甲基；5_((雙（二甲 基胺基）甲基胺基）甲基)π比啶_3_基甲基；5_(胺基甲基户比啶 -2-基甲基；5-(胺基甲基）,比啶_3_基甲基；5_(羥基曱基）吼 唆-3-基甲基；5-(第三丁氧基羰基胺基甲基)·吡啶基曱 基；5-(三氟甲基)_吡啶-2_基曱基；5_胺基戊基；5_胺基吼 唆-2-基曱基；6-((雙(二曱基胺基)伸曱基胺基）甲基}ϋ比啶_2_ 基）曱基；6-(4-乙醯基哌畊_；!_基）吡啶_3_基甲基）；6_(胺基 甲基比鳴>2-基）甲基；卜胺基己基；胺基羰基曱基；苯曱 基；環丙基甲基；二曱基胺基羰基曱基；異丙基；異噚唑 -5-基甲基；曱氧基羰基甲基；甲基；曱基胺基羰基甲基； 畤唑-2-基曱基；哌啶_4-基曱基；丙_2_烯基；吡畊-2-基 曱基；吼啶-2-基甲基；吡啶_2_基曱基-N_氧化物；也H 基曱基；σ比啶各基甲基_N_氧化物；吡啶-4-基曱基；嘆吩 -2-基曱基；及噻吩、3_基甲基。 2〇 在式II化合物之特定實施例中，Z3係選自-(CH2)rR ’ 其中r係選自1、2及3，而以2〇係選自視需要經取代之芳基及 視需要經取代之雜芳基。 在式II化合物之特定實施例中，z3係選自2-(3-甲基苯 基）乙基、2-(1Η-咪唑_4_基）乙基、2_(1_曱基-1H-咪唑基） 44 200823188 乙基、2-(2,3-二氟苯基）乙基、2-(2,5-二氟苯基）乙基、2-(2,6_ . 二氟苯基）乙基、2-(2-氯苯基）乙基、2-(2-氰基苯基）乙基、 • 2-(2-氟苯基）乙基、2-(2-羥基苯基）乙基、2-(2-甲氧基苯基） . 乙基、2-(2-甲基苯基）乙基、2-(3-(三氟甲基）苯基）乙基、 5 2-(3,4-二氟苯基）乙基、2-(3,5-二氟苯基)乙基、2-(3,5-二甲 基-1H-吡唑-1_基）乙基、2-(3,5-二甲基-1H-吡唑_4_基）乙 基、2-(3-胺甲醯基苯基）乙基、2-(3-羧基苯基）乙基、2-(3-氣基苯基）乙基、2-(3-氣苯基)_2-(輕基)-乙基、2-(3 -氣苯基） 乙基、2-(3-^ntb^-2-基）乙基、2-(3-甲氧基綠基苯基）乙 10 基、2-(3-甲氧基苯基）乙基、2-(3-曱基苯基）乙基、2-(4-胺 基苯基）乙基、2-(4-氯苯基）乙基、2-(4-氟苯基）乙基、2-(4-羥基苯基）乙基、2-(苯并[d][l，3]二氧環戊烯-5-基）乙基、 2-(咬喃-2-基）乙基、2-(經基)-2-(苯基）乙基、2-(苯基）乙 基、2-(11比0定-2-基）乙基、2-(^比0定-3-基）乙基、2-(1¾•吩-2-15 基）乙基、2-苯基丙-1-基、3-(1Η-咪唑-1-基）丙-1-基、3-苯 基丙基、苯甲基、。比σ定-2-基甲基、吼ϋ定-3-基曱基及嗟吩 -3-基曱基。 在式II化合物之特定實施例中，Ζ3為2-(吡啶-2-基）乙 基。 20 在式II化合物之特定實施例中，Ζ1係選自視需要經一 或二個由下列選出之基團取代之芳基：氰基、_基、羥基、 曱醯基、視需要經取代之烷基、視需要經取代之烯基、視 需要經取代之烷氧基、羧基、視需要經取代之烷氧基羰 基、視需要經取代之醯基、視需要經取代之胺基羰基、視 45 200823188 需要經取代之胺基、視需要經取代之雜環烷基、視需要經 之#务基、視需要經取代之甲脉基及視需要經取代之 石二^基。在式π化合物之特定實施例中，z1係選自視需要 ^ 或二個由下列選出之基團取代之苯基：氰基、i基、 $基、甲酿基、視需要經取代之低碳烷基、低碳烯基、低 石反燒氧基、羧基、視需要經取代之低碳烷氧基羰基、低碳 醉其 一 -皿土、二烷基胺基、乙醯基胺基、視需要經氰基、芳烷基 和雜芳燒基取代之甲脒基以及胺基羰基。在式II化合物之 特定實施例中，Z1係選自苯基、2-胺基羰基苯基、2-氟苯 基、氯苯基、2-羥基苯基、2-曱基苯基、2-甲氧基苯基、 2_氛基苯基、2_氰基曱基苯基、2-乙烯基苯基、2-甲醯基苯 基、3,4-二氟苯基、3_曱基苯基、3_氯苯基、3_氟苯基、3_ 氛基苯基、3-二甲基胺基苯基、3-曱氧基苯基、3-甲氧基 甲基苯基、3-羥基苯基、3-三氟曱基苯基、4-胺基羰基苯 基、4_氟苯基、4-氯苯基、4-甲基苯基、4-羥基苯基、4-氰基笨基、4-曱氧基苯基、4-經基甲基苯基、4-三氟甲基 笨基、4-曱氧基羰基苯基、4-二曱基胺基苯基、4-乙醯基 苯基、4-羧基苯基、4-乙基苯基、4-乙醯基胺基苯基、3,4-二氯苯基、3,4-二氟苯基、2,3-二曱基苯基、2,5-二甲基苯 基、2,4-二曱基苯基、3,5-二曱基苯基、3,4-二曱基苯基、 2-氯_4_氟-苯基、2-氰基-4-氟-苯基、2-氯-6-氟-苯基、2_氯 •4-曱氧基·本基、2-氣基-4-甲氧基-苯基、2-氰基-6-氟·苯 基、2-氯-5-氟-苯基、2-氰基-5-氟-苯基、2-氣-4-甲基苯基、 2-氯-4-經基曱基-苯基、2-(Ν-(σ比咬-3-基甲基）曱脒基)笨基 46 200823188 及2-氰基_4_曱基苯基。Aminomethylmethylcyclopentyl; 3-carboxypropyl; 3-hydroxypropyl, ·yl; 4-(aminomethylpyridin-2-ylmethyl; t(N-dipyridin-3-ylmethyl) ; 4-(t-butoxycarbonylamino)-benzylidene; 4-methylamino group, each methyl group; 4-methylbenzyl; 4-morpholinylpyridin-3-yl Methyl; 4_piperidinylpyridine-3-ylmethyl; 5-((bis(dimethylamino)methylamino)methyl)π-pyridyl-3-ylmethyl; 5-(aminomethyl) Alkylpyridin-2-ylmethyl; 5-(aminomethyl), pyridyl-3-ylmethyl; 5-(hydroxyindenyl)indol-3-ylmethyl; 5-(third Oxycarbonylaminomethyl)pyridylfluorenyl; 5-(trifluoromethyl)-pyridin-2-ylindenyl; 5-aminopentyl; 5-aminoindole-2-ylindenyl ;6-((bis(didecylamino))alkylamino)methyl}pyridinium-2-yl) fluorenyl; 6-(4-ethylhydrazine-based; 3_ylmethyl); 6-(aminomethylpyrazine>2-yl)methyl;aminohexyl;aminocarbonylcarbonyl;phenylhydrazine;cyclopropylmethyl; dimercaptoamine Carbonyl fluorenyl; isopropyl; isoxazol-5-ylmethyl; decyloxycarbonylmethyl; methyl; decylaminocarbonyl ; oxazol-2-ylindenyl; piperidinyl-4-ylindenyl; propen-2-alkenyl; pyridin-2-ylindenyl; acridin-2-ylmethyl; pyridine_2-yl Mercapto-N-oxide; also H-based fluorenyl; σ-pyridylmethyl-N-oxide; pyridin-4-ylindenyl; ephen-2-ylindenyl; and thiophene, 3-phenyl Methyl. In a particular embodiment of the compound of formula II, Z3 is selected from the group consisting of -(CH2)rR' wherein r is selected from 1, 2 and 3, and 2 is selected from aryl as desired. And optionally substituted heteroaryl. In a particular embodiment of the compound of formula II, z3 is selected from the group consisting of 2-(3-methylphenyl)ethyl, 2-(1Η-imidazolium-4-yl)ethyl , 2_(1_Mercapto-1H-imidazolyl) 44 200823188 Ethyl, 2-(2,3-difluorophenyl)ethyl, 2-(2,5-difluorophenyl)ethyl, 2- (2,6_. Difluorophenyl)ethyl, 2-(2-chlorophenyl)ethyl, 2-(2-cyanophenyl)ethyl, • 2-(2-fluorophenyl)ethyl , 2-(2-hydroxyphenyl)ethyl, 2-(2-methoxyphenyl). Ethyl, 2-(2-methylphenyl)ethyl, 2-(3-(trifluoromethyl) Phenyl)ethyl, 5 2-(3,4-difluorophenyl)ethyl, 2-(3,5-difluorophenyl)ethyl, 2-(3,5-dimethyl -1H-pyrazole-1_yl)ethyl, 2-(3,5-dimethyl-1H-pyrazol-4-yl)ethyl, 2-(3-aminoformamidophenyl)ethyl , 2-(3-carboxyphenyl)ethyl, 2-(3-carbophenyl)ethyl, 2-(3-phenylphenyl)_2-(light-based)-ethyl, 2-(3- Ether phenyl) ethyl, 2-(3-^ntb^-2-yl)ethyl, 2-(3-methoxychlorophenyl)ethyl 10, 2-(3-methoxyphenyl Ethyl, 2-(3-indolylphenyl)ethyl, 2-(4-aminophenyl)ethyl, 2-(4-chlorophenyl)ethyl, 2-(4-fluorophenyl Ethyl, 2-(4-hydroxyphenyl)ethyl, 2-(benzo[d][l,3]dioxol-5-yl)ethyl, 2-(biting-2- Ethyl, 2-(trans)-2-(phenyl)ethyl, 2-(phenyl)ethyl, 2-(11-0-but-2-yl)ethyl, 2-(^ ratio 0--3-yl)ethyl, 2-(13⁄4•phen-2-yl)ethyl, 2-phenylprop-1-yl, 3-(1Η-imidazol-1-yl)propan-1- Base, 3-phenylpropyl, benzyl,. The ratio is σ-2-ylmethyl, hydrazin-3-ylindenyl and porphin-3-ylindenyl. In a particular embodiment of the compound of formula II, hydrazine 3 is 2-(pyridin-2-yl)ethyl. In a particular embodiment of the compound of formula II, hydrazine 1 is selected from aryl groups which are optionally substituted with one or two groups selected from the group consisting of cyano, cyano, hydroxy, decyl, optionally substituted. Alkyl, optionally substituted alkenyl, optionally substituted alkoxy, carboxy, optionally substituted alkoxycarbonyl, optionally substituted fluorenyl, optionally substituted aminocarbonyl, optionally 45 200823188 Requires substituted amino groups, optionally substituted heterocycloalkyl groups, optionally as desired, substituted aspirinyl groups, and optionally substituted stone groups. In a particular embodiment of the compound of formula π, z1 is selected from phenyl as desired or two substituted groups selected from the group consisting of cyano, i-, phenyl, aryl, and optionally substituted. Carboalkyl, lower alkenyl, low-stone anti-alcohol, carboxyl, optionally substituted lower alkoxycarbonyl, low-carbon drunk-dipod, dialkylamino, ethenyl A mercapto group and an aminocarbonyl group substituted with a cyano group, an aralkyl group and a heteroaryl group, as needed. In a particular embodiment of the compound of Formula II, Z1 is selected from the group consisting of phenyl, 2-aminocarbonylphenyl, 2-fluorophenyl, chlorophenyl, 2-hydroxyphenyl, 2-nonylphenyl, 2- Methoxyphenyl, 2-aminophenyl, 2-cyanononylphenyl, 2-vinylphenyl, 2-methylindenylphenyl, 3,4-difluorophenyl, 3-hydrazino Phenyl, 3-chlorophenyl, 3-fluorophenyl, 3-aminophenyl, 3-dimethylaminophenyl, 3-methoxyphenyl, 3-methoxymethylphenyl, 3 -hydroxyphenyl, 3-trifluorodecylphenyl, 4-aminocarbonylphenyl, 4-fluorophenyl, 4-chlorophenyl, 4-methylphenyl, 4-hydroxyphenyl, 4-cyano Base, 4-methoxyphenyl, 4-carbylmethylphenyl, 4-trifluoromethylphenyl, 4-nonyloxycarbonylphenyl, 4-didecylaminophenyl, 4 - Ethylphenyl, 4-carboxyphenyl, 4-ethylphenyl, 4-ethylguanidinophenyl, 3,4-dichlorophenyl, 3,4-difluorophenyl, 2, 3-didecylphenyl, 2,5-dimethylphenyl, 2,4-didecylphenyl, 3,5-didecylphenyl, 3,4-didecylphenyl, 2- Chlorine_4_fluoro-phenyl, 2-cyano-4-fluoro-phenyl, 2-chloro-6-fluoro-phenyl, 2-chloro-4-indolyloxy-based, 2-gas 4-methoxy-phenyl, 2-cyano-6-fluoro-phenyl, 2-chloro-5-fluoro-phenyl, 2-cyano-5-fluoro-phenyl, 2-gas-4 -methylphenyl, 2-chloro-4-transmethylindenyl-phenyl, 2-(anthracene-(σ-Bit-3-ylmethyl)indolyl), stylyl 46 200823188 and 2-cyano 4_decylphenyl.

選自氮及甲基。在式Π化合物之特定實施例中，r1為氣 本發明係提供至少一 可接受鹽類之化學品 R係選自氫及視需要 之特定實施例中，R1係 種述自式III化合物及其醫藥Selected from nitrogen and methyl. In a particular embodiment of the hydrazine compound, r1 is a gas. The present invention provides at least one acceptable salt. The chemical R is selected from the group consisting of hydrogen and, if desired, a particular embodiment, and the R1 species is derived from a compound of formula III and medicine

式III R1及R4係獨立地選自氫、視需要經取代之醯基、視 需要經取代之院基、氰基、鹵基、疊氮基、視需要經取代 之胺基、視需要經取代之烷氧基羰基、視需要經取代之胺 基幾基、磺醯基、亞磺醯基及硫烷基； Z1為視需要經取代之雜芳基； Z2係選自氫、視需要經取代之甲脒基、羧基、視需要 經取代之烷氧基羰基、視需要經取代之醯基、視需要經取 代之烯基、視需要經取代之烷基及視需要經取代之胺基羰 基； 47 200823188 z3係選自視需要經取代之芳烷基及視需要經取代之 . 雜芳烷基；及· • R3係選自氫及視需要經取代之烷基。 . 在式III化合物之特定實施例中，Z1係選自視需要經 5 一或二個由下列選出之基團取代之雜芳基：氰基、鹵基、 羥基、曱醯基、視需要經取代之烷基、視需要經取代之烯 基、視需要經取代之烷氧基、羧基、視需要經取代之烧氧 基羰基、視需要經取代之醯基、視需要經取代之胺基羰 基、視需要經取代之雜環烷基、視需要經取代之雜芳基、 10 視需要經取代之甲脒基及視需要經取代之磺醯基。 在式III化合物之特定實施例中，Z1係選自1H-吡唑-3-基；1H-吡唑-4-基；1H-三唑-5-基；1-曱基-1H-吡唑-4-基； 1-甲基-1H-吡唑-5-基；2-(羥基曱基）噻吩-3-基；2,2’-二吡 啶；2,3’-二吡啶；2,4’-二吡啶；2-氰基噻吩-3-基；2-曱醯 15 基噻吩-3-基；3-(羥基曱基)噻吩-2-基；3-氰基-1-曱基-1H- 吡唑-4-基；3-甲醯基噻吩-2-基；4-氰基噻吩-3-基；4-曱基 噻吩-2-基；4-曱基噻吩-3-基；5-(1-羥基乙基)噻吩-2-基； 5-(胺基曱基)噻吩-2-基；5-(羥基曱基)噻吩-2-基；5-(羥基 甲基）噻吩-3-基；5-乙醯基噻吩-2-基；5-氰基-1H-吡唑-4-20 基；5-氰基-1-曱基-1H-吡唑-4-基；5-氰基噻吩-2-基；5-曱 醯基噻吩-2-基；5-曱醯基噻吩-3-基；3-(胺基曱基)噻吩-2-基；異nf唑-4-基；噻唑-2-基；噻吩-2-基；及噻吩-3-基。 在式III化合物之特定實施例中，Z2係選自羧基、視需 要經取代之烷氧基羰基、視需要經取代之醯基、視需要經 48 200823188 取代之烯基及視需要經取代之烧基。 在式III化合物之特定實施例中，z2係選自羧基、視需 要經取代之派咬基羰基、視需要經取代之吡啶基羰基、視 需要經取代之低碳烷基、視需要經取代之低碳烯基及低碳 烧氧基幾基。 在式111化合物之特定實施例中，Z2係選自2-(曱基胺 基）-2-氧乙基、2-胺基-2-氧乙基、3·胺基-3-氧丙基、 (2-(N-乙酸基胺基曱基)旅啶小基)魏基；（2_胺基曱基哌啶 -1-基)幾基；1-經基_2_胺基-乙基；2_《甲基磺醯胺基）甲基) 哌啶-1-基羰基；2-(甲基胺基羰基）乙烯基；2_(吡啶基曱 基)-2Η-四吐-5-基；胺基甲基；羧基；曱氧基羰基；吡啶 -2-基羰基；吡啶-3-基羰基；及吡啶-4_基羰基。 在式III化合物之特定實施例中，R3係選自氫及視需要 經取代之低碳烧基。在式ΙΠ化合物之特定實施例中，R3 係選自氳及低碳烷基。在式m化合物之特定實施例中， R係選自氫及甲基。在式in化合物之特定實施例中，r3 為氳。 在式III化合物之特定實施例中，R4係選自氫、氰基、 鹵基、疊氮基、視需要經取代之胺基羰基及視需要經取代 之炫基。在式III化合物之特定實施例中，R4係選自氫、氰 基、氯、溴、氟、疊氮基、視需要經取代之烷基胺基羰基 及視需要經取代之甲基。在式ΠΙ化合物之特定實施例中， R4係選自氫、氰基、氯、溴、疊氮基、π比啶-3-基曱基胺 基羰基、胺基曱基及羥基甲基。在式m化合物之特定實施 49 200823188 例中，R4為氫。 -在式111化合物之特.定實施例中，Z2為-C(0)NR2R5，其 中R2係選自視需要經取代之烷基及視需要經取代之環烷 基；而R5係選自氫及視需要經取代之烷基。 在式III化合物之特定實施例中，R2係選自視需要經取 代之甲基、視需要經取代之乙基、視需要經取代之丙基、 視需要經取代之丁基、視需要經取代之戊基、視需要經取 代之己基、視需要經取代之環丙基、視需要經取代之環戊 基及視需要經取代之環己基，其中各視需要經取代之基團 係視需要經一、二或三個由下列選出之基團取代：視需要 經取代之方基、視需要經取代之雜芳基、視需要經取代之 雜環烧基、視需要經取代之環烧基、視需要經取代之胺基 羰基、視需要經取代之胺基、羥基、羧基、視需要經取代 之烧氧基幾基及視需要經取代之烧氧基。 在式III化合物之特定實施例中，R2係選自甲基及乙 基，其中曱基和乙基基團係視需要經一或二個由下列選 出之基團取代：視需要經取代之芳基、視需要經取代之 雜芳基、視需要經取代之雜環烷基、視需要經取代之環 烷基、視需要經取代之胺基羰基、視需要經取代之胺基、 羥基、羧基、視需要經取代之烷氧基羰基及視需要經取 代之烷氧基。 在式III化合物之特定實施例中，R2係選自（1气2_胺基 乙基坐基）曱基；（1-(甲基石黃酿基)旅0定冬基）甲 基，（1-乙酿基娘咬-3-基）甲基；（1_乙酿基吼略唆_2_基）甲 50 200823188 基；(1H-咪唑-2_基）曱基；(1H-吼唑_3_基）甲基；(1•甲基 他唑_3_基）甲基；（1-甲基-1H-吡唑_5_基)甲基；胺基幾 • 基）乙基胺基）羰基甲基；（2-(胺基甲基)吡啶_3_基）甲基； (2-(羧基）乙基胺基)羰基曱基；（2-(二甲基胺基）乙基胺基) 5 羰基甲基；(2-(羥基）乙基胺基)羰基甲基；（2-(甲基胺基) 乙基胺基)羰基曱基；（2-(N-曱基(第三丁氧基幾基)_胺 基）乙基胺基)羰基甲基；（2-氧哌啶-3-基）甲基；（3_(二甲基 胺基）丙基胺基)裁基甲基；（3-(經基）乙基胺基)幾基甲基； (3-(弟二丁乳基叛基胺基）丙基胺基)幾基甲基；（4_(胺基甲 1〇 基）11比淀-2-基）曱基；（5-(胺基甲基）u比唆_2_基）甲基； • (6-((153- ^一氧基異°引。朵淋-2-基）甲基）吼咬_2_基）甲基· ^ (6-(2-胺基乙基胺基)吼啶-2-基）曱基；(6-(3-胺基丙基胺基） σ比咬-2-基）曱基；（6-(胺基甲基户比咬-2-基）曱基；（心(經基 曱基）吼啶_2_基）甲基；（6_溴吡啶1基）甲基；（甲基續醯二 15 基)#厌基曱基，（σ比σ定_2-基）乙基胺基；1-(2-(第三丁氣基幾 基胺基）乙基)_1Η_吼唑-3-基甲基；1-(2-(第三丁氧基幾基 胺基）乙基)_1H_吡唑-5-基曱基；1-(胺基羰基)-2_(胺基)_乙 -1-基；1-(胺基羰基)-3-(胺基)·丙基；1-(胺基羰基)_4_(胺 基)-丁基；1-(胺基羰基)-4-(苯曱基氧基羰基胺基戊基； 20 i-(胺基#厌基)-5-(胺基)-戊基；ι_(胺基幾基）乙小基；ι_(幾 基)-2-(胺基)-乙-1_基；1-(二曱基胺基羰基⑽基乙小 基；1_(羥基）-2-(胺基羰基甲基胺基）乙小基；1_(經 基)-2-(乙氧基幾基甲基胺基）乙小基；(經基)_2十比咬_2_ 基甲基胺基）乙-1-基；1_(曱氧基羰基>2-(胺基)-乙4_基； 51 200823188 1- (曱氧基羰基)-2-(第三丁氧基羰基胺基)-乙-1_基；1-(甲 . 氧基羰基）乙-1-基；1-(甲基胺基羰基)-2-(胺基)-乙-1-基(2 • occ)，1-(曱基胺基綠基）乙-1 -基，1 -胺基綠基-2-輕基"乙-1 _ 基，1-甲乳基綠基-2-經基-乙-1-基，2·(2-胺基eth乳基）乙 5 基，2-(2-胺基乙基)-ϋ比咬-6-基甲基，2-(2-胺基乙基胺基） 乙基；2-(3-氟苯基）乙基；2-(3-曱氧基羰基）乙基；2_(6-(胺 基曱基）ϋ比咬-2-基）乙基，2-(乙酿基胺基）乙基，2-(胺基） 乙基，2-(胺基祿基)-2-(乙酿基胺基)-乙-1-基，2-(胺基緣 基)-2-(胺基)-乙-1-基，2-(胺基搂基）乙基，2-(胺基曱基） 10 吼σ定-5-基曱基，2-(竣基-2-(胺基)-乙-1 -基，2-(二曱基胺基） , 乙基，2-(二甲基胺基綠基)-2-(胺基)-乙-1 -基，2-(乙氧基 羰基）乙基；2-(甲氧基羰基)-2-(乙醯基胺基)-乙-1-基；2-(曱 氧基幾基)-2-(胺基)-乙-1-基，2-(曱氧基綠基胺基）乙基； 2- (曱基胺基）乙基；2-(甲基胺基羰基)-2-(乙醯基胺基)-乙 15 -1 -基，2-(曱基胺基綠基)-2-(胺基)-乙-1 -基，2-(曱基石黃酉龜 胺基）乙基，2-(曱乳基綠基)-2-(胺基)-乙-1-基，2-(N-(弟二 丁氧基被基)-N-(曱基)-胺基）乙基，2-(旅0井-1-基）乙基， 2-(吼畊-2-基）乙基；2-(吼啶-2-基）乙基；2-(啦啶-3-基）乙 基；2-(第三丁氧基羰基胺基甲基)吼啶-3-基曱基；2-(第三 20 丁氧基羰基胺基曱基)吼啶-6-基曱基；2-(三氟曱基)-吼啶 -6-基曱基，2-胺基°比咬-3-基曱基，2-胺基0比咬-5-基甲基， 2-氯吼啶-5-基曱基；2-氰基吼啶-5-基曱基；2-羥基-3-胺基 -丙-1 -基，2-經基乙基，2-甲氧基乙-1 -基，2-甲氧基°比。定-3_ 基曱基；2-曱氧基吼啶-5-基曱基；2-曱基吼啶-3-基曱基； 52 200823188 2-曱基吡啶-5-基曱基；2-甲基吡啶_6_基曱基；3_(2_胺基乙 基)環己基）甲基；3-(4-甲基旅，井基)丙基；3_(胺基仏（甲 • 基胺基羰基）丙基；3-(胺基羰基）丙基；3-(胺基甲基)苯 、 曱基，3·(胺基曱基户比咬_2_基曱基；3_(曱氧基羰基）丙基； 5 甲基月女基罗厌基）丙基，3-(三氧曱基)_π比咬-2-基甲基；3 4_ 一氟本曱基，3-胺基曱基π比唆-4-基甲基；3-胺基丙基；3_ 胺甲酿基環戊基；3-叛基丙基；3-經基丙基；3-曱氧基丙 基；4_(胺基甲基)』比咬-2-基曱基；4-(Ν，Ν-二曱基胺基)吡 唆-3-基曱基；4-(第三丁氧基羰基胺基)_嗎琳基甲基；4_ 1〇 胺基丁基；4-胺基曱基^1比咬-3-基曱基；4-氰基苯甲基；4- • 氟苯曱基；4-甲基胺基吼唆-3-基甲基；4-甲基苯曱基；4-嗎啉基吡啶-3-基甲基；4-哌畊基吡啶-3-基曱基；5-((雙（二 甲基胺基）曱基胺基）甲基户比啶-3-基曱基；5-(胺基曱基)u比 ϋ定-2-基曱基；5-(胺基曱基)吼咬-3-基甲基；5-(羥基曱基） 15 吼啶-3-基曱基；5-(第三丁氧基羰基胺基曱基)-π比啶_2一基 曱基；5-(三氟甲基)-吼啶-2-基曱基；5-胺基戊基；5-胺基 吼啶-2-基甲基；6-((雙(二甲基胺基)伸甲基胺基）甲基)π比啶 -2-基）甲基，6-(4-乙酿基旅呼-1-基)ϋ比σ定-3-基甲基），6-(胺 基曱基户比啶-2-基曱基；6-胺基己基；胺基羰基曱基；苯 20 甲基；環丙基曱基；二曱基胺基羰基甲基；異丙基；異噚 唑-5-基曱基；甲氧基羰基曱基；甲基；甲基胺基羰基曱 基；υ亏唾_2_基甲基；娘。定-4-基曱基，丙-2-細-1-基，吼^井-2-基曱基；吡啶-2-基甲基；吡啶-2-基曱基-Ν-氧化物；吡啶 -3-基曱基；吡啶-3-基曱基-Ν-氧化物；吡啶-4-基曱基；噻 53 200823188 吩-2-基甲基，及ϋ塞吩-3-基曱基。 在式JII化合物之特定實施例中，Ζ3係選自 • -(CH2)rR20，其中r係選自1、2及3，而R20係選自視需要經 、 取代之芳基及視需要經取代之雜芳基。 5 在式III化合物之特定實施例中，Z3係選自2-(3-曱基苯 基）乙基、2-(1Η-咪唑-4-基）乙基、2-(1-曱基-1H-咪唑-4-基) 乙基、2-(2,3-二氟苯基）乙基、2-(2,5-二氟苯基）乙基、2-(2,6-二氟苯基）乙基、2-(2-氯苯基）乙基、2-(2-氰基苯基）乙基、 2-(2-氟苯基）乙基、2-(2-羥基苯基）乙基、2-(2-曱氧基苯基) 1〇 乙基、2-(2-曱基苯基）乙基、2-(3-(三氟曱基）苯基）乙基、 . 2-(3,4-二氟苯基）乙基、2-(3,5-二氟苯基）乙基、2-(3,5•二甲 基-1H-吼唑-1-基）乙基、2-(3,5-二甲基-1H-吡唑-4-基）乙 基、2-(3-胺曱醯基苯基）乙基、2-(3-羧基苯基）乙基、2-(3-氣基苯基）乙基、2-(3 -氣苯基)-2-(輕基)-乙基、2_(3_氣苯基) 15 乙基、2-(3-氣^比咬-2-基）乙基、2-(3-甲乳基祿基苯基）乙 基、2-(3-曱氧基苯基）乙基、2-(3-甲基苯基）乙基、2-(4-胺 基苯基）乙基、2-(4-氯苯基）乙基、2-(4-氟苯基）乙基、2-(4-羥基苯基）乙基、2-(苯并[d][l，3]二氧環戊烯-5-基）乙基、 2-(呋喃2-基）乙基、2-(羥基)-2-(苯基）乙基、2-(苯基）乙基、 2〇 2-(°比ϋ定-2-基）乙基、2-(°比ϋ定-3-基）乙基、2-(σ塞吩-2-基）乙 基、2-苯基丙-1-基、3-(1Η-咪唑-1-基）丙-1-基、3-苯基丙 基、苯甲基、吡啶_2_基曱基、吡啶-3-基曱基及噻吩-3-基 曱基。 在式III化合物之特定實施例中，Ζ3係選自3-氟苯乙 54 200823188 基、3,5-二氰苯乙基及2十比啶-2-基）乙基。在式m化合 物之特定實施例中，Ζ3為2-(吡啶-2-基）乙基。 在式III化合物之特定實施例中，Ri係選自氫及視需要 經取代之低碳烷基。在式III化合物之特定實施例中，Rl 係選自氫及低碳烷基。在式冚化合物之特定實施例中， R1係選自氫及甲基。在式ΙΠ化合物之特定實施例中，Rl 為氫。 本發明係提供至少一種選自式Iv化合物及其醫藥上 可接受鹽類之化學品Formula III R1 and R4 are independently selected from the group consisting of hydrogen, optionally substituted thiol, optionally substituted, cyano, halo, azide, optionally substituted amine, optionally substituted Alkoxycarbonyl, optionally substituted amino, sulfonyl, sulfinyl and sulfanyl; Z1 is optionally substituted heteroaryl; Z2 is selected from hydrogen, optionally substituted a mercapto group, a carboxyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted thiol group, an optionally substituted alkenyl group, an optionally substituted alkyl group, and an optionally substituted aminocarbonyl group; 47 200823188 z3 is selected from an optionally substituted aralkyl group and optionally substituted. Heteroaralkyl; and • R3 is selected from the group consisting of hydrogen and optionally substituted alkyl. In a particular embodiment of the compound of formula III, Z1 is selected from heteroaryl which is optionally substituted with 5 or two groups selected from the group consisting of cyano, halo, hydroxy, decyl, optionally Substituted alkyl group, optionally substituted alkenyl group, optionally substituted alkoxy group, carboxyl group, optionally substituted alkoxycarbonyl group, optionally substituted fluorenyl group, optionally substituted aminocarbonyl group , optionally substituted heterocycloalkyl, optionally substituted heteroaryl, 10 optionally substituted formazan, and optionally substituted sulfonyl. In a particular embodiment of the compound of Formula III, Z1 is selected from the group consisting of 1H-pyrazol-3-yl; 1H-pyrazol-4-yl; 1H-triazol-5-yl; 1-indolyl-1H-pyrazole 4-yl-1; 1-methyl-1H-pyrazol-5-yl; 2-(hydroxyindenyl)thiophen-3-yl; 2,2'-dipyridine; 2,3'-dipyridine; 4'-bipyridine; 2-cyanothiophen-3-yl; 2-indole-15-thiophen-3-yl; 3-(hydroxyindenyl)thiophen-2-yl; 3-cyano-1-indenyl -1H-pyrazol-4-yl; 3-carbamimidyl-2-yl; 4-cyanothiophen-3-yl; 4-mercaptothiophen-2-yl; 4-mercaptothiophen-3-yl 5-(1-hydroxyethyl)thiophen-2-yl; 5-(aminomercapto)thiophen-2-yl; 5-(hydroxyindenyl)thiophen-2-yl; 5-(hydroxymethyl) Thiophen-3-yl; 5-ethenylthiophen-2-yl; 5-cyano-1H-pyrazole-4-20; 5-cyano-1-indenyl-1H-pyrazol-4-yl 5-cyanothiophen-2-yl; 5-nonylthiophen-2-yl; 5-nonylthiophen-3-yl; 3-(aminomercapto)thiophen-2-yl; iso-nfazole 4-yl; thiazol-2-yl; thiophen-2-yl; and thiophen-3-yl. In a particular embodiment of the compound of formula III, Z2 is selected from the group consisting of a carboxy group, an optionally substituted alkoxycarbonyl group, an optionally substituted thiol group, an alkenyl group optionally substituted by 48 200823188, and optionally substituted. base. In a particular embodiment of the compound of Formula III, the z2 is selected from the group consisting of a carboxy group, an optionally substituted ketone carbonyl group, an optionally substituted pyridylcarbonyl group, an optionally substituted lower alkyl group, optionally substituted. Lower alkenyl and low carbon alkoxy groups. In a particular embodiment of the compound of formula 111, Z2 is selected from the group consisting of 2-(decylamino)-2-oxoethyl, 2-amino-2-oxyethyl, 3-amino-3-oxypropyl , (2-(N-acetoxyaminoindenyl) beryllyl))-propyl; (2-aminocyanopiperidin-1-yl)yl; 1-trans-base_2-amino-B 2; "methylsulfonylamino" methyl) piperidin-1-ylcarbonyl; 2-(methylaminocarbonyl)vinyl; 2-(pyridylfluorenyl)-2Η-tetras-5-yl Aminomethyl; carboxy; decyloxycarbonyl; pyridin-2-ylcarbonyl; pyridin-3-ylcarbonyl; and pyridin-4-ylcarbonyl. In a particular embodiment of the compound of formula III, R3 is selected from the group consisting of hydrogen and optionally substituted low carbon alkyl. In a particular embodiment of the hydrazine compound, R3 is selected from the group consisting of hydrazine and lower alkyl. In a particular embodiment of the compound of formula m, R is selected from the group consisting of hydrogen and methyl. In a particular embodiment of the compound in the formula, r3 is deuterium. In a particular embodiment of the compound of Formula III, R4 is selected from the group consisting of hydrogen, cyano, halo, azide, optionally substituted aminocarbonyl, and optionally substituted thio. In a particular embodiment of the compound of formula III, R4 is selected from the group consisting of hydrogen, cyano, chloro, bromo, fluoro, azide, optionally substituted alkylaminocarbonyl, and optionally substituted methyl. In a particular embodiment of the hydrazine compound, R4 is selected from the group consisting of hydrogen, cyano, chloro, bromo, azide, π-pyridine-3-yldecylaminocarbonyl, aminoguanidino and hydroxymethyl. In the specific implementation of the compound of formula m 49 200823188 In the example, R4 is hydrogen. - In a specific embodiment of the compound of formula 111, Z2 is -C(0)NR2R5, wherein R2 is selected from an alkyl group optionally substituted and a cycloalkyl group optionally substituted; and R5 is selected from hydrogen And alkyl groups which are optionally substituted. In a particular embodiment of the compound of formula III, R2 is selected from the group consisting of optionally substituted methyl, optionally substituted ethyl, optionally substituted propyl, optionally substituted butyl, optionally substituted. a pentyl group, optionally substituted hexyl group, optionally substituted cyclopropyl group, optionally substituted cyclopentyl group, and optionally substituted cyclohexyl group, wherein each of the optionally substituted groups is optionally subjected to One, two or three are substituted by a group selected as follows: a substituted group, optionally substituted heteroaryl, optionally substituted heterocyclic alkyl, optionally substituted cycloalkyl, The substituted aminocarbonyl group, optionally substituted amino group, hydroxyl group, carboxyl group, optionally substituted alkoxy group, and optionally substituted alkoxy group, if necessary. In a particular embodiment of the compound of formula III, R2 is selected from the group consisting of methyl and ethyl, wherein the thiol and ethyl groups are optionally substituted by one or two groups selected from the group consisting of: Substituted, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, optionally substituted cycloalkyl, optionally substituted aminocarbonyl, optionally substituted amine, hydroxy, carboxy An alkoxycarbonyl group which may be substituted, if appropriate, and an alkoxy group which may be optionally substituted. In a particular embodiment of the compound of Formula III, R2 is selected from the group consisting of (1 gas 2-aminoethyl) thiol; (1-(methyl scutellaria) bridging 0 dimethyl base) methyl, ( 1-乙乙基娘-3-yl)methyl; (1_乙乙基吼 唆_2_基)甲50 200823188 基; (1H-imidazole-2_yl) fluorenyl; (1H-吼Azole-3-(yl)methyl; (1;methyl-methyl-azol-3-yl)methyl; (1-methyl-1H-pyrazole-5-yl)methyl; aminyl)ethyl Amino)carbonylmethyl; (2-(aminomethyl)pyridine-3-yl)methyl; (2-(carboxy)ethylamino)carbonylindenyl; (2-(dimethylamino)) Ethylamino) 5 carbonylmethyl; (2-(hydroxy)ethylamino)carbonylmethyl; (2-(methylamino)ethylamino)carbonyl fluorenyl; (2-(N-曱) (3-tertoxyalkyl)-amino)ethylamino)carbonylmethyl; (2-oxopipridin-3-yl)methyl; (3-(dimethylamino)propylamino) ) benzyl methyl; (3-(trans)ethylamino)ylmethyl; (3-(di-butyl-butyl- thiolamino)propylamino)methylidene; (4_( Aminomethyl 1 fluorenyl) 11-doped-2-yl) fluorenyl; (5-(aminomethyl)u to 唆_2_yl Methyl; (6-((153-^-oxy-iso-iso-indolyl)))))))))) Amino) acridine-2-yl) fluorenyl; (6-(3-aminopropylamino) σ-bit-2-yl) fluorenyl; (6-(aminomethyl-to-bit II) -yl) fluorenyl; (heart (via fluorenyl) acridine-2-yl)methyl; (6-bromopyridinyl)methyl; (methyl hydrazine 2 15 yl) # 曱 曱 曱, (σ ratio σ-_2-yl) ethylamino group; 1-(2-(t-butanylamino)ethyl)_1Η-oxazol-3-ylmethyl; 1-(2- (t-butoxymethylamino)ethyl)_1H-pyrazol-5-ylindenyl; 1-(aminocarbonyl)-2-(amino)-eth-1-yl; 1-(amino Carbonyl)-3-(amino)-propyl; 1-(aminocarbonyl)_4-(amino)-butyl; 1-(aminocarbonyl)-4-(phenylhydrazyloxycarbonylaminopentyl) 20 i-(Amino # 厌基)-5-(amino)-pentyl; i-(amino)ethyl; i-(yl)-2-(amino)-B-1 1-(didecylaminocarbonylcarbonyl (10)-ethyldiamine; 1-(hydroxy)-2-(aminocarbonylmethylamino)ethyl small; 1-(trans)-2-(ethoxy) Methylamino) ethyl bromide; (base) _2 ten bite_2_ Methylamino)ethyl-1-yl; 1_(decyloxycarbonyl>2-(amino)-ethyl-4-yl; 51 200823188 1-(decyloxycarbonyl)-2-(t-butoxy Alkylcarbonylamino)-ethyl-1-yl; 1-(methyloxycarbonyl)eth-1-yl; 1-(methylaminocarbonyl)-2-(amino)-eth-1-yl ( 2 • occ), 1-(decylamino green) ethyl-1-yl, 1-amino-chloro-2-yl-yl group "B-1 yl, 1-methyllacyl-green-2- Benzyl-ethyl-1-yl, 2-(2-amino-ethothyl)ethyl-5,2-(2-aminoethyl)-indole-bital-6-ylmethyl, 2-(2- Aminoethylamino)ethyl; 2-(3-fluorophenyl)ethyl; 2-(3-indolyloxycarbonyl)ethyl; 2-(6-(amino fluorenyl) hydrazine-2 -yl)ethyl, 2-(ethionylamino)ethyl, 2-(amino)ethyl, 2-(amino-based)-2-(ethenylamino)-ethyl-1- Base, 2-(amino aryl)-2-(amino)-eth-1-yl, 2-(aminoindenyl)ethyl, 2-(aminoindenyl) 10 吼σ定-5- Base group, 2-(mercapto-2-(amino)-ethyl-1-yl, 2-(didecylamino), ethyl, 2-(dimethylamino-chloro)-2- (amino)-ethyl-1-yl, 2-(ethoxycarbonyl)ethyl; 2-(methoxycarbonyl)-2-(ethenylamino)-eth-1-yl; 2-(decyloxy)-2-(amino)-eth-1-yl, 2-(decyloxyaminoamino)ethyl; 2-(decylamino)ethyl; 2- (Methylaminocarbonyl)-2-(ethenylamino)-ethyl 15 -1 -yl, 2-(decylamino green)-2-(amino)-ethyl-1-yl, 2 -(曱基石黄酉龟 amino)ethyl, 2-(indolyl-yl-yl)-2-(amino)-eth-1-yl, 2-(N-(di-dibutoxy) -N-(indenyl)-amino)ethyl, 2-(Lv.-1-yl)ethyl, 2-(indol-2-yl)ethyl; 2-(acridin-2-yl) Ethyl; 2-(oxaridin-3-yl)ethyl; 2-(t-butoxycarbonylaminomethyl)acridin-3-ylindenyl; 2-(third 20-butoxycarbonyl) Aminoalkyl)acridin-6-ylindenyl; 2-(trifluoromethyl)-acridin-6-ylindenyl, 2-amino-based -3-ylindenyl, 2-amino 0 ratio bit-5-ylmethyl, 2-chloroacridin-5-ylindenyl; 2-cyanoacridin-5-ylindenyl; 2-hydroxy-3-amino-propan-1-yl, 2-Phenylethyl, 2-methoxyethyl-1-yl, 2-methoxyl ratio. -3 - fluorenyl; 2-nonoxyacridin-5-ylindenyl; 2-mercaptoacridin-3-ylindenyl; 52 200823188 2-mercaptopyridine-5-ylindenyl; Methylpyridine_6_ylindenyl; 3-(2-aminoethyl)cyclohexyl)methyl; 3-(4-methyl brigade, well base) propyl; 3-(aminopurine (methylamine) 3-carbonyl)propyl; 3-(aminocarbonyl)propyl; 3-(aminomethyl)benzene, fluorenyl, 3·(amino fluorenyl quinone than _2 yl hydrazino; 3_(oxygen Benzyl carbonyl) propyl; 5 methyl virginal ruthenyl) propyl, 3-(trioxoyl)_π ratio -2-ylmethyl; 3 4 _ fluoro- fluorenyl, 3-amino hydrazine π 唆 唆-4-ylmethyl; 3-aminopropyl; 3-aminoglycosylcyclopentyl; 3-reradyl; 3-propylpropyl; 3-methoxypropyl; 4_ (aminomethyl)" than 2-carboxyl group; 4-(anthracene, fluorenyl-didecylamino)pyridin-3-ylindenyl; 4-(t-butoxycarbonylamino) _ 琳 基 甲基 methyl; 4 〇 1 amino butyl; 4-amino fluorenyl ^ 1 than -3- fluorenyl; 4-cyanobenzyl; 4- • fluorophenyl fluorenyl; Methylaminoindol-3-ylmethyl; 4-methylphenylindenyl; 4-morpholinylpyridin-3-ylmethyl; 4-piperidinylpyridin-3-ylindenyl ; 5-((bis(dimethylamino)decylamino)methylbutyryl-3-ylindenyl; 5-(aminoindenyl)u than deuterated-2-ylindenyl; -(aminomercapto) aceto-3-ylmethyl; 5-(hydroxyindenyl) 15 acridine-3-ylindenyl; 5-(t-butoxycarbonylaminoindenyl)-π ratio Pyridin-2-ylindenyl; 5-(trifluoromethyl)-acridin-2-ylindenyl; 5-aminopentyl; 5-aminoacridin-2-ylmethyl; 6-(( Bis(dimethylamino)methylamino)methyl)π-pyridin-2-yl)methyl, 6-(4-ethyl-branyl-bran-1-yl)pyrene sigma-3- Methyl), 6-(amino-based fluorenyl-2-pyridyl; 6-aminohexyl; aminocarbonylcarbonyl; benzene 20 methyl; cyclopropyl fluorenyl; dimercaptoamine Carbonylmethyl; isopropyl; isoxazol-5-ylindenyl; methoxycarbonylhydrazino; methyl; methylaminocarbonylcarbonyl; hydrazine salicyl-2-ylmethyl; 4-ylindenyl, prop-2-yl-1-yl, oxime-2-ylindenyl; pyridin-2-ylmethyl; pyridin-2-ylindenyl-indole-oxide; pyridine-3 - fluorenyl; pyridin-3-ylindenyl-indole-oxide; pyridin-4-ylindenyl; thia 53 200823188 phen-2-ylmethyl, and decet-3-ylindenyl. In a particular embodiment of the compound of formula JII, Ζ3 is selected from the group consisting of: -(CH2)rR20, wherein r is selected from 1, 2 and 3, and R20 is selected from the group consisting of an optionally substituted, substituted aryl group and optionally substituted Heteroaryl. 5 In a particular embodiment of the compound of formula III, Z3 is selected from the group consisting of 2-(3-mercaptophenyl)ethyl, 2-(1Η-imidazol-4-yl)ethyl, 2-(1 -mercapto-1H-imidazol-4-yl)ethyl, 2-(2,3-difluorophenyl)ethyl, 2-(2,5-difluorophenyl)ethyl, 2-(2, 6-difluorophenyl)ethyl, 2-(2-chlorophenyl)ethyl, 2-(2-cyanophenyl)ethyl, 2-(2-fluorophenyl)ethyl, 2-( 2-hydroxyphenyl)ethyl, 2-(2-decyloxyphenyl) 1 fluorene ethyl, 2-(2-mercaptophenyl)ethyl, 2-(3-(trifluoromethyl)benzene Ethyl, 2-(3,4-difluorophenyl)ethyl, 2-(3,5-difluorophenyl)ethyl, 2-(3,5•dimethyl-1H-indole Zin-1-yl)ethyl, 2-(3,5-dimethyl-1H-pyrazol-4-yl)ethyl, 2-(3-aminoindenylphenyl)ethyl, 2-( 3-carboxyphenyl)ethyl, 2-(3-carbophenyl)ethyl, 2-(3-(phenyl)-2-(light)-ethyl, 2-(3-p-phenyl) 15 ethyl, 2-(3-qi^biti-2-yl)ethyl, 2-(3- Lacyl phenyl)ethyl, 2-(3-decyloxyphenyl)ethyl, 2-(3-methylphenyl)ethyl, 2-(4-aminophenyl)ethyl, 2-(4-chlorophenyl)ethyl, 2-(4-fluorophenyl)ethyl, 2-(4-hydroxyphenyl)ethyl, 2-(benzo[d][l,3] Oxycyclopentene-5-yl)ethyl, 2-(furan-2-yl)ethyl, 2-(hydroxy)-2-(phenyl)ethyl, 2-(phenyl)ethyl, 2〇2 -(°~ϋ-2-yl)ethyl, 2-(°-pyridin-3-yl)ethyl, 2-(σ-cephen-2-yl)ethyl, 2-phenylpropan-1 -yl, 3-(1Η-imidazol-1-yl)propan-1-yl, 3-phenylpropyl, benzyl, pyridin-2-ylindolyl, pyridin-3-ylindenyl and thiophene-3 - Base base. In a particular embodiment of the compound of formula III, the oxime 3 is selected from the group consisting of 3-fluorophenylethyl 54 200823188, 3,5-dicyanophenethyl and 20-pyridin-2-yl)ethyl. In a particular embodiment of the compound of formula m, hydrazine 3 is 2-(pyridin-2-yl)ethyl. In a particular embodiment of the compound of formula III, Ri is selected from the group consisting of hydrogen and optionally substituted lower alkyl. In a particular embodiment of the compound of Formula III, R1 is selected from the group consisting of hydrogen and lower alkyl. In a particular embodiment of the hydrazine compound, R1 is selected from the group consisting of hydrogen and methyl. In a particular embodiment of the hydrazine compound, R1 is hydrogen. The present invention provides at least one chemical selected from the group consisting of a compound of the formula Iv and a pharmaceutically acceptable salt thereof

式IV >〇 其中 R及R係獨立地選自氫、視需要經取代之醢基、視需 要經取代之烧基、氰基、_基、疊氮基、視需要經取代之 胺基、視需要經取代之烷氧基羰基、視需要經取代之胺基 羰基、橫醯基、亞續醯基及硫烧基；ζι係選自視需要經取 代之芳基及視需要經取代之雜芳基；z2係選自氫、羧基、 視需要經取代之烷氧基羰基、視需要經取代之醯基、視需 要經取代之烯基、視需要經取代之烧基、祝需要红取代之 甲脒基及視需要經取代之胺基羰基； Z為視需要經取代之烧基；及 55 200823188 r3係選自氳及視需要經取代之烷基。 - 在式IV化合物之特定實施例中，Z1係選自係視需要 經一或二個由下列選出之基團取代之芳基··氰基、鹵基、 • 羥基、、甲醯基、視需要經取代之烷基、視需要經取代之烯 土 視品要經取代之烧氧基、叛基、視需要經取代之烧氧 土罗火基視需要經取代之蕴基、視需要經取代之胺基幾 f、視需要經取代之胺基視需要經取代之雜環烷基、視 需要經取代之雜芳基、視需要經取代之曱脒基及視需要經 取代之磺醯基；以及係視需要經一或二個由下列選出之基 ίο 團取代之雜芳基：氰基、鹵基、羥基、甲醯基、視需要經 • 取代之燒基、視需要經取代之烯基、視需要經取代之烧氧 基、羧基、視需要經取代之烷氧基羰基、視需要經取代之 基、視需要經取代之胺基幾基、視需要經取代之雜環燒 基、視需要經取代之雜芳基、視需要經取代之甲脉基及視 15 需要經取代之石黃醯基。 在式IV化合物之特定實施例中，z1係選自係視需要經 一或二個由下列選出之基團取代之芳基：氰基、鹵基、輕 基、甲醯基、視需要經取代之低碳烷基、視需要經取代之 低碳烯基、視需要經取代之低碳烷氧基、羧基、視需要經 20 取代之低碳烷氧基羰基、視需要經取代之低碳醯基、視需 要經取代之胺基羰基、視需要經取代之雜環烷基、視需要 經取代之雜芳基及視需要經烷基取代之胺基；以及係視需 要經一或二個由下列選出之基團取代之雜芳基··氰基、自 基沒基、甲基、視需要經取代之低奴烧基、視需要經 56 200823188 取代之低碳烯基、視需要經取代之低碳烷氧基、羧基、才 需要經取代之低碳烷氧基羰基、視需要經取代之^碳= 基、視而要經取代之胺基羰基、視需要經取代之雜環燒 基、視需要經取代之雜芳基及視需要經烷基取代之胺基。 在式IV化合物之特定實施例中，ζι係選自苯基、ιΗ_ 吡唑-3-基；1H-吼唑_4_基；iH_三唑_5_基；曱基-1H_吡 唑-4-基；1-曱基-1H-吡唑_5_基；2-胺基曱基噻吩-5-基；2-氰基噻吩-3-基；2-甲醯基噻吩_3_基；2_曱醯基噻吩-4_基； 2H-吡咯-Κ511)·基；2-羥基曱基噻吩_3_基；2-羥基曱基噻 吩-4-基；2_羥基甲基噻吩-5-基；3-胺基曱基噻吩-2-基； 3-氰基小甲基-1Η-吡唑冰基；3-氰基噻吩-4_基；3-曱醯基 噻吩-2-基；3-羥基甲基噻吩_2_基；4-曱基噻吩-2-基；4-曱基噻吩_3_基；5·(1羥基乙-1-基)-噻吩-2-基；5-乙醯基噻 吩-5-基；氰基-1Η—吡唑-4-基；5-氰基-1-甲基-1Η-吡唑-4-基；5-氰基噻吩1基·’ 5-甲醯基噻吩-2-基；5-羥基曱基噻 吩-2-基；異畤嗤+基；吡啶-2-基；吡啶-3-基；吡啶-4-基；噻唑-2-基；嗟吩-2-基；及噻吩-3-基。在式IV化合物 之特定實施例中，ζ1為苯基。 在式IV化合物之特定實施例中，ζ2係選自羧基、視 需要經取代之烷氧基羰基、視需要經取代之醯基、視需要 經取代之烯基及視需要經取代之烷基。 在式IV化合物之特定實施例中，Ζ2係選自羧基、視 需要經取代之ϋ比唆基甲基羰基、視需要經取代之哌啶基羰 基、視需要經取代之12比啶基羰基、視需要經取代之低碳烷 57 200823188 基、視需要經取代之低碳烯基及低碳烷氧基羰基。 在式IV化合物之特定.實施例中，Z2係選自吡啶-3-基甲 基羰基、（2-(N-乙醯基胺基曱基)哌啶小基）羰基；（2_胺基 曱基旅11 定-1-基）幾基；1-經基_2_胺基·乙基；2-((曱基石黃醯 胺基）曱基)σ底咬-1-基幾基；2-(曱基胺基獄基）乙稀基；2十比 啶-3-基甲基)-2Η-三唑-5-基曱基；胺基甲基；羧基；曱氧 基幾基；比咬_2_基幾基；π比唆-3-基幾基；及吼咬-4-基幾 基。 在式IV化合物之特定實施例中，Ζ2為-C(0)NR2R5其中 R2係選自視需要經取代之烷基及視需要經取代之環烧 基；而R5係選自氫及視需要經取代之烧基。 在式IV化合物之特定實施例中，R2係選自視需要經取 代之甲基、視需要經取代之乙基、視需要經取代之丙基、 視需要經取代之丁基、視需要經取代之戊基、視需要經取 代之己基、視需要經取代之環丙基、視需要經取代之環戊 基及視需要經取代之環己基，其中各視需要經取代之之基 團係視需要經一、二或三個由下列選出之基團取代··視需 要經取代之芳基、視需要經取代之雜芳基、視需要經取代 之雜環烷基、視需要經取代之環烷基、視需要經取代之胺 基羰基、視需要經取代之胺基、羥基、羧基、視需要經取 代之烧氧基幾基及視需要經取代之烧氧基。 在式IV化合物之特定實施例中，R2係選自甲基及乙 基’其中該曱基及乙基基團係視需要經一或二個由下列選 出之基團取代：視需要經取代之芳基、視需要經取代之雜 58 200823188 芳基、視需要經取代之雜環烷基、視需要經取代之環烷 基、視需要經取代之胺基羰基、視需要經取代之胺基、羥 • 基、羧基、視需要經取代之烷氧基羰基及視需要經取代之 . 炫氧基。 5 在式IV化合物之特定實施例中，R2係選自（μ(2-胺基 乙基)-m^比唑_3-基）曱基；（1-(甲基磺醯基）哌啶冬基）甲 基；（1-乙酸基派咬-3-基）甲基；（1-乙酸基啦略咬_2_基）甲 基；（1H_味唾-2-基）甲基；（1Η_σ比唾-3-基）甲基；（ι_甲基-IH-吼嗤-3-基）曱基；（1-甲基基）甲基；（2-(胺基獄 1〇 基）乙基胺基）幾基甲基；（2-(胺基甲基)吼咬_3_基）甲基； . (2_(羧基）乙基胺基)羰基曱基；（2-(二甲基胺基）乙基胺基） 羰基曱基；（2-(羥基）乙基胺基）羰基甲基；（2-(甲基胺基） 乙基胺基）羰基甲基；（2-(Ν-甲基(第三丁氧基羰基)_胺 基）乙基胺基)羰基曱基；（2-氧基哌啶-3-基）曱基；（3_(二甲 15 基胺基）丙基胺基）幾基甲基；（3-(經基）乙基胺基）魏基曱 基’（3-(弟二丁氧基祿基胺基）丙基胺基)幾基甲基；（4_ (胺 基甲基）σ比咬-2-基曱基；（5-(胺基甲基）π比π定基）曱基； (6-((1，3- ^一乳基兴°引ϋ朵琳-2-基）曱基）u比u定基）曱基； (6_〇胺基乙基胺基户比啶_2_基）甲基；(6_(3_胺基丙基胺基） 20 吼11定基）曱基，（6-(胺基曱基)吼咬-2-基）曱基；（6_(經基 曱基)吼啶-2-基）甲基；（6_溴吼啶_2_基）甲基；（曱基磺醯胺 基)$厌基曱基’（0比唆-2-基）乙基胺基；1-(2-(第三丁氧基獄 基胺基）乙基)-lH-u比唑-3-基曱基；1-(2-(第三丁氧基羰基胺 基）乙基)-1Η』比唑_5_基曱基；l(胺基羰基)_2_(胺基)_乙小 59 200823188 基，ι·(胺基幾基；μ(胺基)_丙基；(胺基幾基)_4_(胺基)_ -丁基，h(胺基羰基(苯甲基氧基羰基胺基)_戊基；μ(胺 基幾基）_5_(胺基）-戊基；1-(胺基羰基）乙-1-基；1_(叛 • 基)·2-(胺基)·乙小基；1_(二甲基胺基羰基)_2_(胺基)_乙小 5 基；h(羥基）-2_(胺基羰基甲基胺基）乙小基；1-(羥 基)-2-(乙氧基羰基甲基胺基）乙_丨_基；1_(羥基)_2_卜比啶_2_ 基甲基胺基）乙-l-基；〗-(甲氧基羰基>2_(胺基卜乙]—基； 1- (甲氧基羰基)-2-(第三丁氧基羰基胺基)_乙4_基；1_(曱氧 基幾基）乙-1-基；1_(曱基胺基羰基)_2-(胺基 > 乙-；[_基(2 10 occ) ; Η甲基胺基羰基）乙小基；1-胺基羰基-2_羥基-乙小 • 基；丨-曱氧基羰基羥基乙小基；2_(2_胺基乙氧基）乙基； . 2_(2_胺基乙基)-σ比啶-6-基甲基；2-(2-胺基乙基胺基）乙基； 2- (3-氟苯基）乙基；2-(3-曱氧基羰基）乙基；2-(6-(胺基曱基） 吼啶-2-基）乙基；2_(乙醯基胺基）乙基；2-(胺基）乙基；2-(胺 15 基羰基)-2-(乙醯基胺基)-乙-1-基；2-(胺基羰基)-2-(胺基)_ 乙-1-基；2-(胺基羰基）乙基；2-(胺基甲基)吼啶-5_基甲基； 2-(羧基)_2-(胺基)-乙-1-基；2-(二曱基胺基）乙基；2-(二曱 基胺基羰基)-2-(胺基)-乙-1-基；2-(乙氧基羰基）乙基；2-(曱 氧基羰基)-2-(乙醯基胺基)-乙-1-基；2-(曱氧基羰基)-2-(胺 2〇 基)_乙-1-基；2-(甲氧基羰基胺基）乙基；2-(甲基胺基）乙基； 2-(曱基胺基羰基)-2-(乙醯基胺基)-乙-1-基；2-(曱基胺基羰 基)-2-(胺基)-乙-1-基；2-(曱基磺醯胺基）乙基；2-(曱氧基 羰基)-2-(胺基)-乙-1-基；2-(N-(第三丁氧基羰基)-N-(曱基)-胺基）乙基；2-(哌畊-1-基）乙基；2-(咕畊-2-基）乙基；2-(。比 200823188 咬-2·基）乙基；2-〇b唆-3-基）乙基；2-(第三丁氧基幾基胺 基曱基)吼啶-3-基曱基；2-(第三丁氧基羰基胺基曱基)吼啶 -6-基甲基；2_(三氟曱基)-吡啶-6-基曱基；2_胺基吡啶-3-， 基甲基；2-胺基吡啶-5-基甲基；2-氯吡啶-5-基曱基；2- 5 氰基吡啶-5-基曱基；2-羥基-3_胺基-丙-1-基；2-羥基乙基； 2- 曱氧基乙-1-基；2-甲氧基吡啶-3-基曱基；2-曱氧基吡啶 -5·基曱基；2-曱基吼啶-3-基曱基；2-曱基吡啶-5-基曱基； 2·甲基。比咬-6-基曱基；3-(2-胺基乙基)環己基）曱基；3-(4-曱基哌畊-1-基）丙基；3-(胺基)-3-(曱基胺基羰基）丙-1-基； 10 3-(胺基羰基）丙基；3-(胺基曱基）苯曱基；3-(胺基曱基)吡 咬-2-基曱基；3-(甲氧基幾基）丙基；3_(曱基胺基戴基）丙 基；3-(三氟曱基)-吡啶-2-基曱基；3,4-二氟苯曱基；3-胺 基曱基吼啶-4-基曱基；3-胺基丙基；3-胺曱醯基環戊基； 3- 羧基丙基；3-羥基丙基；3-甲氧基丙基；4-(胺基曱基)- 15 吡啶-2-基曱基；4-(N，N-二曱基胺基)吡啶-3-基曱基；4_(第 三丁氧基羰基胺基)-嗎啉基曱基；4-胺基丁基；4-胺基曱 基吼啶-3-基曱基；4-氰基苯甲基；4-氟苯曱基；4-曱基胺 基吼啶_3_基曱基；4-甲基苯曱基；4_嗎啉基u比啶-3-基曱基； 4- 哌畊基吡啶-3-基曱基；5-((雙(二甲基胺基）曱基胺基）曱 20 基)吡啶-3-基曱基；5-(胺基曱基)吡啶-2-基曱基；5-(胺基 曱基)吡啶-3-基曱基；5_(羥基曱基)吡啶-3-基曱基；5-(第 三丁氧基幾基胺基甲基)-^比咬-2·基曱基；5-(三氟曱基)-吼 唆-2-基曱基；5-胺基戊基；5-胺基^比咬-2-基甲基；6-((雙(二 曱基胺基)伸曱基胺基）曱基)吼啶_2_基）曱基；6-(4-乙醯基 200823188 σ辰11 井-1-基户比咬-3-基甲基）；6-(胺基甲基)u比咬冬基）曱基； 6-月女基己基，胺基幾基曱基；本甲基；環丙基甲基；二曱 基胺基羰基甲基；異丙基；異4唑-5-基甲基；曱氧基羰基 甲基；甲基；曱基胺基羰基甲基；噚唑_2_基甲基；哌啶_4_ 基曱基，丙-2-細-1-基；π比口井-2-基甲基；π比唆基甲基； 定-2-基甲基氧化物；η比咬-3-基甲基；π比唆基甲基 -Ν-氧化物；吡啶_4_基曱基；噻吩-2-基甲基；及噻吩_3_ 基曱基。 10 在式IV化合物之特定實施例中，R2為吡啶-3_基曱基。 在式IV化合物之特定實施例中，R5係選自氫及低碳烷 基。在式IV化合物之特定實施例中，R5係選自氳及曱基。 在式IV化合物之特定實施例中，R5為氫。 15 20 、牡八a籾疋貫施例T，Z」係選自視需要經取 代之環烷基烷基、視需要經取代之雜環烷基烷基。在式Iv ^合物之特定實關巾，自仰狀2()其^係選自 1、2、及3而R20係選自視雹最級说化上〜 u ^ ^ 兄而要經取代之雜環烷基及視需要 經取代之環烷基。 τ 2其、21¥化合1 物之特定實施例中，Z3係選自(四氫呋喃 義基）甲基、！-減環己基f基、2_(1，3_二氧戊環_2_基）乙 二、2-(11基錢斗基化基、吵氧基咪㈣小基）己 ς、2-=-乳基派咬小基）乙基、2_(2_氧基料咬小基）己 土 2-%<、己-1-烯基乙基、2_環己基乙基及2_嗎琳基乙基。 在式IV化合物之特定實施例中，r1係選自氮及視需 要經取代之低魏基。在式IV化合物之特定實施例中， 62 200823188 R1係選自氫及低碳烷基。在式IV化合物之特定實施例 中，R1係選自氳及曱基。在式IV化合物之特定實施例中， R1為氫。 • 在式IV化合物之特定實施例中，R3係選自氬及視需要 5 經取代之低碳烷基。在式IV化合物之特定實施例中，汉3 係選自氳及低碳烷基。在式IV化合物之特定實施例中， R3係選自氮及曱基。在式IV化合物之特定實施例中，汉3 為氳。 在式IV化合物之特定實施例中，R4係選自氫、氰基、 10 鹵基、豐氣基、視需要經取代之胺基幾基及視需要經取代 - 之烷基。在式IV化合物之特定實施例中，R4係選自氫、氮 基、氯、溴、氟、疊氮基、視需要經取代之烷基胺基羰基 及視需要經取代之曱基。在式IV化合物之特定實施例中， R係运自虱、fL基、氣、溴、疊氮基、tr比u定_3 _基曱基胺基 15 #厌基、胺基甲基及备基甲基。在式IV化合物之特定實施例 中，R4為氫。 ' 在特定實施例中，式I化化合物係選自 N-甲基（6_苯基-2-[(2_苯基乙基)胺基]化比啶基)}甲醯胺 {6-苯基-2_[(2-苯基乙基)胺基](3_π比啶基丙_2_烯基曱 20 醯胺 1 {6_苯基-2-[(2-苯基乙基)胺基](3_t定基)}|(3』比啶基甲 基）甲酸胺 N-(曱基乙基）{6_苯基_2_[(2_(2_„比咬基）乙基)胺基]ο比咬 63 200823188 {6-苯基-2-[(2-(2-吡啶基）乙基）胺基](3_吡啶基）}_ν_(2^λ -啶基甲基）甲醯胺 5 10 15 20 {6-苯基-2-[(2-(2-吡啶基）乙基）胺基](3_吡啶基）}_N_(4_t 口疋基甲基）甲酸胺（2_{[2_(3，甲基苯基）乙基]胺基卜卜苯基 (3-吼啶基))_N_丙-2-烯基甲醯胺 {6-苯基-2-[(2·(2_吡啶基）乙基）胺基](3_吡啶基）}_义(4_吡 啶基）甲_ Ν_甲基(2_{[2♦甲基苯基）乙基]胺基笨 基(3-咣啶基)）甲醯胺 Ν-(氧雜戊環ι基甲基）(6_苯基_2κ2_π比咬基）乙基 基](3-吡啶基)}甲醯胺 N-[((2S)氧雜戊環-2-基）甲基](6_苯基-2-[(2-(2-,比啶基）乙 基)胺基](3-吡啶基)}甲醯胺 {笨基2 [(2-(2_t定基）乙基）胺基](ρ比咬基 咬基甲基）甲酿胺 =)己甲：基乙基)胺基]—6·苯基(3,基)陶- (6_苯基_2-[(3-苯基丙基)胺基]ο比咬基)}_Ν_(3_π比咬基 基)甲酿胺Ν-(1，3·Μ_2-基甲基){6_苯基_2_[(2_(2_^ 乙基）胺基](3_吡啶基）}甲醯胺 土 Ν-(味唾-2-基甲基）{6_苯基_2_[(2_(2_吼σ定基）乙基）胺 基](3_吡啶基)}甲醯胺 =[((3SM -乙酿基D比略唆_3_基）甲基]{6_苯基_2|心比 啶基）乙基)胺基](3-吡啶基）}甲醯胺 {6-苯基-2-[(2-(2“比唆基）乙基)胺基](n定基》仰“比 64 200823188 啶基）甲醯胺、 {•2-[(3-甲基了基)胺基]-6-苯基〇比,定基)}|(3』比嚏 基）甲醯胺 土 {2-[(2-環己基乙基）胺基]-6-苯基(3-π比咬基）}_Ν_(3_σ比咬吴 甲基）甲酸胺 Ν-{[1-(甲基磺醯基)(3-哌啶基)]甲基丨{6_苯基_2_[(2_(2_吡 啶基）乙基)胺基](3-吼啶基)}甲醯胺 2-(胺基曱基)旅咬基6-苯基_2-[(2_(2“比啶基）乙基)胺基κ3_ 吡啶基）酮 1 N-m-w-苯基-2_[(2〇比啶基）乙基)胺基]_3_n比啶基}幾 基)-2-哌啶基]甲基}乙醯胺 2-{[(甲基磺醯基)胺基]曱基}哌啶基心苯基-2_[(2<2_^比啶 基）乙基)胺基](3-°比°定基）酉同 15 N-[(l-曱基口比嗤_5_基）甲基]{卜苯基_2_[(2_(2“比啶基）乙 胺基](3-吡啶基）}甲醯胺 土 {6-苯基-2-[(2-(2-吡啶基）乙基）胺基](3_吡啶基）}_N_(吡唑 -3-基曱基）曱酿胺 N-(異崎唑-5_基曱基）{6•苯基_2_[(2_(2_吡啶基）乙基）胺 基](3-吼啶基)}甲醯胺 N-苯曱基{6_苯基-2-[(2-(2_t定基）乙基)胺基](3“比啶Formula IV > wherein R and R are independently selected from the group consisting of hydrogen, optionally substituted thiol, optionally substituted alkyl, cyano, yl, azide, optionally substituted amine, a substituted alkoxycarbonyl group, an optionally substituted aminocarbonyl group, a fluorenyl group, a hydrazine group, and a thiol group, optionally substituted; an aryl group selected from an optionally substituted aryl group and optionally substituted An aryl group; z2 is selected from the group consisting of hydrogen, a carboxyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted fluorenyl group, an optionally substituted alkenyl group, an optionally substituted alkyl group, and a red substitution. A mercapto group and an optionally substituted aminocarbonyl group; Z is an optionally substituted alkyl group; and 55 200823188 r3 is selected from the group consisting of anthracene and optionally substituted alkyl. - In a particular embodiment of the compound of formula IV, Z1 is selected from the group consisting of aryl, cyano, halo, hydroxy, carbyl, and The substituted alkyl group, the optionally substituted olefinic product to be substituted, the alkoxy group, the thiol group, the optionally substituted oxy-oxygen sulphate, the substituted base, and the optionally substituted amine a substituent, optionally substituted heteroalkyl, optionally substituted heteroaryl, optionally substituted sulfhydryl, and optionally substituted sulfonyl; and Heteroaryl substituted by one or two groups selected by the following groups: cyano, halo, hydroxy, formamyl, optionally substituted alkyl, optionally substituted alkenyl, A substituted alkoxy group, a carboxyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted group, an optionally substituted amino group, an optionally substituted heterocyclic group, and optionally a heterocyclic group are required. Substituted heteroaryl, optionally substituted formethine and visual 15 Acyl yellow stone. In a particular embodiment of the compound of Formula IV, z1 is selected from aryl which is optionally substituted with one or two groups selected from the group consisting of cyano, halo, light, mercapto, optionally substituted Lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, carboxy, optionally substituted 20 lower alkoxycarbonyl, optionally substituted lower hydrazine a substituted, substituted carbonylcarbonyl group, optionally substituted heterocycloalkyl group, optionally substituted heteroaryl group, and optionally substituted alkyl group; and optionally by one or two The following selected groups are substituted with a heteroaryl-cyano group, a carbaryl group, a methyl group, a sub-alkali group which is optionally substituted, a lower alkenyl group which is optionally substituted by 56 200823188, and optionally substituted. a lower alkoxy group, a carboxyl group, a substituted lower alkoxycarbonyl group, an optionally substituted carbon group, an optionally substituted aminocarbonyl group, an optionally substituted heterocyclic group, A substituted heteroaryl group and an alkyl group substituted with an alkyl group as needed. In a particular embodiment of the compound of Formula IV, the oxime is selected from the group consisting of phenyl, iota-pyrazol-3-yl; 1H-carbazole-4-yl; iH-triazole-5-yl; thiol-1H-pyrazole 4-yl; 1-mercapto-1H-pyrazole-5-yl; 2-aminomercaptothiophen-5-yl; 2-cyanothiophen-3-yl; 2-carbamimidyl _3_ 2; mercaptothiophene-4-yl; 2H-pyrrole-oxime 511)-yl; 2-hydroxymethylthiophene-3-yl; 2-hydroxyindolylthiophen-4-yl; 2-hydroxymethylthiophene -5-yl; 3-aminomercaptothiophen-2-yl; 3-cyano small methyl-1 Η-pyrazole ice; 3-cyanothiophen-4-yl; 3-mercaptothiophene-2 -yl; 3-hydroxymethylthiophene-2-yl; 4-mercaptothiophen-2-yl; 4-mercaptothiophene-3-yl; 5·(1hydroxyethyl-1-yl)-thiophene-2- 5-(Ethylthiophen-5-yl; cyano-1Η-pyrazol-4-yl; 5-cyano-1-methyl-1Η-pyrazol-4-yl; 5-cyanothiophene 1 5-'Methylmercaptothiophen-2-yl; 5-hydroxydecylthiophen-2-yl; isoindole+yl; pyridin-2-yl; pyridin-3-yl; pyridin-4-yl; thiazole -2-yl; porphin-2-yl; and thiophen-3-yl. In a particular embodiment of the compound of Formula IV, hydrazine 1 is a phenyl group. In a particular embodiment of the compound of Formula IV, the oxime 2 is selected from the group consisting of a carboxy group, an optionally substituted alkoxycarbonyl group, an optionally substituted thiol group, an optionally substituted alkenyl group, and an optionally substituted alkyl group. In a particular embodiment of the compound of Formula IV, the oxime 2 is selected from the group consisting of a carboxy group, optionally substituted fluorenylmethylcarbonyl, optionally substituted piperidinylcarbonyl, optionally substituted 12-pyridylcarbonyl, If desired, the substituted lower alkane 57 200823188, if desired, substituted lower alkenyl and lower alkoxycarbonyl. In a particular embodiment of the compound of Formula IV, Z2 is selected from the group consisting of pyridin-3-ylmethylcarbonyl, (2-(N-ethylindolyl fluorenyl)piperidinyl)carbonyl; (2-amino曱基旅11定-1-yl) benzyl; 1-trans-base_2-aminoethyl; 2-((fluorenyl sulphate) fluorenyl) σ bottom-1-yl group; 2-(decylamine-based) ethylidene; 2 decapyridin-3-ylmethyl)-2Η-triazol-5-ylindenyl; aminomethyl; carboxy; decyloxy; More than a bit of a 2-amino group; π is more than a 唆-3-yl group; and a bite-4-yl group. In a particular embodiment of the compound of Formula IV, Ζ2 is -C(O)NR2R5 wherein R2 is selected from alkyl optionally substituted alkyl and optionally substituted cycloalkyl; and R5 is selected from hydrogen and optionally Replace the base. In a particular embodiment of the compound of formula IV, R2 is selected from the group consisting of optionally substituted methyl, optionally substituted ethyl, optionally substituted propyl, optionally substituted butyl, optionally substituted. a pentyl group, optionally substituted hexyl group, optionally substituted cyclopropyl group, optionally substituted cyclopentyl group, and optionally substituted cyclohexyl group, wherein each of the optionally substituted groups is optionally required Substituted by one, two or three groups selected by the following: optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, optionally substituted naphthenic A substituted, substituted aminocarbonyl group, an optionally substituted amino group, a hydroxyl group, a carboxyl group, an optionally substituted alkoxy group, and an optionally substituted alkoxy group. In a particular embodiment of the compound of Formula IV, R2 is selected from the group consisting of methyl and ethyl' wherein the thiol and ethyl group are optionally substituted by one or two groups selected from the group consisting of: Aryl, optionally substituted, heteropoly 58 200823188 aryl, optionally substituted heterocycloalkyl, optionally substituted cycloalkyl, optionally substituted aminocarbonyl, optionally substituted amine, Hydroxy group, carboxyl group, optionally substituted alkoxycarbonyl group and optionally substituted. 5 In a particular embodiment of the compound of formula IV, R2 is selected from the group consisting of (μ(2-aminoethyl)-m^bizozol-3-yl)indenyl; (1-(methylsulfonyl)piperidine Methyl; methyl (1-acetate)-3-(methyl)-methyl (1-acetoxy)-methyl; (1H-flavor-2-yl)methyl; (1Η_σ than sal-3-yl)methyl; (ι-methyl-IH-indol-3-yl)indenyl; (1-methyl)methyl; (2-(amine-based) Ethylamino)methylidene; (2-(aminomethyl) 吼3_yl)methyl; (2-(carboxy)ethylamino)carbonyl fluorenyl; (2-(two) Methylamino)ethylamino)carbonylcarbonyl; (2-(hydroxy)ethylamino)carbonylmethyl; (2-(methylamino)ethylamino)carbonylmethyl; (2- (Ν-methyl(t-butoxycarbonyl)-amino)ethylamino)carbonylcarbonyl; (2-oxypiperidin-3-yl)indenyl; (3_(dimethyl-15-amino) ) propylamino)methylidene; (3-(trans)ethylamino)weiylmercapto-(3-(di-dibutoxy-ylamino)propylamino) (4_(Aminomethyl) σ than bit-2-yl fluorenyl; (5-(Amino A) π π π 曱 曱 曱 ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; Ethylamino-based pyridin-2-yl)methyl; (6-(3-aminopropylamino) 20 吼11-decyl) fluorenyl, (6-(amino fluorenyl) guan-2-yl曱 ;; (6_(via fluorenyl) acridine-2-yl)methyl; (6-bromoacridin-2-yl)methyl; (fluorenylsulfonylamino) # 曱基曱基' (0 唆-2-yl)ethylamino; 1-(2-(t-butoxy-phenyl)ethyl)-lH-u-pyrazol-3-ylindenyl; 1-(2 -(t-butoxycarbonylamino)ethyl)-1Η"biazole_5_ylindenyl; l(aminocarbonyl)_2_(amino)_乙小59 200823188 基,ι·(amino group Base; μ(amino)-propyl; (amino group)_4_(amino)_-butyl, h(aminocarbonyl(benzyloxycarbonylamino)-pentyl; μ(amino group a few groups) _5_(amino)-pentyl; 1-(aminocarbonyl)eth-1-yl; 1_(indolyl)·2-(amino)·ethyl small group; 1_(dimethylamino group Carbonyl)_2_(amino)-ethyl-5 base; h(hydroxy)-2_(aminocarbonylmethylamino)ethyl small group; 1-(hydroxy)-2-(ethoxycarbonylmethylamino) B_丨_yl; 1_(hydroxy)_2_bubiridin-2-ylmethylamino)ethyl-1-yl;-(methoxycarbonyl>2_(aminophenyl)-yl; 1-(A Oxycarbonyl)-2-(t-butoxycarbonylamino)-ethyl 4-yl; 1-(decyloxy)ethyl-1-yl; 1-(decylaminocarbonyl)_2-(amino >B-; [_yl (2 10 occ); Ηmethylaminocarbonyl) ethyl small group; 1-aminocarbonyl-2-hydroxy-ethyl small group; fluorenyl-nonyloxycarbonyl hydroxyethyl small group ; 2 —( 2 —aminoethoxy)ethyl; 2 —(2-aminoethyl)-σ-pyridin-6-ylmethyl; 2-(2-aminoethylamino)ethyl; 2-(3-fluorophenyl)ethyl; 2-(3-decyloxycarbonyl)ethyl; 2-(6-(aminoindolyl)acridin-2-yl)ethyl; 2_(acetamidine Ethylamino)ethyl; 2-(amino)ethyl; 2-(amine 15-ylcarbonyl)-2-(ethionylamino)-eth-1-yl; 2-(aminocarbonyl)-2 -(amino)-ethyl-1-yl; 2-(aminocarbonyl)ethyl; 2-(aminomethyl)acridin-5-ylmethyl; 2-(carboxy)_2-(amino) -ethyl-1-yl; 2-(didecylamino)ethyl; 2-(didecylaminocarbonyl)-2-(amino)-eth-1-yl; 2-(ethoxycarbonyl) Ethyl; 2-(decyloxycarbonyl)-2-(ethinylamine) -ethyl-1-yl; 2-(decyloxycarbonyl)-2-(amine 2 fluorenyl)-eth-1-yl; 2-(methoxycarbonylamino)ethyl; 2-(methyl Amino)ethyl; 2-(decylaminocarbonyl)-2-(ethionylamino)-eth-1-yl; 2-(decylaminocarbonyl)-2-(amino)-B -1-yl; 2-(decylsulfonylamino)ethyl; 2-(decyloxycarbonyl)-2-(amino)-eth-1-yl; 2-(N-(third butoxy Carbonyl)-N-(indenyl)-amino)ethyl; 2-(pipedino-1-yl)ethyl; 2-(indol-2-yl)ethyl; 2-(. Than 200823188 bite 2-ethyl) ethyl 2-pyridin-3-yl)ethyl; 2-(t-butoxyaminoamino) acridine-3-ylindenyl; (t-butoxycarbonylaminomethyl) acridine-6-ylmethyl; 2-(trifluoromethyl)-pyridin-6-ylindenyl; 2-aminopyridine-3-ylmethyl; 2-aminopyridin-5-ylmethyl; 2-chloropyridin-5-ylindenyl; 2- 5 cyanopyridine-5-ylindenyl; 2-hydroxy-3-amino-propan-1-yl 2-hydroxyethyl; 2-decyloxyethyl-1-yl; 2-methoxypyridin-3-ylindenyl; 2-decyloxypyridin-5-ylindenyl; 2-mercaptoacridine 3-ylindenyl; 2-mercaptopyridine-5-ylindenyl; 2·methyl. Ratio of 6-ylindenyl; 3-(2-aminoethyl)cyclohexyl)indenyl; 3-(4-indolylpiperidin-1-yl)propyl; 3-(amino)-3 -(decylaminocarbonyl)propan-1-yl; 10 3-(aminocarbonyl)propyl; 3-(aminoindenyl)phenylhydrazine; 3-(aminomercapto)pyridin-2- 3-mercapto-propyl; 3-(methoxyl-yl)propyl; 3-(indolylamino)propyl; 3-(trifluoromethyl)-pyridin-2-ylindenyl; 3,4-di Fluorobenzoyl; 3-aminomercaptoacridin-4-ylindenyl; 3-aminopropyl; 3-aminoindenylcyclopentyl; 3-carboxypropyl; 3-hydroxypropyl; -methoxypropyl; 4-(aminoalkyl)- 15 pyridin-2-ylindenyl; 4-(N,N-didecylamino)pyridin-3-ylindenyl; 4_(third Butoxycarbonylamino)-morpholinylfluorenyl; 4-aminobutyl; 4-aminomercaptoacridin-3-ylindenyl; 4-cyanobenzyl; 4-fluorophenylmethyl 4-mercaptoaminopyridinium-3-ylsulfonyl; 4-methylphenylhydrazino; 4-morpholinylu-pyridin-3-ylindenyl; 4-piperidinylpyridin-3-ylindole 5-((bis(dimethylamino)decylamino)phosphonium 20-yl)pyridin-3-ylindenyl; 5-(aminoindenyl)pyridin-2-ylindenyl; 5-( Aminoalkyl)pyridin-3-ylindenyl; 5-(hydroxyindenyl)pyridin-3-ylindenyl; 5-(t-butoxymethylaminomethyl)-^biter-2-ylindenyl; 5-(trifluoromethyl)-hydrazine Indole-2-ylindenyl; 5-aminopentyl; 5-amino-2-poly-2-ylmethyl; 6-((bis(didecylamino))alkyl) Acridine 2_yl) fluorenyl; 6-(4-ethyl fluorenyl 200823188 σ chen 11 well -1- basal than bit-3-ylmethyl); 6-(aminomethyl) u ratio biting winter Base group; 6-month-female hexyl group, amino group fluorenyl group; methyl group; cyclopropylmethyl group; dimercaptoaminocarbonylmethyl group; isopropyl group; iso-4-azole-5-yl group Base; oxime oxycarbonylmethyl; methyl; decylaminocarbonylmethyl; carbazole-2-ylmethyl; piperidine _4_ fluorenyl, prop-2-yl-1-yl; π ratio Well-2-ylmethyl; π-mercaptomethyl; dent-2-ylmethyl oxide; η ratio -3-ylmethyl; π-pyridylmethyl-hydrazine-oxide; pyridine_4曱 曱 ;; thiophen-2-ylmethyl; and thiophene _3 yl fluorenyl. In a particular embodiment of the compound of Formula IV, R2 is pyridin-3-ylindenyl. In a particular embodiment of the compound of Formula IV, R5 is selected from the group consisting of hydrogen and lower alkyl. In a particular embodiment of the compound of Formula IV, R5 is selected from the group consisting of guanidine and sulfhydryl. In a particular embodiment of the compound of Formula IV, R5 is hydrogen. 15 20 , 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。 。. In the specific solid towel of the formula Iv ^, from the shape of the back 2 () is selected from 1, 2, and 3 and the R20 is selected from the highest level of visual 〜 ~ u ^ ^ brother to be replaced A heterocycloalkyl group and optionally a substituted cycloalkyl group. In a specific embodiment of the τ 2 and 21 ¥ compound, Z3 is selected from (tetrahydrofuranyl)methyl, - Cyclohexylf group, 2_(1,3-dioxolan-2-yl)ethane, 2-(11-hydroxyl-based, arsenyl (tetra)-yl), 2-= - 乳基派咬基)Ethyl, 2_(2_oxylate bite small base) hexyl 2-%<,hex-1-enylethyl, 2_cyclohexylethyl and 2_line Base ethyl. In a particular embodiment of the compound of formula IV, r1 is selected from the group consisting of nitrogen and, if desired, a substituted low-wei group. In a particular embodiment of the compound of Formula IV, 62 200823188 R1 is selected from the group consisting of hydrogen and lower alkyl. In a particular embodiment of the compound of Formula IV, R1 is selected from the group consisting of hydrazine and hydrazine. In a particular embodiment of the compound of Formula IV, R1 is hydrogen. • In a particular embodiment of the compound of Formula IV, R3 is selected from the group consisting of argon and, if desired, a substituted lower alkyl group. In a particular embodiment of the compound of Formula IV, the Han 3 is selected from the group consisting of hydrazine and lower alkyl. In a particular embodiment of the compound of Formula IV, R3 is selected from the group consisting of nitrogen and sulfhydryl. In a particular embodiment of the compound of Formula IV, Han 3 is 氲. In a particular embodiment of the compound of Formula IV, R4 is selected from the group consisting of hydrogen, cyano, 10 halo, alkoxy, optionally substituted amino and optionally substituted alkyl. In a particular embodiment of the compound of Formula IV, R4 is selected from the group consisting of hydrogen, nitrogen, chlorine, bromine, fluorine, azide, optionally substituted alkylaminocarbonyl, and optionally substituted sulfhydryl. In a particular embodiment of the compound of Formula IV, the R system is derived from hydrazine, fL radical, gas, bromine, azide, tr. _3 _ mercaptoalkylamine 15 # 厌 base, aminomethyl and preparation Methyl group. In a particular embodiment of the compound of Formula IV, R4 is hydrogen. In a particular embodiment, the compound of formula I is selected from the group consisting of N-methyl(6-phenyl-2-[(2-phenylethyl)amino)]pyridyl)]carbamamine {6- Phenyl-2-[[2-phenylethyl)amino](3_π-pyridylpropan-2-enylindole 20 decylamine 1 {6-phenyl-2-[(2-phenylethyl)amine Base](3_t定基)}|(3"pyridylmethyl)formic acid amine N-(mercaptoethyl){6_phenyl_2_[(2_(2_„bito)ethyl)amino] ο比咬63 200823188 {6-Phenyl-2-[(2-(2-pyridyl)ethyl)amino](3_pyridyl)}_ν_(2^λ-pyridylmethyl)carhamamine 5 10 15 20 {6-Phenyl-2-[(2-(2-pyridyl)ethyl)amino](3_pyridyl)}_N_(4_t-mercaptomethyl)carboxylic acid amine (2_{[ 2_(3,methylphenyl)ethyl]aminopyabphenyl(3-acridinyl))_N_prop-2-enylcarboxamide {6-phenyl-2-[(2·( 2_pyridyl)ethyl)amino](3_pyridyl)}_(4_pyridyl)methyl- Ν-methyl (2_{[2♦methylphenyl)ethyl]aminophenyl (3-Aridinyl))carzamide-(oxapentamethoxymethyl)(6-phenyl_2κ2_π than dimethyl)ethyl](3-pyridyl)}carbamamine N- [((2S)oxapentan-2-yl)methyl](6-phenyl-2-[(2-(2-, pyridine) Ethyl)amino](3-pyridyl)}carbamamine {stupyl 2 [(2-(2-t-decyl)ethyl)amino)] (ρ 咬 咬 咬 甲基 甲基) = Alkenyl: ethethyl)amino]-6 phenyl (3, yl) porphyrin - (6-phenyl 2 -[(3-phenylpropyl)amino] ο than bite)}_Ν_( 3_π ratio basement) amide-(1,3·Μ_2-ylmethyl){6_phenyl_2_[(2_(2_^ethyl)amino](3_pyridyl)} formazan Amine sulphate-(salt-2-ylmethyl){6_phenyl_2_[(2_(2_吼σ定)ethyl)amino](3_pyridyl)}carbamamine=[( (3SM-ethylidene D ratio slightly 唆_3_yl) methyl]{6_phenyl_2|indenyl)ethyl)amino](3-pyridyl)}carbamamine {6- Phenyl-2-[(2-(2"-indolyl)ethyl)amino](n-decyl) “"比比64 200823188 pyridine" formazan, {•2-[(3-methyl) Amino]-6-phenylindole ratio, fixed base)}|(3′′ 嚏 ))methalin {2-[(2-cyclohexylethyl)amino]-6-phenyl (3- π than bite base)}_Ν_(3_σ than bite Wu methyl) formic acid amine Ν-{[1-(methylsulfonyl)(3-piperidinyl)]methyl hydrazine {6_phenyl_2_[(2_( 2-(pyridyl)ethyl)amino](3-acridinyl)}carbamamine 2-(amino fluorenyl) brigade bite 6-phenyl_2-[ (2_(2"-pyridyl)ethyl)amino κ3_pyridyl)one 1 Nmw-phenyl-2_[(2〇pyridyl)ethyl)amino]_3_npyridyl}yl)-2 -piperidinyl]methyl}acetamide 2-{[(methylsulfonyl)amino]hydrazino}piperidinylphenylphenyl-2_[(2<2_^pyridyl)ethyl)amine Base] (3-° ratio ° base) 酉 15 N-[(l-曱基口比嗤_5_yl)methyl]{卜phenyl_2_[(2_(2"-pyridyl)ethylamine (3-pyridyl)}carbammine {6-phenyl-2-[(2-(2-pyridyl)ethyl)amino](3_pyridyl)}_N_(pyrazole-3 -based fluorene amine N-(isosazol-5-ylindenyl){6•phenyl_2_[(2_(2-pyridyl)ethyl)amino](3-acridinyl) }Metformin N-phenylhydrazino {6_phenyl-2-[(2-(2-t-decyl)ethyl)amino] (3" pyridine

甲醯胺 i W N-曱基{6-苯基-2-[(2-(2-吡啶基）乙基）胺基](3_吡啶基 醯胺 N-[((3R)吡咯啶_3_基）甲基]{6_苯基_2_[(2_(2_吡啶基）乙基） 65 20 200823188 ， 胺基](3-吡啶基)}甲醯胺 {6_苯基-·2_[(2-苯基乙基)胺基K3』比啶基士凡叫2』比唆基) 乙基）甲醯胺 1 {卜苯基_2_[(2·苯基乙基)胺基Κ3_π比啶基定基) 5 乙基）曱醯胺 1 N-曱基-2-({6-苯基-2-[(2-苯基乙基)胺基](3-吡啶基)}羰基 胺基）乙醯胺 & N，N-二曱基-2-({6_苯基j_[(2_苯基乙基)胺基](3_吡啶基》 羰基胺基）乙醯胺 〇 N-(胺甲醯基甲基）{6_苯基_2_[(2_苯基乙基）胺基](3_吡啶 基)}曱醯胺 (2_{[2-(2_氧基哌啶基）乙基]胺基丨冬苯基（3_ ^比咬 基))以-(3-吼咬基甲基）甲醯胺 (2-{[2-(1-曱基（4-哌啶基））乙基]胺基卜6_苯基（3_ π比啶 5 基))-Ν_(3-吼啶基甲基）甲醯胺 {6-苯基-2-[(2-(2-噻吩基）乙基）胺基](3_吡啶基）}_队(3_吡 啶基曱基）曱醯胺 (2-{[2-(1-曱基咪唑_4_基）乙基]胺基}_6_苯基（3_吡咬 基))-Ν_(3-吼啶基曱基）曱醯胺 0 {2-[(2-(2-呋喃基）乙基）胺基]-6_苯基(3_d比啶 啶基曱基）曱醯胺 （ {2-[(氧雜戊環_2_基曱基）胺基]_6_苯基(3_u比啶基 吡啶基甲基）甲醯胺 {2-[(2_(1，3_二氧戊環_2_基）乙基）胺基]冬苯基（3_ ^比啶 66 200823188 基)}-N-(3-吼啶基甲基）甲醯胺 {2_[(3_味嗤基丙基)胺基]_6·苯基(3_吡啶基)}_Ν_(3_σ比咬基 • 甲基）甲醯胺 & {2-[(2-嗎啉-4-基乙基)胺基]-6-苯基(3_σ比啶基比啶 5 基甲基）甲醯胺 {6-苯基-2-[(2-苯氧基乙基)胺基](3_吡啶基）}_N_(3_吼啶基 甲基）甲醯胺 m(2_(2H-苯并[3,4.，3·間二氧雜環戊稀各基）乙基）胺 基]-6-苯基(3-口比啶基)}_Ν-(3·吼啶基甲基）甲醯胺 1〇 N_[((3S)吼咯啶-3-基）曱基]{6-苯基比啶基）乙基） 胺基](3-吡啶基)}曱醯胺 [6_苯基_2-(丙基胺基)(3_吼啶基)]_Ν_(3_吡啶基曱基）曱醯 胺 2-({6-苯基-2-[(2-苯基乙基）胺基;|_3_,比啶基丨羰基胺基）乙 15 酸甲酯 =[((3R)-1-乙醯基吡咯啶基）甲基]{6_笨基_2_[(2_(2_吡 咬基）乙基)胺基](3_吼啶基》甲醯胺 1 [((2s)-i-乙醯基吡咯啶士基）曱基](6_笨基冬[叫2-咕 σ疋基）乙基)胺基](3_σ比咬基）}甲酿胺 2〇 {6_苯基_2_[苯甲基胺基](3_0Jtu定基定基曱基）甲 酸胺 N-[(l-乙酸基(3_痕唆基))曱基]{6_苯基比咬基）乙 基)胺基](3-吡啶基）}甲醯胺 {6_苯基-2-[(2_(2-吼啶基）乙基）胺基](3_吡啶基)}-N-(3_噻 67 200823188 吩基曱基）曱醯胺 • {6-苯基-2-1(2-(2-11比唆基).乙基）胺基](3-°比淀基）}_N-(2-^ 吩基曱基）甲醯胺 (2-{[2-(2-氧基咪唑咬基）乙基]胺基卜6-苯基（3-吼啶 基))-Ν-(3-吼啶基曱基）曱醯胺 (2-{〇(2-氧基。比咯啶基）乙基]胺基}_6_苯基（3-咐啶 基))-Ν-(3-吼啶基曱基）曱醯胺 {2-[(2_π米唾-4-基乙基)胺基]-6-苯基(3-0比。定基口定 基曱基）甲醯胺 (2-{[(經基環己基）曱基]胺基}_6_苯基(3-吼咬基))-Ν-(3-σΛ 啶基曱基）甲醯胺 (2-{[2_(3,5-二曱基吼唑-4-基）乙基]胺基}-6-苯基（3_吼啶 基))_N_(3-u比啶基曱基）甲醯胺 0{[2_(3,5-二曱基π比唑基）乙基]胺基卜6_苯基（3_σ比啶 基))-Ν-(3-吡啶基曱基）甲醯胺 (2_{[2-(2-氯苯基）乙基]胺基}_6_(2_氰基苯基）(3_ π比啶 基基甲基）曱醯胺 (6_(2_氰基苯基）-2- {[2_(2_甲基苯基）乙基]胺基} 〇比啶 基))-Ν-(3-吼啶基曱基）曱醯胺 (6-(2-氰基苯基）_2_{[2_(2-氟苯基）乙基]胺基丨(3_ σ比啶 基))-N_(3-u比啶基甲基）甲醯胺 (6-(2-氰基苯基{[2-(2-氰基苯基）乙基]胺基} (3_。比啶 基))-Ν_(3_σ比咬基曱基）曱醯胺 {6-(2-氣基苯基）_2_[(2-(2_噻吩基）乙基）胺基](3_ σ比啶 68 200823188 基)}-Ν·(3-吼啶基曱基）曱醯胺 {6-(2-氰基苯基）·2-[(2-(2-呋喃_基）乙基）胺基](3-吼啶 • 基)}-Ν-(3-吡啶基曱基）甲醯胺 - {6_苯基-2-[(2-(2-11比1[2定基）乙基）胺基](3-17比17定基）}-1^-丙-2- 5 烯基甲醯胺 (2-{[2-(3-氟（2-吼啶基））乙基]胺基}-6-苯基（3-吼啶 基))-Ν-(3-吼啶基曱基）曱醯胺 N-[(l-曱基啦唑-3-基）甲基]{6-苯基-2-[(2-(2-吼啶基）乙基) 胺基](3-吡啶基)}甲醯胺 ίο N-[(l-乙醯基(4-哌啶基)）曱基]{6-苯基-2-[(2-(2-吼啶基）乙 基)胺基](3-吼啶基)}甲醯胺 2-[( {6 -苯基-2-[(2-(2-吼σ定基）乙基）胺基]比唆基}搂基胺 基）甲基]嗎啉-4-羧酸第三丁酯 {6_苯基-2-[(2-(2-σ比σ定基）乙基）胺基](3 -。比σ定基）}-Ν-(2 -ϋ比 15 啶基）甲醯胺 (2-{[2-(3-曱基苯基）乙基]胺基}-6-苯基(3-吨啶基))-Ν-(3- 吡啶基甲基）甲醯胺 (6-(2-氣基苯基）-2- {[2-(2-經基苯基）乙基]胺基} (3- 0比唆 基))-N-(3-吼啶基曱基）曱醯胺 2〇 N-{[2-(胺基曱基)(3-吼啶基)]甲基}{6-咐唑-4-基-2-[(2-(2- 吡啶基）乙基)胺基](3-吡啶基）}曱醯胺 N-{(lR)-2-[(5-氟-2-{[2-(3-氟苯基)-2-羥基乙基]胺基}-6_ 口比唑-4-基(3-吼啶基))羰基胺基]-異丙基}-2-[(第三丁氧基) 羰基胺基]乙醯胺 69 200823188 {5_氟-6-吡唑-4-基-2-[(2-吡唑乙基）胺基](3-吡啶 基)}-N-(3-吡啶基甲基）曱醯胺. . • N-[(lR)-2-({5-氟-6-口比唑-4-基-2_[(2-吼唑基乙基）胺基](3- . 吼17定基)}幾基胺基)-異丙基]-2-胺基乙酸胺 5 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-Ν-{[6-(三氟甲基)(2-吼啶基)]甲基}曱醯胺 (6-(2-氣基苯基）-2_{[2-(3-氣苯基）乙基]胺基}(3- °比ϋ定 基))-Ν-{[5-(三氟甲基)(2^比啶基)]甲基}曱醯胺 (6-(2-鼠基苯基）-2-{[2-(3-氣苯基）乙基]胺基）(3- °比σ定 ίο 基))-Ν-{[3-(三氟曱基)(2-吼啶基)]甲基}曱醯胺 N-[(6-氯(3-吼啶基)）曱基](6-(2-氰基苯基)-2-{[2-(3-氟苯基) 乙基]胺基}(3-吡啶基)）曱醯胺 (6-(2-氰基(3-噻吩基))-2-{[2-(3-氟苯基）乙基]胺基}(3-口比 啶基))-N-(3-吡啶基曱基）甲醯胺 15 (2E)-3-(2-{[2-(3-氣苯基）乙基]胺基}-6-苯基（3- σ比^定 基))-Ν-曱基丙-2-烯醯胺 (6-(2-鼠基苯基）-2-{[2-(3-氣苯基）乙基]胺基}(3_吼ϋ定 基))-Ν-{[6-(甲基胺基)(3-吼啶基)]曱基}曱醯胺Ν-{[6-(二 曱基胺基)(3-吼啶基)]曱基}(6-(2-氰基苯基)-2-{[2-(3-氟苯 2〇 基）乙基]胺基}(3-咐啶基)）曱醯胺（2-{[2-(3-氟苯基）乙基] 胺基}-4-(羥基曱基)-6-苯基(3-吼啶基))-Ν-(3-吼啶基曱基） 甲醯胺 Ν-[(5-胺基(2·-比啶基)）曱基](6-(2-氰基苯基)-2-{[2-(3-氟苯 基）乙基]胺基}(3-吼啶基)）曱醯胺 70 200823188 (2-{〇(3-氟苯基）乙基;I胺基卜Η經基曱基苯基比口定 • 基))-N_(3-吡啶基曱基)甲醯胺 . (2-{[2_(3-氟苯基）乙基]胺基苯基-5-[N-(3-吼啶基甲基) ， 胺甲醯基](弘吡啶基))-N-(3-吡啶基曱基）甲醯胺（5_(2_重 5 氮-2_氮雜乙烯基)-2_{[2-(3-氟苯基）乙基]胺基}_6_笨基(3_ 吼啶基))_N_(34啶基曱基）甲醯胺 (5_(胺基甲基)_2_{[2_(3_氟苯基）乙基]胺基}_6_苯基^吼啶 基))_Ν-(3-ϋ比咬基曱基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基卜6_〇_甲基吡唑_4_基)(3_吡啶 ίο 基))-Ν-(3-吡啶基甲基）曱醯胺 Ν-({6-[3,3-雙（二甲基胺基)_2_氮雜丙_2_烯基](2_σ比啶基）} 甲基)(6-(2-氰基苯基)-2-{[2-(3_氟苯基）乙基]胺基}(3:咬 基)）甲醯胺 Ν-[(6-{[(第三丁氧基）羰基胺基]曱基}(2_σ比啶基））曱 15 基](6-(2_氰基苯基）_2—{[2-(3_氟苯基）乙基]胺基}(3_吡啶 基)）曱醯胺 Ν-{[4-(胺基甲基）(3_ σ比啶基）]甲基}(6_(2_氰基苯 基）-2-{[2-(3-氟苯基）乙基]胺基}(3_吼啶基））甲醯胺 Ν-{[3-(胺基甲基）(4_ σ比啶基）]甲基}(6_(2_氰基苯 '° 基氟苯基）乙基]胺基}(3-吼咬基)）曱酿胺 (5溴2-{[2-(3_氟本基）乙基]胺基卜6_ π比唾_4_基（3_吼咬 基))-Ν-(3_吼啶基甲基）曱醯胺 (5-溴-2-{[2-(3-氟苯基）乙基]胺基}_6_(1•甲基^比唑_4_基)(3_ 吡啶基))-队(3_吡啶基甲基）曱醯胺 71 200823188 (6-(5 -鼠基ϋ比嗤-4-基)-2- {[2-(3 -氣苯基）乙基]胺基}(3-°比σ定 -基))-Ν-(3-吼啶基曱基）甲醯胺 (5-氣基-2-{[2-(3-鼠苯基）乙基]胺基}-6-(1-甲基11比嗤-4-基)(3-吼啶基))-Ν-(3-吼啶基曱基）甲醯胺 5 (2-{[2-(3-氟苯基）乙基]胺基}-6-吼唑-3-基（3-吼啶 基))-Ν-(3-吼啶基甲基）曱醯胺 (6-(3氣基-1-曱基ϋ比唾-4-基）_2- {[2-(3-氟苯基）乙基]胺 基}(3-吡啶基))-N-(3_吡啶基曱基）曱醯胺 (6-(5-氰基-1 -甲基吼唑-4-基）-2- {[2-(3-氟苯基）乙基]胺 ίο 基}(3-吡啶基))-N-(3-吡啶基甲基）曱醯胺 . 2-[(2_{[2-(3-氣苯基）乙基]胺基}-6-σ比α坐-4-基（3-°比σ定基)) 羰基胺基]-Ν-甲基乙醯胺 2-[(2-{[2-(3-氟苯基）乙基]胺基甲基吼唑-4-基)(3-口比 啶基))羰基胺基]-N-曱基乙醯胺 15 (5-氣-2-{[2-(3-氣苯基）乙基]胺基}-6_(1-曱基11比17坐-4-基)(3_ 吡啶基))-N-(3 -吡啶基甲基）曱醯胺 N-{[6-(胺基甲基)(2-吼啶基)]曱基)(5-溴-2-{[2-(3-氟苯基) 乙基]胺基}-6-苯基(3-吼啶基)）甲醯胺 N-[(l- {2-[(第三丁氧基）羰基胺基]乙基}吡唑-3_基）曱 2〇 基](6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基)）曱醯胺 N-[(l-{2-[(第三丁氧基）羰基胺基]乙基}吼唑-5-基）甲 基](6-(2-氣基苯基）-2-{[2-(3 -氣苯基）乙基]胺基}(3-吼σ定 基)）曱醯胺 72 200823188 N-{[1_(2-胺基乙基）吼唑_3_基]甲基}(6_(2-氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3- π比咬基））甲酿胺 Ν-{[1-(2-胺基乙基）吨唑-5-基]曱基）(6-(2-氰基苯 基）-2-{[2-(3-氟苯基）乙基]胺基}(3- π比嚏基））曱酿胺 N_{[6-(胺基甲基)(2_吼啶基)]曱基}(2_{[2_(3_氟苯基）乙基] 胺基卜6-(1-甲基口比唑-4-基）(3-吼啶基)）曱醯胺队{[6-(胺 基甲基)(2·-比啶基)]甲基}(2-{[2-(3_氟苯基）乙基]胺基}_6_ 吡唑-4-基(3-吡啶基)）甲醯胺 N-{[6_(胺基甲基)(2_吼啶基)]甲基}(5，_2_{[2_(3_氣苯基) 乙基]胺基}-6-(1-甲基吼唾-4_基）(3-吼咬基））甲酿胺 N_[((2R)_5-氧基π比咯啶_2基）甲基](6_(2_氰基苯 基）-2_{[2-(3-氟苯基）乙基]胺基}(3_ ο比σ定基））曱酿胺 N_[((2S)_5_氧基π比咯啶_2_基）甲基](6-(2_氰基苯 基）-2-{[2-(3-氟苯基）乙基]胺基}(3_吼啶基））甲醯胺 N- {3-[(5S)-5-(2-重氮-2-氮雜乙烯基）-2-氧基吼略啶]丙 基}(6-(2-氰基苯基）·2-{[2-(3-氟苯基）乙基]胺基}(3 j比啶 基)）甲醯胺 N-[((2S)-l-{3-[(第三丁氧基）羰基胺基]丙基卜：氧基。比咯 啶-2-基）曱基](6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-吡啶基)）甲醯胺 N-{[(2S)-l-(2-胺基乙基>5-氧基吡咯啶_2_基]甲基}(6_(2_ 氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基比啶基》甲醯胺 N-{[(2S)-l-(3-胺基丙基)-5-氧基π比咯啶-2_基]甲基}(6_(2_ 氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3_吼啶基》甲醯胺 73 200823188 ，其★ ·2·氧基蝴丙基}(6·(2_氰基 本基Η-ί[2-(3-氟本基）乙基]胺基}(3_吼咬基 闕⑽小㈣紅基)錢細贿基跑^ 氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3髮基))甲酿胺 N- {3-[(5R)-5-(2-重氮_2_氮雜乙烯基)_2_氧基鱗咬]丙 基}(6-(2_氰基苯基氟苯基）乙基]胺 基)）甲醯胺 N- {3-((5R)’5-(胺基甲基)_2_氧基吼略唆]丙基}(6必氛基 苯基)·2_{[2-(3-敦苯基）乙基]胺基}(3♦定基》甲酿胺 Ν- {2_[(5S)·5-(胺基甲基)_2_氧基鱗。定]乙基丨(6々乳基 苯基)_2-{[2-(3-就苯基）乙基]胺基}(3_n比咬基))甲辟胺 N-叫㈣-5-(胺基甲基)_2_氧基吼略咬]乙基^(2_氛基 苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3“比咬基)）甲酿胺 15 20 州⑽士氧基π比略咬_2_基）甲基](2|(3_氣苯基）乙基] 胺基}-6-吡唑-3-基(3-吡啶基)）甲醯胺 基)甲基](2鄉氟苯邮 本基)-2-{[2-(3-氟苯基）乙基]胺基}(3 -2-基甲基）甲_ ^基肺十比洛咬 版基}-6-吼嗤+基(3-吡啶基)）甲醯胺 Nim(第三丁氧基）麟胺基]乙基 ί=胺氰基__{[2_(3_氣细乙基]胺細二比咬 74 200823188 N-[(l - {3-[(弟二丁氧基）幾基胺基]丙基}σ比略咬基）甲 基](6-(2-氰基笨基)-2-{[2-(3-氟苯基）乙基]胺基}(3_吡啶 ^ 基)）甲醯胺 Ν-{[1-(2-胺基乙基）π比咯啶_2_基]甲基}(6_(2_氰基苯 5 基）-2-{[2-(3β氟苯基）乙基]胺基}(3-吼啶基））甲醯胺 Ν-{[1-(3•胺基丙基）口比咯啶_2_基]甲基）(6_(2-氰基苯 基)-2_{[2_(3-氟苯基）乙基]胺基}(3_如定基)）甲醯胺 2-({(2S)-2-胺基-3-[(6_(2-氰基苯基)-2-{[2♦說苯基）乙基] 胺基}(3-吼咬基))幾基胺基]丙基}胺基）乙酸甲酯 ίο 2-({(2S)-2-月女基-3-[(2-{[2-(3-氟苯基）乙基]胺基卜6_(ι_甲 基吼唑_4_基)(3』比。定基))幾基胺基]丙基）胺基）乙酸甲酯 N-[((2S)-6-氧基哌基）甲基](2_{[2_(3_氟苯基）乙基]胺 基}-6-吼唾_4_基(3』比咬基)）曱醯胺 N-[((2S)-6-氧基哌畊_2_基）甲基](6_(2_氰基苯基)_2_{[2_(3_ 5 氟苯基）乙基]胺基Κ3-σ比啶基)）甲醯胺N-[((2R)-4-{3-[(第 二丁氧基)羰基胺基]丙基卜6-氧基哌畊基）甲基](6-(2_氰 基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3_σ比啶基)）甲醯胺 N-[((2S)_6-氧基哌畊_2_基）甲基](2_{[2_(3_氟苯基）乙基]胺 基}冬(1_甲基吡唑冰基)(3—吡啶基)）甲醯胺N_[((2S)各氧 3 基哌畊基）甲基](2-{[2-(3-氟苯基）乙基]胺基卜6_吼唑_3_ 基(3-吼啶基)）甲醯胺 N-{[(2R)-4-(3-胺基丙基)_6_氧基哌畊_2_基]甲基）(6_(2_氰基 本基）2 {[2 (3-氟本基）乙基]胺基定基)）甲酿胺 N {[(2R)-4-(3-胺基丙基）_6_氧基旅σ井_2_基]曱 75 200823188 基}(2-{[2-(3-氟苯基）乙基]胺基}_6_(ι_甲基σ比唾_4_基）(3_ -吡啶基)）曱醯胺 N_[((2R)_6_氧基哌啡_2_基）曱基](6_〇氰基苯基)_2_{[2-(3-氟 苯基）乙基]胺基}(3_ϋ比啶基)）甲醯胺N-{[(2S)-4-(2-胺基乙 基)-6-氧基哌畊-2-基]甲基}(6-(2-氰基苯基)_2-{[2-(3-氟苯基) 乙基]胺基}(3_u比啶基)）曱醯胺 N-{[(2S)_4_(3-胺基丙基)-6-氧基哌畊_2_基]曱基}(6_(2_氰基 苯基)_2_{[2_(3-氟苯基）乙基]胺基}(3“比啶基))曱醯胺 N_({(2R)-1_[4-(1，3-二氧苯并[c]唑啉 _2_基）丁 基>5-氧基吼 咯啶_2_基}曱基)(6_(2_氰基苯基)_2_{[2_(3_氟苯基）乙基]胺 基}(3-吡啶基)）曱醯胺 N_({(2R)小[^(^二氧苯并⑷唑啉_2_基）戊基]冬氧基吼 略咬-2_基}甲基)(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-吡啶基)）甲醯胺 (2R)-2-{[(6-(2-氰基苯基)_2-{[2-(3_氟苯基）乙基]胺基}(3- °比ϋ定基））羰基胺基]甲基}氧基吡咯啶羧酸第三丁酯 n_[((2r)吼咯啶基](6_(2_氰基苯基pup—氟苯 基）乙基]胺基}(3-吼啶基)）甲醯胺 N-{[(2R)-1_(4-胺基丁基)_5_氧基吡咯啶_2_基]甲基}(6_(2_ 氰基苯基)-2-{[2_(3-氟苯基）乙基]胺基}(3-吡啶基)）甲醯胺 N-{[(2R)-l-(5-胺基戊基)_5_氧基吼咯啶基]甲基}(6_(2_ 氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3_吼啶基乃甲醯胺 (2_{[2-(3-氟苯基）乙基]胺基卜6· σ比唑_4_基（3_ ^比啶 基))-Ν-(吡唑-3-基甲基）甲醯胺 76 200823188 ({[2(3氟笨基）乙基]胺基甲基吼哇冰基)(3_σ比口定 基))-Ν十比唑-3-基甲基）甲醯胺 (2_{[2-(3-氟苯基）乙基]胺基卜卜吼唑！基。比啶 基))-Ν十比唑-3_基甲基）甲醯胺 N_[((2R>H4-[(第三丁氧基）幾基胺基]丁酸基卜比哈务2_ 基）甲基](卜(2_氰基苯基)_2_{[2♦氟苯基）乙基]胺基}(3_ 吡啶基)）曱醯胺 N-{[(2R)_1_(3_胺基丙醯基）u比咯唆_2_基]甲基》(6_(2_氰基 笨基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吡咬基)）甲醯胺 N-{[1_(3_胺基丙基）吼唑_3_基]甲基}(6_(2_氰基苯 基)-2_{[2_(3_氟苯基）乙基]胺基}(3_吼啶基)）甲醯胺 N-{[l-(3-胺基丙基）吼唑_3_基]甲基}(2_{[2_(3_氟苯基）乙 基]月女基}-6-(1-甲基吼唾冰基）(3_ α比唆基））甲醯胺 Ν-{[1-(3-胺基丙基）吡唑-3 —基]曱基}(2_{[2_(3_氟苯基）乙 基]胺基}_6-σ比嗤_3_基(3_σ比咬基)）甲酸胺 Ν-{〇(3-胺基丙基）吡唑-5-基]甲基}(2-{[2-(3-氟苯基）乙 基]胺基甲基π比唑_4_基χ3_吡啶基》甲醯胺 Ν-{[1-(3-胺基丙基户比唑-5-基]曱基}(2-{[2-(3-氟苯基）乙 基]胺基卜6-吡唑-3_基(3-吡啶基)）曱醯胺 N-[((2R)-l-{2_[(弟二丁氧基)幾基胺基]乙基比略口定_2_基） 曱基](6-(2-氰基苯基)-2_{〇(3-氟苯基）乙基]胺基比咬 基)）甲醯胺 N-[((2R)-1 -{3-[(弟二丁氧基）幾基胺基]丙基}。比略咬_2_基） 曱基](6-(2-氰基苯基)-2-{|>(3-氟苯基）乙基]胺基^3_吼咬 77 200823188 基)）曱醯胺 N-{[(2R)-l-(2-胺基乙基）吡咯啶冬基]甲基}(6_(2_氰基苯 基）-2-{[2-(3-氟苯基）乙基]胺基}(3_ ,比啶基》甲醯胺 N-{[(2R)-l-(3-胺基丙基）π比咯啶-2_基]甲基}(6•(孓氰基苯 5 基氟苯基）乙基]胺基}(3-。比咬基））曱酿胺 N-[(l-{2_[(第三丁氧基）羰基胺基]乙基丨，比唑_3_基）曱 基]〇{[2-(3-氟苯基）乙基]胺基卜比唑_3_基(3_σ比啶基)） 曱醯胺 Ν-{[1-(2-胺基乙基）吡唑_3_基]曱基}(2-{[2_(3_氟苯基）乙 10 基]胺基}«唑-4-基(3_吼咬基))甲醯胺 Ν-{[1_(2-胺基乙基）π比唑_3_基]曱基k2_u2<3_氟苯基）乙 基]胺基}-6-咐唑-3-基(3-n比咬基)）曱醯胺 Ν-{[1-(2_胺基乙基）吼唑冬基]甲基}(2_{[2_(3_氟苯基）乙 基]胺基}-6-吼唑-3-基(3-吼唆基)）甲醯胺 15 N-{l>(2-胺基乙基）ϋ比唑-3-基]曱基}(2-{[2-(3-氟苯基）乙基] 胺基}-6-(1-曱基吡唑-4-基）(3-吡啶基)）曱醯胺Ν-{[1-(2-胺 基乙基）啦唑_5_基]甲基}(2_{[2_(3_氟苯基）乙基]胺基}_6_(1_ 曱基吡唑-4-基）(3-吡啶基））曱醯胺N_{[(2R)_i_(3_胺基丙 基)各氧基哌畊基]甲基}(6-(2-氰基苯基)-2-{[2-(3_氟苯基) 20 乙基]胺基}(3-吡啶基)）曱醯胺 N-{[(2R)-l-(3-胺基丙基）-6-氧基娘务2_基]曱 基}(2_{[2-(3-氟苯基）乙基]胺基卜6-(1-曱基口比口坐-4-基)(3-吡啶基)）甲醯胺 N-{[(2R)_l-(3-胺基丙基）_6-氧基σ底σ井-2-基]甲 78 200823188 基}(2- {[2-(3-氣笨基）乙基]胺基}-6-°比°坐_4_基(3-°比σ定基)) ...曱醯胺. . _ ' N-{[(2R)-l-(3-胺基丙基）-6-氧基哌啡-2-基]曱 基}(2_{[2-(3 -鼠苯基）乙基]胺基}- 6-ϋ比峻-3-基(3-ϋ比σ定基)) 5 曱醢胺 Ν-[((2R)-1-乙醯基吡咯啶-2-基）甲基](6-(2-氰基苯 基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基））曱醯胺 N-{[(2R)-l-(甲基磺醯基）吼咯啶-2-基]曱基}(6-(2-氰基苯 基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基））甲醯胺 ίο N-[((2R)-1-甲基吡咯啶-2·基）曱基](6-(2-氰基苯 . 基）-2-{[2-(3-氟苯基）乙基]胺基}(3 j比啶基））曱醯胺 N-[((2R)-1，1-二甲基吡咯啶-2-基）甲基](6-(2-氰基苯 基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基））甲醯胺 N-[((2R) -1 - {[3-( 1，3 -二氧苯弁[c]11坐琳-2-基）丙基]石黃酷基} 15 σ比咯咬-2-基）甲基](6-(2-氣基苯基)-2-{[2-(3-氣苯基）乙基] 胺基)(3-吼啶基)）曱醯胺 N_({(2R)-l-[(2-胺基乙基)磺醯基]吼咯啶-2-基}甲基)(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基)）曱醯胺 N-({(2R)-l-[(3-胺基丙基)磺醯基]吼咯啶-2-基}甲基)(6-(2-2〇 鼠基苯基)-2-{[2-(3-亂苯基）乙基]胺基} (3-吼σ定基)）曱酿胺 Ν-{[1-(3-胺基丙基）吼唑-3-基]曱基}(2-{[2-(3-氟苯基）乙 基]胺基}-6-吼唑-4-基(3-吼啶基)）甲醯胺 Ν-{[1-(3-胺基丙基）口比。坐-5-基]曱基}(2-{[2-(3-氣苯基）乙 基]胺基}-6-n比唑-4-基(3-吡啶基)）甲醯胺 79 200823188 N-[((2R)-l-{3-[(第三丁氧基）羰基胺基]丙基卜5氧基π比咯 唆_2_基）甲基]〇{[2_(3_氟苯基）乙基;|胺基卜6_(1_甲基吼唑 -4-基)(3-吼咬基)）甲酿胺 N-{[(2R)-1_(3-胺基丙基）-5-氧基π比咯唆_2_基]甲 基}(6-{1_[( —甲基胺基）（二亞甲基）甲基]σ比唾_4_ 基}-2_{[2-(3-氟本基）乙基]胺基}(3_ π比ϋ定基））甲酿胺 N-{[(2R)-l-(3-胺基丙基）_5_氧基π比咯啶_2_基]甲 基}(2_{[2_(3_氟苯基）乙基；]胺基}_6_(1_甲基吼唑冰基)(3_ 吡啶基)）甲醯胺 (2R)_2-{[(2_{[2-(3-氟苯基）乙基]胺基甲基吼口坐-4· 基)(3-σ比唆基))幾基胺基]曱基}。比洛咬叛基第三丁酯 N_{[(2R)_l-(3-胺基丙基）_5_氧基π比咯啶_2_基]曱 基}(2-{〇(3-氟苯基）乙基]胺基}_6』比唑_4_基(3』比啶基)） 甲醯胺 N_[((2R)-l-{3_[(第三丁氧基）幾基胺基]丙基卜5_氧基吼咯 咬-2-基）曱基](6-(2-氰基苯基)-2-{[2_(3-氟苯基）乙基]胺 基}(3-吡啶基)）曱醯胺 N-(2_胺基1甲基丙基氰基苯基)_2_{[2_(3-氟苯基） 乙基]胺基}(3-σ比唆基)）曱酸胺 N-[((2R)。比略咬-2-基）曱基](2_{[2_(3-氟苯基）乙基]胺 基}-6-吼唑-4-基(3-吼啶基)）曱醯胺 N_[((2R)。比咯啶_2_基）曱基](2_{[2-(3_氟苯基）乙基]胺 基}-6-(1-甲基吡唑-4-基)(3-吼啶基)）曱醯胺 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 80 200823188 基）)-N-{2-曱基-2·[(曱基磺醯基）胺基]丙基}曱醯胺 N-[((2R)-l-{2-[(第三丁氧基）羰基胺基]乙醯基}吼咯啶-2-• 基）甲基](2-{[2_(3-氟苯基）乙基]胺基卜6-(1-甲基吼唑-4- 基)(3-吡啶基)）曱醯胺 5 N-[((2R)-l-{3-((第三丁氧基）羰基胺基]丙醯基}吼咯啶-2_ 基）甲基](2-{[2-(3-氟苯基）乙基胺基}-6-(1-甲基吼唑-4-基)(3-吡啶基)）甲醯胺 N-[((2R)_l-{4-[(第三丁氧基）羰基胺基]丁醯基}吼咯啶-2-基）甲基](2-{[2-(3-氟苯基）乙基]胺基曱基吼唑-4-10 基)(3-吡啶基)）甲醯胺 N-{[(2R)-l-(2-胺基乙醯基)吼咯啶-2-基]甲基}(2-{[2-(3-氟 苯基）乙基j胺基甲基吼17坐-4-基)(3-°比°定基)）曱酿胺 N-{[(2R)-l-(3-胺基丙醯基）吼咯啶-2-基]曱基}(2-{[2-(3-氟 苯基）乙基]胺基甲基吼唑-4-基)(3-吼啶基)）甲醯胺 15 N-{[(2R)-l-(4-胺基丁醯基户比咯啶-2-基曱基}(2-{[2-(3-氟 苯基）乙基]胺基}-6-(1-甲基吼唑-4-基)(3-吼啶基)）曱醯胺 N-((2S)-2-胺基丙基)(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙 基]胺基}(3-吼啶基)）甲醯胺 2-[(第三丁氧基）羰基胺基]-N-{2-[(6-(2-氰基苯 2〇 基）-2- {[2-(3 -氣苯基）乙基]胺基} (3-17比σ定基））魏基胺 基]-第三丁基}乙醯胺4-[(第三丁氧基）羰基胺 基]-Ν- {2-[(6-(2-氰基苯基）-2- {[2-(3-氟苯基）乙基]胺 基}(3-吼啶基））羰基胺基]-第三丁基} 丁醯胺N-{(1 S)-2-[(6-(2 -氣基苯基)-2- {[2-(3-氣苯基）乙基]胺基}(3_ 81 200823188 他啶基))羰基胺基]-異丙基}-4-[(第三丁氧基)羰基胺基] 丁醯胺 _ . # . . _ N-[((2R)_l-{5_[(第三丁氧基)羰基胺基]戊醯基}吼咯啶 -2-基）曱基](6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-吡啶基)）曱醯胺 2-胺基_N-{2-[(6-(2-氰基苯基）-2_{[2_(3_氟苯基）乙基]胺 基}(3-吼咬基））幾基胺基]-第三丁基}乙酸胺4-胺基 _N-{2-[(6_(2_氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基}(3_口比 咬基))羰基胺基]-第三丁基} 丁醯胺N_ {[(2R)_丨_(N_曱基胺 曱酿基)吼咯啶_2_基]曱基}(6_(2_氰基苯基)_2][2_(3_就苯基) 乙基]胺基}(3-吼咬基)）甲驢胺 (2R)_2_{[(6_(2-氰基苯基)_2_{[2_(3_氟笨基）乙基]胺基)(3_吡 σ疋基))羰基胺基]甲基}吡咯啶羧酸曱酯 虱基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3_吡啶基))羰基胺 基l·異丙基卜2-胺基乙醯胺N_{(ls)_2_[(6_(2_氰基苯 基)士{[2_(3-氟苯基）乙基]胺基}(3_,比啶基肢基胺基^異 丙基卜4_胺基丁_ N-{[(2R)小(5-胺基戊酿基)吼略咬 基]:基}(6-(2_氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基}(3_ 比口疋基））甲醯胺n_r2S)_2K曱基磺醯基）胺基]丙 ，}(6_(2-氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基}&吼咬 基)）甲酸胺 ⑵^2-{[(6_(2_氰基笨基)_2_{[2_(3_氣苯基）乙基]胺基办 比疋基））羰基胺基]甲基}吡咯啶羧酸2_胺基乙基酯 N咖曱基胺基）丙基](6_(2_氰基苯基)-2_{〇(3_氟苯 82 200823188 基）乙基]胺基}(3-吼啶基)）甲醯胺 N-((2R)-2-胺基丙基)(6-(2-氰i基苯基)-2- {[2-(3 -氣苯基)乙基] ' 胺基}(3-吡啶基)）曱醯胺 . N_[(2R)-2-(曱基胺基）丙基](6-(2•氰基苯基)-2_{[2-(3-氟苯 5 基）乙基]胺基}(3-吼啶基)）曱醯胺N-{(2S)-2-[曱基（甲基 磺蕴基)胺基]丙基}(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基] 胺基}(3-吡啶基)）甲醯胺 N-{(2R)-2-[(甲基磺醯基）胺基]丙基}(6-(2-氰基苯 基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基））甲醯胺 ίο N-{(2R)-2-[曱基（甲基磺醯基）胺基]丙基}(6-(2-氰基苯 基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基））甲醯胺 N-{(lR)-2-[(6-(2-氣基苯基）-2-{[2-(3-氣苯基）乙基]胺 基}(3-吼啶基))羰基胺基]-異丙基}-2-[(第三丁氧基）羰基 胺基]乙醯胺 15 N-{(lR)_2-[(6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺 基}(3·-比啶基))羰基胺基]-異丙基}-2-[(第三丁氧基）羰基 胺基]-Ν-甲基乙醯胺 N-{(lR)-2-[(6-(2-鼠基苯基）-2-{[2-(3-氣苯基）乙基]胺 基}(3-吼啶基))羰基胺基]-異丙基}-4-[(第三丁氧基）羰基 20 胺基]丁醯胺 N-{(lR)-2_[(6-(2•氰基苯基）-2-{[2-(3-氟苯基）乙基]胺 基}(3-吼啶基))羰基胺基]-異丙基}-4-[(第三丁氧基）羰基 胺基]-N-曱基丁醯胺 N-{(lS)-2-[(6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺 83 200823188 基KL定基))幾基胺基]-異丙基卜2_胺基_N•甲基乙醯胺 Ν_«ΐδ)ι[(6·(2_氰基苯基>2_{[2分氟苯基）乙基]胺 土 }(3比σ疋基))幾基胺基]-異丙基卜4_胺基_ν_甲基丁酿胺 N-«m)i[(6-(2_氰基苯基）-2-{[2_(3_氟苯基）乙基]胺 基}(l定基))幾基胺基]-異丙基}_2_胺基乙醯胺 N_«lR)l[(6-(2_氰基苯基>2_{[2_(3_ i苯基）乙基]胺 基}(夂吡啶基))羰基胺基]_異丙基}_4_胺基丁醯胺 R)_2-[(6-(2_氰基苯基）_2_{[2_(3_氟苯基）乙基]胺 基}(3·-比啶基))羰基胺基]_異丙基卜4-胺基_N_甲基丁醯胺 N_{(lR)-2_[(6_(2_氰基苯基从似分氟苯基）乙基]胺 基}(3-吡啶基))羰基胺基]_異丙基}_2_胺基以_甲基乙醯胺 (5-氟-2-{[2-(3_氟苯基）乙基]胺基卜6_(1_甲基σ比唑_4_ 基)(3“比啶基))_Ν_(3_吡啶基甲基）甲醯胺 N_{[(2R)-1_(2-胺基乙醯基）吡咯啶_2_基]甲基}(6_(2_氰基 本基)_2-{[2-(3-氟苯基）乙基]胺基}(3_吼。定基)）曱醯胺 N-{[(2R)-1—(4-胺基丁醯基)吡咯啶-2_基]甲基}(6_(2_氰基 本基)-2-{[2-(3-氟苯基）乙基]胺基}(3_σ比咬基)）曱醯胺 N-{[(2R)-l-(3-胺基丙基)-5-氧基π比略咬_2_基]甲基}(6_(2_ 氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3_σ比啶基)）甲醯胺 (2-{[2-(3-氟本基）乙基]胺基}_6· σ比嗤_4_基（3_吼口定 基))_Ν_(3-σ比ϋ定基甲基）甲酸胺 {6-(3-氯苯基）_2_[(2-(2-吼啶基）乙基）胺基Κ3_ σ比啶 基W-N-P·13比咬基甲基）甲酿胺 {2-[(2-(2-口比咬基）乙基）胺基]各[3一(三氟甲基）苯基](3_吼 84 200823188 啶基）}-N-(3-吡啶基甲基）曱醯胺 {6-[3-(二甲基胺基）苯基]-2-[(2-(2-吼啶基)乙基）胺基](3-’ 吡啶基)}-N-(3-吡啶基曱基）曱醯胺 . {6-(2-鼠苯基）-2-[(2·(2- σ比咬基）乙基）胺基](3-吼ϋ定 5 基)}-Ν-(3-吡啶基甲基）甲醯胺 {6-(2-曱基苯基）-2-[(2-(2-啦啶基）乙基）胺基](3-吼啶 基)}_N-(3-吡啶基甲基）甲醯胺 {6-(2-曱氧基苯基）-2-[(2-(2-吼啶基）乙基）胺基](3-吼啶 基)}-N-(3-吡啶基甲基）甲醯胺 ίο {6-(2_氧基本基）-2-[(2-(2-吼17定基）乙基）胺基](3- °比口定 基）}-N-(3-吡啶基甲基）曱醯胺 {2-[(2-(2-。比咬基）乙基）胺基]_6-(2- 11塞吩基）(3- 0比σ定 基）}-Ν-(3-吡啶基甲基）甲醯胺 {6-(4-乙基苯基）_2-[(2-(2- ^比σ定基）乙基）胺基](3- ^比口定 15 基)}-Ν-(3-吡啶基甲基）甲醯胺 {6-(4-曱基(2-噻吩基))-2-[(2-(2-吼啶基）乙基)胺基](3-吼啶 基）} -N-(3 -吡啶基甲基）曱醯胺 {6-(3-經基笨基）-2-[(2-(2-111比σ定基）乙基）胺基](3-吼口定 基）}-Ν-(3-吡啶基甲基）甲醯胺 20 {6-(3-曱氧基苯基）-2-[(2-(2-吼啶基）乙基）胺基](3-吼啶 基)}-N-(3-吡啶基曱基）曱醯胺 {6-(3-氰基苯基）-2-[(2-(2-。比啶基）乙基）胺基](3-吼啶 基)}-N-(3-吡啶基曱基）甲醯胺 {6-(3,5-二甲基苯基）-2-[(2-(2-吼啶基）乙基）胺基](3-吼啶 85 200823188 基)}-N-(3-吼啶基甲基）曱醯胺 {6-(3,4-二甲基苯基)-2-[(2-(2·-比啶基)乙基)胺基](3_口比啶 • 基)}-N-(3-吼啶基甲基）曱醯胺 • {6-(3_氣苯基）_2-[(2-(2- σ比σ定基）乙基）胺基](3_ 0比π定 5 基)}-Ν-(3-吡啶基甲基）曱醯胺 {6-(3-甲基苯基）-2-[(2-(2_。比啶基）乙基）胺基](3_吼啶 基）}-N-(3-吡啶基甲基）甲醯胺 (2-{[2_(4-氯苯基）乙基]胺基}-6-苯基(3-吨啶基))-Ν·(3-吼 啶基甲基）甲醯胺 ίο {6-(2,4-二曱基苯基）-2-[(2-(2-0比咬基）乙基）胺基](3_啤咬 基）}-Ν-(3-吡啶基曱基）曱醯胺 {6-(2,5-二甲基苯基）-2-[(2-(2-吼啶基）乙基）胺基](3-吼啶 基）}-N-(3-吡啶基曱基）曱醯胺 {6-(4-曱基(3-噻吩基))-2-[(2-(2-u比啶基）乙基)胺基](3-吼啶 15 基)}-N-(3-吡啶基曱基）曱醯胺 (2_{[2-(3-甲氧基苯基）乙基]胺基}-6-苯基（3-吼啶 基))-N-(3 j比啶基曱基）曱醯胺 (2_{[2·(3-氟苯基）乙基]胺基}-6-苯基(3-吼啶基))_N-(3口比 啶基甲基）曱醯胺 2〇 {2-[(2-(2- ϋ比ϋ定基）乙基）胺基]-6-(3- σ塞吩基）(3-。比口定 基)}-Ν-(3-吡啶基曱基）曱醯胺 {6-(2-氯苯基）-2-[(2-(2- ϋ比σ定基）乙基）胺基](3- ϋ比σ定 基)}-Ν-(3-吡啶基曱基）曱醯胺 (2-{[2-(2-氯苯基）乙基]胺基}-6-苯基(3-啦啶基))，-(3-口比 86 200823188 啶基曱基）甲醯胺 (2-{[2-(2-甲氧基笨基）乙基]胺基》_6_笨基（3_ ^比唆 ' 基))-Ν-(3_吼啶基甲基）曱醯胺 (2-{[2-(2·甲基苯基）乙基]胺基}_6_苯基(3_u比啶基))_Ν·(3_ 5 吡啶基甲基）曱醯胺 (2-{[2-(2-氟苯基）乙基]胺基}_6_苯基(3』比π定基))_Ν_(3_σ比 啶基曱基）曱醯胺 (2-{[2-(2,6-二氟苯基）乙基]胺基苯基（3_ σ比咬 基))-N_(3-u比啶基甲基）曱醯胺 1〇 (2-([2-(3,5_二氟苯基）乙基]胺基}_6_苯基（3_ σ比唆 基))-N-(3-u比啶基甲基）曱醯胺 (2-{[2-(3,4·二氟苯基）乙基]胺基}_6_笨基（3_ ^比咬 基))-Ν-(3-吼啶基曱基）曱醯胺 (2-{[2-(2,5-二氟苯基）乙基]胺基}_6•苯基（3_ u比咬 15 基))-N-(3-u比啶基甲基）曱醯胺 [6-苯基-2-Q2-[3-(三氟曱基）苯基]乙基}胺基）(3_ σ比啶 基)]-义(3-吼咬基甲基）甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基}_6_(4-曱基(2-11塞吩基))(3_吼 啶基))-Ν-(3-吼啶基曱基）甲醯胺 20 (2-{[2-(3-氟苯基）乙基]胺基}-6-(3_嘆吩基）(3_ ^比^定 基))-Ν-(3-吼啶基甲基）甲醯胺 (2- {[2_(2 -氣基本基）乙基]胺基} 苯基(3_ 11比u定基))_Ν (3 吡啶基甲基）甲醯胺 (2- {[2-(3-氣基本基）乙基]胺基卜6-苯基(3-!?比u定基))_ν (3 87 200823188 吡啶基曱基）甲醯胺 -(2- {_[2-(4-經基苯基）乙基]胺基}-6-苯基(3-^比ϋ定基))-N-(3_ ' 吡啶基曱基）曱醯胺 (2-{[2-(2-羥基苯基）乙基]胺基}-6-苯基(3·^比啶基))-N-(3_ 5 吡啶基甲基）曱醯胺 (2-{[2-(4-胺基苯基）乙基]胺基卜6-苯基(3-吼啶基))-N-(3- 吡啶基曱基）甲醯胺 3-[2-({6-苯基-3-[N-(3-吼啶基曱基）胺甲醯基]-2-吼啶基} 胺基）乙基]苯甲醯胺 ίο (2- {[2-(3,5-二氟苯基）乙基]胺基} -6-(3-噻吩基）(3•吼啶 基))-N-(3-吼啶基甲基）甲醯胺 (2-{[2-(3,5_二氟苯基）乙基]胺基}-6-(4-曱基(2-噻吩基))(3-吡啶基))-N-(3 -吡啶基曱基）曱醯胺 (2-{[2-(3,5-二氟苯基）乙基]胺基}_6-(2-氰基苯基)(3-吼啶 15 基))-N-(3-吼啶基甲基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(2-噻吩基）(3-吼啶 基定基曱基）甲酿胺 (2- {[2-(3,5-二氟苯基）乙基]胺基} -6_(2-噻吩基）(3-吼啶 基))-N-(3-吡啶基甲基）甲醯胺 2〇 3-[2-({6-本基-3·[Ν-(3-ϋ比ϋ定基曱基）胺曱酿基]-2-口比11定基} 胺基）乙基]苯曱酸甲酯 2-(6-{[2-(3-氟苯基）乙基]胺基}-5-[N-(3_u比啶基曱基)胺曱 醯基]-2-吡啶基）苯甲醯胺 (6-(4-氟苯基）_2-{[2_(3-氟苯基）乙基]胺基}(3_。比啶 88 200823188 基))-N-(3-吡啶基曱基）曱醯胺 3-[2-({6_苯基-3-[N-(3-吼啶基曱基）胺曱醯.基]-2-吼啶基} ' 胺基）乙基]苯曱酸 (6_(2_氯-4-氟苯基)-2·{[2-(3-氟苯基）乙基]胺基}(3_ϋ比咬 5 基))-Ν-(3-吼啶基曱基）曱醯胺 (2-{[2-(3,5-二氟苯基）乙基]胺基}-6-(4_氟苯基）(3·-比啶 基))_N-(3^比啶基曱基）甲醯胺 (2- {[2-(4-氣苯基）乙基]胺基} -6_苯基（3-ϋ比ϋ定基))-N-(3- 口比 啶基曱基）曱醯胺 ίο {6-(2_輕基苯基）-2-[(2-(2-ϋ比0定基）乙基）胺基](3-ϋ比口定 基)}-Ν-(3-吼啶基甲基）甲醯胺{6-(4-羥基苯基)-2-[(2-(2-吼啶基）乙基)胺基](3-吼啶基)}-N-(3-吼啶基甲基）曱醯胺 (6-(2-鼠基-4-亂苯基)-2-{[2-(3 -氣苯基）乙基]胺基}(3-。比唆 基))-N-(3-吼啶基甲基）甲醯胺 15 (6-(2-氯-6-氣苯基）-2- {[2-(3 -氣苯基）乙基]胺基} (3 _ ^比σ定 基))-Ν-(3-吼啶基甲基）甲醯胺 (6-(2-氣-5 -曱氧基苯基)-2-{[2-(3 -氣苯基）乙基]胺基}(3_ϋ比 啶基))-Ν-(3 -吼啶基曱基）曱醯胺 (6-(2-氣基-6-氣苯基)-2-{[2-(3 -氣苯基）乙基]胺基}(3-吼咬 2〇 基))-N-(3-吼啶基曱基）曱醯胺 (6_(2_氟苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3- ϋ比咬 基))-Ν-(3-吼啶基曱基）甲醯胺 (6-(2-氣基-5 -曱氧基苯基)-2- {[2-(3-氟苯基）乙基]胺基} (3 _ 吼啶基))-N-(3-吼啶基曱基）曱醯胺 89 200823188 (2-{[2_(2,3-二氟苯基）乙基]胺基}·6-(2-氰基苯基)(3-吼啶 基))-Ν_(3-吼啶羞甲基)曱醯胺 . . _ (6-(2-氯-5-氟苯基）-2- {[2-(3-氟苯基）乙基]胺基）(3- 0比ϋ定 基))-Ν-(3-吼啶基曱基）曱醯胺 5 (6-(2 -鼠基-5 -鼠苯基)-2-{[2-(3 -氣苯基）乙基j胺基}(3-ϋ比σ定 基))-Ν-(3-咕啶基曱基）甲醯胺 (6-(3-氟苯基）-2-{[2-(3_氟苯基）乙基]胺基}(3-吼啶 基))-N-(3-吼啶基曱基）甲醯胺 (6-[2-(氰基曱基）苯基]-2-{[2-(3-氟苯基）乙基]胺基}(3-口比 ίο 啶基))-N-(3-吡啶基曱基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-[3-(羥基甲基）(2-噻吩 基)](3-吼啶基))-N-(3-吼啶基曱基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(5-甲醯基(3-噻吩基))(3-吡啶基))-N-(3 _吡啶基甲基）曱醯胺 15 (2-{[2-(3-氟苯基）乙基]胺基}-6-[5-(羥基曱基）(3-噻吩 基)](3-吼啶基))-N-(3-吡啶基曱基）曱醯胺 (6-(2-氯-4-甲基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-(3-吼啶基曱基）甲醯胺 (6-(2-氰基-4-曱基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-口比 2〇 啶基))-N-(3-吡啶基曱基）甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-[3-(羥基曱基）苯基](3-口比 啶基))-N-(3-吼啶基曱基）曱醯胺 (2-{[2-(3_氟苯基）乙基]胺基}-6-[3-(甲氧基曱基）苯基](3-吡啶基))-N-(3-吡啶基甲基）曱醯胺 90 200823188 =-(1Η切，4-四唾基）_2_{[2 (3氟苯基）乙基 .基}(3-吼啶基))_N_(3_nfc啶基曱基）曱醯胺 (=-[2-乳羥基甲基）苯基]_2_{[2_(3_氟苯基）乙基 土 }(3-。比口定基))-N_(3_n比錄曱基）甲贐胺 (2R)Methionine i W N-mercapto{6-phenyl-2-[(2-(2-pyridyl)ethyl)amino](3_pyridylguanamine N-[((3R) pyrrolidine_ 3_yl)methyl]{6_phenyl_2_[(2_(2-pyridyl)ethyl) 65 20 200823188 , Amino](3-pyridyl)}carbamamine {6_phenyl-· 2_[(2-Phenylethyl)amino K3" is more than 2 benzyl) ethyl carbamide 1 { phenyl phenyl 2-[(2 phenylethyl) amine Κ3_πpyridyl group) 5 ethyl) decylamine 1 N-mercapto-2-({6-phenyl-2-[(2-phenylethyl)amino](3-pyridyl)}carbonyl Amino)acetamide & N,N-dimercapto-2-({6-phenylj_[(2-phenylethyl)amino](3-pyridyl)carbonylamino)acetamide 〇N-(Aminomethylmethyl){6_phenyl_2_[(2-phenylethyl)amino](3_pyridyl)}decylamine (2_{[2-(2_oxygen) (piperidinyl)ethyl]aminopyrrolidine (3_^ than butyl))-(3-indoleylmethyl)formamide (2-{[2-(1-indenyl)) -piperidinyl))ethyl]aminobiphenyl 6-phenyl (3_ π-pyridyl-5-yl))-indole-(3-acridinylmethyl)carbenamide {6-phenyl-2-[(2 -(2-thienyl)ethyl)amino](3_pyridyl)}_team (3_pyridylfluorenyl) decylamine (2-{ [2-(1-mercaptopimidyl-4-yl)ethyl]amino}_6_phenyl(3_pyridyl))-indole-(3-acridinylindenyl)decylamine 0 {2- [(2-(2-furyl)ethyl)amino]-6-phenyl (3-d-pyridinyl fluorenyl) decylamine ( {2-[(oxapenta-2-ylindenyl)) Amino]_6_phenyl (3_u-pyridylpyridylmethyl)forminamine {2-[(2_(1,3-dioxolan-2-yl)ethyl)amino]dongphenyl ( 3_^Bistidine 66 200823188 ))}-N-(3-Acridinemethyl)carbamamine {2_[(3_Misopropyl)amino]_6·Phenyl (3_pyridyl)} _Ν_(3_σ ratio 咬基•methyl)methanoamine & {2-[(2-morpholin-4-ylethyl)amino]-6-phenyl (3_σ-pyridylpyridinyl 5-ylmethyl) Carbenamide {6-phenyl-2-[(2-phenoxyethyl)amino](3_pyridyl)}_N_(3_acridinylmethyl)carbenamide m(2_(2H -benzo[3,4.,3.dioxanyl)ethyl)amino]-6-phenyl(3-hydroxypyridyl)}_Ν-(3· acridineyl Methionamine 1〇N_[((3S))pyridin-3-yl)indolyl]{6-phenylpyridinyl)ethyl)amino](3-pyridyl)}decylamine 6_phenyl_2-(propylamino)(3_acridinyl)]_Ν_(3_pyridinyl) guanamine 2-({ 6-phenyl-2-[(2-phenylethyl)amino;|_3_,pyridylhydrazinylcarbonyl)methylhexanoic acid methyl ester=[((3R)-1-ethinylpyrrolidinyl) )methyl]{6_stupyl_2_[(2_(2_pyridyl)ethyl)amino](3_acridinyl)carbamamine 1 [((2s)-i-ethinylpyrrole]啶 基 曱 ] ] ] 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 6 Amino group] (3_0Jtu-based decyl fluorenyl) carboxylic acid amine N-[(l-acetoxy (3- fluorenyl)) fluorenyl] {6_phenyl benzyl group) ethyl) amide] (3- Pyridyl)}mercaptoamine {6_phenyl-2-[(2-(2-acridinyl)ethyl)amino](3_pyridyl)}-N-(3_thia 67 200823188 phenyl曱醯) 曱醯amine • {6-phenyl-2-1 (2-(2-11 fluorenyl).ethyl)amino] (3-° ratio of decyl)}_N-(2-^ phenyl Mercaptoamine (2-{[2-(2-oxyimidazolyl)ethyl]amino) 6-phenyl(3-acridinyl))-indole-(3-acridinylhydrazine Base) guanamine (2-{〇(2-oxyl).比 啶 ) ) ) 乙基 乙基 乙基 乙基 乙基 乙基 乙基 { { { { { 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- Ethyl)amino]-6-phenyl (3-0 ratio; decyl decyl fluorenyl) formamide (2-{[(ylcyclohexyl) fluorenyl)amino}_6_phenyl (3-吼-))-Ν-(3-σΛ 曱 曱 曱)carbamamine (2-{[2_(3,5-dimercaptooxazol-4-yl)ethyl]amino}-6- Phenyl (3_acridinyl))_N_(3-u-pyridylhydrazino)carbenamide 0{[2_(3,5-diindolylpyridazolyl)ethyl]aminobib 6_benzene (3_σ-pyridyl))-Ν-(3-pyridylfluorenyl)formamide (2_{[2-(2-chlorophenyl)ethyl]amino}_6_(2-cyanophenyl) (3_ π-pyridylmethyl) decylamine (6-(2-cyanophenyl)-2-{[2_(2-methylphenyl)ethyl]amino} 〇pyridinyl))- Ν-(3-Acridinesulfanyl) decylamine (6-(2-cyanophenyl)_2_{[2_(2-fluorophenyl)ethyl]aminopurine (3_ σ-pyridyl)) -N_(3-u-pyridylmethyl)carbamamine (6-(2-cyanophenyl{[2-(2-cyanophenyl)ethyl)amino} (3_.pyridyl) )-Ν_(3_σ ratio thiol sulfhydryl) decylamine {6-(2-carbylphenyl)_2_[(2-(2-)thyl)ethyl)amino](3_ σ pyridine 68 200823188 基)}-Ν·(3-Acridinesulfanyl)guanamine {6-(2-cyanophenyl)·2-[(2-(2-furanyl)ethyl)amine (3-Acridine•yl)}-Ν-(3-pyridylfluorenyl)carbamamine - {6_phenyl-2-[(2-(2-11 to 1[2])ethyl) Amino](3-17 to 17-based)}-1^-prop-2-5-alkenylcarboxamide (2-{[2-(3-fluoro(2-acridinyl))))] }-6-phenyl(3-acridinyl))-indole-(3-acridinylfluorenyl) decylamine N-[(l-fluorenyloxazol-3-yl)methyl]{6- Phenyl-2-[(2-(2-acridinyl)ethyl)amino](3-pyridyl)}carbamamine ίο N-[(l-ethinyl(4-piperidinyl)) Mercapto]{6-phenyl-2-[(2-(2-acridinyl)ethyl)amino](3-acridinyl)}carbamidine 2-[({6-phenyl-2) -[(2-(2-吼σ定基)ethyl)amino]pyridyl}decylamino)methyl]morpholine-4-carboxylic acid tert-butyl ester {6_phenyl-2-[ (2-(2-σ ratio σ-decyl)ethyl)amino](3 -. σ σ base)}-Ν-(2-pyrene than 15 pyridine)carbamamine (2-{[2-(3) -nonylphenyl)ethyl]amino}-6-phenyl(3-tonidinyl))-indole-(3-pyridylmethyl)formamide (6-(2-carbylphenyl)) -2- {[2-(2-Phenylphenyl)ethyl]amino} (3- 0 thiol))- N-(3-Acridinesulfanyl)guanamine 2〇N-{[2-(aminomercapto)(3-acridinyl)]methyl}{6-carbazol-4-yl-2 -[(2-(2-pyridyl)ethyl)amino](3-pyridyl)}decylamine N-{(lR)-2-[(5-fluoro-2-{[2-(3) -fluorophenyl)-2-hydroxyethyl]amino}-6_ oxazole-4-yl(3-acridinyl)carbonylamino]-isopropyl}-2-[(third butoxide) Carboxyamino]acetamide 69 200823188 {5_Fluoro-6-pyrazol-4-yl-2-[(2-pyrazolethyl)amino](3-pyridyl)}-N-( 3-pyridylmethyl)guanamine. • N-[(lR)-2-({5-fluoro-6-portobazin-4-yl-2_[(2-oxazolylethyl)amine) (5-(2-cyanophenyl)-2-{[2-(3-(3-cyanophenyl)-2-{[2-(3-) Fluorophenyl)ethyl]amino}(3-acridinyl))-indole-{[6-(trifluoromethyl)(2-acridinyl)]methyl}decylamine (6-(2) -ylphenyl)-2_{[2-(3-phenylphenyl)ethyl]amino}(3- ° ϋ定基))-Ν-{[5-(trifluoromethyl)(2^ Pyridyl)]methyl}decylamine (6-(2-murolylphenyl)-2-{[2-(3-phenylphenyl)ethyl]amino) (3- ° ratio σ ίο Base))-Ν-{[3-(trifluoromethyl)(2-acridinyl)]methyl}nonylamine N-[(6-chloro(3-acridinyl))indenyl](6 -(2- Phenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))decylamine (6-(2-cyano(3-thienyl))- 2-{[2-(3-fluorophenyl)ethyl]amino}(3-hydroxypyridinyl)-N-(3-pyridylfluorenyl)carbenamide 15 (2E)-3-( 2-{[2-(3-Phenylphenyl)ethyl]amino}-6-phenyl (3- σ ^ 定))-Ν-mercaptoprop-2-enium amide (6-(2) -murinophenyl)-2-{[2-(3-phenylphenyl)ethyl]amino}(3_吼ϋ定基))-Ν-{[6-(methylamino)(3- Acridinyl)]hydrazino} amidoxime-{[6-(didecylamino)(3-acridinyl)]fluorenyl}(6-(2-cyanophenyl)-2-{ [2-(3-Fluorophenyl 2 decyl)ethyl]amino}(3-acridinyl))decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}- 4-(hydroxyindenyl)-6-phenyl(3-acridinyl))-indole-(3-acridinylhydrazino)carbamidine-[(5-amino(2·-pyridyl) )) fluorenyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl)) decylamine 70 200823188 ( 2-{〇(3-Fluorophenyl)ethyl; I-aminopurine via hydrazinoylpyryldiyl group))-N-(3-pyridylfluorenyl)carbenamide. (2-{ [2-(3-fluorophenyl)ethyl]aminophenyl-5-[N-(3-acridinylmethyl), amine-mercapto]] Base))-N-(3-pyridylfluorenyl)formamide (5_(2_he 5-5-aza- azavinyl)-2_{[2-(3-fluorophenyl)ethyl]amine Base}_6_stupyl (3_acridinyl))_N_(34 pyridinemethyl)carbamamine (5-(aminomethyl)_2_{[2_(3_fluorophenyl)ethyl]amino}_6 _Phenyl-pyridinyl))_Ν-(3-indole-based thiol) decylamine (2-{[2-(3-fluorophenyl)ethyl)aminobiphenyl 6_〇_methyl Pyrazole_4_yl)(3_pyridineίο))-Ν-(3-pyridylmethyl)decylamine-({6-[3,3-bis(dimethylamino)_2_) Azapropan-2-enyl](2_σ-pyridyl)}methyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3: gnach base)) carbamide oxime-[(6-{[(t-butoxy)carbonylamino] fluorenyl}(2_σ-pyridyl)) 曱15 yl] (6-(2-cyano) Phenyl)_2-{[2-(3-fluorophenyl)ethyl]amino}(3_pyridyl)) amidoxime-{[4-(aminomethyl)(3_ σ-pyridinium) Base]]methyl}(6_(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_acridinyl))carbenamide-{ [3-(Aminomethyl)(4_ σ-pyridyl)]methyl}(6-(2-cyanobenzene'°-fluorophenyl)ethyl]amino}(3-anthraquinone))曱Amine (5bromo 2-{[2-(3_fluorine) Ethyl]amino]aminobi 6_ π than salivation_4_yl (3_吼nyl))-Ν-(3_acridinylmethyl)decylamine (5-bromo-2-{[2- (3-Fluorophenyl)ethyl]amino}_6_(1•methyl^bazole_4_yl)(3_pyridyl))-team (3_pyridylmethyl)decylamine 71 200823188 (6 -(5-murine-based 嗤-4-yl)-2-{[2-(3-(phenylphenyl)ethyl]amino}(3-° ratio σ-base))-Ν-(3 -Acridinesulfonyl)carbamide (5-carbyl-2-{[2-(3-murophenyl)ethyl]amino}-6-(1-methyl 11 嗤-4-yl) (3-(Acridine))-indole-(3-acridinylfluorenyl)carbamamine 5 (2-{[2-(3-fluorophenyl)ethyl]amino}-6-carbazole -3-yl(3-acridinyl))-indole-(3-acridinylmethyl)decylamine (6-(3-carbyl-1-indenylpyrene-pyry-4-yl)_2- { [2-(3-Fluorophenyl)ethyl]amino}(3-pyridyl))-N-(3-pyridylfluorenyl)decylamine (6-(5-cyano-1 -methyl) Oxazol-4-yl)-2-{[2-(3-fluorophenyl)ethyl]amine ίο }(3-pyridyl))-N-(3-pyridylmethyl)decylamine. 2-[(2_{[2-(3-Phenylphenyl)ethyl]amino}-6-σ ratio α sit-4-yl (3-° ratio σ base)) carbonylamino]-Ν-A Ethylamine 2-[(2-{[2-(3-fluorophenyl)ethyl]aminomethyloxazol-4-yl) (3-port Pyridyl))carbonylamino]-N-mercaptoacetamide 15 (5-Gas-2-{[2-(3-phenylphenyl)ethyl]amino}-6-(1-indenyl 11比-4-yl)(3_pyridyl))-N-(3-pyridylmethyl)decylamine N-{[6-(aminomethyl)(2-acridinyl)]fluorenyl (5-Bromo-2-{[2-(3-fluorophenyl)ethyl]amino}-6-phenyl(3-acridinyl))carbenamide N-[(l- {2- [(Tertidinoxy)carbonylamino]ethyl}pyrazole-3-yl)indolyl](6-(2-cyanophenyl)-2-{[2-(3-fluorobenzene) Ethyl]amino}amino}(3-acridinyl))decylamine N-[(l-{2-[(t-butoxy)carbonylamino]ethyl}oxazol-5-yl) Methyl](6-(2-carbophenyl)-2-{[2-(3-(phenyl)ethyl]amino}}(3-吼σ定基)) decylamine 72 200823188 N-{ [1_(2-Aminoethyl)carbazole-3-yl]methyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3- π ratio bite base)) 甲 Ν Ν -{[1-(2-aminoethyl) oxazol-5-yl] fluorenyl) (6-(2-cyanophenyl)-2- {[2-(3-Fluorophenyl)ethyl]amino}(3- π-fluorenyl)) an amine N_{[6-(aminomethyl)(2_acridinyl)] fluorenyl }(2_{[2_(3_Fluorophenyl)ethyl]aminobib 6-(1-methyl-portyrazole-4-yl)(3- Pyridyl)) guanamine group {[6-(aminomethyl)(2·-pyridyl)]methyl}(2-{[2-(3-fluorophenyl)ethyl]amino} _6_pyrazol-4-yl(3-pyridyl))carbenamide N-{[6-(aminomethyl)(2_acridinyl)]methyl}(5,_2_{[2_(3_气Phenyl)ethyl]amino}-6-(1-methylindole-4-yl)(3-anthraquinone))cartoamine N_[((2R)_5-oxyπpyrrolidine_ 2-yl)methyl](6-(2-cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl]amino}(3_ ο σ σ base)) anthraquinone N_[(( 2S)_5_oxyπpyrrolidyl-2-yl)methyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}( 3_Aridinyl))carbamide N- {3-[(5S)-5-(2-diazo-2-azinovinyl)-2-oxoindole]propyl} (6- (2-cyanophenyl)·2-{[2-(3-fluorophenyl)ethyl]amino}(3 j-pyridyl))carbenamide N-[((2S)-l-{ 3-[(Tertibutoxy)carbonylamino]propyl: oxy. (r-bromo-2-yl)indenyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))- Indoleamine N-{[(2S)-l-(2-aminoethyl> 5-ethoxypyrrolidin-2-yl]methyl}(6_(2_cyanophenyl)-2-{[2 -(3-fluorophenyl)ethyl]aminopyridinylcarbamidine N-{[(2S)-l-(3-aminopropyl)-5-oxypyrrolidine-2_ Methyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_acridinyl)carbamamine 73 200823188 , its ★ 2.Ethyloxypropyl}(6·(2_cyano basic Η-ί[2-(3-fluorobenzyl)ethyl)amino} (3_吼 阙 阙 (10) small (four) red base) money贿 基 ^ ^ cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3 propyl)) aryl amine N- {3-[(5R)-5 -(2-diazo-2_azavinyl)_2-oxyscale bite]propyl}(6-(2-cyanophenylfluorophenyl)ethyl]amino))carboxamide N- {3-((5R)'5-(Aminomethyl)_2-oxyl oxime]propyl}(6-enylphenyl)·2_{[2-(3-d-phenyl)ethyl Amino}(3♦定基甲甲甲胺Ν- {2_[(5S)·5-(aminomethyl)_2_oxyscale. {[2-(3-Phenyl)ethyl]amino} (3_n than bite)) N-called (tetra)-5-(aminomethyl)_2-oxy oxime bite] ethyl^(2_ylphenyl)-2-{[2-(3-fluorophenyl)ethyl]amine Base} (3" than bite base)) arylamine 15 20 state (10) oxy π ratio slightly bite _2 _ yl) methyl] (2 | (3 _ phenyl) ethyl] amine -6 -pyrazol-3-yl(3-pyridyl))carboxamido)methyl](2 fluorophenyl benzyl)-2-{[2-(3-fluorophenyl)ethyl]amino }(3 -2-ylmethyl)methyl _ ^-based lung 10 洛 洛 }}}-6-吼嗤+-(3-pyridyl))carboxamide Nim (t-butoxy)-lanamine ]ethyl ί=amine cyano __{[2_(3_ gas fine ethyl) amine fine two ratio bite 74 200823188 N-[(l - {3-[(dibutyloxy))) Propyl}σ ratio slightly biting) methyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_pyridine^yl) )carbendazim-{[1-(2-aminoethyl)π-pyrrolidinyl-2-yl]methyl}(6_(2-cyanobenzene-5yl)-2-{[2-(3β Fluorophenyl)ethyl]amino}(3-acridinyl))carbenamide-{[1-(3•aminopropyl)-perpyridyl-2-yl]methyl)(6_( 2-cyanophenyl)-2_{[2_(3-fluorophenyl)ethyl]amino} (3_ as defined)) formamide 2-({(2S)-2-amino-3- [(6_(2-cyanophenyl)-2-{[2 Phenyl)ethyl]amino}(3-indole))methylamino)propyl}amino)acetate ίο 2-({(2S)-2-month female -3-[ (2-{[2-(3-Fluorophenyl)ethyl]aminophenyl 6-(ι-methylcarbazole_4_yl) (3) ratio. Basement)) Methylamino)propyl)amino)acetate N-[((2S)-6-oxypiperazyl)methyl](2_{[2_(3_fluorophenyl)ethyl] Amino}-6-吼Salt_4_yl (3) than octyl)) guanamine N-[((2S)-6-oxypiped_2_yl)methyl](6_(2_ Cyanophenyl)_2_{[2_(3_5 fluorophenyl)ethyl]aminoindole 3-σpyridinyl))carbenamide N-[((2R)-4-{3-[(second Oxy)carbonylamino]pyridyl 6-oxypipedyl)methyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine Base}(3_σ-pyridyl))carbendazim N-[((2S)_6-oxypiperidin-2-yl)methyl](2_{[2_(3_fluorophenyl)ethyl]amine }冬(1_methylpyrazole ice-based)(3-pyridyl))carbenamide N_[((2S) Oxygen 3-ylpipedyl)methyl](2-{[2-(3-fluoro) Phenyl)ethyl]aminobiphenyl 6-carbazole _3_yl (3-acridinyl))carbenamide N-{[(2R)-4-(3-aminopropyl)-6-oxyphene Plowing _2_yl]methyl)(6_(2-cyano basic) 2 {[2 (3-fluorobenzyl)ethyl]amino group)) amide N {[(2R)-4-( 3-aminopropyl)_6_oxyl brigade σ__2_yl]曱75 200823188 }}(2-{[2-(3-fluorophenyl)ethyl]amino}}_6_(ι_methyl σ ratio salivation_4_yl)(3_-pyridyl))曱醯N_[((2R)_6_oxypiperidin-2-yl)indenyl](6-indolylphenyl)_2_{[2-(3-fluorophenyl)ethyl]amino}(3_ϋ ratio Pyridyl))carzamide N-{[(2S)-4-(2-aminoethyl)-6-oxypiped-2-yl]methyl}(6-(2-cyanophenyl) _2-{[2-(3-fluorophenyl)ethyl]amino}(3_u-pyridyl))guanamine N-{[(2S)_4_(3-aminopropyl)-6-oxygen (5-(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amino} ({(2R)-1_[4-(1,3-dioxobenzo[c]oxazol-2-yl)butyl> 5-oxyindoleidine-2-yl} fluorenyl) (6_ (2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amino}(3-pyridyl))decylamine N_({(2R) small [^(^dioxybenzo) (4) oxazoline_2-yl)pentyl]tooxopurine bite -2_yl}methyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl) Ethyl]amino}(3-pyridyl))carboxamide (2R)-2-{[(6-(2-cyanophenyl)_2-{[2-(3-fluorophenyl)ethyl) Amino}(3-° ϋ定基))carbonylamino]methyl}oxypyrrolidinecarboxylic acid tert-butyl ester n_[((2r) fluorenyl)] (6-(2-cyanophenyl) Pup-fluorophenyl)ethyl]amino}(3-acridinyl))carbenamide N-{[(2R)-1_(4- Benzyl)_5_oxypyrrolidinium-2-yl]methyl}(6-(2-cyanophenyl)-2-{[2_(3-fluorophenyl)ethyl]amino}(3-pyridine Base))carbamide N-{[(2R)-l-(5-aminopentyl)-5-oxypyridinyl]methyl}(6_(2_cyanophenyl)-2-{[ 2-(3-Fluorophenyl)ethyl]amino}(3_acridinyl iscarhamamine (2_{[2-(3-fluorophenyl)ethyl]amino) 6 σ azole _ 4_yl (3_^pyridyl))-indole-(pyrazol-3-ylmethyl)carbamamine 76 200823188 ({[2(3Fluoro)ethyl)aminomethyl) ) (3_σ specific base)) - Ν 比 oxazol-3-ylmethyl) meglumine (2_{[2-(3-fluorophenyl)ethyl] aminibbazole! base.比 基))-Ν 比 比 -3 -3 -3 -3 -3 _ ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) )methyl](Bu(2_cyanophenyl)_2_{[2♦fluorophenyl)ethyl]amino}(3_pyridyl))guanamine N-{[(2R)_1_(3_amine比 比 ) ) ) ) 唆 唆 唆 唆 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- Pyridyl))carbendazim N-{[1_(3_aminopropyl)carbazole-3-yl]methyl}(6_(2-cyanophenyl)-2_{[2_(3_fluoro Phenyl)ethyl]amino}(3_acridinyl))carbenamide N-{[l-(3-aminopropyl)carbazole-3-yl]methyl}(2_{[2_( 3_fluorophenyl)ethyl]moon-female}-6-(1-methylindole) (3_α-indenyl))carbenamide-{[1-(3-aminopropyl) Pyrazol-3-yl]fluorenyl}(2_{[2_(3_fluorophenyl)ethyl]amino}}_6-σ 嗤_3_yl (3_σ ratio) 〇(3-Aminopropyl)pyrazol-5-yl]methyl}(2-{[2-(3-fluorophenyl)ethyl]aminomethylpyrazole_4_ylindole-3-pyridine 》 醯 醯 Ν - {[1-(3-Aminopropyl carbazol-5-yl) fluorenyl}(2-{[2-(3-fluorophenyl)ethyl]amino) -pyrazole-3-yl(3-pyridyl))indole Amine N-[((2R)-l-{2_[(di-dibutoxy))-ylamino]ethyl succinyl _2-yl) fluorenyl](6-(2-cyanophenyl) -2_{〇(3-fluorophenyl)ethyl]amino group than dimethyl group))carbamamine N-[((2R)-1 -{3-[(dibutyloxy)) group ]propyl}. than slightly biting _2_yl) fluorenyl](6-(2-cyanophenyl)-2-{|>(3-fluorophenyl)ethyl]amine ^3_吼Bite 77 200823188 base)) indoleamine N-{[(2R)-l-(2-aminoethyl)pyrrolidinyl]methyl}(6_(2-cyanophenyl)-2-{[ 2-(3-Fluorophenyl)ethyl]amino}(3_,pyridyl)carbamamine N-{[(2R)-l-(3-aminopropyl)π-pyrrolidine-2_ Methyl}(6•(孓cyanobenzene5-fluorophenyl)ethyl]amino}(3-. than bite)) an amine N-[(l-{2_[(third) Oxy)carbonylamino]ethyl hydrazide, oxazol-3-yl) fluorenyl] 〇{[2-(3-fluorophenyl)ethyl]aminopyrazole _3_yl (3_σ-pyridyl) )) amidoxime-{[1-(2-aminoethyl)pyrazole-3-yl]indenyl}(2-{[2_(3-fluorophenyl)ethylamino]amino}« Azul-4-yl (3 吼 基)) carbamide Ν-{[1_(2-aminoethyl) π-biazole _3_yl] fluorenyl k2_u2 <3_Fluorophenyl)ethyl]amino}-6-oxazol-3-yl (3-n-bitenyl)) amidoxime-{[1-(2-aminoethyl)anthracene Azolylene]methyl}(2_{[2_(3_fluorophenyl)ethyl]amino}-6-oxazol-3-yl(3-indenyl)carbamamine 15 N-{l&gt (2-aminoethyl)indolozol-3-yl]fluorenyl}(2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-mercaptopyrazole 4-yl)(3-pyridyl)) amidoxime-{[1-(2-aminoethyl)oxazolyl-5-yl]methyl}(2_{[2_(3_fluorophenyl) Ethyl]amino}_6_(1_decylpyrazol-4-yl)(3-pyridyl))decylamine N_{[(2R)_i_(3-aminopropyl)oxypiperyl ]methyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl) 20 ethyl]amino}(3-pyridyl))decylamine N-{[ (2R)-l-(3-Aminopropyl)-6-oxyanthene 2-yl]indenyl}(2_{[2-(3-fluorophenyl)ethyl]aminobib 6-( 1-曱 base mouth -4-yl)(3-pyridyl))carboxamide N-{[(2R)_l-(3-aminopropyl)_6-oxy σ bottom σ well-2 -基]甲78 200823188 基}(2- {[2-(3-)-yl)ethyl]amino}-6-° ratio ° sitting _4_ base (3-° ratio σ base).. . 曱醯 amine. . _ ' N-{[(2R)-l-(3-Aminopropyl)-6-oxypiperidin-2-yl] fluorenyl} (2_{[2 -(3-murine phenyl)ethyl]amino}- 6-indole-tris-3-yl (3-indole ratio sigma)) 5 amidoxime-[(2R)-1-ethenyl Pyrrrolidin-2-yl)methyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))indole Indoleamine N-{[(2R)-l-(methylsulfonyl)oxaridin-2-yl]fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3 -fluorophenyl)ethyl]amino}(3-acridinyl))carbenamide ίο N-[((2R)-1-methylpyrrolidin-2-yl)indolyl](6-(2 -cyanobenzene.yl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3 j-pyridyl))guanamine N-[((2R)-1,1- Dimethylpyrrolidin-2-yl)methyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl) )) methotrexate N-[((2R) -1 - {[3-( 1,3 -dioxybenzoquinone [c]11-salt-2-yl)propyl] sulphate] 15 σ ratio Bite-2-yl)methyl](6-(2-carbophenyl)-2-{[2-(3-phenylphenyl)ethyl]amino)(3-acridinyl))曱Indoleamine N_({(2R)-l-[(2-aminoethyl)sulfonyl]oxaridin-2-yl}methyl)(6-(2-cyanophenyl)-2-{ [2-(3-Fluorophenyl)ethyl]amino}(3-acridinyl))decylamine N-({(2R)-l-[(3-aminopropyl)sulfonyl] Roar Pyridin-2-yl}methyl)(6-(2-2〇-muroleylphenyl)-2-{[2-(3- disordered phenyl)ethyl]amino} (3-吼σ定基)) Brewed amine Ν-{[1-(3-aminopropyl)oxazol-3-yl]fluorenyl}(2-{[2-(3-fluorophenyl)ethyl]amino}-6- Indazole-4-yl(3-acridinyl))carboxamide-{[1-(3-aminopropyl) port ratio. -5-yl] fluorenyl}(2-{[2-(3-phenylphenyl)ethyl]amino}-6-n-pyrazol-4-yl(3-pyridyl))carbenamide 79 200823188 N-[((2R)-l-{3-[(Tertidinoxy)carbonylamino]propyl)5oxyπpyrrole_2_yl)methyl]〇{[2_(3 _Fluorophenyl)ethyl;|Aminobi 6_(1-methyloxazol-4-yl)(3-anthraquinone))N-{[(2R)-1_(3-Amino) Propyl)-5-oxyπpyrrole-2-yl]methyl}(6-{1_[(-methylamino)(dimethylene)methyl]σ) than salivation_4_yl}- 2_{[2-(3-Fluorobenzyl)ethyl]amino} (3_ π ϋ ϋ ))) 甲-N-{[(2R)-l-(3-Aminopropyl)_5_ Oxygen Π-pyrrolidinyl-2-yl]methyl}(2_{[2_(3-fluorophenyl)ethyl;]amino}_6_(1-methylcarbazole) (3_pyridyl)) Indoleamine (2R)_2-{[(2_{[2-(3-fluorophenyl)ethyl]aminomethyl) is a 4-(yl)-() group) ]曱基}. Bilo bite t-butyl butyl N_{[(2R)_l-(3-aminopropyl)_5_oxy π-pyridyl-2-yl] fluorenyl} (2-{〇(3-fluorine) Phenyl)ethyl]amino}_6"pyrazole_4_yl (3"pyridinyl))carzamide N_[((2R)-l-{3_[(t-butoxy))amine ] 丙基 5 _ 5 _ 5 5 5 ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] ] (3-pyridyl)) decylamine N-(2-amino-1methylpropylcyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amino} (3-σ 唆Base)) decanoic acid N-[((2R). than slightly bit-2-yl) fluorenyl](2_{[2_(3-fluorophenyl)ethyl]amino}-6-carbazole-4 -yl (3-acridinyl)) decylamine N_[((2R).pyrrolidinyl-2-yl)indenyl](2_{[2-(3-fluorophenyl)ethyl]amino} -6-(1-methylpyrazol-4-yl)(3-acridinyl)) decylamine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl) Ethyl]amino}(3-acridine 80 200823188))-N-{2-mercapto-2·[(fluorenylsulfonyl)amino]propyl}decylamine N-[(( 2R)-l-{2-[(Tertibutoxy)carbonylamino]ethinyl}pyrrolidin-2-yl)methyl](2-{[2_(3-fluorophenyl)) Aminobutyryl 6-(1-methyloxazol-4-yl)(3-pyridyl)) Indoleamine 5 N-[((2R)-l-{3-((t-butoxy)carbonylamino)propanyl}pyrrolidin-2-yl)methyl](2-{[2-( 3-fluorophenyl)ethylamino}-6-(1-methyloxazol-4-yl)(3-pyridyl))carbenamide N-[((2R)_l-{4-[( Third butoxy)carbonylamino]butanyl}indolyl-2-yl)methyl](2-{[2-(3-fluorophenyl)ethyl]aminoindolyl carbazole-4-10 (3-pyridyl))carboxamide N-{[(2R)-l-(2-aminoethyl)indolyl-2-yl]methyl}(2-{[2-( 3-fluorophenyl)ethyljaminomethylhydrazine 17-spin-4-yl) (3-° ratio ° base)) anthraquinone N-{[(2R)-l-(3-aminopropionamidine) (2-)[2-([3-(3-fluorophenyl)ethyl]aminomethyloxazol-4-yl)(3-acridinyl)) Indoleamine 15 N-{[(2R)-l-(4-aminobutyrydinylpyrrolidin-2-ylindenyl}(2-{[2-(3-fluorophenyl)ethyl]amino} -6-(1-methyloxazol-4-yl)(3-acridinyl)) decylamine N-((2S)-2-aminopropyl)(6-(2-cyanophenyl) -2{[2-(3-Fluorophenyl)ethyl]amino}(3-acridinyl))carinamide 2-[(tatabutoxy)carbonylamino]-N-{ 2-[(6-(2-Cyanophenyl 2 fluorenyl)-2-{[2-(3-(phenylphenyl)ethyl)amino}} (3-17 σ 定 base)) Weilkylamino]-t-butyl}acetamide 4-[(tatabutoxy)carbonylamino]-indole-{2-[(6-(2-cyanophenyl)-2-) { [2-(3-Fluorophenyl)ethyl]amino}(3-acridinyl))carbonylamino]-tert-butyl}butanamine N-{(1 S)-2-[(6 -(2-oxophenyl)-2-{[2-(3-phenylphenyl)ethyl]amino}(3_ 81 200823188 tharidinyl))carbonylamino]-isopropyl}-4- [(Tertibutoxy)carbonylamino]butanamine _ . # . . _ N-[((2R)_l-{5_[(Tertidinoxy)carbonylamino]pentanyl} 吼(2-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl)) decylamine 2-Amino-N-{2-[(6-(2-cyanophenyl)-2_{[2_(3-fluorophenyl)ethyl]amino}(3-indole)) Amino]-t-butyl}acetic acid amine 4-amino-N-{2-[(6-(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amino}( 3_mouth ratio bite base))carbonylamino]-tert-butyl}butylamine N_ {[(2R)_丨_(N_mercaptoamine oxime) 吼 啶 _2 _ _ _ _ _ }(6_(2_Cyanophenyl)_2][2_(3_(phenyl)ethyl]amino}(3-吼))carbamamine (2R)_2_{[(6_(2- Cyanophenyl)_2_{[2_(3_fluorophenyl)ethyl]amino)(3_pyridyl)疋 疋)))carbonylamino]methyl}pyrrolidinium carboxylic acid decyl phenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3-pyridyl)) Carbonylaminol isopropyl isopropyl 2-aminoacetamide N_{(ls)_2_[(6_(2-cyanophenyl)s{{2_(3-fluorophenyl)ethyl]amino} (3_, pyridine group benzyl amine isopropyl group 4 _ _ _ _ N-{[(2R) small (5-amino pentyl) 吼 slightly bite base]: base} (6-( 2_cyanophenyl)_2_{[2_(3_fluorophenyl)ethyl]amino}(3_ 疋 疋))carbamamine n_r2S)_2K sulfhydryl)amino]propyl,} (6_(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amino}& 吼 base)) formic acid amine (2)^2-{[(6_(2_cyano) Base)_2_{[2_(3_气phenyl)ethyl]amine-based fluorenyl))carbonylamino]methyl}pyrrolidinic acid 2-aminoethyl ester N currylamine) (6-(2-cyanophenyl)-2_{〇(3_fluorobenzene 82 200823188)ethyl]amino}(3-acridinyl))carbenamide N-((2R)-2 -aminopropyl)(6-(2-cyanoiphenyl)-2-{[2-(3-(phenylphenyl)ethyl] 'amino}(3-pyridyl))decylamine. N_[(2R)-2-(decylamino)propyl](6-(2·cyanophenyl)-2_{[2-(3-fluorophenyl5-yl)ethyl]amino}} - aridinyl)) indoleamine N-{(2S)-2-[indolyl(methylsulfonyl)amino]propyl}(6-(2-cyanophenyl)-2-{[ 2-(3-Fluorophenyl)ethyl]amino}(3-pyridyl))carbenamide N-{(2R)-2-[(methylsulfonyl)amino]propyl}(6 -(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))carbenamide ίο N-{(2R)-2- [mercapto (methylsulfonyl)amino]propyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3- Acridinyl))carzamide N-{(lR)-2-[(6-(2-carbylphenyl)-2-{[2-(3-phenylphenyl)ethyl]amino}} 3-acridinyl))carbonylamino]-isopropyl}-2-[(tatabutoxy)carbonylamino]acetamide 15 N-{(lR)_2-[(6-(2- Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3·-pyridyl))carbonylamino]-isopropyl}-2-[(third Butoxy)carbonylamino]]-indole-methylacetamide N-{(lR)-2-[(6-(2-murylphenyl)-2-{[2-(3-phenylphenyl) Ethyl]amino}(3-acridinyl))carbonylamino]-isopropyl}-4-[(tatabutoxy)carbonyl 20 amide]butanamine N-{(lR)- 2_[(6-(2•Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))carbonyl Amino]-isopropyl}-4-[(tatabutoxy)carbonylamino]-N-mercaptobutylamine N-{(lS)-2-[(6-(2-cyanobenzene) ))-2-{[2-(3-fluorophenyl)ethyl]amine 83 200823188 KL-based)) arylamino]-isopropyl bromide 2-amino-N-methylacetamide Ν «ΐδ)ι[(6·(2_Cyanophenyl)>2_{[2 fluorophenyl)ethyl]amine earth}(3 σ 疋 )))) arylamino]-isopropyl b 4_Amino_ν_methylbutanamine N-«m)i[(6-(2-cyanophenyl)-2-{[2_(3-fluorophenyl)ethyl]amino}( l base)) alkylamino]-isopropyl}_2-aminoacetamide N_«lR)l [(6-(2_cyanophenyl)2_{[2_(3_ iphenyl)) Amino](indolyl)(carbonyl)aminocarbonyl]-isopropyl}_4-aminobutyric acid R)_2-[(6-(2-cyanophenyl)_2_{[2_(3_ Fluorophenyl)ethyl]amino}(3·-pyridyl))carbonylamino]-isopropylbutanyl 4-amino-N-methylbutyramine N_{(lR)-2_[(6_ (2-cyanophenyl group from fluorophenyl)ethyl]amino}(3-pyridyl))carbonylamino]-isopropyl}_2-amino group with _methylacetamide (5- Fluor-2-{[2-(3-fluorophenyl)ethyl]aminobib 6_(1_methylσpyrazole_4_yl) (3"pyridinyl))_Ν_(3_pyridylmethyl) )carbamamine N_{[(2R)- 1-(2-Aminoethyl)pyrrolidinyl-2-yl]methyl}(6-(2-cyano basic)_2-{[2-(3-fluorophenyl)ethyl]amino}(3) _Roar. Basement)) Indoleamine N-{[(2R)-1—(4-aminobutylidene)pyrrolidin-2-yl]methyl}(6-(2-cyano basic)-2-{[2-( 3-fluorophenyl)ethyl]amino} (3_σ ratio bite)) indoleamine N-{[(2R)-l-(3-aminopropyl)-5-oxypi ratio slightly bite_ 2_yl]methyl}(6_(2_cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_σ-pyridyl))carbenamide (2-{ [2-(3-Fluorobenzyl)ethyl]amino}_6· σ 嗤_4_yl (3_吼口定基))_Ν_(3-σ比ϋ定基methyl)carboxylic acid amine {6-( 3-Chlorophenyl)_2_[(2-(2-acridinyl)ethyl)amino Κ3_ σ-pyridyl WNP·13 than dimethylmethyl) amide {2-[(2-(2-) Methyl)amino][3-(trifluoromethyl)phenyl](3_吼84 200823188 pyridine)}-N-(3-pyridylmethyl)decylamine {6 -[3-(Dimethylamino)phenyl]-2-[(2-(2-acridinyl)ethyl)amino](3-'pyridyl)}-N-(3-pyridyl)曱 曱醯) guanamine. {6-(2-murine phenyl)-2-[(2·(2- σ 咬)ethyl)amino]](3-吼ϋ定5基)}-Ν -(3-pyridylmethyl)formamide {6-(2-mercaptophenyl)-2-[(2-(2-oxaridinyl)ethyl)amino](3-acridinyl) }_N-(3-Pyridylmethyl) A Indole {6-(2-decyloxyphenyl)-2-[(2-(2-acridinyl)ethyl)amino](3-acridinyl)}-N-(3-pyridyl) Methyl)carbamamine ίο {6-(2-oxycarbyl)-2-[(2-(2-indolyl)ethyl)amino](3-°-specific)}-N-( 3-pyridylmethyl)guanamine {2-[(2-(2-)-yl)ethyl)amino]_6-(2- 11-septyl) (3- 0 sigma) -Ν-(3-Pyridylmethyl)carbamamine {6-(4-ethylphenyl)_2-[(2-(2-^^^)yl)ethyl)amino](3-^ ratio Mouth 15 base)}-Ν-(3-pyridylmethyl)carbamamine {6-(4-mercapto(2-thienyl))-2-[(2-(2-acridinyl)) (amino)(3-acridinyl)}-N-(3-pyridylmethyl)decylamine {6-(3-pyridyl)-2-[(2-(2-111 ratio) σ定)ethyl)amino](3-indolyl)}-indole-(3-pyridylmethyl)carbamamine 20 {6-(3-decyloxyphenyl)-2-[(2 -(2-acridinyl)ethyl)amino](3-acridinyl)}-N-(3-pyridylfluorenyl)decylamine {6-(3-cyanophenyl)-2- [(2-(2-.pyridyl)ethyl)amino](3-acridinyl)}-N-(3-pyridylfluorenyl)carbenamide {6-(3,5-dimethyl Phenyl)-2-[(2-(2-acridinyl)ethyl)amine ](3-Acridine 85 200823188)}-N-(3-Acridinemethyl)guanamine {6-(3,4-dimethylphenyl)-2-[(2-(2· -pyridyl)ethyl)amino](3_mouthpyridinyl)}-N-(3-acridinylmethyl)decylamine • {6-(3_ phenyl)_2-[ (2-(2-σ ratio σ定基)ethyl)amino](3_0 to π定5 base)}-Ν-(3-pyridylmethyl)decylamine {6-(3-methylbenzene) Base)-2-[(2-(2_. (pyridyl)ethyl)amino](3_acridinyl)}-N-(3-pyridylmethyl)carbenamide (2-{[2_(4-chlorophenyl)ethyl]amino) }-6-phenyl(3-tonpyridyl))-Ν·(3-acridinylmethyl)methamine ίο {6-(2,4-dimercaptophenyl)-2-[(2 -(2-0 to dimethyl)amino)amino](3_beer nitrile)}-Ν-(3-pyridylfluorenyl) decylamine {6-(2,5-dimethylphenyl) -2-[(2-(2-Acridine)ethyl)amino](3-acridinyl)}-N-(3-pyridylfluorenyl) decylamine {6-(4-曱) (3-thienyl))-2-[(2-(2-u-pyridyl)ethyl)amino](3-acridinyl 15yl)}-N-(3-pyridylfluorenyl)fluorene Indoleamine (2_{[2-(3-methoxyphenyl)ethyl]amino}-6-phenyl(3-acridinyl))-N-(3 j-pyridylfluorenyl)fluorene Amine (2_{[2·(3-fluorophenyl)ethyl]amino}-6-phenyl(3-acridinyl))-N-(3-hydroxypyridylmethyl)decylamine 2〇{ 2-[(2-(2-indolyl)ethyl)amino]-6-(3- σ-septyl)(3-.Butyl)}-Ν-(3-pyridylfluorenyl)曱醯amine {6-(2-chlorophenyl)-2-[(2-(2-pyridylpyroxy)ethyl)amino](3-indenium σ-based)}-Ν-(3- Pyridyl indenyl) decylamine (2-{[2-(2-chlorophenyl)ethyl)amine }--6-phenyl(3-piperidinyl)),-(3-port ratio 86 200823188 pyridine fluorenyl) formamide (2-{[2-(2-methoxyphenyl)ethyl) Amino group _6_stupyl (3_^ 唆' group))-Ν-(3_acridinylmethyl) decylamine (2-{[2-(2.methylphenyl)ethyl) Amino}_6_phenyl (3_u-pyridyl))_Ν·(3_ 5 pyridylmethyl)decylamine (2-{[2-(2-fluorophenyl)ethyl]amino}_6_benzene Base (3" to π-base))_Ν_(3_σ-pyridyl-fluorenyl) decylamine (2-{[2-(2,6-difluorophenyl)ethyl]aminophenyl) (3_ σ ratio bite Base))-N_(3-u-pyridylmethyl)decylamine 1〇(2-([2-(3,5-difluorophenyl)ethyl]amino}}_6_phenyl (3_ σ) Bisyl))-N-(3-u-pyridylmethyl)decylamine (2-{[2-(3,4·difluorophenyl)ethyl]amino}}_6_styl (3_ ^Bit base))-Ν-(3-acridinylfluorenyl) decylamine (2-{[2-(2,5-difluorophenyl)ethyl]amino}}_6•phenyl (3_ u ratio bites 15))-N-(3-u-pyridylmethyl)decylamine [6-phenyl-2-Q2-[3-(trifluoromethyl)phenyl]ethyl}amine (3_ σ-pyridyl)]-yi (3-吼2-methyl)carbamamine (2-{[2-(3-fluorophenyl)ethyl]amino}}_6_(4-indenyl) 2-11 thiophene)) (3_吼Base))-Ν-(3-acridinylfluorenyl)carbamamine 20 (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(3_ spur) 3_^比^定基))-Ν-(3-acridinylmethyl)carbamamine (2- {[2_(2-alkyl)ethyl]amino}phenyl) (3_11 than u) )_Ν(3 pyridylmethyl)carbamamine (2- {[2-(3-carbyl)ethyl]amino) 6-phenyl (3-!? ratio u))_ν (3 87 200823188 pyridyl fluorenyl)carzamide-(2-{_[2-(4-p-phenylphenyl)ethyl]amino}-6-phenyl(3-^ ϋ ϋ))-N-( 3_ 'Pyridylmercapto) decylamine (2-{[2-(2-hydroxyphenyl)ethyl]amino}-6-phenyl(3·^pyridyl))-N-(3_ 5 Pyridylmethyl)decylamine (2-{[2-(4-aminophenyl)ethyl]aminobiphenyl 6-phenyl(3-acridinyl))-N-(3-pyridylhydrazine Methionine 3-[2-({6-phenyl-3-[N-(3-Acridinesulfonyl)aminecarbamyl]-2-acridinyl}amino)ethyl]benzene Methionine ίο (2- {[2-(3,5-difluorophenyl)ethyl]amino} -6-(3-thienyl)(3•acridinyl))-N-(3- Acridine methyl)carbamamine (2-{[2-(3,5-difluorophenyl)ethyl]amino}-6-(4-indolyl(2-thienyl))(3- Pyridyl))-N-(3-pyridylfluorenyl)fluorene (2-{[2-(3,5-Difluorophenyl)ethyl]amino}_6-(2-cyanophenyl)(3-acridinyl 15yl))-N-(3-acridine Methyl) decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(2-thienyl)(3-acridinyl fluorenyl) amide ( 2-{[2-(3,5-Difluorophenyl)ethyl]amino}-6-(2-thienyl)(3-acridinyl))-N-(3-pyridylmethyl)- Indole 2〇3-[2-({6-本基-3·[Ν-(3-ϋ比ϋ定基基基) amine 曱 ]]]]-2-yl ratio 11 base} Amino)ethyl] Methyl benzoate 2-(6-{[2-(3-fluorophenyl)ethyl]amino}-5-[N-(3_u-pyridylfluorenyl)amine fluorenyl]-2-pyridine Benzobenzamide (6-(4-fluorophenyl)_2-{[2_(3-fluorophenyl)ethyl]amino} (3_. Bispin 88 200823188 base))-N-(3-pyridylfluorenyl) decyl 3-[2-({6-phenyl-3-[N-(3-acridinyl) fluorenyl) .]]][Athranyl]-2-amino]benzoic acid (6-(2-chloro-4-fluorophenyl)-2.{[2-(3-fluorophenyl)ethyl] Amino}(3_ϋ 咬5 base))-Ν-(3-acridinylfluorenyl) decylamine (2-{[2-(3,5-difluorophenyl)ethyl]amino}- 6-(4-fluorophenyl)(3·-pyridyl))_N-(3^pyridinyl)carbamidine (2-{[2-(4-phenylphenyl)ethyl)amine } -6 phenyl (3-indole hydrazide)) -N-(3-mouthpyridinyl) guanamine ίο {6-(2_light phenyl)-2-[(2 -(2-indole 0-butyryl)ethyl)amino](3-indole-butoxy)}-indole-(3-acridinylmethyl)carbenamide {6-(4-hydroxyphenyl)- 2-[(2-(2-Acridine)ethyl)amino](3-acridinyl)}-N-(3-acridinylmethyl)decylamine (6-(2-murine) -4- disordered phenyl)-2-{[2-(3-(phenyl)ethyl]amino}}(3-.pyridyl))-N-(3-acridinylmethyl)formamidine Amine 15 (6-(2-chloro-6-gasphenyl)-2-{[2-(3-(phenylphenyl)ethyl)amino}} (3 _ ^ σ 定 base))-Ν-(3 -Acridinemethyl)carbamamine (6-(2-a-5-methoxyphenyl)-2-{[2-(3-)phenyl) Amino](3_ϋpyridinyl))-Ν-(3-indolylfluorenyl)guanamine (6-(2-carbyl-6-phenylphenyl)-2-{[2-( 3-(phenyl)ethyl]amino}(3-吼2〇))-N-(3-acridinyl) decylamine (6-(2-fluorophenyl)-2-{ [2-(3-Fluorophenyl)ethyl]amino}(3-indenyl)-indole-(3-acridinylfluorenyl)carbenamide (6-(2-carbyl-5) -nonyloxyphenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3 _ acridine))-N-(3-acridinyl) decylamine 89 200823188 (2-{[2_(2,3-Difluorophenyl)ethyl]amino}·6-(2-cyanophenyl)(3-acridinyl))-Ν_(3-acridine Shame methyl) guanamine. . _ (6-(2-chloro-5-fluorophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino) (3- 0 ϋ Basement))-Ν-(3-acridinylfluorenyl) decylamine 5 (6-(2-murine-5-murine phenyl)-2-{[2-(3-phenylphenyl)ethyl J-amino}(3-indole σ-based))-Ν-(3-acridinylfluorenyl)formamide (6-(3-fluorophenyl)-2-{[2-(3-fluorobenzene) Ethyl]amino}amino}(3-acridinyl))-N-(3-acridinylfluorenyl)carbenamide (6-[2-(cyanoindolyl)phenyl]-2-{ [2-(3-Fluorophenyl)ethyl]amino}(3-port ratio ίο pyridine))-N-(3-pyridylfluorenyl) decylamine (2- {[2-(3-Fluorophenyl)ethyl]amino}-6-[3-(hydroxymethyl)(2-thienyl)](3-acridinyl))-N-(3-吼Amidyl hydrazide (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(5-methylindolyl (3-thienyl))(3-pyridyl) )-N-(3 _Pyridylmethyl)decylamine 15 (2-{[2-(3-fluorophenyl)ethyl]amino}-6-[5-(hydroxyindenyl)(3- Thienyl)](3-acridinyl))-N-(3-pyridylfluorenyl)decylamine (6-(2-chloro-4-methylphenyl)-2-{[2-(3) -fluorophenyl)ethyl]amino}(3-acridinyl))-N-(3-acridinylfluorenyl)carbenamide (6-(2-cyano-4-nonylphenyl) -2-{[2-(3-fluorophenyl)ethyl]amino} (3-port ratio 2 aridinyl))-N-(3-pyridylfluorenyl)carboxamide (2-{[ 2-(3-Fluorophenyl)ethyl]amino}-6-[3-(hydroxyindenyl)phenyl](3-hydroxypyridyl)-N-(3-acridinylfluorenyl) Indoleamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-[3-(methoxyindolyl)phenyl](3-pyridyl))-N-( 3-pyridylmethyl)decylamine 90 200823188 =-(1Η切,4-tetrasyl)_2_{[2(3fluorophenyl)ethyl.yl}(3-acridinyl))_N_(3_nfc Acridine-based decylamine (=-[2-lactohydroxymethyl)phenyl]_2_{[2_(3-fluorophenyl)ethyl Earth } (3-. Specific base)) -N_(3_n than 曱 base) formamide (2R)

基K3-吼唆基))縣胺基]_N_曱基丁賴 ]&C (=)-2_胺基_4|(2_氰基苯基)_2_{[2-(3_氣苯基） 基}(3-吡啶基))羰基胺基]_N_曱基丁醯胺 ΓΓΐ Ϊ汶羥基丙基)(6_(2_氰基苯基)-2·(3_氟_ 乙基]胺基}(3』比u定基》甲醯胺 =-[(2-{[(弟三丁氧基）羰基胺基]甲基八3_吡啶基 二氛基笨基)一氣苯基)乙基]胺基}(一 15 20 氣 =)乙細基}.6-苯基(3.^基肺似 =r=f)rr基)而}(2.{[2.(3_氟笨基)乙基] 月女基}-6-本基(3-吡啶基乃甲醯胺 苯基m(2_(2心基）乙基)胺基](3-_ 土 }} N-(3_口比σ疋基甲基〉曱酸胺 =-(胺基甲基)(3,基)]甲基}(2侧域苯基)乙基] 月女基}-6-吡唑_3·基(3_吡啶基)）甲醯胺 基甲基)(3,基)]甲基}(2侧3_氣苯基)乙基] (1〒基口比嗤""4_基乂3』比"定基》甲酸胺N-[((3R)(3_ 氏疋土））甲基](6|氰基苯基於{j>(3_氣苯基）乙基]胺 91 200823188 基}(3-吡啶基)）甲醯胺 (6-(2'氰基苯基）_2_{[；2-(3-氟苯基）乙基]胺基}(3_ σ比啶 基))-Ν-(4-派唆基甲基）甲驢胺 Ν-{[1_(2_胺基乙醯基哌啶基曱基你_(2_氰基笨 基)-2_{[2_(3-氟苯基）乙基]胺基》(3_σ比啶基)）甲醯胺 Ν_{[Η3_胺基丙醯基形_哌啶基）]曱基从6_(2_氰基笨 基)-2-{[2-(3-氟苯基）乙基]胺基}(3_。比啶基)）曱醯胺 N-{[(3S)-l-(2-胺基乙醯基)(3_哌啶基曱基}(6_(2_氰基苯 基)-2_{[2-(3-氟苯基）乙基]胺基}(3_σ比啶基)）甲醯胺 n_{[(3s)-i_(3_胺基丙醯基）…辰啶基)]甲基}(6_(2_氰基苯 基)_2_{[2-(3-氟苯基）乙基]胺基}(3_吡啶基)）曱醯胺 ϊ=[(1-乙醯基(4-哌啶基)）甲基](6-(2_氰基苯基)_2-{[2_(3_氟 苯基）乙基]胺基}(3_π比咬基)）甲醯胺 N_[((3S)小乙酸基（3_哌啶基））曱基](6_(2_氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3_σ比啶基)）甲醯胺 Ν-{[1-(4-胺基丁醯基）(4-π底啶基）]甲基）(6-(2-氰基苯 基)-2-{[2-(3-氟笨基）乙基]胺基}(3_σ比咬基)）甲醯胺 4-{[(6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基卜3-。比咬 基)幾基胺基]甲基}σ辰咬叛酸曱酯 N-[((2R)(2-旅咬基))曱基](6_(2•氰基苯基)_2_{[2_(3_氟苯基) 乙基]胺基}(3-0比。定基)）曱酸胺 N-{[(2R)_ 1 -〇胺基乙醯基乂2_旅啶基)]甲基}(6_(2_氮基苯 基)-2_{[2-〇氟苯基）乙基]胺基}(3』比啶基)）曱醯胺 N-{[(2R)-l-(3-胺基丙醯基)(2_旅啶基)]曱基}(6_(2_氰基苯 92 200823188 基)-2-{[2-(3-氟苯基）乙基]胺基}(3_σ比啶基》甲醯胺 Ν_{[(·-1-(4,基丁醯基)(2_旅咬基)]甲基}(6_(2_氮基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3^比咬基)） 聊糾乙酿基（2-派唆基））甲基基苯 5 基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吡啶基)）甲醯胺 (叫2-{[(6-(2-氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基你 吼咬基))叛基胺基]甲基}旅。定致酸甲酯 N-({(2R)-l-[(3-胺基丙基)續醯基](2_派啶基甲基州2_ 氮基苯基)-2-{[2-(3-氣苯基）乙基]胺基}(3“比咬基))甲酸胺 1〇 柯⑹卟1-甲基（2_旅咬基））甲基](6-(2-氰基苯 基)-2-{[2_(3-氟苯基）乙基]胺基}(3^比啶基))甲酸胺 • N_{[(2R)小((2R)-2,3-二胺基丙醯基）(2-哌啶基）]曱 基}(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3♦定 基)）甲醯胺 15 队爪汉)小((汉)_2,4-二胺基丁酸基）(2-哌啶基）]甲 基}(6-(2·氰基苯基)-2-{[2-(3_a苯基）乙基]胺基}(3+定 基)）甲醯胺 N_{[(2R)-H(2R)-2,5-二胺基戍醯基）(2_哌啶基）]曱 基}(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3“比唆 2〇 基)）曱醯胺 n_({(2r)-h(2_胺基乙基)礦醯基定基甲基 氮基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3“比咬基))甲酿胺 N-{[(2R)-l-((2S)-2,5-二胺基戊醯基）(2_ 哌啶基）]甲 基}(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼咬 93 200823188 基)）曱醯胺 5 10 15 20 N-{[(2R)-1-((2S)_2-胺基丙醯基)(2-旅唆基)]甲基}(6-(2-氰 基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-π比咬基)）甲醯胺 N_{[(2R)-l-((2R)-2-胺基丙醯基)(2-旅口定基)]曱基⑽心-氰 基苯基)_2-{[2_(3-敗苯基）乙基]胺基}(3_吼σ定基)）甲酿胺 (2R)-2-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基)(孓 吼啶基))羰基胺基]甲基}哌啶羧酸2-氯乙基酯 (2R)_2_{[(6_(2_氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基 ϋ比咬基))羰基胺基]甲基} 12辰咬叛酸胺基乙基酯 N-{[(2R)-1_(4-胺基丁 醯基）吡咯啶基]甲基}(2_{[2_(3 ^ 二氟苯基）乙基]胺基卜6_(2_氰基苯基)(3“比咬基))甲醯胺 N-{[(2R)-l-(4-胺基丁酿基)鱗咬_2_基]甲基}氛 基)_2_[(2·環己-1-烯基乙基)胺基](3_π比咬基)}甲_ 3 {[3 (N {[(2R)-l-(4_胺基丁酿基)π比略咬_2_基]甲基}胺 酿基)-6-(2-氰基苯基)(2+定基)]胺基}_ν，ν_二甲基丙酿 胺Base K3-mercapto)) county amine group]_N_mercaptobutylene] &C (=)-2_amino group_4|(2_cyanophenyl)_2_{[2-(3_气Phenyl) phenyl}(3-pyridyl))carbonylamino]]N-mercaptobutylamine ΓΓΐ Ϊ 羟基 hydroxypropyl)(6-(2-cyanophenyl)-2·(3_fluoro-ethyl Amino} (3) is more than a given group of meglumine =-[(2-{[(ditrimoxy)carbonylamino]methyl octa-triphenyl-diyl) phenyl) Ethyl]amino}(a 15 20 gas =) ethyl group}.6-phenyl (3.^ base lung like =r=f)rr base) and (2.{[2.(3_fluorine)笨基)ethyl] 月女基}-6-benyl (3-pyridylcarbamidine phenyl m(2_(2)yl)ethyl)amine](3-_土}} N-( 3_mouth ratio σ疋 methyl group> decanoic acid=-(aminomethyl)(3,yl)]methyl}(2 side domain phenyl)ethyl] 月女基}-6-pyrazole _ 3·yl (3_pyridyl))carboxamidomethyl)(3,yl)]methyl}(2-side 3_gasphenyl)ethyl] (1〒 base ratio 嗤""4 _基乂3′′′′′′′′′′′′′′′′′′′′’’’’''''''''''''''''' 91 200823188 】}(3-pyridyl))carboxamide (6-(2'-cyanophenyl)_2_{[; 2-(3-fluorophenyl)ethyl]amino} (3_ σ ratio Base))-Ν-(4-pyrylmethyl)carbamamine-{[1_(2_aminoethylhydrazinopiperidinyl) _(2-cyanophenyl)-2_{[ 2-(3-fluorophenyl)ethyl]amino"(3_σ-pyridyl))carboxamide Ν{{Η3_aminopropionyl-piperidinyl]]fluorenyl from 6-(2-cyano) Styrene)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_.pyridyl))indoleamine N-{[(3S)-l-(2-amino-ethyl (3)piperidinyl fluorenyl}(6-(2-cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl]amino}(3_σ-pyridyl))carboxamidine Amine n_{[(3s)-i_(3_aminopropenyl)... succinyl)]methyl}(6_(2-cyanophenyl)_2_{[2-(3-fluorophenyl) Amino](3_pyridyl)) amidoxime = [(1-ethylindenyl(4-piperidinyl))methyl](6-(2-cyanophenyl)_2-{[ 2_(3-fluorophenyl)ethyl]amino} (3_π ratio), formamide N_[((3S) small acetate (3-piperidinyl)) fluorenyl] (6_(2-cyano) Phenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_σ-pyridyl))carbenamide-{[1-(4-aminobutylidene) (4- π 啶 基 ))] methyl) (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3_σ ratio) 4-{[(6-(2-cyanophenyl)-2-{[2-(3- Fluorophenyl)ethyl]aminopurin-3-. N-[(2R)(2-Butyl))]]] 2_(3-fluorophenyl)ethyl]amino} (3-0 ratio. base)) decanoic acid N-{[(2R)_ 1 -nonylaminoindolyl 2 _ pyridine)] Methyl}(6_(2-nitrophenyl)-2_{[2-fluorenylphenyl)ethyl]amino}(3′′pyridinyl))decylamine N-{[(2R)-l -(3-Aminopropenyl)(2_Bistidyl)]fluorenyl}(6_(2-cyanobenzene 92 200823188)-2-{[2-(3-fluorophenyl)ethyl] Amino}(3_σ-pyridyl)carboxamide Ν{{(·-1-(4, butyl decyl)(2_Benbityl)]methyl}(6_(2-nitrophenyl)-2- {[2-(3-Fluorophenyl)ethyl]amino} (3^ than bite)) 纠 乙 乙 (2-派唆基)) methyl phenyl 5 yl)-2-{[ 2-(3-Fluorophenyl)ethyl]amino}(3-pyridyl))carbenamide (called 2-{[(6-(2-cyanophenyl)_2_{[2_(3_fluoro) Phenyl)ethyl]amino group you bite base)) tetamine group] methyl} brigade. Methyl carboxylic acid N-({(2R)-l-[(3-aminopropyl)] hydrazino] (2-p- pyridylmethyl state 2_nitrophenyl)-2-{[2- (3-Phenylphenyl)ethyl]amino} (3" than butyl)) formic acid amine 1 〇 (6) 卟 1-methyl (2 _ 咬 ))) methyl] (6-(2-cyanide) Alkyl phenyl)-2-{[2_(3-fluorophenyl)ethyl]amino}(3^pyridyl))carboxylic acid amine • N_{[(2R) small ((2R)-2,3- Diaminopropionyl)(2-piperidinyl)]fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}( 3♦定基))carbamamine 15 team claws) small ((han) 2,4-diaminobutyric acid) (2-piperidinyl)]methyl} (6-(2·cyanophenyl) )-2-{[2-(3_aphenyl)ethyl]amino}(3+decyl))carbenamide N_{[(2R)-H(2R)-2,5-diaminodecyl) (2-piperidinyl)]fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3" than 唆2〇 Base)) indoleamine n_({(2r)-h(2_aminoethyl)indole decylmethylnitrophenyl)-2-{[2-(3-fluorophenyl)ethyl] Amino} (3" than a butyl group)) Alanine N-{[(2R)-l-((2S)-2,5-diaminopentenyl)(2_piperidinyl)]methyl} (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3-bite 93 200823 188 base)) indoleamine 5 10 15 20 N-{[(2R)-1-((2S)_2-aminopropenyl) (2-teletonyl)]methyl}(6-(2- Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-π ratio) carbamide N_{[(2R)-l-((2R) -2-aminopropyl fluorenyl) (2-branched aryl)] fluorenyl (10) heart-cyanophenyl)_2-{[2_(3-phenylphenyl)ethyl]amino} (3_吼σ Basement)) mercaptoamine (2R)-2-{[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino)(acridinyl) )) carbonylamino]methyl}piperidinecarboxylic acid 2-chloroethyl ester (2R)_2_{[(6_(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amine Base ϋ 咬 base)) carbonylamino] methyl} 12-bit bite acid aminoethyl ester N-{[(2R)-1_(4-aminobutylidene)pyrrolidinyl]methyl} (2_{ [2_(3^Difluorophenyl)ethyl]aminobib 6_(2-cyanophenyl) (3" than butyl))carbamide N-{[(2R)-l-(4-amine Butyl ketone) scale bite _2_yl]methyl} aryl)_2_[(2·cyclohex-1-enylethyl)amino] (3_π ratio) _ 3 {[3 ( N {[(2R)-l-(4_Aminobutyryl)π ratio slightly biting _2_yl]methyl}amine aryl)-6-(2-cyanophenyl)(2+) Amine}_ν,ν_dimethylpropanol

Va)Tu2(-1 本基)-2-[(2-本基乙基)胺基](3_吡啶基）}甲醯胺 ^{[(2RH-(4-胺基丁醯基)料咬_2_基]甲基丨㈣2-氛芙 N:i[(、27R)婚胺基丁 _料2_基]甲基Η6·(2-氰基 94 200823188 N-{[(2R)-l_((2S)-2,3-二胺基丙醯基）σ比咯啶_2_基]甲 基}(6_(2_氰基苯基氟苯基）乙基]胺基}(3_σ比啶 基)）甲醯胺 N_{[(2R)-l-((2S)-2_胺基-3-甲氧基丙酸基）σ比咯唆_2_基]曱 基}(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-π比咬 基)）甲醯胺 N_{[(2R)-l_((2S)-2-胺基-3_經基丙驢基）σ比咯务2-基]曱 基}(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3_吼啶 基)）甲醯胺 Ν-{[2-(胺基甲基)(3-π比啶基)]曱基}(5_氟_2_{[2_(3_氟苯基) 乙基]胺基}_6』比唾_3_基(3_σ比咬基)）甲醯胺 N-{[(2R)-l-(2-胺基乙醯基）吼咯啶-2_基]甲基》(5_氟 -2-{|；2-(3-氟苯基）乙基]胺基比唾_3_基(3_σ比淀基)）甲醯 胺 N-{[(2R)-l-((2S)-2-胺基_3_羥基丙醯基）,比咯啶_2_基]甲 基}(5-氟-2-{[2-(3_氟苯基）乙基]胺基卜6_σ比唑_3_基(3 比口定 基)）甲醯胺 n_{[(2R)-1-((2S)_2-胺基丙酿基）吼略咬_2_基]曱基}(5-氟 -2-{[2-(3-氟苯基）乙基]胺基}-6^比唾_3-基(3-11比淀基)）甲酿 胺 N_{[(2R)_l-(4-胺基丁醯基）吼咯啶_2_基]甲基}(5•氟 -2-{I；2-(3-氟笨基）乙基]胺基卜6-吡唑—3-基(3-吡啶基)）甲醯 胺 脱 {6-(2-氰基苯基)_2-[(2-氧雜戊環_2_基乙基）胺基](3“比唆 95 200823188 基)}-Ν-(3-σ比ϋ定基曱基）曱酸胺 N_((2R)_2-胺基丙基）(5-氟_2_{[2-(3·氟苯基）乙基]胺 基}-6-(1-曱基吼唾-4-基)(3-°比咬基)）甲酿胺 N-{(1 R)-2-[(5-氟-2-{[2-(3_ 氟苯基）乙基]胺基甲基 口比唾_4_基）（3-u比唆基))幾基胺基]_異丙基卜2_[(第三丁氧基） 羰基胺基]乙醯胺N-{(lR)-2-[(5-氟-2-{[2_(3_氟苯美J二 胺基}修甲基棒4.基)(3._基)^基^=] 基}-2-胺基乙醯胺 N-[((2R)-5-氧基吼咯啶-2-基）曱基](5_氟_2_{[2_(3_氟苯基） 乙基]胺基}_6_(1-曱基吼唑_4_基)(3_π比咬基)）甲酿胺 N_{(lS)-2-[(5-氟-2-{[2-(3-氟苯基）乙基]胺基}_6_(1_曱基 吡唑-4-基）(3-吡啶基))羰基胺基]_異丙基卜2_胺基乙醯 胺 N-{(1R)_2_[(5·氟-2_{[2-(3-氟苯基）乙基]胺基卜甲 基口比哇冬基)(3•吼啶基))幾基胺基p異丙基卜2，基乙 醯胺 N-{(lR)-2-[(5-氟-2-{[2_(3-氟苯基）乙基]胺基卜6_(1_曱基 口比唑-4-基)(3-咐啶基))羰基胺基]_異丙基}_4_[(第三丁氧基） 羰基胺基]丁醯胺 N_{(1R)_2_[(5H{[2_(3_氟苯基）乙基]胺基}冬(1_甲基口比 唑-4-基)(3-吡啶基))羰基胺基]_異丙基卜4-胺基丁醢胺 N-{(2R)-2-[(2_曱氧基乙基)胺基]丙基}(5备2-{[2_(3_氟苯 基）乙基]胺基}冬(1_曱基π比唾_4_基砂吼啶基》甲醯胺 N_{(2R)_2_[(第三丁氧基)幾基胺基]丙基阶氣冬似分氟 96 200823188 苯基）乙基]胺基}-6-吼嗤-4-基(3-°比唆基)）甲酿胺 N_((2R)-2-胺基丙基）(5-氟1{[2-(3-氟_苯基）乙基]胺 基} _6-σ比口坐-4-基(3-吼唆基)）甲醯胺 N-{(lR)-2-[(5-氟-2-{[2-(3-氟苯基）乙基]胺基}_6_(1_甲基吼 唾冰基)(3』比啶基))幾基胺基]_異丙基}乙醯胺 土 N-{(2R)-2-[(曱基磺醯基)胺基]丙基}(5_氟_2_{[2-(3_氟苯基) 乙基]胺基卜6-(1-甲基吡唑-4-基）（3-吡啶基)）曱醯胺 N_ {(1 R)_2_[(5_氟{[2_(3_氟苯基）乙基]胺基）_6_吼嗤冰 基(3·-比啶基))羰基胺基]-異丙基}_2_胺基乙醯胺 (5-氟-2- {[2-(3-氟本基）乙基]胺基卜6_吼σ坐_4_基（3_吼ti定 基))-1^-(2-吼唆基甲基）甲驢胺 N-{(2R)-2-[(2’基乙基)胺基]丙基氣苯基） 乙基]胺基卜6-(1-曱基吡唑-4-基)(3-吡啶基)）曱醯胺 N-{(2R)_2_[(胺甲酸基甲基）胺基]丙基}(5_氟_2_似_(3_氟 苯基）乙基]胺基卜6-(1-甲基吡唑-4-基)(3_吡啶基)）甲醯胺 N-{(1R)_2_[(5-氣_2_{[2_(3_氟苯基）乙基]胺基卜卜(卜甲基 比唾-4·基)(3-°比。疋基))幾基胺基]_異丙基卜2_(二甲基胺基） 乙酸胺 N-{(lR)-2-[(5-氟-2-{[2-(3-說苯基）乙基]胺基}_6仆甲基 吡唑-4-基)(3-吡啶基))羰基胺基]_異丙基}(2S)_2_[(第三丁 氧基)叛基胺基]-3-經基丙酸胺 N-{(lR)-2-[(5-氟-2-{[2-(3_氟苯基）乙基]胺基外⑴甲 基吡唑-4-基）(3-吡啶基)）羰基胺基]_異丙基}(28)_2_胺 基-3-羥基丙醯胺 97 200823188 N-{(lR)_2-[(5-氟-2-{[2-(3-氟苯基）乙基]胺基甲基 ， 吼哇I基)(3_吼啶基))幾基胺基]_異丙基卜2_胺基1甲基 丙隨胺 n-(4-{6-[(2_(2』比啶基）乙基)胺基]冬[N_(3_吡啶基甲基)胺 5 甲酿基定基}苯基）乙酿胺 N-((1R)-1_{[(5_氟-2-{[2_(3-氟苯基）乙基]胺基}-6-(1_ 曱基 吼唾_4_基)(3_吼啶基))幾基胺基]曱基丨丙基)_2_[(第三丁氧 基)羰基胺基]乙醯胺 N-((lR)-l-{[(5-氟_2-{[2-(3-氟苯基）乙基]胺基卜6-(1-甲基 1〇 吡唑基）(3-吡啶基))羰基胺基]甲基}丙基）-2-胺基乙醯 胺 • N ((lR)-l-{[(5-氟_2-{[2-(3 -氟苯基）乙基]胺基比唾 基(>比咬基))幾基胺基]曱基}丙基)_2_[(第三丁氧基德基 胺基]乙酿胺 Ν ((1 R)-l-{[(5-氟-2-{[2-(3_氣苯基）乙基]胺基卜6-σ比唾一4_ 基(3-啦啶基))羰基胺基]甲基丨丙基)_2_胺基乙醯胺 N {(lR)-2-[(5_氟_2-{[2_(3_氟苯基）乙基]胺基卜6-(ι_甲基 吡唑基)(3_吡啶基))羰基胺基l·異丙基}(2S)_2-胺基丙醯 胺 2〇 N-((2R)士經基士甲基丁基)(5_氟_2_ {[2分氟苯基）乙基] 胺基甲基吡唑_4-基)(3·吡啶基)）甲醯胺 (胺基甲基）(3_,比啶基)]甲基}(6_(2_氰基苯 基)-2·{[2-(3_氟苯基）乙基]胺基}(3_σ比々基》甲酿胺 Ν-{[2-(胺基甲基)(3_σ比咬基)]甲基}(2鲁㈣苯基亿基] 98 200823188 胺基}-6-吡唑-4-基(3-吡啶基)）甲醯胺 (6-(2-氧基苯基）-2-{[2-(3-氣·苯基）乙基]胺基}(3-σ比ϋ定 • 基))-Ν-(3-吡啶基曱基）曱醯胺 * {6-(4-乙驢基本基）-2-[(2-(2-11比σ定基）乙基）胺基](3-11比唆 5 基)}-Ν-(3-吡啶基曱基）曱醯胺 4-{6-[(2-(2-吼啶基）乙基）胺基]-5-[Ν-(3-吼啶基曱基）胺曱 醯基]-2-吼啶基}苯曱酸曱酯 {2-[(2-(2-啦啶基）乙基）胺基]-6-[4-(三氟曱基）苯基](3-口比 啶基）}-Ν-(3-吡啶基甲基）甲醯胺 ίο 4-{6-[(2-(2-吼啶基）乙基）胺基]-5-[Ν-(3-吼啶基甲基）胺曱 醯基]-2-u比啶基}苯甲酸 Ν-(3-口比啶基曱基）{6-(4-口比啶基）-2-[(2-(2-吼啶基）乙基）胺 基](3-吡啶基）}曱醯胺 Ν-(3-吼啶基曱基）{6-(2-吼啶基）-2_[(2-(2-啦啶基）乙基）胺 15 基](3-吡啶基）}甲醯胺 {6-(3,4-二氮苯基）-2·[(2-(2-吼ϋ定基）乙基）胺基](3-ϋ比σ定 基）}-Ν-(3_吡啶基甲基）曱醯胺 {6-[4-(羥基甲基）苯基]-2-[(2-(2-吼啶基）乙基）胺基](3-吼 啶基)}-Ν-(3-吡啶基曱基）曱醯胺 2〇 {6-(4-曱氧基苯基）-2-[(2-(2-咐啶基）乙基）胺基](3-吼啶 基)}-N_(3-吡啶基甲基）甲醯胺 {6-(4-曱基笨基）-2-[(2-(2-吼啶基）乙基）胺基](3-吼啶 基）}-N_(3-吡啶基甲基）甲醯胺 {6·(4-氯苯基）-2-[(2-(2-吼啶基）乙基）胺基](3-咐啶 99 200823188 基)}-Ν-(3-吼啶基甲基）甲醯胺 {6-(4'氟苯基）-2_[(2-(2-吼啶基）乙基）胺基](3_ π比啶 Α 基)卜队(3_吼啶基甲基）甲醯胺 . {6_苯基_2-[(2·(2_吡啶基）乙基）胺基](3_吡啶基）}_义(3_吡 5 啶基甲基）甲醯胺 {6-(3,4_二氟苯基）-2_[(2-(2-吡啶基）乙基）胺基](3_吡啶 基)}-N-(3_ti比咬基甲基）甲酿胺 {6_本基-2-[(2-(3-σ比咬基）乙基）胺基](3_π比咬基）卜Ν_(3_σ比 啶基甲基）甲醯胺 10 (6-[4_(二曱基胺基）苯基]_2-[(2_(2-口比啶基）乙基）胺基](3_ 吡啶基)}_Ν-(3-η比啶基甲基）甲醯胺 Ν-(3』比咬基甲基）{6_(3』比啶基啶基）乙基）胺 基](3-吡啶基）}甲醯胺 4-{6_[(2-(2』比啶基）乙基）胺基]_5_[Ν_(3_σ比啶基曱基）胺曱 I5 酉胜基]-2-0比咬基}苯甲酿胺 {2 [(2 &基-2-本基乙基)胺基]苯基(3-吼。定基)}_Ν-(3_π比 咬基甲基）甲酸胺 {2_[(2-(2·-比啶基）乙基）胺基]_6_(2_乙烯基苯基）(3_ ^比啶 基)}善(3』比啶基曱基）曱醯胺 20 {6-[2-(曱氧基甲基）苯基]_2-[(2-(2-吼啶基）乙基）胺基](3_ 也咬基)}_Ν_(3-π比啶基曱基）曱醯胺 {6-(2-曱酿基笨基）_2_[(2_(2·吼啶基）乙基）胺基]&吡咬 基)}-N-(3-吡啶基甲基）曱醯胺 (2-{[2-(3_氟苯基）_2_羥基乙基]胺基卜6_苯基吼啶 100 200823188 基))-N-(3-吡啶基甲基）曱醯胺 (6-(2_篆基本基)-2_{[2-(3_氟苯基)-2-¾基乙基]胺基}(3-n比 啶基))-N-(3_u比啶基甲基）甲醯胺 {2-[(2-(2-ϋ比唆基）乙基）胺基]-6_(1，3-三峻-2-基）(3_吼π定 基)}-N-(3-吡啶基甲基）曱醯胺 {6-(1_曱基口比唑基)_2_[(2_(2』比啶基）乙基）胺基](3』比啶 基)}-N-(3-吡啶基曱基）甲醯胺 (2 {[2_(3_氟本基）乙基]胺基卜6-(2-甲酸基(3_σ塞吩基))(3_ °比啶基))-Ν-(3-口比啶基甲基）曱醯胺 10 15 20 {6-(4_亂基本基）_2-[(2_(2- π比u定基）乙基）胺基](3_ σ比咬 基)}-Ν-(3_吼啶基甲基）甲醯胺 [2-{[2-〇氟苯基）乙基]胺基卜6_(6_([2_(3_氣苯基）乙基]胺 基卜5-[Ν-(3-吡啶基甲基）胺甲醯基](2_ π比啶基）)(3_吡啶 基AN-》吡啶基甲基）曱醯胺 (2 {[2-(3-氟本基）乙基]胺基}_6_[2-(經基甲基）(3_ σ塞吩 基)](3_吡啶基))_ν_(3-吡啶基曱基）曱醯胺 土刀 (2 {[2-(3-氟本基）乙基]胺基卜6-異u号味_4_基（3_。比口定 基))-队(3_吡啶基甲基）曱醯胺 疋 乙酿基㈣吩基))_2·{[2·㈣苯基）乙基]胺基你 t疋基))-Ν_(3』比啶基曱基）甲醯胺 (6-[3_(胺基甲基)(2_嗟吩基)]_2_ {[2_(3_氟苯基）乙基]胺 暴Η3%唆基))-Ν_(3_σ比啶基甲基）甲醯胺 軋苯基）乙基]胺基}_6_[5_(羥基乙基於噻吩 土）](3』比啶基))_Ν_(3_σ比啶基曱基）曱醯胺 101 200823188 (6-(4-氰基(3-噻吩基))-2-{[2-(3-氟苯基）乙基]胺基}(3-口比 啶基))-N-(3-吡啶基_曱基）甲醯胺 . . (6-[5-(胺基甲基）(2-σ塞吩基）]-2- {[2_(3_氣苯基）乙基]胺 基}(3-吡啶基))-Ν-(3-吡啶基曱基）曱醯胺 5 (2-{[2-(3-氟苯基）乙基]胺基}-6-(3-甲醯基(2-噻吩基))(3- 吡啶基))-N-(3-吡啶基曱基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(5-曱醯基(2-噻吩基))(3-吼啶基))-Ν-(3-吡啶基曱基）曱醯胺 (6-(5-鼠基(2-嗟吩基))-2- {[2-(3 -氣苯基）乙基]胺基} (3-π比 ίο 啶基))_Ν-(3_吡啶基曱基）曱醯胺 (6_(3,4_二氣苯基）-2- {[2-(3-氣苯基）乙基]胺基}(3- ^比σ定 基))-Ν-(3-吼啶基甲基）曱醯胺 ’ Ν-{[5-(胺基曱基）(3-吼啶基）]曱基}(6-(2-氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基)）曱醯胺（6-(2-15 氮基苯基）-2-{[2-(3-氣苯基）乙基]胺基}(3-吼口定 基))-N-{[5-(羥基甲基）（3·-比啶基)]甲基}曱醯胺 N-({5-[3,3-雙（二甲基胺基)-2-氮雜丙-2-烯基](3-吼啶基）} 曱基)(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-u比啶 基)）曱醯胺 2〇 N-{[3-(胺基曱基）(2-吼啶基）]曱基}(6-(2-氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基)）曱醯胺 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基）)-N-[(3-{[(6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺 基}(3-吼啶基))羰基胺基]曱基}(2-吡啶基)）曱基]曱醯胺 102 200823188 N-[(2-{[2-(3-氟苯基）乙基]胺基}_6_苯基（3_吼啶基》甲 基1(3-吡啶基胺基）甲醯胺. (5_氯_6_(2_氰基苯基)_2_{|>(3-氣苯基）乙基]胺基}(3』比唆 基))-Ν-(3-吼啶基甲基）甲醯胺 (5_漠_6_(2-氰基苯基)-2-{[2_(3_氣苯基）乙基]胺基}(3“比啶 基))-N_(3«%b^基甲基）〒酿胺 氰基·6-(2_氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基办吼 11 定基))-N-(3-吡啶基甲基）甲醯胺 沁[(2-氯p-t定基)）甲基](6♦氰基苯基)_2_㈣3_氟苯基) 乙基]胺基}(3-吡啶基)）曱醯胺 Υ({2-[(2-胺基乙基）胺基](3_吼啶基）}甲基)(6_(2_氰基苯 基）-2-{[2-(3-氟苯基）乙基]胺基}(3_ D比啶基））曱醯胺 (2_{[2-(3-氟苯基）乙基]胺基}_5_氧基節并[3,2刘σ比啶j 基)-Ν-(3-吼啶基甲基）曱醯胺 (6-(2-氰基苯基）_2_{[2-(3_氟苯基）乙基]胺基}(3_ σ比啶 基))_N-[(6_氧基(2_哌啶基》甲基]甲醯胺 N|{3-[(第三丁氧基)幾基胺基]丙基卜6_氧基(2_略唆基》 甲基](6-(2_氰基苯基)_2_{[2_(3_氣苯基）乙基]胺基比啶 基)）甲醯胺 Ν·{[1-(3-胺基丙基)_6_氧基(2_派π定基)]甲基}(6♦氰基苯 基)_2_{[2-(3-說苯基）乙基]胺基}(3心定基))甲醯胺（6_(2_ 就基苯基)-2-{[2·(3_氟苯基）乙基]胺基}(3Κ基肺_(2_ ϋ辰啶基甲基）甲醯胺 队[(1-{2-[(第三丁氧基）羰基胺基]乙醯基}(2_哌啶基)）甲 103 200823188 基](6_(2_鼠基苯基)1{[2♦氟苯基）乙基]胺基比啶 基)）甲醯胺 5 10 15 20 N {[1 (2-胺基乙醯基）(2_哌啶基乃甲基》(6_(2_氰基苯 基)-2_{[2_(=氟苯基）乙基]胺基你吼咬基))甲賴 N_[(l_{3_[—(第二丁氧基)幾基胺基]丙隨基你旅咬基))甲 土]( (2氰基苯基)_2][2_(3_氟苯基）乙基]胺基}(3_σ比啶 ={[1 (3-月女基丙醯基）(2-哌啶基）]甲基氰基苯 土）2 {〇(3_氟苯基）乙基]胺基办吼啶基)）甲醯胺 (6-(2-氰基苯基）_2·{[2_(3_氟苯基）乙基]胺基}(3_。比啶 基))_Ν_{[1-(甲基確酿基)(2·旅唆基曱基}甲酸胺 N_[((2R)-6_氧基（2_哌啶基》甲基](6_(2_氰基苯 基）2 {[2 (3-氟笨基）乙基]胺基》(3_σ比啶基)）曱醯胺 >^-[((2RH_{3_[(第三丁氧基德基胺基]丙基卜6_氧基(2_旅 疋基)）甲基](6_(2_氰基苯基)_2_{[2_(3_氟苯基）乙基]胺 基}(3-吡啶基)）甲醯胺 N i(2R)小(3_胺基丙基)_6•氧基(2«基)]曱基}(6-(2-氰 基苯基)-2][2_(3_氟苯基）乙基]胺基办口比咬基甲酿胺月 乙基J版基}(3』比啶基)）甲醯胺 小乙醯基(3_哌啶基))甲基](6_(2_氰基苯 基)士{[2_(3-氟苯基）乙基]胺基}(n定基))甲酿胺 =====基)乙基]_(3- 104 200823188 N_[((3R)-l-{2-[(第三丁氧基)幾基胺基]乙酿基}(3_^σ定基)) 曱基](6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3_吡啶 基)）甲醯胺 N-[((3R)-卜{3-[(第三丁氧基)羰基胺基]丙醯基}(3_哌啶基)) 甲基](6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3_σ比啶 基)）甲酸胺 N-[((3R)小{4_[(第三丁氧基)幾基胺基]丁醯基)(3«基)) 曱基](6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3_σ比啶 基)）甲醯胺 N-{[(3R)-1-(2-月女基乙醯基)(3-τι辰咬基)]甲基}(6_(2_氰基苯 基)_2-{[2-(3-氟本基）乙基]胺基}(3-11比咬基)）曱酿胺 N_{[(3R)-l-(3-胺基丙醯基)(3-哌啶基)]曱基}(6_(2_氰基苯 基)-2-{[2-(3-敦苯基）乙基]胺基}(3_π比咬基)）甲酿胺 N_{[(3R)-l-(4-胺基丁醯基)(3_哌啶基)]甲基氰基苯 基）2_{[2-(3_亂本基）乙基]胺基}(3_吼11 定基)）甲酿胺 ”（{(2以)-1_[4-(1，3_二氧基苯并[(：]嗤琳_2_基）丁基]_6_氧基 (2-哌啶基）}甲基)(6_(2_氰基苯基)_2_{[2_(3_氟苯基）乙基] 胺基}(3-吡啶基)）甲醯胺 N {[(2R)-1_(4-月女基丁基)-6-氧基(2-口辰咬基)]甲基氰 基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3_σ比淀基)）曱酿胺 N-[((3S，4S，2R，5R)-3,4,5,6_四絲(2η_3,4,5,6_ 四氫旅喃-2_ 基))甲基](6-(2-氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基}(3_ °比啶基)）甲醯胺 [5 (N {[(2R)-l-(3-胺基丙基)_5_氧基σ比略口定_2_基]甲基} 105 200823188 °定基]苯甲醯 胺甲醯基)-6-{[2-(3-氟苯基）乙基]胺基卜2_吡 Μ 5 10 15 20 N_[2-((2R)_2· {[(6_(2_ 氰基苯基)_2_ {[2_(3_ 氣苯基）乙胺 基}(3-吡啶基))羰基胺基]曱基}吡咯啶基)(ls)_^甲美 基乙基](第三丁氧基）甲醯胺 土 --乳 N_ {[(2R)_ 1 _((2S)_2-胺基丙醯基）σ比咯啶1基]甲基 氰基苯基)_2][2_(3_氟苯基）乙基；]胺基}(3』比唆基))甲 N-[(lR)-2_((2R)-2- {[(6_(2_ 氰基苯基)_2_{[2_(3_ 氟苯基皿)乙 基]胺基}(3-吡啶基))羰基胺基]甲基丨吡咯啶基甲基 氧基乙基](第三丁氧基）甲醯胺 N-{[(2R)小((2R)_2_胺基丙醯基）σ比咯啶_2_基]甲基）(6_(2 氰基苯基)-2-{R-(3-氟苯基）乙基]胺基比啶基》曱醯胺 N_{[(2R)_l_((2S)-2,5_二胺基戊醯基）σ比咯啶士基]曱 基}(6_(2_氰基苯基)-2_{[2_(3_氟苯基）乙基]胺基}^比啶 基)）甲醯胺 Ν-[(2-氯(3鲁定基)）甲基](2_{[2_(3_氟苯基）乙基]胺基卜卜 口比唾-4-基(3-0比^定基)）曱酿胺 Ν-({2-[(3-胺基丙基）胺基](3-吼啶基)}甲基)(2-{[2_(3•氟苯 基）乙基]胺基}-6-吼唾冰基(3_ϋ比。定基)）曱酸胺 Ν-({2-[(2-胺基乙基）胺基](3_π比啶基)}曱基)(2_{[2_(3_氟苯 基）乙基]fee基}-6-吼唾冰基(3-u比u定基)）曱酸胺 (2R)-2_{[(5_氟-2-{[2-(3-氟苯基）乙基]胺基}_6仆曱基吼唑 _4-基)(3-吼咬基))羰基胺基]甲基比略咬羧酸第三丁酯 n-[((2r户比洛唆1基）甲基](5_n{[2_(3_氟苯基）乙基擔 106 200823188 基）-6-(1-甲基吡唑_4_基)(3_吡啶基)）曱醯胺 [(()1 {2-[(弟二丁氧基）幾基|基]乙醯基比嘻咬_2_ 基）甲基]〇氟_2][2_(3_氟苯基）乙基]胺基卜6_(1_甲基吼唑 -4-基)(3-吡啶基》甲醯胺 (ί[2 (3氟本基）乙基]胺基卜& ^比唾冬基（3_ π比咬 土））N ({2-[(2-輕基乙基)胺基](3_π比唆基)）甲基）甲酿胺 队[(2_{[(第三丁氧基)幾基胺基]甲基}(3_σ比啶基)）曱基](5_ 氟2 {[2 (3-氟本基）乙基]胺基卜6-U比唾_4_基(3-17比τι定基)）甲 酿胺 队{[2-(胺基甲基)(3_σ比啶基)]甲基}(5-氟_2_{[2_(3_氟苯基） 乙基]胺基}«唑_4_基(3』比啶基)）甲醯胺 [((2R) 1-{2-[(弟二丁氧基）幾基胺基]乙酿基}σ比略唆_2_ 基）曱基](5-氟-2-{[2-(3-氟苯基）乙基]胺基卜6_σ比唑_4_基 (3-ϋ比咬基)）甲酿胺 N_{[(2RH_(2-胺基乙醯基）π比略咬_2_基]甲基}(5_就 _2_{[2-(3-氟苯基）乙基]胺基}_6_吡唑_4_基(3_吡咬基)）甲酿 胺 服 N [((2R)-l-(3_[(弟二丁氧基）幾基胺基]丙酸基丨。比咯咬_2_ 基）甲基](5_氟·2_{[2-(3_氟苯基）乙基]胺基卜卜吼峻冰基 (3-吡啶基)）甲醯胺 N-{[(2R)小(3-胺基丙酸基）π比嘻。定_2_基]甲基氟 _2_{[2-(3-氟苯基）乙基]胺基卜6H4-基(3-u比ϋ定基)）甲酸 胺 N_[((2R)小{4-[(第三丁氧基）幾基胺基]丁醯基比咯咬_2_ 107 200823188 基）曱基Κ5|2-{[2-(3-氟苯基）乙基]胺基}如比唑_4_基 (3-σ比-咬基)）甲酿胺 Ν-{[(2R)-1 _(4_胺基丁醯基）吡咯啶基]甲基氟 -2-{〇(3-氟苯基）乙基]胺基卜卜吡唑冰基心比啶 醯 5 胺 ^ N-[((2R)吨略唆_2_基）甲基](5_氟_2_{[2_(3_氣苯基）乙基]胺 基}_6_吡唑_4_基（3-吡啶基)）甲醯胺 f n-[((2rH-{3_[(第三丁氧基)縣胺基]丙基卜5_氧基咕洛 α定-2.基）甲基](5_氟_2-{[2_(3_敦苯基）乙基]胺基}如比峻 10 -4-基(3_吡啶基)）曱醯胺 N_{[(2R)-l-(3-胺基丙基)-5-氧基π比略唆基]甲基}(5-氟 _2_{[2-(3-氣苯基）乙基]胺基}_“比唑+基&比啶基)）甲醯 胺 N-(胺曱醯基曱基)(5_氟-2_{[2_(3·氟苯基）乙基]胺基}_6_。比 15 唑-4-基(3-吡啶基)）甲醯胺 2-[(5-氟-2-{[2-(3-氟苯基）乙基]胺基}_6_吼唑_4_基（3_口比 '啶基))羰基胺基]-N-曱基乙醯胺 N-[((2R)-l-{(2S)-2-[(第三丁氧基）羰基胺基]_3_羥基丙醯 基}吼咯啶-2-基）曱基](5-氟-2-{[2-(3-氟苯基）乙基;]胺 2〇 基}-6-吡唑-4-基(3-吡啶基)）曱醯胺 N-{[(2R)-l-((2S)-2-胺基-3-經基丙酸基）吼嘻咬_2_基]曱 基}(5-亂-2-{[2-(3-氣本基）乙基]胺基}_6_11比0坐_4-基(3-11比咬 基)）甲醯胺 [3-(胺基曱基)-6-苯基(2_σ比咬基)][2-(3_氟苯基）乙基]胺 108 200823188 N-[(2_{[(弟二丁氧基)艘基胺基]甲基}(3_u比σ定基)）甲基](5 氟-2_{[2-(3-氟苯基）乙基]胺基}_6_(2_π比咬基)(3_σ比咬基 曱醯胺 ι N_{[2-(胺基甲基)(3-响啶基)]甲基}(5•氟-2_{[2_(3_氟苯基） 乙基]胺基}冬(2_吼咬基)(3_吼。定基)）甲醯胺 (5_氣-2-{[2_(3-氟苯基）乙基]胺基}_6_(1_甲基吡唑ι基 口比唆基))-N-〇經基甲基丙基）甲醯胺 土 10 15 20 (5_氟-2-{[2-(3_氟苯基）乙基]胺基}_6仆甲基吼唾冰 吡啶基))-N-(3-羥基_2,2_二甲基丙基）曱醯胺 =2=2_甲基_3_氧基丁基)(5|2侧3_氣苯旬乙基] 女基甲基吡唑4基)(3_π比啶基)）甲醯胺 N-((2R)-3_經基_2,3_二甲基丁基乂5_氟_2_{[2_(3_氣 ，]^基}-6-(1-甲基対_4_基)(3_吼咬基)）甲酸胺土 氟丁氧基)幾基胺基]乙酸2_(叫2-{[(5_氟_2-似-(3- 胺基]胺基}冬(1_甲基吼唾冰基)(3_°比咬基))絲 胺基]甲基}氮咀基)-2-氧基乙基酯 乙酸2侧_2_{[(漆2侧3_氟苯基）乙基]胺 基基乙基Γ4-基)(3♦定基))縣胺基]甲基如 i i[(5L_(3·氣苯基）乙基]胺 基^基乙基Γ姆㈣基))編基]甲基_ ψ 109 200823188 N-({2-[(3-胺基丙基）胺基](3_吡啶基）}曱基χ6_(2_氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3_吡啶羞)）甲醯胺 (5-氟-2-{[2-(3-氟苯基）乙基]胺基}_6_吡唑_4_基（3_吡啶 基))-Ν-(3^比啶基甲基）〒醯胺 5 n-{[(2RM-(2-胺基乙醯基）吡咯啶_2_基]甲基氟 _2-{[2-(3-氟苯基）乙基]胺基卜^(丨-甲基0比唑_4_基)(3_σ比啶 基)）甲酿胺 (6-(2-氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基卜4_甲基比 啶基))_Ν-(3-吡啶基曱基）曱醯胺 10 (6-(2_氰基苯基）_2_ί[2-(3-氟苯基）乙基]胺基}(3_吼啶 基))·Ν_[(6_嗎琳_4_基(3』比咬基)）曱基]曱醯胺 (6<2_氰基苯基）_2·{Ι>(3-氟苯基）乙基]胺基}(3_ π比啶 基))_Ν-[(6_π比咯啶基(3_吡啶基)）甲基]甲醯胺 (6-(2-氰基苯基）_2_{[2_(3_氟苯基）乙基]胺基}(3•吼啶 15 基))-N_[(6-哌畊基(3_°比啶基)）曱基]甲醯胺 N-{[6_(4-乙醯基哌畊基）(3^比啶基曱基氰基苯 基)-2-{[2_(3_氟苯基）乙基]胺基定基》甲酿胺 义[(6_漠(2_°比咬基))甲基](6必氰基苯基)_2_{[2_(3_氟苯基) 乙基]胺基}(3-吡啶基)）曱醯胺 2〇 2很{[2_(3_氟苯基）乙基]胺基}邻_(經基曱基)(2_嗟吩 基)](3』比啶基))幾基胺基]_N_甲基乙醯胺叫2_胺曱醯基 乙，)(2 {[2_(3_氟苯基）乙基]胺基卜6_[5_(經基甲基)(2_嗟 吩基)](3-吡啶基)）曱醯胺 土 (2_ {[2-(3β氟苯基）乙基]胺基卜6-[5-(羥基曱基）(2_噻吩 110 200823188 基)](3^比啶基))-N-(2-吼啶基甲基）甲醯胺 —N-(胺甲醯基甲基)(2-{[2-(3-氟苯基）乙基]胺基}-6-[5-(羥 基甲基)(2_噻吩基)](3-吼啶基)）甲醯胺 2- [(6-(2-氣基苯基）-2- {[2-(3-氟苯基）乙基]胺基} (3-吼σ定 5 基))羰基胺基]-Ν-(曱基磺醯基）乙醯胺 Ν-{[3-(胺基曱基)環己基]曱基}(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基)）曱醯胺 3- [(6-(2 -篆基苯基)-2 -{[2-(3_氣苯基）乙基]胺基}-3-°比σ定基) 羰基胺基]環丙烷甲醯胺 1〇 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-(2-哌畊基乙基）曱醯胺 (6-(2-氣基苯基）-2-{[2-(3-氣苯基）乙基]胺基}(3-ϋ比咬 基))-Ν-(2-吼畊-2-基乙基）曱醯胺 (6-(2-氣基苯基）-2-{[2-(3-氣苯基）乙基]胺基}(3- °比σ定 15 基))-Ν十比畊-2-基甲基）甲醯胺 N-((lS)-5-胺基-1-胺甲醯基戊基）(6-(2-氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基)）曱醯胺N-(3-胺基-1-胺曱醯基丙基)(6-(2-氰基苯基)-2-{[2-(3-氟苯基） 乙基]胺基}(3-吡啶基)）曱醯胺 20 N-{(1R)-1-胺曱醯基-5-[(苯基曱氧基）羰基胺基]戊 基} (6-(2-氣基苯基）-2- {[2-(3-氟苯基）乙基]胺基} (3-吼σ定 基)）甲醯胺 N-(4-胺基-1-胺曱醯基丁基)(6-(2-氰基苯基)-2-{[2-(3-氟苯 基）乙基]胺基}(3-吼啶基)）曱醯胺 111 200823188 N_((1R)_5-胺基小胺甲醯基戊基）(6_(2_氰基苯 基）2 {[2·(3-氟本基）乙基]胺基比唆基)）甲醯胺 Ν-({6-[(2-胺基乙基）胺基](2_σ比啶基））甲基)(6_(2_氰基苯 基)-2-{[2-(3_氟苯基）乙基]胺基}(3_吡啶基)）甲醯胺 Ν-({6-[(3-胺基丙基）胺基](2比啶基）}甲基)(6_(2_氰基苯 基)-2-{[2-(3_氟苯基）乙基]胺基}(3_吼啶基 n](4rh-胺甲醯基_4_[(6_(2_氰基苯基)_2_{[2_(3_氣苯基） 乙基]胺基}(3』比啶基))幾基胺基]丁基丨（苯基甲氧基）甲醯 胺 N-((lS)-4_胺基胺甲醯基丁基）(6_(2_氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基比唆基)）甲酸胺 N-((lR)-4-胺基小胺甲醯基丁基）(6_(2_氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼咬基)）甲醯胺 (6-(2-氰基苯基）_2_{[2-(3-氟苯基）乙基]胺基}(3-,比啶 基))_N-(吡略啶-3-基甲基）曱醯胺 Ν-{[1-(2_胺基乙醯基比咯啶_3_基]甲基}(6_(2_氰基苯 基)-2-{〇(3-氟苯基）乙基]胺基}(3_吼啶基)）甲醯胺 Ν-{[1-(3-胺基丙醯基）π比咯啶_3_基]甲基}(6_(2_氰基苯 基)-2-{[2·(3_氟本基）乙基]胺基定基)）曱酸胺 N-{[1-(4-胺基丁醯基）π比咯啶冬基]曱基}(6_(2_氰基苯 基)-2-{[2-(3_氟本基）乙基]胺基}(3_σ比η定基)）曱醢胺 N-[(l-乙隨基u比略咬冬基）曱基](6-(2-氰基苯基)_2_{[2_(3_ 氟苯基）乙基]胺基}(3-°比咬基)）曱隨胺 Ν-{[1-(3-胺基丙基）π比咯啶冬基]曱基}(6_(2_氰基苯 112 200823188 基)_2_{[2_(3-氟苯基）乙基]胺基}(3_吼。定基)）甲酿胺 N-(3-胺基-2-胺曱醯基丙基)(6-(2-氰基苯基)-2-{[2-(3-氟苯 基）乙基]胺基}(3_吼咬基)）曱酿胺 (2][2_(3_氟苯基）乙基]胺基}_6_(1_曱基吼唑_4_基)(3』比啶 基))-N-[(6-氧基哌畊_2_基）曱基]甲醯胺（2_{[2-(3-氟苯基) 乙基]胺基卜6_吼唑冰基(3-吼啶基))善[(6-氧基哌啡-2-基） 甲基]甲醯胺 (2-{[2_(3_氟苯基）乙基]胺基）_6_ σ比唾_5_基（3_ σ比咬 基))_Ν_[(6-氧基哌π井_2_基）曱基]甲醯胺 Ν-{[(2S)-4-(甲基磺醯基氧基哌啡_2_基]甲基八6_(2_氰基 苯基)-2-{[2-(3-氟苯基）乙基]胺基）(3-,比啶基)）甲醯胺 N-[((2S)-4-乙醯基氧基哌畊_2_基）曱基κ6_(2_氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基比咬基)）甲酸胺 N-[((2S)-4_甲基_6_氧基哌畊_2_基）甲基](6_(2-氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3_吡咬基)）甲醯胺 (6-(2-鼠基苯基）_2_ {[2_(3_氟苯基）乙基]胺基丨&吼啶 基))-N_{2_[(甲基胺基)幾基胺基]乙基丨甲酸胺 N-(2_{[(2-胺基乙基）磺醯基]胺基}乙基）(6<2•氰基苯 基:)_2][2_(3-氟苯基）乙基]胺基}(3♦定基)）曱醯胺 柯似)吼口各咬_2_基）甲基](Μ·氰基苯基)_2_{[2分氣苯 基）乙基]胺基}〇π比啶基)）甲醯胺 2-胺基_Ν- {2_[(6_(2_氰基苯基)_2_{[2_(3_氟苯基）乙胺 基}(3-吼咬基))幾基胺基]乙基丨乙酿胺 3_胺基-Ν· {2-[(6_(2_氰基苯基从{[2_(3_氟苯基）乙基]胺 113 200823188 基}(3-吼啶基))羰基胺基]乙基}丙醯胺 4-胺基-N- {2-[(6-(2-鼠基苯基)-2- {[2-(3-氣苯基）乙基]胺_ 基}(3-吼啶基))羰基胺基]乙基} 丁醯胺 2- [(第三丁氧基）羰基胺基]-Ν_{2·[(6_(2_氰基苯 5 基)-2-{[2-(3 -氣苯基）乙基]胺基}(3比σ定基))搂基胺基]乙 基卜Ν-甲基乙醯胺 4-[(第三丁氧基）羰基胺基]-Ν-{2-[(6-(2-氰基苯 基)_2-{[2-(3-氟苯基）乙基]胺基}(3^比啶基))羰基胺基]乙 基}-沁曱基丁醯胺 ίο N-{[(2S)-l-(2-胺基乙醯基户比咯啶_2_基]甲基}(6-(2-氰基 苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基)）曱醯胺 N-{[(2S)-l-(3-胺基丙醯基）吼咯啶-2-基]曱基}(6-(2-氰基 苯基)-2- {[2-(3 -氣苯基）乙基]胺基}(3-ntbσ定基)）曱酸胺 N-{[(2S)-l-(4-胺基丁醯基）吼咯啶-2-基]曱基}(6-(2-氰基 15 苯基)-2-{[2-(3-氣苯基）乙基]胺基）(3-1¾σ定基)）曱酸胺 2 -胺基_N_ {2-[(6-(2_氣基苯基）-2- {[2-(3-氣苯基）乙基]胺 基}(3-吼啶基))羰基胺基]乙基卜N-曱基乙醯胺 3 -胺基-N- {2-[(6-(2-篆基苯基）-2 - {[2-(3-氣苯基）乙基]胺 基}(3-吼啶基))羰基胺基]乙基}-N-曱基丙醯胺 20 4-胺基-N-{2-[(6-(2-鼠基苯基）-2 -{[2-(3-氣苯基）乙基]胺 基}(3·-比啶基))羰基胺基]乙基}-N-曱基丁醯胺 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吨啶 基))-N-{2-[甲基（曱基磺醯基)胺基]乙基}曱醯胺 3- 胺基-N-(2-胺基乙基)-2-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯 114 200823188 . 基）乙基]胺基}(3-吡啶基))羰基胺基]甲基}丙醯胺 -N-(2-魏基胺基-2-曱基丙基)(6_(2_氰基苯基)-2-{[2-(3-氟苯. 基）乙基]胺基} (3-吼啶基)）甲醯胺 N_((2S)_2-胺基-3-hyd r氧基丙基）(6_(2_氰基苯 5 基)-2_{[2_(3-氟苯基）乙基]胺基}(3』比咬基)）曱醯胺 N-((lS)-l-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3_ °比咬基))魏基胺基]甲基}_2_經基乙基)-2-胺基乙醯胺 2-胺基乙酸（2S)-2-(2-胺基乙醯基胺基>3-[(6-(2-氰基苯 基)-2_{〇(3_氟苯基）乙基]胺基}(3_t定基))幾基胺基]丙 1〇 基酯 N-((lR)-l-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基 吼咬基))羰基胺基]甲基卜2-曱基丙基)_2_羥基乙醯胺 N_((1R)_1_{[(6_(2_氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基办 吡啶基))羰基胺基]甲基}-2-甲基丙基)_2-胺基乙醯胺 15 N-((2R)-2-胺基I甲基戊基)(H2_氰基苯基)_2_ {[2-(3_氟 苯基）乙基]胺基}(3_吼啶基)）甲醯胺 N-((lR)_l-{[(6-(2_氰基苯基)_2u3_氣苯基）乙基了胺基办 吡啶基))羰基胺基]甲基卜3-曱基丁基)_2_羥基乙醯胺 队((1以)_1-{[(6—(2_氰基苯基)1{[2分氟苯基）乙基]胺基办 20 t定基))幾基胺基]曱基卜曱基丁基)士胺基乙酿胺 N-((lR)-2-胺基小{[(6-(2-象基苯基)士{[2_(3_氟苯基）乙基] 胺基}(3♦定基))幾基胺基]曱基}乙基)1胺基乙酿胺 N-((1R)-2-胺基必氰基苯基叫[2_^_氣苯基）乙基] 胺基}(3-吼咬基))獄基胺基]甲基}乙基)_2_經基乙醯胺 115 200823188 N-((3R)_2_氧基(3_哌啶基伙6·…氰基苯基)_2_{[2_(3-氣苯基) 乙基]胺基}(3-°比唆基)）甲醯胺 {2_[((2R)-2-苯基丙基)胺基；j_6_苯基(3-吼啶基)}_N_(3』比啶 基曱基）甲醯胺 5 10 15 20 N_(胺甲醯基乙基)(6_(2_氰基苯基)_2_{[2-(3_氟苯基）乙基] 胺基}(3-吡啶基)）甲醯胺 n-((ir)_i-胺甲醯基乙基)(6_(2_氰基苯基)_2-{[2_(3_氟苯基) 乙基]胺基}(3-吡啶基)）甲醯胺 (2S)_2_[(6_(2_氰基苯基)_2_{[2_(3_氣苯基）乙基做基你吼 啶基））羰基胺基]丙酸甲酯甲基（2R)_2_[(6_(2_氰基苯 基)-2-{[2-(3-氟本基）乙基]胺基}(3-σ比咬基))幾基胺美 酸曱酯 1』 2-[(6_(2_氰基苯基)_2][2_(3_氟苯基）乙基]胺基卜p 羰基胺基]乙酸甲酯 土 基]胺基}(3- u比咬 基]胺基}(3-吡啶 (6-(2-氰基苯基）_2_ {[2-(3-氟苯基）乙 基))_队(2_羥基乙基）曱醯胺 (6-(2-氰基苯基）_2_{[2_(3_氟苯基）乙 基))_N-(2-甲氧基乙基）甲醯胺 柯2_(二曱基胺基）乙基](6_(2_氰基苯基峰叫^氣苯 乙基]胺基}(3-π比咬基)）曱醯胺 弟三丁氧基)_Ν_曱基羰基胺基]乙基}(6_(2_氰基 基)-2-{[2-(3-氟苯基）乙基]胺基}(3“比唆基)）甲釀“ 鼠基苯基）-2-{[2-(3-氟苯基）乙基]胺基丨(3_ π比 基))-Ν-[2-(曱基胺基）乙基]曱醯胺 116 200823188 Ν·(3-胺基丙基)(6-(2-鼠基苯基)-2-{[2-(3 -氣苯基）乙基]胺 基}(3-吡啶基)）曱醯胺 .. (2S)-2-[(6-(2-鼠基苯基)-2- {[2-(3-氟苯基）乙基]胺基}(3_°比 啶基))羰基胺基]-Ν-曱基丙醯胺 5 (6-(2-氰基苯基）_2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-[2-(曱氧基羰基胺基）乙基]曱酸胺 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-{2-[(曱基磺醯基)胺基]乙基}曱醯胺 3- [(6-(2-鼠基苯基)-2-{[2-(3-氟苯基）乙基]胺基}-3-°比0定基) ίο 羰基胺基]丙酸乙酯 4- [(6-(2-氰基苯基）-2- {[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))羰基胺基]-Ν-曱基丁醯胺 • Ν-(3-胺曱驢基丙基）(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙 基]胺基}(3-ϋ比啶基)）甲醯胺 15 Ν-(2-胺基乙基)(6-(2 -鼠基苯基)-2- {[2-(3-氣苯基）乙基]胺 基}(3-吼啶基)）曱醯胺 (6-(2-氣基苯基）-2-{[2-(3-氣苯基）乙基]胺基}(3_ ^比口定 基))-N-[(4-氟苯基）曱基]曱醯胺 (6-(2-鼠基苯基）_2- {[2-(3-氣笨基）乙基]胺基}(3 -外匕σ定 2〇 基))-Ν-[(4-氰基苯基）曱基]曱醯胺 N_((1S)-1-胺曱醯基-2-羥基乙基）(6-(2-氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基)）曱醯胺（6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3·-比啶基))-N-(3-羥基丙基）甲醯胺 117 200823188 (6-(2-氛基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3- ^比σ定 基))-Ν-(3-甲氧基丙基）甲醯胺 . (2S)_2-[(6-(2-氣基苯基)-2-{[2-(3_氟苯基）乙基]胺基}(3-σΛ 啶基))羰基胺基]-3-羥基丙酸甲酯 5 (2R)_2-[(6_(2-氰基苯基)-2-{〇(3-氟苯基）乙基]胺基}(3-口比 啶基))羰基胺基]-3-羥基丙酸曱酯 (6-(2-氣基苯基）-2-{[2-(3-氣苯基）乙基]胺基}(3-11比咬 基))-Ν·(2-吼啶基甲基）甲醯胺 (6-(2-氣基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-σ比咬 1〇 基))-Ν-[(4-曱基苯基）甲基]甲醯胺 (6-(2-氣基苯基）-2-{[2-(3-氣苯基）乙基]胺基}(3- ^比σ定 基))-Ν-[(6-曱基(3-吼啶基)）曱基]曱醯胺 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3·-比啶 基))-N-[(6-曱基(2-口比啶基)）曱基]曱醯胺 15 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3_吼啶 基))-N-(2-(2-吼啶基）乙基）甲醯胺 (6-(2 -氣基苯基)-2 -{[2-(3 -氣苯基）乙基]胺基}(3-°比 啶基))-N-(2-(3-吼啶基）乙基）曱醯胺 N-[(6-胺基(3-吼啶基)）曱基](6-(2-氰基苯基)-2_{[2-(3-氟苯 2〇 基）乙基]胺基}(3-吼啶基)）曱醯胺 (6-(2-氰基苯基）_2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-[(6-曱氧基(3-咐啶基)）曱基]曱醯胺 (6-(2-氣基苯基）-2- {[2-(3 -氣苯基）乙基]胺基}(3- ^比σ定 基))-Ν-[(2-曱基(3-吼啶基)）曱基]曱醯胺 118 200823188 N-[(2-胺基(3-°比口定基)）甲基](6-(2-鼠基苯基)-2_{[2-(3 -氣苯 _基）乙基]胺基}(3-吡啶基)）甲醯胺_ (6-(2-氣基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3- ntb唆 基))-N-[(2_甲氧基(3-吼啶基)）甲基]甲醯胺 5 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-Ν-[(1-羥基(2-吼啶基)）曱基]甲醯胺 (6-(2-鼠基苯基）-2·{[2-(3·氣苯基）乙基]胺基}(3- utb唆 基))-Ν-[(1-羥基(3-吼啶基)）甲基]曱醯胺 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 ίο 基))_N-[3-(4-曱基哌畊基）丙基]甲醯胺 、 （6-(2-氰基苯基）-2-{[2-(3- I苯基）乙基]胺基}(3-吼啶 基))-Ν-(環丙基曱基）曱醯胺 Ν-[2-(二甲基胺基）乙基]-2-[(6-(2 -氣基苯基)-2-{[2-(3 -氣苯 基）乙基]胺基}(3-吼啶基))羰基胺基]乙醯胺 15 2-[(6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))羰基胺基]-Ν-(2-羥基乙基）乙醯胺 Ν-(2-胺曱醯基乙基)-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基） 乙基]胺基} (3-^比σ定基))祿基胺基]乙酿胺 342-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}-3-口比 20 啶基)羰基胺基]乙醯基胺基}丙酸 Ν-{3_[(第三丁氧基）羰基胺基]丙基}-2-[(6-(2-氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3-扯啶基))羰基胺基]乙 醯胺 Ν-[3-(二曱基胺基）丙基]-2_[(6-(2-氰基苯基)-2-{[2-(3-氟苯 119 200823188 ，）乙基]胺基}(3-吡啶基))羰基胺基]乙醯胺2_[(6_(2_氰基 本基）2-{[2:(3_氟笨基）乙基]胺基Ι(3_ π比咬基））羰基胺 基]-N-(3-經基丙基）乙蕴胺 二-(2_[(第三丁氧基)春曱基羰基胺基]乙基卜2你♦氰基 笨基）2 {[2 (3-氟笨基）乙基]胺基}(3_π比咬基))幾基胺基] 乙醯胺 2-[(6-(2-氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基}η比啶 基))幾基胺基]-Ν-[2-(甲基胺基）乙基]乙醯胺 10 15 (2S)-3-胺基-2_[(6_(2_氰基苯基峰收仏氣苯基）乙基]胺 基}(3』比啶基))羰基胺基]丙酸甲酯 N_((lS)-2-胺基小胺甲醯基乙基）(6_(2_氰基苯 基)-2_{[2-(3-氟苯基）乙基]胺基}(3_π比唆基)）甲酸胺 (2S)_3_[(弟二丁氧基）羰基胺基]_2七6_(2_氰基苯 基)-2_{[2-(3_氟苯基）乙基]胺基}(3_吼咬基》幾基胺基]丙 (2S)_3_[(第三丁氧基）羰基胺基 «丨(3⑽基肢絲細- =====妨邮細 (2S)-3-胺基_2_[(6_(2_氰基苯基从叫3_ 基}(3-口比咬基))幾基胺基砰，队二甲基兩釀胺土 " =3Γ=(6_(2_氰基苯基>2训3德苯基）乙基]胺 基}(3-比。疋基))羰基胺基]丙酸 120 20 200823188 (2S)-2-胺基-3-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-啦啶基))羰基胺基]丙酸曱酯 (2S)-2-(乙醯基胺基)_3-[(6_(2-氰基苯基)-2-{[2-(3-氟苯基) 乙基]胺基}(3-吡啶基))羰基胺基]丙酸甲酯 5 10 15 20 N-((2S)_2_胺基-2-胺甲酸基乙基）(6_(2_氰基苯 基)-2_{〇(3_氟苯基）乙基]胺基}(3-π比π定基)）甲醯胺 N-{(1S)_1_胺甲醯基-2-[(6_(2_氰基苯基)_2_{[2_(3_氟苯基) 乙基]胺基}(3-吡啶基))羰基胺基]乙基}乙醯胺 (2S)-2-胺基·3_[(6-(2-氰基苯基)-2_{[2-(3-氟苯基）乙基]胺 基}(3_吼啶基))羰基胺基]_Ν_甲基丙醯胺 (2S)1胺基-3-[(6_(2_氰基苯基峰似分氟苯基）乙基]胺 基}(3_吼啶基))幾基胺基]-Ν,Ν-二f基丙醯胺 (2s)_2-胺基_h(6_(2_氰基苯基)_2_{[2_(3_氣苯基）乙基]胺 基}(3』比啶基))羰基胺基]丙酸 ⑽-2-(乙酿基胺基奸⑹私氰基苯基)_2_{[2_(3_氣苯基） 乙基]胺基}(3_吼啶基))幾基胺基]-N-甲基丙酸胺 (=)-3-胺基_2_[(6_(2_氰基苯基)_2_{[2_(3_氣苯基）乙基]胺 基}(3-吡啶基D羰基胺基]丙酸甲酯 = 1R>2_胺基小胺甲醯基乙基）(6-(2-氰基苯 基氟苯基）乙基]胺基}(3“比絲))甲酸胺 胺H[(6_㈣絲基)_2泰㈣細乙基]胺 土}(3_吡口疋基))羰基胺基]_N_甲基丙醯胺 =ϋ^3_[(6_(2_氛基苯基)·2-{[2·(3-氟苯基）乙基]胺 土 }〇比欠基))羰基胺基]丙酸甲酯 121 200823188 N-((2R)-2_胺基-2_胺甲醯乙基)(6_(2_氰基苯基)_2_ {[2_(3_ 象本基）乙基]胺基}(3-π比唆基)）曱醯胺 (6-(2-氰基苯基）_2_{[2_(3-氟苯基）乙基]胺基}(3_ ^比啶 基))-N_(lL坐_2_基甲基）曱醯胺 5 (2S>2-[(6-(2-氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基}(3_,比 咬基))叛基胺基]-3-經基曱基丙酸胺 N-[(6-氰基（3_吼啶基））曱基](2_{[2_(3_氟苯基）乙基]胺 基}-6-苯基(3-吼咬基)）曱醯胺 N-{[6-(胺基甲基)(3_π比啶基)]甲基)(2-{[2_(3-氟苯基）乙基〕· 10 胺基}_6_苯基(3-吡啶基)）甲醯胺 Ν-[(3,4-二氟苯基）甲基](6_(2_氰基苯基)_2_{[2_(3_氟苯基） 乙基]胺基} (3-吼咬基)）甲醯胺 4-[(6-(2-氰基苯基)-2-{[2_(3_氟苯基）乙基]胺基卜3_吼啶基) 羰基胺基]丁酸 15 3_[(6-(2_氰基苯基氟苯基）乙基]胺基}(3_吼啶 基))羰基胺基]_Ν_曱基丙醯胺 4-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}_3_π比啶基) 羰基胺基]丁酸甲酯 1 2-胺基-l-(2-{[2-(3_氟苯基）乙基]胺基卜6_笨基(3_σ比啶基)） 20 乙-1_醇 Ν-{2_[(6_(2_氰基苯基)_2_{[2_(3·氟苯基）乙基]胺基卜比 π定基)数基胺基]乙基}乙酿胺 (叫2-[(6_(2·氰基苯基)·2·{[2_(3_氟苯基）乙基]胺基}(3』比 σ疋基))叛基胺基]-Ν-甲基丙酿胺 122 200823188 N-{[4-(胺基曱基）(2_ u比啶基）]甲基}(6_(2_氰基苯 _基)-2-{[2-(3-氟苯基）乙基；|胺基}(3_吡啶基》甲醯胺 N_[(5_{[(第三丁氧基）羰基胺基]甲基八2_。比啶基））甲 基](6-(2-氰基本基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼唆 基)）甲醯胺 N-{[5-(胺基曱基）(2_ ,比啶基）]甲基}(6_(2_氰基苯 基)-2-{[2_(3-氟苯基）乙基]胺基}(3_π比唆基)）曱驢胺 Ν-{[4-(胺基甲基)(2·-比啶基)]曱基}(2-{[2_(3_氟苯基）乙基] 胺基}-6-苯基(3-吼咬基)）曱酸胺 Ν-{[5-(胺基甲基)(2_π比啶基)]曱基}(2_{[2_(3_氟苯基）乙基] 胺基}_6-苯基(3-吼π定基)）曱醢胺 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3_ σ比咬 基))-Ν-(異啐唑-5-基曱基）曱醯胺 2-{[2·(2_{[2_(3-氟苯基）乙基]胺基}-6_苯基（3_υ比唆基))_2_ 羥基乙基]胺基}乙醯胺 123 200823188 基}(3-吡啶基)）曱醯胺 N-{2-[6-(胺基甲基）(2-吼啶基）]乙基}(6-(2-氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基)）曱醯胺 Ν-{2·[6-(胺基曱基)(2-吼啶基)]乙基}(2-{[2-(3-氟苯基）乙 5 基]胺基}-6-苯基(3-吼啶基)）甲醯胺 N-{[6-(2•胺基乙基）(2-咐啶基）]甲基}(6-(2_氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基)）曱醯胺 N-{[6-(2-胺基乙基)(2-吼啶基)]曱基}(2-{[2-(3-氟苯基）乙 基]胺基}-6-苯基(3·-比啶基)）甲醯胺 ίο N-[2-(2-胺基乙氧基）乙基](6-(2-氰基苯基)-2_ {[2_(3_氟苯 基）乙基]胺基}(3-吡啶基)）甲醯胺 (6-(2-氣基苯基）-2_{[2-(3-氣苯基）乙基]胺基}(3- °比σ定 ‘ 基))-Ν-{[6-(羥基曱基)(2-吼啶基)]曱基}甲醯胺 N-{[3-(胺基曱基）苯基]曱基}(6·(2-氰基苯基)-2-{[2-(3-氟 15 苯基）乙基]胺基}(3-吼啶基)）曱醯胺 2-[(6_(2-氣基苯基）-2- {[2-(3 -氟苯基）乙基]胺基} (3-17比咬 基))羰基胺基]-N，N-二甲基乙醯胺 N-{2-[(2-胺基乙基）胺基]乙基}(6-(2-氣基苯基）-2-{[2-(3_ 氟苯基）乙基]胺基}(3-吼啶基)）曱醯胺 20 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3- η比啶 基))-Ν-[(2-氧基(3-哌啶基)）甲基]曱醯胺 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-(吼唑-3-基甲基）曱醯胺 (6-(2-氣基苯基）-2-{[2-(3-氣苯基）乙基]胺基}(3- °比ϋ定 124 200823188 基))以_[(1_甲基吡唑基）甲基]甲醯胺 - N-{[4-(胺基甲基)苯基]曱基}(6_(2_氰基苯基)_2_氟 苯基）乙基]胺基}(3-ϋ比咬基)）甲酸胺 Ν-[(6-{[(2-胺基乙基)胺基]甲基}(2_吡啶基)）甲基](6_(2_氰 5 基笨基)-2-{[2-(3-氟苯基）乙基]胺基}(3-°比唆基)）甲臨胺 6_{[(6♦氰基苯基)-2-{[2_〇氟苯基）乙基]胺基卜Ρ比啶 基)幾基胺基]甲基}σ比咬-2-叛酸甲酉旨 6_{[(6-(2-氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基比啶 基)羰基胺基]甲基}吼啶-2-羧酸 1〇 6][(6_(2_氰基苯基口_{[2_(3_氟苯基）乙基]胺基}_3_,比啶 - 基)羰基胺基]曱基}吡啶-2-甲醯胺 (6-(2-氰基苯基）-2-{[2·(3-氟苯基）乙基]胺基}(3_ σ比啶 基))-Ν-[(1-曱基吼唑_5_基）曱基]甲醯胺 N-((3S)-l-{2-[(第三丁氧基）羰基胺基]乙基}_2-氧基〇_哌 15 絲))(6_(2_氰基苯基)_2-{[2-(3-氟苯基）乙基]胺基}(3“比 啶基)）曱醯胺 N_[(3S)小(2_胺基乙基)氧基（3_旅啶基爪氰基苯 基)_2_{[2_(3_氟苯基）乙基]胺基}(3“比啶基)）曱醯胺 N例(聊2-氧基_3_[(苯基甲氧基）幾基胺基]旅咬基}乙 基)(6_(2_氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基泊“比咬 基)）曱醯胺 =2-((38)-3-胺基-2-氧基旅啶基）乙基](6_(2_氰基苯 基)-2-{[2-(3·氟苯基）乙基]胺基}(3+定基))曱酸胺 队{[2-(胺基曱基）苯基]曱基丨(6♦氰基苯 125 200823188 苯基）乙基]胺基}(3-吼咬基)）甲酿胺 (6-(2-氰基苯基）_2_{〇(3-氟苯基）乙基]胺基比啶 基))_Ν-[(2_氧基°比洛唆_3_基）罗基]甲酿胺 Ν_[(2-{2-[(第三丁氧基）羰基胺基]乙基}(3_处啶基》甲 5 10 15 20 基](6-(2-氰基笨基)-2-{[2-(3-氟苯基)乙基]胺基}(3_σ比啶 基)）甲醯胺 Ν_{〇(2-胺基乙基）(3_ u比啶基）]甲基}(6_(2_】 基)-2-{[2-(3-氟本基）乙基]胺基}(3-12比唆基)）甲酸胺 Ν-{2-[3-(胺基甲基）(2_ ,比啶基）]乙基}(6_(2_氰基苯 基)-2-{[2-(3-氟笨基）乙基]胺基}(3-σ比咬基)）甲醯胺 =((3S)-2-氧基吡咯啶-3—基)(6_(2_氰基苯基)_2_ {[2_(3_氟 本基）乙基]胺基}(3-吼咬基)）甲酿胺 (6_(2_氰基苯基）_2_{[2_(3_氟苯基）乙基]胺基泊_吼^ 基))-Ν-{[1-(2-經基乙基)_2_氧基(3_π底唆基)]曱基}曱酸胺 Ν-{[1-(2-胺基乙基)_2_氧基(3_π辰咬基)]曱基啊2_氛基苯 基)-2_{[2-(3_氟笨基）乙基]胺基j(3_n比咬基)）甲醉 ㈣-氰基苯基）-2-{[2-(3_氟苯基）乙基]胺^3_π比咬 基))善{[1-(3-重氮基·3_氮雜丙各稀基) 甲基}甲醯胺 疋疋基)] (=(2-氰基苯基）-2-{[2_(3_氟苯基）乙基] Ν♦重氮-3-氮雜丙_3_稀基)姆 以 曱基]甲醯胺 疋基）） G暴J月女基}(3_吡啶基)）甲醯胺 ) 126 200823188 N-[((2R)_1-甲基哌畊：基）甲基](6_(2_氰基苯基)_2_{[2_(3_ 氟苯基）乙基]胺基}(3-吡啶基)）曱醯胺 N-[((2R)-1-乙醯基哌畊_2_基）甲基](6_(2_氰基苯 基)_2_{[2_(3·氟本基）乙基]胺基}(3-吼σ定基)）曱醯胺 Ν- {[(2R)-1-(乙基磺醯基）哌畊_2_基]曱基} (6-(2_氰基苯 基)-2_{|>(3_氟苯基）乙基]胺基}(3』比啶基)）甲醯胺 (2R)_2_{[(6-(2•氛基苯基)_2_{[2_(3_氟苯基）乙基]胺基}(3_ 吡啶基))羰基胺基]甲基}哌畊羧酸甲酯N-[((2S)-1-乙醯基 -4-曱基哌畊_2_基）甲基](6_(2_氰基苯基>2-{[2_(3_氟苯基) 乙基]胺基} (3』比唆基)）甲醯胺 (2s)_2_ {[(6-〇氰基苯基)_2_ {[2分氟苯基）乙基]胺基）(3_ 吡啶基))羰基胺基]甲基}_4_甲基哌畊羧酸甲酯 N_ {[(2R)-1 -(2-胺基乙醯基）哌畊_2_基]甲基丨(6_(2_氰基苯 基)-2-{[2-(3-氟本基）乙基]胺基}(3-11比咬基)）甲酿胺 N_{[(2R)_1_(3_胺基丙醯基）哌畊-2_基]甲基}(6-(2_氛基苯 基)-2-{[2-(3-氟笨基）乙基]胺基定基)）甲酸胺 柯⑽小⑷胺基丁醯基）旅啡士基]甲基}(6_(2_氛基苯 基)-2_{〇〇氟笨基）乙基]胺基}(3_σ比啶基)）甲醯胺 队{[(2S)-1_(2-胺基乙酿基)_4_甲基井士基]甲基}(6必 氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基}(3_吼咬基)）甲酿胺 队{[(2s)-i-(3_胺基丙醯基)_4_甲基哌__2_基]甲基}(6存 氰基苯基)々-{[2♦氟苯基）乙基]胺基}(3_吼咬基))曱醯胺 队{[(2s)-i_(4_胺基丁酿基甲基旅呼冬基]甲基㈣ 氰基苯基)-2_{[2_(3-氟苯基）乙基]胺基}(3_σ比咬基))曱酶胺 127 200823188 N-{[(2SM|胺基乙醯基）派0井_2_基]$基}(6_(2_氰基苯 基）2 {[2. (3_氟本基）乙基]胺基定基)）甲兹 购傅胺基丙酿基則确甲氣基苯 基）2 {[2-(3-氟本基）乙基]胺基}(3^比。定基)）甲酿胺 购邻-胺基丁酿基則确甲氰基笨 基)-2-{P-(3-鼠苯基）乙基]胺基}(3_吡啶基乃甲醯胺 —{[(2S) 4 (2-私基乙醯基）甲基娘__2_基]甲基）(6_(2_ 氰土笨基）2 {[2_(3_氟苯基）乙基]胺基}(3_。比咬基))甲酸胺 —{[(2S) 4 (3-版基丙酿基）_ι_甲基娘。井_2_基]甲基》(6_(2_ 氰土苯基）2 {[2_(3_氟苯基）乙基]胺基你吼唆基))甲驢胺 —{[(2S) 4 (4-月女基丁醯基)]_甲基派喷_2_基]甲基⑽-(2_ 氮基苯基)-2-{[2_(3_氟苯基）乙基]胺基}(3_t定基))甲酸胺 2-(6-(2-氰基苯基）_2_ {[2_(3_氟苯基）乙基]胺基比啶 基))-N_(3-吡啶基甲基）乙醯胺 15 20 =㈣_M_二乙酿基^井_2_基）甲基](6_(2_氛基苯 ^「U {[2 (3氟苯基）乙基]胺基°比唆基））甲酸胺 /[i( )_4_曱基哌口井_2-基）曱基](6_(2-氰基苯基)-2-{[2-(3_ =基）乙基]胺基}(3_吼咬基))甲_ n_[((2r)氮心域） ](6_(2_亂基苯基m(3_氟苯基〉乙基]胺 基)）甲醯胺 {[(^^ *)"2- {[2-(3- a ^ } (3- π σ疋基))羰基胺基]甲基}氮0旦羧酸甲酯 =-{[2-(3-氟^基）乙基]胺基}_6_(1_甲基吼唾_4_基心比啶 ))[(2氧基比略欠-3-基）甲基]子酿胺（2_{[2_(3氣苯 128 200823188 基）乙基]胺基}-6-1¾σ坐-4-基(3-σ比117定基))-N-[(2-乳基^比咯17定 . -3-基）曱基]甲醯胺_ N-{[(2R)-l-(2-羥基乙醯基）吼咯啶-2-基]甲基}(6-(2•氰基 苯基)-2-{[2-(3_氟苯基）乙基]胺基}(3-吼啶基)）曱醯胺 5 4-((2R)-2-{[(6-(2-泉基苯基）-2-{[2-(3-氟苯基）乙基]胺 基}(3-啦啶基))羰基胺基]曱基}吼咯啶基)-4-氧基丁酸甲酯 N-{[(2R)-l-(4-羥基丁醯基户比咯啶-2-基]甲基}(6-(2-氰基 苯基）-2- {[2-(3-氣苯基）乙基]胺基}(3 -吼σ定基））曱酿胺 N-{[(2R)-l-(2-羥基乙醯基)u比咯啶-2-基]曱基}(2-{[2-(3-氟 ίο 苯基）乙基]胺基曱基σ比ϋ坐-4-基)(3-1^12定基)）甲酿胺 4_((2R)-2- {[(2- {[2-(3_鼠苯基）乙基]胺基}-6-(1-曱基°比口坐 -4-基）(3-吼啶基))羰基胺基]甲基}吼咯啶基）-4-氧基丁酸 甲酯 N-{[(2R)-l-(4-羥基丁醯基)吼咯啶-2-基]曱基}(2-{[2-(3-氟 15 苯基）乙基]胺基曱基吼唑-4-基)(3-吼啶基)）甲醯胺 N-[((2R)-1-乙醯基氮吸-2-基）曱基](6-(2-氰基苯 基)-2-{[2-(3-氣苯基）乙基]胺基} (3-。比17定基)）甲酿胺 N-{[(2R)-l-(曱基磺醯基）氮哩-2-基]曱基}(6-(2-氰基苯 基)-2- {[2-(3-氣苯基）乙基]胺基}(3-ϋ比σ定基)）曱酿胺 20 N-{[(2R)-l-(2-胺基乙醯基）氮π旦-2-基]甲基}(6-(2-氰基苯 基)-2-{[2-(3 -氟苯基）乙基]胺基}(3-ϋ比咬基)）曱酸胺 N-{[(2R)-l-(3-胺基丙醯基）氮哩-2-基]曱基}(6-(2-氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基)）曱醯胺 N-{[(2R)-l-(4-胺基丁醯基）氮哩_2_基]曱基}(6-(2-氰基苯 129 200823188 基)-2-{[2-(3-氟苯基）乙基]胺基吡啶基》甲醯胺 N_ {[(2R)小(2_經基乙醯基）氮0旦_2_基]甲基}(6_(2_氰基苯 基)_2-{[2_(3-氟苯基）乙基]胺基}(3-σ比啶基)）甲醯胺 4-((2R)_2-{[(6_(2_ 氰基苯基）-2-{[2_(3_ 氟苯基）乙基]胺 基}(3“比啶基))幾基胺基]甲基}氮。旦基)冬氧基丁酸甲酯 N-{[(2R)-1_(4-羥基丁醯基）氮哩_2_基]曱基}(卜(2_氰基苯 基)-2-{[2-(3_氣苯基）乙基]胺基}(3』比。定基)）甲醯胺 N-(氮雜全氫氮呼（azaperhydroepin)-2-基曱基）(6-(2-氰基 笨基)_2_ {[2-(3-氟苯基）乙基]胺基}(3_吼唆基)）甲醯胺 Ν]Ι>(2_胺基乙醯基）氮雜全氫氮呼-2_基]曱基}(卜(2_氰基 苯基)-2-{[2_(3-氟苯基）乙基]胺基}(3_tr比啶基)）甲醯胺 N][H3_胺基丙醯基）氮雜全氫氮呼—2-基]甲基}(6_(2_氰基 苯基)-2-{[2-(3·氟苯基）乙基]胺基}(3 ^比啶基)）甲醯胺 n-{[1-(4-胺基丁醯基）氮雜全氫氮呼基]甲基}(6_(2_氰基 本基)-2-{[2-(3-亂本基）乙基]胺基}(3-。比咬基)）甲酿胺 Ν·[(1-{3-[(弟二丁氧基）幾基胺基]丙基卜2-氧基吼咯咬_3_ 基）曱基](6-(2-氰基苯基)-2_{|>(3-氟苯基）乙基]胺基}(3_ "比啶基)）甲醯胺 义{[1-(3_胺基丙基)-2-氧基吼咯啶-3-基]曱基}(6-(2-氰基 苯基)_2-{[2_(3-氟苯基）乙基]胺基}(3_π比啶基)）曱醯胺 Ν-[(1-{3-[(第三丁氧基）羰基胺基]丙基卜2-氧基π比咯啶_3_ 基）甲基](2-{[2-(3-氟苯基）乙基]胺基}_6』比唑_4_基(3_吼口定 基)）甲酿胺 Ν_{[Η3-胺基丙基)_2_氧基π比咯啶_3_基]曱基}(2-{|>(3-氣 130 200823188 苯基）乙基]胺基}-6-吼唑-4-基(3-批啶基)）曱醯胺 N-[(l_{3-[(第三丁氧基）羰基胺基]丙基}-2-氧基吼咯啶-3-基）甲基](2_{[2-(3_氟苯基）乙基]胺基}-6-(1-曱基吼°坐-4-基)(3-吼啶基)）曱醯胺Ν-{[1-(3-胺基丙基)-2-氧基池咯啶 5 ·3_基]甲基}(2-{[2_(3-氟苯基）乙基]胺基}_6_(1_曱基吼唑 -4-基)(3-吡啶基)）甲醯胺 (2R)_2-{[(2-{[2_(3-氟苯基）乙基]胺基卜6_吼唑-4-基（3_口比 咬基))幾基胺基]甲基}吼洛咬叛酸第三丁酯 N_{[(2R)-l-(2-羥基乙醯基)π比咯啶_2_基;|曱基 ίο 苯基）乙基]胺基}-6_η比嗤-4-基(3_吼咬基)）曱醯胺 (卜(2_氰基苯基）_2-{[2_(3-氟苯基）乙基]胺基}(3- σ比啶 基))-Ν_[(7-氧雜全氫氮呼(oxoazaperhydroepin)-〕基）曱基] 甲醯胺2-{[2-(3-氟苯基）乙基]胺基}-6』比唑斗基(3_吡咬 基))-N-[(7-氧雜全氫氮呼-2-基）曱基]曱醯胺 15 2-{[2-(3-氟本基）乙基]胺基）-6-(1-曱基吼唾-4-基）(3-。比σ定 基))·Ν-[〇氧雜全氫氮呼基）甲基]曱醯胺 N-[(l_{3-[(第三丁氧基）羰基胺基]丙基}_7_氧雜全氫氮呼 -2-基）曱基](6-(2•氰基苯基）-2-{[2-(3-氟苯基）乙基]胺 基}(3-吼咬基)）曱醯胺 2〇 Ν_{[1-(3_胺基丙基）-7-氧雜全氫氮呼 (oxoazaperhydroepin)-2-基]曱基}(6-(2_ 氰基苯 基)-2-{[2-(3_氟苯基）乙基]胺基}(3_吼咬基)）曱醯胺 N_{[(2R)_H4·羥基丁醯基)σ比咯啶_2_基]曱基}(2_{[2_(3_就 苯基）乙基]胺基}-6-吼唑_4_基(3“比啶基)）甲醯胺 131 200823188 N-{[(2R)-l-(2-羥基乙醯基）氮哩_2_基]甲基}(2_{[2_(3_氟苯 基）乙基]胺基K6-[5-(羥基甲基)(2-噻吩基)](3_吡啶基)）甲 醯胺 N-{[(2R)_l-(2,3_二羥基丙醯基）氮哩_2_基]甲基}(6_(2_氰基 5 笨基氟苯基）乙基]胺基}(3-σ比咬基)）甲酸胺 (2R)-2- {[(2- {[2-(3-氟苯基）乙基]胺基}_6_,比唑_4•基(3_吼 啶基))羰基胺基]甲基}氮咀羧酸第三丁酷 N_[((2R)氮哩_2_基）曱基](2_{[2_(3_氟笨基）乙基]胺基}各 吡唑-4-基(3-吡啶基)）甲醯胺 10 N-[2-((2R)-2-{[(6_(2-氰基苯基Η-{[2-(3-氟苯基）乙基]胺 基}(3-吼啶基））羰基胺基]甲基}氮0旦基）(1SH_(羥基曱 基)-2-氧基乙基](第三丁氧基）曱醯胺 n-{[(2r)小((2s)_2_胺基各羥基丙醯基）氮咀_2_基]甲 基}(6-(2-氰基苯基)-2-{[2_(3_氣苯基）乙基]胺基}(3二比啶 15 基)）甲醯胺 N-[(lR)-2-((2R)-2- {[(6-(2-氰基苯基)_2_{[2_(3_ 氟笨基）乙 基]胺基}(3-吡啶基))羰基胺基]甲基}氮。旦基）(經1基曱 基)-2-氧基乙基](第三丁氧基）曱醯胺 N-{[(2R)-l-((2R)-2-胺基_3_羥基丙醯基）氮咀_2_基 2〇 基}(6_(2_氰基苯基)_2][2-(3-氟苯基）乙基]胺基}(3_Dtba定 基)）甲醯胺 N-[2_((2R)_2_ {[(6必氰基苯基Η- {Μ3·氣苯基）乙基]胺 基}(3·-比啶基))羰基胺基]曱基丨氮。旦基胺基丙 基)_2_氧基乙基](第三丁氧基）曱醯胺 土 132 200823188 N-{[(2R)-l-((2S)-2,5-二胺基戊醯基）氮。旦 _2_ 基]甲 基}(6-(2-氰基笨基)-2- {[2-(3-氟苯基）乙基]胺基}(3-u比唆 基)）甲醯胺 N_{[(2R)_1_(2·經基乙醯基）氮。旦_2_基]甲基}(2_《[2_(3·氟笨 基）乙基]胺基}-6-吼唾_4_基(3_σ比咬基)）甲酸胺 N-[((2R)-l-{2_[(第三丁氧基)幾基胺基]乙醯基}氮0旦么基） 甲基](2_{[2-(3_氟苯基）乙基]胺基卜6_π比备‘基(3_σ比σ定基)) N-{[(2R)-l-(2-胺基乙醯基）氮哩_2_基]甲基}(2_{[2_(3-氟笨 基）乙基]胺基}_6_咐^坐-4-基(3-吼咬基)）甲驢胺 (2R)-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基比 唆基))幾基胺基]-3-經基_N-甲基丙醯胺N-[(6_漠（2-吡咬 基)）曱基](2-{[2-(3-氟苯基）乙基]胺基}_6_。比唾_4_基(3_11比 σ定基)）甲驢胺 Ν-({6-[(3-胺基丙基)胺基](2_吼啶基)}甲基)(2_{[2_(3_氟苯 基）乙基]胺基}_6-u比唾_4_基(3_π比咬基)）甲醯胺 Ν-({6-[(2-胺基乙基)胺基](2-σ比啶基)}甲基)(2_{[2_(3_氟苯 基）乙基]胺基卜6-吡唑-4-基(3-吡啶基)）甲醯胺 (2_{[2_(3-氟苯基）乙基]胺基}_6^比唑冰基（3_ σ比啶 基))-Ν-({6-[(2-羥基乙基)胺基](2_σ比啶基)》甲基）甲醯胺 ^^•2-{[(2_{[2-(3-氟苯基）乙基]胺基}_6_吡唑_4_基(3_吡 啶基))羰基胺基]曱基}氮0旦羧酸甲酯 >H((2R)_l-{3-[(第三丁氧基）羰基胺基]丙醯基丨吡咯啶一2_ )甲基](5氟-2-{[2-(3-氟苯基）乙基]胺基卜6-(1-甲基π比唾 133 200823188 -4-基)(3-吡啶基)）甲醯胺 N_{[(2R)小(3-胺基丙醯基）口比嘻咬_2-基]甲基）(5气 -2_{[2_(3_氟苯基）乙基]胺基卜6_(1_甲基口比唾基)(3_口比— 5 N-[((2R)-l-{4-[(第三丁氧基）羰基胺基]丁醯基丨吡咯啶 基）甲基](5_氟-2-{[2_(3_氟苯基）乙基]胺基卜6_(1_甲基〇比唑 _4_基)(34bn定基)）甲醯胺 N_{[(2R)-l-(4-胺基丁隨基）π比咯咬_2_基]曱基}(5_氟 -2_{[2-(3_氟苯基）乙基]胺基卜6_(1_甲基吼嗤冰基)(3』比。定 10 基)）甲醯胺 足 N-[(2][(第三丁氧基)幾基胺基]甲基}(3_吼啶基》曱基] . 氟β2-{[2-(3-氟苯基）乙基]胺基}-6-(1-甲基吼唑_4_某吖 啶基)）甲醯胺 Ν-{[2-(胺基曱基)(3_u比啶基)]曱基}(5-氟·2_{[2_(3_氟苯基） 15 乙基]胺基卜6-(1β·甲基吡唑-4-基)(3-吡啶基)）甲醯胺 N_[((2R)小{3-[(第三丁氧基）羰基胺基]丙基卜^氧基吡咯 啶士基）甲基](5_n{[2_(3_氟苯基）乙基]胺基卜叫-甲 基吼唾-4-基)(3-吼啶基)）曱醯胺 N_{[(2R)-1_(3-胺基丙基)_5_氧基π比咯啶-2_基]曱基}(5_氟 2〇 _2][2-(3-氟苯基）乙基]胺基甲基吡唑冰基)(3_吡啶 基)）曱醯胺 N_{[(2R)-l-(2,3_二羥基丙醯基）吡咯啶_2_基]曱基}(5-氟 2 {[2-(3_氟本基）乙基]胺基卜6-(1-曱基吼。坐冰基)(3_0比咬 基)）曱醯胺 134 200823188 (2-{[2-(3-氟苯基）乙基]胺基卜經基乙基）吼唑I 基](3^比啶基))-N_(3」比啶基甲基）曱醯胺 (2R)-2- {[(6-(2-氰基苯基)-5養{[2_(3_氣苯基）乙基]胺 基}(3_吼咬基))幾基胺基]甲基P比17各咬魏酸第=丁酷 5 咯^基）曱基](6_(2_氰基苯胸_ 氟苯基）乙基]胺基}(3_Π比啶基)）甲醯胺 义[(2_{[(第三丁氧基）羰基胺基]甲基}(3^比啶基》甲 基](2_{[2_〇氟苯基）乙基]胺基}_6_K2_經基乙基）吼唑 -4-基](3-°比咬基)）甲酿胺 10 N普(胺基曱基)(3_°比咬基)]甲基}(2-{[2-(3-氟苯基）乙基]胺 基}-6-[1-(2_經基乙基)吼κ基](3_t定基)） N-[(2-{[(第三丁氧基）羰基胺基]甲基}(3_吡啶基乃甲 基](6_(2-氰基苯基)-5-氟_2_{[2_(3_氟苯基）乙基]胺基}(3_ 吡啶基)）甲醯胺 15 N-{[2-(胺基甲基)(3_°比啶基)]甲基}(6_(2-氰基苯基)_5_氟 2 {[2-(3-氟本基）乙基]胺基比咬基)）甲酿胺 >H((2R)-l-{2-[(第三丁氧基）羰基胺基]乙醯基丨吡咯啶 基）曱基](6-(2-氰基苯基)_5_氟_2_ {[2_(3_氟苯基 基}(3-吡啶基)）甲醯胺 '° 队爪21^1^2-胺基乙醯基）吡咯啶-2-基]甲基}(6_(孓氰美 苯基)_5H{〇(3-氟苯基）乙基]胺基K3_u比啶基》曱酸胺 N [((2R)-l-{3-[(弟二丁氧基）幾基胺基]丙酸基比略唆j 基）甲基](6-(2-氰基苯基)_5•氟_2_{[2_(3_氟苯基）乙基]胺 基}(3_吡啶基)）甲醯胺 土 135 200823188 N-{[(2R)_1_(3_胺基丙醯基）π比咯啶士基]曱基⑽-^氮基 苯基)-5-氟-2-{[2_(3-氟苯基）乙基]胺基}(3_π比唆基)）甲醯胺 N-[((2R)小{4-[(第三丁氧基）幾基胺基]丁醯基丨吡咯咬_2_ 基）甲基](6-(2-氰基苯基)-5•氟-2- {[2-(3-氟苯基）乙基]胺 5 .基}(3-吡啶基)）曱醯胺 N-{[(2R)_1_(4-胺基丁醯基)吼咯啶_2_基]曱基}(卜(2_氰基苯 基)_5_敦_2-{[2_(3_氟苯基）乙基]胺基}(3』比啶基)）曱酸胺 N-[((2R)-l-{3-[(第三丁氧基）羰基胺基]丙基卜5_氧基吼咯 啶-2-基）曱基](6-(2-氰基苯基)-5-氟-2-{[2-(3-氟苯基）乙基] 1〇 胺基}(3-吡啶基)）曱醯胺 N-{[(2R)小(3_胺基丙基)_5_氧基口比略咬_2_基]曱基 氰基苯基)-5-氟-2-{[2-(3-氟苯基）乙基]胺基}(3_u比啶基甲 醯胺 N-{[(2R)-i_(2,3·二經基丙醯基）口比口各咬_2_基]甲基⑽-仏氣 15 基笨基氟-2-{[2_(3-氟苯基）乙基]胺基}(3-吼啶基)）甲醯 胺 服 N-[2-((2R)-24[(5_ 氟 _2_{[2-(3-氟苯基）乙基]胺基卜6_(1β 甲 基吡唑冰基)(3_吼啶基))魏基胺基]曱基}τΙ比咯啶基)(is)小 曱基-2-氧基乙基](第三丁氧基）曱醯胺 20 N-{[(2R)_1-((2S)_2-胺基丙酿基户比嘻。定_2_基]甲基}(5_氣 -2-{[2_(3_氣本基）乙基]胺基}_6-(1_甲基π比唾_4_基)(3_。比咬 基)）曱醯胺 N_[((2R)-l-{(2S)-2,5-雙[(第三丁氧基）幾基胺基]戊醯基} 口比咯啶-2-基）甲基](5_氟_2_{[2_(3_氟苯基）乙基]胺 136 200823188 基卜6_〇甲基吼唑_4_基)(3_π比啶基)）甲醯胺 ' N-{[(2R)_l-((2S)-2,5‘胺基戊醯基)吼略咬^基]甲基 氟-2-{[2-(3-氟苯基）乙基]胺基}_6-(1-甲基吡唑_4-基)(3_吡 啶基)）甲醯胺 5 NK(2R)-2][(5H{[>(3-氟苯基）乙基]胺基卜6_(1-甲 基吼唑-4-基）(3-吼啶基））羰基胺基]甲基丨吼咯啶 基)(lS)-l-(羥基甲基>2-氧基乙基](第三丁氧基）甲醯胺 N- {[(2R)-1 -((28)-2-胺基_3_羥基丙醯基）吡咯啶_2-基]甲 基} (5-氟-2- {[2-(3-氟苯基）乙基]胺基}_6_(1 _曱基吡唑_4一 10 基)(3-吡啶基)）曱醯胺 4-((2R)l{[(5-就-2_{[2_(3_ 氟苯基）乙基]胺基}_6_(1_ 甲基 吼唑-4-基）(3-吼啶基))羰基胺基]曱基丨吼咯啶基)_4_氧基 丁酸曱酯 Ν-{[(2Κ)-1-(4-羥基丁醯基）吡咯啶_2_基]曱基}(5_氟 15 -2-{[2_(3_氟苯基）乙基]胺基}·6仆甲基吡唑I基)(3』比啶 基)）曱醯胺 叫(2-{[(第三丁氧基)幾基胺基]曱基}(3_π比啶基)）曱基](5_ 氣基2 {[2-(3-氟本基）乙基]胺基卜6-(ι_曱基σ比嗤_4_基)(3_ °比唆基)）甲酿胺 2〇 Ν_{[2你基甲基)(3_啦咬基)]曱基}(5_氰基·2_{[2_(3_氟苯基) 乙基]胺基}_卜(1_甲基吡唑I基)(>比啶基)）曱醯胺 n-[h(5r)-5_{[(5_氰基冬{[2_(3_氧笨基）乙基]胺基卜卜(ι_ 甲基u比唑-4-基)(3_吼啶基))羰基胺基]甲基卜2_氧基吡咯啶 基）丙基](第三丁氧基）曱醯胺 137 200823188 N-{[(2R)-l-(3_胺基丙基)_5_氧基吡咯啶_2_基]甲基}(5_气 基-2-{[2-(3-氟苯基）乙基]胺基}_6_(1_甲基吡唑_4_基月比 啶基)）甲醯胺 (2R)-2-{.氰基_2_{[2_(3_氟苯基）乙基]胺基}邻-甲基 比上4基)(3-π比咬基))幾基胺基]甲基}n比洛咬敌酸三 酯 _ 柯《叫料唆_2_基）曱基](5_氰基_2_{[2_(3_氣苯基）乙釗 胺基甲基吡唑_4_基)(3_吡啶基)）曱醯胺 N-[((2R)-1_{4_[(第三丁氧基）羰基胺基]丁醯基丨吡咯啶 基）甲基](5_氰基_2_{[2_(3_氟苯基）乙基]胺基卜卜⑴甲基口比 唾-4-基)(3-吨唆基)）甲醯胺 N-{[(2R)_l-(4-胺基丁醯基）吡咯啶-2_基]曱基}(5_氰基 -2-{[2-(3-氟苯基）乙基]胺基}_6_(1_甲基吼唑_4_基乂3_。比啶 基)）甲酿胺 Ν-[(2-{[(第三丁氧基）羰基胺基]甲基}(3_σ比啶基乃甲 基](2-{[2-(3-氟苯基）乙基]胺基卜5_甲基乂气^甲基。比唑_4_ 基)(3-吡啶基)）甲醯胺 N-{[2_(胺基甲基)(3』比啶基)]甲基}(2_{[2_(3_氟苯基）乙基] 胺基甲基-6-(1-甲基吡唑_4-基)(3_吡啶基甲醯胺 N-[((2R)-l-{3-[(第三丁氧基）羰基胺基]丙基卜5_氧基吼咯 口疋-2·基）甲基](2][2-(3-氟苯基）乙基]胺基卜5_甲基各& 甲基吡唑-4 -基)(3 -吡啶基)）甲醯胺 N-{[(2R)-l-(3-胺基丙基）_5_氧基π比咯啶_2•基]甲 基泊-狀仏氟苯幻乙基诚基卜^甲基各士甲基吡唾冰 138 200823188 基)(3-°比咬基)）曱酿胺 (2R)-2][(2_{[2_(3-氟苯基）乙基]胺基}_5:曱基_6_(1_甲基 吼嗤-4-基)(3-吼啶基))羰基胺基]甲基}吡咯啶羧酸第三丁 酯 5 N_[((2R) ϋ比嘻啶1基）曱基](2-{[2_(3_氟苯基）乙基]胺 基}-5-曱基-6-(1-甲基吡唑_4_基)(3-u比啶基)）甲醯胺 N-[((2R)-l-{4-[(第三丁氧基）羰基胺基]丁醯基）吡咯啶_2_ 基）曱基](2-{[2-(3-氟苯基）乙基]胺基}_5_甲基_6_(1_甲基〇比 唑-4-基)(3-吡啶基)）甲醯胺 10 N-{[(2R)-l-(4-胺基丁 醯基)π比略咬_2_基]甲基}(2_{[2_(3_氟 苯基）乙基]胺基卜5-甲基-6-(1-曱基π比唑-4-基）（3-吡啶基)) 甲醯胺 & (2R)-2_{[(5-氰基-2-{[2-(3-氟苯基）乙基]胺基卜6_吼唾_4- 基(3_σ比咬基))幾基胺基]曱基各唆缓酸第三丁酉旨 15 队[((211户比咯啶_2_基）甲基;|(5_氰基_2-{[2-(3-氟苯基）乙基] 胺基}_6_吡唑-4-基(3-吼咬基)）曱醯胺 N-[((2R)-l-{4-[(第三丁氧基）羰基胺基]丁醯基ρ比咯啶_2_ 基）曱基J(5-氰基-2-{[2_(3_氟苯基）乙基]胺基卜6』比唑_4_基 (3-°比咬基)）曱驢胺 2〇 队{[(211)小(4-胺基丁醯基）σ比咯啶-2-基]甲基}(5_氰基 2 {[2-(3-氟笨基）乙基]胺基}_6_σ比唾_4_基(3_σ比咬基)）曱醯 胺 ^ 5[((211)-1]3_[(第二丁氧基）幾基胺基]丙基}_5_氧基吼咯 °疋_2_基）甲基;|(5_氰基_2_{[2_(3_氣苯基）乙基]胺幻如比峻 139 200823188 -4-基(3-吡啶基)）曱醯胺 N-{[(2R)-l-(3-胺基丙基)-5-氧基吼咯啶-2-基]甲基}(5-氰 基-2-{[2-(3-氣苯基）乙基]胺基}-6-11比0坐-4-基(3-11比咬基)）甲 酿胺 5 N-[(2-{[(第三丁氧基）羰基胺基]甲基}(3-吼啶基)）甲基](5- 氰基-2-{[2-(3-氟苯基）乙基]胺基}-6-吼唑-4-基(3-吼啶基)) 甲醯胺 N-{[2-(胺基曱基)(3^比啶基)]曱基}(5-氰基氟苯 基）乙基]胺基比唑-4-基(3-吼啶基)）曱醯胺 ίο N-[(2-{[(第三丁氧基）羰基胺基]曱基}(3-吼啶基））曱 基](6-(2-氣基苯基）-2-{[2_(3-氣苯基）乙基]胺基}-5-甲基 (3-吡啶基)）曱醯胺 N-{[2-(胺基曱基）(3-吼啶基）]曱基}(6·(2-氰基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}-5-甲基(3-吼啶基)）曱醯胺 15 N-(3-((5R)-5-{[(6-(2-氰基苯基)-2-{[2-(3·氟苯基）乙基]胺 基}-5-曱基(3-。比啶基))羰基胺基]甲基}-2_氧基吼咯啶基) 丙基](第三丁氧基）甲醯胺 N- {[(2R) -1 -(3 -胺基丙基)-5 -乳基口比嘻11 定-2 -基]曱基}(6-(2_ 氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}-5-曱基(3-吼啶基)) 20 甲酿胺 5-氯-2-{[2-(3-氟苯基）乙基]胺基}-6-(1-曱基叱唑-4-基）吼 啶-3-羧酸曱酯 N-[(2-{[(第三丁氧基）羰基胺基]曱基)(3-吼啶基)）曱基](5-氯-2-{[2-(3-氟苯基）乙基]胺基曱基啦唑-4-基)(3·口比 140 200823188 啶基)）甲醯胺 n-{[2_(胺基甲基)(3_σ比啶基)]甲基}(5_氯_2_{[2_(3_氣苯基） 乙基]胺基卜6_(1_曱基吡唑冰基)(3_σ比啶基)）甲醯胺 [((2R)_l-{3_[(第三丁氧基）羰基胺基]丙基卜5_氧基吡咯 m)甲基](5·氯心]!^3德苯基）乙基]胺基卜石仆甲 基吡唑-4-基)(3-吡啶基)）甲醯胺 N-{[(2R)-l-(3-胺基丙基)_5_氧基吡咯啶-2_基]甲基}(5•氯 -2-{[2-(3-氟苯基）乙基]胺基}_6_(1•甲基吡唑_4_基)(3_吡啶 基)）甲醯胺 (2幻_2][(5-氯_2-{[2_(3-氟苯基）乙基]胺基卜6仆甲基u比唑 4基)(3』比u定基))幾基胺基]曱基}σ比咯。定魏酸第三丁酉旨 n-[((2r)吡咯啶士基）曱基](5_氣_2][2_(3_氟苯基）乙^胺 基卜6-(1-曱基吡唑_4_基)(3_吼啶基)）甲醯胺 N-[((2R)-l_{4-[(第三丁氧基）羰基胺基]丁醯基丨吡咯啶 基）甲基](5_氯_2-[2-(3-氟苯基）乙基]胺基卜6_(1_曱基吼哇 -4-基)(3-吡啶基)）曱醯胺 N-{[(2R)-1_(4-胺基丁酿基）u比略咬_2_基]甲基}(5-氯 -2-{[2-(3-氟苯基）乙基]胺基}_6_(1_甲基吡唑_4_基)(3_吡二 基)）甲酿胺 疋 N-{3-[(第三丁氧基)羰基胺基]丙基}(5_氟_2_{[2_(3_氟苯基） ^基]胺基曱基吡唑_4_基)(3-吡啶基)）甲醯胺N_(t 月女基丙基)(5-氟-2-{[2-(3-氟苯基）乙基]胺基卜6_(丨_曱基。比 嗤-4-基)(3-吡啶基)）曱醯胺 (2R)-3-[(5-氟-2-{[2-(3-氟苯基）乙基]胺基•甲基叹唾 141 200823188 -4-基)(3-吡啶基))羰基胺基]_2_甲基丙酸甲酯 调_3俗氟-2-{[2_(3-氟苯基）乙基]胺基卜6_〇_甲基吼唑 -4·基)〇π比唆基))幾基胺基]_2_ f基丙酸 氧基)幾基胺基]養{3_[(5-氟_2_{[2_(3·氟苯基） =:基}邻-甲基吡唑_4_基)(3_吡啶基 基}乙醯胺 2-胺基例3_[(5_氟_2侧3_氟苯基）乙基]胺基}件甲 基吡唑_4_基）（3_吡啶基))羰基胺基]丙基 N-i3m{[2-(3-氣苯基）乙基]胺基卜6_=甲基㈣ -4-基)-3-吡啶基)羰基胺基]丙基}乙醯胺 甲基㈣Μ%2办氣苯基）乙基] 月女基甲基吡唑_4-基)(3_吡啶基)）甲醯胺 15 20 胺/醯基丙基)(5·氟娜-(3;苯基)乙基]胺 基}冬(1_甲基吡唑冰基)(3_吡啶基)）甲醯胺 叫3-[(5-氟-2_{[2_(3_氟苯基）乙基]胺基}_6仆甲基吼唑 -4-基)(3-吡啶基))羰基胺基]_2_甲基甲基丙醯胺 (5-氟-2- {[2-(3-氟苯基）乙基]胺基卜“比 基))-N-(吡唑-3-基甲基）甲醯胺 丞〇比疋 (5_氟-2-{[2-(3-氟苯基)乙基]胺基}_6仆甲基。比唾. 吼啶基))-N十比唑-3-基曱基）曱醯胺 =2吵4_重氮_2_甲基_4氮雜丁_4_烯基)(5食2_咖-氣 本基）乙基]胺基曱基吼唾冰基）（n定基))甲 5-氟_2-{[2-(3-氟苯基）乙基]胺基}_6_(1_甲基吨唾_4_^ 吡啶基)3-甲基氮〇旦基酮 土八^ 142 200823188 N-((2S)-3-胺基-2-甲基丙基)(5-氟-2-{[2-(3-氟苯基）乙基] 胺基甲基吡唑-4-基)(3-吡啶基))曱醯胺 N-{(2R)-3-[(5-氟-2-{[2_(3-氟苯基）乙基]胺基}_6-(1 -曱基 口比唑-4-基)(3-吼啶基))羰基胺基]-2-曱基丙基}-2-[(第三丁 5 氧基)凝基胺基]乙酸胺 N- {(2R)_3-[(5-氣-2-{[2-(3-氣苯基）乙基]胺基}-6-(1-甲基 σ比嗤-4-基)(3-11比咬基))被基胺基]-2-曱基丙基}-2-胺基乙酸 胺 N-{(2R)-3-[(5-氟-2-{[2-(3-氟苯基）乙基]胺基甲基 1〇 吼唑-4-基)(3-吼啶基))羰基胺基]-2-甲基丙基}-2-羥基乙醯 胺 (2R)-2-{[(5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-(1-曱基口比 ' 唑-4-基)(3-吼啶基))羰基胺基]曱基}氮哩羧酸第三丁酯 N-[((2R)氮哩-2-基）曱基](5-氟-2- {[2-(3-氟苯基）乙基]胺 15 基}-6-(1-曱基吡唑-4-基)(3-吡啶基)）曱醯胺 N-[((2R)_l-{2-[(第三丁氧基）羰基胺基]乙醯基}氮哩-2-基) 甲基](5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-(1-甲基吼唑-4-基)(3-吼啶基)）曱醯胺 N-{[(2R)-l-(2-胺基乙醯基）氮呕-2-基]曱基}(5-氟 20 -2-{|：2-(3-氟苯基）乙基]胺基}-6-(1-曱基吼唑-4-基)(3-吼啶 基)）曱醯胺 N-[((2R)-l-{4-[(第三丁氧基)羰基胺基]丁醯基}氮^旦-2-基) 曱基](5-氣-2-{[2-(3-鼠苯基）乙基]胺基}-6-(1-曱基0比嗤-4_ 基)(3-吼啶基)）曱醯胺 143 200823188 N_{[(2R)-1_(4_胺基丁醯基）氮口旦_2_基]甲基}(5_氟 -2-{[2-(3-氟苯基）乙基]胺基卜6-(1-甲基吼唑_4_基)(3_吡啶 基X)甲驢胺 N_{[(2 R)-l-(2_羥基乙醯基）氮哩_2-基]甲基》(5_氟 _2_{[2_(3_氟苯基）乙基]胺基卜6_(1_甲基吡唑_4_基)(3_0比啶 基)）甲醯胺 (2S)-3-[(5-氟-2-{[2-(3-氟苯基）乙基]胺基}_6_(1_甲基^比唑 -4-基)(3-吼啶基))羰基胺基]_2_甲基丙酸甲酯 N-((2S)-3-羥基-2-甲基丙基)(5_氟_2_{[2_(3_氟苯基）乙基] 胺基}-6-(1-甲基吡唑_4_基)(3_吡啶基)）甲醯胺 N-((2R)-3-羥基_2_甲基丙基)(5_氟_2_{[2_(3_氟苯基）乙基] 胺基} -6-吼唾-4-基(3-吼咬基)）甲酸胺 (2R)-H(5·氟_2_{〇〇氟苯基）乙基]胺基卜6_σ比唑基(3_ σ比咬基))幾基胺基]-2-甲基丙酸甲酯 (2R)-3-[(6_(2-氛基苯基)-2-{[2-(3_氟苯基）乙基]胺基 啶基))羰基胺基]-2-甲基丙酸甲酯 N-((2 R)-3-羥基甲基丙基）（6_(2_氰基苯基)_2-{[2_(3•氟 苯基）乙基]胺基} (3-吼咬基)）甲醯胺 队[(2,2_二甲基（1，3_二.惡烷士基)）甲基](5_氟_2_{[2_(3_ 氟 笨基）乙基]胺基}-6-(1-曱基吼嗤-4-基)(3_吼。定基)）曱酸胺 (5-氟-2-{[2-(3-氟苯基）乙基]胺基}_6-(1_甲基11比唾_4_基)(3一 吼啶基))_N-|>羥基_2_(經基曱基）丙基]曱醯胺 1^[(2,2_二甲基（1，3_二噁烷_5_基)）甲基](5·氣 氟 苯基）乙基]胺基}-6』比唑-4-基(3_ϋ比咬基)）甲醯胺 144 200823188 (5-氣-2- {[2-(3-氣苯基）乙基]胺基}-6-ϋ比唾-4-基（3- 0比σ定 . 基))-Ν-[3-^έ基-2-(殖基.曱基）丙基].曱酸胺 Ν·[(2,2-二曱基（1，3-二σ惡烧_5_基））曱基](6-(2_氣基苯 基)-2-{[2-(3-氟苯基）乙基]胺基}(3·-比啶基)）甲醯胺 5 (6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-[3-羥基-2-(羥基曱基）丙基]甲醯胺 (2R)-2-{[(5-氟_2-{[2-(3-氟苯基）乙基]胺基卜6-(1•曱基口比 唑-4-基)(3-吼啶基))羰基胺基]曱基}丁酸曱酯 N-((2R)-2-乙基-3-經基丙基）(5 -氣-2-{[2-(3 -氣苯基）乙基] ίο 胺基}-6-(1-曱基吡唑-4-基)(3-吡啶基)）曱醯胺 、 （2R)-2-{[(5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-吼唑-4-基 (3-吼啶基))羰基胺基]曱基} 丁酸曱酯 N-((2R)-2-乙基-3-輕基丙基）(5 -氣-2·{[2-(3-氣苯基）乙基] 胺基}-6-吡唑-4-基(3-吼啶基)）曱醯胺 15 (2R)-2-[(第二丁氧基）魏基胺基]-3-[(5-氣-2-{[2-(3-氣苯基) 乙基]胺基}-6-(1-曱基吼唑-4-基)(3-吼啶基))羰基胺基]丙 酸甲酯 (2R)-2-胺基-3-[(5-氟-2-{[2-(3-氟苯基）乙基]胺基曱 基吼唑-4-基)(3-吼啶基))羰基胺基]丙酸曱酯 20 N-((lR)-l-{[(5-氣-2-{[2-(3-鼠苯基）乙基]胺基}-6-(1-曱基 口比唑-4-基)(3·-比啶基))羰基胺基]曱基}-2-羥基乙基)（第三 丁氧基）甲醯胺 N-((2R)-2-胺基-3-經基丙基）(5 -氣-2-{[2-(3 -氣苯基）乙基] 胺基}-6-(1-曱基吼唑-4-基)(3-吡啶基)）曱醯胺 145 200823188 1^-((1以)-1_{[(5-氣_2-{[2-(3-氣苯基）乙基]胺基}_6-口比口坐-4-基(3-吼啶基))羰基胺基]曱基}-2-羥基乙基)（第三丁氧基) 甲醯胺 N-((2R)-2-胺基-3-輕基丙基)(5-氣_2-{[2-(3 -氣苯基）乙基] 5 胺基}-6-吡唑-4-基(3-吡啶基)）曱醯胺 N-(2,3-二經基丙基）(5-氣-2-{[2-(3_亂苯基）乙基]胺 基}-6-(1-曱基吡唑-4-基)(3-吡啶基)）曱醯胺 1^-(2,3-二經基丙基）(5-氣-2-{[2-(3-氣苯基）乙基]胺基}_6-吡唑-4-基(3-吡啶基)）甲醯胺 ίο (2R)-3_{[2 -胺基-5-默ι_6-(1-曱基1^比 ϋ坐-4 -基）(3-口比 口定基）]祿 基胺基卜2-甲基丙酸曱酯 N_{[(2R)-l-(2-羥基-2-甲基丙醯基）氮哩-2-基]曱基}(5-氟 -2-{[2-(3-氟苯基）乙基]胺基曱基咐唑-4-基)(3-吼啶 基)）甲醯胺 15 (2R)-2 -{[(5-氣 _2-{[2-(3 -亂苯基）乙基]胺基}- 6-0比 ϋ坐-4 -基 (3-吼啶基))羰基胺基]曱基}氮哩羧酸第三丁酯 N-{[(2R)-l-(2-羥基乙醯基）氮。旦-2-基]曱基}(5-氟 -2-{[2-(3-氟苯基）乙基]胺基}-6-n比唑-4-基(3-吼啶基)）甲醯 胺 20 N-[((2R)氮口旦-2-基）曱基](5-氟-2- {[2-(3-氟苯基）乙基]胺 基}-6-吡唑-4-基(3-吼啶基)）曱醯胺 N-{[6-(胺基曱基)(2-咕啶基)]曱基}(2-{[2-(3-氟苯基）乙基] 胺基}-6-苯基(3-咐啶基)）曱醯胺 N_{[6-(胺基曱基）(2-吼啶基）]曱基}(6-(2-氰基苯 146 200823188 基)-2·{[2-(3-氟苯基）乙基]胺基}(3-ty比啶基)）甲醯胺 N-(fe甲酿基曱基)(6_(2_氰基苯基)_2_{[2-(3-氟笨基）乙基] 胺基}(3-吡啶基)）曱醯胺 N-(2-胺甲醯基乙基）(6_(2_氰基苯基乃2_{[2-(3_氟苯基）乙 基]胺基}(3“比咬基))甲醯胺 2-[(6-(2-氰基苯基)_2-{[2-(3-氟苯基）乙基]胺基}(3-°比啶 基))幾基胺基]_Ν-甲基乙醯胺及 义((38)-2_氧基(3_派咬基))(6_(2_氰基笨基)-2-{[2-(3-1苯 基）乙基]胺基}(3-吡啶基)）曱醯胺。 10 本發明係提供至少一種選自式V化合物及其醫藥上可 接受鹽類之化學品Va)Tu2(-1 benzyl)-2-[(2-propenylethyl)amino](3_pyridyl)}carbamamine^{[(2RH-(4-aminobutylidene)) bite_ 2_yl]methyl oxime (tetra) 2- yinfu N:i[(,27R) martenylamine butyl-2-yl]methyl oxime 6·(2-cyano 94 200823188 N-{[(2R)-l_( (2S)-2,3-diaminopropionyl)σ-pyridyl-2-yl]methyl}(6-(2-cyanophenylfluorophenyl)ethyl]amino}(3_σ-pyridyl) Base))carbamamine N_{[(2R)-l-((2S)-2_amino-3-methoxypropionic acid) σ 唆 唆 _ _ _ _ _ } } } } } } } } 2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-π ratio), formamide N_{[(2R)-l_((2S) )-2-amino-3-ylpyridinyl)σ-pyrrol-2-yl]fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl) Ethyl]amino}(3_acridinyl))carbenamide-{[2-(aminomethyl)(3-π-pyridyl)]fluorenyl}(5_fluoro_2_{[ 2_(3_fluorophenyl)ethyl]amino}_6" than salivation_3_yl (3_σ ratio), formamide N-{[(2R)-l-(2-aminoethyl fluorenyl) ) 吼 啶 -2 -2 _ _ _ 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 Indoleamine N-{[(2R)-l-((2S)-2-amino-3_hydroxypropenyl), pyridin-2-yl]methyl}(5- Fluor-2-{[2-(3-fluorophenyl)ethyl]aminobib 6_σ-biazole _3_yl (3 specific base)) formamide n_{[(2R)-1-((2S) ) 2 -Aminopropyl aryl) 吼 咬 _2 _ _ _ _ 曱 } } } 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 3-yl (3-11 ratio of decyl)) of the entrained amine N_{[(2R)_l-(4-aminobutylidene)pyridinium-2-yl]methyl}(5•fluoro-2-{I ; 2-(3-Fluorophenyl)ethyl]aminobiphenyl 6-pyrazole-3-yl(3-pyridyl)carbalamine de{6-(2-cyanophenyl)_2-[( 2-oxapenta-2-ylethyl)amino] (3" 唆95 200823188 】)-Ν-(3-σ specific hydrazino) decanoic acid N_((2R)_2-amine (propyl)(5-fluoro_2_{[2-(3.fluorophenyl)ethyl]amino}-6-(1-mercaptopurin-4-yl) (3-° ratio bite base) )N-{(1 R)-2-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]aminomethyl) than salivyl-4) (3- u is fluorenyl)) benzylamino] isopropyl isopropyl 2-[(t-butoxy)carbonylamino]acetamide N-{(lR)-2-[(5-fluoro-2-{ [2_(3_Fluorophene J diamine)} methyl group 4. base) (3._yl) ^ group ^=] base}-2-aminoacetamide N-[((2R)- 5-oxopurridin-2-yl)indenyl](5_fluoro_2_{[2_(3-fluorophenyl)ethyl]amino}_6_(1- Indole carbazole _4_yl) (3_π ratio bite base)) mercaptoamine N_{(lS)-2-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amine }}_6_(1_decylpyrazol-4-yl)(3-pyridyl))carbonylamino]-isopropylbut-2-aminoacetamide N-{(1R)_2_[(5·fluoro -2_{[2-(3-Fluorophenyl)ethyl]aminomethane methyl group than wowicyl) (3 • acridinyl)) arylamino group p isopropyl bromide 2, acetylamine N- {(lR)-2-[(5-fluoro-2-{[2_(3-fluorophenyl)ethyl]amino)b 6_(1_曱-hydroxypyrazole-4-yl)(3-acridine Base))carbonylamino]-isopropyl]_4_[(t-butoxy)carbonylamino]butanamine N_{(1R)_2_[(5H{[2_(3_fluorophenyl)ethyl]] Amino} Winter (1-methylpyrazole-4-yl)(3-pyridyl))carbonylamino]-isopropyl-4-aminobutyramine N-{(2R)-2-[ (2_decyloxyethyl)amino]propyl}(5-prepared 2-{[2_(3-fluorophenyl)ethyl]amino} winter (1_mercapto-π-salt_4_base sand Acridine-based carbenamide N_{(2R)_2_[(t-butoxy)alkylamino]propyl-order gas-like fluorinated 96 200823188 Phenyl)ethyl]amino}-6-吼嗤4-yl (3-° thiol))caraamine N_((2R)-2-aminopropyl)(5-fluoro 1{[2-(3-fluoro-phenyl)ethyl]amine Base} _6-σ is more than -4- base (3- Mercapto))carbamide N-{(lR)-2-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}_6_(1_methylhydrazine (3)pyridyl))aminoamino]-isopropyl}acetamido N-{(2R)-2-[(indolylsulfonyl)amino]propyl} (5_ Fluorine_2_{[2-(3-fluorophenyl)ethyl]aminobib 6-(1-methylpyrazol-4-yl)(3-pyridyl))decylamine N_ {(1 R) _2_[(5_Fluoro{[2_(3_fluorophenyl)ethyl]amino)_6_吼嗤 基 (3·-pyridyl))carbonylamino]-isopropyl}_2-amino Acetamide (5-fluoro-2-{[2-(3-fluorobenyl)ethyl]amine), 6_吼σ, _4_yl (3_吼ti))-1^-(2 -mercaptomethyl)carbamamine N-{(2R)-2-[(2'-ylethyl)amino]propyl phenyl)ethyl]aminopyr 6-(1-mercaptopyridyl) Oxazol-4-yl)(3-pyridyl)) decylamine N-{(2R)_2_[(aminoformylmethyl)amino]propyl}(5_fluoro_2_like_(3_fluorine Phenyl)ethyl]aminobib 6-(1-methylpyrazol-4-yl)(3_pyridyl))carbenamide N-{(1R)_2_[(5-gas_2_{[2_ (3_Fluorophenyl)ethyl]aminobib (bu Methyl to sal-4) (3-° ratio. Mercapto)) arylamino]-isopropyl isopropyl 2-(dimethylamino)acetic acid amine N-{(lR)-2-[(5-fluoro-2-{[2-(3- benzene) Ethyl]amino}_6 servomethylpyrazol-4-yl)(3-pyridyl))carbonylamino]]isopropyl](2S)_2_[(t-butoxy)-demethylamine N-{(lR)-2-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amine-based (1)methylpyrazole- 4-yl)(3-pyridyl))carbonylamino]]-isopropyl}(28)_2-amino-3-hydroxypropionamide 97 200823188 N-{(lR)_2-[(5-fluoro- 2-{[2-(3-fluorophenyl)ethyl]aminomethyl, oxime I)) (3_acridinyl))alkylamino]-isopropyl-2-amine 1 Alkylpropanoid with n-(4-{6-[(2_(2′′)pyridyl)ethyl)amino]N-[N-(3-pyridylmethyl)amine 5 mercaptoyl}phenyl) Amine amine N-((1R)-1_{[(5-fluoro-2-{[2_(3-fluorophenyl)ethyl)amino}-6-(1_ fluorenyl s- 4_yl) 3_Acridine))aminoamino]mercaptopropyl)2-[(t-butoxy)carbonylamino]acetamide N-((lR)-l-{[(5-fluoro_ 2-{[2-(3-fluorophenyl)ethyl]aminobi 6-(1-methyl 1 oxapyrazolyl)(3-pyridyl))carbonylamino]methyl}propyl)- 2-Aminoacetamide • N ((lR)-l-{[(5-fluoro_2-{[2 -(3-Fluorophenyl)ethyl]amino group than spyryl (> bite base)) arylamino] fluorenyl} propyl)_2_[(t-butoxy-decylamino) Amine oxime ((1 R)-l-{[(5-fluoro-2-{[2-(3-)-phenyl)ethyl]aminopyr-6-σ is more than a pyridyl 4-yl group ))carbonylamino]methyl propyl propyl) 2 -aminoacetamide N {(lR)-2-[(5-fluoro 2 -{[2_(3_fluorophenyl)ethyl]amino) 6-(ι_methylpyrazolyl)(3_pyridyl))carbonylaminol l-isopropyl}(2S)_2-aminopropionamide 2〇N-((2R)士经士士Methyl butyl)(5_fluoro_2_{[2 fluorophenyl)ethyl]aminomethylpyrazole-4-yl)(3·pyridyl))carbenamide (aminomethyl) 3_,pyridinyl)]methyl}(6_(2-cyanophenyl)-2·{[2-(3-fluorophenyl)ethyl]amino}(3_σ 々 》) -{[2-(Aminomethyl)(3_σ ratio)>Methyl}(2R (tetra)phenylylene) 98 200823188 Amino}-6-pyrazol-4-yl (3-pyridyl) Methionine (6-(2-oxyphenyl)-2-{[2-(3-)-phenyl)ethyl]amino}(3-σ比ϋ定•基))-Ν- (3-pyridylfluorenyl) decylamine * {6-(4-ethylhydrazineyl)-2-[(2-(2-11- σ-decyl)ethyl)amino] (3-11 唆5 base)}-Ν-(3-pyridine Sulfhydryl) decyl 4-{6-[(2-(2-acridinyl)ethyl)amino]-5-[indolyl-(3-acridinylhydrazinyl)amine fluorenyl]-2 -2-acridinyl}nonyl benzoate {2-[(2-(2-oxaridinyl)ethyl)amino]-6-[4-(trifluoromethyl)phenyl](3-port ratio Pyridyl)}-indole-(3-pyridylmethyl)carbamamine ίο 4-{6-[(2-(2-acridinyl)ethyl)amino]-5-[Ν-(3- Acridine methyl)amine fluorenyl]-2-u-pyridyl}benzoic acid oxime-(3-mouthpyridinyl){6-(4-mouthpyridyl)-2-[(2 -(2-acridinyl)ethyl)amino](3-pyridyl)} amidoxime-(3-acridinylfluorenyl){6-(2-acridinyl)-2_[(2 -(2-oxaridinyl)ethyl)amine 15 yl](3-pyridyl)}carbamamine {6-(3,4-diazophenyl)-2·[(2-(2-吼ϋ) Alkyl)ethyl)amino](3-indole ratio sigma)}-Ν-(3_pyridylmethyl)decylamine {6-[4-(hydroxymethyl)phenyl]-2-[( 2-(2-Acryl)ethyl)amino](3-acridinyl)}-indole-(3-pyridinyl) decylamine 2〇{6-(4-decyloxyphenyl) -2-[(2-(2-Acridine)ethyl)amino](3-acridinyl)}-N-(3-pyridylmethyl)carbenamide {6-(4-fluorenyl) Styryl)-2-[(2-(2-acridinyl)ethyl)amino]( 3-acridinyl)}-N_(3-pyridylmethyl)formamide {6·(4-chlorophenyl)-2-[(2-(2-acridinyl)ethyl)amino] (3-Acridine 99 200823188 base)}-Ν-(3-Acridinemethyl)carbamamine {6-(4'fluorophenyl)-2_[(2-(2-acridinyl)ethyl) Amino](3_ π-pyridinyl) b (3_acridinylmethyl)carbamamine. {6_phenyl_2-[(2·(2-pyridyl)ethyl)amine (3_pyridyl)}_(3_pyridinyl)methylguanidamine {6-(3,4-difluorophenyl)-2_[(2-(2-pyridyl)ethyl) Amino](3_pyridyl)}-N-(3_ti than dimethylmethyl)cartoamine {6_benyl-2-[(2-(3-σ))ethyl)amino group (3_π ratio bite base) diazepam _(3_σ-pyridylmethyl)carbamamine 10 (6-[4_(didecylamino)phenyl]_2-[(2_(2-hydroxypyridinyl)) Amino]](3_pyridyl)}_Ν-(3-η-pyridylmethyl)carbamamine-(3′′biti-methyl){6_(3′′pyridinyl)ethyl Amino](3-pyridyl)}carbamidine 4-{6_[(2-(2′i-pyridyl)ethyl)amino]]_5_[Ν_(3_σ-pyridylhydrazino)amine 曱I5 酉胜基]-2-0 than bite base} benzoic acid {2 [(2 & yl-2-ylethyl)amino] phenyl (3-oxime. Basement)}_Ν-(3_π than dimethylmethyl)carboxylic acid amine {2_[(2-(2--pyridyl)ethyl)amino]]6_(2_vinylphenyl)(3_^pyridyl) ) good (3 比 啶 曱 曱 曱醯) decylamine 20 {6-[2-(decyloxymethyl)phenyl]_2-[(2-(2-acridinyl)ethyl)amino ] (3_ also bite base)}_Ν_(3-π-pyridylthiol) guanamine {6-(2-曱基基基基)_2_[(2_(2·吼)yl)ethyl)amine ]&Pyridine)}-N-(3-Pyridylmethyl)decylamine (2-{[2-(3-fluorophenyl)_2-hydroxyethyl]aminobiphenyl 6-phenylindole Acridine 100 200823188 base))-N-(3-pyridylmethyl)decylamine (6-(2_篆基基基)-2_{[2-(3-fluorophenyl)-2-3⁄4ylethyl Amino}(3-n-pyridyl)-N-(3_u-pyridylmethyl)carbenamide {2-[(2-(2-indolyl)ethyl)amino)-6_ (1,3-tris-2-yl)(3_吼π-decyl)}-N-(3-pyridylmethyl)decylamine {6-(1_曱 口 比 唑 唑 ) _2 _2 _2) 2_(2"pyridyl)ethyl)amino](3"pyridinyl)}-N-(3-pyridylfluorenyl)carbenamide (2 {[2_(3_fluorobenyl)ethyl) Aminobutyr 6-(2-formic acid (3_σsecenyl))(3_°pyridyl))-indole-(3-hydroxypyridylmethyl)decylamine 10 15 20 {6-(4_ Basic base)_2-[(2_(2- π ratio u)yl)ethyl)](3_ σ ratio thiol)}-Ν-(3_acridinylmethyl)formamidine [2-{[ 2-〇fluorophenyl)ethyl]aminobib 6_(6-([2_(3-)-phenylphenyl)ethyl]amino-5-[Ν-(3-pyridylmethyl)aminecarboxyl] (2_ π-pyridyl)) (3_pyridyl AN-"pyridylmethyl)decylamine (2 {[2-(3-fluorobenzyl)ethyl]amino}}_6_[2-(base group) Methyl)(3_ σ thiophene)](3_pyridyl))_ν_(3-pyridylfluorenyl) guanamine knives (2 {[2-(3-fluorobenzyl)ethyl]amine卜6- 异u号味_4_基(3_. 比比定基))-Team (3_pyridylmethyl) amidoxime 酿 ethyl (4) phenyl))_2·{[2·(tetra)phenyl Ethyl]amino group you t疋 base))-Ν_(3′′ 啶 曱 曱 ))carbamamine (6-[3_(aminomethyl)(2_嗟 phenyl)]_2_ {[2_( 3_fluorophenyl)ethyl]amine Η3% 唆 )))-Ν-(3_σ-pyridylmethyl)carbamamine phenyl)ethyl]amino}_6_[5_(hydroxyethyl to thiophene) (3 比 啶 基))) Ν ( ( ( ( ( 101 101 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 Ethyl]amino}(3-cyclopyridyl)-N-(3-pyridyl-fluorenyl) Methionamine. (6-[5-(Aminomethyl)(2-σsecenyl)]-2-{[2_(3_-phenylphenyl)ethyl]amino}(3-pyridyl) ))-Ν-(3-pyridylfluorenyl)guanamine 5 (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(3-methylindenyl (2-thiophene) ()-(3-pyridyl))-N-(3-pyridylfluorenyl)decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(5- Mercapto(2-thienyl))(3-acridinyl))-indole-(3-pyridylfluorenyl)decylamine (6-(5-murine(2-nonyl))-2 - {[2-(3-Phenylphenyl)ethyl]amino} (3-π比ίο pyridine))-Ν-(3_pyridylfluorenyl) decylamine (6_(3,4_二气) Phenyl)-2-{[2-(3-phenylphenyl)ethyl]amino}(3-^pyridine))-indole-(3-acridinylmethyl)decylamine Ν- {[5-(Aminoguanidino)(3-acridinyl)]fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine }}(3-acridinyl)) decylamine (6-(2-15-nitrophenyl)-2-{[2-(3-phenylphenyl)ethyl]amino} (3-吼Basement))-N-{[5-(hydroxymethyl)(3·-pyridyl)]methyl}decylamine N-({5-[3,3-bis(dimethylamino)- 2-Azapropen-2-enyl](3-acridinyl)}indenyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl) Amino](3-u-pyridyl))indolide 2〇N-{[3-(aminoindenyl)(2-acridinyl)]fluorenyl}(6-(2-cyano) Phenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))decylamine (6-(2-cyanophenyl)-2-{[ 2-(3-Fluorophenyl)ethyl]amino}(3-acridinyl))-N-[(3-{[(6-(2-cyanophenyl)-2-{[2- (3-fluorophenyl)ethyl]amino}(3-acridinyl))carbonylamino]mercapto}(2-pyridyl))indenyl]nonanyl 102 200823188 N-[(2-{ [2-(3-Fluorophenyl)ethyl]amino}_6_phenyl(3-arridinyl)methyl 1(3-pyridylamino)carbamamine. (5_Chloro_6_(2 _Cyanophenyl)_2_{|>(3-Phenylphenyl)ethyl]amino}(3"-indenyl)-indole-(3-acridinylmethyl)carbenamide (5_ _6_(2-Cyanophenyl)-2-{[2_(3-hydrophenyl)ethyl]amino}(3"pyridinyl))-N_(3«%b^ylmethyl) Brewing amine cyano-6-(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amine 吼11 base))-N-(3-pyridylmethyl) A Amidoxime [(2-chloropt-decyl))methyl](6♦cyanophenyl)_2_(tetra)3-fluorophenyl)ethyl]amino}(3-pyridyl))indoline ({2- [(2-Aminoethyl)amino](3_acridinyl)}methyl) ( 6_(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_D-pyridyl))guanamine (2_{[2-(3-fluoro) Phenyl)ethyl]amino}}5-oxyl[3,2 succinylpyridinyl)-indole-(3-acridinylmethyl)decylamine (6-(2-cyanobenzene) Base)_2_{[2-(3-fluorophenyl)ethyl]amino}(3_ σ-pyridyl))-N-[(6-oxy(2-piperidinyl)methyl]carbamamine N |{3-[(Tertidinoxy)monoylamino]propyl b 6-oxy (2-l-fluorenyl) methyl](6-(2-cyanophenyl)_2_{[2_( 3_gasphenyl)ethyl]aminopyridinyl))carbenamide·{[1-(3-aminopropyl)-6-oxy (2_pin π-decyl)]methyl} (6 ♦Cyanophenyl)_2_{[2-(3-]phenyl)ethyl]amino}(3-centered))carbenamide (6_(2_indolylphenyl)-2-{[2·( 3-(fluorophenyl)ethyl]amino}(3Κ-l-lung _(2_ ϋ 啶 基 yl)methylcarbendazim [(1-{2-[(T-butoxy)carbonylamino]B Mercapto}(2_piperidinyl))methyl 103 200823188 base](6_(2_murophenyl) 1{[2♦fluorophenyl)ethyl]aminopyridinyl))carbenamide 5 10 15 20 N {[1 (2-Aminoethyl)-(2-piperidinyl-methyl) (6-(2-cyanophenyl)-2_{[2_(=fluorophenyl)ethyl]amine Base you bite base) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) Fluorophenyl)ethyl]amino}(3_σ-pyridyl={[1 (3-month-female-propyl)-(2-piperidinyl)]methylcyanobenzene) 2 {〇(3_Fluorine Phenyl)ethyl]amino-based acridine))carboxamide (6-(2-cyanophenyl)_2·{[2_(3-fluorophenyl)ethyl]amino} (3_.比 基 ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) 6_(2_Cyanophenyl)2 {[2(3-Fluorophenyl)ethyl]amino"(3_σ-pyridyl))decylamine>^-[((2RH_{3_[(third Butoxy-decylamino]propyl b 6-oxy (2_brupyl))methyl](6-(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl] Amino}(3-pyridyl))carboxamide N i(2R) small (3-aminopropyl)_6•oxy (2«yl)]fluorenyl}(6-(2-cyanophenyl) )-2][2_(3_Fluorophenyl)ethyl]amine-based than the bite-based amide amine Ethyl J-base} (3 比 pyridine group)) carbamide amine acetaminophen (3 _piperidinyl))methyl](6-(2-cyanophenyl)s{{2_(3-fluorophenyl)ethyl]amino}(n-decyl))-armamamine===== base Ethyl]_(3-104 200823188 N_[((3R)-l-{2-[(Tertidinoxy))-ylamino]ethyl}}(3_^σ基基)) fluorenyl]( 6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_pyridyl))carbenamide N-[((3R)-卜{ 3-[(Tertidinoxy)carbonylamino]propanyl}(3-piperidinyl))methyl](6-(2-cyanophenyl)-2-{[2-(3- Fluorophenyl)ethyl]amino}(3_σ-pyridyl)) Amine N-[((3R) small {4_[(Tertidinoxy))-ylamino]butanyl)(3«yl))indenyl](6-(2-cyanophenyl)-2-{ [2-(3-Fluorophenyl)ethyl]amino}(3_σ-pyridyl))carzamide N-{[(3R)-1-(2-month-glycosyl) (3-τι)辰基基)]methyl}(6_(2_cyanophenyl)_2-{[2-(3-fluorobenzyl)ethyl]amino} (3-11 than bite)) anthraquinone N_ {[(3R)-l-(3-Aminopropyl)-(3-piperidinyl)]fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3-d-benzene) Ethyl]amino} (3_π ratio), arylamine N_{[(3R)-l-(4-aminobutylidene)(3-piperidinyl)]methylcyanophenyl)2_ {[2-(3_乱本基)ethyl]amino}(3_吼11定基))))) ({(2)-1_[4-(1,3-dioxybenzo) [(:]嗤琳_2_yl)butyl]_6_oxy(2-piperidinyl)}methyl)(6_(2-cyanophenyl)_2_{[2_(3_fluorophenyl) Ethyl]amino}(3-pyridyl))carbenamide N {[(2R)-1_(4-month-female butyl)-6-oxy(2-mouth butyl)] methyl cyanide Phenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3_σ ratio decyl)) an amine N-[((3S,4S,2R,5R)-3, 4,5,6_four filaments (2η_3,4,5,6_ tetrahydro britylene-2_yl))methyl](6-(2-cyanophenyl)_2_{[2_( 3-fluorophenyl)ethyl]amino} (3_ ° pyridine))carbamamine [5 (N {[(2R)-l-(3-aminopropyl)_5_oxy σ ratio slightly Oral _2_yl]methyl} 105 200823188 °定定]benzamide carbazyl)-6-{[2-(3-fluorophenyl)ethyl]aminopyr 2_pyridinium 5 10 15 20 N_[2-((2R)_2· {[(6_(2_ cyanophenyl)_2_ {[2_(3_ phenylphenyl)ethylamino}(3-pyridyl))carbonylamino] fluorenyl} Pyrrolidinyl)(ls)_^methylmethicidyl](t-butoxy)carbamamine--milk N_ {[(2R)_ 1 _((2S)_2-aminopropenyl) σByridine 1 yl]methylcyanophenyl)_2][2_(3-fluorophenyl)ethyl;]amino}(3′′-indenyl))N-[(lR)-2_( (2R)-2-{[(6_(2_Cyanophenyl)_2_{[2_(3_fluorophenyl)ethyl]amino}(3-pyridyl))carbonylamino]methylpyrrolidine Methyloxyethyl](t-butoxy)carbamamine N-{[(2R) small ((2R)_2-aminopropenyl) σ-pyridyl-2-yl]methyl) (6_(2 cyanophenyl)-2-{R-(3-fluorophenyl)ethyl]aminopyridinyl guanamine N_{[(2R)_l_((2S)-2,5_ Diaminopentydenyl) σ-pyridyl] fluorenyl}(6-(2-cyanophenyl)-2_{[2_(3-fluorophenyl)ethyl]amino}}pyridyl) ) Amidoxime-[(2-chloro(3-)-methyl)ethyl](2_{[2_(3-fluorophenyl)ethyl]amine) is more than sal-4-yl (3-0) Basement)) Acrylamine-({2-[(3-aminopropyl)amino](3-acridinyl)}methyl)(2-{[2_(3•fluorophenyl)ethyl) Amino}-6-吼 吼 冰 基 (3 ϋ 。. Basement)) Amidoxime-({2-[(2-aminoethyl)amino](3_π-pyridyl)}indenyl)(2_{[2_(3_fluorophenyl)ethyl]fee }}-6-吼 吼 冰 ( (3-u ratio u base)) decanoic acid amine (2R)-2_{[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amine _}6 曱 曱 吼 吼 _ _ 4- _ _ _ _ _ _ _ _ _ 羰 羰 羰 羰 羰 羰 羰 羰 羰 羰 羰 羰 羰 羰 羰 羰 羰 羰 羧酸 羧酸 羧酸 羧酸 羧酸 羧酸 羧酸 羧酸 羧酸 羧酸 羧酸 羧酸(5_n{[2_(3_fluorophenyl)ethyl hydroxy 106 200823188 yl)-6-(1-methylpyrazole-4-yl)(3-pyridyl)) decylamine [(() 1 {2-[(di-dibutoxy)-yl)-yl]ethinyl-based 嘻2_yl)methyl]fluorene-2][2_(3-fluorophenyl)ethyl]amine 6_(1-methyloxazol-4-yl)(3-pyridyl)carbamamine (ί[2(3fluoro)ethyl)amino)b & ^ than spityl base (3_π ratio bite Earth))N ({2-[(2-light-ethyl)amino](3_π-indenyl))methyl)carbanamine [[2_{[(T-butoxy))-ylamino ]methyl}(3_σ-pyridyl))indenyl](5_fluoro 2 {[2(3-fluorobenzyl)ethyl]aminobib 6-U than salivyl-4-yl (3-17 than τι定基) )) Aromatine {{2-(Aminomethyl)(3_σ-pyridyl)]methyl}(5-fluoro_2_{[2_(3_fluorophenyl)ethyl]amino}}azole _ 4_yl (3′′pyridinyl))carboxamide [((2R) 1-{2-[(di-dibutoxy))amino]yl}}σ ratio 唆_2_ base)曱(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]aminobib 6_σ-biazole _4_yl (3-indole ratio)) aryl amine N_{[(2RH_ (2-Aminoethyl fluorenyl) π ratio slightly bite _2 _ yl] methyl} (5 _ _2_{[2-(3-fluorophenyl)ethyl]amino}}_6_pyrazole _4 _ base (3_pyridyl)) ketoamine N [((2R)-l-(3_[(dibutyloxy)))] propyl hydrazide. Methyl](5_Fluoro.2_{[2-(3-fluorophenyl)ethyl]aminodibubu 吼 冰 冰 (3-pyridyl)carbamamine N-{[(2R) small ( 3-aminopropionic acid) π 嘻 嘻 定 _ _2 嘻 嘻 嘻 嘻 嘻 定 定 嘻 定 定 定 定 定 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- 3- )) formic acid amine N_[((2R) small {4-[(Tertidinoxy)) ylamino] butyl hydrazide ratio _2_ 107 200823188 曱) 曱 Κ 5|2-{[2-(3- Fluorophenyl)ethyl]amino}e.e., such as carbazole _4_yl (3-sigma ratio-bite group), urethane-{[(2R)-1 _(4-aminobutylidene)pyrrolidinyl ]methylfluoro-2-{〇(3-fluorophenyl)ethyl]aminopyabazole ice-based heart 醯 醯5 amine ^ N-[((2R) ton 唆_2_ base) (5_fluoro_2_{[2_(3_ phenyl)ethyl]amino}_6_pyrazole-4-yl (3-pyridyl))carbenamide f n-[((2rH- {3_[(Tertidinoxy) County Amino] Propyl 5-Oxylindole α--2.yl)methyl](5_Fluoro-2-{[2_(3_Denyl)) Ethyl]amino} such as 峻10 -4-yl (3_pyridyl)) decylamine N_{[(2R)-l-(3-aminopropyl)-5-oxy π ratio 唆Methyl}(5-fluoro_2_{[2-(3-phenylphenyl)ethyl]amino}}""pyrazole+yl&pyridinyl))carbenamide N-(amine oxime) (曱基基)(5_Fluoro-2_{[2_(3·fluorophenyl)ethyl]amino}}_6_. Ratio 15-oxazol-4-yl(3-pyridyl))carbenamide 2-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}}_6_carbazole_4 _ group (3_mouth ratio 'pyridyl))carbonylamino]-N-mercaptoacetamide N-[((2R)-l-{(2S)-2-[(t-butoxy)carbonyl) Amino]_3_hydroxypropanyl}pyridin-2-yl)indenyl](5-fluoro-2-{[2-(3-fluorophenyl)ethyl;]amine 2〇}}-6 -pyrazol-4-yl(3-pyridyl))decylamine N-{[(2R)-l-((2S)-2-amino-3-transpropionic acid) 吼嘻_2 _基]曱基}(5-乱-2-{[2-(3-气本基)ethyl]amino}}_6_11 sits _4-base (3-11 ratio) and formamide [3-(Aminoguanidino)-6-phenyl (2_σ ratio)][2-(3-Fluorophenyl)ethyl]amine 108 200823188 N-[(2_{[(di-butoxy) ) anthranyl]methyl}(3_u ratio σ-decyl))methyl](5-fluoro-2_{[2-(3-fluorophenyl)ethyl]amino}_6_(2_π ratio) (3_σ) Tetamine ι N_{[2-(aminomethyl)(3-fluoridinyl)]methyl}(5•fluoro-2_{[2_(3_fluorophenyl)ethyl]amine }冬(2_吼咬基)(3_吼.定基))Methylamine (5_气-2-{[2_(3-fluorophenyl)ethyl]amino}}_6_(1_methylpyridyl) Imazon oxime to sulfhydryl))-N-hydrazinomethylpropyl)carbamamine 10 15 20 (5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}_6 servylmethylhydrazine pyridyl))-N-(3-hydroxy-2,2_2 Methyl propyl) decylamine = 2 = 2 - methyl _ 3 oxy butyl) (5 | 2 side 3 _ Benzene ethyl) Female methyl pyrazole 4 yl) (3 π pyridine group )) Methionine N-((2R)-3_transyl 2,3-dimethylbutylhydrazine 5_fluoro_2_{[2_(3_气,]^基}-6-(1- Methyl hydrazine _4_yl) (3 吼 吼 ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) Amino group] winter (1_methyl hydrazine) (3_° ratio), silky amino]methyl}nitropyryl)-2-oxoethyl ester acetate 2 side_2_{[ (lacquer 2 side 3_fluorophenyl)ethyl]aminoethyl hydrazide 4-yl) (3♦ fixed)) county amine group] methyl such as ii [(5L_(3 · phenyl) ethyl] amine ^ Γ Γ ( 四 四 ] ] 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 _Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_pyridine)) formamide (5-fluoro-2-{[2-(3- Fluorophenyl)ethyl]amino}_6_pyrazole_4_yl(3_pyridyl))-indole-(3^pyridylmethyl)decylamine 5 n-{[(2RM-(2) -aminoethenyl)pyrrolidine_2_yl]A Fluorine-2-{[2-(3-fluorophenyl)ethyl]amine b ((丨-methyl 0-pyridyl-4)-) (3_σ-pyridyl))caraamine (6-(2) -Cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]aminobi-4-yl-pyridyl))-Ν-(3-pyridylfluorenyl) decylamine 10 (6-( 2_cyanophenyl)_2_ί[2-(3-fluorophenyl)ethyl]amino}(3_acridinyl))·Ν_[(6_?琳_4_基(3" ratio bite base )) thiol] guanamine (6 <2_Cyanophenyl)_2·{Ι>(3-fluorophenyl)ethyl]amino}(3_ π-pyridyl))-Ν-[(6_πpyrrolidyl(3_pyridyl)) )methyl]carbamamine (6-(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amino}(3• acridine-15-yl))-N_[(6- Piperene (3_° to pyridyl)) mercapto]carbamamine N-{[6_(4-ethylhydrazine) (3^pyridinylcyanophenyl)-2-{[ 2_(3_Fluorophenyl)ethyl]amine-based alkaloids [(6_漠(2_°比咬))methyl](6-cyanophenyl)_2_{[2_(3_ Fluorophenyl)ethyl]amino}(3-pyridyl))decylamine 2〇2 very {[2_(3-fluorophenyl)ethyl]amino} o-(via fluorenyl) (2 _ 嗟 基 ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) Aminobi 6_[5_(transmethyl)(2_nonyl)](3-pyridyl)) guanamine (2_{[2-(3βfluorophenyl)ethyl)amine 6-[5-(hydroxyindenyl)(2_thiophene 110 200823188)](3^pyridyl))-N-(2-acridinylmethyl)carbenamide-N-(aminocarbazinyl) Methyl)(2-{[2-(3-fluorophenyl)ethyl]amino}-6-[5-(hydroxymethyl)(2-thiophenyl)](3-acridinyl))- Guanamine 2 - [(6-(2-carbophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3-吼σ定5 base))carbonylamino]-Ν- (曱-sulfonyl) acetamidine-{[3-(aminomercapto)cyclohexyl]fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3-fluoro Phenyl)ethyl]amino}(3-acridinyl))guanamine 3-[(6-(2-indolylphenyl)-2 -{[2-(3-)phenyl)ethyl Amino}-3-° ratio σ base) carbonylamino]cyclopropanecarbamamine 1〇(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl Amino}(3-acridinyl))-N-(2-piperidinylethyl)decylamine (6-(2-carbylphenyl)-2-{[2-(3-p-benzene) Ethyl)amino}(3-indenyl)-indole-(2-indole-2-ylethyl)decylamine (6-(2-carbylphenyl)-2-{ [2-(3-Phenylphenyl)ethyl]amino}(3-° ratio σ15 base))-Ν10-plough-2-ylmethyl)carbamamine N-((lS)-5 -amino-1-amine-mercaptopentyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl) )) indoleamine N-(3-amino-1-aminomercaptopropyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl] Amino}(3-pyridyl))decylamine 20 N-{(1R)-1-amineindolyl-5-[(phenyldecyloxy)carbonylamino]pentane } (6-(2-carbophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3-吼σ定基))carboxamide N-(4-amino -1-aminomercaptobutyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))indole Indoleamine 111 200823188 N_((1R)_5-Aminosamineamine-mercaptopentyl)(6-(2-cyanophenyl)2 {[2·(3-fluorobenzyl)ethyl]aminopyridinium Base)) indoleamine-({6-[(2-aminoethyl)amino](2_σ-pyridyl))methyl)(6-(2-cyanophenyl)-2-{[2 -(3_fluorophenyl)ethyl]amino}(3_pyridyl))carbenamide-({6-[(3-aminopropyl)amino](2-pyridyl)}A (6)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_acridinyl]](4rh-aminemethanyl_4_[ (6_(2_Cyanophenyl)_2_{[2_(3_气phenyl)ethyl]amino}(3′′pyridinyl))alkylamino]butyl hydrazine (phenylmethoxy) Methionine N-((lS)-4_aminoamine-mercaptobutyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine N-((lR)-4-amine-based small amine-mercaptobutyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)) Ethyl]amino}(3-anthraquinone))carbenamide (6-(2- Phenyl))_2_{[2-(3-fluorophenyl)ethyl]amino}(3-,pyridyl))-N-(pyrrolidin-3-ylmethyl)decylamine-{ [1-(2-amino-2-indenylpyrrolidinyl-3-yl]methyl}(6-(2-cyanophenyl)-2-{indole(3-fluorophenyl)ethyl]amino} (3_Acridine))carbamamine-{[1-(3-aminopropionyl)π-pyridyl-3-yl]methyl}(6-(2-cyanophenyl)-2 -{[2·(3_Fluorobenzyl)ethyl]amino group)) decanoic acid N-{[1-(4-aminobutylidene) π-pyridylpyridinyl] fluorenyl}(6_(2 _Cyanophenyl)-2-{[2-(3-fluorobenyl)ethyl]amino}(3_σ ratio η-based)) decylamine N-[(l-ethyl with base u ratio slightly biting winter (6-(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amino} (3-° ratio), 曱 Ν Ν { - { [ 1- (3-aminopropyl)π-pyrrolidinoyl]mercapto}(6_(2-cyanobenzene 112 200823188)_2_{[2_(3-fluorophenyl)ethyl]amino}(3_ Roar. Basement)) N-(3-Amino-2-aminomercaptopropyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl) Amino}(3_吼)) an amine (2][2_(3-fluorophenyl)ethyl]amino}_6_(1_mercaptocarbazole_4_yl) (3) ratio Pyridyl))-N-[(6-oxypipedin-2-yl)indolyl]carbamamine (2_{[2-(3-fluorophenyl)ethyl]amino)b 6-carbazole (3-Acridine))[[6-oxypiperidin-2-yl)methyl]carbamamine (2-{[2_(3-fluorophenyl)ethyl]amino)_6_ σ Than the saliva _5_ group (3_ σ ratio bite base)) _ Ν _ [(6-oxypipe pi _ 2 _ _ yl) hydrazino] carbamide Ν-{[(2S)-4-(methyl sulfonate氧基oxypiperidin-2-yl]methyl octa-6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino)(3-,pyridyl) Methionine N-[((2S)-4-ethinyloxypiped_2_yl)indolyl κ6_(2-cyanophenyl)-2-{[2-(3-fluorophenyl) Ethyl]amino group butyl group)) formic acid amine N-[((2S)-4_methyl_6_oxypiperidin-2-yl)methyl](6-(2-cyanophenyl) -2-{[2-(3-fluorophenyl)ethyl]amino}(3_pyridyl))carbamamine (6-(2-murylphenyl)_2_ {[2_(3_fluorine) Phenyl)ethyl]amino hydrazine & aridinyl))-N_{2_[(methylamino)alkylamino] Ethyl decanoic acid amine N-(2_{[(2-aminoethyl)sulfonyl]amino}ethyl) (6 <2•Cyanophenyl:)_2][2_(3-fluorophenyl)ethyl]amino}(3♦定))) 曱醯 柯 吼 吼) ](Μ·cyanophenyl)_2_{[2 gas phenyl)ethyl]amino}〇π-pyridyl))carbamamine 2-amino Ν-{2-[(6_(2-cyanide) Phenyl))_2_{[2_(3_fluorophenyl)ethylamino}(3-indole)) arylamino]ethyl hydrazide 3_amino-Ν· {2-[( 6_(2-cyanophenyl from {[2_(3-fluorophenyl)ethyl]amine 113 200823188 }(3-Acridine)carbonylamino]ethyl}propanamine 4-amino- N-{2-[(6-(2-N-phenylphenyl)-2-{[2-(3-phenylphenyl)ethyl]amine)-yl}(3-acridinyl)carbonylamino] Ethyl}butanamine 2-[(tatabutoxy)carbonylamino]-indole_{2·[(6_(2-cyanobenzene-5yl)-2-{[2-(3-phenylphenyl) Ethyl]amino}(3 σ 定 ))) fluorenylamino]ethyl bromide-methylacetamide 4-[(tatabutoxy)carbonylamino]-Ν-{2-[ (6-(2-Cyanophenyl)_2-{[2-(3-fluorophenyl)ethyl]amino}(3^pyridyl))carbonylamino]ethyl}-mercapto醯amine ίο N-{[(2S)-l-(2-Aminoethyl fluorenylpyrrolidinyl-2-yl]methyl}(6-(2-cyanophenyl)-2-{[2 -(3-fluorophenyl)ethyl]amino}(3- Pyridyl)) indoleamine N-{[(2S)-l-(3-aminopropionyl)oxaridin-2-yl]fluorenyl}(6-(2-cyanophenyl)-2 - {[2-(3-Phenylphenyl)ethyl]amino}(3-ntbσ-based)) decanoic acid N-{[(2S)-l-(4-aminobutylidene)pyrrolidin-2 -yl]fluorenyl}(6-(2-cyano15 phenyl)-2-{[2-(3-phenylphenyl)ethyl]amino)(3-13⁄4σ-based)) decanoic acid amine 2 - Amino-_N_ {2-[(6-(2-)-ylphenyl)-2-{[2-(3-phenylphenyl)ethyl]amino}(3-acridinyl))carbonylamino Ethyl b-N-mercaptoacetamide 3-amino-N- {2-[(6-(2-mercaptophenyl)-2 - {[2-(3-phenylphenyl)ethyl]] Amino}(3-acridinyl))carbonylamino]ethyl}-N-mercaptopropionamide 20 4-Amino-N-{2-[(6-(2-n-phenylphenyl)-) 2-{{2-(3-Phenylphenyl)ethyl]amino}(3·-pyridyl))carbonylamino]ethyl}-N-mercaptobutylamine (6-(2-cyanide) Phenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-tonidyl))-N-{2-[methyl(fluorenylsulfonyl)amine Ethyl}decylamine 3-amino-N-(2-aminoethyl)-2-{[(6-(2-cyanophenyl)-2-{[2-(3-fluorobenzene) 114 200823188 .  Ethyl]amino}(3-pyridyl))carbonylamino]methyl}propanamine-N-(2-Wittylamino-2-mercaptopropyl) (6-(2-cyano) Phenyl)-2-{[2-(3-fluorobenzene).  Ethyl]amino}amino}(3-acridinyl))carboxamide N_((2S)_2-amino-3-hydoxypropyl)(6-(2-cyanobenzene-5yl)- 2_{[2_(3-fluorophenyl)ethyl]amino}(3′′) 曱醯amine N-((lS)-l-{[(6-(2-cyanophenyl)) -2-{[2-(3-Fluorophenyl)ethyl]amino} (3_ ° ratio), carbylamino]methyl}_2-ylamino)-2-aminoethyl hydrazine Amine 2-aminoacetic acid (2S)-2-(2-aminoethenylamino)>3-[(6-(2-cyanophenyl)-2_{〇(3_fluorophenyl)) Amino group}(3_t-decyl))alkylamino]propanyl ester N-((lR)-l-{[(6-(2-cyanophenyl)-2-{[2-( 3-fluorophenyl)ethyl]amino carbazyl))carbonylamino]methyl-2-mercaptopropyl)_2-hydroxyacetamide N_((1R)_1_{[(6_(2-cyanide) Phenyl))_2_{[2_(3-fluorophenyl)ethyl]amine-based pyridyl))carbonylamino]methyl}-2-methylpropyl)_2-aminoacetamide 15 N- ((2R)-2-aminolmethylpentyl)(H2_cyanophenyl)_2_ {[2-(3-fluorophenyl)ethyl]amino}(3_acridinyl)) A Indoleamine N-((lR)_l-{[(6-(2-cyanophenyl)_2u3_gasphenyl)ethyl-amino-pyridyl))carbonylamino]methyl-3-yl Butyl)_2_hydroxyacetamidine team ((1)_1-{[(6- (2_Cyanophenyl)1{[2 fluorophenyl)ethyl]amine base 20 t base)) arylamino] hydrazinyl butyl) sulfhydryl amine N-((lR ,-2-amino group, small {[(6-(2-p-phenylphenyl)-{[2_(3-fluorophenyl)ethyl]amino}(3♦)))alkylamino] fluorenyl }Ethyl)1-aminoethylamine N-((1R)-2-amino-based cyanophenyl][2_^_phenylphenyl)ethyl]amino}(3-吼)) Aminomethyl]methyl}ethyl)_2_yl acetamide 115 200823188 N-((3R)_2_oxy(3_piperidinyl 6·...cyanophenyl)_2_{[2_(3 - gas phenyl) ethyl]amino} (3-° thiol)) formamide {2_[((2R)-2-phenylpropyl)); j_6_phenyl (3-acridine) Base)}_N_(3"pyridylhydrazinyl)carbamamine 5 10 15 20 N_(amine-mercaptoethyl)(6_(2-cyanophenyl)_2_{[2-(3-fluorophenyl) Ethyl]amino}(3-pyridyl))carbenamide n-((ir)_i-aminocarbamidoethyl)(6_(2-cyanophenyl)_2-{[2_(3_ Fluorophenyl)ethyl]amino}(3-pyridyl))carbenamide (2S)_2_[(6_(2-cyanophenyl)_2_{[2_(3_ phenyl)ethyl) Your acridine))carbonylamino]propionic acid methyl ester methyl(2R)_2_[(6_(2-cyanophenyl)-2-{[2-(3-fluorobenzyl)ethyl]amino) }(3-σ ratio bite base)) benzylamine methacrylate 1 』 2-[(6_(2-cyanophenyl)_2][2_(3-fluorophenyl)ethyl]amine b Carbonylamino]methyl acetate methyl]amino}(3-u-bito)amino}(3-pyridine(6-(2-cyanophenyl)_2_ {[2-(3-fluorophenyl) Ethyl))_Team (2-hydroxyethyl) decylamine (6-(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl))-N-(2-methoxy Benzyl)carbendazim 2_(didecylamino)ethyl](6-(2-cyanophenyl) is a gas phenethyl]amino}(3-π ratio) Amine-tert-butoxy)-Ν-mercaptocarbonylamino]ethyl}(6-(2-cyano)-2-{[2-(3-fluorophenyl)ethyl]amino} (3"唆 唆))) ""N-phenylphenyl"-2-{[2-(3-fluorophenyl)ethyl]aminopurine (3_ π-base))-Ν-[2-(decylamine) Ethyl] decylamine 116 200823188 Ν·(3-Aminopropyl)(6-(2-n-phenylphenyl)-2-{[2-(3-(phenylphenyl)ethyl)amino) } (3-pyridyl)) decylamine. .  (2S)-2-[(6-(2-Mercaptophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}}(3_~pyridyl))carbonylamino] -Ν-mercaptopropionamide 5 (6-(2-cyanophenyl)_2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))-N- [2-(decyloxycarbonylamino)ethyl]decanoic acid amine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3 -acridinyl))-N-{2-[(decylsulfonyl)amino]ethyl}decylamine 3- [(6-(2-murylphenyl)-2-{[2- (3-fluorophenyl)ethyl]amino}-3-° ratio 0 base) ίο carbonylamino]ethyl propionate 4- [(6-(2-cyanophenyl)-2- {[2 -(3-fluorophenyl)ethyl]amino}(3-acridinyl))carbonylamino]-indole-mercaptobutylamine Ν-(3-aminomercaptopropyl) (6- (2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-indolyl)-methaneamine 15 Ν-(2-aminoethyl (6-(2-N-phenylphenyl)-2-{[2-(3-phenylphenyl)ethyl]amino}(3-acridinyl))decylamine (6-(2-gas) Phenyl)-2-{[2-(3-phenylphenyl)ethyl]amino}(3_^specific),N-[(4-fluorophenyl)indenyl]decylamine 6-(2-muropylphenyl)_2- {[2-(3-oxaphenyl)ethyl]amino}(3 -exopurine 2 fluorenyl))-Ν-[(4- Phenyl) indenyl] indoleamine N_((1S)-1-amineindol-2-hydroxyethyl)(6-(2-cyanophenyl)-2-{[2-(3- Fluorophenyl)ethyl]amino}(3-acridinyl))decylamine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine }}(3·-pyridyl))-N-(3-hydroxypropyl)methalamine 117 200823188 (6-(2-aminophenyl)-2-{[2-(3-fluorophenyl) Ethyl]amino}(3-^pyridyl)-indole-(3-methoxypropyl)formamide.  (2S)_2-[(6-(2-Vinylphenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-σΛpyridyl))carbonylamino]- Methyl 3-hydroxypropionate 5 (2R)_2-[(6-(2-cyanophenyl)-2-{〇(3-fluorophenyl)ethyl]amino}(3-hydroxypyridyl) ) carbonylamino]-3-hydroxypropionate oxime ester (6-(2-carbophenyl)-2-{[2-(3-phenylphenyl)ethyl]amino} (3-11 than bite Base))-Ν(2-acridinylmethyl)formamidine (6-(2-carbophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}( 3-σ ratio bit 〇1))-Ν-[(4-mercaptophenyl)methyl]carbamamine (6-(2-carbylphenyl)-2-{[2-(3- gas Phenyl)ethyl]amino}(3-^specific sigma))-indole-[(6-fluorenyl(3-acridinyl))indolyl]nonanylamine (6-(2-cyanobenzene) -2{[2-(3-Fluorophenyl)ethyl]amino}(3·-pyridyl))-N-[(6-fluorenyl(2-hydroxypyridinyl))fluorene Amidoxime 15 (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_acridinyl))-N-(2 -(2-acridinyl)ethyl)carbenamide (6-(2-(phenylphenyl)-2-]{[2-(3-)phenyl)ethyl]amino} (3-° ratio Pyridyl))-N-(2-(3-acridinyl)ethyl)decylamine N-[(6-amino(3-acridinyl))indenyl](6-(2-cyano) Phenyl)-2_{[2-(3 -fluorophenyl-2-mercapto)ethyl]amino}(3-acridinyl))decylamine (6-(2-cyanophenyl)_2-{[2-(3-fluorophenyl)ethyl) Amino}(3-acridinyl))-N-[(6-decyloxy(3-acridinyl))indolyl]decylamine (6-(2-carbophenyl)-2- {[2-(3-Phenylphenyl)ethyl]amino}(3-^pyridine))-indole-[(2-indolyl(3-acridinyl))indolyl]nonanyl 118 200823188 N-[(2-Amino (3-°-Butyl))methyl](6-(2-n-phenylphenyl)-2_{[2-(3-(phenyl)-yl)ethyl]amine (3-pyridyl))carbenamide _ (6-(2-carbophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3- ntb fluorenyl) ))-N-[(2-methoxy(3-acridinyl))methyl]methaneamine 5 (6-(2-cyanophenyl)-2-{[2-(3-fluorobenzene) Ethyl]amino}amino}(3-acridinyl))-indole-[(1-hydroxy(2-acridinyl))indolyl]carbamamine (6-(2-murylphenyl)- 2·{[2-(3·Phenylphenyl)ethyl]amino}(3- utbinyl))-indole-[(1-hydroxy(3-acridinyl))methyl]decylamine ( 6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinium) group_N-[3-(4-mercaptopiperidone) Plough base) propyl] formamide, (6-(2-cyanophenyl)-2-{[2-(3-Iphenyl)ethyl]amino} (3-吼) Base))-Ν-(cyclopropylindenyl) amidoxime-[2-(dimethylamino)ethyl]-2-[(6-(2-carbophenyl)-2-{{ [2-(3-(phenyl)ethyl]amino}(3-acridinyl))carbonylamino]acetamide 15 2-[(6-(2-cyanophenyl)-2-{ [2-(3-Fluorophenyl)ethyl]amino}(3-acridinyl))carbonylamino]-indole-(2-hydroxyethyl)acetamidoxime-(2-aminoindenyl) Ethyl)-2-[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}} (3-^ ratio σ-based)) lutylamine Ethylamine 342-[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}}-3-portyl 20 acyl)carbonylamine ]]Ethylamino}}propionic acid propionate-{3_[(tatabutoxy)carbonylamino]propyl}-2-[(6-(2-cyanophenyl)-2-{[2 -(3-fluorophenyl)ethyl]amino}(3-diaridyl))carbonylamino]acetamidoxime-[3-(didecylamino)propyl]-2_[(6- (2-cyanophenyl)-2-{[2-(3-fluorobenzene119 200823188,)ethyl]amino}(3-pyridyl))carbonylamino]acetamide 2_[(6_(2) _Cyanogen base) 2-{[2:(3_Fluorophenyl)ethyl]amino hydrazine (3_π ratio), carbonylamino]-N-(3-propylpropyl) acetylamine Di-(2_[(Tertidinoxy))indolylcarbonylamino]B卜2 you ♦ cyano phenyl) 2 {[2 (3-fluorophenyl)ethyl]amino} (3_π than butyl)) arylamino] acetamidine 2-[(6-(2- Cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amino}η-pyridyl))alkylamino]-indole-[2-(methylamino)ethyl]acetamidine Amine 10 15 (2S)-3-Amino-2_[(6-(2-cyanophenyl)-p-phenylene)ethyl]amino}(3′′pyridinyl))carbonylamino]propionic acid Methyl N-((lS)-2-amine-based small amine-mercaptoethyl)(6-(2-cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl]amino}( 3_π 唆 )))) formic acid amine (2S) _3_[(dibutyloxy)carbonylamino]_2 hexa-6-(2-cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl Amino}(3_吼 基 》 几 几 几 几 几 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 2S)-3-Amino-2_[(6_(2-cyanophenyl) is called 3_yl} (3-mouth ratio), a few amino-amine oxime, dimethyl dimethyl-branched amine " 3Γ=(6_(2_cyanophenyl>2 training 3-dephenyl)ethyl]amino} (3- ratio. Mercapto))carbonylamino]propionic acid 120 20 200823188 (2S)-2-Amino-3-[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)) Ethyl]amino}(3-lideridinyl))carbonylamino]propionic acid decanoate (2S)-2-(ethinylamino)_3-[(6-(2-cyanophenyl)-2 -{[2-(3-Fluorophenyl)ethyl]amino}(3-pyridyl))carbonylamino]methyl propionate 5 10 15 20 N-((2S)_2_Amino-2- Aminocarboxylic acid ethyl)(6_(2-cyanophenyl)-2_{〇(3-fluorophenyl)ethyl]amino}(3-π ratio π-decyl))carbenamide N-{(1S )_1_Aminomethylmercapto-2-[(6-(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amino}(3-pyridyl))carbonylamino]B Acetylamine (2S)-2-amino-3·[(6-(2-cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl]amino}} (3_吼Pyridyl))carbonylamino]-indole-methylpropanamide (2S)1amino-3-[(6-(2-cyanophenyl)-like fluorophenyl)ethyl]amino} (3_ Acridinyl))alkylamino]-indole, indole-di-f-propionylamine (2s)_2-amino _h(6_(2-cyanophenyl)_2_{[2_(3_-phenylphenyl) Ethyl]amino}(3′′pyridinyl))carbonylamino]propionic acid (10)-2-(ethyl aryl amide (6) cyanophenyl)_2_{[2_(3_ phenyl) Ethyl]amino}(3_acridinyl))alkylamino]-N- Methylpropionic acid amine (=)-3-amino 2-[(6-(2-cyanophenyl)_2_{[2_(3-)phenyl)ethyl]amino}(3-pyridyl Dcarbonyl) Amino]methyl propionate = 1R>2_Amino-amine amine-mercaptoethyl)(6-(2-cyanophenylfluorophenyl)ethyl]amino}(3"bis))carboxylic acid Amine amine H[(6_(tetra)silyl)_2泰(tetra)fineethyl]amine](3_pyrrole))carbonylamino]_N_methylpropionamide=ϋ^3_[(6_(2_ Base phenyl)·2-{[2·(3-fluorophenyl)ethyl]amine earth}〇 欠 base))carbonylamino]methyl propionate 121 200823188 N-((2R)-2-amine -2-2-aminocarbazide ethyl)(6_(2-cyanophenyl)_2_ {[2_(3_ _ _ _ yl) ethyl]amino} (3-π fluorenyl)) decylamine (6 -(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amino}(3_^pyridinyl))-N_(lL sitting_2_ylmethyl)decylamine 5 (2S>2-[(6-(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amino}} (3_, than bityl)) tetamine group]-3- N-[(6-Cyano(3-acridinyl))indenyl](2_{[2_(3-fluorophenyl)ethyl]amino}-6-phenyl) 3-indenyl)) indoleamine N-{[6-(aminomethyl)(3_π-pyridyl)]methyl)(2-{[2_(3-fluorophenyl)ethyl]· 10 Amine base}_6_ (3-pyridyl))carbenamide-[(3,4-difluorophenyl)methyl](6-(2-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl Amino} (3-anthraquinone))cardamate 4-[(6-(2-cyanophenyl)-2-{[2_(3-fluorophenyl)ethyl]amino)b_ Acridineyl)carbonylamino]butyric acid 15 3_[(6-(2-cyanophenylfluorophenyl)ethyl]amino}(3_acridinyl))carbonylamino]]ΝΝ曱propyl Indole 4-[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}}_3_π-pyridyl)carbonylamino]butyric acid methyl ester 1 2-Amino-l-(2-{[2-(3-fluorophenyl)ethyl]aminobiphenyl 6-styl (3_σ-pyridyl)) 20-Ethyl-1-oxo-{2_[( 6_(2_Cyanophenyl)_2_{[2_(3·fluorophenyl)ethyl]aminobib π-decyl)-based amino]ethyl}ethylamine (called 2-[(6_(2) ·Cyanophenyl)·2·{[2_(3_fluorophenyl)ethyl]amino}(3′′ σ疋))) 叛 胺 胺 ] 122 122 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 -{[4-(Aminoguanidino)(2_u-pyridyl)]methyl}(6-(2-cyanobenzene-yl)-2-{[2-(3-fluorophenyl)ethyl; Amino}(3_pyridyl)carbamamine N_[(5_{[(t-butoxy)carbonylamino]methyl octa]. Bisyl))methyl](6-(2-cyanyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-indolyl))carbenamide N -{[5-(aminoindenyl)(2_,pyridyl)]methyl}(6-(2-cyanophenyl)-2-{[2_(3-fluorophenyl)ethyl]amino }(3_π比唆基)) amidoxime-{[4-(aminomethyl)(2·-pyridyl)]fluorenyl}(2-{[2_(3_fluorophenyl)ethyl) Amino}-6-phenyl(3-anthraquinone)) Amidoxime-{[5-(aminomethyl)(2_π-pyridyl)]fluorenyl}(2_{[2_(3_ Fluorophenyl)ethyl]amino}_6-phenyl(3-吼π-decyl))decylamine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)) Ethyl]amino}(3_σ ratio)-Ν-(isoxazol-5-ylindenyl)guanamine 2-{[2·(2_{[2_(3-fluorophenyl)) Amino]-6-phenyl (3_fluorenyl) hydrazinyl)-2-hydroxyethyl]amino}acetamide 123 200823188 }}(3-pyridyl)) decylamine N-{2-[6- (aminomethyl)(2-acridinyl)]ethyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3 -acridinyl)) amidoxime-{2·[6-(aminomercapto)(2-acridinyl)]ethyl}(2-{[2-(3-fluorophenyl)ethyl 5 Amino]-6-phenyl(3-acridinyl))carbenamide N-{[6-(2•Amino) (2-(acridinyl)]methyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl) )) indoleamine N-{[6-(2-aminoethyl)(2-acridinyl)]fluorenyl}(2-{[2-(3-fluorophenyl)ethyl]amino} -6-phenyl(3·-pyridinyl))carbenamide ίο N-[2-(2-aminoethoxy)ethyl](6-(2-cyanophenyl)-2_ {[ 2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))carbenamide (6-(2-carbylphenyl)-2_{[2-(3-phenylphenyl)ethyl) Amino}(3-° ratio σ定' base))-Ν-{[6-(hydroxyindenyl)(2-acridinyl)]fluorenyl}carbenamide N-{[3-(amino group) Phenyl)phenyl]fluorenyl}(6.(2-cyanophenyl)-2-{[2-(3-fluoro15phenyl)ethyl]amino}(3-acridinyl)) Indole 2-[(6-(2-carbophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}} (3-17 butyl) carbonylamino]-N , N-dimethylacetamide N-{2-[(2-aminoethyl)amino]ethyl}(6-(2-carbylphenyl)-2-{[2-(3_fluoro Phenyl)ethyl]amino}(3-acridinyl))decylamine 20 (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine (3-(3-pyridinyl))-indole-[(2-oxy(3-piperidinyl))methyl]decylamine (6-(2-cyanophenyl)-2-{[ 2 -(3-fluorophenyl)ethyl]amino}(3-acridinyl))-N-(oxazol-3-ylmethyl)decylamine (6-(2-carbylphenyl)- 2-{[2-(3-Phenylphenyl)ethyl]amino} (3-° ratio 124124 200823188)) _[(1-methylpyrazolyl)methyl]carbamamine- N-{[4-(Aminomethyl)phenyl]fluorenyl}(6-(2-cyanophenyl)_2-fluorophenyl)ethyl]amino}(3-indole) Amidoxime-[(6-{[(2-aminoethyl)amino]methyl}(2_pyridyl))methyl](6-(2-cyano-5-phenyl)-2-{[2 -(3-fluorophenyl)ethyl]amino}(3-° thiol))methylamine 6_{[(6♦ cyanophenyl)-2-{[2_〇fluorophenyl) Aminodipyridinyl)aminoamino]methyl}σ is more than 6-{[(6-(2-cyanophenyl)_2_{[2_(3_) Fluorophenyl)ethyl]aminopyridinyl)carbonylamino]methyl}acridine-2-carboxylic acid 1〇6][(6_(2_cyanophenyl)_{[2_(3_fluorine) Phenyl)ethyl]amino}_3_,pyridyl-yl)carbonylamino]indenyl}pyridine-2-carboxamide (6-(2-cyanophenyl)-2-{[2·(3) -fluorophenyl)ethyl]amino}(3_ σ-pyridyl))-indole-[(1-mercaptocarbazole-5-yl)indolyl]carbamamine N-((3S)-l- {2-[(Tertibutoxy)carbonylamino]ethyl}_2-oxygen Base 哌 哌 哌 哌 哌 ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) (3S) small (2_aminoethyl)oxy (3_Bistidyl-p-cyanophenyl)_2_{[2_(3-fluorophenyl)ethyl]amino} (3"-pyridyl) Nindolamine N (Liao 2-oxy_3_[(phenylmethoxy)alkylamino] brigade base} ethyl) (6_(2_cyanophenyl)_2_{[2_(3 _Fluorophenyl)ethyl]aminopoline "Bitter base") decylamine = 2-((38)-3-amino-2-oxobenzylidene)ethyl](6_(2-cyanide) Phenyl))-2-{[2-(3.fluorophenyl)ethyl]amino}(3+decyl)) decanoic acid amine {{2-(aminomercapto)phenyl]indenyl hydrazine (6♦Cyanobenzene 125 200823188 Phenyl)ethyl]amino}(3-anthraquinone))cartoamine (6-(2-cyanophenyl)_2_{〇(3-fluorophenyl)B Aminopyridinyl))_Ν-[(2_oxyl) 甲 唆 3 3 ] ] ] ] 甲 [ [ [[2-{2-[(Tertibutoxy)carbonylamine Ethyl]ethyl}(3_exidyl)methyl 5 10 15 20 yl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3_σ-pyridyl))carbamamine Ν{{〇(2-aminoethyl)(3_u-pyridyl)]methyl}(6_(2_]yl)-2-{[2-(3-fluoro Base) B Amino}(3-12-indenyl))amine hydrazide-{2-[3-(aminomethyl)(2_,pyridyl)]ethyl}(6-(2-cyanophenyl) -2-{[2-(3-Fluorophenyl)ethyl]amino} (3-σ ratio), formamide = ((3S)-2-oxypyrrolidin-3-yl) ( 6_(2_Cyanophenyl)_2_ {[2_(3_fluorobenyl)ethyl]amino}(3-anthraquinone))cartoamine (6_(2-cyanophenyl)_2_{[ 2_(3_Fluorophenyl)ethyl]aminol 吼 吼 基 ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) Acid amine Ν-{[1-(2-aminoethyl)_2-oxy (3_π辰)] fluorenyl 2_ylphenyl)-2_{[2-(3_fluorophenyl) Ethyl]amine j (3_n than bite)) A drunk (tetra)-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine ^3_π than bite)) good{[ 1-(3-diazo3·aza-propyl)methyl}carbamimidinyl]] (=(2-cyanophenyl)-2-{[2_(3_fluorobenzene) Ethyl]ethyl] Ν♦diazo-3-azapropan-3-3-diyl)m-mercapto]carbamamine fluorenyl)) G storm J-month female base} (3_pyridyl)) formamide 126 200823188 N-[((2R)_1-methylpiped: yl)methyl](6_(2-cyanophenyl)_2_{[2_(3_fluorophenyl)ethyl]amino}} -pyridyl)) indoleamine N-[(( 2R)-1-Ethyl peptidyl-2-yl)methyl](6-(2-cyanophenyl)_2_{[2_(3·fluorobenzyl)ethyl]amino}(3-吼σ Basement)) Amidoxime - {[(2R)-1-(ethylsulfonyl)piped_2_yl] fluorenyl} (6-(2-cyanophenyl)-2_{|> (3_fluorophenyl)ethyl]amino}(3′′pyridinyl))carboxamide (2R)_2_{[(6-(2•aminophenyl)_2_{[2_(3_fluorobenzene) Ethyl]amino]amino}(3_pyridyl))carbonylamino]methyl}piperidinecarboxylic acid methyl N-[((2S)-1-ethylindol-4-ylpiperidine_2_ Methyl](6_(2_cyanophenyl)2-{[2_(3_fluorophenyl)ethyl]amino}} (3′′ 唆 )))carbamamine (2s)_2_ { [(6-Indolyl phenyl)_2_ {[2 fluorophenyl)ethyl]amino)(3_pyridyl))carbonylamino]methyl}_4_methylpipedine methyl ester N_ { [(2R)-1 -(2-Aminoethyl)piperidinyl-2-yl]methylindole (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)) Ethyl]amino}(3-11 than butyl)) arylamine N_{[(2R)_1_(3_aminopropenyl)piped-2_yl]methyl}(6-(2_ Aromatic phenyl)-2-{[2-(3-fluorophenyl)ethyl]aminodinyl))carboxylic acid amine ke (10) small (4) aminobutanyl) brityl] methyl} (6_(2_ Aromatic phenyl)-2_{〇〇 笨 笨Ethyl]amino}amino}(3_σ-pyridyl))carbamamine {{(2S)-1_(2-aminoethyl aryl)_4_methyl oxime]methyl}(6-cyanide) Phenyl))_2_{[2_(3_fluorophenyl)ethyl]amino}(3_吼))) Amine Amine Group {[(2s)-i-(3_Aminopropyl) _4_Methylpiperone_2-yl]methyl}(6-sodium-cyanophenyl)indole-{[2♦fluorophenyl)ethyl]amino}(3_吼 基 base)) guanamine group { [(2s)-i_(4_Aminobutyrylmethyl buckwheat)methyl(tetra)cyanophenyl)-2_{[2_(3-fluorophenyl)ethyl]amino}(3_σ ratio Biting base)) chymidine amine 127 200823188 N-{[(2SM|aminoethyl fluorenyl) sent 0 well_2_yl]$yl}(6_(2_cyanophenyl)2 {[2.  (3_Fluorobenzyl)ethyl]amino group))) The methyl phenyl propyl group is a gas-based phenyl) 2 {[2-(3-fluorobenzyl)ethyl]amino} (3^ ratio. fixed base)) the production of o-aminobutanyl is a cyano cyano]-2-{P-(3-murophenyl)ethyl]amino} (3_pyridine) Benthocarbamide-{[(2S) 4 (2- ethoxyethyl)methylanthene __2_yl]methyl)(6_(2_Cyanide) 2 {[2_(3_fluorobenzene) Ethyl]amino]amino} (3_. than bite)) formic acid amine—{[(2S) 4 (3-type propyl aryl)_ι_methyl mother. Well_2_yl]methyl"(6_(2_Cyanogenylphenyl)2 {[2_(3_fluorophenyl)ethyl]amino) fluorenyl))carbamide-{[(2S) 4 (4-月女基丁醯基)]_methyl派喷_2_基]methyl(10)-(2_nitrophenyl)-2-{[2_(3_fluorophenyl)ethyl]amine} 3_t定))) formic acid amine 2-(6-(2-cyanophenyl)_2_ {[2_(3-fluorophenyl)ethyl]aminopyridinyl))-N-(3-pyridylmethyl) Acetamide 15 20 = (4) _M_ diethyl aryl ^ well _2 _ base) methyl] (6_(2_ aryl benzene ^ "U {[2 (3 fluorophenyl) ethyl) amine ° 唆Base)) formic acid amine / [i( )_4_ mercapto piperazine 2 -yl) fluorenyl](6_(2-cyanophenyl)-2-{[2-(3_=yl)ethyl] Amino}(3_吼 基))) _ n_[((2r) nitrogen core domain)] (6_(2_ 乱 phenyl phenyl m(3_fluorophenyl)ethyl]amino)) Amine {[(^^ *)"2- {[2-(3- a ^ } (3- π σ疋))carbonylamino]methyl}nitrogen 0-carboxylic acid methyl ester=-{[2 -(3-fluoromethyl)ethyl]amino}_6_(1_methylhydrazine_4_ylbiazine))[(2oxypyrano-3-yl)methyl]bristamine (2_{[2_(3 gas benzene 128 200823188 yl) ethyl]amino}-6-13⁄4σ sit-4-yl (3-σ ratio 117 base))-N-[(2-乳基^比咯17 Set .  3-yl)mercapto]carbamamine_N-{[(2R)-l-(2-hydroxyethyl)indolyl-2-yl]methyl}(6-(2•cyanobenzene) ))-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl)) decylamine 5- 4-((2R)-2-{[(6-(2) -Querylphenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-oxaridinyl))carbonylamino]indenyl}pyridinyl)-4-oxo Methyl butyrate N-{[(2R)-l-(4-hydroxybutanyl carbaryl-2-yl)methyl}(6-(2-cyanophenyl)-2- {[2- (3-Phenylphenyl)ethyl]amino}(3 -吼σ定基)) an amine N-{[(2R)-l-(2-hydroxyethyl)-pyrrolidin-2-yl曱 }}}(2-{[2-(3-fluoroίο phenyl)ethyl)amino fluorenyl σ ϋ -4--4-yl) (3-1^12 base)) amide 4_(( 2R)-2-{[(2-{[2-(3_鼠phenyl)ethyl]amino}-6-(1-indolyl) is 3-pyridyl )) carbonylamino]methyl}pyridinyl)-4-oxobutanoic acid methyl N-{[(2R)-l-(4-hydroxybutylidene)pyridin-2-yl]fluorenyl} (2-{[2-(3-Fluoro15 phenyl)ethyl]aminomercaptoindazole-4-yl)(3-acridinyl))carbenamide N-[((2R)-1- Ethyl thiol-2-yl) fluorenyl](6-(2-cyanophenyl)-2-{[2-(3-phenylphenyl)ethyl]amino} (3-. ratio 17 Base)) N-{[(2R)-l-(indolylsulfonyl)azin-2-yl]indenyl}(6-(2-cyanophenyl)-2-{[2 -(3-Phenylphenyl)ethyl]amino}(3-indole ratio σ-based)) anthraquinone 20 N-{[(2R)-l-(2-aminoethenyl)nitrogen π- 2-yl]methyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-indole ratio)-capric acid amine N-{[(2R)-l-(3-Aminopropionyl)azin-2-yl]indenyl}(6-(2-cyanophenyl)-2-{[2-(3- Fluorophenyl)ethyl]amino}(3-acridinyl)) decylamine N-{[(2R)-l-(4-aminobutylidene)azepine-2-yl]fluorenyl}(6 -(2-cyanobenzene 129 200823188 yl)-2-{[2-(3-fluorophenyl)ethyl]aminopyridinyl]carbamamine N_ {[(2R) small (2_ thiopyridinium) Base) nitrogen 0 denier 2_yl]methyl}(6_(2-cyanophenyl)_2-{[2_(3-fluorophenyl)ethyl]amino}(3-σ-pyridyl)) Methionine 4-((2R)_2-{[(6_(2_ cyanophenyl)-2-{[2_(3-fluorophenyl)ethyl]amino}}(3"pyridyl)) Amino]methyl}nitrogen. Danyl) Methyl butyrate butyrate N-{[(2R)-1_(4-hydroxybutanyl)azinium-2-yl]indenyl}(Bu(2_cyanophenyl)-2-{[ 2-(3_Phenylphenyl)ethyl]amino}(3′′.. 定))Carbendamine N-(azaperhydroepin-2-ylindenyl)(6-(2) -cyano-phenyl)_2_ {[2-(3-fluorophenyl)ethyl]amino}(3_fluorenyl))carboxamide Ν]Ι>(2_aminoethyl hydrazino) aza All-hydrogen nitrogen- 2 -yl]indenyl}(Bu(2_cyanophenyl)-2-{[2_(3-fluorophenyl)ethyl]amino}(3_tr-pyridyl))carboxamidine Amine N][H3_aminopropionyl)aza-hydrogenazol-2-yl]methyl}(6-(2-cyanophenyl)-2-{[2-(3·fluorophenyl) Ethyl]amino}(3^pyridyl))carbenamide n-{[1-(4-aminobutylidene) aza-hydrogenhamoyl]methyl}(6_(2-cyanyl) -2-{[2-(3-乱本基)ethyl]amino}(3-. 咬 咬))) 甲 Ν Ν [(1-{3-[(di-di-butoxy)) Amino group] propyl 2-oxyindole bite _3_yl) fluorenyl](6-(2-cyanophenyl)-2_{|>(3-fluorophenyl)ethyl]amino group }(3_ "Bistidyl))carbendazim {{1-(3-aminopropyl)-2-oxyindoledin-3-yl]fluorenyl}(6-(2-cyano) Phenyl)_2-{[2_(3- Phenyl)ethyl]amino}(3_π-pyridyl)) amidoxime-[(1-{3-[(t-butoxy)carbonylamino]propyl-2-oxypi) Acridine_3_yl)methyl](2-{[2-(3-fluorophenyl)ethyl]amino}_6"pyrazole_4_yl (3_吼口定基))甲甲胺Ν_{[ Η3-Aminopropyl)_2_oxyπpyrrolidine_3_yl]fluorenyl}(2-{|>(3-gas 130 200823188 phenyl)ethyl]amino}-6-carbazole 4-yl(3-b-pyridyl)) decylamine N-[(l_{3-[(tatabutoxy)carbonylamino]propyl}-2-oxindyrridin-3-yl )methyl](2_{[2-(3-fluorophenyl)ethyl]amino}-6-(1-indolyl oxime-4-yl)(3-acridinyl)) decylamine Ν-{[1-(3-Aminopropyl)-2-oxychamopyridinium 5·3_yl]methyl}(2-{[2_(3-fluorophenyl)ethyl]amino} _6_(1_mercaptooxazol-4-yl)(3-pyridyl))carboxamide (2R)_2-{[(2-{[2_(3-fluorophenyl)ethyl]amino) _ oxazol-4-yl (3 _ mouth ratio dimethyl group)) arylamino] methyl} 吼 咬 bite tartrate third butyl N_{[(2R)-l-(2-hydroxyethyl fluorenyl)比 咯 咯 _2 _2 _2 曱 曱 曱 曱 曱 ί ί ί ί ί ί ί ί ί ί ί ί ί ί ί ί ί ί ί ί ί ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( )_2-{[2_(3-fluorophenyl)ethyl] }}(3- σ-pyridyl))-Ν_[(7-oxahydrohazinyl)-mercapto]carbamamine 2-{[2-(3-fluorophenyl)- Amino]amino}-6"pyrazole (3_pyridyl))-N-[(7-oxaperhydroazin-2-yl)indenyl]nonanyl 15 2-{[2 -(3-Fluorobenzyl)ethyl]amino)-6-(1-mercaptopurin-4-yl) (3-. Ratio σ base))·Ν-[〇oxaperhydrohamoxyl)methyl]decylamine N-[(l_{3-[(t-butoxy)carbonylamino]propyl}_7_oxygen (6-(2.Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-anthracene) )) indoleamine 2〇Ν_{[1-(3_aminopropyl)-7-oxahydrohydrogen nitrogen (oxoazaperhydroepin-2-yl)fluorenyl}(6-(2_cyanophenyl) -2-{[2-(3-fluorophenyl)ethyl]amino}(3_吼)-) guanamine N_{[(2R)_H4·hydroxybutanyl) σ-pyrrolidine-2-yl曱 }}}(2_{[2_(3_就Phenyl)ethyl]amino}-6-carbazole_4_yl (3"pyridyl)carbamamine 131 200823188 N-{[(2R )-l-(2-hydroxyethyl hydrazino)azinium-2-yl]methyl}(2_{[2_(3-fluorophenyl)ethyl]amino K6-[5-(hydroxymethyl)( 2-thienyl)](3_pyridyl))carinamide N-{[(2R)_l-(2,3-dihydroxypropionyl)azinium-2-yl]methyl}(6_(2 _Cyano 5 phenylfluorophenyl)ethyl]amino} (3-σ ratio) carboxylic acid amine (2R)-2- {[(2- {[2-(3-fluorophenyl)) Amino group}_6_,biazole_4•yl(3_acridinyl))carbonylamino]methyl}nitrogen carboxylic acid tert-butyl N_[((2R)azepine-2-yl)anthracene Base](2_{[2_(3_ Fluoryl)ethyl]amino}pyrazol-4-yl(3-pyridyl))carbenamide 10 N-[2-((2R)-2-{[(6-(2-cyanobenzene) -{[2-(3-Fluorophenyl)ethyl]amino}(3-acridinyl))carbonylamino]methyl}nitro}idyl)(1SH_(hydroxyindenyl)-2- Oxyethyl](t-butoxy)decylamine n-{[(2r) small((2s)_2_amino-hydroxypropyl)-nitrol-2-yl]methyl}(6- (2-Cyanophenyl)-2-{[2_(3-hydrophenyl)ethyl]amino}(3 dipyridyl 15 yl))carinamide N-[(lR)-2-(( 2R)-2-{[(6-(2-Cyanophenyl)_2_{[2_(3_fluorophenyl)ethyl]amino}(3-pyridyl))carbonylamino]methyl}nitrogen. Danyl) (1 fluorenyl)-2-oxyethyl](t-butoxy)decylamine N-{[(2R)-l-((2R)-2-amino]_3_ Hydroxypropyl hydrazino) nitrogen oxime 2 yl 2 fluorenyl}(6-(2-cyanophenyl)_2][2-(3-fluorophenyl)ethyl]amino}(3_Dtba-based)) Amine N-[2_((2R)_2_ {[(6-Butylphenyl)-{Μ3·gasphenyl)ethyl]amino}(3·-pyridyl))carbonylamino]indolyl nitrogen. Danylaminopropyl)_2-oxyethyl](t-butoxy)guanamine 132 200823188 N-{[(2R)-l-((2S)-2,5-diaminopenta Niobium) nitrogen. _2_2_yl]methyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-u-indolyl)) formamidine Amine N_{[(2R)_1_(2·-peyridinyl) nitrogen. _2_yl]methyl}(2_[[2_(3·Fluoro)ethyl]amino}-6-吼Salt_4_yl (3_σ ratio))-N-[(( 2R)-l-{2_[(Tertibutoxy)alkylamino]ethenyl}N-oxanyl]methyl](2_{[2-(3-fluorophenyl)ethyl]amine Keb 6_π is more than 'base (3_σ ratio σ base)) N-{[(2R)-l-(2-aminoethyl fluorenyl) hydrazin-2-yl]methyl}(2_{[2_(3 -Fluorophenyl)ethyl]amino}_6_咐^ sit-4-yl (3-indolyl))carzamide (2R)-2-[(6-(2-cyanophenyl)- 2-{[2-(3-fluorophenyl)ethyl]aminopyrimidinyl))alkylamino]-3-carbyl-N-methylpropionamide N-[(6_漠(2 -pyridyl))indenyl](2-{[2-(3-fluorophenyl)ethyl]amino}_6_. than salivyl-4 (3_11 to sigma)) formamide Ν-( {6-[(3-Aminopropyl)amino](2_acridinyl)}methyl)(2_{[2_(3_fluorophenyl)ethyl]amino}}_6-u than saliva_ 4_based (3_π ratio bite)) methotrexate-({6-[(2-aminoethyl)amino](2-σ-pyridyl)}methyl) (2_{[2_(3 _Fluorophenyl)ethyl]aminobi b 6-pyrazol-4-yl(3-pyridyl))carboxamide (2_{[2_(3-fluorophenyl)ethyl]amino}_6^ ratio Azulene (3_ σ-pyridyl))-Ν-({6-[(2-hydroxyethyl)amino)] (2_σ-pyridyl) )"Methyl)carbamamine ^^•2-{[(2_{[2-(3-fluorophenyl)ethyl]amino}_6_pyrazole_4_yl(3_pyridyl))carbonyl Amino]mercapto}N-oxocarboxylic acid methyl ester>H((2R)_l-{3-[(t-butoxy)carbonylamino]propenylpyrrolidinium-2_)methyl]( 5-fluoro-2-{[2-(3-fluorophenyl)ethyl]aminodiphenyl 6-(1-methylπ than saliva 133 200823188 -4-yl)(3-pyridyl))carbenamide N_ {[(2R) small (3-aminopropionyl) mouth is more than bite 2 -yl] methyl) (5 gas - 2_{[2_(3_fluorophenyl)ethyl]amino)b 6_( 1_methyl port than salyl) (3_port ratio - 5 N-[((2R)-l-{4-[(t-butoxy)carbonylamino]butyrylpyrrolidinyl)methyl] (5_Fluoro-2-{[2_(3_fluorophenyl)ethyl]aminobib 6_(1-methylpyrazole _4_yl) (34bn fixed)) formamide N_{[(2R )-l-(4-aminodindinyl)π ratio 咯_2_yl] fluorenyl}(5_fluoro-2_{[2-(3-fluorophenyl)ethyl]aminobib 6_( 1_methylhydrazine base) (3" ratio. 10 base)) formazan foot N-[(2][(t-butoxy)alkylamino]methyl} (3_ acridine Base  Fluorine β2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-methylcarbazole_4_an acridinyl))carbenamide-{[2-(amine (3_u-pyridyl)]hydrazino}(5-fluoro·2_{[2_(3_fluorophenyl) 15 ethyl]aminobi b 6-(1β·methylpyrazol-4-yl (3-pyridyl))carzamide N_[((2R) small {3-[(t-butoxy)carbonylamino]propyl)-oxypyrrolidinyl)methyl](5_n{ [2_(3-fluorophenyl)ethyl]amine-based-methylhydrazin-4-yl)(3-acridinyl))nonylamine N_{[(2R)-1_(3-amino group Propyl)_5_oxyπpyrrolidin-2-yl]fluorenyl}(5-fluoro-2-indole-2][2-(3-fluorophenyl)ethyl]aminomethylpyrazole ice-based) (3_pyridyl)) indoleamine N_{[(2R)-l-(2,3-dihydroxypropionyl)pyrrolidinyl-2-yl]indenyl}(5-fluoro 2 {[2-( 3_Fluorobenzyl)ethyl]aminodibu 6-(1-indolyl hydrazine. sitting on ice base) (3_0 ratio biting base)) decylamine 134 200823188 (2-{[2-(3-fluorophenyl) Ethyl]amino-aminopyridylethyl)carbazole-yl](3^pyridyl)-N-(3"-pyridylmethyl)decylamine (2R)-2- {[(6-(2) -Cyanophenyl)-5-recept {[2_(3_ phenylphenyl)ethyl]amino}(3_吼 基))) arylamino]methyl P ratio 17 each bite Wei acid == Cool 5 咯 ^ base) 曱 base (6_(2_Cyanophenyl chest)-fluorophenyl)ethyl]amino}(3_abridinyl))carbenamide [(2_{[(t-butoxy)carbonylamino]methyl) }(3^pyridinyl)methyl](2_{[2_〇fluorophenyl)ethyl]amino}_6_K2_ylidylethyl)oxazol-4-yl](3-° ratio bite base) ) 甲 胺 amine 10 N (amino sulfhydryl) (3 ° ° bite base)] methyl} (2-{[2-(3-fluorophenyl)ethyl]amino}-6-[1- (2_Pentylethyl) 吼κ-yl](3_t-decyl)) N-[(2-{[(Tertidinoxy)carbonylamino]methyl}(3-pyridylmethyl)](6_ (2-cyanophenyl)-5-fluoro_2_{[2_(3-fluorophenyl)ethyl]amino}(3_pyridyl))carbenamide 15 N-{[2-(amino-methyl) Base) (3_° pyridine group)] methyl}(6_(2-cyanophenyl)_5_fluoro 2 {[2-(3-fluorobenzyl)ethyl]amine group than bite base)) Amine >H((2R)-l-{2-[(Tertidinoxy)carbonylamino]ethinylpyrrolidinyl)indenyl](6-(2-cyanophenyl)_5_ Fluorine_2_ {[2_(3_fluorophenyl)}(3-pyridyl))carboxamide '° Claw 21^1^2-aminoethylidene)pyrrolidin-2-yl]methyl} (6_(孓Cymenephenyl)_5H{〇(3-fluorophenyl)ethyl]amino K3_u-pyridyl-based decanoic acid N [((2R)-l-{3-[(di-butoxy) Base Propionate base ratio 唆j )) methyl](6-(2-cyanophenyl)_5•fluoro_2_{[2_(3_fluorophenyl)ethyl]amino}(3_pyridine Base)) methotrexate 135 200823188 N-{[(2R)_1_(3_aminopropenyl) π-pyridyl] fluorenyl (10)-(nitrophenyl)-5-fluoro-2- {[2_(3-Fluorophenyl)ethyl]amino}(3_π-indenyl))carinamide N-[((2R) small {4-[(t-butoxy)alkylamino]醯 醯 丨 咯 咯 _2 _2 _2 _2 _2 _2 _2 _2 _2 _2 _2 _2 _2 _2 _2 甲基 甲基 . . . . . . . . . . 咯 咯 咯 . 咯 咯 咯 }}(3-pyridyl)) decylamine N-{[(2R)_1_(4-aminobutylidene)pyrrolidine-2-yl]fluorenyl}(b(2_cyanophenyl)_5_敦_2-{[2_(3_Fluorophenyl)ethyl]amino}(3′′pyridinyl))decanoic acid N-[((2R)-l-{3-[(third butoxide) (carbonyl)amino]propyl 5-pyroxypyridin-2-yl)indenyl](6-(2-cyanophenyl)-5-fluoro-2-{[2-(3-fluoro Phenyl)ethyl] 1 fluorenylamino}(3-pyridyl)) decylamine N-{[(2R) small (3-aminopropyl)_5_oxyl port ratio slightly bite_2_yl] Mercaptocyanophenyl)-5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}(3_u-pyridylcarboxamide N-{[(2R)-i_(2 , 3 · di-propyl propyl sulfhydryl) mouth bite each bite_2_yl] methyl (10)-helium 15 benzylidene fluoride-2-{[2_(3-fluorophenyl)ethyl]amino} (3-Acridine))carbendazim N-[2-((2R)-24[(5-fluoro-2-{{2-(3-fluorophenyl)ethyl))amino) 6_(1β A (pyridyl)-based (3-acridinyl)))-ylamino] hydrazinyl] oxime-pyridyl) (is) fluorenyl-2-oxyethyl](t-butoxy) hydrazine Indoleamine 20 N-{[(2R)_1-((2S)_2-Aminopropyl aryl-based oxime. _2_2_yl]methyl}(5_气-2-{[2_(3_气Benzo)ethyl]amino}_6-(1_methylπ than sal-4_yl) (3_. ratio Base)) indoleamine N_[((2R)-l-{(2S)-2,5-bis[(t-butoxy)amino)ylpentanyl}-pyrrolidin-2-yl )methyl](5_fluoro_2_{[2_(3_fluorophenyl)ethyl]amine 136 200823188 kib 6_〇methylcarbazole _4_yl)(3_π-pyridyl))carboxamide 'N-{[(2R)_l-((2S)-2,5'-aminopentenyl)) 甲基 咬]]methylfluoro-2-{[2-(3-fluorophenyl)ethyl Amino}_6-(1-methylpyrazole-4-yl)(3-pyridyl))carhamamine 5 NK(2R)-2][(5H{[>(3-fluorophenyl)) Ethyl]aminodibu 6-(1-methyloxazol-4-yl)(3-acridinyl))carbonylamino]methyloxaridinyl)(lS)-l-(hydroxymethyl>; 2-oxyethyl](t-butoxy)carbamamine N- {[(2R)-1 -((28)-2-amino]-3-hydroxypropyl)pyrrolidine-2- Methyl]methyl 5-(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}_6_(1 _mercaptopyrazole-4-10 base) (3-pyridyl)) Indoleamine 4-((2R)l{[(5-is-2_{[2_(3_fluorophenyl)ethyl]amino}_6_(1_methylcarbazol-4-yl)(3-acridine Base))carbonylamino]mercaptopyridinyl)_4_oxybutyrate oxime-{[(2Κ)-1-(4-hydroxybutylidene)pyrrolidine-2-yl]fluorenyl}( 5_Fluorine 15 -2-{[2_(3_fluorophenyl) Amino group}6 servoylmethylpyrazole I group) (3 比 pyridine group)) decylamine is called (2-{[(Tertidinoxy)) ylamino) sulfhydryl} (3_π ratio Pyridyl))indenyl](5_ gas group 2 {[2-(3-fluorobenzyl)ethyl)amino group 6-(ι_曱基σ比嗤4_yl) (3_ ° 唆 base )) 甲, 酿 〇Ν { { { { { { { { { { { { { { 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲_Bu (1-methylpyrazole I group) (> pyridine group)) decylamine n-[h(5r)-5_{[(5-cyano winter {[2_(3_oxyphenyl)) Ethyl]amine oxib (ι_methylu-pyrazol-4-yl)(3_acridinyl))carbonylamino]methyl-2-pyrrolidinyl)propyl](third butoxy曱醯amine 137 200823188 N-{[(2R)-l-(3-aminopropyl)_5-oxypyrrolidine-2-yl]methyl}(5_气基-2-{[2 -(3-Fluorophenyl)ethyl]amino}_6_(1_methylpyrazole_4_ylidinyl))carbenamide (2R)-2-{. Cyano 2-{{2_(3-fluorophenyl)ethyl]amino} o-methyl to 4 yl) (3-π ratio thiol)) arylamino] methyl}n Diacid triester _ 柯 "叫唆 唆_2_ base 曱 ]]] (5_ cyano_2_{[2_(3_ phenylphenyl) acetamidomethylpyrazole _4_ group) (3 _Pyridinyl)) indoleamine N-[((2R)-1_{4_[(t-butoxy)carbonylamino]butanylpyrrolidinyl)methyl](5-cyano-2_{[2_ (3_Fluorophenyl)ethyl]aminobib (1) methyl-portage saliva-4-yl) (3-ton fluorenyl))carbenamide N-{[(2R)_l-(4-amino group Butyryl)pyrrolidin-2-yl]fluorenyl}(5-cyano-2-{[2-(3-fluorophenyl)ethyl]amino}_6_(1_methylcarbazole_4_ylindole 3_.pyridinyl))caraamine-[(2-{[(t-butoxy)carbonylamino]methyl}(3_σ-pyridylmethyl)] 2-{[2-(3 -fluorophenyl)ethyl]aminopurine 5_methyloxime^methyl.biazole_4_yl)(3-pyridyl))carbenamide N-{[2_(aminomethyl) (3 "Byridinyl"]methyl}(2_{[2_(3_fluorophenyl)ethyl]aminomethyl-6-(1-methylpyrazole-4-yl)(3-pyridylcarboxamidine) Amine N-[((2R)-l-{3-[(t-butoxy)carbonylamino]propyl 5-yloxypyrrole-2)yl]methyl](2][2 -(3-Fluorine Phenyl)ethyl]aminopurine 5-methyl&methylpyrazol-4-yl)(3-pyridyl))carbenamide N-{[(2R)-l-(3-amino Propyl) _5_oxy π-pyridyl 2 yl] methyl oxo-like fluorobenzene phenethyl ethyl keb ^ methyl ketone methyl pyridinium 138 200823188 base) (3-° ratio bite Base)) an amine (2R)-2][(2_{[2_(3-fluorophenyl)ethyl]amino}}5: fluorenyl-6-(1-methyl-4-yl) 3-acridinyl))carbonylamino]methyl}pyrrolidinecarboxylic acid tert-butyl ester 5 N_[((2R) ϋ 嘻 acridine 1 yl) fluorenyl](2-{[2_(3_fluorobenzene) Ethyl]amino]amino}-5-mercapto-6-(1-methylpyrazole-4-yl)(3-u-pyridyl))carbenamide N-[((2R)-l- {4-[(Tertidinoxy)carbonylamino]butanyl)pyrrolidinyl-2-yl)indenyl](2-{[2-(3-fluorophenyl)ethyl]amino}_5-methyl _6_(1_Methylpyrazole-4-yl)(3-pyridyl))carinamide 10 N-{[(2R)-l-(4-aminobutylidene) π ratio slightly bite_2_ Methyl}(2_{[2_(3_fluorophenyl)ethyl]aminopurine 5-methyl-6-(1-indolylpyrazole-4-yl)(3-pyridyl)) Methionine & (2R)-2_{[(5-cyano-2-{[2-(3-fluorophenyl)ethyl]amino)b 6_吼sa_4-yl (3_σ ratio bite base )) arylamino] fluorenyl唆 第三 第三 第三 第三 酉 酉 15 15 15 ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( 15 }_6_pyrazol-4-yl (3-anthraquinone)) indoleamine N-[((2R)-l-{4-[(t-butoxy)carbonylamino]butanylpyrrolidone _2 基 J J ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( ( Amine 2〇{{(211)小(4-aminobutylidene)σpyrrolidin-2-yl]methyl}(5-cyano 2 {[2-(3-fluorophenyl)ethyl]amine Base}_6_σ is more than salivation_4_yl (3_σ ratio). 曱醯amine^5[((()))]]]]吼 疋 疋 _ _ _ _ _ _ _ _ _ _ 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 2008 Indoleamine N-{[(2R)-l-(3-aminopropyl)-5-oxyindole-2-yl]methyl}(5-cyano-2-{[2- (3-Phenylphenyl)ethyl]amino}-6-11 is 0--4-yl (3-11 than bite)) amide 5 N-[(2-{[(T3) Carbonylamino]methyl}(3-acridinyl))methyl](5-cyano-2-{[2-(3-fluorophenyl)ethyl]amino}-6-carbazole 4-yl(3-acridinyl)methaneamine N-{[2-(amine Indenyl)(3^pyridyl)]fluorenyl}(5-cyanofluorophenyl)ethyl]aminopyrazol-4-yl(3-acridinyl))indolide ίο N-[( 2-{[(Tertidinoxy)carbonylamino]indenyl}(3-acridinyl))indenyl](6-(2-carbylphenyl)-2-{[2_(3-gas Phenyl)ethyl]amino}-5-methyl(3-pyridyl))decylamine N-{[2-(aminoindenyl)(3-acridinyl)]indenyl}(6· (2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}-5-methyl(3-acridinyl))decylamine 15 N-(3- ((5R)-5-{[(6-(2-Cyanophenyl)-2-{[2-(3.fluorophenyl)ethyl]amino}}-5-fluorenyl (3-. Pyridyl))carbonylamino]methyl}-2-oxalylpyridinyl)propyl](t-butoxy)carbamamine N- {[(2R) -1 -(3 -amino group) Propyl)-5-milk base ratio 嘻11 -2-2-yl]fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino }-5-mercapto (3-acridinyl)) 20 mercaptoamine 5-chloro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-indenyl hydrazine Oxazol-4-yl)acridine-3-carboxylic acid oxime ester N-[(2-{[(t-butoxy)carbonylamino]indolyl)(3-acridinyl))indenyl](5 -Chloro-2-{[2-(3-fluorophenyl)ethyl]aminomercaptoxazole-4-yl) (3. mouth ratio 140 200823188 pyridine)) formamide n-{[2_( Aminomethyl)(3_σ-pyridyl)]methyl}(5_chloro_2_{[2_(3_-phenylphenyl)ethyl]aminobib 6_(1_mercaptopyrazole) (3_σ Bipyridyl))carbamide [((2R)_l-{3_[(t-butoxy)carbonylamino]propyl b-5-oxypyrrole m)methyl](5·chlorine)!^ 3-dephenyl)ethyl]aminopyrazine methylpyrazol-4-yl)(3-pyridyl))carboxamide N-{[(2R)-l-(3-aminopropyl)_5_ Oxypyrrolidin-2-yl]methyl}(5•chloro-2-{[2-(3-fluorophenyl)ethyl]amino}_6_(1•methylpyrazole_4_yl)( 3_pyridyl))carbamamine (2 magic_2)[( 5-Chloro-2-{[2_(3-fluorophenyl)ethyl]aminobiphenyl 6 servoyl methyl u-pyrazole 4 yl) (3′′-u-based))-based amino group] fluorenyl}σ ratio Oops.魏定魏的三丁酉为n-[((2r)pyrrolidinyl)indolyl](5_气_2][2_(3_fluorophenyl)ethylaminopurine 6-(1-fluorenyl) Pyrazole_4_yl)(3_acridinyl))carbenamide N-[((2R)-l_{4-[(t-butoxy)carbonylamino]butanylpyrrolidinyl)methyl (5-Chloro-2-[2-(3-fluorophenyl)ethyl]aminobib 6-(1_indolyl wow-4-yl)(3-pyridyl))decylamine N-{ [(2R)-1_(4-Aminobutyryl)u ratio slightly biting 2_yl]methyl}(5-chloro-2-{[2-(3-fluorophenyl)ethyl]amine }_6_(1_methylpyrazole_4_yl)(3_pyridinyl))caraamine 疋N-{3-[(tatabutoxy)carbonylamino]propyl} (5-fluoro _2_{[2_(3_Fluorophenyl)^yl]aminomercaptopyrazole_4_yl)(3-pyridyl))carbenamide N_(t-monthly propyl) (5-fluoro- 2-{[2-(3-Fluorophenyl)ethyl]aminobiphenyl 6_(丨_曱yl. 嗤-4-yl)(3-pyridyl))decylamine (2R)-3-[ (5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino]methyl snail 141 200823188 -4-yl)(3-pyridyl))carbonylamino]_2-methyl Methyl propionate _3 sulphur-2-{[2_(3-fluorophenyl)ethyl]aminobib 6_〇_methylcarbazole-4·yl) 〇π 唆 )))) Amino]_2_f-propionic acidoxy)amine {3_[(5-fluoro_2_{[2_(3·fluorophenyl)=:yl} o-methylpyrazole-4-yl)(3-pyridyl}ethylamine 2-amino Example 3_[(5_Fluoro-2 side 3_fluorophenyl)ethyl]amine}methylpyrazole_4_yl)(3_pyridyl))carbonylamino]propyl N-i3m{[ 2-(3-Phenylphenyl)ethyl]aminobib 6_=methyl(tetra)-4-yl)-3-pyridyl)carbonylamino]propyl}ethylamine methyl (tetra) Μ%2 phenyl Ethyl]urephetylmethylpyrazole-4-yl)(3-pyridyl)methaneamine 15 20 amine/mercaptopropyl)(5·fluna-(3;phenyl)ethyl] Amino} Winter (1-methylpyrazolyl) (3_pyridyl))carhamamine is called 3-[(5-fluoro-2_{[2_(3-fluorophenyl)ethyl]amino} _6 Served methyloxazol-4-yl)(3-pyridyl))carbonylamino]22-methylmethylpropanamide (5-fluoro-2-{[2-(3-fluorophenyl)) Amino-based "Bipyl")-N-(pyrazol-3-ylmethyl)carbamamine oxime (5-fluoro-2-{[2-(3-fluorophenyl)ethyl) Amino group}_6 servant methyl.  Acridinyl))-N-dodezol-3-ylindenyl)guanamine = 2 noisy 4_diazo 2_methyl_4 azadin_4_alkenyl) (5 food 2_ coffee - Gas-based) ethyl]aminoindolyl sulfonium) (n-based)) 5-fluoro-2-({[2-(3-fluorophenyl)ethyl]amino}}_6_(1_A Base ton saliva _4_^ pyridyl) 3-methyl carbazinone octene 142 200823188 N-((2S)-3-amino-2-methylpropyl) (5-fluoro-2-{ [2-(3-Fluorophenyl)ethyl]aminomethylpyrazol-4-yl)(3-pyridyl))decylamine N-{(2R)-3-[(5-fluoro-2) -{[2_(3-fluorophenyl)ethyl]amino}_6-(1-indolylpyrazole-4-yl)(3-acridinyl))carbonylamino]-2-mercaptopropyl }}-2-[(Tertiary 5-oxo)- ylamino]acetic acid amine N- {(2R)_3-[(5-Gas-2-{[2-(3-phenylphenyl)ethyl) Amino}-6-(1-methylσ-pyridin-4-yl) (3-11 ratio octyl))-aminoamino]-2-mercaptopropyl}-2-aminoacetic acid amine N -{(2R)-3-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]aminomethyl 1oxazol-4-yl)(3-acridinyl) )carbonylamino]-2-methylpropyl}-2-hydroxyacetamidine (2R)-2-{[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amine }}-6-(1-oxime-based ratio 'oxazol-4-yl)(3-acridinyl))carbonylamino]mercapto}indenocarboxylic acid tert-butyl N-[((2R)azepin-2-yl)indolyl](5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amine 15 yl}-6-(1-fluorenyl) Pyrazol-4-yl)(3-pyridyl))decylamine N-[((2R)_l-{2-[(Tertibutoxy)carbonylamino]ethenyl}N-indole-2- Methyl](5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-methyloxazol-4-yl)(3-acridinyl) )) indoleamine N-{[(2R)-l-(2-aminoethenyl)azup-2-yl]indenyl}(5-fluoro20-2-{|:2-(3- Fluorophenyl)ethyl]amino}-6-(1-indolylcarbazol-4-yl)(3-acridinyl))decylamine N-[((2R)-l-{4-[ (t-butoxy)carbonylamino]butanyl}nitrogen-2-yl)indenyl](5-gas-2-{[2-(3-murophenyl)ethyl]amino}-6 -(1-indolyl 0 to 嗤-4_yl)(3-acridinyl)) decylamine 143 200823188 N_{[(2R)-1_(4-aminobutylidene) nitrogen oxan-2-yl] A (5_Fluoro-2-{[2-(3-fluorophenyl)ethyl]aminobiphenyl 6-(1-methylcarbazole-4-yl)(3-pyridyl X)carhamamine N_{[(2 R)-l-(2-hydroxyethyl) hydrazin-2-yl]methyl"(5_fluoro_2_{[2_(3_fluorophenyl)ethyl]amino) 6_(1-methylpyrazole-4-yl)(3_0-pyridyl))carzamide (2S)-3-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl) Amine base}_6_(1_甲Methylpyrazol-4-yl)(3-acridinyl))carbonylamino]2-methylpropanoate N-((2S)-3-hydroxy-2-methylpropyl) (5_ Fluorine_2_{[2_(3_fluorophenyl)ethyl]amino}-6-(1-methylpyrazole-4-yl)(3-pyridyl))carbenamide N-((2R) -3-hydroxy-2-methylpropyl)(5_fluoro_2_{[2_(3-fluorophenyl)ethyl]amino} -6-oxime-4-yl (3-inchyl) ) carboxylic acid amine (2R)-H(5·fluoro_2_{〇〇fluorophenyl)ethyl]aminobib 6_σ-bisazolyl (3_ σ ratio thiol)) arylamino]-2-methyl propyl Methyl ester (2R)-3-[(6-(2-aminophenyl)-2-{[2-(3-fluorophenyl)ethyl]aminopyridinyl))carbonylamino]-2- Methyl methacrylate N-((2 R)-3-hydroxymethylpropyl)(6-(2-cyanophenyl)_2-{[2_(3•fluorophenyl)ethyl]amino} (3-bite base)) methotrexate team [(2,2_dimethyl (1,3_2. Ethylene group))methyl](5_fluoro_2_{[2_(3_fluorophenyl)ethyl]amino}-6-(1-indolyl-4-yl) (3_吼. Base)) decanoic acid amine (5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}_6-(1_methyl 11 than sal-4)-(3-anthene) Base))_N-|>Hydroxy-2_(ylhydrazino)propyl]decylamine 1^[(2,2-dimethyl(1,3-dioxane-5-yl))methyl ](5·Fluorophenyl)ethyl]amino}-6′′-pyrazol-4-yl (3_ϋbite)) formamide 144 200823188 (5-gas-2- {[2-(3- Phenyl)ethyl]amino}-6-indole than sal-4-yl (3- 0 ratio σ.  Base))-Ν-[3-^έ基-2-(colony. Mercapto)propyl]. Amidoxime Ν·[(2,2-dimercapto(1,3-diosole oxazeto-5))indolyl](6-(2-aphthylphenyl)-2-{[2- (3-fluorophenyl)ethyl]amino}(3·-pyridinyl))carbenamide 5 (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl) Ethyl]amino}(3-acridinyl))-N-[3-hydroxy-2-(hydroxyindenyl)propyl]carbenamide (2R)-2-{[(5-fluoro_2 -{[2-(3-Fluorophenyl)ethyl]aminobiphenyl 6-(1•曱-hydroxypyrazole-4-yl)(3-acridinyl))carbonylamino]indenyl}butyric acid N-((2R)-2-ethyl-3-propylpropyl)(5-gas-2-{[2-(3-(phenylphenyl)ethyl)]] 1-mercaptopyrazole-4-yl)(3-pyridyl))decylamine, (2R)-2-{[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl) Amino}-6-oxazol-4-yl(3-acridinyl))carbonylamino]mercapto} butyl butylate N-((2R)-2-ethyl-3-light propyl (5-Gas-2·{[2-(3-Phenylphenyl)ethyl)amino}-6-pyrazol-4-yl(3-acridinyl)) decylamine 15 (2R)- 2-[(Secondoxy)Weissylamino]-3-[(5-gas-2-{[2-(3-phenylphenyl)ethyl]amino}-6-(1-曱) (oxazol-4-yl)(3-acridinyl))carbonylamino]propionic acid methyl ester (2R)-2-amino-3-[(5-fluoro-2-{[2-(3- Fluorophenyl)ethyl]amino fluorenyl (oxazol-4-yl)(3-acridinyl))carbonylamino]propionate decanoate 20 N-((lR)-l-{[(5-gas-2-{[2-(3-murine benzene) Ethyl]amino}-6-(1-indolylpyrazole-4-yl)(3·-pyridyl))carbonylamino]indenyl}-2-hydroxyethyl) (third Butoxy)carbamamine N-((2R)-2-amino-3-carbylpropyl)(5-Gas-2-{[2-(3-(phenylphenyl)ethyl)]amino} -6-(1-mercaptooxazol-4-yl)(3-pyridyl))decylamine 145 200823188 1^-((1)-1_{[(5-gas_2-{[2- (3-Phenylphenyl)ethyl]amino}_6-ylpyryl-4-yl(3-acridinyl)carbonylamino]]yl}-2-hydroxyethyl) Benzoamine N-((2R)-2-amino-3-carbopropyl)(5-gas_2-{[2-(3-)phenyl)ethyl]5-amino}- 6-pyrazol-4-yl(3-pyridyl))decylamine N-(2,3-dipropylpropyl)(5-gas-2-{[2-(3_ disordered phenyl)) Amino]-6-(1-mercaptopyrazole-4-yl)(3-pyridyl))decylamine 1^-(2,3-dipropylpropyl)(5-gas-2) -{[2-(3-Phenylphenyl)ethyl]amino}_6-pyrazol-4-yl(3-pyridyl))carbenamide ίο (2R)-3_{[2-amino-5 - 默ι_6-(1-曱-based 1^ than ϋ--4-yl) (3-port specific base)] tromethamine-based 2-methylpropionate _N_{[( 2R)-l-(2-hydroxy-2-methylpropenyl)azin-2-yl]fluorenyl}(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amine (oxazol-4-yl)(3-acridinyl))carbenamide 15 (2R)-2 -{[(5-gas_2-{[2-(3-)-phenyl)ethyl ]amino}- 6-0 than ϋ--4-yl(3-acridinyl))carbonylamino]]hydrazino}azanecarboxylic acid tert-butyl ester N-{[(2R)-l-(2 -Hydroxyethyl)nitrogen. -2--2-yl] fluorenyl}(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-n-pyrazol-4-yl (3-acridinyl) Carbenamide 20 N-[((2R)azan-2-yl)indenyl](5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6- Pyrazol-4-yl(3-acridinyl)) decylamine N-{[6-(aminomercapto)(2-acridinyl)]fluorenyl}(2-{[2-(3- Fluorophenyl)ethyl]amino}-6-phenyl(3-acridinyl)) decylamine N_{[6-(aminoindolyl)(2-acridinyl)]fluorenyl}(6 -(2-cyanobenzene 146 200823188 yl)-2·{[2-(3-fluorophenyl)ethyl]amino}(3-typyridyl))carbenamide N-(fe-branthyl) Mercapto)(6_(2-cyanophenyl)_2_{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))decylamine N-(2-aminocarbazinyl) Ethyl)(6-(2-cyanophenyl is 2_{[2-(3-fluorophenyl)ethyl]amino}} (3" than octyl)) carbamide 2-[(6-(2) -Cyanophenyl)_2-{[2-(3-fluorophenyl)ethyl]amino}(3-°-pyridyl))alkylamino]-Ν-methylacetamide and 38) -2 -oxy (3 - ketone)) (6-(2-cyanophenyl)-2-{[2-(3-1phenyl)ethyl]amino} (3-pyridyl) )) guanamine. The present invention provides at least one compound selected from formula V and pharmaceutically acceptable salts thereof. Of chemicals

式V 其中 15 R1係選自氫、視需要經取代之醯基、視需要經取代之 烷基、氰基、_基、疊氮基、視需要經取代之胺基、視需 要經取代之姨*乳基叛基、視需要經取代之胺基纟厌基、叾黃酉蠢 基、亞$黃酿基及硫基； /係選自氫、視需要經取代之芳基、視需要經取 雜芳基、視需要經取代之環減、”要經取代之雜環= 147 20 200823188 基、氰基、視需要經取代之絲、視需要經取代之驢基、 視需要經取代之烷氧基羰基、視需要經取代之胺基、視需 要經取代之胺基羰基、視需要經取代之甲脒基、視需要2 取代之烧氧基、視需要經取代之芳基氧基、視需要經取代 之雜芳基氧基、視需要經取代之雜環烷基氧基、視需要經 取代之烯基、視需要經取代之炔基、磺醯基、亞磺醯基= 硫烧基； Ζ2係選自氫、視需要經取代之甲脒基、羧基、視需要 經取代之烷氧基羰基、視需要經取代之醯基、視需要經取 代之烯基、視需要經取代之烷基、視需要經取代之雜環烷 基、視需要經取代之雜芳基及視需要經取代之胺基羰基； ζ係遠自視需要經取代之烧基及視需要經取代之雜 芳烷基；R3係選自氫及視需要經取代之烷基；及 R6係選自氫、視需要經取代之醯基、視需要經取代之 烷基、氰基、i基、疊氮基、視需要經取代之胺基、視需 要經取代之烷氧基羰基、視需要經取代之胺基羰基、磺醯 基、亞磺醯基及硫烷基。 〃 在式V化合物之特定實施例中，Z1係選自經一、二或 ，個由下列選出之基團取代之苯基：^基、烷基、烷氧基、 氰基及視需要經取代之醯基。在式v化合物之特定實施例 中，Z1係選自3,4-二氟苯基及2_氰基苯基。 在式V化合物之特定實施例中，ζ2係選自曱基胺基羰 基、甲基胺基羰基甲基胺基羰基、乙基胺基羰基、丙基胺 基羰基及異丙基胺基羰基，其中甲基、乙基、丙基及異丙 148 200823188 基基團係視需要經一、二或三個獨立地由下列選出之基團 _ 取代··視需要經取代之甲氧基、視需要經取代之乙氧基、 視需要經取代之苯基及視需要經取代之σ比咬基。在式v化 合物之特定實施例中’ ζ2係選自曱基胺基羰基甲基胺基羰 5 基、2-曱氧基乙-1-基胺基羰基、苯曱基胺基羰基、異丙基 胺基羰基、11比啶基甲基胺基羰基及17比啶-4-基甲基胺基羰 基。 在式V化合物之特定實施例中，Ζ3係選自經一、二或 三個獨立地由下列選出之基團取代之乙基、甲基及丙基： ίο 視需要經取代之芳基及視需要經取代之雜芳基。在式V化 合物之特定實施例中，Ζ3係選自視需要經取代之苯基及視 需要經取代之吡啶基取代之乙基及甲基。在式V化合物之 ’ 特定實施例中，Ζ3係選自2-(3-氟苯基）乙基、2-(3-甲基苯基) 乙基、2十比咬-2-基）乙基、2-(3-甲基苯基）乙基及α比唆_2_ 15 基曱基。 在式V化合物之特定實施例中，Ri係選自氫及視需要 經取代之低碳烧基。在式V化合物之特定實施例中，R1係 選自氳極低竣烧基。在式V化合物之特定實施例中，ri係 選自氣及甲基。在式V化合物之特定實施例中，r1為氫。 20 在式V化合物之特定實施例中，R3係選自氫及視需要 經取代之低碳烷基。在式V化合物之特定實施例中，汉3係 選自氫及低碳烧基。在式V化合物之特定實施例中，r3係 選自胤及甲基。在式V化合物之特定實施例中，R3及氫。 在式V化合物之特定實施例中，R6係選自氫、氰基、 149 200823188 鹵基、疊氮基、視需要經取代之胺基羰基及視需要經取代 之烷基。在式V化合物之特定實_施例中，R6係選自氳、氰 基、氣、溴、氟、疊氮基、視需要經取代之烷基胺基羰基 及視需要經取代之甲基。在式V化合物之特定實施例中， R6係選自氳、氰基、氯、溴、疊氮基、吼咬各基曱基胺基 叛基、胺基曱基及羥基甲基。在式V化合物之特定實施例 中，R6為氳。 10 15 在特定實施例中，式V化合物係選自 (H2-氰基苯基）-4-{[2_(3-氟苯基）乙基]胺基}(3_ u比咬 基))-队(3_吼啶基曱基）曱醯胺； 2-[(6-(2-氰基苯基）-4- {[2-(3-氟苯基）乙基]胺基丨(3·吡唆 基))#厌基胺基]-N-甲基乙醢胺及 [={[2-(3_氟苯基）乙基]胺基}-6_(2_{亞胺基比啶基甲』 胺基]甲基}苯基)(3_π比啶基)]善(3_吼啶基曱基）甲醯胺。 本發明係提供至少一種選自式¥1化合物盆 可接受鹽類之化學品 /、商条一Wherein 15 R1 is selected from the group consisting of hydrogen, optionally substituted thiol, optionally substituted alkyl, cyano, yl, azide, optionally substituted amine, optionally substituted oxime *milk-based rebel, as needed, substituted amino-based ruthenium, ruthenium, ruthenium, ruthenium, and thiol; / selected from hydrogen, optionally substituted aryl, as needed Heteroaryl, optionally substituted ring reduction, "heterocyclic ring to be substituted = 147 20 200823188 base, cyano group, optionally substituted silk, optionally substituted sulfhydryl group, optionally substituted alkoxylate Alkylcarbonyl, optionally substituted amino group, optionally substituted aminocarbonyl group, optionally substituted formazan group, optionally substituted alkoxy group, optionally substituted aryloxy group, optionally as needed Substituted heteroaryloxy, optionally substituted heterocycloalkyloxy, optionally substituted alkenyl, optionally substituted alkynyl, sulfonyl, sulfinyl = thiol; Ζ 2 is selected from the group consisting of hydrogen, optionally substituted formazan, carboxyl, optionally substituted alkoxycarbonyl, optionally taken And the substituted alkenyl group, optionally substituted alkyl group, optionally substituted heterocycloalkyl group, optionally substituted heteroaryl group and optionally substituted aminocarbonyl group; Far from self-requiring a substituted alkyl group and optionally substituted heteroarylalkyl group; R3 is selected from hydrogen and optionally substituted alkyl; and R6 is selected from hydrogen, optionally substituted thiol, An alkyl group, a cyano group, an i group, an azide group, an optionally substituted amino group, an optionally substituted alkoxycarbonyl group, an optionally substituted aminocarbonyl group, a sulfonyl group, or a substituted group, if necessary. Sulfoalkyl and sulfanyl. In a particular embodiment of the compound of formula V, Z1 is selected from phenyl, alkyl, alkoxy substituted by one, two or one selected from the group selected below. , cyano and optionally substituted fluorenyl. In a particular embodiment of the compound of formula v, Z 1 is selected from the group consisting of 3,4-difluorophenyl and 2-cyanophenyl. Specific embodiments of the compound of formula V Medium, ζ 2 is selected from the group consisting of a mercaptoaminocarbonyl group, a methylaminocarbonylmethylaminocarbonyl group, an ethylaminocarbonyl group, a propylaminocarbonyl group, and a different A propylaminocarbonyl group in which a methyl group, an ethyl group, a propyl group and an isopropyl group 148 200823188 group are optionally substituted by one, two or three groups selected from the following: a methoxy group, an optionally substituted ethoxy group, an optionally substituted phenyl group, and optionally a substituted sigma ratio. In a specific embodiment of the compound of formula v, 'ζ2 is selected from a mercaptoaminocarbonyl group. Methylaminocarbonyl 5 group, 2-decyloxyethyl-1-ylaminocarbonyl, phenylhydrinylcarbonyl, isopropylaminocarbonyl, 11-pyridylmethylaminocarbonyl and 17-pyridine- 4-Methylaminocarbonylcarbonyl. In a particular embodiment of the compound of Formula V, the oxime 3 is selected from the group consisting of one, two or three ethyl, methyl and propyl groups independently substituted with the groups selected below: ίο The substituted aryl group and the optionally substituted heteroaryl group as needed. In a particular embodiment of the compound of formula V, hydrazone 3 is selected from the group consisting of optionally substituted phenyl and optionally substituted pyridyl substituted ethyl and methyl groups. In a particular embodiment of the compound of formula V, the oxime 3 is selected from the group consisting of 2-(3-fluorophenyl)ethyl, 2-(3-methylphenyl)ethyl, 2:10-but-2-yl) Base, 2-(3-methylphenyl)ethyl and α 唆_2_ 15 fluorenyl. In a particular embodiment of the compound of formula V, Ri is selected from the group consisting of hydrogen and optionally substituted low carbon alkyl groups. In a particular embodiment of the compound of formula V, R1 is selected from the group consisting of ruthenium ruthenium. In a particular embodiment of the compound of formula V, ri is selected from the group consisting of gas and methyl. In a particular embodiment of the compound of formula V, r1 is hydrogen. In a particular embodiment of the compound of formula V, R3 is selected from the group consisting of hydrogen and optionally substituted lower alkyl. In a particular embodiment of the compound of formula V, the Han 3 is selected from the group consisting of hydrogen and a low carbon alkyl group. In a particular embodiment of the compound of formula V, r3 is selected from the group consisting of hydrazine and methyl. In a particular embodiment of the compound of formula V, R3 and hydrogen. In a particular embodiment of the compound of Formula V, R6 is selected from the group consisting of hydrogen, cyano, 149 200823188 halo, azido, optionally substituted aminocarbonyl, and optionally substituted alkyl. In a particular embodiment of the compound of formula V, R6 is selected from the group consisting of hydrazine, cyano, gas, bromine, fluorine, azide, optionally substituted alkylaminocarbonyl and optionally substituted methyl. In a particular embodiment of the compound of formula V, R6 is selected from the group consisting of hydrazine, cyano, chloro, bromo, azide, thiol thiol, thiol and hydroxymethyl. In a particular embodiment of the compound of formula V, R6 is deuterium. In a particular embodiment, the compound of formula V is selected from the group consisting of (H2-cyanophenyl)-4-{[2-(3-fluorophenyl)ethyl]amino} (3_u to butyl))- a group of (3-(acridinyl) decylamine; 2-[(6-(2-cyanophenyl)-4-{[2-(3-fluorophenyl)ethyl]aminopurine (3 ·pyridinyl))# anoylamino]-N-methylacetamide and [={[2-(3-fluorophenyl)ethyl]amino}-6_(2_{iminopyridinium) Alkyl]amino]methyl}phenyl)(3_π-pyridyl)]good (3_acridinyl)carbamamine. The present invention provides at least one chemical selected from the group consisting of a compound of the formula:

式VI 其中 20 R及R4係獨立地選自氫、氰基、鹵基、羥基、疊氮 150 200823188 基、硝基、㈣縣、亞㈣基、硫 烧氧基、視需要經取代頓氧美 取代之 基氧基、視需暴妳Μ *基視而要^取代之胺基幾 、工代之芳基氧基、視需要經取代之雜芳 基氧基、視需要經取代之雜’方 =氧基祕_、·要經取代之烧基、視需要經取代之 二二見需躲取代之縣、視需要經取代之芳基氧基、視 萬要經^代之綠、視需紐取代之雜綠、視需要經取 代之雜環絲、視需要經取狀胺基、視需要經取代之酿 10 15 基視為要[取代之胺基幾基及視需要經取代之 carbaminodoyl ； Z係送自視需要經取代之環烧基及視需要經取代之 雜壞烧基； Z2係選自氫、視需要經取代之曱肺基、羧基、視需要 經取代之烷氧基羰基、視需要經取代之醯基、視需要經取 代之烯基、視需要經取代之烷基、視需要經取代之雜環烷 基、視需要經取代之雜芳基及視需要經取代之胺基羰基； z係選自齒基及視需要經取代之烧基；及 R3係選自氫及視需要經取代之烷基。 在式VI化合物之特定實施例中，Z2係選自羧基、視需 要經取代之烷氧基羰基、視需要經取代之醯基、視需要經 取代之烯基及視需要經取代之烷基。· 在式VI化合物之特定實施例中，Z2係選自羧基、視需 要經取代之哌啶基羰基、視需要經取代之吡啶基羰基、視 需要經取代之低碳烷基、視需要經取代之低碳烯基及低碳 151 20 200823188 烷氧基羰基。 在式VI化合物之_特定實施例中，z2係選自（2-(N-乙醯 基胺基甲基)娘啶-1-基)羰基；(2-胺基甲基哌啶-1-基)羰基； 1-羥基-2-胺基-乙基；2-((甲基石黃醯胺基）曱基)哌啶-1-基羰 5 基；2-(甲基胺基羰基）乙烯基；2_(吼啶_3_基曱基)-2H-三唑 -5-基；胺基曱基；羧基；曱氧基羰基；吼啶-2-基羰基； 吼唆-3-基幾基；及σ比ϋ定_4_基幾基。 在式VI化合物之特定實施例中，R3係選自氫及視需 要經取代之低碳烷基。 10 在式VI化合物之特定實施例中，R3係選自氳及低碳 烧基。 在式VI化合物之特定實施例中，R3係選自氫及曱基。 在式VI化合物之特定實施例中，R3為氫。 在式VI化合物之特定實施例中，Z2為-C(0)NR2R5,其 15 中R2係選自視需要經取代之烷基及視需要經取代之環烷 基；而R5係選自氫及視需要經取代之烧基。 在式VI化合物之特定實施例中，R4係選自氫、氰基、 鹵基、疊氮基、視需要經取代之胺基羰基及視需要經取代 之烧基。 20 在式VI化合物之特定實施例中，R4係選自氳、氰基、 氯、溴、氟、疊氮基、視需要經取代之烷基胺基羰基及視 需要經取代之甲基。 在式VI化合物之特定實施例中，R4係選自氫、氰基、 氯、漠、疊氣基、σ比咬-3-基曱基胺基数基、胺基曱基及 152 200823188 經基甲基。 -在^νι化合物之特定實義巾，r4為氫。 在式VI化合物’定實關巾，r5係選自氳及低碳燒 基。 5 在式VI化合物之特定實施财，r5係選自氫及甲基。 在式VH匕合物之特定實施例中，R5為氳。 在式VI化&amp;物之4寸疋貫施例中，R2係選自視需要經取 代之甲基、視需要經取代之乙基、視需要經取代之丙基、 視需要經取代之丁基、視需要經取代之戊基、視需要經取 1〇 «之己基、視〶要經取代之環丙基、視需要經取代之環戊 基及視需要經取代之環己基，其中各視需要經取代之基團 •需要經―、二或三個由下列選出之基團取代：視需要 經取代之芳基、視需要經取代之雜芳基、視需要經取代之 雑％蜿基、視需要經取代之環烷基、視需要經取代之胺基 15 羰基、視需要經取代之胺基、羥基、羧基、視需要經取代 之烷氧基羰基及視需要經取代之烷氧基。 在式VI化合物之特定實施例中，R2係選自曱基及乙 基’其中甲基及乙基基圑係視需要經經一或二個由下列選 出之基團取代：視需要經取代之芳基、視需要經取代之雜 20 芳基、視需要經取代之雜環烷基、視需要經取代之環烷 基、視需要經取代之胺基羰基、視需要經取代之胺基、羥 基、羧基、視需要經取代之烷氧基羰基及視需要經取代之 烷氧基。 在式VI化合物之特定實施例中，R2係選自（1-(2-胺基 153 200823188 乙基比唑-3_基）甲基；（1-(甲基磺醯基)哌啶各基）曱 基；（1-乙醯基哌啶-3-基）甲基；（1-乙醢基吡咯啶-2-基）甲 基；(1H-咪唑_2_基）曱基；(1Hj比唑-3-基）曱基；(1-曱基-1H-吡唑-3-基）曱基；（1-甲基_1H_吡唑_5_基）曱基；（2-(胺基羰 5 基）乙基胺基）幾基甲基；（2-(胺基甲基)。比咬-3-基）甲基； (2-(羧基）乙基胺基)羰基甲基；（2-(二甲基胺基）乙基胺基） 羰基甲基；（2-(羥基）乙基胺基）羰基甲基；（2-(甲基胺基） 乙基胺基）羰基曱基；（2-(N-甲基-N-(第三丁氧基羰基)-胺 基）乙基胺基)羰基甲基；（2-氧基哌啶-3-基）曱基；（3-(二曱 10 基胺基）丙基胺基）羰基甲基；（3-(羥基）乙基胺基）羰基曱 - 基；（3_(第三丁氧基羰基胺基）丙基胺基)羰基甲基；（4-(胺 .基甲基)咐啶-2-基）曱基；（5_(胺基甲基户比啶_2_基）曱基； (6_((1，3_二氧基異吲哚—2-基）曱基)吼啶—2-基）甲基；（6-(2_ 胺基乙基胺基)吼啶-2-基）甲基；（6-(3-胺基丙基胺基)吼啶 15 基）曱基；（6&lt;胺基甲基)吡啶-2-基）甲基；（6-(羥基曱基） 吡啶-2-基）曱基；（6_溴咐啶-2-基）甲基；（曱基磺醯胺基） 魏基甲基；（吼啶-2-基）乙基胺基；（第三丁氧基羰基 胺基）乙基)-1Η-吼唑冬基甲基；1-(2_(第三丁氧基羰基胺基) 乙基)·1Η-口比唾_5_基甲基；1_(胺基羰基)_2_(胺基)_乙小基； 20 Η胺基幾基&gt;3_(胺基)丙基；Η胺基幾基)_4_(胺基)-丁基； 1-(胺基羰基)-4-(苯甲基氧基羰基胺基戊基；〗_(胺基羰 基)_5_(胺基)戊基；1-(胺基羰基）乙基；L(叛基)_2_(胺 基)-乙-1-基；1-(二甲基胺基羰基)_2_(胺基卜乙-丨—基；丨_(羥 基)-2-(胺基&amp;基甲基胺基）乙_ι_基；丨_(經基)_2_(乙氧基幾 154 200823188 基甲基胺基）乙-1-基；1-(羥基)-2-(吼咬-2-基甲基胺基）乙 -1-基’ 1-(甲乳基&gt;厌基)-2-(胺基)-乙-1-基；ι_(·曱氧基罗炭 基)-2-(第三丁氧基羰基胺基)_乙-i-基；1β(甲氧基羰基）乙 -1-基’ 1_(曱基月女基爹厌基)-2-(胺基)_乙-1-基(2 〇cc) ; 1-(曱 5 基胺基幾基）乙-1-基；1-胺基叛基-2-經基-乙-1-基；1-甲氧 基幾基-2_經基-乙-1_基；2-(2-胺基乙氧基）乙基；2-(2-胺基 乙基)-吼啶-6-基曱基；2-(2-胺基乙基胺基）乙基；2-(3-氟 本基）乙基；2-(3 -甲氧基裁基）乙基；2-(6-(胺基甲基)π比咬 -2-基）乙基；2-(乙醯基胺基）乙基；2-(胺基）乙基；2-(胺基 1〇 羰基&gt;2-(乙醯基胺基)-乙-1-基；2-(胺基羰基)_2-(胺基)-乙 • 基；2-(胺基幾基）乙基；2-(胺基曱基)吼咬_5_基甲基； „ 2-(叛基)-2-(胺基)-乙-1-基；2-(二甲基胺基）乙基；2-(二甲 基胺基羰基)-2-(胺基)-乙-1-基；2-(乙氧基羰基）乙基；2-(曱 氧基搂基)-2-(乙酿基胺基)-乙-1-基；2-(曱氧基幾基)-2-(胺 15 基)·乙小基；2-(甲氧基幾基胺基）乙基；2·(曱基胺基）乙基； 2-(曱基胺基幾基)-2-(乙醯基胺基)-乙-1-基；2-(曱基胺基幾 基)-2-(胺基)-乙-1-基；2-(曱基續醯胺基）乙基；2_(曱氧基 幾基)-2-(胺基)-乙-1-基；2-(N-(第三丁氧基幾基)_叛基（甲 基)_胺基）乙基；2-(旅_小基）乙基；2十比啡-2-基）乙基； 20 2十比咬-2-基）乙基；2-(σΛσ定-3-基）乙基；2-(第三丁氧基幾 基胺基甲基)吼啶-3-基曱基；2-(第三丁氧基羰基胺基曱基) 吡啶-6-基曱基；2-(三氟甲基)-吡啶_6_基曱基；2-胺基咣咬 -3-基曱基；2-胺基°比咬-5-基曱基；2-氯°比唆-5-基曱基； 2-氰基咕咬-5-基曱基；2-羥基-3-胺基-丙-1-基；2-羥基乙 155 200823188 基；2-甲氧基乙-1-基；2·曱氧基吼啶-3-基甲基；2-甲氧基 吡啶-5·基Τ基；2-曱基吡啶-3-基曱基；2-甲基吡啶-5-基 曱基；2-甲基吡啶_6_基曱基；3_(2_胺基乙基)環己基）曱基； 3-(4-曱基哌畊-1-基）丙基；3-(胺基)-3-(甲基胺基羰基）丙—μ 5 基；3_(胺基羰基）丙基；3-(胺基甲基)苯甲基；3-(胺基甲 基)吼啶-2-基甲基；3-(曱氧基羰基）丙基；3-(曱基胺基羰 基）丙基；3-(三氟甲基)-π比啶-2-基甲基；3,4-二氟苯曱基； 3-胺基甲基吼啶-4-基甲基；3-胺基丙基；3-胺甲醯基環戊 基；3-羧基丙基；3-羥基丙基；3-甲氧基丙基；4·(胺基曱 ίο 基)-17比咬-2-基甲基；4-(Ν，Ν-二甲基胺基)吼咬-3-基甲基； • 4-(第三丁氧基裁基胺基)-嗎琳基曱基；4-胺基丁基；4-胺 基甲基吼啶-3-基曱基；4-氰基苯甲基；4-氟苯甲基；4-曱 基胺基吡啶-3-基曱基；4-曱基苯甲基；4-嗎啉基吡啶_3_ 基曱基；4-哌π井基吼啶-3-基曱基；5-((雙（二甲基胺基）甲 15 基胺基）曱基)σ比咬-3-基曱基；5-(胺基曱基)吼tr定_2_基甲基； 5-(胺基甲基)吡啶-3-基甲基；5-(羥基甲基)吡啶-3-基曱基； 5- (弟二丁氧基幾基胺基曱基)-π比咬_2_基甲基；5-(三氟曱 基定-2-基曱基；5-胺基戊基；5-胺基°比咬-2-基甲基； 6- ((雙（二曱基胺基）伸曱基胺基）甲基）吼啶_2_基）曱基； 20 6_(4_乙醯基哌畊]_基)°比啶-3-基曱基）；6_(胺基甲基)π比啶 -2-基）曱基，6-胺基己基；胺基幾基曱基；苯甲基；環丙 基曱基’一曱基胺基幾基甲基；異丙基；異4唾-5-基甲基； 曱氧基Ik基甲基；曱基；曱基胺基叛基曱基；υ号哇_2_基甲 基；旅17定-4·基甲基；丙_2_婦_1_基；π比〇井_2_基甲基；σ比唆 156 200823188 -2-基甲基；吼啶-2-基甲基-N-氧化物；吡啶-3-基甲基；吡 -鳴&gt;3-基甲基-N-氧化物；吡啶基甲基；噻吩_2_基甲基； 及。塞吩-3-基甲基。 在式VI化合物之特定實施例中，z3係選自鹵基及視需 要經取代之低碳烷基。 10 15 20 在式VI化合物之特定實施例中，z3係選自卣基、視需 要經取代之甲基、視需要經取代之乙基及視需要經取代之 丙基，其中甲基、乙基及丙基基團係視需要經經一或二個 由下列選出之基團取代羥基、視需要經取代之芳基、 J經取代之雜芳基、視需要經取代之雜環烷基、‘： 代之環烷基及視需要經取代之芳基氧基。 、、'二 在式vi化合物之特定實施例中，Z3係選自2-(3_曱美# =)^乙基、（四氳呋喃2_基）甲基、丨_羥基環己基甲基、本 —氧戊環-2-基）乙基、2_(IH-味唆-4-基）乙基、2_(1 ，3- ，+基)乙基、2-(1_甲基旅唆冰基)乙基、2_(2,3_基； 土)乙基、2_(2,5_二氟苯基）乙基、2_(2,6_二氣苯基）乙二本 /氯苯基）乙基、2_(2_氰基苯基）乙基、2_(2-氣'、 二2-(2-經基苯基)乙基、2♦曱氧基苯基)乙基、二乙 二求基)乙基、2-(2-氧基坐唆+基)乙基、2_⑺氣二 -基）乙基、2-(2-氧基吡咯啶小基）乙基 :氏口疋 笨基)乙基、2-(3,4·二氟苯基)乙基曱旬 2飯甲基，基)乙基二^ 2)乙基、2-(3-胺甲醯基苯基)乙基、2普羧基笨：唑 土 _(3-鼠基苯基）乙基、2_(3_氟苯基&gt;2_(經基)_乙基、 157 200823188 乙基、2分氟终2_基)乙基、冰甲氧基 基）乙基、2-(3_甲氧基苯基）乙基、2_(3_甲基苯基）乙基^ 胺基苯基）乙基、 5 10 15 20 經基苯基）乙基、2-(苯并剛3]間二氧雜戊婦_5_基）乙義、 Μ咬喃2·基）乙基、2_⑽基)_2_(苯基）乙基、2_(苯基）乙^、 2十比唆-2-基）乙基、2_(吼唆_3_基）乙基、2十塞吩 己小烯紅基、2_環己基乙基、2_嗎储乙土基、 本乳土乙基、2-本基丙小基、3_d米哇〈女丙小灵、 =基丙基、苯甲基、氯、異戊基、内基、龄2_基甲 σ比ϋ定基甲基及嗟吩-3-基甲基。 在式W化合物之特定實施例中，23係選自吵氣苯 基）乙基及2-(吡啶-2-基）乙基。 在式VI化合物之特定實施例中， 雜環烧基，其中各基團係視需要婉 ^自衣坑基及 基團取代:氮基、，基、；:要;4二個由™^ 燒基、視需要經取代之稀/視！視需要經取代之 基、視需要經取代之垸經取代之烧氧基、叛 视需要經取代之胺基3 :Λί、視需要經取代之醯基、 銥取代之土厌土視而要經取代之胺基、視需要 ==:炫基、視需要經取代之雜芳基、視需要經取 代之曱脒基及視f要經取代之續酸基。 之特定實施例中，zl係選自環烧基及 係視需要經-或二個由下列選出之 低，ΓΑ齒基、經基、甲酿基、視需要經取代之 ^基、視需要經取代之低碳稀基、視需要經取代之低 158 200823188 碳烷氧基、羧基、視需要經取代之低碳烷氧基羰基、視需 要經取代之醯基、視需要經取代之胺基羰基、視_需要經取 代之雜環烷基、視需要經取代之雜芳基、視需要經取代之 曱脒基及視需要經取代之磺醯基。 5 在式VI化合物之特定實施例中，Z1係選自1-(2Η)-(曱 氧基羰基)-3,4-二氫吼啶-4-基；1-(2Η)-(曱氧基羰基)-5,6-二鼠吼咬-心基， 1-(2Η)-(曱氧基曱基)-5,6-二氫吼啶4-基； 1-(2Η)-(第三丁氧基羰基)-5,6-二氳吼啶-4-基； ίο 1 -(2 Η)-5,6-二鼠 0比 °定-4-基， • 1-(乙醯基)-4,5-二氫咪唑-2-基； - 1_(二甲基胺甲醯基)-1，2,3,6-四氫。比啶-4-基； 1- （曱氧基甲基)-4、5-二氫咪唑-2-基； 1 -氣基-4,5-二氮-111_味σ坐-2-基， 15 1 -甲基-1，2,3，6_四鼠11比。定-4-基， 2- (乙醯基胺基曱基)吡咯啶-1_基； 2-(¾基曱基)嗎^林基； 2-(羥基甲基)吡咯啶-1-基； 2-(曱氧基甲基)吼咯啶-1-基；2H-u比咯-1(5H)-基； 20 2-羥基嗎啉基；2-甲基-4-(第三丁氧基羰基)-哌畊-1-基；2_ 氧基-5-輕基-娘σ定基； 2-氧基娘畊基； 2-氧基旅咬基； 2-氧基吼咯咬基； 159 200823188 3-(3,3-二曱基脈基)17比嘻咬-1-基， . 3-(胺基甲基)-1[7比咯17定-1_基， 3-(羧基曱基)-吼咯啶基； 3-(二甲基胺基基， 5 3-(二曱基胺基曱基)/比咯啶-1-基； 3-(羥基曱基)吡咯啶-1-基； 3-(甲氧基碳基胺基)比咯σ定基； 3-(甲基磺醯基)吼咯啶-1-基； 3-(Ν-乙醯基-Ν-甲基)-胺基曱基)-吼咯啶小基； ίο 3-(^比ϋ定-4-基）ϋ比鳴^ ^定-1 -基， • 3-(第三丁氧基羰基胺基)-吼咯啶基； 、 3-(三氟曱基)吡咯啶-1-基； 3,3-二氟吡咯啶基； 3-乙醯基胺基吡咯啶基； 15 3 -胺基^比咯^定-1 -基， 3 -氣ϋ比嘻ϋ定-1 -基， 3-羥基曱基吡咯啶-1-基； 3-羥基吡咯啶小基； 3- 曱氧基曱基吡咯啶-1-基； 20 3-曱基胺基-吡咯啶基； 3 -乳基娘1:1井-1 -基， 4- (乙醯基)-哌畊-1-基； 4-(胺基甲基)旅咬-1-基， 4-(乙氧基叛基)-派17井-1-基； 160 200823188 4-(乙氧基羰基)-哌啶基； 4-(甲基磺醯基)環己-1-烯基； 4-(N，N-二甲基胺基羰基)-哌畊-1-基； 5 4-(第三丁氧基羰基胺基)-哌啶-1-基； 4-(第三丁氧基幾基胺基甲基)_σ底咬-1-基； 4.5- 二氫唾-咪嗤-2-基； 4.5- 二氫畤唑-2-基； 4-羥基-4-苯基哌啶-1-基； ίο 4-經基乙基-派淀-基； ' 4-經基甲基-派淀-基； 、 4-經基派唆基； 4-甲基胺基羰基-哌啶基； 4-甲基11井-1-基， 15 4-曱基哌啶基； 4-氧基環己-1-烯基； 5.6- 二氫吡啶-1(2Η)-基； 氮°旦基； 環己-1-烯基； 20 環己基； 壞戍-1 -細基， 環戊基； 嗎淋基； 派ϋ井基； 161 200823188 旅17定基； 。比咯咬基；及 σ塞嗎淋基。 5 10 15 20 在式VI化合物之特定實施例中，R1係選自氫及視需 要經取代之低碳烷基· 在式VI化合物之特定實施例中，Ri係選自氫及低碳 烷基。 在式VI化合物之特定實施例中，R1係選自氳及曱基。 在式VI化合物之特定實施例中，Rl為氣。 在特定實施例中，式VI化合物係選自 (2-{[2-(3-氣苯基）乙基]胺基}如底啶基〇比啶基 吡啶基甲基）甲醯胺 N-⑽S)小(6-{[2-(3_氟苯基）乙基]胺基}_5供(3“比咬基 甲基)胺曱酿基](2-吼*基)户比,各咬_3_基] (6翁玲基鱗蝴嫁(3-氟苯!胺基}(3. 吼啶基))-Ν·«(胺甲醯基曱基）甲醯胺 2-[(6-«3R)·3-經基料咬基从{[2_(3_氟苯基）乙基]胺 基}(3-吼咬基))幾基胺基]·N_甲基乙_ (6_(阅-3_經美 一甲基曱醯胺 6-吼嘻口定 N-(胺甲酿基甲基)(2·{[2_(3_氟苯基）乙基]胺基 基（3_吡啶基)）甲醯胺 土 •氟苯基）乙基]胺 (6-[(3R)-3-(羥基甲基）吼咯啶基]_2_{[2_(3 基}(3-吡啶基))-Ν-(3-吡啶基甲基）甲醯胺 162 200823188 (6-{(3S)-3-[(甲基胺基）曱基]吼咯啶基}-2-{[2-(3-氟苯基） 乙基]胺基}(3_j比啶基·))-Ν-(3-吼啶基甲基）曱蘼胺_ N-{[(3R)-l-(6-{[&gt;(3-氟苯基）乙基]胺基卜5-[Ν-(3-吼啶基 甲基）胺甲醯基](2-吡啶基))吡咯啶-3-基]曱基}-Ν-甲基乙 5 醯胺 (6-{(3S)-3-[(二甲基胺基）曱基]吼咯啶基卜2-{[2-(3-氟苯基) 乙基]胺基}(3-吡啶基))-N-(3-吡啶基曱基）甲醯胺 (2- {[2-(3-氣苯基）乙基]胺基}-6-(2-乳基派σ定基）(3-吼咬 基))-N-(3-吼啶基甲基）甲醯胺 ίο (6-[(3S)-3-(胺基曱基)吼咯啶基]-2-{[2-(3-氟苯基）乙基]胺 • 基}(3-吡啶基))-N-(3-吡啶基甲基）曱醯胺 - N-[(6-胺基（3-吼啶基））甲基](2- {[2-(3-氟苯基）乙基]胺 基} -6-吡咯啶基(3-吼啶基)）曱醯胺 N-(2-胺曱醯基乙基）(2-{[2-(3-氟苯基）乙基]胺基}-6-吼咯 15 啶基(3-吡啶基)）甲醯胺 (6-((3R)-3-羥基吼咯啶基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吡啶基))-Ν-(3 -吡啶基曱基）曱醯胺 (2 - {[2-(3 -氣苯基）乙基]胺基} - 6-(2 -乳基σ比咯σ定基)(3-^比口定 基))-N-(3-吼啶基甲基）甲醯胺 2〇 (2-{[2-(3-氣本基）乙基]胺基}-6- ϋ比咯σ定基（3- ϋ比口定 基))-Ν-(3^比啶基甲基）甲醯胺 (6-((3R)-3-羥基吼咯啶基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吡啶))-N-(2-胺曱醯基乙基）甲醯胺 (6-((3S)-3-羥基吼咯啶基)-2-{[2-(3-氟苯基）乙基]胺基}(3- 163 200823188 吼啶基))-Ν-(3-吼啶基甲基）甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-[4-(羥基甲基）哌啶基](3-吼啶基))-Ν-(3-吡啶基甲基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(5-羥基-2-氧基哌啶基)(3-5 吡啶基))-N-(3-吡啶基甲基）甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基卜6-(3-氧基哌畊基）(3-吼啶 基))-N-(3-吼啶基甲基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(4-曱基哌畊基）(3-吼啶 基))-N-(3-吡啶基甲基）曱醯胺 ίο (2-{[2-(3-氟苯基）乙基]胺基卜6-[4-(2-羥基乙基）哌啶 基](3-吼啶基))-N-(3-吡啶基甲基）曱醯胺 4-(6-{[2-(3-氟苯基）乙基]胺基卜5-[N-(3-吼啶基曱基）胺甲 醯基](2-吼啶基))-3-氧基哌畊羧酸第三丁酯 (2- {[2-(3-氟苯基）乙基]胺基}-6-(2-氧基哌畊基）(3·-比啶 15 基))-N-(3-吼啶基曱基）曱醯胺 (2- {[2-(3-氟苯基）乙基]胺基}-6-(2-氧基哌啶基）(3-吼啶 基))-N，N-二曱基甲醯胺 (6-[(3S)-3-(羥基甲基）咕咯啶基]-2-{[2-(3-氟苯基）乙基]胺 基}(3-吡啶基))-N-(3-吡啶基甲基）曱醯胺 2〇 2-[(2_{[2-(3-鼠苯基）乙基]胺基}-6-17比嘻0定基(3-0比0定基))幾 基胺基]-N_曱基乙醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(3-吼咯啉基）(3·-比啶 基))-Ν_(3-π比啶基曱基）甲醯胺 (6-((3S)-3 -胺基σ比咯σ定基)-2-{[2-(3 -氣苯基）乙基]胺基}(3_ 164 200823188 吼咬基))_N-(3』比咬基甲基）甲醯胺 n_-[(3r)小(6_{[2_(3 一氟苯基）乙基]胺基}-5_[Ν_(3』比啶基甲 基）胺甲酿基](2』比啶基))。比咯0定冬基](二甲基胺基）甲醯 胺 5 (6_氮σ旦基-24[2_(3-氟苯基）乙基]胺基}(3_吼啶 基))-Ν-(3_吡唆基甲基）甲醯胺 {2-[(2-(2-吼咬基）乙基）胺基]_6_ σ比咯啶基（3_ σ比啶 基)}-Ν-(3-吡啶基甲基）甲醯胺 {6-(4-甲基哌啶基）_2_[(2-(2_吡啶基）乙基）胺基](3_吡啶 1〇 基)}_队(&gt;比啶基甲基）甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基卜唑啉基_2_基)(3_口比 唆基))-N-(3-u比咬基甲基）甲醯胺 (f_((3R)_3_經基吡咯啶基峰㈣3-氣苯基）乙基]胺基}(3_吼 σ疋基))-N-{[2-(胺基曱基χ3_吡啶基)]甲基丨甲醯胺 15 Ν_{1&gt;(胺基曱基）(3-吼啶基）]甲基}(6_環戊小烯基 _2-{[2-(3-氟苯基）乙基]胺基}(3_吡咬基)）曱醯胺 (6_((3S)_3_氟吼略咬基)_2_ {[2_(3_氟苯基）乙基]胺基}〇比 咬基))_N_{〇(胺基甲基)(3_t定基)]甲基}甲醯胺 (6_((叫3-氟.比咯啶基泣似分氟苯基）乙基]胺基泊』比 20 &quot;定基胺基甲基)(3•吼咬基)]甲基}甲酸胺 則[2-(胺基甲基)(3_吼咬基)]甲基}(2_{[2_(3_氣苯基）乙基] 胺基}-6-哌啶基(3-吡啶基》曱醯胺 N-{[2-(胺基甲基)(3“比咬基)]甲基}(2_{[2_(3_氟苯基）乙基] 胺基卜6-吡咯啶基(3_吡啶基)）曱醯胺 165 200823188 N [(3S)-l_(6-{[2-(3-氟苯基）乙基]胺基卜5-[队(3-吼咬基甲 基)胺甲醯基](2-吡啶基))吡咯啶_3-基]甲氧基甲醯胺 4|{[2-(3-氟苯基）乙基]胺基卜5]N_[(N_甲基胺甲酸基） 甲基]甲酉皿基}-2-口比a定基)]，2, 5,6-四氫吼咬幾酸甲酯 [(3R) 1 (6_{[2_(3_氟苯基）乙基]胺基）_5_[队(3_吼咬基甲 基)月女甲I基](2-π比.定基))σ比嘻咬各基]曱氧基甲醯胺 =基，基)乙基)胺基砂㈣卿 邮細基砂 二基i:二(ι’2,5’6-·_μ (5-氣-2-{[2-(3 # 15 20 基)陶Μ基;旬=]竭料靖卜比咬 2_(6_{[2 3 &amp;疋基甲基）甲醯胺 醯基]乙基]胺基卜5_[N_(3'°比咬基甲基)胺甲 ㈣唾讀酸甲酉旨 基}〇比唆基))’Ν β 2_基))_2_{[2_(3-氟苯基）乙基]胺 N-m2RVw ) 比啶基曱基）甲醯胺 胺 ）乙基]胺基卜6_鱗唆基〇比唆基)）甲醯 乳比11各唆基)-5_氟_2_{[2_(3_氟苯基）乙基]胺基泊. 166 200823188 口比唆基))_N_{|&gt;(胺基曱基比啶基w甲基j曱醯胺 (6-((3R)-3_羥基吼咯啶基)_5•氟_2_{[&gt;(3_氟苯基〉乙基擔 基}(3-吡啶基))-Ν-[(2·{[(第三丁氧基）羰基胺基]甲基}(3_ 口比啶基)）曱基]甲醯胺 (6-((3R)-3-羥基吼咯啶基)_5_氟_2][2_(3_氟苯基）乙基]胺 基}(3-吡啶基))-Ν_{[2·(胺基甲基)(3_吡啶基)]曱基}甲醯胺 (6-(1-乙醯基(4-1，2,5,6_四氫吡啶基氟苯基）乙 基]胺基}(3_σ比咬基))專(3』比咬基甲基）甲贐胺 (2-{|&gt;(3-氟苯基）乙基]胺基卜卜叫又认凹氳^比啶基砂 t定基))-Ν-(3-吼啶基甲基）曱醯胺 4_(6-{[2-(3-氟苯基）乙基]胺基卜比啶基曱基）胺曱 ife基]-2-吼啶基)-1，2, 5,6-四氳吡啶羧酸第三丁酯 (6-ί衣戊基-2-{[2-(3-氟苯基）乙基]胺基} (3_吼啶基))_n_(3_ σ比咬基甲基）甲醯胺 (6-(1，4-二氧雜螺基[4 5]癸-7_烯_8_基)_2_{[2_(3_氟苯基）乙 基]胺基}(3“比啶基))專(3_π比啶基甲基）曱醯胺 (6 {[2 (3氟本基）乙基]胺基卜比ϋ定基甲基）胺甲 酉皿基]_2_ 口比唆基)-ΐ，2,5,6-四氫π比咬竣酸甲酯 (6- 戊-1-烯基_2-{[2-(3_氟苯基）乙基]胺基}(3_ σ比啶 基))-Ν-(3-吡啶基曱基）甲醯胺 N-{(lR)-2_[(5_氟_2_{[2♦氟苯基）乙基]胺基卜6_吡咯啶基 (3-口比唆基))幾基胺基]_異丙基卜2-[(第三丁氧基)幾基胺基] 乙酸胺 (2-{[2-(3_氣本基）乙基]胺基}_6-(4-氧基環己_卜稀基)(&gt;比 167 200823188 啶基))-N-(3-吼啶基甲基）甲醯胺 ..(6-((3R)-3-氟吼咯啶基）-_5-氟-2-{[2-(3-氟苯基）乙基]胺 基}(3-吼啶基))-N-[(2-{[(第三丁氧基）羰基胺基]甲基}(3-吼啶基)）甲基]曱醯胺 5 (6-壤己基-2-{[2-(3-亂苯基）乙基]胺基}(3-吼ϋ定 基))-Ν-(3-吼啶基曱基）甲醯胺 (6-壤己-1-細基-2-{[2-(3-氣苯基）乙基]胺基}(3- °比σ定 基))_Ν_(3-吼啶基甲基）甲醯胺 N-[((2R)-l-{3-[(第三丁氧基）羰基胺基]丙基卜5-氧基吼咯 ίο ϋ定-2-基）甲基](5-氣-2-{[2-(3-氣苯基）乙基]胺基}-6-117比洛17定 ' 基(3-吼啶基)）甲醯胺 (6-[1-(Ν，N-二曱基胺曱醯基）(4-1，2,5,6-四氫啦唆 基)]-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基))-Ν-(3·-比啶基 曱基）甲醯胺 15 (5- &gt;臭-2- {[2-(3-氣苯基）乙基]胺基} -6-σ比咯咬基（3-ϋ比ϋ定 基))-Ν-(3-吼啶基曱基）甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(1-曱基(4-1，2,5,6-四氫口比 啶基))(3-吼啶基))-Ν-(3-吼啶基曱基）曱醯胺 4-(6-{[2-(3-亂苯基）乙基]胺基}-5-[!^-(3-1?比11定基甲基）胺曱 20 醯基]-2-吼啶基)-1，4,5,6-四氳u比啶羧酸曱酯（2-{[2-(3-氟苯 基）乙基]胺基} _6-(2-味嗤淋-2-基)(3-ϋ比ϋ定基))-N-(3-atbσ定基 甲基）曱醯胺 N-{[(2R)-l-(4-胺基丁醯基）吼咯啶_2_基]甲基}(5-氟 -2- {[2-(3 -氣苯基）乙基]胺基}-6_ntb咯σ定基(3-ϋ比σ定基)）甲酿 168 5 15 200823188 胺 n(2^i4彻三丁氧基)羰基胺基]丁·醒基卜各咬-2· 口比啶基))甲醯胺 虱本土）乙基歸厂6♦各絲(3_ N {[(2R)小(2_胺基乙醯基）吡咯啶_2_基】尹基 本基）乙基]胺基}_6“比略絲心比絲))甲釀 :f :):1:{,[(第三丁氧基)羰基胺基]乙醯基”比咯啶-2· 土)甲基Κ5^_2·ί[2·(3_氟苯基）乙基]胺 吡啶基)）甲醯胺 1 基曱基)(3,基)]曱基}(5_氟_2-{[2-(3-氟苯基） 乙基]I女基}-6-吡咯啶基(3_吡啶基)）甲醯胺 t[((2Rh比咯咬-2-基）甲基](5_氟_2_{[2_(3_氟苯基）乙基]胺 基}-6-吡咯啶基(3-π比啶基》甲醯胺 (2R)_2_{[〇氟{[2_(3_氟苯基）乙基]胺基卜卜咕咯啶基 (3-吡啶基))羰基胺基]甲基}吡咯啶羧酸第三丁酯 N_{[2-(胺基甲基）(3-吡啶基）]曱基}(6_環丙基_5_氟 _2-{[2_(3-氟苯基）乙基]胺基}(3_π比咬基)）曱醯胺 N_{(1 R)-2-[(5-氟-2-{[2-(3_說苯基）乙基]胺基卜6-吼略口定 基(3-吼唆基))叛基胺基]-異丙基卜2-胺基乙酸胺 〇{[2-(3-氟苯基）乙基]胺基}_6_[1_(曱基磺醯 基）(4-1，2,5,6-四氫σ比啶基)](3-°比咬基))-队(3-吼唆基曱基） 曱醯胺 [4_(6_{[2-(3-氟苯基）乙基]胺基卜5_[Ν_(3』比啶基曱基)胺曱 20 200823188 醯基](2-啦啶基))哌畊基]-N，N-二甲基甲醯胺 4-(6-{[2-(3-氟苯基)_乙基]胺基}-5-[N-(3-口比咬基甲基)胺甲 醯基]-2-u比啶基)哌畊羧酸曱酯 (6-(3-胺基0比咯11 定基)·2_{[2-(3-氟苯基）乙基]胺基}(3_σ比咬 5 基))-Ν-(3-吡啶基甲基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-嗎琳-4-基（3_ π比咬 基))-Ν-(3^比啶基甲基）曱醯胺 (6-[(2R)-2-(羥基曱基)吼咯啶基]_2-{[2_(3_氟苯基）乙基]胺 基}(3_0比咬基))-Ν-(3-σ比咬基甲基）曱酿胺 〇 2-[(6-((33)_3-經基吼口各咬基）-2-{[2-(3-氟苯基）乙基]胺 基}(3-吡啶基))羰基胺基]-N-甲基乙醯胺 2-[(2-{[2-(3_氟苯基）乙基]胺基卜6-(4_經基旅n定基)(3_σ比咬 基))羰基胺基]-Ν-曱基乙醯胺 (第三丁氧基)-Ν-[1·(6-{[2-(3-氟苯基）乙基]胺基}-5_[ν_(3_ 5 吼啶基甲基）胺甲醯基](2-吡啶基））吡咯啶_3_基]甲酿胺 (6-[(3R)-3_(二曱基胺基)D比咯啶基]_2_{[2_(3_氣苯基）乙基] 月女基}(3-ϋ比咬基))_Ν-(3-ϋ比咬基曱基）曱酿胺 2-[(H(3S)_3-氟吼咯啶基)-2-{[2_(3_氟苯基）乙基]胺基}(3_ °比咬基))羰基胺基]_N_曱基乙醯胺 3 2-[(6-((3R)冬羥基吼咯啶基）_2_ {[2_(3_氟苯基）乙基]胺 基}(3,吡啶基))羰基胺基]-N-甲基乙醯胺 氟苯基）乙基]胺基}_5_[N-(3』比啶基曱基)胺 甲酿基]_2-吡啶基)吼洛啶-3-基]乙酸 (2_{[2-(3·氟苯基）乙基]胺基}-6-(3-(4-吼唆基）π比略咬 170 200823188 基)(3-吡啶基))_沁(3_吡啶基甲基）曱醯胺 2修(3,3::二氣鱗絲&gt;2·ί[2·(3-氟苯基）乙基]胺基}(3-°比咬基))¾基胺基]甲基乙酿胳 Ν-{[6-(胺基甲基)(2』比咬基)]甲基Κ2_{[2_(3_氣苯基)乙 胺基}-6-吡咯啶基(3_吡啶基)）甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基}_6_[3_(三氟甲基）吼咯啶 基](3·吡啶基))-Ν-(3-吡啶基曱基）甲醯胺 (6-(3,3-二氟t各咬基)_2_{[2_(3_氣苯基）乙基]胺基》比 啶基))-Ν-(3-吡啶基甲基）甲醯胺 10 Ν-{[6-(胺基甲基)(2_吼咬基甲基}(2_{[2_(3_氟苯基)乙基] 胺基}-6-派咬基(3-n比咬基)）甲酿胺 (H(3S)-3-經基吼略咬基)_2_{[2_(3_氟苯基）乙基]胺基办n比 啶基))-Ν-{[6-(胺基甲基)(2_t定基)]曱基}曱醯胺 15 (6-((3R)-玲基鱗咬基)_2_{[2_(3_氟苯基）乙基]胺基心比 啶基))-N-{[6-(胺基甲基)(2_吡啶基)]甲基 ㈣⑽-3·氟料絲)_2_{[2_(3_氟苯基）乙基]胺基}化比 啶基))-沁(3_吡啶基曱基）曱醯胺 (H4-(胺基曱基)派啶基]-2·{[2_(3_敦苯基）乙基]胺基}(3 &quot;比啶基))-N-(3-吡啶基曱基）曱醯胺 20 2-[〇{|&gt;〇氟苯基）乙基]胺基}_6«基(3_吼口定基))幾基 胺基]-N-曱基乙醯胺 &amp; (2·{[2·(3-氟苯基）乙基胺基}-6q3_(曱基磺醯基）^比咯啶 基]〇吡啶基))·Ν-(3-吡啶基曱基）甲醯胺 (6-[(2S)-2-(曱氧基甲基)鱗唆基]_2_{[2_(3_氣苯基）乙基] 171 200823188 胺基}(3-吡啶基))-N-(3-吡啶基曱基）曱醯胺 (第二丁氧基）_Ν-{.[1-(6-_{[2-(3-氟苯基）乙基]胺 .基}-5-[N-(3-吼啶基曱基）胺曱醯基](2-吼啶基))(4-哌啶基)] 甲基}曱醯胺 5 (弟二 丁乳基)-Ν-[1-(6-{[2-(3-氣苯基）乙基]胺基}-5-[N-(3- 吡啶基曱基)胺甲醯基](2-吡啶基))(4-哌啶基)]曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基卜6-(4-羥基-4-苯基哌啶基)(3-吼啶基))-N-(3-吡啶基曱基）甲醯胺 1-(6-{[2-(3-氟苯基）乙基]胺基}-5-[1^-(3_11比咬基甲基）胺曱 10 醯基]-2-吡啶基)哌啶-4-羧酸乙酯 * (6-((3S)-3-氟吼咯啶基)-2-{[2-(3-氟苯基）乙基]胺基}(3-口比 啶基))-N-(3-吡啶基曱基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-[4-(N-曱基胺曱醯基)哌啶 基](3-吼啶基))-N-(3-吼啶基曱基）曱醯胺 15 (2-{[2-(3-氣苯基）乙基]胺基}-6-(4-經基旅咬基）(3-11比。定 基))_Ν_(3-π比啶基甲基）曱醯胺 (2-{[2-(3-氣苯基）乙基]胺基}-6- 11 底12井基（3-吼σ定 基))-Ν-(3-吼啶基甲基）曱醯胺 (6-((3S)-3-羥基哌啶基)-2-{[2-(3-氟苯基）乙基]胺基}(3-口比 2〇 啶基))-N-(3-吼啶基曱基）曱醯胺 N-[l-(6-{[2-(3 -氟苯基）乙基]胺基}_5-[Ν-(3-σΛϋ定基曱基)胺 甲醯基]-2^比啶基）吡咯啶-3-基]乙醯胺 (2- {[2-(3-氟苯基）乙基]胺基}-6-[2-(羥基曱基）嗎啉-4-基](3-吼啶基))-N-(3-吼啶基曱基）曱醯胺 172 200823188 (6_[(3S)_3_(甲基胺基)吼咯啶基]-2_{[2-(3-氟苯基）乙基]胺 基}(3-吼啶基》_N-(3_吡啶基甲基）甲醯胺 (2-{[2-(3_ 鼠苯基）乙基]胺基 jj-d^thiazaperhydroir^·基) (3_0比°疋基))-队(3-〇比咬基甲基）甲醮胺 (6-(1，1-二氧基（i，4_thiazaperliydroin_4_*))-2·{[2-(3-氟苯 基）乙基]胺基}(3-吼咬基))-Ν-(3·σΛσ定基曱基）甲醯胺 (6-(4-乙醯基哌畊基)_2-{[2-(3_氟苯基）乙基]胺基}(3_0比啶 基))-N-(3-吡啶基曱基）甲醯胺 (2-{[2-(3 -氟苯基）乙基]胺基卜6-(4·^辰咬基。辰ϋ定基)(3-π比cr定 基))-N-(3-吡啶基曱基）曱醯胺及 4·(6-{[2-(3-氟苯基）乙基]胺基}-5-[N_(3-ai：b咬基曱基）胺曱 酿基]-2-吡啶基)哌畊羧酸乙酯。 本發明係提供至少一種選自式VII化合物及其醫藥上 可接受鹽類之化學品Wherein 20 R and R 4 are independently selected from the group consisting of hydrogen, cyano, halo, hydroxy, azide 150 200823188, nitro, (d), sub (tetra), sulfur alkoxy, optionally substituted Substituted oxy group, as needed violent 妳Μ *Substituted amine group, aryloxy group of the work, heteroaryloxy group as needed, substituted as needed = oxy secret _, · to be replaced by the burning base, as needed to replace the two or two to see the need to avoid the county, as needed to replace the aryloxy, as the general green generation, as needed Substituted heterochloro, substituted heterocyclic filaments, optionally taken amino groups, optionally substituted, 10 15 groups are considered to be [substituted amino groups and optionally substituted carbaminodoyl; Z Providing self-respecting substituted cycloalkyl groups and optionally substituted hetero-calcining bases; Z2 is selected from the group consisting of hydrogen, optionally substituted silicyl groups, carboxyl groups, optionally substituted alkoxycarbonyl groups, A substituted thiol group, an optionally substituted alkenyl group, an optionally substituted alkyl group, an optionally substituted heterocycloalkyl group, Optionally substituted heteroaryl and optionally substituted aminocarbonyl; z is selected from the group consisting of a dentate group and optionally substituted alkyl; and R3 is selected from the group consisting of hydrogen and optionally substituted alkyl. In a particular embodiment of the compound of formula VI, Z2 is selected from the group consisting of a carboxy group, an alkoxycarbonyl group optionally substituted, an optionally substituted thiol group, an optionally substituted alkenyl group, and an optionally substituted alkyl group. In a particular embodiment of the compound of formula VI, Z2 is selected from the group consisting of a carboxy group, optionally substituted piperidinylcarbonyl, optionally substituted pyridylcarbonyl, optionally substituted lower alkyl, optionally substituted Lower alkenyl and low carbon 151 20 200823188 alkoxycarbonyl. In a particular embodiment of the compound of formula VI, z2 is selected from the group consisting of (2-(N-ethylidinomethyl)methylnidanyl-1-yl)carbonyl; (2-aminomethylpiperidin-1- Carbonyl; 1-hydroxy-2-amino-ethyl; 2-((methyl sulphate) fluorenyl)piperidin-1-ylcarbonyl-5; 2-(methylaminocarbonyl) Vinyl; 2_(acridinyl-3-ylindenyl)-2H-triazol-5-yl;amino fluorenyl; carboxy; oxiranyloxycarbonyl; acridine-2-ylcarbonyl; indole-3-yl a few bases; and σ ratios determine _4_ bases. In a particular embodiment of the compound of formula VI, R3 is selected from the group consisting of hydrogen and, if desired, a substituted lower alkyl group. In a particular embodiment of the compound of formula VI, R3 is selected from the group consisting of hydrazine and a lower alkyl group. In a particular embodiment of the compound of Formula VI, R3 is selected from the group consisting of hydrogen and sulfhydryl. In a particular embodiment of the compound of Formula VI, R3 is hydrogen. In a particular embodiment of the compound of Formula VI, Z2 is -C(0)NR2R5, wherein R2 is selected from an optionally substituted alkyl group and optionally substituted cycloalkyl; and R5 is selected from hydrogen and Substituted burnt base as needed. In a particular embodiment of the compound of Formula VI, R4 is selected from the group consisting of hydrogen, cyano, halo, azide, optionally substituted aminocarbonyl, and optionally substituted alkyl. In a particular embodiment of the compound of formula VI, R4 is selected from the group consisting of hydrazine, cyano, chloro, bromo, fluoro, azide, optionally substituted alkylaminocarbonyl and optionally substituted methyl. In a particular embodiment of the compound of Formula VI, R4 is selected from the group consisting of hydrogen, cyano, chloro, dimethyl, azide, σ, -3-ylmercaptoalkyl, amino fluorenyl, and 152 200823188 base. - In a specific practical towel of ^νι compound, r4 is hydrogen. In the compound of formula VI, the crucible is fixed, and r5 is selected from the group consisting of hydrazine and a low carbon alkyl group. 5 In the specific implementation of the compound of formula VI, r5 is selected from the group consisting of hydrogen and methyl. In a particular embodiment of the formula VH composition, R5 is deuterium. In the 4-inch embodiment of the formula VI, R2 is selected from the group consisting of an optionally substituted methyl group, an optionally substituted ethyl group, an optionally substituted propyl group, and optionally substituted. a pentyl group which is substituted according to the need, and a cyclohexyl group which is substituted by a ring, a cyclopentyl group which is optionally substituted, and a cyclohexyl group which is optionally substituted, as the case requires. Substituted groups need to be replaced by -, two or three groups selected by the following: aryl groups which are optionally substituted, heteroaryl groups which are optionally substituted, optionally substituted 雑% thiol, A substituted cycloalkyl group, an optionally substituted amino group 15 carbonyl group, an optionally substituted amino group, a hydroxyl group, a carboxyl group, an optionally substituted alkoxycarbonyl group, and an optionally substituted alkoxy group, if necessary. In a particular embodiment of the compound of Formula VI, R2 is selected from the group consisting of fluorenyl and ethyl' wherein methyl and ethyl hydrazine are optionally substituted by one or two groups selected from the group consisting of: An aryl group, optionally substituted hetero 20 aryl group, optionally substituted heterocycloalkyl group, optionally substituted cycloalkyl group, optionally substituted aminocarbonyl group, optionally substituted amino group, hydroxy group And a carboxyl group, an alkoxycarbonyl group optionally substituted, and an alkoxy group which may be optionally substituted. In a particular embodiment of the compound of Formula VI, R2 is selected from the group consisting of (1-(2-amino 153 200823188 ethylbisoxazol-3-yl)methyl; (1-(methylsulfonyl)piperidinyl) (1)-(Ethylpyridinyl-3-yl)methyl; (1-ethinylpyrrolidin-2-yl)methyl; (1H-imidazolium-2-yl)indenyl; (1Hj (1 - fluorenyl-1H-pyrazol-3-yl) fluorenyl; (1-methyl-1H-pyrazole-5-yl) fluorenyl; (2-( Aminocarbonyl 5 yl) ethylamino) benzyl methyl; (2-(aminomethyl). butyl-3-yl)methyl; (2-(carboxy)ethylamino)carbonylmethyl (2-(dimethylamino)ethylamino)carbonylmethyl; (2-(hydroxy)ethylamino)carbonylmethyl; (2-(methylamino)ethylamino)carbonyl Mercapto; (2-(N-methyl-N-(t-butoxycarbonyl)-amino)ethylamino)carbonylmethyl; (2-oxypiperidin-3-yl)indenyl; (3-(didecylamino)propylamino)carbonylmethyl; (3-(hydroxy)ethylamino)carbonylindole-yl; (3-(t-butoxycarbonylamino)propyl) Amino)carbonylmethyl; (4-(amine.ylmethyl)acridin-2-yl)indenyl; (5_( (6-((1,3-dioxyisoindol-2-yl)indolyl)-acridyl-2-yl)methyl; (6-( 2-(Aminoethylamino)pyridin-2-yl)methyl; (6-(3-aminopropylamino) acridine 15 yl) fluorenyl; (6 &lt;Aminomethyl)pyridin-2-yl)methyl;(6-(hydroxyindenyl)pyridin-2-yl)indenyl;(6-bromoacridin-2-yl)methyl; Sulfolamyl) Weilkylmethyl; (acridin-2-yl)ethylamino; (t-butoxycarbonylamino)ethyl)-1 fluorene-carbazole-methyl-methyl; 1-(2_( Tributoxycarbonylamino) ethyl)·1Η-oral ratio sal-5_ylmethyl; 1_(aminocarbonyl)_2_(amino)-ethylidene; 20 amidino group&gt;3_( Amino)propyl; decylamino) 4-(amino)-butyl; 1-(aminocarbonyl)-4-(benzyloxycarbonylaminopentyl; _(aminocarbonyl) _5_(Amino)pentyl; 1-(aminocarbonyl)ethyl; L(reactive)_2_(amino)-eth-1-yl; 1-(dimethylaminocarbonyl)_2_(aminopurine) B-oxime-yl; 丨-(hydroxy)-2-(amino&amp;methylamino)ethyl-yl-yl; 丨-(trans-base)_2_(ethoxy 154 200823188 methylamino group Ethyl-1-yl; 1-(hydroxy)-2-(indole-2-ylmethylamino)eth-1-yl' 1-(methyllacyl) ruthenyl-2-(amino group) )-Ethyl-1-yl; i-(·曱oxycarboyl)-2-(t-butoxycarbonylamino)-ethyl-i-yl; 1β(methoxycarbonyl)eth-1-yl ' 1_(曱基月女基爹基基)-2-(Amino)-Ethyl-1-yl (2 〇cc); 1-(曱5-aminoamino)ethyl-1-yl; 1-amine 2-dimethoxy-2-yl-ethyl-1-yl; 1-methoxy-l-yl-trans-yl-1-yl; 2-(2-aminoethoxy)ethyl; 2- (2-Aminoethyl)-acridin-6-ylindenyl; 2-(2-aminoethylamino)ethyl; 2-(3-fluorobenzyl)ethyl; 2-(3- Methoxylated) ethyl; 2-(6-(aminomethyl)π-buty-2-yl)ethyl; 2-(ethionylamino)ethyl; 2-(amino)ethyl 2-(amino 1 carbonyl) &gt;2-(ethenylamino)-eth-1-yl;2-(aminocarbonyl)_2-(amino)-ethyl; 2-(amine Ethyl)ethyl; 2-(amino fluorenyl) 吼5-ylmethyl; „ 2-(inferior)-2-(amino)-eth-1-yl; 2-(dimethyl Ethylamino)ethyl; 2-(dimethylaminocarbonyl)-2-(amino)-eth-1-yl; 2-(ethoxycarbonyl)ethyl; 2-(methoxycarbonyl) -2-(Ethylamino)-eth-1-yl; 2-(decyloxy)-2-(amine 15 yl)·ethyl small group; 2-(methoxylamino group) Ethyl; 2·(decylamino)ethyl; 2-(decylamino)-2-(ethenylamino)-eth-1-yl; 2-(decylamino) Base)-2- (amino)-ethyl-1-yl; 2-(indolyl hydrazino)ethyl; 2-(decyloxy)-2-(amino)-eth-1-yl; 2-(N -(Tertibutoxymethyl)-recalcyl (methyl)-amino)ethyl; 2-(Brigade_small)ethyl; 2:10-pyridyl-2-yl)ethyl; 20 2 Than-2-yl)ethyl; 2-(σΛσ-3-yl)ethyl; 2-(t-butoxymethylaminomethyl) acridine-3-ylindenyl; 2-( Third butoxycarbonylaminoalkyl)pyridin-6-ylindenyl; 2-(trifluoromethyl)-pyridine-6-ylindenyl; 2-aminopurine-3-ylindenyl; -Amino group ratio -5-yl fluorenyl group; 2-chloro-ratio 唆-5-yl fluorenyl; 2-cyano quinone-5-yl fluorenyl; 2-hydroxy-3-amino-propyl- 1-yl; 2-hydroxyethyl 155 200823188; 2-methoxyethyl-1-yl; 2 decyloxy aridin-3-ylmethyl; 2-methoxypyridin-5-yl fluorenyl; 2-mercaptopyridine-3-ylindenyl; 2-methylpyridin-5-ylindenyl; 2-methylpyridine-6-ylindenyl; 3-(2-aminoethyl)cyclohexyl)fluorenyl 3-(4-mercaptopiperidin-1-yl)propyl; 3-(amino)-3-(methylaminocarbonyl)propan-5-yl; 3-(aminocarbonyl)propyl; -(aminomethyl)benzyl; 3-(aminomethyl)acridin-2- Methyl; 3-(decyloxycarbonyl)propyl; 3-(decylaminocarbonyl)propyl; 3-(trifluoromethyl)-π-pyridin-2-ylmethyl; 3,4- Difluorophenyl fluorenyl; 3-aminomethyl acridin-4-ylmethyl; 3-aminopropyl; 3-amineindolylcyclopentyl; 3-carboxypropyl; 3-hydroxypropyl; 3-methoxypropyl; 4 (amino 曱 ο ο ο ο ο ο ο ο ο ο ο ο ο ο • 4-(t-butoxy arylamino)-morphinyl fluorenyl; 4-aminobutyl; 4-aminomethyl acridine-3-ylindenyl; 4-cyanobenzyl 4-fluorobenzyl; 4-mercaptoaminopyridin-3-ylindenyl; 4-mercaptobenzyl; 4-morpholinylpyridine_3_ylindenyl; 4-piperidinyl acridine -3-ylindenyl; 5-((bis(dimethylamino)methyl15-ylamino)indolyl) σ ratio -3-yl fluorenyl; 5-(amino fluorenyl) 吼tr _ 2-methylmethyl; 5-(aminomethyl)pyridin-3-ylmethyl; 5-(hydroxymethyl)pyridin-3-ylindenyl; 5-(dimethyleneoxyaminopurine) Base) - π ratio bit _2 _ methyl group; 5-(trifluoromethyl decyl-2-yl fluorenyl; 5-aminopentyl group; 5-amino group ratio bit-2-ylmethyl group; 6 - ((bis(didecylamino)曱 胺 ) ) 甲基 甲基 甲基 20 20 20 20 ; 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 20 π 啶 啶 -2-yl) fluorenyl, 6-aminohexyl; amino fluorenyl; benzyl; cyclopropyl fluorenyl 'monodecylaminomethyl; isopropyl; 4-salt-5-ylmethyl; oxime Ikylmethyl; fluorenyl; decylamino thiol thiol; nickname wah_2_ylmethyl; brigade 17 1-4 amino group; _2_妇_1_基;π比〇井_2_ylmethyl; σ ratio 唆156 200823188 -2-ylmethyl; acridin-2-ylmethyl-N-oxide; pyridine-3- Methyl; pyridyl&gt;3-ylmethyl-N-oxide;pyridylmethyl;thiophene-2-ylmethyl; Cephen-3-ylmethyl. In a particular embodiment of the compound of formula VI, z3 is selected from the group consisting of halo and, if desired, substituted lower alkyl. 10 15 20 In a particular embodiment of the compound of formula VI, z3 is selected from the group consisting of fluorenyl, optionally substituted methyl, optionally substituted ethyl and optionally substituted propyl, wherein methyl, ethyl And a propyl group is optionally substituted by one or two groups selected from the group consisting of the following, optionally substituted aryl, J substituted heteroaryl, optionally substituted heterocycloalkyl, ' : substituted cycloalkyl and optionally substituted aryloxy. In a particular embodiment of the compound of formula vi, the Z3 is selected from the group consisting of 2-(3_曱美#=)^ethyl, (tetrahydrofuran-2-yl)methyl, 丨-hydroxycyclohexylmethyl , Ben-oxopentan-2-yl)ethyl, 2-(IH-Miso-4-yl)ethyl, 2-(1,3-,+yl)ethyl, 2-(1_methyl 唆Ice-based ethyl, 2_(2,3-based; earth)ethyl, 2_(2,5-difluorophenyl)ethyl, 2_(2,6-diphenyl)ethylenediyl/chlorobenzene Ethyl, 2-(2-cyanophenyl)ethyl, 2-(2-a', di-(2-phenylphenyl)ethyl, 2♦ decyloxyphenyl)ethyl, Ethyl, ethyl 2-(2-oxo-purinyl)ethyl, 2-(7)-di-(yl)ethyl, 2-(2-oxypyrrolidine)ethyl: ethyl Styyl) ethyl, 2-(3,4·difluorophenyl)ethyl 曱 2 2 rice methyl, yl) ethyl bis 2) ethyl, 2-(3-aminomethyl phenyl) Ethyl, 2 carboxy carboxy stupid: oxazolium _(3-mumylphenyl)ethyl, 2_(3_fluorophenyl) 2_(radio)-ethyl, 157 200823188 ethyl, 2 fluoro end 2 _ base) ethyl, ice methoxy) ethyl, 2-(3-methoxyphenyl)ethyl, 2-(3-methylphenyl)ethyl]aminophenyl)ethyl, 5 10 15 20 phenylphenyl)ethyl, 2-(benzo-3)-dioxapentanyl-5-yl), acetyl, 2,(2)yl)_2_(phenyl)ethyl Base, 2_(phenyl)ethyl, 2,decain-2-yl)ethyl, 2_(吼唆_3_yl)ethyl, dioxin, 2,cyclohexylethyl , 2_? storage of soil base, the present ethyl ether, 2-propenylpropyl small group, 3_d Miwa <female propionate, = propyl group, benzyl, chlorine, isopentyl, internal group, Age 2 _ 甲 σ ϋ ϋ 基 甲基 甲基 methyl and 嗟 -3--3-methyl. In a particular embodiment of the compound of formula W, 23 is selected from the group consisting of noisy phenyl)ethyl and 2-(pyridin-2-yl)ethyl. In a particular embodiment of the compound of formula VI, a heterocycloalkyl group, wherein each group is optionally substituted with a benzyl group and a group: a nitrogen group, a group, a group; Base, depending on the need to replace the thin / visual! Substituted bases, substituted as needed, substituted alkoxy groups, accustomed to substituted amino groups 3: Λί, optionally substituted sulfhydryl groups, ruthenium substituted soils Substituted amine group, if desired ==: leucoyl, heteroaryl substituted as needed, optionally substituted thiol and repeating acid group to be substituted. In a particular embodiment, zl is selected from the group consisting of a cycloalkyl group and a system selected from the group consisting of - or two of which are selected from the group consisting of the following: a dentate base, a thiol group, a mercapto group, an optionally substituted group, and optionally Substituted low carbon dilute, as low as desired 158 200823188 Carboalkoxy, carboxy, optionally substituted lower alkoxycarbonyl, optionally substituted fluorenyl, optionally substituted aminocarbonyl And, optionally, a substituted heterocycloalkyl group, optionally substituted heteroaryl group, optionally substituted thiol group, and optionally substituted sulfonyl group. 5 In a particular embodiment of the compound of formula VI, Z1 is selected from the group consisting of 1-(2Η)-(decyloxycarbonyl)-3,4-dihydroacridin-4-yl; 1-(2Η)-(oxygen) Alkyl carbonyl)-5,6-two rat bite-cardiac, 1-(2Η)-(decyloxymethyl)-5,6-dihydroacridin-4-yl; 1-(2Η)-(第Tributoxycarbonyl)-5,6-diacridin-4-yl; ίο 1 -(2 Η)-5,6-two mice 0 to -4-yl, • 1-(ethenyl) - 4,5-dihydroimidazol-2-yl; - 1_(dimethylaminocarbamimidyl)-1,2,3,6-tetrahydro. Bipyridin-4-yl; 1-(decyloxymethyl)-4,5-dihydroimidazol-2-yl; 1-carbyl-4,5-diaza-111_flavory-2-yl , 15 1 -methyl-1, 2, 3, 6_ four mice 11 ratio. 4-yl, 2-(ethylhydrazinylfluorenyl)pyrrolidin-1_yl; 2-(3⁄4 fluorenyl)yl-linyl; 2-(hydroxymethyl)pyrrolidin-1-yl ; 2-(decyloxymethyl)oxaridin-1-yl; 2H-upyr-1(5H)-yl; 20 2-hydroxymorpholinyl; 2-methyl-4-(third Oxycarbonyl)-piperidin-1-yl; 2-methoxy-5-light-anthracenyl; 2-oxynipine; 2-oxybendyl; 2-oxyindole; 159 200823188 3-(3,3-Dimercaptoyl) 17-bite-l-yl, . 3-(Aminomethyl)-1[7-pyrene 17-yl, 3-(carboxyl Mercapto)-indolyl; 3-(dimethylamino, 5 3-(didecylamino)-pyrrolidin-1-yl; 3-(hydroxyindenyl)pyrrolidine- 1-yl; 3-(methoxycarbonylamino)pyrrolidine; 3-(methylsulfonyl)pyridin-1-yl; 3-(indolyl-indole-methyl )-amino-mercapto)-pyridinyl small group; ίο 3-(^比ϋ定-4-yl)ϋ比鸣^^-1 -yl, • 3-(t-butoxycarbonylamino group)吼-pyridinyl; 3-(trifluoromethyl)pyrrolidin-1-yl; 3,3-difluoropyrrolidinyl; 3-ethenylaminopyrrolidinyl; 15 3 -amino group比定定-1 - base, 3- gas ratio test -1 - base 3-hydroxydecylpyrrolidin-1-yl; 3-hydroxypyrrolidine small group; 3-decyloxypyridylpyridin-1-yl; 20 3-decylamino-pyrrolidinyl; 3 -late Niang 1:1 well-1 -yl, 4-(ethenyl)-piped-1-yl; 4-(aminomethyl) brigade-1-yl, 4-(ethoxy-rebase)-派17井-1-基; 160 200823188 4-(ethoxycarbonyl)-piperidinyl; 4-(methylsulfonyl)cyclohex-1-enyl; 4-(N,N-dimethyl Aminocarbonyl)-piped-1-yl; 5 4-(t-butoxycarbonylamino)-piperidin-1-yl; 4-(t-butoxymethylaminomethyl)_σ 1-2 base; 4.5-dihydrosa-imidol-2-yl; 4.5-dihydrooxazol-2-yl; 4-hydroxy-4-phenylpiperidin-1-yl; ίο 4-carbyl Ethyl-precipitate-based; '4-transmethyl-precipitated-yl; 4-pyridylthiol; 4-methylaminocarbonyl-piperidinyl; 4-methyl-11 well-1 -yl, 15 4-mercaptopiperidinyl; 4-oxycyclohex-1-enyl; 5.6-dihydropyridine-1(2Η)-yl; nitrogen ° danyl; cyclohex-1-enyl; 20 cyclohexyl; gangrene-1 - fine base, cyclopentyl; morphine; sentiment well base; 161 200823188 brigade 17 fixed base; More than a bite base; and σ plugin. 5 10 15 20 In a particular embodiment of the compound of formula VI, R 1 is selected from the group consisting of hydrogen and optionally substituted lower alkyl. In a particular embodiment of the compound of formula VI, Ri is selected from the group consisting of hydrogen and lower alkyl. . In a particular embodiment of the compound of Formula VI, R1 is selected from the group consisting of hydrazine and hydrazino. In a particular embodiment of the compound of Formula VI, R1 is a gas. In a particular embodiment, the compound of formula VI is selected from the group consisting of (2-{[2-(3-phenylphenyl)ethyl]amino}}] hydrazinylindolinylpyridinylmethyl)carbenamide N- (10) S) small (6-{[2-(3-fluorophenyl)ethyl]amino}}5 for (3" than dimethylmethyl)amine hydrazine base (2-吼*yl) household ratio, each Bite _3_ base] (6 Wenling base scale butterfly (3-fluorobenzene! Amino) (3. acridine)) - Ν · « (aminocarbamoyl) carbamide 2-[( 6-«3R)·3-based base bite from {[2_(3-fluorophenyl)ethyl]amino}(3-indole))alkylamino]N_methylethyl (6_(read -3_Memei-methyl decylamine 6 - 吼嘻口定 N-(amine-mercaptomethyl) (2·{[2_(3_fluorophenyl)ethyl]amino) (3_pyridyl))carbammine•fluorophenyl)ethyl]amine (6-[(3R)-3-(hydroxymethyl))pyridinyl]_2_{[2_(3 base}(3 -pyridyl))-indole-(3-pyridylmethyl)formamide 162 200823188 (6-{(3S)-3-[(methylamino)indolyl]pyridinyl}-2-{ [2-(3-fluorophenyl)ethyl]amino}(3_j-pyridyl))-indole-(3-acridinylmethyl)decylamine _ N-{[(3R)-l- (6-{[&gt;(3-Fluorophenyl)ethyl]aminopyr-5-[indolyl-(3-acridinylmethyl)amine-carbamoyl](2-pyridyl))pyrrolidine-3 - ] mercapto}-Ν-methylethyl 5 decylamine (6-{(3S)-3-[(dimethylamino)indolyl]pyrrolidinyl 2-{[2-(3-fluorobenzene) Ethyl]amino}(3-pyridyl))-N-(3-pyridylfluorenyl)carbenamide (2-{[2-(3-phenylphenyl)ethyl]amino}- 6-(2-lactyl sigma) (3-anthracene))-N-(3-acridinylmethyl)carbenamide ίο (6-[(3S)-3-(amino fluorenyl) Ethrolidinyl]-2-{[2-(3-fluorophenyl)ethyl]amine•yl}(3-pyridyl))-N-(3-pyridylmethyl)decylamine-N -[(6-amino(3-acridinyl))methyl](2-{[2-(3-fluorophenyl)ethyl]amino}-6-pyrrolidinyl (3-acridinyl) )) indoleamine N-(2-aminomercaptoethyl)(2-{[2-(3-fluorophenyl)ethyl]amino}-6-pyrrole 15 pyridine (3-pyridyl) )) Myramine (6-((3R)-3-hydroxypyridinyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))-oxime -(3-pyridylfluorenyl)guanamine (2-{[2-(3-)-phenyl)ethyl]amino}-6-(2-milyl-sigma-pyrrolidine) (3-^ Binary base))-N-(3-Acridinemethyl)carbamamine 2〇(2-{[2-(3-))ethyl]amino}-6-indole σ determinate (3- ϋ 口 定 base))-Ν-(3^pyridylmethyl)carbamamine ( 6-((3R)-3-hydroxypyridinyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridine))-N-(2-amine oxime Base ethyl)carbamamine (6-((3S)-3-hydroxypyridinyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3- 163 200823188 acridine Base))-Ν-(3-acridinylmethyl)methalamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-[4-(hydroxymethyl)piperidin (pyridyl)(3-acridinyl))-indole-(3-pyridylmethyl)decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(5 -hydroxy-2-oxypiperidinyl)(3-5 pyridinyl))-N-(3-pyridylmethyl)carbamamine (2-{[2-(3-fluorophenyl)ethyl] Aminobi 6-(3-oxypipedyl)(3-acridinyl))-N-(3-acridinylmethyl)decylamine (2-{[2-(3-fluorophenyl) Ethyl]amino}-6-(4-mercaptopiperidinyl)(3-acridinyl))-N-(3-pyridylmethyl)decylamine ίο (2-{[2-( 3-fluorophenyl)ethyl]aminobi 6-[4-(2-hydroxyethyl)piperidinyl](3-acridinyl))-N-(3-pyridylmethyl)decylamine 4-(6-{[2-(3-Fluorophenyl)ethyl]aminopyr-5-[N-(3-acridinylindolyl)aminecarbamyl](2-acridinyl))- 3-oxypiperidinecarboxylic acid tert-butyl ester (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(2-oxyl) Plough base) (3·-bipyridyl 15 yl))-N-(3-acridinylfluorenyl) decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6 -(2-oxypiperidinyl)(3-acridinyl))-N,N-dimercaptocarboxamide (6-[(3S)-3-(hydroxymethyl))pyridinyl]- 2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))-N-(3-pyridylmethyl)decylamine 2〇2-[(2_{[2 -(3-murophenyl)ethyl]amino}-6-17 嘻0 base (3-0 to 0 base)) arylamino]-N-mercaptoacetamide (2-{[2 -(3-fluorophenyl)ethyl]amino}-6-(3-indolyl)(3·-pyridyl))-indole-(3-π-pyridylhydrazino)carbenamide ( 6-((3S)-3 -amino σ 咯 σ 定 ))-2-{[2-(3 - phenylphenyl)ethyl]amino} (3_ 164 200823188 吼 base))_N-(3比 咬 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基 基Stuffed base] (2" than pyridine)).比 0 定 定 ]]] (dimethylamino)carbamamine 5 (6-nitrosyl-denyl-24 [2-(3-fluorophenyl)ethyl]amino} (3_ aridinyl)) -Ν-(3_pyridinylmethyl)formamide {2-[(2-(2-)-yl)ethyl)amino]_6_ σpyrrolidyl (3_ σ-pyridyl)}- Ν-(3-Pyridylmethyl)formamide {6-(4-methylpiperidinyl)_2_[(2-(2-pyridyl)ethyl)amino](3_pyridine 1 fluorenyl) }_Team (&gt;pyridylmethyl)carbamamine (2-{[2-(3-fluorophenyl)ethyl)aminooxazolyl-2-yl) (3_ 唆 唆 唆) ))-N-(3-u-bitomethyl)carbamamine (f_((3R)_3_pyridylpyridinyl peak (tetra) 3-phenylene)ethyl]amino} (3_吼σ疋Base))-N-{[2-(aminomercaptopurine 3_pyridyl)]methylindoleamine 15 Ν_{1&gt;(aminomercapto)(3-acridinyl)]methyl}( 6_cyclopentenyl-2-({(2-fluorophenyl)ethyl]amino}(3_pyridyl)) decylamine (6_((3S)_3_ 吼 吼 slightly bite Base)_2_ {[2_(3_fluorophenyl)ethyl]amino} 〇 咬 base)) _N_{〇 (aminomethyl) (3_t-based)] methyl} formamide (6_((called 3-fluoro.pyrrolidyl-like fluorophenyl)ethyl]amine-based moieties than 20 &quot;dentylaminomethyl)(3•吼))methyl }Hydric acid amine then [2-(aminomethyl)(3_吼 基)]methyl}(2_{[2_(3_ phenyl)ethyl]amino}-6-piperidinyl (3 -pyridyl"decalamine N-{[2-(aminomethyl)(3"-bite)]methyl}(2_{[2_(3_fluorophenyl)ethyl]aminodibu 6- Pyrrolidinyl (3_pyridyl)) decylamine 165 200823188 N [(3S)-l_(6-{[2-(3-fluorophenyl)ethyl]amine-based 5--[Team (3-吼Ketylmethyl)amine-mercapto](2-pyridyl)pyrrolidin-3-yl]methoxycarbamidine 4|{[2-(3-fluorophenyl)ethyl]aminopurine 5 ]N_[(N_Methylaminocarbamic acid)methyl]methyl sulfonate}}-2-port ratio a)),2,5,6-tetrahydroindolyl acid methyl ester [(3R) 1 ( 6_{[2_(3_Fluorophenyl)ethyl]amino)_5_[Team (3_ 吼 基 甲基 甲基))] [ 2- 甲 I ( ( 2- 2- 2- 2- σ σ σ σ σ σ ] 曱 methoxy carbamide = yl, yl) ethyl) amine sand (four) qing ji fine sand two base i: two (ι'2, 5'6-·_μ (5-gas-2-{[2 -(3 # 15 20 基)陶Μ基;旬=]Exhaustion Jingbie than bite 2_(6_{[2 3 & decylmethyl)carbamamine]ethyl]amine b 5_[N_ (3'° ratio dimethyl group) amine A (tetra) sputum oxime group 〇 〇 唆 base)) 'Ν β 2 _ base)) _2_{[2_(3-fluorophenyl)ethyl] Amine N-m2RVw) pyridyl hydrazinyl) carbamide amine) ethyl] amide 6 6 唆 唆 〇 ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) 2_(3_Fluorophenyl)ethyl]amine beryl. 166 200823188 唆 唆 base))_N_{|&gt;(Amino hydrazinopyridyl w methylj decylamine (6-((3R)) -3_hydroxypyridinyl)_5•fluoro_2_{[&gt;(3_fluorophenyl>ethyl-supporting}}(3-pyridyl))-Ν-[(2·{[(third Oxy)carbonylamino]methyl}(3_cyclopyridinyl))indenyl]carbenamide (6-((3R)-3-hydroxypyridinyl)_5_fluoro_2][2_(3 _Fluorophenyl)ethyl]amino}(3-pyridyl))-Ν_{[2·(aminomethyl)(3_pyridyl)]decyl}carbamamine (6-(1-B) Sulfhydryl (4-1,2,5,6-tetrahydropyridylfluorophenyl)ethyl]amino} (3_σ ratio), specifically (3 比 咬 methyl) carbamide (2- {|&gt;(3-Fluorophenyl)ethyl]amine-based 卜卜又 认 氲^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^^ -{[2-(3-fluorophenyl)ethyl]aminobibupyridinyl)amine oxime]-2-acridinyl)-1,2,5,6-tetrapyridyl carboxylic acid Third butyl ester (6-ί-pentyl-2-{[2-(3-fluorophenyl)ethyl]amino} (3_acridinyl))_n_(3_ σ ratio Ketylmethyl)carhamamine (6-(1,4-dioxaspiro[4 5]indole-7-ene-8-yl)_2_{[2_(3-fluorophenyl)ethyl]amine (3"-pyridyl) benzyl (3_π-pyridylmethyl) decylamine (6 {[2 (3 fluoro) yl)ethyl)aminopyrbidine methyl)amine ]_2_ 唆 唆 ))-ΐ, 2,5,6-tetrahydro π ratio methyl phthalate (6-pent-1-enyl 2 -{[2-(3-fluorophenyl)ethyl) Amino}(3_ σ-pyridyl))-Ν-(3-pyridylfluorenyl)carbamamine N-{(lR)-2_[(5_fluoro_2_{[2♦fluorophenyl)B Aminobutyryl 6-pyrrolidinyl (3-hydroxypyrimidinyl))alkylamino]-isopropylbut-2-[(tatabutoxy)alkylamino]acetic acid amine (2-{ [2-(3_Gasyl)ethyl]amino}_6-(4-oxocyclohexyl) (&gt; 167 200823188 pyridine))-N-(3-acridinyl) Methylamine: (6-((3R)-3-fluoropyridinyl)-_5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}(3- Acridineyl))-N-[(2-{[(Tertidinoxy)carbonylamino]methyl}(3-acridinyl))methyl]decylamine 5 (6-lymphoterol-2 -{[2-(3- disordered phenyl)ethyl]amino}(3-decyl))-indole-(3-acridinylfluorenyl)carhamamine (6-leaf-1-pyrene) Base-2-{[2-(3-phenylphenyl)ethyl] Amino}(3-° ratio σ-based))_Ν-(3-acridinylmethyl)carbamamine N-[((2R)-l-{3-[(t-butoxy)carbonylamino] Propyl 5-oxopurine ίο ϋ -2--2-yl)methyl](5-gas-2-{[2-(3-phenylphenyl)ethyl]amino}-6-117 pir 17-'(3-Acridine)methaneamine (6-[1-(Ν,N-didecylamine fluorenyl)) (4-1,2,5,6-tetrahydroxanthyl) )]-2-{[2-(3-Fluorophenyl)ethyl]amino}(3-acridinyl))-indole-(3·-pyridylhydrazino)carbenamide 15 (5- &gt;Smelly-2-{[2-(3-Phenylphenyl)ethyl]amino} -6-σ ratio thiol (3-indolyl)-indole-(3-acridinyl) Methionine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-indenyl) (4-1,2,5,6-tetrahydropyridinyl) )) (3-Acridine))-Ν-(3-acridinylfluorenyl) decylamine 4-(6-{[2-(3-)-phenyl)ethyl]amino}-5- [!^-(3-1? than 11-decylmethyl)amine 曱20 mercapto]-2-pyridinyl)-1,4,5,6-tetramethylenepyridinium carboxylate (2-{ [2-(3-Fluorophenyl)ethyl]amino} _6-(2- miso-2-yl)(3-indolyl)-N-(3-atbσ-decylmethyl)曱Indoleamine N-{[(2R)-l-(4-aminobutylidene)-pyridin-2-yl]methyl}(5-fluoro-2-{[2-(3-) Ethyl]amino}-6_ntb sigma-based (3-indole σ-based group)) 760 5 15 200823188 Amine n (2^i4 tricbutoxy)carbonylamino] butyl awake each bite - 2. 口 啶 基 ))))) 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲 甲Ethyl]amino}_6"bile silky silk)) brewing: f:):1:{,[(t-butoxy)carbonylamino]ethinyl"pyrrolidine-2· Methyl)5Κ_2·ί[2·(3_fluorophenyl)ethyl]aminepyridinyl))carbenamide 1 fluorenyl)(3,yl)]fluorenyl}(5_fluoro_2 -{[2-(3-Fluorophenyl)ethyl]I-aryl}-6-pyrrolidinyl (3-pyridyl))carbenamide t[((2Rh is more than adenyl-2-yl)methyl (5_Fluoro-2_{[2_(3_fluorophenyl)ethyl]amino}-6-pyrrolidinyl (3-π-pyridyl)carboxamide (2R)_2_{[〇氟{[ 2-(3-fluorophenyl)ethyl]aminobibupyridinyl (3-pyridyl))carbonylamino]methyl}pyrrolidinecarboxylic acid tert-butyl ester N_{[2-(amino-methyl) (3-pyridyl)]fluorenyl}(6_cyclopropyl_5_fluoro_2-{[2_(3-fluorophenyl)ethyl]amino} (3_π ratio) Amine N_{(1 R)-2-[(5-fluoro-2-{[2-(3_ phenyl)ethyl]amino)b 6-吼 口 定 吼唆 (3-mercapto)) 叛 胺 胺 ] - 2- 2- [ [ [ [ {[2-(3-fluorophenyl)ethyl]amine}}_6_[1_( Mercaptosulfonyl)(4-1,2,5,6-tetrahydroσ-pyridyl)](3-° ratio) II--(3-mercaptopurine) decylamine [4_ (6_{[2-(3-Fluorophenyl)ethyl]aminophenyl 5_[Ν_(3′′ 啶 曱 曱 ))) 曱 20 200823188 醯 ]] (2-oxaridinyl)) piperene] -N,N-dimethylformamide 4-(6-{[2-(3-fluorophenyl)-ethyl]amino}-5-[N-(3-mouth ratio dimethyl) Aminomethyl]-2-u-pyridyl) piperidinyl carboxylic acid oxime ester (6-(3-Amino 0-pyrene 11-denyl)·2_{[2-(3-fluorophenyl)ethyl]amine Base}(3_σ than bite 5 base))-Ν-(3-pyridylmethyl)decylamine (2-{[2-(3-fluorophenyl)ethyl)amino}-6-line- 4-yl (3_π ratio), -Ν-(3^pyridylmethyl)guanamine (6-[(2R)-2-(hydroxyindenyl))pyridinyl]_2-{[ 2_(3_fluorophenyl)ethyl]amino}(3_0 ratio), -Ν-(3-σ ratio dimethyl group) 〇 〇 〇 2-[(6-((33)_3-咬{{2-(3-Fluorophenyl)ethyl]amino}(3-pyridyl))carbonylamino]]-N-methylacetamide 2-[ (2-{[2-(3-fluorophenyl)ethyl]aminophenyl 6-(4 _基基旅n定基)(3_σ ratio bite base))carbonylamino]-Ν-mercaptoacetamide (t-butoxy)-Ν-[1·(6-{[2-(3-fluoro Phenyl)ethyl]amino}-5_[ν_(3_5 acridinylmethyl)aminecarboxylidene](2-pyridyl)pyrrolidinyl-3-yl]cartoamine (6-[(3R) -3_(didecylamino) D is more than pyridyl]_2_{[2_(3_ phenyl)ethyl] 女女基}(3-ϋ比基基))_Ν-(3-ϋ ratio Bite-based thiol amine 2-[(H(3S)_3-fluoropyridinyl)-2-{[2_(3-fluorophenyl)ethyl]amino} (3_ ° than bite base) )carbonylamino]_N_mercaptoacetamide 3 2-[(6-((3R)-glycol-hydroxypyridinyl)_2_ {[2_(3-fluorophenyl)ethyl]amino} (3, Pyridyl))carbonylamino]-N-methylacetamide fluorophenyl)ethyl]amino}_5_[N-(3"pyridylhydrazino)amine-based]2-pyridyl)indole Loridin-3-yl]acetic acid (2_{[2-(3.fluorophenyl)ethyl]amino}-6-(3-(4-indolyl)π ratio slightly biting 170 200823188 base) (3 -pyridyl))-沁(3_pyridylmethyl)decylamine 2 repair (3,3:: digasline filaments &gt;2·ί[2·(3-fluorophenyl)ethyl]amine }(3-° than bite base)) 3⁄4 胺 胺 ] 甲基 甲基 甲基 { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { { _ _ _ _ Phenyl) Amino}-6-pyrrolidinyl(3-pyridyl))carbenamide (2-{[2-(3-fluorophenyl)ethyl]amino}_6_[3_(trifluoromethyl)anthracepin (pyridyl)(3·pyridyl))-indole-(3-pyridylfluorenyl)carbenamide (6-(3,3-difluorot each)>_2_{[2_(3_gasphenyl) Ethyl]amino"pyridyl))-indole-(3-pyridylmethyl)carbamamine 10 Ν-{[6-(aminomethyl)(2_吼 基 methyl)} (2_{ [2_(3_Fluorophenyl)ethyl]amino}-6-pyro-based (3-n ratio bite base)) mercaptoamine (H(3S)-3- via 吼 吼 ))_2_{ [2-(3-fluorophenyl)ethyl]amine-based n-pyridyl))-Ν-{[6-(aminomethyl)(2_t-decyl)]decyl}nonylamine 15 (6-( (3R)-Lingji scale bite base)_2_{[2_(3_fluorophenyl)ethyl]amine cardinyl))-N-{[6-(aminomethyl)(2_pyridyl) )]methyl(tetra)(10)-3·fluorine filament)_2_{[2_(3_fluorophenyl)ethyl]amino}-pyridyl))-indole (3_pyridylfluorenyl) decylamine (H4) -(aminoindenyl)pyridinyl]-2·{[2_(3_d-phenyl)ethyl]amino}(3 &quot;pyridyl))-N-(3-pyridylfluorenyl) Indoleamine 20 2-[〇{|&gt;〇fluorophenyl)ethyl]amino}_6«yl (3_吼口定))alkylamino]-N-mercaptoacetamide &amp; ( 2·{[2·(3-fluorobenzene) Ethylamino}-6q3_(fluorenylsulfonyl)^pyrrolidyl]phosphonium))·Ν-(3-pyridylfluorenyl)carbenamide (6-[(2S)-2-) (曱oxymethyl) fluorenyl]_2_{[2_(3_-phenylphenyl)ethyl] 171 200823188 Amino}(3-pyridyl))-N-(3-pyridylfluorenyl)fluorene Amine (second butoxy)_Ν-{.[1-(6-_{[2-(3-fluorophenyl)ethyl]amine.yl}-5-[N-(3-acridinyl) Aminomethyl](2-acridinyl))(4-piperidinyl)]methyl}decylamine 5 (di-butyl)-indole-[1-(6-{[2- (3-Phenylphenyl)ethyl]amino}-5-[N-(3-pyridylfluorenyl)aminecarbinyl](2-pyridyl))(4-piperidinyl)]decylamine (2-{[2-(3-Fluorophenyl)ethyl]aminobi 6-(4-hydroxy-4-phenylpiperidinyl)(3-acridinyl))-N-(3-pyridine Carbenyl)carbamide 1-(6-{[2-(3-fluorophenyl)ethyl]amino}}-5-[1^-(3_11 than dimethylmethyl)amine 曱10 fluorenyl] Ethyl-2-pyridyl)piperidine-4-carboxylate* (6-((3S)-3-fluoropyridinyl)-2-{[2-(3-fluorophenyl)ethyl]amine (N-(3-pyridyl) decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-[4 -(N-nonylaminoindolyl)piperidinyl](3-acridinyl))-N-(3-acridinylfluorenyl) ) indoleamine 15 (2-{[2-(3-phenylphenyl)ethyl]amino}-6-(4-yl-based brittle base) (3-11 ratio). Basement))_Ν_(3-π-pyridylmethyl)decylamine (2-{[2-(3-phenylphenyl)ethyl)amino}-6- 11 bottom 12 well base (3-吼σ Basement))-Ν-(3-Acridinemethyl)guanamine (6-((3S)-3-hydroxypiperidinyl)-2-{[2-(3-fluorophenyl)ethyl] Amino}(3-port ratio 2 aridinyl))-N-(3-acridinylfluorenyl) decylamine N-[l-(6-{[2-(3-fluorophenyl)ethyl) Amino}_5-[Ν-(3-σΛϋ定基曱基)aminemethanyl]-2^pyridylpyrrolidin-3-yl]acetamidamine (2- {[2-(3-fluoro) Phenyl)ethyl]amino}-6-[2-(hydroxyindenyl)morpholin-4-yl](3-acridinyl))-N-(3-acridinylfluorenyl) decylamine 172 200823188 (6_[(3S)_3_(Methylamino)oxaridinyl]-2_{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl)_N-(3 _Pyridylmethyl)carbamamine (2-{[2-(3_鼠phenyl)ethyl)amino)jj-d^thiazaperhydroir^·)) (3_0比°疋基))-Team (3-〇 Methylamine (6-(1,1-dioxy(i,4_thiazaperliydroin_4_*))-2·{[2-(3-fluorophenyl)ethyl]amino}(3- Bite base))-Ν-(3·σΛσ定基基基)carbamamine (6-(4-ethinylpipedyl)_2-{[2-(3-fluorophenyl)ethyl]amine }(3_0 pyridine group))-N -(3-pyridylfluorenyl)carzamide (2-{[2-(3-fluorophenyl)ethyl]amino)- 6-(4·^chenchenyl. Chentidine) (3-π Ratio to cr))-N-(3-pyridylfluorenyl)guanamine and 4·(6-{[2-(3-fluorophenyl)ethyl]amino}-5-[N_(3- Ai:b octadecyl)amine oleyl]-2-pyridyl) piperidine carboxylic acid ethyl ester. The present invention provides at least one chemical selected from the group consisting of a compound of formula VII and a pharmaceutically acceptable salt thereof.

式VII 其中 R1及R4係獨立地選自氫、氰基、鹵基、羥基、疊氮 基、確基、續醯基、亞續酿基、硫烧基、視需要經取代之 燒氧基、視需要經取代之醯氧基、視需要經取代之胺基羰 基氧基、視需要經取代之芳基氧基、視需要經取代之雜芳 173 200823188 基氧基、《要經取代之雜環絲氧基、視 烷氧基羰基、視需要經取代之烷基、視需代:: ί 、視需要經取代之芳基氧基、視 要經取代之雜芳基、視需要經取 代之雜祕基、視S魏取狀絲、視需趣取代之酿 基、視需要經取代之胺基羰基及視需要經取代之 carbaminodoyl ； 10 15 Z1係選自氫、氰基、視需要經取代之烷基、視需要經 取代之醯基、視需要經取代之烷氧基羰基、視需要經取= 之胺基、視需要經取代之胺基羰基、視需要經取代之甲胨 基、視需要經取代之烷氧基、視需要經取代之芳基氧基、 視需要經取代之雜芳基氧基、視需要經取代之雜環烷^氧 基、視需要經取代之烯基、視需要經取代之炔基、磺酿1、 亞磺醯基及硫烷基； Z2係選自氫、視需要經取代之甲脒基、羧基、視需要 經取代之院氧基幾基、視需要經取代之醯基、視需要經取 代之烯基、視需要經取代之烧基、視需要經取代之雜環烧 基、視需要經取代之雜芳基及視需要經取代之胺基羰基； Z3係選自視需要經取代之烷基；及 R係每自鼠及視需要經取代之烧基。 在式VII化合物之特定實施例中，z2係選自羧基、視需 要經取代之烧氧基幾基、視需要經取代之醯基、視需要經 取代之烯基及視需要經取代之烷基。 在式VII化合物之特定實施例中，Z2係選自羧基、視 174 20 200823188 需要經取代之哌啶基羰基、視需要經取代之吡u定基幾基、 -視需要經取代之低碳烷基·、視需要經取代之低嚷稀基及低 碳烷氧基羰基。 在式VII化合物之特定實施例中，Z2係選自（2_(队乙醯 5 基胺基甲基)哌啶-1-基)幾基；(2-胺基甲基哌啶七基)幾基； 1-羥基-2-胺基-乙基；2-((甲基磺醯胺基）曱基)哌咬基幾 基；2-(甲基胺基幾基）乙稀基；2-(吼咬-3-基甲基)_2H_三唾 -5-基曱基，胺基曱基；叛基；甲氧基幾基；u比咬_2_基罗炭 基，0比咬-3-基綠基，及吼咬-4-基幾基。 10 在式VII化合物之特定實施例中，R3係選自氫及視需 • 要經取代之低碳烧基。在特定實施例中，R3係選自氳及低 碳烧基。在式VII化合物之特定實施例中，R3係選自氫及 甲基。在式VII化合物之特定實施例中，R3為氫。 在式VII化合物之特定實施例中，R4係選自氫、氰基、 15 _基、疊氮基、視需要經取代之胺基羰基及視需要經取代 之烷基。在式VII化合物之特定實施例中，R4係選自氫、 氰基、氯、溴、氟、疊氮基、視需要經取代之烷基胺基羰 基及視需要經取代之甲基。在式VII化合物之特定實施例 中，R4係選自氳、氰基、氯、溴、疊氮基、吼啶-3-基甲基 20 胺基羰基、胺基曱基及羥基曱基。在式VII化合物之特定 實施例中，R4為氫。 在式VII化合物之特定實施例中，R5係選自氫及低碳 烷基。在式VII化合物之特定實施例中，R5係選自氫及曱 基。在式VII化合物之特定實施例中，R5為氫。 175 200823188 在式vn化合物之特定實施例中，Z2為-C(0)-NR2R5， - 其中R2係選自視需要經取代之烷基及視需要經取代之環 烷基；而R5係選自氫及視需要經取代之烷基。 在式VII化合物之特定實施例中，R2係選自視需要經 5 取代之甲基、視需要經取代之乙基、視需要經取代之丙 基、視需要經取代之丁基、視需要經取代之戊基、視需要 經取代之己基、視需要經取代之環丙基、視需要經取代之 環戊基及視需要經取代之環己基，其中各視需要經取代之 基團係視需要經一、二或三個由下列選出之基團取代··視 10 需要經取代之芳基、視需要經取代之雜芳基、視需要經取 ' 代之雜環炫基、視需要經取代之環烧基、視需要經取代之 胺基羰基、視需要經取代之胺基、羥基、羧基、視需要經 取代之烷氧基羰基及視需要經取代之烷氧基。 在式VII化合物之特定實施例中，R2係選自甲基及乙 15 基，其中甲基及乙基基團係視需要經經一或二個由下列選 出之基團取代：視需要經取代之芳基、視需要經取代之雜 芳基、視需要經取代之雜環烷基、視需要經取代之環烷 基、視需要經取代之胺基羰基、視需要經取代之胺基、羥 基、羧基、視需要經取代之烷氧基羰基及視需要經取代之 20 烧氧基。 在式VII化合物之特定實施例中，R2係選自（1-(2-胺基乙 基)-lH-u比唑-3-基）甲基；（1-(甲基磺醯基)哌啶_3-基）甲基； (1-乙酿基娘唆-3-基）甲基；（1-乙酿基吼洛唆-2-基）甲基； (1H-咪唑-2-基）甲基；（111-吼唑-3_基）甲基；士甲基-1H- 176 200823188 吡唑-3-基）曱基；（1_甲基-1H-吡唑_5_基）曱基；（2-(胺基羰 •基）乙基胺基）幾基甲基；（2-(胺基甲基）π比T2定-3-基）甲基； (2-(缓基）乙基胺基)幾基甲基；（2_(二曱基胺基）乙基胺基) 羰基曱基；（2-(羥基）乙基胺基)幾基甲基；（2_(甲基胺基) 5 乙基胺基）羰基曱基；（2-(N-曱基(第三丁氧基羰基)-胺 基）乙基胺基)羰基甲基；（2-氧基痕咬-3-基）曱基；（3-(二甲 基胺基）丙基胺基）羰基曱基；（3-(羥基）乙基胺基）羰基曱 基；（3-(第三丁氧基羰基胺基）丙基胺基)羰基甲基；（4_(胺 基曱基)吼啶·2_基）甲基；〇(胺基甲基）π比啶_2_基）曱基； ίο (6-((1，3-二氧基異ϋ引噪琳-2-基）甲基）π比咬_2_基）曱基； (6-(2_胺基乙基胺基)吼啶-2-基）甲基；（6-(3-胺基丙基胺基） 吼咬-2-基）曱基；（6-(胺基曱基)吼唆-2-基）曱基；（6-(經基 曱基)吼啶_2_基）曱基；（6_漠吡啶_2_基）曱基；（曱基磺醯胺 基）羰基甲基；（σ比啶-2-基）乙基胺基；1-(2-(第三丁氧基羰 15 基胺基）乙基)_1H-吡唑-3-基曱基；1-(2-(第三丁氧基羰基胺 基）乙基)_1H-吡唑冬基曱基；ι_(胺基羰基&gt;2_(胺基)_乙小 基；1-(胺基幾基)_3_(胺基)-丙基；1_(胺基幾基)_4_(胺基)_ 丁基；Η胺基羰基)|(苯曱基氧基羰基胺基)_戊基；h(胺 基羰基）-5-(胺基）-戊基；1_(胺基羰基）乙基；ι_(羧 20 基)-2_(胺基&gt; 乙-1—基；1_(二曱基胺基羰基)-2-(胺基)-乙-1- 基；1-(羧基)_2_(胺基羰基甲基胺基）乙小基；1-(經基)_2_(乙 氧基羰基曱基胺基）乙-1-基；1_(羥基)_2_(π比啶_2_基曱基胺 基）乙-1-基；1-(曱氧基羰基)_2_(胺基)_乙_1_基；}_(曱氧基 羰基)-2-(第三丁氧基羰基胺基&gt;乙_；^基；丨_(曱氧基羰基) 177 200823188 乙-1-基，1-(甲基胺基綠基)-2-(胺基)-乙-1-基(2 occ)，1-(曱 基胺基羰基）乙-1-基；胺基羰基-2-羥基-乙小基；1-甲氧 基援基-2-經基-乙-1 -基，2-(2-胺基乙氧i基）乙基，2-(2-胺基 乙基定-6-基曱基，2·(2-胺基乙基胺基）乙基，2-(3-氣 5 苯基）乙基，2-(3-曱氧基域基）乙基，2-(6-(胺基甲基比咬 -2-基）乙基；2-(乙醯基胺基）乙基；2-(胺基）乙基；2-(胺基 綠基)-2-(乙酸基胺基)-乙-1-基，2-(胺基_炭基)-2-(胺基)-乙 -1-基，2-(胺基搂基）乙基，2-(胺基曱基）ϋ比σ定-5-基甲基， 2-(竣基)-2-(胺基)_乙-1-基，2-(二甲基胺基）乙基，2-(二甲 1〇 基胺基域基)-2-(胺基)-乙-1 -基，2-(乙乳基緣基）乙基，2-(曱 乳基綠基)-2-(乙酿基胺基)-乙-1-基，2-(甲氧基魏基)-2-(胺 基)-乙-1-基，2-(曱氧基綠基胺基）乙基，2-(曱基胺基）乙基； 2-(甲基胺基_炭基)-2-(乙驢基胺基)-乙-1-基，2-(曱基胺基祿 基)-2-(胺基)-乙-1-基，2-(甲基石黃酸胺基）乙基，2-(甲乳基 15 缓基)-2-(胺基)-乙-1 -基，2-(N-(第二丁氧基域基)-N-(曱基)_ 胺基）乙基，2-(旅12井-1-基）乙基，2-(ϋ比0井-2-基）乙基，2-(ϋ比 啶-2-基）乙基；2十比啶-3-基）乙基；2-(第三丁氧基羰基胺 基甲基)吼ϋ定-3-基曱基，2-(第二丁乳基搂基胺基曱基)°比。定 -6-基曱基；2-(三氟曱基)-吡啶-6-基曱基；2-胺基吡啶-3-2〇 基曱基；2-胺基吡啶-5-基曱基；2-氯吡啶-5·基甲基；2- 氣基吼^定-5-基甲基，2-輕基-3-胺基-丙-1-基，2-經基乙基； 2-曱氧基乙-1-基；2-曱氧基吼啶-3-基曱基；2-曱氧基啦啶 -5-基曱基；2-曱基吼啶-3-基曱基；2-曱基吼啶-5-基曱基； 2_曱基吼啶-6-基甲基；3-(2-胺基乙基)環己基）甲基；3-(4- 178 200823188 甲基哌畊-1-基）丙基；3-(胺基)-3_(甲基胺基羰基）丙-；[-基； 3-(胺基羰基）丙基；3-(胺基曱基)苯曱基；3-(胺基曱基)吡 啶-2-基曱基；3-(曱氧基羰基）丙基；3-(曱基胺基羰基）丙 基；3-(三氟甲基)-吡啶-2-基曱基；3,4-二氟苯甲基；3-胺 5 基甲基吡啶-4-基曱基；3-胺基丙基；3-胺曱醯基環戊基； 3-羧基丙基；3-羥基丙基；3-甲氧基丙基；4-(胺基曱基)-吡啶-2-基甲基；4-(N，N-二甲基胺基)吡啶-3-基甲基；4-(第 三丁氧基羰基胺基)-嗎琳基甲基；4-胺基丁基；4-胺基甲 基吼啶-3-基曱基；4-氰基苯甲基；4-氟苯曱基；4-甲基胺 ίο 基σ比咬基曱基；4-甲基苯曱基；4-嗎淋基^比唆-3_基甲基； • 4-哌畊基。比啶-3-基甲基；5-((雙（二甲基胺基）甲基胺基）甲 基）咐啶-3-基曱基；5-(胺基曱基)吼啶-2-基曱基；5-(胺基 曱基）吼啶_3_基曱基；5-(羥基甲基)吼啶-3-基曱基；5-(第 三丁氧基羰基胺基甲基)-吼啶-2-基曱基；5-(三氟甲基比 15 啶-2-基曱基；5-胺基戊基；5-胺基吼啶-2-基甲基；6-((雙(二 曱基胺基)伸甲基胺基）曱基)吼啶-2-基）甲基；6-(4-乙醯基 哌畊-1-基;Kb啶-3-基甲基）；6-(胺基甲基户比啶-2-基）曱基； 6-胺基己基；胺基羰基曱基；苯曱基；環丙基曱基；二曱 基胺基羰基甲基；異丙基；異崎唑-5-基曱基；曱氧基羰基 2〇 曱基；甲基；甲基胺基羰基曱基；噚唑-2-基甲基；哌啶-4- 基甲基；丙-2-烯-1-基；吡畊-2-基曱基；吡啶-2-基甲基； 吡啶-2-基甲基-N-氧化物；吡啶-3-基曱基；吡啶-3-基曱基 -N-氧化物；吡啶-4-基甲基；噻吩-2-基曱基；及噻吩-3-基甲基。 179 200823188 在式VII化合物之特定實施例中，Z3係選自視需要經 .取代之低碳烷基。 _ _ 在式VII化合物之特定實施例中，Z3係選自視需要經 取代之曱基、視需要經取代之乙基及視需要經取代之丙 5 基，其中曱基、乙基及丙基基團係視需要經一或二個由下 列選出之基團取代：羥基、視需要經取代之芳基、視需要 經取代之雜芳基、視需要經取代之雜環烷基、視需要經取 代之環烷基及視需要經取代之芳基氧基。 在式VII化合物之特定實施例中，Z3係選自2-(3-曱基 10 苯基）乙基、（四氫呋喃2-基）曱基、1-羥基環己基曱基、 • 2-(1，3-二氧戊環-2-基）乙基、2-(1Η-咪唑-4-基）乙基、2-(1- 曱基-1H-咪唑-4-基）乙基、2-(1-曱基哌啶-4-基）乙基、2-(2,3-二氟苯基）乙基、2-(2,5-二氟苯基）乙基、2-(2,6-二氟苯基) 乙基、2-(2-氣苯基）乙基、2-(2-氮基苯基）乙基、2-(2-鼠苯 15 基）乙基、2-(2-羥基苯基）乙基、2-(2-曱氧基苯基）乙基、2-(2- 曱基苯基）乙基、2-(2-氧基味17坐ϋ定-1-基）乙基、2-(2-氧基旅 啶-1-基）乙基、2-(2-氧基吼咯啶-1-基）乙基、2_(3·(三氟曱 基）苯基）乙基、2-(3,4-二氟苯基）乙基、2-(3,5-二氟苯基）乙 基、2-(3,5·二曱基-1Η-吡唑-1-基）乙基、2-(3,5-二曱基-1Η-2〇 吼唑-4-基）乙基、2_(3_胺曱醯基苯基）乙基、2-(3-羧基苯基) 乙基、2-(3-鼠基苯基）乙基、2-(3-氣苯基)-2-(經基)-乙基、 2-(3-氟苯基）乙基、2-(3-氟吼啶-2-基）乙基、2-(3-曱氧基羰 基苯基）乙基、2-(3-甲氧基苯基）乙基、2-(3-曱基苯基）乙 基、2-(4-胺基苯基）乙基、2-(4-氣苯基）乙基、2-(4-氣苯基) 180 200823188 乙基、2-(4-羥基苯基）乙基、2-(苯并[d][l，3]間二氧雜戊烯 基）乙基、2_(吱鳴2_基）乙基、2_(經基)_2_(苯基）乙基、 2-(苯基）乙基、2十比°定·2_基）乙基、2十比咬各基）乙基、2_(嗟 吩-2-基）乙基、2-環己-1-烯基乙基、2-環己基乙基、厶嗎琳 基乙基、本氧基乙基、2-苯基丙小基、3-(1Η-味唾_ι_笑) 丙-1-基、3-苯基丙基、苯曱基、氣、異戊基、丙基、^比啶 -2-基曱基、ϋ比啶-3-基曱基及噻吩-3-基曱基。 在式vii化合物之特定實施例中，ζ3係選自2_(3•氟 苯基）乙基及2-(吡啶-2-基）乙基。 在式VII化合物之特定實施例中，ζι係選自氰基、鹵 基、視需要經取代之醯基、視需要經取代之烯基、視需要 經取代之烷氧基羰基、視需要經取代之烷基、視需要經取 代之胺基、視需要經取代之胺基羰基及視需要經取代之甲 肺基。 在式νπ化合物之特定實施例中，Z1係選自醯基、烯 基、烷氧基羰基、烷基、胺基、胺基羰基及曱脒基，其中 ，基團係視需要經-、二或三個由下列選出之基團取代： 氰基、鹵基、羥基、甲醯基、視需要經取代之烷基、視需 要經取代之烯基、視需要經取代之烧氧基、減、視需要 經取代之烧氧基縣、視需要經取代之醯基、視需要經取 代之f基羰基、視需要經取代之雜環絲、視需要經取代 ^雜方基、視需要經取代之f職及視需要經取代之石黃酿 基。 在式Vn化合物之特定實施例中，Z1係選自（5-氧基- 181 200823188 四氫呋喃2-基）甲基胺基；（E)-N’-氰基-N，N-二甲基甲脒 基；（Ζ)-4·(Ν-(2-羥基_乙基)-N，N’-雙（曱氧基羰基).甲肺基); (Z)-丁-2-細-2-基，1-乙乳基乙-1-基，1-乙乳基乙細基， 羥基乙-1-基胺基2-曱氧基乙-1-基胺基；2-甲基丙-1-烯 5 基，3-(曱氧基綠基)-丙-2-細-2-基，3-(N，N-二曱基胺基)幾 基-丙-1 -基胺基，3 -胺基域基-丙-1 -基胺基，3 -經基丙-1 _ 基胺基，3 -曱乳基-丙-1 -細基，3 -曱氧!基丙-1 -基胺基，3 _ 曱乳基丙基，3 -甲基丁 -2-炸-2-基，4-((atbϋ定-3-基曱基）胺 基羰基）丁基胺基；4-(Ν，Ν-二曱基胺基）羰基-丁-1-基胺 10 基；4-(Ν-甲基胺基）羰基-丁-1-基胺基；4-胺基羰基-丁-1- • 基胺基；乙醯基；胺基羰基；曱脒基；氯；氰基；二甲基 、 胺基；乙氧基羰基；氫；曱氧基羰基；甲基胺基；Ν-(2- 羥基乙基)-Ν-(乙醯基)-胺基；Ν-(2-羥基乙基)-Ν-(甲基)-胺 基；Ν-(2-羥基丙-1-基:)-Ν-(曱基)-胺基；Ν-(曱基)-胺基羰 15 基；Ν-(吼啶-2-基甲基）胺基；Ν-(吼啶-3-基甲基）胺基； Ν-(吼啶-4-基曱基)胺基；Ν，Ν-二曱基曱脒基；Ν-氰基甲脒 基；Ν-甲基-Ν-乙醯基胺基；及丙-1-烯基。 在式VII化合物之特定實施例中，R1係選自氫及視需 要經取代之低碳烷基。在式VII化合物之特定實施例中， 2〇 R1係選自氫及低碳烷基。在式VII化合物之特定實施例 中，R1係選自氫及曱基。在式VII化合物之特定實施例 中，R1係選自氫。 在特定實施例中，式VII化合物係選自 Ν-{[6-(胺基甲基)(2^比啶基)]曱基}(2-{[2-(3-氟苯基）乙基] 182 200823188 胺基卜5-(3-吡啶基)(3-吡啶基)）甲醯胺 n-{[6_(胺基甲基)(2_吡啶基)]甲基}(2_{[2_(3_氟苯基）乙基] 胺基比啶基)(3_π比啶基)）甲醯胺 Ν-{[6-(胺基甲基比啶基)]甲基}(2_{[2_(3_氟苯基）乙基] 5 胺基卜5〆1-甲基吡唑-4-基)(3-吡啶基)）甲醯胺 N-{[6-(胺基甲基）(2_ σ比啶基）]甲基}(5_(2_氰基苯 基)-2-([2-(3-氟本基）乙基]胺基比咬基)）甲酿胺 (5-氰基-2-{[2-(3-氟苯基）乙基]胺基}(3_0比啶基 啶基甲基)曱醯胺 10 (5_溴_2_{[2_(3_氟苯基）乙基]胺基}(3』比啶基))-Ν_[(6_甲基 (2-吡啶基)）甲基]甲醯胺 土 (5-溴-6-氯-2-{[2-(3-氟苯基）乙基]胺基}(3_η比啶基)&gt;ν_(2_ 吡啶基甲基）甲醯胺 5·漠-2-{[2_(3-氟苯基）乙基]胺基}吡啶j遗酸 15 $氧基鼠本基）乙基]胺基}σ比唆-3-魏g复甲酷Wherein R 1 and R 4 are independently selected from the group consisting of hydrogen, cyano, halo, hydroxy, azido, thio, decyl, sulfenyl, thiol, optionally substituted alkoxy, An optionally substituted methoxy group, optionally substituted aminocarbonyloxy group, optionally substituted aryloxy group, optionally substituted heteroaryl 173 200823188 oxy group, "heterocyclic ring to be substituted" Alkyloxy, retinyloxycarbonyl, optionally substituted alkyl, as needed: ί, optionally substituted aryloxy, heteroaryl which is optionally substituted, optionally substituted The secret base, the S-we take the silk, replace the brewing base as needed, replace the aminocarbonyl as needed and replace the carbaminodoyl as needed; 10 15 Z1 is selected from hydrogen, cyano, and optionally substituted An alkyl group, optionally substituted fluorenyl group, optionally substituted alkoxycarbonyl group, optionally substituted amine group, optionally substituted aminocarbonyl group, optionally substituted formazan group, optionally substituted Substituted alkoxy, optionally substituted aryloxy, optionally substituted heteroaryloxy a substituted heterocycloalkyloxy group, optionally substituted alkenyl group, optionally substituted alkynyl group, sulfonate 1, sulfinyl group and sulfanyl group; Z2 is selected from hydrogen, as needed Substituted mercapto group, carboxyl group, optionally substituted alkoxy group, optionally substituted fluorenyl group, optionally substituted alkenyl group, optionally substituted alkyl group, optionally substituted a cycloalkyl group, optionally substituted heteroaryl group, and optionally substituted aminocarbonyl group; Z3 is selected from an alkyl group optionally substituted; and R is an alkyl group which is substituted from the mouse and optionally substituted. In a particular embodiment of the compound of formula VII, z2 is selected from the group consisting of a carboxy group, an optionally substituted alkoxy group, an optionally substituted thiol group, an optionally substituted alkenyl group, and an optionally substituted alkyl group. . In a particular embodiment of the compound of formula VII, Z2 is selected from the group consisting of carboxy, 174 20 200823188, substituted piperidinylcarbonyl, optionally substituted pyridyl, - optionally substituted lower alkyl · A low sulfhydryl group and a lower alkoxycarbonyl group which are substituted as needed. In a particular embodiment of the compound of formula VII, the Z2 is selected from the group consisting of (2_(Tetraethylene-5-aminomethyl)piperidin-1-yl); (2-aminomethylpiperidineheptyl) 1-hydroxy-2-amino-ethyl; 2-((methylsulfonylamino)indolyl)piperidinyl; 2-(methylaminomethyl)ethenyl; 2- (吼 bit-3-ylmethyl)_2H_tris-7-ylindenyl, amine fluorenyl; thiol; methoxy group; u ratio bite _2 _ carbocarb, 0 bite - 3-based green group, and bite-4-yl group. In a particular embodiment of the compound of formula VII, R3 is selected from the group consisting of hydrogen and, if desired, a low carbon alkyl group to be substituted. In a particular embodiment, R3 is selected from the group consisting of hydrazine and a low carbon alkyl group. In a particular embodiment of the compound of formula VII, R3 is selected from the group consisting of hydrogen and methyl. In a particular embodiment of the compound of formula VII, R3 is hydrogen. In a particular embodiment of the compound of formula VII, R4 is selected from the group consisting of hydrogen, cyano, 15-yl, azide, optionally substituted aminocarbonyl, and optionally substituted alkyl. In a particular embodiment of the compound of formula VII, R4 is selected from the group consisting of hydrogen, cyano, chloro, bromo, fluoro, azide, optionally substituted alkylaminocarbonyl and optionally substituted methyl. In a particular embodiment of the compound of formula VII, R4 is selected from the group consisting of hydrazine, cyano, chloro, bromo, azido, acridine-3-ylmethyl 20 aminocarbonyl, amine fluorenyl and hydroxy fluorenyl. In a particular embodiment of the compound of formula VII, R4 is hydrogen. In a particular embodiment of the compound of formula VII, R5 is selected from the group consisting of hydrogen and lower alkyl. In a particular embodiment of the compound of formula VII, R5 is selected from the group consisting of hydrogen and sulfhydryl. In a particular embodiment of the compound of formula VII, R5 is hydrogen. 175 200823188 In a particular embodiment of the compound of formula vn, Z2 is -C(0)-NR2R5, wherein R2 is selected from alkyl optionally substituted alkyl and optionally substituted cycloalkyl; and R5 is selected from Hydrogen and optionally substituted alkyl. In a particular embodiment of the compound of formula VII, R2 is selected from the group consisting of optionally substituted methyl, optionally substituted ethyl, optionally substituted propyl, optionally substituted butyl, optionally Substituted pentyl group, optionally substituted hexyl group, optionally substituted cyclopropyl group, optionally substituted cyclopentyl group and optionally substituted cyclohexyl group, wherein each of the optionally substituted groups is optionally required Substituted by one, two or three groups selected from the following: 10 depending on the desired aryl group, optionally substituted heteroaryl group, if desired, substituted heterocyclic thiol, optionally substituted a cycloalkyl group, an optionally substituted aminocarbonyl group, an optionally substituted amino group, a hydroxyl group, a carboxyl group, an optionally substituted alkoxycarbonyl group, and an optionally substituted alkoxy group. In a particular embodiment of the compound of formula VII, R2 is selected from the group consisting of methyl and ethyl, wherein the methyl and ethyl groups are optionally substituted with one or two groups selected from the group consisting of: Aryl group, optionally substituted heteroaryl group, optionally substituted heterocycloalkyl group, optionally substituted cycloalkyl group, optionally substituted aminocarbonyl group, optionally substituted amine group, hydroxyl group Carboxylic acid, optionally substituted alkoxycarbonyl and optionally substituted 20 alkoxy groups. In a particular embodiment of the compound of formula VII, R2 is selected from the group consisting of (1-(2-aminoethyl)-lH-u-pyrazol-3-yl)methyl; (1-(methylsulfonyl)pipech (1-Ethyl)-3-yl)methyl; (1-ethenylindolo-2-yl)methyl; (1H-imidazol-2-yl) Methyl; (111-carbazole-3-yl)methyl; s-methyl-1H- 176 200823188 pyrazol-3-yl) fluorenyl; (1-methyl-1H-pyrazole-5-yl) Mercapto; (2-(aminocarbonyl)ethylamino)methylmethyl; (2-(aminomethyl)π ratio T2-3-yl)methyl; (2-(sustained base) Ethylamino)methylidene; (2-(didecylamino)ethylamino)carbonylcarbonyl; (2-(hydroxy)ethylamino)methylidene; (2_(methyl) Amino) 5 ethylamino)carbonylcarbonyl; (2-(N-fluorenyl(t-butoxycarbonyl)-amino)ethylamino)carbonylmethyl; (2-oxygen bite- (3-(dimethylamino)propylamino)carbonylindenyl; (3-(hydroxy)ethylamino)carbonylindenyl; (3-(t-butoxy) Carbonylamino)propylamino)carbonylmethyl; (4-(aminoindenyl)acridin-2-yl)methyl; Methyl)π-pyridyl-2-yl) fluorenyl; ίο (6-((1,3-dioxyisoindole)-) (6-(2-aminoethylamino) acridine-2-yl)methyl; (6-(3-aminopropylamino) guan-2-yl) fluorenyl; (6 -(aminoindenyl)indol-2-yl)indenyl; (6-(transalkyl)acridinyl-2-yl)indenyl; (6-indiyl-2-yl)indenyl; Mercaptosulfonylamino)carbonylmethyl; (σ-pyridin-2-yl)ethylamino; 1-(2-(t-butoxycarbonyl-15-amino)ethyl)_1H-pyrazole- 3-ylindenyl; 1-(2-(t-butoxycarbonylamino)ethyl)_1H-pyrazol-ylindole; i-(aminocarbonyl)&gt;2-(amino)-ethylidene;1-(Aminomethyl)_3_(amino)-propyl; 1-(amino)- 4-(amino)-butyl; decylaminocarbonyl)|(phenylhydrazinooxycarbonylamino)_ Amyl; h(aminocarbonyl)-5-(amino)-pentyl; 1-(aminocarbonyl)ethyl; i-(carboxy 20-yl)-2-(amino)&gt;ethyl-1-yl;Dimercaptoaminocarbonyl]-2-(amino)-eth-1-yl; 1-(carboxy)_2-(aminocarbonylmethylamino)ethyl small group; 1-(radio)_2_(ethoxy Alkylcarbonyl amidino) 1-yl; 1-(hydroxy)_2_(π-pyridin-2-ylhydrazino)ethyl-1-yl; 1-(decyloxycarbonyl)_2-(amino)-ethyl-1-yl; (曱oxycarbonyl)-2-(t-butoxycarbonylamino)&gt;B-;^; 丨-(曱oxycarbonyl) 177 200823188 Ethyl-1-yl, 1-(methylamino green 2-(amino)-eth-1-yl (2 occ), 1-(decylaminocarbonyl)ethyl-1-yl; aminocarbonyl-2-hydroxy-ethyl small group; 1-methyl Oxyl-yl-2-transyl-ethyl-1-yl, 2-(2-aminoethyloxyiyl)ethyl, 2-(2-aminoethylhex-6-ylindenyl, 2· (2-Aminoethylamino)ethyl, 2-(3-cyclopentaphenyl)ethyl, 2-(3-indolyloxy)ethyl, 2-(6-(aminomethyl) Than-2-yl)ethyl; 2-(ethionylamino)ethyl; 2-(amino)ethyl; 2-(amino-chloro)-2-(acetamido)-B -1-yl, 2-(amino-carbyl)-2-(amino)-eth-1-yl, 2-(aminoindenyl)ethyl, 2-(aminoindenyl)pyrene ratio σ 5-aminomethyl, 2-(indenyl)-2-(amino)-eth-1-yl, 2-(dimethylamino)ethyl, 2-(dimethyl 1 decylamino) Domain group)-2-(amino)-ethyl-1-yl, 2-(ethyl lactyl)ethyl, 2-(indoleyl-based)-2-(ethenylamine) )-Ethyl-1-yl, 2-(methoxypropenyl)-2-(amino)-eth-1-yl, 2-(decyloxygreen amino)ethyl, 2-(fluorenyl) Amino)ethyl; 2-(methylamino-carbyl)-2-(ethionylamino)-eth-1-yl, 2-(decylamino)yl-2-(amino) )-Ethyl-1-yl, 2-(methyllithium amide)ethyl, 2-(methyllacyl 15 thio)-2-(amino)-ethyl-1-yl, 2-(N -(Second butoxy-based)-N-(indenyl)-amino)ethyl, 2-(Brigade 12-1-yl)ethyl, 2-(ϋ比0井-2-yl) Ethyl, 2-(indolyl-2-yl)ethyl; 2 decapyridin-3-yl)ethyl; 2-(t-butoxycarbonylaminomethyl)pyridin-3-yl Sulfhydryl, 2-(second butyl-based mercaptoamino group) ratio. -6-ylindenyl; 2-(trifluoromethyl)-pyridin-6-ylindenyl; 2-aminopyridine-3-2indolyl; 2-aminopyridin-5-ylfluorenyl ; 2-chloropyridin-5-ylmethyl; 2-carbyl hydrazino-5-ylmethyl, 2-carbyl-3-amino-propan-1-yl, 2-ylethyl; 2 -nonyloxyethyl-1-yl; 2-nonoxyacridin-3-ylindenyl; 2-nonyloxypyridin-5-ylindenyl; 2-mercaptoacridin-3-ylindolyl ; 2-mercaptoacridin-5-ylindenyl; 2-mercaptoacridin-6-ylmethyl; 3-(2-aminoethyl)cyclohexyl)methyl; 3-(4- 178 200823188 Methylpiped-1-yl)propyl; 3-(amino)-3_(methylaminocarbonyl)propan-;[-yl; 3-(aminocarbonyl)propyl; 3-(amino hydrazine Benzophenyl; 3-(aminomercapto)pyridin-2-ylindenyl; 3-(decyloxycarbonyl)propyl; 3-(decylaminocarbonyl)propyl; 3-(trifluoro Methyl)-pyridin-2-ylindenyl; 3,4-difluorobenzyl; 3-amine5-methylpyridin-4-ylindenyl; 3-aminopropyl; 3-aminoindenyl Cyclopentyl; 3-carboxypropyl; 3-hydroxypropyl; 3-methoxypropyl; 4-(aminomercapto)-pyridin-2-ylmethyl; 4-(N,N-dimethyl Amino)pyridin-3-ylmethyl; 4-(third butoxy Aminomethyl)-morphinylmethyl; 4-aminobutyl; 4-aminomethyl acridine-3-ylindenyl; 4-cyanobenzyl; 4-fluorophenylindenyl; 4- Methylamine ίο σ 比 咬 ; ;; 4-methylphenyl fluorenyl; 4- 淋 基 ^ 唆 唆 _ _ _ _ • • ; Bispin-3-ylmethyl; 5-((bis(dimethylamino)methylamino)methyl)acridin-3-ylindenyl; 5-(aminoindenyl)acridine-2 -ylindenyl; 5-(aminoindenyl)acridine-3-ylhydrazinyl; 5-(hydroxymethyl)acridin-3-ylindenyl; 5-(t-butoxycarbonylaminol) ())-Acridine-2-ylindenyl; 5-(trifluoromethyl to 15-pyridin-2-ylindenyl; 5-aminopentyl; 5-aminoacridin-2-ylmethyl; 6 -((bis(didecylamino)methylamino)indolyl)acridin-2-yl)methyl; 6-(4-ethinylpiperidin-1-yl; Kbpyridine-3- Methyl); 6-(aminomethyl-bipyridin-2-yl)indenyl; 6-aminohexyl; aminocarbonylcarbonyl; phenylhydrazine; cyclopropylhydrazino; dimercaptoamine Carbonylmethyl; isopropyl; isoxazol-5-ylindenyl; oximeoxycarbonyl 2 fluorenyl; methyl; methylaminocarbonylcarbonyl; oxazol-2-ylmethyl; piperidine 4-ylmethyl; prop-2-en-1-yl; pyridin-2-ylindenyl; pyridin-2-ylmethyl; pyridin-2-ylmethyl-N-oxide; pyridin-3- Base group; pyridin-3-ylindenyl-N-oxide; pyridin-4-ylmethyl; thiophen-2-ylindenyl; and thiophen-3-ylmethyl. 179 200823188 In a particular embodiment of the compound of Formula VII, Z3 is selected from the group consisting of a lower alkyl group as desired. _ _ In a particular embodiment of the compound of formula VII, Z3 is selected from the group consisting of an optionally substituted thiol group, an optionally substituted ethyl group, and an optionally substituted propyl group, wherein fluorenyl, ethyl and propyl groups are present. The group is optionally substituted by one or two groups selected from the group consisting of hydroxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, optionally Substituted cycloalkyl and optionally substituted aryloxy. In a particular embodiment of the compound of formula VII, Z3 is selected from the group consisting of 2-(3-indolyl 10 phenyl)ethyl, (tetrahydrofuran-2-yl)indenyl, 1-hydroxycyclohexyldecyl, • 2-(1) , 3-dioxolan-2-yl)ethyl, 2-(1Η-imidazol-4-yl)ethyl, 2-(1-indolyl-1H-imidazol-4-yl)ethyl, 2- (1-mercaptopipridin-4-yl)ethyl, 2-(2,3-difluorophenyl)ethyl, 2-(2,5-difluorophenyl)ethyl, 2-(2, 6-difluorophenyl)ethyl, 2-(2-phenylphenyl)ethyl, 2-(2-nitrophenyl)ethyl, 2-(2-murolylphenyl)ethyl, 2- (2-hydroxyphenyl)ethyl, 2-(2-decyloxyphenyl)ethyl, 2-(2-decylphenyl)ethyl, 2-(2-oxy-flavor 17-sodium 1-yl)ethyl, 2-(2-oxybendidin-1-yl)ethyl, 2-(2-oxyindole-1-yl)ethyl, 2-(3.(trifluorofluorene) Phenyl)ethyl, 2-(3,4-difluorophenyl)ethyl, 2-(3,5-difluorophenyl)ethyl, 2-(3,5·didecyl-1Η -pyrazol-1-yl)ethyl, 2-(3,5-dimercapto-1Η-2oxazol-4-yl)ethyl, 2-(3-aminodecylphenyl)ethyl, 2-(3-carboxyphenyl)ethyl, 2-(3-murophenyl)ethyl, 2-(3-phenylphenyl)-2-(radio)-B , 2-(3-fluorophenyl)ethyl, 2-(3-fluoroacridin-2-yl)ethyl, 2-(3-decyloxycarbonylphenyl)ethyl, 2-(3- Methoxyphenyl)ethyl, 2-(3-indolylphenyl)ethyl, 2-(4-aminophenyl)ethyl, 2-(4-phenylphenyl)ethyl, 2-( 4-Phenylphenyl) 180 200823188 Ethyl, 2-(4-hydroxyphenyl)ethyl, 2-(benzo[d][l,3]dioxopentenyl)ethyl, 2_(吱2_yl)ethyl, 2_(radio)_2_(phenyl)ethyl, 2-(phenyl)ethyl, 2 decyl-2-yl)ethyl, 20 octyl Ethyl, 2_(嗟-phen-2-yl)ethyl, 2-cyclohex-1-enylethyl, 2-cyclohexylethyl, indolyl ethyl, ethoxyethyl, 2-benzene Propyl group, 3-(1Η-味唾_ι_笑) Prop-1-yl, 3-phenylpropyl, phenylhydrazino, qi, isopentyl, propyl, pyridin-2-yl Indenyl, indole-3-ylindenyl and thiophen-3-ylindenyl. In a particular embodiment of the compound of formula vii, ζ3 is selected from the group consisting of 2-(3•fluorophenyl)ethyl and 2-(pyridin-2-yl)ethyl. In a particular embodiment of the compound of formula VII, oxime is selected from the group consisting of cyano, halo, optionally substituted fluorenyl, optionally substituted alkenyl, optionally substituted alkoxycarbonyl, optionally substituted An alkyl group, an optionally substituted amino group, an optionally substituted aminocarbonyl group, and optionally a substituted methyl group. In a particular embodiment of the compound of formula νπ, Z1 is selected from the group consisting of a decyl group, an alkenyl group, an alkoxycarbonyl group, an alkyl group, an amine group, an amine carbonyl group, and a fluorenyl group, wherein the group is optionally subjected to - and Or three substituted groups selected from the group consisting of: cyano, halo, hydroxy, methionyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxy, minus, If necessary, substituted alkoxylates, optionally substituted sulfhydryl groups, optionally substituted f-based carbonyl groups, optionally substituted heterocyclic filaments, optionally substituted heterocyclyl groups, optionally substituted f and the replacement of the stone yellow base. In a particular embodiment of the compound of formula Vn, Z1 is selected from the group consisting of (5-oxy-181 200823188 tetrahydrofuran-2-yl)methylamino; (E)-N'-cyano-N,N-dimethylmethyl Sulfhydryl; (Ζ)-4·(Ν-(2-hydroxy-ethyl)-N,N'-bis(decyloxycarbonyl).methyl lung); (Z)-butyl-2-fine-2 -yl, 1-ethyllactylethyl-1-yl, 1-ethyllactylthio, hydroxyethyl-1-ylamino 2-methoxyethoxy-1-ylamino; 2-methylpropane- 1-alkenyl group, 3-(decyloxygreen)-propan-2- fine-2-yl, 3-(N,N-didecylamino)methyl-propyl-1-ylamino, 3-aminoamino-propan-1 -ylamino, 3-propenyl-1-ylamino, 3-hydrazino-propan-1-yl, 3-oxo! propyl-1 Amino group, 3 _ 曱lacyl propyl, 3-methylbutan-2-furan-2-yl, 4-((atbϋ-3-ylmercapto)aminocarbonyl)butylamino; 4- (Ν,Ν-didecylamino)carbonyl-butan-1-ylamine 10; 4-(indolyl-methylamino)carbonyl-butan-1-ylamino; 4-aminocarbonyl-butyl- 1- • arylamino; ethyl hydrazide; aminocarbonyl; fluorenyl; chloro; cyano; dimethyl, amine; ethoxycarbonyl; hydrogen; oxiranylcarbonyl; methylamine; (2-hydroxyethyl) -Ν-(ethinyl)-amine; Ν-(2-hydroxyethyl)-oxime-(methyl)-amine; Ν-(2-hydroxyprop-1-yl:)-Ν-(曱-amino group; fluorenyl-(fluorenyl)-aminocarbonyl 15 group; fluorenyl-(acridin-2-ylmethyl)amino group; fluorenyl-(acridin-3-ylmethyl)amino group; -(acridin-4-ylindenyl)amino group; fluorene, fluorenyl-dialkyl fluorenyl group; fluorenyl-cyanomethyl fluorenyl group; fluorenyl-methyl-fluorenyl-ethenylamino group; - alkenyl. In a particular embodiment of the compound of formula VII, R1 is selected from the group consisting of hydrogen and, if desired, a substituted lower alkyl group. In a particular embodiment of the compound of formula VII, 2〇 R1 is selected from the group consisting of hydrogen and lower alkyl. In a particular embodiment of the compound of formula VII, R1 is selected from the group consisting of hydrogen and sulfhydryl. In a particular embodiment of the compound of formula VII, R1 is selected from the group consisting of hydrogen. In a particular embodiment, the compound of formula VII is selected from the group consisting of Ν-{[6-(aminomethyl)(2^pyridyl)]fluorenyl}(2-{[2-(3-fluorophenyl)) Base] 182 200823188 Aminobu 5-(3-pyridyl)(3-pyridyl))carbenamide n-{[6-(aminomethyl)(2-pyridyl)]methyl}(2_{[ 2_(3-fluorophenyl)ethyl]aminopyridinyl)(3_π-pyridyl))carbenamide-{[6-(aminomethylpyridinyl)]methyl}(2_{[ 2-(3-fluorophenyl)ethyl]5-aminophenyl 5〆1-methylpyrazol-4-yl)(3-pyridyl))carbenamide N-{[6-(aminomethyl) (2_ σ-pyridyl)]methyl}(5_(2-cyanophenyl)-2-([2-(3-fluorobenzyl)ethyl]amino) aryl)) -Cyano-2-{[2-(3-fluorophenyl)ethyl]amino}(3_0-pyridylpyridylmethyl)decylamine 10 (5_bromo-2_{[2_(3_fluorine) Phenyl)ethyl]amino}(3′′pyridyl))-Ν_[(6-methyl(2-pyridyl))methyl]carbammine (5-bromo-6-chloro-2- {[2-(3-Fluorophenyl)ethyl]amino}(3_η-pyridyl)&gt;ν_(2_pyridylmethyl)carbamamine-5·di-2-{[2_(3-fluorobenzene) Ethyl]amino}amino}pyridine j oleic acid 15 $oxynozyl)ethyl]amino}σ 唆-3- Wei g Fu Jia cool

Nit.二氧基苯并[c]㈣1基）甲基](2♦定基)}甲 基)(5备2-{[2-(3 —氟苯基）乙基]胺基泊 ㈣-.氟笨邮細邮^；·)^ 基曱基）曱醯胺 20 叫[6_(胺基甲基)(2_吼咬基Μ曱基}(5-演-2-{[2_(3_氟苯基） 乙基]胺基}(3“比啶基)）甲醯胺 Ν:{[6-(胺基曱基)(2_t定基)]甲基他㈣3_氣苯基）乙基] 胺基}-5-(2 ^比啶基)(3-吼啶基)）甲醯胺 6-[(4-胺曱酸基丁基)胺基]_2·{[2_(3_氟苯基）乙基]胺基}吼 183 200823188 啶-3-羧酸甲酯 5·[(6-{[2_(3_氟苯基)乙基]胺基}_-5-[Ν-(3-σΛσ定基甲基)胺曱 醯基](2_吼啶基))胺基]-Ν，Ν_二甲基戊醯胺 5-[(6-{[2-(3 -氟苯基）乙基]胺基}-5-[Ν-(3-σΛσ定基曱基)胺甲 5 醯基](2-吡啶基))胺基]甲基戊醯胺 (6-[(4-胺甲醯基丁基）胺基]-2-{[2-(3-氟苯基）乙基]胺 基}(3-吼啶基))-Ν·(3-吡啶基甲基）曱醯胺 4- [(6_ {[2-(3 -氟苯基）乙基]胺基}-5-[Ν-(3_σ比σ定基甲基)胺曱 醯基](2-吡啶基))胺基]-Ν，Ν-二甲基丁醯胺 ίο (6-[(3-胺曱醯基丙基）胺基]-2-{[2-(3-氟苯基）乙基]胺 基}(3-吡啶基))-Ν-(3_吡啶基甲基）曱醯胺 (6-(二甲基胺基）-2-{[2-(3-氟苯基）乙基]胺基}(3_吼啶 基))-Ν-(3-吼啶基曱基）曱醯胺 5- [(6-{[2-(3-氟苯基）乙基]胺基比咬基甲基)胺曱 15 醯基](2^比啶基))胺基]-Ν-(3-吼啶基甲基）戊醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(曱基胺基）(3 j比啶 基))_Ν_(3_π比啶基曱基）甲醯胺 1^-(6-{[2-(3-氣苯基）乙基]胺基}-5-[1^-(3-11比唆基甲基）胺甲 醯基](2-吡啶基))-Ν-曱基乙醯胺 2〇 Ν-(6-{[2-(3-氟苯基）乙基]胺基}-5-[Ν-(3-啦啶基曱基)胺曱 醯基](2-吨啶基))-Ν-(2-羥基乙基）乙醯胺 6- {[2-(3-氟苯基）乙基]胺基}-5-[Ν-(3-吼啶基曱基）胺曱醯 基]吡啶-2-甲醯胺 (6-氰基-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶基))-Ν-(3-口比 184 200823188 °定基甲基）甲醯胺 (2-{[2-(3_氣苯基）乙基]胺基}_6_[(3-吡啶基甲基）胺基] &quot;比&quot;定基》1(3』比啶基甲基）甲醯胺 (6-[(虱基胺基）亞胺基甲基]-2_{[2_(3_氟苯基）乙基]胺 基}(3』比π定基))_N_(3』比咬基甲基）甲醯胺 (6-((1 Ζ)、Κ甲基丙小烯基）_2_{[2_(3_氟苯基）乙基]胺 基}(3_°比啶基))-Ν-(3-吼啶基甲基）甲醯胺 (2_{[2_(3-氟苯基）乙基]胺基}_6_(Ν_甲基胺甲醯基)(3_吡啶 基))-Ν-(3-比啶基甲基）甲醯胺 6 {[2-(3-氟苯基）乙基]胺基j_5_[n_(3_吡啶基甲基）胺甲醯 基]吼咬&gt;2-羧酸曱酯 (2-{[2-(3-氟苯基）乙基]胺基比啶基甲基）胺基](1 17比咬基))1(3』比啶基甲基）甲醯胺 (6_(jl Ε)丙-1_烯基&gt;5_溴_2_{[2_(3_氟苯基）乙基]胺基}(3_ 口比σ定基))_ Ν - (3 - π比啶基甲基）甲醯胺 甲基（2Ε)-3-(6-{〇(3-氟苯基）乙基]胺基卜5·[Ν_(3_σ比啶基 曱基)胺曱醯基](2_σ比啶基))丁_2_烯酸曱酯 (2_{[2-(3-氟苯基）乙基]胺基比啶基曱基）胺基](3_ σ比唆基))-Ν_(3-吡啶基曱基）曱醯胺 6-{1&gt;〇氟苯基）乙基]胺基卜5_阶(3-σ比啶基曱基)胺曱醯 基]°比咬-2-叛酸乙酯 (6-((1Ε)丙-1-烯基)_2_{1&gt;(3_氟苯基）乙基]胺基比啶 基))-N-(3-咣啶基曱基）曱醯胺 (6_((1E)丙小烯基)_5_氰基_2_{[2_(3_氟苯基）乙基]胺基泊_ 185 200823188 吡啶基))-N-(3-吡啶基曱基）曱醯胺 (2-{[2-(3_氟苯基）乙基]胺基卜6-(2-曱基丙+烯基比啶 基))_N-(3』比啶基曱基）曱醯胺 (6-[(二曱基胺基）亞胺基曱基]_2_{[2_(3-氟苯基）乙基]胺 基}(3_吼啶基))-Ν_(3_π比啶基曱基）曱醯胺 (6-[(1Ε)-1-(二曱基胺基&gt;2_氰基_2_氮雜乙烯基&gt;2_{[2_(3_ 氟苯基）乙基]胺基}(3_π比啶基))_Ν-(3-吡啶基甲基）曱醯胺 6-{[2_(3_氣苯基）乙基]胺基卜5_[ν_(3』比啶基甲基）胺曱醯 基]ϋ比唆-2-曱醯胺 2-[0{|&gt;(3-氟苯基）乙基]胺基卜5_苯基(3_π比啶基))叛基胺 基]曱基乙醯胺 (6·((1Ε)丙_1_烯基)_2_{|&gt;(3_氟苯基）乙基]胺基}(3_n比啶 基))_N-{[2_(胺基曱基)(3_σ比啶基)]甲基}甲醯胺 2_[(5_(2_氰基苯基)_2_{[2_(3_氟苯基）乙基]胺基泊』比啶 基))幾基胺基]甲基乙酸胺 (6-((1Ε)-3_甲氧基丙+烯基）_2_{[2_(3_氟苯基）乙基]胺 基}(3』比咬基))_Ν_(3_吼啶基甲基）曱醯胺 (6_(eth乳基乙基）_2_{[2_(3_氟苯基）乙基]胺基丨(3_吼啶 基))善(3_吼啶基曱基）曱醯胺 (6乙I基2 {[2_(3-氟苯基）乙基]胺基}(3_吼0定基))_n_(3_ 吡啶基甲基）甲醯胺 (6-((1Ε)丙-1-稀基)_5_氟_2_{[2_(3_氟苯基）乙基]胺基丨〇比咬 基))-N-{〇(胺基甲基⑹“比。定基)]曱基}曱_ (6-(⑽丙-1-烯基卜氟列吵氟苯基）乙基]胺基你吼 186 200823188 °疋基))-N-[〇{[(第三丁氧基）羰基胺基]曱基}(3_吡啶 -甲基]曱醯胺 N-{[2-(胺基曱基)(3_吼咬基)]甲基丨(5备2_{[2_(3_氣苯基) 乙基]胺基}(3_吡啶基)）甲醯胺 (2 {[2 Ο氟笨基）乙基]胺基泊^比。定基))_Ν_(3_σ比啶基 基）曱醯胺 (6-(1，2-一甲基丙+烯基&gt;2_{[2办氣苯基）乙基]胺基砂 吡啶基))-Ν-(3-吡啶基甲基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}_6_(3-甲氧基丙基）(3_。比啶 基))-N-(3_u比啶基曱基）甲醯胺 (H1-乙氧基乙酸基)_2H氧笨基）乙基]胺基}(3^比啶 基))1(3_吼啶基曱基）曱醯胺 (={[2_(3_氟苯基）乙基]胺基}_6_[(2_經基乙基)胺基](μ 啶基))-Ν_(3-吡啶基甲基）曱醯胺 (2_{[2-(3_氟苯基）乙基]胺基}_6_[(2_羥基乙基）甲基胺 基](3_°比咬基))春(3_σ比啶基曱基）甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基卜曱氧基乙基）胺基](3_ 吼。定基))_Ν-(3』比啶基甲基）甲醯胺 (2_{[2-(3-氟苯基）乙基]胺基}_6_[(2_羥基丙基）甲基胺 基](3_σ比咬基))_Ν-(3_π比啶基甲基）甲醯胺 2_{[2-(3-氟苯基）乙基]胺基卜6-[(3-甲氧基丙基)胺基](3-吡 啶基))-Ν-(3-吡啶基甲基）甲醯胺及 (2 {[2-(3_氟本基）乙基]胺基卜6_[(3_經基丙基）胺基](3_口比 σ定基))善(3_π比啶基甲基）曱醯胺。 187 200823188 本文所述之化合物可利用本項技藝中熟知之技術由 市售起始物質及試劑來合成。例如，化合物可如下所述來 製備。 流程1Nit. Dioxybenzo[c](tetra)1yl)methyl](2♦)}methyl)(5-substituted 2-{[2-(3-fluorophenyl)ethyl]aminopoline (tetra)-. Fluoride stupid mail ^;·) ^ base 曱醯) guanamine 20 is called [6_(aminomethyl) (2_吼 Μ曱 base }) (5-演-2-{[2_(3_ Fluorophenyl)ethyl]amino}(3"pyridinyl)carbamidine oxime:{[6-(aminomercapto)(2_t-decyl)]methyl-(tetra)-3-phenylphenyl)ethyl] Amino}-5-(2^pyridyl)(3-acridinyl))carhamamine 6-[(4-aminodecanoylbutyl)amino]_2·{[2_(3_fluorobenzene) Ethyl]amino}amine} 183 200823188 pyridine-3-carboxylic acid methyl ester 5·[(6-{[2_(3_fluorophenyl)ethyl]amino}}-5-[Ν-(3 -σΛσ定基 methyl)amine hydrazino](2_acridinyl))amino]-oxime, Ν_dimethylammoniumamine 5-[(6-{[2-(3-fluorophenyl)) Ethyl]amino}-5-[Ν-(3-σΛσ-decyl)aminomethyl-5-mercapto](2-pyridyl))amino]methylpentamidine (6-[(4-amine A) Nonylbutyl)amino]-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))-indole·(3-pyridylmethyl)decylamine 4-[(6_ {[2-(3-Fluorophenyl)ethyl]amino}-5-[Ν-(3_σ ratio σ定基 methyl)amine fluorenyl](2-pyridyl)) ]-Ν,Ν-dimethylbutyl Amine ίο (6-[(3-Aminomethyl)amino]-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))-Ν-( 3-(Pyridylmethyl)guanamine (6-(dimethylamino)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_acridinyl))-oxime -(3-acridinyl fluorenyl) decylamine 5-[(6-{[2-(3-fluorophenyl)ethyl]amino) butylmethyl)amine 曱15 fluorenyl](2^ Bisyl))amino]-indole-(3-acridinylmethyl)pentanylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(decylamine) (3 j is more than pyridine)) Ν ( ((3_π-pyridyl fluorenyl) carbamide 1^-(6-{[2-(3-phenylphenyl)ethyl]amino}-5-[1 ^-(3-11-decylmethyl)amine-mercapto](2-pyridyl))-fluorenyl-mercaptoacetamide 2〇Ν-(6-{[2-(3-fluorophenyl)) Ethyl]amino}-5-[indolyl-(3-oxaridinyl)aminoindenyl](2-tonyl)-indole-(2-hydroxyethyl)acetamidamine 6- { [2-(3-Fluorophenyl)ethyl]amino}-5-[indolyl-(3-acridinylfluorenyl)amine fluorenyl]pyridine-2-carboxamide (6-cyano-2) -{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))-oxime-(3-mouth ratio 184 200823188 °methyl group) formamide (2-{[2 -(3_gasphenyl)ethyl]amino}_6_[(3-pyridylmethyl)amino ] &quot;比&quot;定基》1(3′′ pyridinemethyl)carbamamine (6-[(decylamino)iminomethyl]-2_{[2_(3_fluorophenyl) B Amino group}(3) than π group))_N_(3" than dimethyl group) formamide (6-((1 Ζ), Κmethylpropanyl))_2_{[2_(3_ Fluorophenyl)ethyl]amino}(3_°pyridyl))-indole-(3-acridinylmethyl)carbenamide (2_{[2_(3-fluorophenyl)ethyl]amino) }_6_(Ν_Methylaminemethanyl)(3_pyridyl))-indole-(3-pyridylmethyl)carbamamine 6 {[2-(3-fluorophenyl)ethyl]amine Base j_5_[n_(3_pyridylmethyl)aminemethanyl]bite&gt; 2-carboxylic acid oxime ester (2-{[2-(3-fluorophenyl)ethyl]aminopyridinyl) Amino] (1 17 to butyl)) 1 (3 比 pyridinemethyl) carbamide (6_(jl Ε) propyl-1_alkenyl] 5_ bromo_2_{[2_(3 _Fluorophenyl)ethyl]amino} (3_ mouth ratio σ base)) Ν ( - (3 - π-pyridylmethyl)carbamamine methyl (2Ε)-3-(6-{〇(3 -fluorophenyl)ethyl]aminopurine 5·[Ν_(3_σ-pyridylhydrazinyl)amine fluorenyl](2_σ-pyridyl))but-2-enoate (2_{[2-( 3-fluorophenyl)ethyl]aminopyridinylamino)amino](3_σ唆唆))-Ν(3-pyridylfluorenyl)曱Amine 6-{1> 〇 fluorophenyl)ethyl]aminopyr 5-order (3-σ-pyridyl fluorenyl)amine thiol] ° than bite-2-reacid ethyl ester (6-(( 1Ε)prop-1-enyl)_2_{1&gt;(3-fluorophenyl)ethyl]aminopyridinyl))-N-(3-acridinylfluorenyl) decylamine (6_((1E) ) propylene small alkenyl)_5_cyano-2_{[2_(3_fluorophenyl)ethyl]amine bero 185 200823188 pyridyl))-N-(3-pyridylfluorenyl) decylamine ( 2-{[2-(3-fluorophenyl)ethyl]aminobi 6-(2-amidinopropyl+alkenylpyridinyl))-N-(3′′pyridylhydrazinyl)guanamine 6-[(didecylamino)imidohydrazino]_2_{[2_(3-fluorophenyl)ethyl]amino}(3_acridinyl))-Ν_(3_π-pyridylthiol) Guanidine (6-[(1Ε)-1-(didecylamino)&gt;2-cyano-2-azavinyl&gt;2_{[2_(3-fluorophenyl)ethyl]amine }(3_π比基基))_Ν-(3-Pyridylmethyl)decylamine 6-{[2_(3_-phenylphenyl)ethyl]aminopurine 5_[ν_(3"-pyridylmethyl Amine oxime] ϋ 唆 曱醯 曱醯 曱醯 2- 2-[0{|&gt;(3-fluorophenyl)ethyl]aminopyridin-5-phenyl (3_π-pyridyl))曱]mercaptoacetamide (6·((1Ε)prop-1-enyl)_2_{|&gt;(3-fluorophenyl)ethyl]amino}(3_n-pyridyl))_ N-{[2_(aminomercapto)(3_σ-pyridyl)]methyl}carbamamine 2_[(5_(2-cyanophenyl)_2_{[2_(3_fluorophenyl)ethyl]] Aminosylpyridinyl))aminoamino]methylacetic acid amine (6-((1Ε)-3-methoxypropenyl+alkenyl)_2_{[2_(3_fluorophenyl)ethyl] Amino}(3" to bite))_Ν_(3_acridinylmethyl)decylamine (6_(eth-milylethyl)_2_{[2_(3-fluorophenyl)ethyl]aminopurine (3_Acridine group)) good (3_acridinyl fluorenyl) decylamine (6 ethyl I yl 2 {[2_(3-fluorophenyl)ethyl]amino} (3_吼0 base) )_n_(3_pyridylmethyl)carbamamine (6-((1Ε)prop-1-yl)_5_fluoro_2_{[2_(3_fluorophenyl)ethyl]aminopyrene Base))-N-{〇(aminomethyl(6)" ratio.定基)]曱基}曱_(6-((10)prop-1-enylfluorophene fluorophenyl)ethyl]amine based 吼186 200823188 °疋基))-N-[〇{[(第Tributoxy)carbonylamino]mercapto}(3_pyridine-methyl)decylamine N-{[2-(aminoindenyl)(3_吼)]methylhydrazine (5 备2_ {[2_(3_气phenyl)ethyl]amino}(3_pyridyl))carboxamide (2 {[2 fluorinyl)ethyl]amine moiepo ratio. base))_Ν_( 3_σ-pyridyl) decylamine (6-(1,2-methylpropane+alkenyl)&gt;2_{[2 phenyl)ethyl]aminopyridinyl))-Ν-(3 -pyridylmethyl)decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}}_6-(3-methoxypropyl)(3_.pyridyl))-N- (3_u-pyridyl fluorenyl)carzamide (H1-ethoxyacetoxy)_2H oxophenyl)ethyl]amino}(3^pyridyl))1(3_acridinyl) hydrazine Indoleamine (={[2_(3_fluorophenyl)ethyl]amino}}_6_[(2-transethylethyl)amino](μ pyridine))-Ν-(3-pyridylmethyl)anthracene Indoleamine (2_{[2-(3-fluorophenyl)ethyl]amino}_6_[(2-hydroxyethyl)methylamino] (3_° ratio), spring (3_σ-pyridyl) Methionine (2-{[2-(3-fluorophenyl)ethyl]aminobiphenyloxyethyl)amine ](3_ 吼.定基))_Ν-(3"pyridylmethyl)carbamamine (2_{[2-(3-fluorophenyl)ethyl)amino}_6_[(2-hydroxypropyl) Methylamino] (3_σ ratio), Ν-(3_π-pyridylmethyl)carbamamine 2_{[2-(3-fluorophenyl)ethyl]aminodibu 6-[(3-A) Oxypropyl)amino](3-pyridyl))-indole-(3-pyridylmethyl)formamide and (2{[2-(3-fluoro)ethyl)ethyl]amino 6_ [(3_Pentylpropyl)amino] (3_port ratio σ base)) Good (3_π-pyridylmethyl)guanamine. 187 200823188 The compounds described herein can be synthesized from commercially available starting materials and reagents using techniques well known in the art. For example, the compounds can be prepared as described below. Process 1

• 有關反應流程1，步驟1，係於式101化合物及過量 的（例如約1.1當量）式Z3NH2化合物於極性溶劑例如DMF 之溶液中，於室溫下加入鹼例如碳酸鉀。將產物，式103 化合物，分離並視需要純化。 ίο 有關反應流程1，步驟2，係於式103化合物、過量 的（例如約2當量）式zbCOHh化合物及鹼例如碳酸鉀，於 極性溶劑例如DMF中加入約0· 1當量的PdCl2.dppf。將反 應混合物約100°C攪拌約4 h。將產物，式105化合物， 分離並視需要純化。 15 有關反應流程1，步驟2，係於式105化合物及過量 的（例如約1.4當量）式R1QNH2化合物於極性溶劑例如 DMF之溶液中，於室溫下加入過量的（例如約1.5當 量)AlMe3。將反應混合物約70QC攪拌至隔夜直到反應完 成。將產物，式107化合物（其中Z2為胺基羰基），分離並 200823188 視需要純化。 除，有相反之朗，否縣克之限定_， mL)之洛劑係構成一體積當量。 （次 若需要’本文所述之化合物及中間物之 藉由任何適合的分離麵化方法例如，過# 、、、姓曰可 錄層=、薄層層析、或厚層層析或這些綠卒之=合。^ ==的分狀分離方法之特定朗係如實例中所提 I然而’其他同等的分開或分離方法當然亦可使用。 10 15 20 右需鱗’（R)及⑻異構物可藉由熟胃本項技術者已 =方絲解晰，例如，藉由形成可分離的非對映異構物 皿讀或複合物’例如藉由結晶；經由形成可分離的非對映 異構物衍生物’例如藉由結晶、氣相_液相或液相層析、 將一種鏡像異構物與鏡像異構物專一試劑之選擇性反 應’例如酵素性氧化作用或還原仙，接著將修式或未終 修飾之鏡像異構物分離；或在財環境下之氣相·液相、^ 液相層析，例如於對掌載體上，如帶有結合對掌配體 ，或在對〜敎存在下。應了解，當所欲的鏡像異構物 藉由上述之分離方法轉化為另一化學品時，可能需要另〜 個步驟以釋出該所欲的鏡像異構物形式。另外，特定的妒 ,異構物可藉由不對稱合成使用光學活性試劑、物質、： 晶及/或溶劑，或藉由不對稱轉化將鏡像異構物轉變^ 一種鏡像異構物。 本文所述的化學品可用於各種涉及平滑肌細胞及/或 非肌肉細胞之應用上。在特定的實施例中，該等化學品可 189 200823188 用於抑制平滑肌肌凝蛋白。兮隹/t的 抑制半ww 4化學品可用於結合及/或 抑制千„肌歸蛋自之祕。物 = :=_如哺乳動物)之平滑肌 活性，但在“时施财，該讀肌 在特定的實施例中σ a曰马人摘 、疑疋白兮望於與口專化學品可用於抑制非肌肉肌 白:活性肉肌凝蛋 蝴如_物)之非肌肉肌凝蛋二或== 貫施例中，該非肌肉肌凝蛋白為人類的。 15 本文所述之化學品可用於治療與平滑肌及/或非肌肉 肌凝蛋白有病之疾病狀態。可藉由本文所述之化學品治療 之此等疾餘態包括(但不限於）高血壓、氣喘、慢性阻塞 性肺疾病、早產陣痛及其類似疾病。應了解，在某些案例 中，細胞並非在不正常的狀態下，但仍需要治療。因此， 在特定的實關巾，本讀述之化學^可應祕細胞或投 予罹患或即將罹患任一種這些疾病或症狀之個體。 更特而言之，本文所述之化學品可用於治療與肌肉張 力不正常增加或過量收縮，或系統、管狀動脈、肺循環以 及微循環平滑肌中之血管平滑肌肌痙攣，例如系統性高血 壓、惡性高血壓、高血壓危象、症狀性高血壓、肺高i壓、 肺梗塞、心絞痛、心肌梗塞、休克情況下微循環失調及在 人類或動物體之其他部位或器官中發生之梗塞。可以本文 所述之化學品治療之其他其疾病或症狀包括： 胃腸平滑肌包含括約肌之痙攣，例如胃痙攣、幽門痙攀及 190 20 200823188• In relation to Reaction Scheme 1, Step 1, a solution of a compound of formula 101 and an excess (e.g., about 1.1 equivalents) of a compound of formula Z3NH2 in a polar solvent such as DMF is added to a base such as potassium carbonate at room temperature. The product, compound of formula 103, is isolated and purified if necessary. Ίο. Reaction Scheme 1, Step 2, is a compound of formula 103, an excess (e.g., about 2 equivalents) of a compound of formula zbCOHh and a base such as potassium carbonate, and about 0.1 equivalent of PdCl2.dppf is added to a polar solvent such as DMF. The reaction mixture was stirred at about 100 ° C for about 4 h. The product, compound of formula 105, is isolated and purified if necessary. 15 Related Reaction Scheme 1, Step 2, is to add an excess (e.g., about 1.5 equivalents) of AlMe3 at room temperature to a solution of a compound of formula 105 and an excess (e.g., about 1.4 equivalents) of a compound of formula R1QNH2 in a polar solvent such as DMF. The reaction mixture was stirred at about 70 QC until overnight until the reaction was completed. The product, compound of formula 107 (wherein Z2 is the aminocarbonyl group), is isolated and purified as needed in 200823188. In addition, there is the opposite, the county gram limit _, mL) of the agent constitutes a volume equivalent. (If sub-required 'the compounds and intermediates described herein by any suitable separation surface method, for example, over #,,, 曰可可层层=, thin layer chromatography, or thick layer chromatography or these green The specific language of the fractal separation method of ^==^== is as mentioned in the example. However, other equivalent separation or separation methods can of course be used. 10 15 20 Right-demand scales (R) and (8) The construct can be resolved by the skilled person, for example, by forming a separable diastereomeric dish reading or complex 'for example by crystallization; by forming a separable non-pair An enantiomeric derivative 'selectively reacts a mirror image isomer with a mirror image isomer specific reagent by, for example, crystallization, gas phase liquid phase or liquid phase chromatography, eg, enzymatic oxidation or reduction Then, the mirror image isomers of the modified or unfinished modification are separated; or in the gas phase, liquid phase, liquid chromatography, for example, on the palm support, such as with a binding pair ligand, or In the presence of ~敎. It should be understood that when the desired mirror image isomer is separated by the above method In the case of another chemical, another step may be required to liberate the desired smectomer form. In addition, specific oximes, isomers may be optically active using asymmetrically active reagents, materials, and: Crystals and/or solvents, or by mirror transformation of a mirror isomer by asymmetric transformation. The chemicals described herein can be used in a variety of applications involving smooth muscle cells and/or non-muscle cells. In embodiments, the chemicals 189 200823188 are used to inhibit smooth muscle myosin. 兮隹/t inhibits half-ww 4 chemicals that can be used to bind and/or inhibit the secrets of the muscles. _ such as mammals) smooth muscle activity, but in the "time to pay, the reading muscle in a specific example σ a 曰 人 人 、 、 、 、 、 、 、 、 、 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 与 口: Non-muscle muscle egg condensed egg 2 or == In the case of the application, the non-muscle myosin is human. 15 The chemicals described herein are useful in the treatment of conditions associated with smooth muscle and/or non-muscle myosin. Such disorders that may be treated by the chemicals described herein include, but are not limited to, hypertension, asthma, chronic obstructive pulmonary disease, premature labor pain, and the like. It should be understood that in some cases, the cells are not in an abnormal state, but treatment is still needed. Thus, in a particular solid towel, the chemistry of the present invention may be administered to an individual suffering from or about to suffer from any of these diseases or conditions. More specifically, the chemicals described herein can be used to treat abnormal or excessive contraction of muscle tone, or vascular smooth muscle tendons in systemic, tubular arteries, pulmonary circulation, and microcirculatory smooth muscle, such as systemic hypertension, malignancy. Hypertension, hypertensive crisis, symptomatic hypertension, high lung pressure, pulmonary infarction, angina pectoris, myocardial infarction, microcirculatory disorders in the case of shock, and infarctions occurring in other parts or organs of humans or animals. Other diseases or conditions that may be treated by the chemicals described herein include: Gastrointestinal smooth muscles including sphincters, such as stomach cramps, pyloric climbing and 190 20 200823188

膽道、胰ϋ、尿道痙攣m结石或寄生蟲刺激 起的痙攣；其他内臟器官痙攣’例如子宮、輸印管等| 氣管-支氣管平滑肌、橫胸肌痙攣，例如夂種氣—、2 困難、驚厥、橫腸抽搐等等；消化道平滑肌之痙擎’吸 胃、小腸及大腸、膽及胰道等；及尿道平滑肌座I 包括 10 15 此外’本文所述之化學品可用於懷孕期間之控制、总 理及分挽處理。此方法特別可用於抑制自發性早產，复如 不處理會導致早產或流產及用於抑制經子宮胎兒手彳 間手術引發的分娩。此方法亦可用於引發過期姙娠之分^ 其中該分娩不是發生在娘娠期間及當其必須引發分挽以 確保正常生產。 再者，本文所述之化學品可用於治療「氣管壁重塑」， 其為一種與特徵為氣管壁增厚及氣管阻塞有關之疾病或 症狀，其可能會例如發生於患有特定呼吸道疾病症狀(例 如阻塞性疾病（COPD))病患之小氣管上。 此寻可以本文所誕供之化學品、組合物及方法治療之 疾病狀態亦包括（但不限於）青光眼及其他眼部適應症。更 特而言之，本文所述之化學品可用於治療與青光眼有關之 疾病或症狀，包括眼壓增高、眼内房水液流降低及視神經 損傷。可以本文所述之化學品、組合物及方法治療之疾病 或症狀包括高眼壓。Biliary tract, pancreatic fistula, urethral 结m stones or parasites stimulated by parasites; other internal organs such as uterus, printing tubes, etc. | tracheal-bronchial smooth muscle, transverse chest tendon, such as sputum, - 2 difficulties, Convulsions, convulsions of the transverse intestines, etc.; the gastrointestinal smooth muscles of the sputum 'sucking, small intestine and large intestine, gallbladder and pancreatic ducts; and urethral smooth muscle loci I include 10 15 In addition, the chemicals described herein can be used for control during pregnancy The Prime Minister and the Deputy. This method is particularly useful for inhibiting spontaneous preterm labor, as long as it does not result in premature birth or miscarriage and for inhibiting labor caused by uterine fetal hand surgery. This method can also be used to trigger an overdue pregnancy where the birth does not occur during the gestation period and when it must initiate a split to ensure normal production. Furthermore, the chemicals described herein can be used to treat "tracheal wall remodeling", a disease or condition associated with thickening of the tracheal wall and obstruction of the trachea, which may occur, for example, in the presence of a specific respiratory disease. (eg obstructive disease (COPD)) on the small trachea of the patient. The disease states that can be treated by the chemicals, compositions, and methods provided herein include, but are not limited to, glaucoma and other ocular indications. More particularly, the chemicals described herein can be used to treat diseases or conditions associated with glaucoma, including increased intraocular pressure, decreased intraocular aqueous fluid flow, and optic nerve damage. Diseases or conditions that can be treated by the chemicals, compositions, and methods described herein include high intraocular pressure.

藉由肌凝蛋白應用ATP水解產生力量。ATP水解增加 會對應肌肉收縮之力量及速度增加。在肌動蛋白的存在 下，刺激肌凝蛋白ATP酶活性超過loo-倍。因此，測量ATP 191 20 200823188 水解不僅測量肌凝蛋白酵素活性亦測量其與肌動蛋白絲 之交互作用。雖然亦可使用其他-生物之肌凝蛋白，但此等 活性分析可應用人類來源之平滑肌肌凝蛋白。亦可使用在 肌凝蛋白結合中鈣之調節角色模型系統。 5 在活體外，ATP水解係與加強活性之平滑肌肌凝蛋白 有關，其可藉由偵測ADP或磷酸之產生來測定，例如美國 專利第6,410,254號中所述。ADP產生亦可藉由將ADP產物 愈NADH氧化物偶合來彳貞測（使用，例如酵素丙酮酸激酶 及乳酸去氳酶）以及偵測NADH之量，例如藉由吸收度或 10 螢光（Greengard, P·，TVaiwre 178 (Part 4534) : 632-634 (1956) ; Mo/ 尸1970 Jan ; 6(1) ·· 31-40)。石彝酸產 生之偵測亦可使用嘌呤核苷磷酸化酶將磷酸產物與嘌呤 類似物之裂解偶合’其產生了吸收度〈乃&quot;6^//^/^0(2(^5^/ 5 d 1992 Jun 1 ; 89(11) : 4884_7)或螢光改變J 15 1990 Mar 1 ; 266(2) : 611-4)。當使用單一測量時，亦可 使用相同樣本依序於不同時間之多次測量以測定蛋白質 活性之絕對速率；此等測量具有較高的特異性，特別是在 具有該等酵素讀數之類似吸收度或螢光特性之試驗化合 物的存在下。 20 試驗化合物可於高度相似方法中使用多孔盤，藉由將 化合物個別置於孔槽中或將其於混合物中試驗來分析。分 析化合物包括目標蛋白質複合物、偶合酵素和基質，然後 可將ATP加入孔槽中並以盤式判讀機測量盤中各孔之吸 收度及螢光。 192 200823188 一種方法係使用384孔盤格式及25 pL反應體積。使用 丙酮酸激酶/乳酸去氫酶偶合酵素系統（Huang TG andPower is produced by the application of ATP hydrolysis to myosin. An increase in ATP hydrolysis will increase the strength and speed of muscle contraction. In the presence of actin, the myosin ATPase activity was stimulated to exceed loo-fold. Therefore, measuring ATP 191 20 200823188 hydrolysis not only measured myosin activity but also measured its interaction with actin filaments. Although other-biological myosin can also be used, these activity assays can be applied to smooth muscle myosin of human origin. A regulatory role model system for calcium in myosin binding can also be used. 5 In vitro, ATP hydrolysis is associated with potentiating smooth muscle myosin, which can be determined by detecting the production of ADP or phosphoric acid, as described in U.S. Patent No. 6,410,254. ADP production can also be detected by coupling ADP products to NADH oxides (using, for example, enzyme pyruvate kinase and lactate dehydrogenase) and detecting the amount of NADH, for example by absorbance or 10 fluorescence (Greengard) , P·, TVaiwre 178 (Part 4534): 632-634 (1956); Mo/ Corpse 1970 Jan; 6(1) ·· 31-40). The detection of the production of linoleic acid can also use the purine nucleoside phosphorylase to couple the cleavage of the phosphoric acid product with the ruthenium analog, which produces an absorbance < is &quot;6^//^/^0(2(^5^ / 5 d 1992 Jun 1 ; 89(11) : 4884_7) or fluorescent change J 15 1990 Mar 1 ; 266(2) : 611-4). When a single measurement is used, the same sample can also be used to measure multiple times of protein activity at different times to determine the absolute rate of protein activity; these measurements have higher specificity, especially in similar absorbances with such enzyme readings. Or in the presence of a test compound of fluorescent properties. 20 Test Compounds Porous discs can be used in highly similar methods by analyzing the compounds individually in wells or by testing them in a mixture. The analysis of the compound includes the target protein complex, the coupling enzyme, and the matrix, and then the ATP can be added to the well and the absorbance and fluorescence of each well in the disk can be measured by a disc reader. 192 200823188 One method uses a 384-well plate format with a 25 pL reaction volume. Use pyruvate kinase/lactate dehydrogenase coupling enzyme system (Huang TG and

Hackney DD. (1994) J Biol Chem 269(23) : 16493-16501) 測量個孔槽之ATP水解之速率。如同熟習本項技術者應會 5 了解的’分析成份係加在缓衝液或試劑中。因為文中所概 述之方法能進行動力測量，培養期間可經最適化以得到適 當去除訊號之背景。分析係以真實時間進行以得到ATP 水解度增加分析之訊號對噪音比例之動力學。 平滑肌肌凝蛋白之選擇性可藉由在一或多種上述分 1〇 析中以其他肌凝蛋白取代來測量並將所得到的結果與使 用心肌同等物所得到的結果作比較。 • 作為平滑肌肌凝蛋白調節劑藉由本文所述之方法所 辨識之化學品，可進一步試驗效力篩選，例如使用透性化 平滑肌形式之條V ’例如雞臉之篩選。約敏感平滑肌條帶 15 係藉由將雞胗組織剖開，接著以1% Triton X-100處理使條 帶可透過外生性的化合物（Bars〇tti，RJ，# 乂，Am J Physiol. 1987 May ; 252(5 Pt 1) : C543-54)。這些條帶可 儲存於-20°C、50%甘油中數星期，使各批之肌肉條帶能 進行多次實驗。實驗之進行係使用20 mM咪唑pH 7.0、5.5 2〇 mM ATP、7 mM MgCl2、55 mM ΚΠ、1 pM Calmodulin 及10 mM EGTA。游離的鈣可藉由加入不同量的CaCl2， 根據MAXChelator之計算式來控制（Patton,等人，Cell Calcium· 35/5 ρρ· 427-431，2004)。使用等容積肌肉纖維裝 置測量等容積張力，使用National Instruments公司 193 200823188Hackney DD. (1994) J Biol Chem 269(23): 16493-16501) measures the rate of ATP hydrolysis of a well. As with those skilled in the art, the analytical component should be added to the buffer or reagent. Because the method outlined in the text enables dynamic measurements, the culture period can be optimized to obtain a background for proper signal removal. The analysis was performed in real time to obtain the kinetics of the signal-to-noise ratio for the ATP hydrolysis degree increase analysis. The selectivity of smooth muscle myosin can be measured by substitution with other myosin in one or more of the above assays and the results obtained are compared to those obtained using myocardial equivalents. • As a smooth muscle myosin modulator, the screening of potency can be further tested by the chemicals identified by the methods described herein, for example using a strip of translucent smooth muscle form V&apos; such as a chicken face. The approximately sensitive smooth muscle strip 15 was made by excising the chicken gill tissue and then treating it with an exogenous compound by treatment with 1% Triton X-100 (Bars〇tti, RJ, # 乂, Am J Physiol. 1987 May ; 252 (5 Pt 1) : C543-54). These strips can be stored in -20 ° C, 50% glycerol for several weeks, allowing multiple bands of muscle strips to be tested. The experiment was carried out using 20 mM imidazole pH 7.0, 5.5 2 mM ATP, 7 mM MgCl2, 55 mM guanidine, 1 pM Calmodulin and 10 mM EGTA. Free calcium can be controlled according to the calculation formula of MAXChelator by adding different amounts of CaCl2 (Patton, et al., Cell Calcium 35/5 ρρ. 427-431, 2004). The equal volume tension was measured using an equal volume muscle fiber device using National Instruments 193 200823188

PCL&quot;MI(M6E-4，16頻道，12位A/D板，Aurora專—之400A 傳導器擷取資料。當於低鈣溶液(pCa 8)中浸诜時，將經 化學去皮之雞胗纖維鬆弛，但當浸洗溶液之游離鈣增加至 pCa 5時，產生等容積張力。這些纖維可藉由在高及低鈣 浸洗溶液間轉換來重複收縮及鬆弛。 首先藉由將鬆弛的纖維以化合物預培養，接著轉置於 化合物之高鈣溶液中，試驗化合物其預防雞胗條帶收縮之 能力。其次’ H由將化合物添加至已於高触液預培養之 纖維中，試驗化合物其使收縮的纖維放鬆之能力。進行前 期實驗以確定抑制效用為可逆的，因此化合物無法對平滑 肌肌凝蛋白造成變性或其他不能修補的損傷。 &amp;化學品細治療上有效缝，例如足以提供前述疾病 狀悲治療之劑量來給藥。_般而言，每日劑量係從約 至約100 mg/kg之體重，例如從約〇丨〇至約丨〇 吆之體重 或從約0.15至約1 mg/kg之體重。因此，就給藥㈣响 人’劑量範圍係每天從約3 5至約7〇〇〇1^，例如每天從約 7至約700 mg，或每天從約10至約100 mg。所投予之活性 =學品之量:當轉依所治療的對象和疾病狀態、患病的 嚴重度、給藥方法和時程以及、冶療醫師之判斷而定；例 如’口服給樂之劑量範圍每天可從約70至約7〇〇 铁 而就靜脈内給藥，劑量範圍每天可從約7GG至約7_邮。、 活性樂劑可分別選擇較長紐㈣血漿半衰期。 文中所迷之化學品之給藥可經由任何能提供類似利 用之可接受的給藥模式，其包括(但不限於）口服、皮下、 194 200823188 靜脈内、鼻内 肌肉内、肺内、陰道、^滲透、舌下、黏膜内、腹胲内、 局部、非經腸及眼内㈣（包括眼内注射）° 口^ 應症。 、、σ7Κ係習用於治療許多本文所述的適 醫藥上可接受纟 10 15 20 形式，例如旋劑、膠I “包括固態、半固態、液態及氣霧 霧劑及類似物。化學，劑、液體、懸浮液、栓劑、氣 給藥’包括注射器^=\以持續或控制釋放劑量形式來 括電轉運)貼布、滴劑等張幫浦、片劑、皮膚滲透（包 或定時脈衝給藥。/化”合類似物，以預定的速率供延長及/ 位劑型來提供。、σ可以適合單一給予準確劑量之單 醫藥品可單獨或與羽^ 醇、乳糖、殿粉、硬月::肖醫藥載體或類似物(例如甘露 鏈羧曱基纖維素、葡、，精鈉、滑石、纖維素、交 組合來給藥。若兩要二明膠、蔗糖、碳酸鎂及類似物） 劑物質，例如^劑、==物亦可含有次量之無毒佐 似物(例如乙_、_ /、增、溶劑、ΡΗ緩衝劑及類 酸山半糖醇s二!r酸納、環狀糊精衍生物、單月桂 夂山术，曰、乙酸三乙醇胺、油酸三乙醇胺)。一般而 言，依照所欲的給藥禮斗、; 舨啲 ,,.Q,0/ ^ 、市核式，请樂組合物可含有從約0.005% 至、力95/。，例如從約〇.5%至約5〇%重量比之至少—種醫藥 品。製備轉劑型之實際方法為熟f本項技術者所知或明 瞭，例如，參見賓州伊斯頓（East〇n) Mack出版公司之PCL&quot;MI (M6E-4, channel 16, 12 A/D board, Aurora special - 400A transmitter for data. When dip in low calcium solution (pCa 8), chemically peeled chicken The ruthenium fibers are slack, but when the free calcium of the immersion solution is increased to pCa 5 , an equal volume tension is produced. These fibers can be repeatedly shrunk and relaxed by switching between high and low calcium leaching solutions. The fiber is pre-cultured with the compound and then transferred to the high calcium solution of the compound to test the compound's ability to prevent the shrinkage of the chicken gill band. Secondly, the compound is added to the fiber that has been pre-cultured in the high-liquid contact, test compound Its ability to relax contracted fibers. Pre-experimental experiments to determine that the inhibitory effect is reversible, so the compound is unable to cause degeneration or other irreparable damage to smooth muscle myosin. &amp; The aforementioned dosage form is administered at a dose of sorrow. In general, the daily dose is from about 100 mg/kg of body weight, for example, from about 〇丨〇 to about 丨〇吆 or from about 0.15 to about 1 mg/k The weight of g. Thus, the dosage range for administration of the drug is from about 35 to about 7 days per day, for example from about 7 to about 700 mg per day, or from about 10 to about 100 mg per day. The activity to be administered = the amount of the product: when the treatment depends on the subject and disease state, the severity of the disease, the method of administration and time course, and the judgment of the medicinal physician; for example, 'oral administration' The dosage range can be administered intravenously from about 70 to about 7 strontium iron per day, and the dosage range can range from about 7 GG to about 7 gram per day. The active agent can select a longer neon (4) plasma half-life, respectively. The administration of the chemical can be via any acceptable mode of administration that provides similar utilization, including but not limited to oral, subcutaneous, 194 200823188 intravenous, intranasal intramuscular, intrapulmonary, vaginal, osmotic, Sublingual, intramucosal, intra-abdominal, intra-abdominal, parenteral, and intraocular (4) (including intraocular injection) °, ^7, σ7Κ is used to treat many of the pharmaceutically acceptable 纟10 described herein. 15 20 Forms, such as spinners, glues I "including solid, semi-solid, liquid and Aerosol sprays and the like. Chemicals, agents, liquids, suspensions, suppositories, gas administration 'including syringes ^=\including electrotransport in the form of continuous or controlled release doses. Patches, drops, etc., tablets, tablets Skin permeation (package or timed pulse administration. / analogy) is provided at a predetermined rate for extended and/or dosage forms. σ may be suitable for single administration of an accurate dose of a single pharmaceutical product, either alone or in combination with , lactose, house powder, hard moon:: Xiao pharmaceutical carrier or similar (such as mannose chain carboxymethyl cellulose, Portuguese, sodium, talc, cellulose, cross combination. If two to two gelatin, sucrose , magnesium carbonate and the like), such as ^, = = can also contain a second amount of non-toxic analogs (such as B _, _ /, increase, solvent, bismuth buffer and acid-like sorbitol s 2, r sodium, cyclodextrin derivatives, single laurel, sputum, triethanolamine acetate, triethanolamine oleate. In general, the composition may be from about 0.005% to 95% in accordance with the desired dosage, 舨啲,, .Q, 0/^, municipal nucleus. For example, at least a pharmaceutical product from about 5% to about 5% by weight. The actual method of preparing the transfusion form is known or known to those skilled in the art, for example, see East Mt Publishing Company, Easton, Pennsylvania.

Remington’s Phannaceutical 。醫藥組合物亦指醫 藥調配物。 曰― 195 200823188 此外，化學品可與其他藥劑、醫藥劑、佐劑及類似物 -共同投予，及醫藥組合物可包括其他藥劑、醫藥劑、佐劑 及類似物。 在特定實施例中，組合物可為片劑或錠劑形式並含有 活性成份、一或多種稀釋劑例如乳糖、蔗糖、磷酸氫鈣及 類似物品；潤滑劑例如硬脂酸鎂或類似物；及結著劑例如 ’又粉、阿拉伯膠、聚乙烯吡咯啶、明膠、纖維素、纖維素 衍生物或類似物。在另一種固體劑型中，散劑、丸劑、溶 10 15 20 液或懸浮液(例如溶於碳酸丙烯酯、蔬菜油或三酸甘油酯) 可包膠於明膠膠囊中。 風液體醫藥組合物，例如可藉由溶解或分散至少一種, 學品及一或多種視需要之醫藥佐劑於載劑中（例如水、/ =水、、葡萄糖水溶液、甘油、二醇、乙醇及類似物）形) Γί懸浮液二我射劑可製備成習用形式，如液態溶 液、如乳液，或在注射前適合溶解或懸浮於液體1 幸巫，形式。包含於此等非經腸組合物中之化學品百分ί 定。考以及化學品活性和施用者需求r 性成吏用溶液中範圍，從約ο.οι%至約ι〇%之； 固體時可使帛i右組合物為賴將轉成上述百分比^ 液，組合物-包含至少—磁 内、眼周及目:品^組合物可以眼内給藥（包細 益 組合物典型址或'、和灌注）。當以眼内給藥時， -水溶液。可加入適合的緩衝系統以預 196 200823188 儲存的狀況下pH變動。當在眼内手術的過程中給藥時， 例如眼球後-或眼周注射及眼内灌注或注射，使用平衡鹽沖 洗溶液可能是必須的。當用於多劑量形式時，可能需要防 腐劑以預防使用期間之微生物污染。 包含至少一種化學品之組合物亦可局部給藥作為眼 邛滴劑、眼部沖洗劑、乳劑、軟膏、凝膠及喷劑。當作為 眼部滴劑或眼部沖洗劑給藥時，活性成份典型地係溶於或 懸浮於適合的載劑中，典型的為無菌水性溶劑。可加入適 合的緩衝系統以預防在儲存的狀況下pH變動。當用於多 劑量形式時，可能需要防腐劑以預防使用期間之微生物污 染。 / 包含至少一種化學品之組合物亦可以氣霧或氣霧器 之溶液或為吹入之細微粉末，單獨或與惰性載劑（例如乳 糖）組合投至呼吸道中。組合物之顆粒典型地具有低於5〇 微米之直徑，低於10微米。 —般而言，將本文所述之化學品應用於篩選平滑肌肌 凝蛋白結合之方法_，平滑肌肌凝蛋白係與載體結合並將 至少一種化學品加到分析中。另外，化學品可與載體結合 並加入平滑肌肌凝蛋白。化合物種類中可尋求的新穎結合 劑包括專一抗體、化學庫篩選中辨識之非天然結合劑、胜 肽類似物等。其中特別有利的為對人類細胞具有低毒性之 候&amp;制之篩選分析。廣泛的各種不同分析可用於此目的， 包括活體外標定的蛋白質-蛋白質結合分析、電泳位移分 析、蛋白質結合之免疫分析、功能性分析(磷酸化分析等） 197 200823188 及類似物。參見，例如美國專利第6,495,337號。 【實施方式】 實例 5 下列實例係用於更完全描述使用本發明之方法。這些 實例係用作說明目的，且不應用於限制本發明之真正範 圍0 實例1 :Remington’s Phannaceutical. Pharmaceutical compositions are also referred to as pharmaceutical formulations.曰 ― 195 200823188 In addition, the chemical may be administered together with other pharmaceutical agents, pharmaceutical agents, adjuvants and the like, and the pharmaceutical composition may include other pharmaceutical agents, pharmaceutical agents, adjuvants and the like. In a particular embodiment, the composition may be in the form of a tablet or lozenge and contain the active ingredient, one or more diluents such as lactose, sucrose, calcium hydrogen phosphate, and the like; a lubricant such as magnesium stearate or the like; The binding agent is, for example, 'powder, gum arabic, polyvinylpyrrolidine, gelatin, cellulose, cellulose derivatives or the like. In another solid dosage form, a powder, a pill, a solution or suspension (e.g., dissolved in propylene carbonate, vegetable oil or triglyceride) may be encapsulated in a gelatin capsule. A liquid liquid pharmaceutical composition, for example, by dissolving or dispersing at least one, a chemical, and one or more optional medical adjuvants in a carrier (eg, water, /=water, aqueous dextrose, glycerol, glycol, ethanol) And the like))) The sputum suspension can be prepared into a conventional form, such as a liquid solution, such as an emulsion, or a form suitable for dissolution or suspension in a liquid prior to injection. The percentage of chemicals contained in such parenteral compositions. The test and the chemical activity and the applicator's demand range from about ο.οι% to about ι〇%; when solid, the 组合i right composition can be converted into the above percentage liquid, The composition - comprising at least - magnetic, periocular, and ocular compositions - can be administered intraocularly (typically or ', and perfused with the composition of the composition). When administered intraocularly, - aqueous solution. A suitable buffer system can be added to pre- 196 200823188 storage conditions for pH changes. When administered during intraocular surgery, such as post-ocular or periocular injections and intraocular perfusion or injection, it may be necessary to use a balanced salt wash solution. When used in multiple dosage forms, a preservative may be required to prevent microbial contamination during use. Compositions comprising at least one chemical may also be administered topically as eye drops, eye rinses, creams, ointments, gels and sprays. When administered as an eye drop or ophthalmic rinse, the active ingredient is typically dissolved or suspended in a suitable carrier, typically a sterile aqueous solvent. A suitable buffer system can be added to prevent pH changes under storage conditions. When used in multiple dosage forms, a preservative may be required to prevent microbial contamination during use. The composition comprising at least one chemical may also be administered to the respiratory tract either as a solution of an aerosol or aerosol or as a fine powder for insufflation, alone or in combination with an inert carrier such as lactose. The particles of the composition typically have a diameter of less than 5 Å microns and less than 10 microns. In general, the chemicals described herein are applied to the method of screening for smooth muscle myosin binding. The smooth muscle myosin binds to the carrier and adds at least one chemical to the assay. Alternatively, the chemical can be combined with a carrier and added to smooth muscle myosin. Novel binders that can be sought in the class of compounds include specific antibodies, non-natural binding agents identified in chemical library screening, peptide analogs, and the like. Of particular interest are screening assays that have low toxicity to human cells. A wide variety of different assays are available for this purpose, including in vitro calibrated protein-protein binding assays, electrophoretic displacement assays, immunoassays for protein binding, functional assays (phosphorylation assays, etc.) 197 200823188 and the like. See, for example, U.S. Patent No. 6,495,337. [Embodiment] Example 5 The following examples are intended to more fully describe the method of using the present invention. These examples are for illustrative purposes and are not intended to limit the true scope of the invention. Example 1:

10 6-(2-氣基苯基)-2-(3 -氣苯乙基胺基)-Ν-(σ比咬-3-基曱基）於驗酸胺 方法A :10 6-(2-Alkylphenyl)-2-(3- gasphenethylamino)-indole-(σ ratio -3-ylindenyl) in acid amine Method A:

於2,6-二氯菸鹼酸(50g，0.26 mol)之曱醇(250 mL)溶液 15 中緩慢地加入亞硫酿氯(22.7 mL，0.312 mol)。將混合物回 流4小時並濃縮，得到2,6-二氯於驗酸曱醋之定量產率白 色固體。 198 200823188Thionite-brewed chlorine (22.7 mL, 0.312 mol) was slowly added to a solution of 2,6-dichloronicotinic acid (50 g, 0.26 mol) in methanol (250 mL). The mixture was refluxed for 4 hours and concentrated to give a quantitative yield of 2,6-dichloro acid as a white solid. 198 200823188

將2,6-二氯菸鹼酸曱酯（53.3g，0·26ιηο1)、3-氟苯乙基 胺（37·3 mL，0·29 mol)、K2C03 (72 g 0·52 mol)及 ΝΜΡ(150 mL)之混合物於l〇〇°C攪拌10小時。將混合物以乙酸乙酯 5 (2 X 300 mL)稀釋並以鹽水清洗。將有機層組合，乾燥 (MgSCU)並濃縮。將殘餘物使用己烷-EtOAc (9 : 1)為溶離 劑以梦膠層析純化’得到6-氣-2-(3-鼠苯乙基胺基)終驗酸 曱酯之白色固體(44 g5 54%)。LRMS (M+H+) m/z 309.0。2,6-dichloronicotinic acid decyl ester (53.3 g, 0·26ιηο1), 3-fluorophenethylamine (37·3 mL, 0·29 mol), K2C03 (72 g 0·52 mol) and A mixture of hydrazine (150 mL) was stirred at 10 ° C for 10 hours. The mixture was diluted with ethyl acetate 5 (2×300 mL) and washed with brine. The organic layers were combined, dried (MgSCU) and concentrated. The residue was purified by EtOAc-EtOAc (EtOAc (EtOAc) (EtOAc) G5 54%). LRMS (M+H+) m/z 309.0.

將6-氯-2-(3-氟苯乙基胺基)菸鹼酸曱酯氯化物（30.8 g, 0.1 mol)、2-氰基苯基硼酸（17.6 g，0.12 mol)、 PdCl2(dppf)2(3.6 g，5·0 mmol)、K2C03 (41·4 g，0·3 mol)及無 水DMF(l〇〇 mL)之混合物以氮脫氣30分鐘。然後將混合 物於100°C攪拌2小時。將混合物以矽藻土過濾並以EtOAc 15 清洗。將濾液以EtOAc稀釋，以鹽水清洗並濃縮至乾。將 殘餘物使用己烷-EtOAc (4 : 1)為溶離劑以矽膠快速層析純 化，得到所欲產物6-(2-氰基苯基)-2-(3-氟苯乙基胺基)菸鹼 酸曱酯之黃色固體(31 g，82%)。LRMS(M+H+)m/z 376.1。 199 2008231886-Chloro-2-(3-fluorophenethylamino) nicotinic acid decyl chloride (30.8 g, 0.1 mol), 2-cyanophenylboronic acid (17.6 g, 0.12 mol), PdCl2 (dppf) A mixture of 2 (3.6 g, 5·0 mmol), K2C03 (41·4 g, 0·3 mol) and anhydrous DMF (10 mL) was degassed with nitrogen for 30 minutes. The mixture was then stirred at 100 ° C for 2 hours. The mixture was filtered over celite and washed with EtOAc. The filtrate was diluted with EtOAc, washed with brine and EtOAc evaporated. The residue was purified by flash chromatography using hexane-EtOAc (4:1) elute Yellow solid nicotinic acid ester (31 g, 82%). LRMS (M+H+) m/z 376.1. 199 200823188

於甲醋6-(2-氰基苯基)-2-(3-氟苯乙基胺基)辂驗酸甲 酯（15 g，40 mmol)、曱醇(80 mL)及 THE (80 mL)混合物中 加入3NNaOH (40 mL)。將混合物於室溫攪拌16小時。將 混合物以2N HC1調整至pH 7。濃縮橫將殘餘物之水溶液 以2N HC1(10 mL)酸化至pH3，得到6-(2_氰基苯基)_2-(3_ 氟苯乙基胺基）菸鹼酸甲酯（14.5 g，100%)之黃色固體。 LRMS (M+H+) m/z 362.1。Methyl 6-(2-cyanophenyl)-2-(3-fluorophenethylamino)-methylacetate (15 g, 40 mmol), methanol (80 mL) and THE (80 mL) 3N NaOH (40 mL) was added to the mixture. The mixture was stirred at room temperature for 16 hours. The mixture was adjusted to pH 7 with 2N HCl. The concentrated aqueous solution of the residue was acidified to pH 3 with 2N EtOAc (10 mL) to afford 6-(2-cyanophenyl)-2-(3-fluorophenylethylamino) nicotinic acid methyl ester (14.5 g, 100 %) yellow solid. LRMS (M+H+) m/z 362.1.

ίο 於6-(2-氰基苯基)-2-(3 -氟苯乙基胺基)於驗酸甲酯（2.8 g，7.76 mmol)之 DMF (28 mL)混合物中加入 HBTU (5.88 g， 15.51 mmol)、H〇Bt(2.1 g，15.51 mmol)然後 3-胺基甲基口比 口定(1·68 g，15.51 mmol)。將反應混合物於室溫擾拌1小時。 將粗產物使用乙腈及Ηβ混合物於RP-HPLC上純化，得 15 到6-(2-氛基苯基)-2·(3-氟苯乙基胺基基甲基) 菸鹼醯胺之淡黃色固體。LRMS(M+H+)m/z 452.2。 200 200823188 方法B :Ίο 6-(2-Cyanophenyl)-2-(3-fluorophenethylamino) was added to a mixture of methyl acetate (2.8 g, 7.76 mmol) in DMF (28 mL). , 15.51 mmol), H〇Bt (2.1 g, 15.51 mmol) then 3-aminomethyl port (1·68 g, 15.51 mmol). The reaction mixture was stirred at room temperature for 1 hour. The crude product was purified by RP-HPLC using acetonitrile and a mixture of Ηβ to give 15 to 6-(2-aminophenylphenyl)-2·(3-fluorophenethylaminomethyl) nicotinic acid Yellow solid. LRMS (M+H+) m/z 452.2. 200 200823188 Method B:

將酸2,6-二氯菸鹼酸(19.2 g，0.1 mol)、N，N’-羰基二咪 唑（CDI，17.8 g，0.11 mmol)及 THE (1 L)之混合物於 60°C 攪 5 拌30分鐘並冷卻至室溫。於混合物中加入3-胺基甲基σ比 啶（10.2 mL，0.1 mol)及 DIEA(21 mL，0.12 mol)。將反應混 合物於室溫攪拌4小時，並以EtOAc稀釋。將有機層以 H20、鹽水清洗，以Na2S04乾燥。將有機溶液濃縮得到 2,6-二氯(吡啶-3-基曱基)菸鹼醯胺(20.5 g，73%)。LRMS ίο (M+H+) m/z 282.0 ； (M+2+H+) m/z 283.9 °Mixing 2,6-dichloronicotinic acid (19.2 g, 0.1 mol), N,N'-carbonyldiimidazole (CDI, 17.8 g, 0.11 mmol) and THE (1 L) at 60 ° C Mix for 30 minutes and cool to room temperature. To the mixture were added 3-aminomethyl-pyridinium (10.2 mL, 0.1 mol) and DIEA (21 mL, 0.12 mol). The reaction mixture was stirred at room temperature for 4 h and diluted with EtOAc. The organic layer was washed with H.sub.2, brine and dried over Na2SO. The organic solution was concentrated to give 2,6-dichloro(pyridin-3-ylmercapto)nicotinamine (20.5 g, 73%). LRMS ίο (M+H+) m/z 282.0 ; (M+2+H+) m/z 283.9 °

將2,6_二氯-N_(口比口定-3-基甲基)於驗醯胺(20.4 g，72.32,6-Dichloro-N_ (mouth ratio -3-methyl group) was tested on guanamine (20.4 g, 72.3

mmol)、3-氟苯乙基胺（η 1 g，79.5 mmol)、K2CO3(20 g 145 mmol)及DMF(200mL)混合物於l〇〇°C攪拌l〇小時。將混 合物以乙酸乙酯（2 X 300 mL)稀釋，並以飽和的氯化銨、 碳酸氫鈉及鹽水清洗。將有機層組合，乾燥（MgS04)並濃 縮。將殘餘物以矽膠層析純化，得到6_氯_2_(3_氟苯乙基 胺基㈣十比啶各基曱基）於鹼醯胺（12.6 g，46%^LRMS (M+H+) m/z 385.1 〇 201 200823188A mixture of mmol), 3-fluorophenethylamine (η 1 g, 79.5 mmol), K 2 CO 3 (20 g 145 mmol) and DMF (200 mL) was stirred at 10 ° C for 1 hour. The mixture was diluted with ethyl acetate (2×300 mL) and washed with sat. aq. sodium chloride, sodium hydrogen carbonate and brine. The organic layers were combined, dried (MgS04) and concentrated. The residue was purified by silica gel chromatography to give 6-chloro-2-(3-fluorophenylethylamino(tetra)-pyridinyl fluorenyl) to decylamine (12.6 g, 46%^LRMS (M+H+) m/z 385.1 〇201 200823188

將6_氯-2_(3_氟苯乙基胺基)-N七比啶-3-基曱基)於鹼 醯胺（1·0 g，2.6 mmol)、2-氰基苯基硼酸(460 mg，3.12 mmol)、PdCl2(dppf)2(140 mg，0·26 mmol、K2CO3(1.08 g，7·8 5 mmol)及無水DMF(8 mL)之混合物以氮脫氣分鐘。然後 將混合物於125°C攪拌1小時。將混合物經由矽藻土過濾 並以EtOAc清洗。將濾液濃縮至乾並以快速矽膠層析純 化，得到所欲產物6-(2-氰基苯基）-2-(3-氟苯乙基胺 基）-N_(吡啶_3_基甲基）菸鹼醯胺之淡黃色固體（740 mg， ίο 63%)。LRMS (M+H+) m/z 452·1。 實例2 :6-Chloro-2_(3-fluorophenethylamino)-N-7-pyridin-3-ylindenyl) to a base amide (1·0 g, 2.6 mmol), 2-cyanophenylboronic acid ( a mixture of 460 mg, 3.12 mmol), PdCl2 (dppf) 2 (140 mg, 0·26 mmol, K2CO3 (1.08 g, 7.8 mmol) and anhydrous DMF (8 mL) was degassed with nitrogen for a few minutes. The mixture was stirred for 1 hour at 125 ° C. The mixture was filtered over EtOAc EtOAc (EtOAc) (3-fluorophenethylamino)-N-(pyridine-3-ylmethyl) nicotinamide as a pale yellow solid (740 mg, ίο 63%). LRMS (M+H+) m/z 452·1 Example 2:

Ν-((2-(胺基甲基广比咬-3-基）甲基)-6-(2-氰基苯基)-2-(3-氟苯 乙基胺基）菸鹼醯胺Ν-((2-(Aminomethyl-methyl-butyl-3-yl)methyl)-6-(2-cyanophenyl)-2-(3-fluorophenylethylamino)nicotinamide

NeOH/THF 0°CNeOH/THF 0°C

於置於3-頸圓底燒瓶之2-溴菸鹼醛(50 g，0·27 mol)、 202 200823188 甲醇(250 mL)及THF (250 mL)混合物中於0°C逐滴加入硼 氳化鈉（10.3 g，0.27 mol)。將反應混合物於0°C攪拌1 _小時 回溫至室溫。將反應混合物以2N HC1(120 mL)調整至pH 7，並濃縮移除曱醇及THF。將生成的混合物置於EtOAc 及鹽水間分溶三次。將有機層組合並以鹽水清洗，以 Na2S04乾燥乾燥並濃縮，得到(2-溴吼啶-3-基）曱醇(51 g)， 其使用時不需進一步純化。LRMS (M+H+) m/z 187·9。Boron was added dropwise at 0 ° C in a mixture of 2-bromonicotinaldehyde (50 g, 0·27 mol), 202 200823188 methanol (250 mL) and THF (250 mL) in a 3-neck round bottom flask. Sodium (10.3 g, 0.27 mol). The reaction mixture was stirred at 0 ° C for 1 hr and warmed to room temperature. The reaction mixture was adjusted to pH 7 with 2N EtOAc (120 mL) and concentrated to remove methanol and THF. The resulting mixture was partitioned three times between EtOAc and brine. The organic layers were combined and washed with brine, dried EtOAc EtOAc EtOAc EtOAc LRMS (M+H+) m/z 187·9.

於(2-溴吡啶-3-基）甲醇(51 g，0·27 mol)、酞醯亞胺(47.6 g，0·32 mol)、三苯基膦（83.8 g，0.32 mol)及 THE (60 mL)混 合物中於0°C逐滴加入DIAD (62 mL，0.32 mol)。讓反應 混合物升溫至室溫並攪拌1小時。將形成的沉澱過濾並以 EtOAc (50 mL)清洗。得到的固體2-((2-溴吡啶-3-基）甲基) 異吲哚啉-1，3-二酮（50.2 g，59%)直接用於下個步驟不需進 一步純化。LRMS (M+H+) m/z 317.1。(2-Bromopyridin-3-yl)methanol (51 g, 0·27 mol), quinone imine (47.6 g, 0·32 mol), triphenylphosphine (83.8 g, 0.32 mol) and THE ( DIAD (62 mL, 0.32 mol) was added dropwise to the mixture at 0 °C. The reaction mixture was allowed to warm to room temperature and stirred for 1 hour. The formed precipitate was filtered and washed with EtOAc (50 mL). The obtained solid 2-((2-bromopyridin-3-yl)methyl)isoindoline-1,3-dione (50.2 g, 59%) was used directly in the next step without further purification. LRMS (M+H+) m/z 317.1.

將溴2_((2_溴吡啶_3_基）甲基）異吲哚啉_1，3_二酮(5〇 g， 0·16 mol)、Zn(CN)2(37.4 g，0.32 mol)、Pd(PPh3)4(18.5 g5 16 203 200823188 mmol)及DMF(160 mL)之混合物以氮脫氣10分鐘，然後於 10〇。〇.攪拌3小時。將混合物以矽藻土過濾並以DMF清 洗。將組合的濾液以EtOAc稀釋，以水、鹽水清洗，乾燥 (Na2S04)並濃縮。將殘餘物以二氯曱烷濕磨，得到所欲產 5 物3-((1,3-二氧基異吲哚啉-2-基）曱基）氰基吼啶之灰白色 固體（35 g，83%)。LRMS (M+H+) m/z 264.0。Bromo 2_((2-bromopyridine-3-yl)methyl)isoindoline_1,3-dione (5〇g, 0·16 mol), Zn(CN)2 (37.4 g, 0.32 mol) A mixture of Pd(PPh3)4 (18.5 g5 16 203 200823188 mmol) and DMF (160 mL) was degassed with nitrogen for 10 minutes and then at 10 Torr. 〇. Stir for 3 hours. The mixture was filtered through celite and washed with DMF. The combined filtrate was diluted with EtOAc (EtOAc)EtOAc. The residue was triturated with methylene chloride to give the desired product, 3-((1,3-dioxyisoindolin-2-yl)indenyl) cyano acridine as a white solid (35 g , 83%). LRMS (M+H+) m/z 264.0.

於3_((1，3_二氧基異^弓卜朵琳-2-基）甲基）氮基σ比口定（10 g， 38 mmol)及甲醇(80 mL)混合物中加入濃HC1(6.5 mL，76 ίο mmol)及10%Pd/C(l g)。將混合物於50PsiH2下劇烈攪拌 6小時。將混合物以矽藻土墊過濾並以曱醇清洗。將組合 的濾液濃縮，得到2-((2-(胺基曱基)吼啶-3-基）曱基）異吲 哚啉-1，3_二酮之定量產率白色固體。LRMS (M+H+) m/z 268·卜Concentrated HC1 was added to a mixture of 3_((1,3-dioxyiso-oxabendolin-2-yl)methyl)nitrosyl σ (1 g, 38 mmol) and methanol (80 mL). 6.5 mL, 76 ίο mmol) and 10% Pd/C (lg). The mixture was vigorously stirred at 50 PsiH 2 for 6 hours. The mixture was filtered through a pad of celite and washed with methanol. The combined filtrate was concentrated to give 2-((2-(aminomercapto) acridine-3-yl)indolyl)isoindole porphyrin-1,3-dione as a quantitative white solid. LRMS (M+H+) m/z 268·b

15 於2-((2-(胺基曱基）吼啶各基）曱基）異吲哚啉-l，3-二 酮 HC1 鹽（44.5 g，0.13 mol)、THE (230 mL)及 H20 (230 mL) 混合物中於0oC加入NaHC〇3(36 g，0.43 mol)，然後加入 Boc20(31.4 g，0.144 mol)。讓混合物升溫至室溫並攪拌2 204 200823188 小日寸。將混合物以乙酸乙酯（2〇〇 mL)稀釋，以水、鹽水清 洗，乾燥並濃i宿。將殘餘物以Et〇Ac(15〇mL)濕磨，得到 所欲產物之白色固體(30g，63%)。將Et〇Ac溶液使用己烷 -EtOAc(l : 1)為溶離劑以矽膠快速層析純化，得到第二部 分之(3_((1，3·二氧基異吲哚啉_2_基）甲基)σ比啶_2_基）甲基胺 曱酸第三丁酯（13.5 g，28%)。LRMS (M+H+)m/z 368.1。15 2-((2-(Aminocarbonyl) acridine each) fluorenyl)isoindoline-l,3-dione HC1 salt (44.5 g, 0.13 mol), THE (230 mL) and H20 (230 mL) NaHC〇3 (36 g, 0.43 mol) was added at 0 °C, then Boc20 (31.4 g, 0.144 mol) was added. Allow the mixture to warm to room temperature and stir 2 204 200823188 small days. The mixture was diluted with ethyl acetate (2 mL), washed with water and brine, dried and concentrated. The residue was triturated with EtOAc (EtOAc) (EtOAc) The Et〇Ac solution was purified by flash chromatography using hexane-EtOAc (1:1) as a solvent to obtain the second part (3-((1,3·dioxyisoindoline-2-yl)) Methyl) σpyridin-2-yl)methylamine decanoate tert-butyl ester (13.5 g, 28%). LRMS (M+H+) m/z 368.1.

於(3-((1 ’3- —乳基異ϋ弓卜朵琳-2-基）甲基)〇比°定-2-基）甲基 胺曱酸第三丁酯（30 g，81 mmol)之MeOH (450 mL)溶液中 於0°C加入肼(25 mL，810 mmol)。讓混合物升溫至室溫並 攪拌至隔夜。將沉澱濾出並濃縮至乾。將殘餘物以二氯甲 烷(500 mL)濕磨並過濾。將濾液濃縮，得到定量產率之 (3-(胺基曱基）吡啶-2-基）甲基胺曱酸第三丁酯（18.7g)。 LRMS (M+H+) m/z 238·卜((3-((1 '3-)-based yttrium oxazolidine-2-yl)methyl) 〇 ° 基-2-yl)methylamine decanoic acid tert-butyl ester (30 g, 81 A solution of mmol (25 mL, 810 mmol) was added at EtOAc. The mixture was allowed to warm to room temperature and stirred until overnight. The precipitate was filtered off and concentrated to dryness. The residue was triturated with methylene chloride (500 mL) and filtered. The filtrate was concentrated to give (3-(aminomercapto)pyridin-2-yl)methylamine decanoic acid tert-butyl ester (18.7 g). LRMS (M+H+) m/z 238·b

於6-(2-氰基苯基)-2-(3-氟苯乙基胺基)菸鹼酸(0.60 g， 1·66 mmol)之 DMF (3 mL)混合物中加入 DIEA(0.329 mL， 2·53 mmol)、HBTU (0.756 g，2·00 mmol)，然後(3-(胺基曱 基)吡啶-2-基）曱基胺曱酸第三丁酯（0.473 g，2·11 mmol)。 205 200823188 將反應混合物於室溫擾摔1小時。將粗混合物使用乙猜及 H20混合物於RP-HPLC上純化，得到（3-((6_-(2-氰基苯 基)-2-(3-氟苯乙基胺基）菸鹼酸醯胺基）甲基）吼啶-2-基）甲 基胺甲酸第三丁酯之淡黃色固體（545 mg，57%)。LRMS 5 (M+H+) m/z 581·3 〇Add DIEA (0.329 mL, a mixture of 6-(2-cyanophenyl)-2-(3-fluorophenethylamino)nicotinic acid (0.60 g, 1.66 mmol) in DMF (3 mL) 2·53 mmol), HBTU (0.756 g, 2·00 mmol), then (3-(aminomercapto)pyridin-2-yl)decylamine decanoic acid tert-butyl ester (0.473 g, 2·11 mmol) ). 205 200823188 The reaction mixture was scrambled at room temperature for 1 hour. The crude mixture was purified by RP-HPLC using a mixture of EtOAc and H20 to give (3-((6--(2-cyanophenyl)-2-(3-fluorophenethylamino)) nicotinic acid decylamine A pale yellow solid (545 mg, 57%) of the dimethyl succinimide. LRMS 5 (M+H+) m/z 581·3 〇

於(3-((6-(2-氰基苯基)-2-(3-氟氟乙基胺基）於鹼醯胺) 曱基户比啶-2-基）甲基胺曱酸第三丁酯（737 mg，1.27 mmol) 之甲醇(6 mL)溶液中於〇°c加入4M HC15 1，4-二噁烷(3 1〇 mL)溶液。讓混合物升溫至室溫並攪拌至2小時。將混合 物濃縮，接著使用乙腈及H20混合物於RP-HPLC上純化， 得到N-((2_(胺基曱基）π比啶_3_基）甲基）冬氰基苯 基)-2-(3-氟苯乙基胺基）菸鹼醯胺之淡黃色固體（545 89%)。LRMS (M+H+) m/z 481.2。 4 15 實例3 :((3-((6-(2-Cyanophenyl)-2-(3-fluorofluoroethylamino))) 醯 户 户 -2- -2- 基 基 基 基 基 ) ) 第 第A solution of tributyl acrylate (737 mg, 1.27 mmol) in methanol (6 mL) was added EtOAc EtOAc EtOAc EtOAc. The mixture was concentrated, and then purified by RP-HPLC using acetonitrile and H20 mixture to give N-((2-(amino fluorenyl) π-pyridyl-3-yl)methyl)-cetylphenyl)-2 - (3-Fluorophenethylamino) nicotinic acid amide as a pale yellow solid (545 89%). LRMS (M+H+) m/z 481.2. 4 15 Example 3:

N-(2-胺基I氧基乙基XL氰基苯基)卻_氟苯乙基胺基)於驗酿胺 206 200823188N-(2-Amino Ioxyethyl XL cyanophenyl) but _fluorophenethylamino) in the amine II 206 200823188

化合物Ν·(2-胺基-2-氧基乙基)-6-(2-氰基苯基)-2·(3- 氟苯乙基胺基)菸鹼酿胺係由6_(2-氰基苯基)-2-(3-氟苯乙 基胺基)於鹼酸及適合的胺2-胺基乙醯胺，根據實例1(方 法A)之製備製程所製備。LRMS (M+H+)m/z418.1。 實例4 :The compound Ν·(2-amino-2-oxyethyl)-6-(2-cyanophenyl)-2·(3-fluorophenethylamino)nicotinamide is composed of 6_(2- Cyanophenyl)-2-(3-fluorophenethylamino) is prepared according to the preparation procedure of Example 1 (Method A) from the base acid and the appropriate amine 2-aminoacetamide. LRMS (M+H+) m/z 418.1. Example 4:

⑻-N-((H4-胺基丁醯基)吡咯啶_2_基)曱基氰基苯基)_2_(3_氟苯乙基胺基)於鹼醯胺(8)-N-((H4-Aminobutyryl)pyrrolidinyl-2-yl)decylcyanophenyl)_2_(3-fluorophenethylamino) in amide

於RB燒瓶中之6-(2-氰基苯基)-2-(3-氟苯乙基胺基) 於驗酸(510 mg，1.41 mmol)、（R)-2-(胺基曱基)口比口各咬-1-缓 酸第三丁酯（424 mg5 2.11 mmol)、HOBT (285 mg，2.11 mmol)及HBTU (800 mg5 2.11 mg)混合物中力口入DMF並將 混合物於室溫攪拌1小時。LC/MS顯示反應完成，將混合 207 15 200823188 物過濾並使用乙腈及水混合物於Rp-hplc上純化，得到 (R)-2-((6-(2-氰基苯基)-2-(3-氟苯·乙基胺基)菸鹼醯胺）曱基) 吡咯啶-1-羧酸第三丁酯（695.1 mg5 91%)。LRMS (Μ +H+)6-(2-Cyanophenyl)-2-(3-fluorophenethylamino) in an RB flask. Acid (510 mg, 1.41 mmol), (R)-2-(amino) fluorenyl ) mouth-to-mouth bite 1-butylic acid tert-butyl ester (424 mg5 2.11 mmol), HOBT (285 mg, 2.11 mmol) and HBTU (800 mg5 2.11 mg) mixture into DMF and mix the mixture at room temperature Stir for 1 hour. LC/MS showed the reaction was completed, mixture 207 15 200823188 was filtered and purified using acetonitrile and water mixture on Rp-hplc to give (R)-2-((6-(2-cyanophenyl)-2-( 3-fluorophenylethylamino)nicotinium amide fluorenyl) pyrrolidine-1-carboxylic acid tert-butyl ester (695.1 mg5 91%). LRMS (Μ +H+)

10 於(R)-2-((6-(2-氰基苯基)-2-(3-氟苯乙基胺基）菸鹼酸 酉蓝胺）曱基）σ比咯咬-1-叛酸第三丁酯（680 mg，1.25 mmol)之 MeOH(20 mL)溶液中加入 HC1(2.0 mL，8 mmol，4M 之二噪 烷溶液）。將反應於室溫攪拌2小時。LC/MS顯示反應完 成。將混合物於減壓下濃縮，得到6-(2-氰基苯基)-2-(3-氟 苯乙基胺基)-N-(吼咯啶-2-基甲基)菸鹼醯胺鹽酸鹽，其使 用時不需進一步純化。LRMS (M+H+)m/z444.2。10(R)-2-((6-(2-Cyanophenyl)-2-(3-fluorophenethylamino)nicotinic acid indigoamine) sulfhydryl) σ ratio -1- Add HCl (2.0 mL, 8 mmol, 4 M dioxane solution) to a solution of dec. The reaction was stirred at room temperature for 2 hours. LC/MS showed the reaction was completed. The mixture was concentrated under reduced pressure to give 6-(2-cyanophenyl)-2-(3-fluorophenethylamino)-N-(puropiperidin-2-ylmethyl)nicotinate The hydrochloride salt was used without further purification. LRMS (M+H+) m/z 444.2.

NHBoc F 於6-(2-氰基苯基)-2-(3-氟苯乙基胺基)-N十比咯啶_2一 基曱基)於驗酿胺鹽酸鹽(95 mg, 0.2 mmol)、4-(第三丁氧基 幾基胺基）丁酸（61 mg，0.3 mmol)、HOBT(41 mg，〇·3 mmol) 及 HBTU(114 mg，0·3 mmol)混合物中加入 DMF(l.〇 mL)及 DIEA(0.1 mL，0.6 mmol)。將反應混合物於室溫擾拌i小 時。LC/MS顯示反應完成。然後將反應混合物過濾、並將淚 208 15 200823188 液使用乙腈及水混合物於RP-HPLC上純化，得到 4-(2-((6-(2-鼠基苯基)-2-(3 -氟苯乙基胺基）於驗酿胺基）甲 基）ϋ比咯咬-1-基）-4-氧基丁基胺甲酸第二丁 S旨（81.2 mg， 65%) 〇 LRMS (Μ +H+) m/z 629·2。NHBoc F in 6-(2-cyanophenyl)-2-(3-fluorophenethylamino)-N-decapyridin-2-ylindenyl) 0.2 mmol), 4-(t-butoxymethylamino)butyric acid (61 mg, 0.3 mmol), HOBT (41 mg, 〇·3 mmol) and HBTU (114 mg, 0.3 mmol) DMF (1. 〇 mL) and DIEA (0.1 mL, 0.6 mmol) were added. The reaction mixture was stirred at room temperature for 1 hour. LC/MS showed the reaction was completed. The reaction mixture was then filtered and the 208 15 200823188 solution was purified on RP-HPLC using acetonitrile and water mixture to afford 4-(2-((6-(2--)----- Phenylethylamine) in the presence of amido)methyl)pyrazine-1-yl)-4-oxobutylaminecarboxylic acid second butyl S (81.2 mg, 65%) 〇LRMS (Μ + H+) m/z 629·2.

於4-(2-((6-(2 -氣基苯基)-2-(3-氣苯乙基胺基）於驗酸 胺基）甲基）吼咯啶-1-基）-4-氧基丁基胺曱酸第三丁酯（71 mg，0.11 mmol)之 MeOH (5.0 mL)溶液中加入 HC1(1.0 mL， 4 mmol，4M之二噁烷溶液）。將反應混合物於室溫攪拌2 小時。LC/MS顯示反應完成。將反應混合物於減壓下濃縮 並將粗產物使用乙腈(0.1% TFA)及水(0.1% TFA)混合物於 RP-HPLC上純化，得到；胺|丁酿基）口比 甲基)-6-(2•氰基苯基)-2-(3-氟苯乙基胺基)菸鹼醯胺之淡黃 色固體(57·1 mg，68%)。LRMS (Μ +H+) m/z 529·2。 實例5 :4-(2-((6-(2-(Phenylphenyl))-2-(3-phenylphenethylamino))-acidic acid)methyl)pyridin-1-yl)-4 To a solution of oxybutylamine decanoic acid tert-butyl ester (71 mg, 0.11 mmol) in MeOH (5.0 mL) EtOAc (1 mL, EtOAc The reaction mixture was stirred at room temperature for 2 hours. LC/MS showed the reaction was completed. The reaction mixture was concentrated under reduced pressure and the crude material was purified using acetonitrile (0.1% TFA) and water (0.1% TFA). (2·Cyanophenyl)-2-(3-fluorophenethylamino)nicotinamide as a pale yellow solid (57·1 mg, 68%). LRMS (Μ +H+) m/z 529·2. Example 5:

(R)-6-(2-氣基苯基)-2-(3-氣苯乙基胺基)-1^-((5-氧基°比洛咬-2-基)甲基)於驗S&amp;胺 209 200823188 H0/，((R)-6-(2-carbophenyl)-2-(3-cephenethylamino)-1^-((5-oxyl-pyridyl-2-yl)methyl) Test S&amp;amine 209 200823188 H0/,(

DIAD, PPh3 HN3l THFDIAD, PPh3 HN3l THF

於（R)-5-(羥基甲基）吡咯啶-2-酮（660 mg，5.73 mmol)、疊氮化氫(10 8 mL，8·60 mmol，〇·8 Μ之曱苯溶液) 及PPh3 (2·25 g，8.60 mmol)之THE溶液中逐滴加入 DIAD。將混合物於室溫攪拌1小時。LCMS顯示反應完 成。將混合物部分濃縮，過濾並以RP-HPLC純化，得到 (R)-5_(疊氮基甲基)π比咯啶_2_酮(730 mg，87%，90%純度）。 LRMS (M+H+)m/z 141·卜(R)-5-(hydroxymethyl)pyrrolidin-2-one (660 mg, 5.73 mmol), hydrogen azide (10 8 mL, 8.60 mmol, 〇·8 曱 曱 benzene solution) DIHD was added dropwise to the PPh3 (2·25 g, 8.60 mmol) of THE solution. The mixture was stirred at room temperature for 1 hour. LCMS showed the reaction was completed. The mixture was partially concentrated, filtered and purified with EtOAc EtOAc EtOAc (EtOAc) LRMS (M+H+)m/z 141·b

Pd/C, H2 MeOHPd/C, H2 MeOH

於(R)-5-(疊氮基甲基比咯啶-2_酮（150 mg，1.07 mmol) 之MeOH溶液中加入Pd/C。將混合物置於殺菌釜中，脫氣 三次，通入30 psi的H2並於室溫下攪拌3〇分鐘。將混合 物過濾並將濾液減壓濃縮’得到(R)_5-(胺基甲基)α比咯u定-2_ 酮（92 mg，75%)。LRMS (Μ +Η+) m/z 115.1。Pd/C was added to a solution of (R)-5-(azidomethylpyrrolidin-2-one (150 mg, 1.07 mmol) in MeOH. The mixture was placed in a sterilizer and degassed three times. 30 psi of H2 and stirring at room temperature for 3 Torr. The mixture was filtered and the filtrate was concentrated under reduced pressure to afford (R) _5-(aminomethyl) s. s. LRMS (Μ +Η+) m/z 115.1.

於置於RB燒瓶中之6-(2-氰基笨基)_2_(3_氟苯乙基胺 基)於驗酸（110 mg，0.30 mmol)、（R)-5_(胺基曱基)σ比咯咬_2_ 酮（52 mg，0·46 mmol)、ΗΟΒΤ (62 mg，0·46 mmol)及 HBTU(174 mg，0.46 mg)混合物中加入DMF並將混合物於 210 200823188 室溫下攪拌1小時。LC/MS顯示反應完成及將混合物過濾 並使用乙腈及水混合物於Rp_HPLC上純化，得到 (R)_6_(2-氰基苯基)·2_(3-氟苯乙基胺基)-N-((5-氧基°比咯啶 -2·基）甲基)菸鹼酿胺(91·6 mg，67%)。LRMS (Μ +H+) nx/z 458.1 〇 實例6 :6-(2-Cyanophenyl)-2-(3-fluorophenethylamino) in an RB flask for acid verification (110 mg, 0.30 mmol), (R)-5-(amino fluorenyl) σ is added to the mixture of _2_ ketone (52 mg, 0·46 mmol), hydrazine (62 mg, 0.46 mmol) and HBTU (174 mg, 0.46 mg) and the mixture is stirred at 210 200823188 at room temperature. 1 hour. LC/MS showed the reaction was completed and the mixture was filtered and purified using EtOAc EtOAc EtOAc EtOAc EtOAc (5-oxyl-pyrrolidin-2-yl)methyl)nicotinamide (91·6 mg, 67%). LRMS (Μ +H+) nx/z 458.1 实例 Example 6:

(ΙΙ)·Ν·((1-(3-胺基丙基)_5_氧基^比咯啶_2_基）曱基)_6—(2_氰基苯基)_2-(3_氟苯 乙基胺基）於驗酸胺(ΙΙ)·Ν·((1-(3-Aminopropyl)_5_oxy^pyrrolidinyl-2-yl)indenyl)_6-(2-cyanophenyl)_2-(3_fluoro Phenylethylamine)

BocHNBocHN

Br^^^NHBoc NaH, DMFBr^^^NHBoc NaH, DMF

15 於 NaH(128 mg，3.21 mmol)之 DMF(5.0 mL)溶液中加 入(R)_5-(疊氮基曱基）吡咯啶-2-酮（300 mg，2·14 mmol)之 DMF(5.0 mL)溶液並於室溫下攪;掉30分鐘，接著加入3_ 溴丙基胺曱酸第三丁酯。將混合物加熱至60°C 2小時並以 飽和的NEUCl溶液進行驟冷。以EtOAc(50 mL X 2)萃取水 層以及將組合的有機層以鹽水清洗，以Na2S04乾燥，過 濾並減壓濃縮’得到（R)-3-(2-(疊氮基甲基)-5-氧基π比洛0定 -1-基）丙基胺曱酸第三丁酯（358 mg之粗產物），將其用於 211 200823188 下個步驟不需純化。LRMS (M+H+-Boc)m/z 198」。15 To a solution of NaH (128 mg, 3.21 mmol) in DMF (5.0 mL) was added (R)_5-(azidodecyl)pyrrolidin-2-one (300 mg, 2·14 mmol) DMF (5.0 The solution was stirred at room temperature for 30 minutes, followed by the addition of 3 - bromopropylamine decanoate. The mixture was heated to 60 ° C for 2 hours and quenched with a saturated NEUC1 solution. The aqueous layer was extracted with EtOAc (50 mL EtOAc)EtOAc. -oxy π piroxicam-l-yl) propylamine decanoic acid tert-butyl ester (358 mg of crude product) was used in 211 200823188. The next step did not require purification. LRMS (M+H+-Boc) m/z 198".

於(R)-3-(2-(疊氮基甲基)_5_氧基σ比咯啶基）丙基胺 甲-夂弟—^ 丁酉曰（300 mg，1 ·〇ΐ mmol)之MeOH溶液中加入MeOH of (R)-3-(2-(azidomethyl)_5-oxy σ-pyridyl)propylamine A-夂-- 酉曰(300 mg, 1 ·〇ΐ mmol) Add in solution

Pd/C。將混合物置於殺菌釜中，脫氣三次，通入3〇psi的 =亚於室溫下攪拌30分鐘。將混合物過濾並將濾液減壓 濃縮^得到(R)-3-(2-(胺基甲基)_5_氧基吡咯啶基）丙基胺 甲酸第二丁酯（180 mg之粒產物）。LRMS (Μ +H+) m/z 198·1。Pd/C. The mixture was placed in a retort, degassed three times, and passed through a 3 psi = sub-room temperature for 30 minutes. The mixture was filtered and the filtrate was concentrated under reduced pressure to give (D)-(2-(aminomethyl)-5-oxypyrrolidinyl)propylamine carboxylic acid as the butyl ester (180 mg of the product). LRMS (Μ +H+) m/z 198·1.

於置於RB燒瓶中之6_(2_氰基苯基)_2_(3_氟苯乙基胺 基)菸鹼酸（110 rng，0.30 mm〇1)、（R)冬(2-(胺基甲基)_5氧 基吼咯啶+基）丙基胺甲酸第三丁酯（125 mg，〇 46 mmol)、HOBT (107 mg，0·46 mmol)及 HBTU (174 mg，0·46 mg)混合物中加入DMF並將混合物於室溫下攪拌丨小時。 LC/MS顯示反應完成，並將混合物過濾及使用乙腈及水 混合物於RP-HPLC上純化，得到⑻_3-(2-((6-(2-氰基苯 基氟苯乙基胺基）菸鹼醯胺基）曱基)-5-氧基π比咯啶 -1-基）丙基胺曱酸第三丁酯（72 mg，39%)。LRMS (Μ +H+) 212 200823188 m/z 615·2 〇6_(2-cyanophenyl)_2_(3-fluorophenethylamino)nicotinic acid (110 rng, 0.30 mm〇1), (R) winter (2-(amino group) in an RB flask Methyl) _5 oxetidinium + propyl propyl propyl methacrylate (125 mg, 〇 46 mmol), HOBT (107 mg, 0·46 mmol) and HBTU (174 mg, 0·46 mg) DMF was added to the mixture and the mixture was stirred at room temperature for a few hours. LC/MS showed the reaction was completed, and the mixture was filtered and purified on RP-HPLC using acetonitrile and water mixture to give (8)- 3-(2-(2-(2-cyanophenylfluorophenylethylamino) nicotine) Amidino) indenyl)-5-oxypyrrolidrol-1-yl)propylamine decanoic acid tert-butyl ester (72 mg, 39%). LRMS (Μ +H+) 212 200823188 m/z 615·2 〇

於(R)-3-(2-((6-(2-氰基苯基)-2_(3-氟苯乙基胺基)終驗 醯胺基）甲基)-5-氧基吼咯啶-1-基）丙基胺甲酸第三丁酯（72 5 mg，0.12 mmol)之 MeOH(5.0 mL)溶液中加入 HCl(l.〇 mL，4 mmol，4M之二噁烷溶液）。將反應混合物於室溫下攪拌2 小時。LC/MS顯示反應完成。將反應混合物減壓濃縮，得 到（R)_N-((1_(3-胺基丙基)_5_氧基吼咯啶-2-基）甲基)_卜(2_ • 氰基苯基)-2-(3-氟苯乙基胺基)菸鹼醢胺鹽酸鹽(75 mg,定 ίο 量）。LRMS (Μ +H+) m/z 515·1。 實例7 :(R)-3-(2-((6-(2-Cyanophenyl)-2-(3-fluorophenethylamino))------ To a solution of hexane (1,5,5 mg, 0.12 mmol) in MeOH (5.0 mL). The reaction mixture was stirred at room temperature for 2 hours. LC/MS showed the reaction was completed. The reaction mixture was concentrated under reduced pressure to give (D)-N-((1-(3-aminopropyl)-5-oxyindolindin-2-yl)methyl)-b (2 - cyanophenyl)- 2-(3-Fluorophenethylamino)nicotinamide hydrochloride (75 mg, fixed amount). LRMS (Μ +H+) m/z 515·1. Example 7:

Ν-((6-(3-胺基丙基胺基)σ比σ定-2-基)甲基)-6-(2-氣基苯基)-2-(3-氟苯乙基胺基)於驗酸胺Ν-((6-(3-Aminopropylamino) σ ratio σ定-2-yl)methyl)-6-(2-carbophenyl)-2-(3-fluorophenethylamine Acid amine

於6-(2-氰基苯基)-2-(3-氟苯乙基胺基)菸鹼酸(582mg， 1.61 mmol)及 6-溴』比口定-2y卜曱基胺（300mg，1·61 mmol)之 DMF溶液中加入CDI(261 mg，1·61 mmol)。將反應混合物 213 200823188 於室溫下攪拌2小時。將反應混合物於RP-HPLC上純化， 得到N-((6-溴,比啶_2_基）甲基)-6-(2-氰基苯基)-2-(3-氟苯.乙 基胺基)终驗酸胺(700mg，82%)。LRMS (M+H+) m/z 530.1。6-(2-Cyanophenyl)-2-(3-fluorophenethylamino)nicotinic acid (582 mg, 1.61 mmol) and 6-bromo-bibend- 2y-decylamine (300 mg, 1· CDI (261 mg, 1.61 mmol) was added to 61 mmol) of DMF solution. The reaction mixture 213 200823188 was stirred at room temperature for 2 hours. The reaction mixture was purified by RP-HPLC to give N-((6-bromo, <RTIgt; </RTI> <RTIgt; </RTI> <RTIgt; </RTI> <RTIgt; </RTI> <RTIgt; Amino acid) Acrylamine (700 mg, 82%). LRMS (M+H+) m/z 530.1.

5 將N_((6-溴吼啶-2-基）曱基)-6-(2-氰基苯基)-2-(3-氟苯 乙基胺基）於驗醯胺（50 mg，0.095 mmol，）及丙_1，3_二胺 (396ul，4.75mmol)之NMP溶液於150°C微波下攪拌15分 鐘。將反應混合物使用乙腈及H20混合物於RP-HPLC上 純化，得到N-((6-(3-胺基丙基胺基户比啶-2-基）甲基)-6-(2-1〇 氰基苯基)-2-(3-氟苯乙基胺基)菸鹼醯胺(28 mg，56 %)。 LRMS (M+H+) m/z 524.1。 實例8 :5 N_((6-Bromoacridin-2-yl)indolyl)-6-(2-cyanophenyl)-2-(3-fluorophenethylamino) was tested on decylamine (50 mg, The NMP solution of 0.095 mmol,) and propionyl-1,3-diamine (396 ul, 4.75 mmol) was stirred under microwave at 150 °C for 15 minutes. The reaction mixture was purified by RP-HPLC using acetonitrile and a mixture of H20 to give N-((6-(3-aminopropylaminocarbazin-2-yl)methyl)-6- (2-1) Cyanophenyl)-2-(3-fluorophenethylamino)nicotinamide (28 mg, 56%). LRMS (M+H+) m/z 524.1.

15 2-(3-氟苯乙基胺基）-6-(111-1〇比17坐-4-基）-&gt;1-(11比咬-3-基甲基）於驗驢胺 方法A :15 2-(3-Fluorophenethylamino)-6-(111-1〇 ratio 17 sits-4-yl)-&gt;1-(11 than -3-ylmethyl) in the test amine method A :

214 200823188 於醋6-氯-2-(3-氟苯乙基胺基)菸鹼酸甲酯（3.08 g，ι〇 mmol)、甲醇(2〇 mL)及THF (20 mL)混合物中加入3N NaOH (10 mL，30 mmol)。將反應混合物於室溫下授拌2 天。將混合物濃縮移除曱醇及THF，並以2NHC1將PH調 整至3。將沉澱過濾並以水清洗得到6_氯_2兴3_氟苯乙基胺 基)菸鹼酸之定量產濾。LRMS(M+H+)m/z 295.1。214 200823188 Add 3N to a mixture of 6-chloro-2-(3-fluorophenethylamino) nicotinic acid methyl ester (3.08 g, ι〇mmol), methanol (2 mL) and THF (20 mL) NaOH (10 mL, 30 mmol). The reaction mixture was stirred at room temperature for 2 days. The mixture was concentrated to remove sterol and THF, and the pH was adjusted to 3 with 2NHC1. The precipitate was filtered and washed with water to give quantitative quantitative filtration of 6-chloro-2, 3-fluorophenethylamino) nicotinic acid. LRMS (M+H+) m/z 295.1.

將6-氯-2-(3-氟苯乙基胺基）菸鹼酸（ΐ〇·6 g，36 &quot; mmo1)、環戊蝴烧（12·72 g，43 mmol)、Pd(PPh3)4(4.2 g，3·6 1° mmo1)、K2C03(14.9 g，108 mmol)及無水 DMF(50 mL)混合 物以氮脫氣10分鐘。然後將混合物於UOQC微波下攪拌2 小時。將混合物經由矽藻土過濾並以DMF清洗。將濾液 以2N HC1(28 mL)調整至PH4。並以EtOAc稀釋。將有機 層以鹽水清洗二次，並濃縮至乾。將殘餘物以二氯曱烷(3〇〇 mL)濕磨。過濾接著以EtOAc (20 mL)清洗，得到2_(3_氟 苯乙基胺基）-6-(IH-吡唑-4-基）菸鹼酸之黃色固體（7.1 g， 61%)。LRMS (M+H+) m/z 327.1 〇6-Chloro-2-(3-fluorophenethylamino)nicotinic acid (ΐ〇·6 g, 36 &quot; mmo1), cyclopentanol (12·72 g, 43 mmol), Pd (PPh3) A mixture of 4 (4.2 g, 3·6 1 ° mmo1), K2C03 (14.9 g, 108 mmol) and anhydrous DMF (50 mL) was degassed with nitrogen for 10 min. The mixture was then stirred under UOQC microwave for 2 hours. The mixture was filtered through celite and washed with DMF. The filtrate was adjusted to pH 4 with 2N HCl (28 mL). It was diluted with EtOAc. The organic layer was washed twice with brine and concentrated to dryness. The residue was wet-milled with dichloromethane (3 mL). Filtration followed by EtOAc (20 mL) gave EtOAc (EtOAc:EtOAc: LRMS (M+H+) m/z 327.1 〇

N-NHN-NH

於2-(3-氟苯乙基胺基)-6-(1Η^比唑-4-基)菸鹼酸(根據 20 實例 1，方法 Α 所製備）(1.0 g，3.07 mmol)之 DMF(10 mL) 215 200823188 溶液中加入 HBTU(1.75 g，4.6 mmol)、HOBt(0.62 g，4.6 mmol)然後胺7(0.66 g，6.13 mmol)。將反應混合物於室溫 下擾拌2小時。將粗混合物使用乙腈及H2〇混合物於 RP-HPLC上純化，得到2_(3_氟苯乙基胺基)-6-(1Η-吡唑-4-基）(吡啶_3_基甲基）菸鹼醯胺之淡黃色固體（0.79 g， 62%) 〇 LRMS (M+H+) m/z 417.1 〇 方法B :2-(3-Fluorophenethylamino)-6-(1Η^boxazol-4-yl)nicotinic acid (prepared according to 20 Example 1, Method )) (1.0 g, 3.07 mmol) of DMF 10 mL) 215 200823188 To the solution were added HBTU (1.75 g, 4.6 mmol), HOBt (0.62 g, 4.6 mmol) then amine 7 (0.66 g, 6.13 mmol). The reaction mixture was scrambled at room temperature for 2 hours. The crude mixture was purified by RP-HPLC using acetonitrile and a mixture of H.sub.2 to afford 2-(3-fluorophenethylamino)-6-(1 -pyrazol-4-yl) (pyridine-3-ylmethyl) Light yellow solid of nicotinamide (0.79 g, 62%) 〇LRMS (M+H+) m/z 417.1 〇Method B:

1° 將6_氯-2-(3-氟苯乙基胺基)-N-(吼啶-3-基甲基)菸鹼 醯胺(根據實例1，方法B所製備)(152 mg，0.39 mmol)、 環戊硼烷（139 mg，0.47 mmol)、Pd(PPh3)4 及 K2C03 之 DMF 混合物於125°C微波反應器中加熱1 h。將混合物使用 EtOAc為溶離劑於矽膠栓上過濾。將濾液濃縮並使用乙腈 15 及水混合物於RP-HPLC上純化，得到2-(3-氟苯乙基胺 基）-6·(1Η_吼唑-4_基）-义（吼啶-3-基甲基）菸鹼醯胺（60.5 mg，37〇/〇)。LRMS (M+H'Boc) m/z 417」。 實例9 : 216 2008231886° 6-Chloro-2-(3-fluorophenethylamino)-N-(acridin-3-ylmethyl)nicotinium amide (prepared according to Example 1, Method B) (152 mg, A mixture of 0.39 mmol), cyclopentane borane (139 mg, 0.47 mmol), Pd(PPh3)4 and K2C03 was heated in a 125 °C microwave reactor for 1 h. The mixture was filtered on a silica gel plug using EtOAc as a solvent. The filtrate was concentrated and purified on RP-HPLC using acetonitrile 15 and water mixture to give 2-(3-fluorophenethylamino)-6·(1Η-indazole-4-yl)-yi (acridine-3) -ylmethyl)nicotinic acid amide (60.5 mg, 37 〇/〇). LRMS (M+H'Boc) m/z 417". Example 9: 216 200823188

N-((2_(胺基甲基)°比唆·》3_基)甲基)_2_(3_氟苯乙基胺基^耶吼唾冬基谈驗贐胺N-((2_(Aminomethyl)° 唆··3_yl)methyl)_2_(3_fluorophenethylamino)^耶吼吼冬基谈赆胺

於6-氯-2-(3-氟苯乙基胺基)終鹼酸（由實例8,方法A 5 所製備）(0·72 g，2.21 mmol)之DMF(5 mL)混合物中加入 DIEA(0.417 mL，2·53 mmol)、HBTU(0.84 g，2·21 mmol)、 HOBt(0.30 g，2·21 mmol)然後胺(3_(胺基甲基户比啶-2-基）曱 基胺甲酸第三丁酯（根據實例2所製備）(0.50 g，2.11 mmol)。將反應混合物於室溫下授摔1小時。將粗混合物 10 使用乙腈及出0混合物於RP-HPLC上純化，得到（3-((2-(3- 氟苯乙基胺基)-6_(1Η_吡唑_4_基)於鹼醯胺基）曱基)α比啶_2_ 基）曱基胺甲酸第三丁酯之淡黃色固體（737 mg，60〇/〇)。 LRMS (M+H+) m/z 546.3 〇Add DIEA to a mixture of 6-chloro-2-(3-fluorophenethylamino)-base acid (prepared from Example 8, Method A 5) (0·72 g, 2.21 mmol) in DMF (5 mL) (0.417 mL, 2.53 mmol), HBTU (0.84 g, 2.21 mmol), HOBt (0.30 g, 2.21 mmol) and then amine (3_(aminomethyl-2-pyridin-2-yl) fluorenyl D-butyl carbamic acid ester (prepared according to Example 2) (0.50 g, 2.11 mmol). The reaction mixture was dropped for 1 hour at room temperature. The crude mixture 10 was purified on RP-HPLC using acetonitrile and a mixture of 0. Obtaining (3-((2-(3-fluorophenethylamino))-6-(1Η-pyrazole-4-yl)-based hydrazinyl)indolyl)α-pyridyl-2-yl)hydrazinocarbamic acid Light yellow solid of the third butyl ester (737 mg, 60 〇/〇). LRMS (M+H+) m/z 546.3 〇

15 於(3-((2-(3-氟苯乙基胺基)_6-(lH-吡唑-4-基)於鹼醢胺 基）曱基）吼啶-2_基）曱基胺曱酸第三丁酯（737 mg，1.27 mmol)之曱醇(6 mL)溶液中於〇〇c力口人4M HC1之1，4-二口惡 217 200823188 烧溶液(3 mL)。將混合物升溫至室溫並攪拌2小時。將混 合物濃縮，接著使用乙腈及H20混合物於RP-HPLC上鈍 化’得到N-((2-(胺基甲基)吼啶-3-基）甲基)_2-(3-氟苯乙基 胺基)-6-(1Η_吼唑-4-基)菸鹼醯胺化合物帶有甲醇(1 ·· 1)之 淡黃色固體(545 mg5 89%)。LRMS (Μ+Η+) m/z 446.2。 實例10 :15(3-((2-(3-Fluorophenethylamino))-6-(lH-pyrazol-4-yl)-based hydrazinyl)indolyl-2-acyl) decylamine A solution of tert-butyl citrate (737 mg, 1.27 mmol) in decyl alcohol (6 mL) in 1,4-c. 217 200823188 (3 mL). The mixture was warmed to room temperature and stirred for 2 hours. The mixture was concentrated, followed by passivation on RP-HPLC using acetonitrile and a mixture of H.sub.2 to afford N-((2-(aminomethyl) acridine-3-yl)methyl)-2-(3-fluorophenethylamine) The 6-(1Η-oxazol-4-yl)nicotinium amide compound has a pale yellow solid (545 mg, 5 89%) of methanol (1··1). LRMS (Μ+Η+) m/z 446.2. Example 10:

N-((2_(胺基甲基)吡啶_3_基)甲基)·5·氟-2-(3-氟苯乙基胺基)-6-(1Η-吡唑-4-基)菸鹼醯胺N-((2_(Aminomethyl)pyridine-3-yl)methyl)·5·fluoro-2-(3-fluorophenethylamino)-6-(1Η-pyrazol-4-yl) Nicotinamide

將2,6-二氯-5-氟於驗酸(1.26 g, 6.0 mmol)、3-氟苯乙 基胺（1.25 mL，9.0 mmol)、DIEA (3.14 mL，18 mmol)及 MeCN (6 mL)混合物回流48小時並濃縮。將殘餘物溶於 EtOAc (120 mL)並以飽和的檸檬酸、水、鹽水清洗，乾燥 15 並濃縮。將有機層組合，乾燥(MgS04)並濃縮。將殘餘物 使用乙腈及H20混合物於RP-HPLC上純化，得到6-氯-5-氟-2-(3-氟苯乙基胺基）菸鹼酸之固體。（920 mg，49%)· LRMS (M+H+) m/z 313.0。 218 2008231882,6-Dichloro-5-fluoro in acid (1.26 g, 6.0 mmol), 3-fluorophenethylamine (1.25 mL, 9.0 mmol), DIEA (3.14 mL, 18 mmol) and MeCN (6 mL) The mixture was refluxed for 48 hours and concentrated. The residue was dissolved in EtOAc (EtOAc)EtOAc. The organic layers were combined, dried (MgS04) and concentrated. The residue was purified on RP-HPLC using EtOAc EtOAc EtOAc (EtOAc) (920 mg, 49%)· LRMS (M+H+) m/z 313.0. 218 200823188

將6-氯-5-氟-2-(3-氟苯乙基胺基)菸鹼酸(2.2 g，7.04 mmol)、4,4,5,5-四曱基_2-(1Η-吡唑-4,基)-1，3,2_二氧雜環戊 硼烧(2.04 g，10.56 mmol)、Pd(PPh3)4(0.81 g，0.71 mmol)、 5 K2C〇3 (2.92g，21.1 mmol)及無水 DMF(10 mL)混合物以氮 脫氣10分鐘。然後將混合物於150°C微波中攪拌3小時。 將混合物經由矽藻土過濾並以DMF (50 mL)清洗。將濾液 以 2NHCl(5mL)調整至 pH4,並以 EtOAc(150mL)稀釋。 * 將有機層以飽和的氯化銨、鹽水清洗，並濃縮至乾。將殘 ίο 餘物以二氯甲烷(30 mL)濕磨。過濾接著以EtOAc (5 mL) 清洗’得到5-氣-2-(3-氣苯乙基胺基)-6-(1 Η-11比。坐-4-基）於 鹼酸之黃色固體(2.1 g，87%)。LRMS (Μ+Η+) m/z 345.3。6-Chloro-5-fluoro-2-(3-fluorophenethylamino)nicotinic acid (2.2 g, 7.04 mmol), 4,4,5,5-tetradecyl-2-(1Η-pyridyl) Oxazol-4,yl)-1,3,2-dioxolane (2.04 g, 10.56 mmol), Pd(PPh3)4 (0.81 g, 0.71 mmol), 5 K2C〇3 (2.92 g, 21.1 The mixture of mmol) and anhydrous DMF (10 mL) was degassed with nitrogen for 10 min. The mixture was then stirred in a microwave at 150 °C for 3 hours. The mixture was filtered through celite and washed with DMF (50 mL). The filtrate was adjusted to pH 4 with 2N EtOAc (5 mL) andEtOAcEtOAc * The organic layer was washed with saturated ammonium chloride, brine and concentrated to dryness. The residue was triturated with dichloromethane (30 mL). Filtration followed by washing with EtOAc (5 mL) afforded &lt;RTI ID=0.0&gt;&gt;&&&&&&&&&&&&& 2.1 g, 87%). LRMS (Μ+Η+) m/z 345.3.

化合物X係由5-氟-2-(3-氟苯乙基胺基)-6-(1Η-吼唑 15 -4-基）菸鹼酸及胺（3-(胺基曱基）吡啶-2-基）甲基胺曱酸第 三丁酯根據製備實例9之製程所製備。LRMS (M+H’）m/z 464.1 〇 219 200823188 實例11 :Compound X is derived from 5-fluoro-2-(3-fluorophenethylamino)-6-(1Η-carbazole 15 -4-yl)nicotinic acid and amine (3-(aminomercapto)pyridine- 2-Benzylmethylamine decanoate tert-butyl ester was prepared according to the procedure of Preparation Example 9. LRMS (M+H') m/z 464.1 〇 219 200823188 Example 11:

(R)·5·氟-2_(3·氟苯乙基胺基)-Ν-((1-(2_經基乙醯基）氮π旦基）曱基-甲基 -1H-吡唑-4-基）菸鹼醯胺(R)·5·Fluoro-2_(3·fluorophenethylamino)-fluorene-((1-(2-)-ylethylhydrazinyl)nitropyridyl)mercapto-methyl-1H-pyrazole -4-yl)nicotinamide

將6-氯-5-氟-2_(3-氟苯乙基胺基)菸鹼酸(參見實例1〇) (15.6g，50 mmol)、環戊硼烧（i2.5g，60 mmol)、Pd(PPh3)4 (5·8 g，5 mmol)、K2CO3(20.7g，150 mmol)及無水 DMF(100 10 mL)混合物以氮脫氣l〇分鐘。然後將混合物於125。〇微波 中攪拌2小時。將混合物經由矽藻土過濾並以DMF清洗。 將濾、液以2N HC1調整至pH 4,並以EtOAc (150 mL)稀釋。 將組合的有機層以鹽水清洗二次，並濃縮至乾。將殘餘物 以EtOAc(200 mL)濕磨。過濾接著以EtOAc(20mL)清洗， 得到5-氟-2-(3-氟苯乙基胺基)-6_(1-甲基-1H_吼唑-4-基)於 鹼酸之黃色固體（14.5 g，85%)。LRMS (M+H+) m/z 359.0。6-Chloro-5-fluoro-2_(3-fluorophenethylamino)nicotinic acid (see Example 1) (15.6 g, 50 mmol), cyclopentaborate (i2.5 g, 60 mmol), A mixture of Pd(PPh3)4 (5·8 g, 5 mmol), K2CO3 (20.7 g, 150 mmol) and anhydrous DMF (100 10 mL) was degassed with nitrogen for 10 min. The mixture was then brought to 125. Stir in the microwave for 2 hours. The mixture was filtered through celite and washed with DMF. The filtrate was adjusted to pH 4 with 2N EtOAc and diluted with EtOAc (150 mL). The combined organic layers were washed twice with brine and concentrated to dryness. The residue was triturated with EtOAc (200 mL). Filtration followed by EtOAc (20 mL) afforded 5-fluoro-2-(3-fluorophenethylamino)-6-(1-methyl-1H-indazol-4-yl) 14.5 g, 85%). LRMS (M+H+) m/z 359.0.

HOHO

Boc2〇Boc2〇

Boc 於 D-氮咀-羧酸(2〇 g，200 mmol)、H20(200 mL)及二噁 220 15 200823188 烷(200 ml)混合物中於0°C以添加漏斗加入Boc20之二π惡 烷溶液（100 mL)。將混合物於室溫下攪拌1小時。濃縮後， 將200 mL乙鍵及200 mL H2〇加到殘餘物中。將水層以 2NHC1酸化pH3-4，然後以200 mLEtOAc萃取。將有機 層乾燥並濃縮，得到定量產率之(R)-l-(第三丁氧基幾基) 氮咀-2-羧酸(40g)。LRMS (M-100+H+) m/z 102.卜 H0^fSlN&quot;B〇C LiBH4, TMSCI HO^\(R) β°° 10 於 2Μ LiBH4 (200 ml，400mmol)之 THF 溶液中於 0〇c 緩慢加入TMSCI(101ml，800 mmol)。讓混合物於升溫至室 溫並於室溫下攪拌30分鐘。在〇°C於混合物中，在1小 時内以添加漏斗加入(R)_l_(第三丁氧基羰基）氮吸冬羧酸 (40g，200 mmol)之200 ml THF溶液。將混合物升溫至室溫 並於至溫下攪:掉2小時。讓混合物冷卻至〇°c，然後以2 mL MeOH處理，接著以40 mL H20處理。移除THF後，以 300 mLEtOAc萃取殘餘物並以300 mL鹽水清洗。將有機 層乾燥並濃縮，得到（R)-2-(經基曱基）氮哩小羧酸第三丁酯 基之無色油狀物（32.5g，87〇/〇)。LRMS (M_100+H+) m/z 132.1。Boc was added to a mixture of D-nitrogen-carboxylic acid (2〇g, 200 mmol), H20 (200 mL) and dioxo 220 15 200823188 alkane (200 ml) at 0 ° C with addition funnel to the addition of Boc20 bis oxoxane Solution (100 mL). The mixture was stirred at room temperature for 1 hour. After concentration, 200 mL of ethyl acetate and 200 mL of H2 were added to the residue. The aqueous layer was acidified to pH 3-4 with 2NHC1 then extracted with 200 mL EtOAc. The organic layer was dried and concentrated to give (R)-l-(t-butoxy-l-yl)-nitrobenzene-carboxylic acid (40 g). LRMS (M-100+H+) m/z 102. 卜H0^fSlN&quot;B〇C LiBH4, TMSCI HO^\(R) β°° 10 in 2Μ LiBH4 (200 ml, 400 mmol) in THF at 0〇 c Slowly add TMSCI (101 ml, 800 mmol). The mixture was allowed to warm to room temperature and stirred at room temperature for 30 minutes. To the mixture was added a solution of (R)_l_(t-butoxycarbonyl)azoxypyrrolidine (40 g, 200 mmol) in 200 ml of THF over 1 hour. The mixture was warmed to room temperature and stirred at room temperature for 2 hours. The mixture was allowed to cool to 〇 ° c then treated with 2 mL MeOH then EtOAc (EtOAc). After the THF was removed, the residue was extracted with 300 mL EtOAc and washed with 300 mL brine. The organic layer was dried and concentrated to give (yield: <RTIgt; </RTI> <RTIgt; </RTI> <RTIgt; </RTI> <RTIgt; LRMS (M_100+H+) m/z 132.1.

1) MsCI, Et3N 2) NaN3, DMF1) MsCI, Et3N 2) NaN3, DMF

Boc 於(R)_2-(羥基甲基）氮哩小羧酸第三丁酯（32.5g, 173 mmol)及 Et3N(27 mL，191 mmol)之 THE (650 mL)混合物中 221 20 200823188 於0°C逐滴加入曱石黃酸氯（14·9 ml，191 mmol)。將混合物 . 攪拌10分鐘。將沉澱濾出並將濾液濃縮。然後將殘餘物 溶於DMF (200 mL)。然後加入疊氮納（34g，519 mmol)。將 混合物於65°C攪拌6小時。然後將300 mL EtOAc及300 5 mL鹽水加入反應混合物中。將有機層乾燥並濃縮。將殘 餘物以Biotage石夕膠層析純化(EtOAc :己烧1 ·· 4)得到 (R)-2-(疊氮基甲基）氮哩小羧酸第三丁酯（32g，87%產率）。 LRMS (M-100+H+) m/z 113.1。 N3/'i^NBoc 1Q 趣 H2N^^NBoc 1〇 將（R)_2-(疊氮基曱基）氮^旦小羧酸第三丁酯（17g，80 mmol)、10% Pd/C (2g)及 MeOH (150mL)混合物於 45 psi 氫下攪拌1小時。將催化劑濾出並將濾液濃縮，得到 (R)-2-(胺基曱基）氮π旦小羧酸第三丁酯（14·9 g，產率 100%) 〇 LRMS (M+H+) m/z 187·3。Boc is a mixture of (R)_2-(hydroxymethyl)azinium small carboxylic acid tert-butyl ester (32.5 g, 173 mmol) and Et3N (27 mL, 191 mmol) in THE (650 mL) 221 20 200823188 at 0 Chlorophyll acid chloride (14·9 ml, 191 mmol) was added dropwise at °C. Mix the mixture. Stir for 10 minutes. The precipitate was filtered off and the filtrate was concentrated. The residue was then dissolved in DMF (200 mL). Then azide (34 g, 519 mmol) was added. The mixture was stirred at 65 ° C for 6 hours. Then 300 mL of EtOAc and 300 5 mL of brine were added to the reaction mixture. The organic layer was dried and concentrated. The residue was purified by EtOAc (EtOAc: EtOAc (EtOAc): EtOAc (EtOAc) rate). LRMS (M-100+H+) m/z 113.1. N3/'i^NBoc 1Q Interest H2N^^NBoc 1〇(R)_2-(azidodecyl)nitrogenated small carboxylic acid tert-butyl ester (17g, 80 mmol), 10% Pd/C ( A mixture of 2 g) and MeOH (150 mL) was stirred at 45 psi hydrogen for 1 hour. The catalyst was filtered off and the filtrate was concentrated to give (R)-2-(aminomercapto) nitrogen pyridine carboxylic acid tert-butyl ester (14·9 g, yield 100%) 〇LRMS (M+H+) m/z 187·3.

於5-氟-2-(3-氟苯乙基胺基)-6_(1-曱基-1Η j比唑-4-基) 於驗酸（14.3 g，40 mmol)及DMF (300mL)混合物中加入 HBTU (18.2 g，48 mmol)及 ΗΟΒΤ(6·49 g，48 mmol)。將混 合物冷卻至0°C，加入8.93 g (48 mmol)之(R)-2-(胺基甲基） 20 氮咀-1-羧酸第三丁酯，接著加入13.9 ml的DIEAa mixture of 5-fluoro-2-(3-fluorophenethylamino)-6-(1-indolyl-1Ηj-pyrazol-4-yl) in acid (14.3 g, 40 mmol) and DMF (300 mL) HBTU (18.2 g, 48 mmol) and hydrazine (6·49 g, 48 mmol) were added. The mixture was cooled to 0 ° C, and 8.93 g (48 mmol) of (R)-2-(aminomethyl) 20 nitrobutane-1-carboxylic acid tert-butyl ester was added followed by 13.9 ml of DIEA.

(80mmol)。將混合物於室溫下攪拌1小時並以300 mL 222 200823188(80 mmol). The mixture was stirred at room temperature for 1 hour and at 300 mL 222 200823188

EtOAc卒取。將有機層以500 mL鹽水清洗，以库a 燥然後濃縮。將殘餘物使用EtOAc : Hex (1 : 1)為、、容离ϋ 以Biotage矽膠層析純化。得到⑻_2-((5-氟_2-(3_氣苯乙美 胺基)-6-(1-曱基坐-4-基）終驗酸胺基）曱基）氣。曰1 羧酸第三丁酯之黃色固體（16·5 g，產率8〇0/(〇 (M+H+) m/z 527·1 〇EtOAc was taken. The organic layer was washed with 500 mL of brine, dried and concentrated. The residue was purified using EtOAc : Hex (1 : 1), EtOAc. (8)_2-((5-Fluoro-2-(3- phenethylamino)amino-6-(1-indolyl-4-yl)-finanic acid)sulfonyl) gas was obtained.曰1 yellow solid of carboxylic acid tert-butyl ester (16·5 g, yield 8〇0/(〇 (M+H+) m/z 527·1 〇

於(R)-2-((5-氟-2-(3 -氣苯乙基胺基）_6-(ι_曱基]Η_σ比 吐-4-基）菸鹼醯胺基）甲基）氮咀_i_羧酸第三丁酯（Μ ^ ίο 31.4mmol)之100 mL DCM混合物中於0〇c緩慢加入三氣 乙酸(24 mL，314 mmol)。將混合物於室溫下攪拌2小時直 到Boc保護基團完全移除。將殘餘物溶於1〇〇mLDMF中 並冷卻至〇。〇於混合物中加入甘醇酸(2.86g，38mm〇1)、 HBTU (14.3g，38mmol)、HOBT (5.1g，38mmol)及 15 mEA(16.4m1，94inmo1)之混合物。將混合物升溫至室溫並 於至溫下攪拌2小時。以EtOAc萃取混合物。將有機層進 一步以1 NNaOH (300ml)及鹽水清洗，乾燥並濃縮。將殘 餘物使用梯度0-40% B為溶離劑（A=二氯甲烷，B=1〇% Me0H之二氯甲炫溶液）置於Biotage矽膠層析純化，得到 20 粗產物。將黃色固體進一步以100 mL· EtOAc濕磨。得到 (R)_5_氟_2-(3_氟苯乙基胺基)4((1(1經基乙醯基）氣口旦 -2-基）甲基)-6_(1-甲基-1U-吡唑_4_基)菸鹼醯胺之淡黃色固 223 200823188 體（12.7g5 83%產率）。LRMS (M+H+) m/z 485·1。 實例12 :(R)-2-((5-fluoro-2-(3- gasphenethylamino)-6-(ι_indolyl)Η_σ ratio -4-yl)nicotinium amide)methyl) Tri-acetic acid (24 mL, 314 mmol) was slowly added to a 100 mL DCM mixture of yt- _i-carboxylic acid tert-butyl ester (Μ^ ίο 31.4 mmol) at 0 〇c. The mixture was stirred at room temperature for 2 hours until the Boc protecting group was completely removed. The residue was dissolved in 1 mL of DMF and cooled to hydr. A mixture of glycolic acid (2.86 g, 38 mm 〇1), HBTU (14.3 g, 38 mmol), HOBT (5.1 g, 38 mmol) and 15 mEA (16.4 ml, 94 inmol) was added to the mixture. The mixture was warmed to room temperature and stirred at room temperature for 2 hours. The mixture was extracted with EtOAc. The organic layer was further washed with 1 N NaOH (300 mL) and brine, dried and concentrated. The residue was purified by Biotage gel chromatography using a gradient of 0-40% B as a solvent (A = methylene chloride, &lt;RTIgt; The yellow solid was further triturated with 100 mL EtOAc. Obtaining (R)_5_fluoro-2-(3-fluorophenethylamino) 4 ((1(1 mercapto)yl)-2-yl)methyl)-6-(1-methyl- 1U-pyrazole-4-yl) Nicotine decylamine pale yellow solid 223 200823188 (12.7 g 5 83% yield). LRMS (M+H+) m/z 485·1. Example 12:

N-(((R)-l-(4-胺基丁醯基户比咯啶-2-基)曱基)-6-(2-氰基苯基)-2-(2-(四 氫-2H-哌喃-2-基)乙基胺基)菸鹼醯胺N-(((R)-l-(4-Aminobutanyl)-pyridin-2-yl)indolyl-6-(2-cyanophenyl)-2-(2-(tetrahydro-2H) -piperidin-2-yl)ethylamino)nicotinamide

iii. TFA/CH2CI2Iii. TFA/CH2CI2

將 2,6-二氯於驗酸（1.0 g，5.21 mmol)、N，N’-幾基二口米 嗤（CDI，l.〇ig，6.25 mmol)及 THE (10 mL)混合物於 60°C ^ 攪拌3〇分鐘並冷卻至室溫。於混合物中加入(R)-2-(胺基曱 基户比略唆_1_缓酸第三丁酯（1〇4 g，6.25 mmol)及DIEA (1·〇3 mL，5.21 mmol) 〇將反應混合物於室溫下攪拌4小 時，並以EtOAc稀釋。將有機層以H20、鹽水清洗，以 NadO4乾燥。將有機層溶液濃縮，接著以30g/() TFA之二 15 氯曱烷（1〇 mL)溶液處理得到（R)-2,6-二氯(吡咯啶-2-基 曱基）菸鹼醯胺TFA鹽之白色固體（1.7 g，84%)cLRMS (M+H+) m/z 274·0。 224 2008231882,6-dichloro acid in acid (1.0 g, 5.21 mmol), N, N'-dibasic rice bran (CDI, 1. 〇ig, 6.25 mmol) and THE (10 mL) mixture at 60 ° C ^ Stir for 3 minutes and cool to room temperature. To the mixture was added (R)-2-(amino hydrazino-based succinyl _1_sodium succinate (1 〇 4 g, 6.25 mmol) and DIEA (1·〇3 mL, 5.21 mmol) 〇 The reaction mixture was stirred at room temperature for 4 h and diluted with EtOAc EtOAc EtOAc EtOAc (EtOAc) 〇mL) solution treatment to give (R)-2,6-dichloro(pyrrolidin-2-ylindenyl)nicotinium amide TFA salt as a white solid (1.7 g, 84%) cLRMS (M+H+) m/ z 274·0. 224 200823188

於4-(苯曱基氧基羰基胺基)丁酸(1.29 g，5.45 mmol)之 DMF(4 mL)混合物中加入 HBTU (2·07 g, 5·45 mmol)、DIEA (3·0 mL，18.17 mmol)然後加入胺(R)_2,6-二氯-Ν-(吡咯啶 5 -2-基甲基)菸鹼醯胺（1.7 g，4.54 mmol)。將反應混合物於室 溫下攪拌1小時。將粗混合物使用EtOAC-MeOH (19 : 1) 以矽膠層析純化，得到(R)-4-(2-((2,6-二氯菸鹼醯胺基）曱基) 吡咯啶-1-基)-4-氧基丁基胺曱酸苯基酯（1.9 g，85%&gt;LRMS (M+H+) m/z493.4。To a mixture of 4-(phenylhydrazinyloxycarbonylamino)butyric acid (1.29 g, 5.45 mmol) in DMF (4 mL), EtOAc (2·············· 18.17 mmol) then amine (R) 2,6-dichloro-indole-(pyrrolidinium 5 -2-ylmethyl)nicotinium amide (1.7 g, 4.54 mmol) was added. The reaction mixture was stirred at room temperature for 1 hour. The crude mixture was purified by EtOAc (EtOAc) eluted elute elute Phenyl -4-butylbutylamine decanoate (1.9 g, 85% &gt; LRMS (M+H+) m/z 493.4.

將氯化物(R)-4-(2-((2,6-二氯菸鹼醯胺基）曱基比咯啶 -1-基)-4-氧基丁基胺甲酸苯甲基酯（150 mg, 0.304 mmol)、 2-(四氫-2H，口辰喃-2_基）乙胺 HC1 鹽（76 mg，0.459 mmol)、 K2C03(125 mg，0.905 mmol)及 DMF (1 mL)混合物於 100°C 15 攪拌10小時。將粗混合物使用乙腈及H20混合物於 RP-HPLC 上純化，得到 4-((R)-2-((6-氯-2-(2-(四氳-2 H-哌 喃-2-基）乙基胺基）於驗酸胺基）甲基）σ比嘻唆-1-基)-4-氧基 丁基胺曱酸苯曱基酯（62 mg，35%)。LRMS (M+H+) m/z 586·3。 225 200823188Chlorination of (R)-4-(2-((2,6-dichloronicotinium)amino)pyridin-1-yl)-4-oxybutylaminecarboxylic acid benzyl ester ( 150 mg, 0.304 mmol), 2-(tetrahydro-2H, phenoxy-2-yl)ethylamine HC1 salt (76 mg, 0.459 mmol), K2C03 (125 mg, 0.905 mmol) and DMF (1 mL) mixture Stir at 100 ° C for 15 hours. The crude mixture was purified by RP-HPLC using acetonitrile and H20 mixture to afford 4-((()) H-piperidin-2-yl)ethylamino)in the acidity of the amino)methyl)σ-pyridin-1-yl)-4-oxobutylamine phthalate (62 mg, 35%). LRMS (M+H+) m/z 586·3. 225 200823188

將4_((R)-2-((6-氯-2-(2-(四氳-2Η-ϋ辰σ南-2_基）乙基胺基) 菸鹼醯胺基）甲基）吼咯啶-1-基)-4-氧基丁基胺甲酸苯甲基 酯（62 mg，0.101 mm〇l)、2-氰基苯基硼酸(23 mg，0.156 5 mmol)、PdCl2(dppf)2(l 1 mg，0·02 mmol)、K2C〇3(92 g，0.667 mmol)及無水DMF(1 mL)混合物於125QC攪拌1 hr。將混 合物經由矽藻土墊過濾並以EtOAc清洗。將濾液濃縮至乾 並使用乙腈及H20混合物於RP-HPLC上純化，得到 4-((1〇_2_((6_(2_氰基苯基)-2-(2-(四氬-2H-哌喃-2-基）乙基 ίο 胺基)菸鹼醯胺基）甲基)吡咯啶-1-基)-4-氧基丁基胺曱酸苯 曱基酯（50 mg，77〇/〇)。LRMS (M+H+) m/z 653.3。4_((R)-2-((6-chloro-2-(2-(tetramethylene-2Η-ϋ辰σ南-2-yl)ethylamino)nicotinium)amino)methyl) Benzyl-1-yl)-4-oxobutylamine benzyl ester (62 mg, 0.101 mm 〇l), 2-cyanophenylboronic acid (23 mg, 0.156 5 mmol), PdCl2 (dppf) A mixture of 2 (1 1 mg, 0·02 mmol), K2C 〇3 (92 g, 0.667 mmol) and dry DMF (1 mL) was stirred at 125Q C for 1 hr. The mixture was filtered through a pad of celite and washed with EtOAc. The filtrate was concentrated to dryness and purified on RP-HPLC using acetonitrile and a mixture of H20 to afford 4-((1 </ RTI> </ RTI> Piperidin-2-yl)ethyl εο ) ) 醯 醯 ) ) ) ) 50 50 50 50 50 50 50 50 50 50 50 50 50 50 50 50 50 50 〇). LRMS (M+H+) m/z 653.3.

XII 於 4-((R)-2-((6-(2-氰基苯基)-2-(2-(四氫-2H_哌喃-2_基) 乙基胺基)於驗醯胺基）曱基）π比嘻唆小基)-4-氧基丁基胺曱 15 酸苯曱基酯（47 mg，0·072 mmol)之MeCN (1 mL)溶液中於 〇°C加入TMSI(72 mg，0·36 mmol)。將混合物於室溫下攪 拌2小時並使用乙腈及h2〇混合物於RP-HPLC上純化， 得到N_(((R)-l-(4-胺基丁醯基户比咯啶冬基）甲基)_6-(2·氰 基苯基)-2-(2-(四氫-2H-哌喃-2-基）乙基胺基)菸鹼醯胺(36 226 200823188 mg，77%)。LRMS (M+H+) m/z 519.3。 實例13 使用類似文中所述之製程，合成及試驗下表之化合 物。 IC50 算數平均 離子 m/z 化學名稱 3.123 M+H 359.2 {6-苯基-2-[(2-(2-σ比咬基）乙基）胺基](3-π比π定基）}-N-丙-2-烯基曱醯胺 6.747 M+H 346.2 N-甲基(2-{[2-(3-甲基苯基)乙基]胺基卜6_苯基(3_σ比啶基)) 甲醯胺 18.628 M+H 332.2 Ν-甲基{6-苯基-2-[(2-苯基乙基）胺基](3_,比啶基）}甲 醯胺 1.062 M+H 358.2 {6-苯基-2-[(2-苯基乙基)胺基](3-吼啶基)}-Ν-丙-2-烯基甲 醯胺 3.74 M+H 372,3 (2^2-(3-甲基苯基）乙基]胺基}_6_苯基(3_。比咬基))-Ν-丙-2-烯基甲醯胺 27.729 M+H 333.2 Ν-曱基{6-苯基·2-[(2_(2·吡啶基）乙基)胺基](3-吼啶基)}甲 驢胺 1.564 M+H 409.2 Ν-苯曱基{6-苯基·2_[(2-(2-吼啶基）乙基)胺基](3』比啶基)} 甲醯胺 0.151 M+H 409.2 {ό-苯基-2_[(2_苯基乙基)胺基](3』比口定基)}_Ν_(3』比咬基甲 基)甲醯胺 13.296 M+H 361.3 Ν-(曱基乙基){卜苯基_2_[(2_(2_,比啶基）乙基)胺基](3_吼。定 基)}曱醯胺 0.463 M+H 410.1 {6_苯基1[(2-(2-吡啶基)乙基)胺基](3_0比啶基)}补(2』比°定 基甲基)甲醯胺 1.29 M+H 410.2 {ό-苯基-2_[(2·(2_吡啶基)乙基)胺基](3_σ比啶基)}養(冬°比咬 基曱基)甲醯胺 5.373 M+H 396.2 {ό-苯基-2_[(2_(2-。比啶基)乙基)胺基](Ρ比啶基)}-Ν-(3-σ*σ定 227 200823188 IC50 算數平均 離子 m/z 化學名稱 7.189 M+H 396.2 基)甲醯胺 · {卜苯基丨[(2-(2-吡啶基)乙基)胺基](3_♦定基)}-N-(2-吼啶 基)甲醯胺 5.209 M+H 396.2 {6_苯基-2·[(2-(2_吼啶基)乙基)胺基](3』比啶基)}-N-(4‘啶 基)甲醯胺 1.721 M+H 415.2 {卜苯基-2_[(2·(2-吼啶基)乙基)胺基](3』比啶基)}-N-〇塞吩 基曱基)曱醯胺 0.683 M+H 415.2 {6_苯基-2-[(2-(2_π比啶基）乙基)胺基]比啶基))W3·噻吩 基曱基)甲醯胺 11.022 M+H 403.3 N-(氧雜戊環_2_基曱基){6-苯基-2-[(2-〇ϋ比啶基）乙基)胺 基](3·σ比啶基))曱醯胺 6.821 M+H 403.2 N-[((2S)氧雜戊環I基)曱基]{6_苯基_2-[(2-(2』比啶基)乙基) 胺基](3』比°定基)}甲醯胺 65.098 M+H 518.2 2_[({6_苯基_2_[(2-(2』比啶基）乙基)胺基]比啶基}羰基胺 基)甲基]嗎琳羧酸第三丁酯 96.68 M+H 458.3 N-[(l-乙醯基(4_哌啶基)）甲基]苯基_2-[(2_(2-0比啶基）乙 基)胺基](3-°比咬基)}曱醯胺 48.434 M+H 458.3 N-[(l-乙醯基(3_哌啶基)）曱基]{6_苯基-2_[(2-(2^比啶基）乙 基)胺基](3·σ比啶基)}曱醯胺 43.709 M+H 416.3 {6·苯基_2-[(2_(2-吼啶基)乙基)胺基](3_吼啶基)}養(4-哌啶 基曱基)甲醯胺 0.532 M+H 413.2 {2-[(2-環己-1-稀基乙基)胺基]-6-苯基(3-°比°定基)}-Ν-(3-σ比 啶基甲基)甲醯胺 5.689 M+H 423.3 {6_苯基_2_[(3-苯基丙基)胺基](3-σ比咬基)}-Ν-(3-σ1^σ疋基曱 基)曱醯胺 2.792 M+H 395.2 {ό-苯基[苯甲基胺基](3-吡啶基)}-Ν-(3-吼啶基甲基)曱醯 胺 4.897 M+H 400.2 Ν-( 1，3-哼唑-2-基曱基){6-苯基-2-[(2-(2-吼啶基）乙基）胺 基](3-吡啶基)}甲醯胺 6.148 M+H 399.1 Ν-(咪唑-2-基曱基){6-苯基-2·[(2-(2-。比啶基）乙基)胺基](3- 吡啶基)}甲醯胺 15.715 M+H 444.3 N-[((2S)-1-乙醯基σ比咯啶-2-基）曱基]{6-苯基-2-[(2-(2·吼啶 228 200823188 IC50 算數平均 離子 m/z 化學名稱 26.904 M+H 444.3 基)乙基)胺基](3-°比唆基)}曱醯胺 N-[((3R)-1·乙醯基。比咯啶_3_基）曱基]{6-苯基-2-[(2-(2-吼啶 基)乙基)胺基](3-吡啶基)}曱醯胺 25.159 M+H 444.3 N-[((3S)-1-乙醯基吡咯咬-3-基）甲基]{6-苯基-2-[(2-(2-吡啶 基)乙基)胺基](3-吡啶基)}甲醯胺 1.335 M+H 390.2 2-({6-苯基-2-[(2-苯基乙基)胺基]-3-啦啶基}羰基胺基)乙酸 甲酯 11.377 M+H 347.1 [6-苯基-2-(丙基胺基)(3-。比啶基)]-N-(3-叱啶基曱基)曱醯胺 2.484 M+H 375.2 {2-[(3-曱基丁基)胺基]-6-苯基(3-吡啶基)}-N-(3-吡啶基甲 基)曱醯胺 1.854 M+H 415.3 {2-[(2-環己基乙基)胺基]-6-苯基(3-吼啶基)}-N-(3-吼啶基 甲基)曱醯胺 20.292 M+H 494.3 曱基石黃醯基)(3-。辰咬基)]甲基} {6-苯基-2-[(2-(2-叫^定 基)乙基)胺基](3-吡啶基)}曱醯胺 18.23 M+H 416.3 2-(胺基甲基)哌啶基6-苯基-2-[(2-(2-吼啶基)乙基)胺基](3-吡啶基)酮 21.154 M+H 458.3 Ν-{[1-({6-苯基-2-[(2-(2-吼啶基）乙基)胺基]-3-咐啶基}羰 基)-2·哌啶基]曱基}乙醯胺 22.226 M+H 494.3 2-{[(甲基磺醯基)胺基]曱基}哌啶基6-苯基-2-[(2-(2-吡啶 基)乙基)胺基](3-吼啶基)酮 1.298 M+H 413.2 N-[(l-曱基吼唑-5-基）甲基]{6-苯基-2-[(2-(2-吼啶基）乙基) 胺基](3-吡啶基)}曱醯胺 2.733 M+H 413.2 N-[(l-曱基吡唑-3-基）甲基]{6-苯基-2-[(2-(2』比啶基）乙基) 胺基](3-吡啶基)}曱醯胺 0.711 M+H 399.2 {6-苯基-2-[(2-(2-吼啶基）乙基)胺基](3-吼啶基)}-N-(吼唑 -3-基曱基)甲醯胺 0.836 M+H 400.2 N-(異π寻唑-5-基曱基）{6-苯基-2-[(2-(2-吼啶基）乙基）胺 基](3-吡啶基)}曱醯胺 62.553 M+H 402.3 N-[((3S)吼咯啶-3-基)甲基]{6-苯基-2-[(2-(2-。比啶基)乙基)胺 基](3-吼啶基)}曱醯胺 53.616 M+H 402.3 N-[((m户比咯啶！基）曱基]{6-苯基-2-[(2-(2-咕啶基）乙基) 胺基](3-吡啶基)}甲醯胺 229 200823188 IC50 算數平均 離子 m/z 化學名稱 5.245 M+H 423.3 {6_本基·2:[(2_本基乙基)胺基](3·π比淀基)}-Ν·(2_(2-τϊ比σ定基) 乙基)曱醯胺 3.093 M+H 423.2 {6·苯基·2·[(2-苯基乙基)胺基](ρ比咬基)卜ν-(2-(3-°比咬基) 乙基)曱醯胺 0.486 M+H 389.2 Ν-甲基-2-({6-苯基-2-[(2-苯基乙基)胺基](3-17比0定基)}獄基 胺基)乙醯胺 30.309 M+H 403.3 Ν，Ν-二曱基-2-({6-苯基-2-[(2-苯基乙基)胺基](3-吡啶基 羰基胺基)乙醯胺 0.81 M+H 375.2 甲酸基甲基)苯基_2-[(2_苯基乙基)胺基]比σ定 基)}曱醯胺 22.145 M+H 430.3 (2][2-(2_氧基哌啶基）乙基]胺基}_6·苯基(3』比啶基))-Ν-(3-吡啶基甲基)曱醯胺 20.145 M+H 430.3 (2-{[2-(1-甲基(4-派咬基)）乙基]胺基}-6-苯基(3-σ比咬 基))-Ν-(3-吡啶基曱基)曱醯胺 0.149 M+H 415.2 {卜苯基_2-[(2-(2-噻吩基)乙基)胺基](3』比啶基)}- Ν-(3-吼啶 基甲基)曱醯胺 32.174 M+H 413.2 (2-{[2-(1-甲基咪唑斗基）乙基]胺基}-6-苯基(3-吼咬 基))-N-(3-吡啶基曱基)甲醯胺 0.294 M+H 399.2 {2-[(2-(2-呋喃基)乙基)胺基]-6-苯基(3·吼啶基)}-N-(3-吼啶 基甲基)甲醯胺 4.835 M+H 389.2 [(氧雜戊環-2-基甲基)胺基]-6-苯基(3-吼啶基)}-N-(3-口比 °定基甲基)甲醯胺 7.122 M+H 405.2 d(2-(l，3-二氧戊環_2_基）乙基）胺基]-6-苯基(3_吼啶 基)}-N-(3-吡啶基曱基)甲醯胺 30.307 M+H 413.3 仏[(3^米唑基丙基)胺基]各苯基(3_吡啶基)}-N-(3·吡啶基 甲基)曱酿胺 37.33 M+H 418.3 《2-[(2-嗎啉-4-基乙基)胺基]-6-苯基(3-吡啶基)}-N-(3-吡啶 基曱基)甲醯胺 20.164 M+H 425.2 於苯基-2-[(2-苯氧基乙基)胺基](3』比啶基)}-N-(3』比啶基 f基)甲酿胺 28.307 M+H 453.2 {2-[(2-(2H-苯并[3,4-d]l，3-二氧環戊烯基）乙基）胺 基]·6-苯基(3』比啶基比啶基甲基)曱醯胺 230 200823188 IC50 算數平均 離子 m/z 化學名稱 - (2-{[2-(2-氧基咪唑啶基）乙基]胺基卜6-苯基（3-吡啶 70.65 M+H 基Χ)-Ν·(3_吡啶基甲基)甲醯胺 氧基吡咯啶基）乙基]胺基}-6-p henyl(3-吡啶 10.62 M+H 416.2 基))-N-(3_吡啶基甲基)甲醯胺 {2-[(2-咪唑-4-基乙基)胺基]-6-苯基(3-°比啶基)}-N-(3-n比啶 9.766 M+H 399.2 基甲基)曱醯胺 (2-{[(羥基環己基)曱基]胺基}各苯基(3_吡啶基))-N-(3-吡啶 7.811 M+H 417.3 基甲基)曱醯胺 (2-{[2-(3,5-二甲基吼唑-4-基）乙基]胺基}-6-苯基(3-吼啶 5.941 M+H 427.2 基))-N-(3-吡啶基甲基)曱醯胺 (2-{[2-(3,5-二曱基吼唑基）乙基]胺基}-6-苯基(3-。比啶 6.833 M+H 427.2 基))-N-(3-吼啶基甲基)甲醯胺 (2-{[2-(2-氣苯基）乙基]胺基}-6-(2-氰基苯基)(3-吼啶 0.028 M+H 468.2 基))-N-(3-吡啶基曱基)甲醯胺 (6-(2-氰基苯基)-2-{[2-(2-曱基苯基）乙基]胺基}(3-吼啶 0.076 M+H 448.2 基))-N-(3-。比啶基曱基)曱醯胺 (6-(2-氰基苯基)-2-{[2-(2-氟苯基）乙基]胺基}(3-吼啶 0.028 M+H 452.2 基))-N-(3-吡啶基甲基)甲醯胺 (6-(2-氰基苯基)-2-{[2-(2-氰基苯基）乙基]胺基}(3-u比啶 0.044 M+H 458.2 基))-N-(3-吼啶基甲基)曱醯胺 {6-(2-氰基苯基)-2-[(2-(2-噻吩基）乙基）胺基](3-。比啶 0.029 M+H 440.2 基)}-N-(3-吸啶基曱基)曱醯胺 {6-(2-氰基苯基)-2-[(2-(2-呋喃基）乙基）胺基](3- η比啶 0.065 M+H 424.2 基)}-Ν-(3-吼啶基曱基)甲醯胺 (2-{[2-(3-氟吡啶基））乙基]胺基}-6-苯基（3-吡啶 1.479 M+H 基))-N-(3-吡啶基甲基)甲醯胺 (2-{[2-(3-甲基苯基）乙基]胺基}-6-苯基(3-吡啶基))-N-(3-吡 0.45 M+H 423.3 啶基曱基)曱醯胺 (6-(2-氰基苯基)-2- {[2-(2-羥基苯基）乙基]胺基} (3-吼啶 0.38 M+H 450.1 基))-N-(3-吡啶基甲基)曱醯胺 N-{[2-(胺基甲基)(3-σ比啶基)]曱基} {6』比唑-4-基-2-[(2-(2-口比 1.238 M+H 429.1 啶基)乙基)胺基](3-吡啶基)}甲醯胺 231 200823188 IC50 算數平均 離子 m/z 化學名稱 N-{(lR)-2-[(5·氟-2·{Ι&gt;(3-氟苯基)·2·瘦基乙基]胺基}-6-口比 嗤冬基(3_°比淀基))#炭基胺基]-異丙基}-2-[(第三丁氧基)羰 14.214 M+H 574.3 基胺基]乙醯胺 {5-氟-6-吼唑-4-基-2-[(2-σ比唑基乙基）胺基](3-吼啶 0.211 M+H 407.3 基)}-Ν-(3-吼啶基甲基)甲醯胺 N-[(lR)-2-({5-氟-6-吡唑-4-基-2-[(2-吡唑基乙基)胺基](3_吡 4.635 M+H 430.3 啶基)}羰基胺基)_異丙基]-2-胺基乙醯胺 (6-(2-氰基苯基)-2_{[2-(3_氟本基）乙基]胺基}(3- °比唆 0.604 M+H 520.1 基))-N-{[6-(三氟甲基)(24啶基)]甲基}甲醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼咬 1.497 M+H 520.1 基))-N-{[5_(三氟甲基)(2-吡啶基)]甲基}曱醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼唆 0.603 M+H 520.1 基))-N-{[3-(三氟曱基)(2-吡啶基)]曱基}曱醯胺 N-[(6·氯(P比啶基))曱基](6_(2_氰基苯基)-2-{[2-(3-氟苯基) 1.789 M+H 486.1 乙基]胺基}(3-吡啶基))甲醯胺 (6-(2-氰基(3-噻吩基))-2-{[2-(3-氟苯基)乙基]胺基}(3·-比啶 0.033 M+H 458.1 基))-N-(3-吼啶基曱基)甲醯胺 (2E)-3-(2-{[2-(3-氟苯基）乙基]胺基}-6-苯基(3-吼啶基))-N- 57.378 M+H 376.1 曱基丙-2-烯醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 0.298 M+H 481.2 基))-N-{[6-(曱基胺基)(3-吼啶基)]曱基}曱醯胺 N-{[6-(二甲基胺基)(3- 〇比啶基）]曱基}(6-(2-氰基苯 30.234 M+H 495.2 基)-2-{[2_(3-氟苯基)乙基]胺基}(3_吼啶基))曱醯胺 (2-{[2_(3-氟苯基)乙基]胺基}-4-(羥基曱基)-6-苯基(3-。比啶 59.114 M+H 457.2 基))-N-(3-吼啶基甲基)甲醯胺 N-[(5·胺基(2·。比啶基))曱基](6_(2_氰基苯基)-2_{|&gt;(3-氟苯 0.021 M+H 467.1 基)乙基]胺基}(3-吡啶基))甲醯胺 (2-{[2-(3-氟苯基)乙基]胺基}-5-(羥基甲基)-6-苯基(3-咕啶 0.625 M+H 457.1 基))-N-(3·吡啶基曱基)曱醯胺 (2-{[2-(3_氟苯基）乙基]胺基}-6-苯基-5-[N-(3-吼啶基甲基） 55.988 M+H 561.2 胺曱醯基](3-吡啶基))-N-(3-吡啶基曱基)甲醯胺 0.428 M+H 482.2 (5-(2-重氮胃2-氮雜乙烯基)-2-{[2-(3-氟苯基)乙基]胺基}-6-苯 232 200823188 IC50 算數平均 離子 m/z 化學名稱 基(3-吡啶基))-&gt;1-(3-°比啶基曱基)曱醯胺 (5-(胺基甲基)-2-{[2·(3-氟苯基）乙基]胺基}-6-苯基(3-吼啶 8.904 M+H 456.1 基))-Ν-(3-吼啶基曱基)甲醯胺 (2-{[2-(3-氟苯基)乙基]胺基}-6-(1-甲基π比唑-3-基）（3』比啶 0.04 M+H 431.2 基))-Ν-(3-吡啶基甲基)甲醯胺 Ν-({6_[3,3-雙(二甲基胺基)-2-氮雜丙-2-烯基](2-口比啶基)}甲 基)(6-(2-氰基苯基)-2-{[2·(3-氟苯基)乙基]胺基}(3-吼啶基)) 0.285 M+H 579.2 甲醯胺 2-(6-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}-34匕啶 1.189 M+Na 603.2 基)羰基胺基]曱基}-2-吡啶基)乙酸第三丁酯 Ν-{[4-(胺基甲基）(3-啦啶基）]甲基}(6-(2-氰基苯 0.401 M+H 481.1 基)-2-{[2-(3_氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 N-{[3-(胺基甲基）(4-吼啶基）]曱基}(6-(2-氰基苯 0.056 M+H 481.1 基)-2_{[2_(3-氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 (5-溴-2-{[2-(3-氟苯基）乙基]胺基}各°比唑-4-基(3-吼啶 0.021 M+H 497.1 基))_N_(3-吼啶基曱基)甲醯胺 (5-&gt;臭-2-{[2-(3-氣本基）乙基]胺基曱基0比°坐-4-基)(3- 0.023 M+H 509.1 吡啶基))-N-(3-吡啶基甲基)甲醯胺 (6-(5-氰基吼唑-4-基)-2-{[2-(3-氟苯基）乙基]胺基}(3-咕°定 0.105 M+H 442.1 基))-N-(3-吼啶基曱基)曱醯胺 (5-氰基-2-{[2-(3·氟苯基）乙基]胺基}-6-(1-曱基吼唑-4- 0.021 M+H 456.1 基)(3-吼啶基))-N-(3-吼啶基甲基)曱醯胺 (2-{[2-(3-氟苯基)乙基]胺基}-6·-比唑-3-基(3』比啶基))-N-(3- 0.124 M+H 417.1 。比啶基甲基)甲醯胺 (6-(3-氰基-1 -甲基吼唑-4-基)-2-{[2-(3-氟苯基）乙基]胺 0.047 M+H 456.1 基}(3-吼啶基))-N-(3-吼啶基甲基)曱醯胺 (6-(5-氣基-1-甲基^比°坐-4-基)-2-{[2-(3-氣苯基）乙基]月女 0.02 M+H 456.1 基}(3-吡啶基))-N-(3-吡啶基甲基)甲醯胺 2-[(2-{[2-(3-氟苯基）乙基]胺基}-6-啦唑-4-基(3-吼啶基))羰 0.328 M+H 397.0 基胺基]-N-曱基乙醯胺 2-[(2-{[2-(3-氟苯基）乙基]胺基}-6-(1-甲基吼唑-4-基)(3-°比 0.35 M+H 411.1 啶基))羰基胺基]-Ν-曱基乙醯胺 233 200823188 IC50 算數平均 離子 m/z 化學名稱 0.021 M+H 465.1 (5-氯-2_{[2-(3-氟苯基）乙基]胺基}-6-(l-甲基吼唑-4-基)(3-吡啶基))-N-(3-吡啶基甲基)甲醯胺 0.604 M+H 536.1 N-{[6-(胺基甲基)(2-吼啶基)]甲基}(5-漠-2-{[2·(3-氟苯基) 乙基]胺基}-6-苯基(3-吡啶基))曱醯胺 2.725 M+Na 606.1 Ν-[(Η2·[(第三丁氧基)羰基胺基]乙基}吼唑_3_基)甲基](6-Ο氰基苯基)_2·{[2-(3·默苯基)乙基]胺基}(3_°比啶基))甲醯 胺 2.2 M+H 584.2 Ν-[(1-{2-[(第三丁氧基）羰基胺基乙基}吼唑-5-基）甲 基](6_(2_氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3_吼啶基)) 甲醯胺 0.296 M+H 484.1 Ν-{[1-(2-胺基乙基）吼唑-3-基]曱基}(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比啶基))曱醯胺 0.032 M+H 484.1 Ν- {[ 1 -(2-胺基乙基）吡唑-5-基]曱基} (6-(2-氰基苯基)-2-{[2_(3_氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 0.136 M+H 460.1 N-{[6_(胺基曱基)(2』比啶基)]甲基}(2-{[2_(3-氟苯基）乙基] 胺基卜6-(1-甲基吡唑冬基)(3-吡啶基))曱醯胺 0.121 M+H 446.1 N-{[6-(胺基甲基)(2』比啶基)]甲基}(2-{|&gt;(3-氟苯基）乙基] 胺基}-6-吡唑-4-基(3-吡啶基))甲醯胺 0.027 M+H 539.1 N-{[6-(胺基甲基)(2-。比啶基)]曱基}(5-溴-2-{[2-(3-氟苯基） 乙基]胺基卜6-(1-甲基吡唑-4-基)(3-吼啶基))曱醯胺 0.013 M+H 458.1 N-[((2R)-5-氧基吼咯啶-2-基）甲基](6-(2-氰基苯 基)-2·{[2·(3_氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 0.133 M+H 458.1 N-[((2S)-5-氧基η比咯啶-2-基)甲基](6-(2-氰基苯基)-2-{[2-(3· 氟苯基)乙基]胺基}(3』比啶基))甲醯胺 16.552 M+H 541.1 N-{3-[(5S)-5-(2-重氮-2-氮雜乙婦基)-2-氧基°比略咬基]丙 基}(6-(2-氰基苯基)-2_{[2-(3-氣苯基)乙基]胺基}(3-吼啶基)) 曱醯胺 4.516 M+H 615.2 N-[((2S)-l-{3_[(第三丁氧基)羰基胺基]丙基卜5_氧基π比咯啶 -2-基)曱基](6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吡啶基))甲醯胺 0.917 M+H 501.1 N-{[(2S)-l-(2-胺基乙基)-5_氧基。比咯啶-2-基]曱基}(6-(2-氰 基苯基&gt;2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 234 200823188 IC50 算數平均 離子 m/z 化學名稱 0.431 M+H 515.2 N-{[(2S)-l-(3-胺基两基)·5·氧基吡咯啶基]曱基} (6-(2-氰 基苯基)_2· {[2-(3 -氟苯基)乙基]胺基} (3』比淀基))甲酸胺 11.658 M+H 515.1 N-{3-[(5S)_5_(fe基曱基)_2_氧基η比洛淀基]丙基)(6· (2_氛基 苯基)-2_{[2_(3-氟苯基)乙基]胺基}(3-吼淀基))甲醯胺 0.11 M+H 501.1 N-{[(2R)-l-(2-胺基乙基Μ-氧基吡咯啶冬基]曱基} (6_(2_氰 基苯基)-2_{[2_(3-氟苯基)乙基]胺基}(3-外b啶基))甲醯胺 5.621 M+H 541.2 N-{3-[(5R)-5_(2·重氮氮雜乙婦基)_2_氧基ϋ比略淀基]丙 基}(6-(2-氰基苯基)-2_{[2-(3·氟苯基)乙基]胺基}(3·吼啶基)) 曱醯胺 4.951 M+H 515.1 N**{H(5R)-5-(胺基甲基)_2*»氧基〇比略唆基]丙基}(6_ (2·氰基 苯基)-2-{[i-(3-氟苯基)乙基]胺基}(3_吼啶基))甲醯胺 17.87 M+H 501.1 N-{2-[(5S)-5·(胺基甲基)-2-氧基〇比π各ϋ定基]乙基}(6- (2_氰基 苯基)·2·{[2·(3_氟苯基)乙基]胺基}(3·吼啶基))曱醯胺 19.454 M+H 501.1 N-{2-[(5R)-5_(胺基曱基)_2_氧基σ比咯啶基]乙基氛基 苯基)-2-{[2_(3·默苯基)乙基]胺基}(3』比啶基))甲醯胺 0.355 M+H 423.1 N-[((2R)-5-氧基π比咯啶1基）甲基](2_{[2-(3_氟苯基）乙基] 胺基}-6-°比唑-3-基(3-吡啶基))曱醯胺 0.156 M+H 437.1 队[((211)-5-氧基啦咯啶冬基）曱基](2_{[2_(3_氟苯基）乙基] 胺基}-6_(1-甲基吡唑斗基)(3_吡啶基))曱醯胺 0.439 M+H 444.0 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-(吡咯啶-2-基甲基)甲醯胺 0.119 M+H 423.1 N-[((m)-5-氧基π比咯啶_2_基）曱基](2_{[2_(3_氟苯基）乙基] 胺基吡唑_4_基〇吡啶基))甲醯胺 4.834 M+H 587.1 N-[(l-{2_[(弟二丁氧基）&gt;炭基胺基]乙基}吼嘻。定冬基）甲 基](6-(2-氰基苯基)-2-{[2-(3_氟苯基)乙基]胺基}(3-吼啶基)) 曱醯胺 2.082 M+H 601.2 N_[(M3-[(第三丁氧基）羰基胺基]丙基}吡咯啶_2_基）曱 基](6-(2-氰基苯基)-2-{[2_(3_氟苯基)乙基；|胺基}(3^比啶基》 甲醯胺 0.758 M+H 487.1 Ν-{[1-(2-胺基乙基)吼咯啶冬基]曱基}(6普氰基苯基)冬 {[2-〇氟苯基)乙基]胺基}(3』比啶基))曱醯胺 3.502 M+H 501.2 Ν-{[1-(4-胺基丁基）σ比咯啶1基]曱基}(6_(2-氰基苯 235 200823188 IC50 算數平均 離子 m/z 化學名稱 基)_2_ {[2-(3-氟苯基)乙基]胺基}(3-吡咬基))曱醯胺 2-({(2S)-2-胺基-3-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基] 0.913 M+H M+H- 505.1 胺基}(3-吡啶基))羰基胺基j丙基}胺基)乙酸曱酯 2-({(2S)·2-胺基-3·[(2·{[2-(3-氟苯基)乙基]胺基)-6- (1-甲基 10.852 OMe 452.3 吡唑-4-基)(3-吡啶基))羰基胺基]丙基}胺基乙酸甲酯 N_[((2S)_6-氧基哌畊基）曱基](2·{[2_(3_ 1苯基）乙基]胺 16.026 M+H 438.2 基}-6-吡唑-4-基(3-吡啶基))曱醯胺 N-[((2S)-6_氧基哌畊-2-基)曱基](6-(2-氰基苯基)-2-{[2-(3-氟 0.819 M+H M+H- 473.1 苯基)乙基]胺基}(3』比啶基))甲醯胺 N-[((2R)-4- {3-[(第三丁氧基）羰基胺基]丙基}-6-氧基哌 畊-2-基）曱基](6-(2-氰基苯基)-2-{[2-(3_氟苯基）乙基]胺 9.536 Boc 530.2 基}(3-吡啶基))曱醯胺 N-[((2S)_6_氧基哌畊1基）曱基](2-{[2-(3-1苯基）乙基]胺 13.056 M+H 452.1 基}-6-(1-甲基吡唑-4-基)(3-吡啶基))曱醯胺 N-[((2S)-6_氧基哌畊冬基）曱基](2_p_(3_氟苯基）乙基]胺 6.391 M+H 438.1 基}-6-吡唑-3-基(3-n比啶基))曱醯胺 N-{[(2R)_4-(3_胺基丙基)-6_氧基哌畊_2_基]曱基}(6- (2-氰基 4.522 M+H 530.2 苯基)·2-{[2_(3_氣苯基)乙基]胺基}(3-π比啶基))曱醯胺 N-{[(2RH-(2-胺基乙基)-6-氧基哌畊-2-基]曱基}(6- (2-氰基 8.4722 M+H 516.2 苯基)-2_{[2_(3-氟苯基)乙基]胺基)(3_吡啶基))曱醯胺 N-[((2R)_6-氧基哌畊·2_基)曱基]氰基苯基)冬 0.155 M+H 473.1 氟苯基)乙基]胺基} (3-°比唆基))曱醯胺 N][(2S)-4_(2-胺基乙基)各氧基哌畊各基]曱基}(6· (2·氰基 0.623 M+H 515.2 苯基)-2-{[2_(3_氟苯基)乙基]胺基比啶基))甲醯胺 N][(2S&gt;4-(3-胺基丙基)_6_氧基π底畊_2_基]甲基}(6_ (2_氰基 2.809 M+H 530.2 苯基)·2-{[2_(3-氟苯基)乙基]胺基比啶基》曱醯胺 队({(211)-1-[4-(1，3-二氧基苯并[c]唑啉_2_基)丁基]_5_氧基0比 °各咬-2-基}曱基)(6_(2_氰基苯基片{[2_(3_氟苯基)乙基]胺 0.376 M+H 659.2 基}(3-吼咬基))甲驗胺 队({(211)-1-[5-(1，3-二氧基苯并[c]唑啉冬基)戊基]_5_氧基吼 咯啶-2-基}甲基)(6-(2-氰基苯基)_2-{[2-(3-氟苯基）乙基]胺 0.266 M+H 673.2 基}(3_吼咬基))曱酿胺 236 200823188 IC50 算數平均 離子 m/z 化學名稱 (2R)_2_{[(6-(2-氰基苯基)-2_{[2_(3-氟苯基)乙基]胺基} (3』比 1.933 M+H 544.2 啶基))羰基胺基]甲基}吡咯啶羧酸第三丁酯 N-{[(2R)-l-(4-胺基丁基)-5氧基吼咯啶-2-基]甲基}(6- (2-氰 0.0517 M+H 529.2 基本基)-2&lt;~{[2-(3 -氟苯基)乙基]胺基}(3-τσ比σ定基))甲醯胺 Ν-{[(2Κ&gt;1·〇胺基戊基)-5_氧基α比咯啶基]曱基}(6_ (2-氰 0.039 M+H 543.2 基本基)_2- {[2_(3-氟苯基)乙基]胺基}(3-ϋ比ϋ定基))曱酸胺 N-[((m)吼咯啶基）曱基](6-(2_氰基苯基)·2·^#•氟苯 0.1738 M+H 444.1 基)乙基]胺基}(3_吡啶基))甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-吼唆-4-基(3- °比咬基))- 0.034 M+H 406.1 N-(吡唑-3-基甲基)曱醯胺 (2-{[2_(3·氟苯基)乙基]胺基曱基σ比唑_4_基）（3_σ比啶 0.031 M+H 420.1 基))-Ν十比唑-3-基甲基)曱酿胺 (2-{[2-(3-氟苯基）乙基]胺基}·6-吼嗤-3-基(3-吼σ定基))- 0.092 M+H 406.1 Ν-(吡唑-3-基曱基)甲醯胺 N-[((2R)-l-{4-[(第三丁氧基）羰基胺基]丁醯基}吼咯啶 基)甲基](6_(2_氰基苯基)_2_{[2-(3·氟苯基)乙基]胺基}(3- 0.432 M+H 629.2 吡啶基))曱醯胺 N-{[(2R)-l-(3-胺基丙醯基)吼咯啶-2-基]曱基}(6- (2-氰基苯 0.047 M+H 515.2 基)-2·{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 Ν-{[1-(3-胺基丙基）吼唑-3-基]曱基}(6-(2-氰基苯基） 0.065 M+H 498.2 -2-{[2-(3·氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 Ν-{[1-(3-胺基丙基户比唑-3-基]曱基}(2-{[2-(3-氟苯基)乙基] 2.686 M+H 477· 1 胺基曱基吡唑-4-基)(3-吡啶基))曱醯胺 Ν-{[1-(3-胺基丙基)吼唑-3-基]曱基}(2-{[2_(3-氟苯基)乙基] 3.764 M+H 463.2 胺基}-6-吡唑-3-基(3-吡啶基))甲醯胺 Ν-{[1-(3-胺基丙基比唑-5-基]甲基}(2-{[2_(3_氟苯基)乙基] 0.228 M+H 477.2 胺基卜6-(1-曱基吡唑-4-基)(3-吡啶基))甲醯胺 Ν-{[1-(3-胺基丙基)吼唑-5-基]曱基}(2-{[2_(3-氟苯基)乙基] 0.462 M+H 463.2 胺基}-6-吡唑-3-基(3-吡啶基))甲醯胺 N-[((2R)-l-{2-[(第三丁氧基)羰基胺基]乙基}吼咯啶-2-基） 甲基](6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-ϋ比啶 3.691 M+H 587.2 基))曱醯胺 237 200823188 IC50 算數平均 離子 m/z 化學名稱 1.341 M+H 601.2 N-[((2R)-l-{3-[(第三丁氧基)羰基胺基]丙基}°比咯啶-2-基) 曱基](6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3-外匕啶 基))曱醯胺 0.705 M+H 487.2 N-{[(2R)-l-(2-胺基乙基户比咯啶-2-基]曱基}(6-(2-氰基苯 基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比啶基))甲醯胺 1.389 M+H 501.2 N_ {[(2R)-1 -(3 _胺基丙基户比咯啶-2-基]曱基} (6-(2-氰基苯 基)-2-{[2_(3_氟苯基)乙基]胺基}(3』比啶基))曱醯胺 11.966 M+H 549.2 Ν-[(1-{2·[(第三丁氧基）羰基胺基]乙基}°比唑-3-基）甲 基](2-{[2_(3-氟苯基)乙基]胺基}-6-吼唑基(3_°比啶基))甲 醯胺 1.488 M+H 449.1 Ν-{[1-(2-胺基乙基比唑-3-基]曱基}(2-{[2_(3_氟苯基)乙基] 胺基}-6-吡唑-4-基(3-吡啶基))曱醯胺 5.506 M+H 449.2 Ν][1-(2-胺基乙基)吼唑-3-基]曱基}(2-{[2-(3_氟苯基)乙基] 胺基}-6-吡唑-3-基(3-吡啶基))甲醯胺 0.634 M+H 449.2 胺基乙基户比唑-5-基]甲基}(2-{[2_(3_氟苯基)乙基] 胺基}-6-咣唑-3-基(3-吡啶基))甲醯胺 1.862 M+H 463.2 Ν-{[1-(2-胺基乙基户比唑-3-基]甲基}(2-{[2_(3_氟苯基)乙基] 胺基}-6-(1-甲基吡唑-4-基)(3-吡啶基))甲醯胺 0.313 M+H 463.3 N- {[ 1-(2-胺基乙基)吼唑-5-基]曱基}(2- {[2-(3-氟苯基)乙基] 胺基}-6-(1-曱基吡唑-4-基)(3-吡啶基))甲醯胺 0.318 M+H 530.3 N-{[(2R)-l-(3-胺基丙基)-6-氧基哌畊冬基]甲基}(6-(2_氰基 苯基)-2-{[2_(3·氣苯基)乙基]胺基}(3』比啶基))曱醯胺 3.562 M+H 509.3 N-{[(2R)-l-(3-胺基丙基)-6-氧基哌畊-2_基]甲基}(2][2-(3-氟苯基)乙基]胺基}-6-(1-曱基吡唑冬基)(3_吡啶基))甲酸胺 2.343 M+H 495.3 N-{[(2R)-l-(3-胺基丙基)各氧基哌4-2-基]甲基}(2_{1&gt;(3-氟苯基)乙基]胺基}-6-吡唑-4-基(3』比啶基))甲醯胺 9.627 M+H 495.3 N-{[(2R)-l-(3-胺基丙基)·6-氧基哌畊-2-基]甲基}(2][2-(3_ 氟苯基)乙基]胺基}-6-吼唑-3-基(3』比啶基))甲醯胺 0.119 M+H 486.2 N-[((2R)-1-乙醯基σ比Ρ各σ定-2-基）甲基](6-(2-氰基本基） _2-{[2-(3-氟苯基)乙基]胺基}(3_σ比啶基))曱醯胺 1.448 M+H 522.2 N-{[(2R)-l-(曱基磺醯基户比咯啶-2-基]曱基}(6-(2-氰基苯 基)·2_{[2-(3-氟苯基)乙基]胺基}(3』比啶基))甲醯胺 238 200823188 IC50 算數平均 離子 m/z 化學名稱 0.214 M+H 458.3 N-[((2R)-1-甲基吼咯啶-2-基）曱基](6-(2-氰基苯基） -2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 2.049 Μ 472.2 N-[((2R)-1，1-二甲基吼咯啶-2-基）甲基](6-(2-氰基苯 基)-2_{[2_(3·氟苯基)乙基]胺基}(3-咕啶基))曱醯胺 11.341 Μ+Η 695.3 N-[((2R)-l-{[3-(l，3·二氧基苯并[c]唑啉-2-基)丙基]磺醯基&gt; 吼咯啶-2-基）甲基](6-(2-氰基苯基)-2_{[2-(3-氟苯基)乙基] 胺基}(3-吡啶基))曱醯胺 0.071 Μ+Η 551.3 N-( {(2R)-H(2-胺基乙基）磺醯基]吼咯啶-2-基}甲基） (6·(2·氰基苯基)-2·{[2-(3·氟苯基)乙基]胺基}(3』比啶基))甲 醯胺 0.234 Μ+Η 565.3 N-({(2R)-l-[(3-胺基丙基）磺醯基ρ比咯啶-2·基}曱基） (6-(2_氣基苯基)-2·{[2-(3-氣苯基)乙基]胺基}(3-ϋΐ^σ定基))甲 醯胺 1.406 Μ+Η 463.1 Ν-{[1-(3-胺基丙基)吼唑-3·基]甲基}(2-{[2-(3-氟苯基)乙基] 胺基}-6-吡唑-4-基(3-吡啶基))甲醯胺 0.095 Μ+Η 463.1 Ν-{[1-(3-胺基丙基)吼唑-5-基]甲基}(2-{[2·(3-氟苯基)乙基] 胺基}-6-吡唑-4-基(3-吡啶基))甲醯胺 1.342 Μ+Η 594.3 N-[((2R)-l-{3-[(第三丁氧基)羰基胺基]丙基}-5-氧基叱咯啶 -2-基)曱基](2_{[2-(3-氟苯基)乙基]胺基}-6-(1-甲基吼唑-4-基)(3-吡啶基))甲醯胺 2.127 Μ+Η 578.4 Ν-{[1-(3-胺基丙基)-5-氧基吡咯啶-2-基]曱基}(6- {1-[(二曱 基胺基)(二曱亞基)甲基]吡唑斗基}-2- {[2-(3-氟苯基)乙基] 胺基}(3-吡啶基))甲醯胺 0.29 Μ+Η 494.3 N-{[(2R)-l-(3-胺基丙基)-5-氧基吼咯啶-2-基]甲基} (2_{[2-(3·氟苯基)乙基]胺基甲基吡唑斗基）（3-吼啶 基))甲醯胺 4.64 Μ+Η 523.3 (2R)-2-{[(2_{[2-(3-氧苯基）乙基]胺基曱基π比〇坐-4_ 基)(3-吡啶基))羰基胺基]曱基}吡咯啶羧酸第三丁醋 0.966 Μ+Η 480.2 N-{[(2R)-l-(3-胺基丙基）-5-氧基π比洛咬-2-基]甲 基Κ2_{[2·(3-氟苯基)乙基]胺基}-6-°比°坐基(3_°比11 定基))曱 醯胺 0.518 Μ+Η 615.3 N-[((2R)-H3_[(第三丁氧基)羰基胺基]丙基}-5-氧基吼咯啶 239 200823188 IC50 算數平均 離子 m/z 化學名稱 0.666 M+H 432.2 -2-基)甲基](6-(2-乳基本基)·2][2-(3-鼠本基)乙基]胺基}(3_ 吡啶基))甲醯胺 Ν-(2-胺基-2-甲基丙基)(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙 基]胺基}(3-吼啶基))甲酸胺 4.746 M+H 409.2 N-[((2R)吼咯啶基)甲基](2-{[2_(3_氟苯基)乙基]胺基}·6-π比0坐_4_基(3-σ比咬基))曱醯胺 3.185 M+H 423.2 N-[((2R)吼咯啶基)甲基](2-{[2_(3·氟苯基)乙基]胺基}-6-(1-甲基吡唑-4-基)(3-吡啶基))甲醯胺 1.473 M+H 510.3 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基} (3- π比啶 基))-N-{2-甲基-2_[(曱基磺醯基)胺基]丙基}曱醯胺 5.532 M+H 580.3 N-[((2R)-l-{2-[(第三丁氧基)羰基胺基]乙醯基p比咯啶-2-基）曱基](2-{[2-(3-氟苯基）乙基]胺基} -6-(1-曱基吼唑-4-基)(3-吡啶基))曱醯胺 5.026 M+H 594.3 N-[((2R)-l-{3-[(第三丁氧基)羰基胺基]丙醯基}吼咯啶-2-基）甲基](2-{[2-(3-氟苯基）乙基]胺基} -6·(1-甲基啦唑-4-基)(3-吼啶基))甲醯胺 3.651 M+H 608.3 N-[((2R)-l-{4-[(第三丁氧基)羰基胺基]丁醯基}吼咯啶-2-基）甲基](2-{[2-(3·氟苯基）乙基]胺基} -6-(1-曱基吼唑-4-基)(3-吼啶基))甲醯胺 0.581 M+H 480.3 N-{[(2R)-l-(2-胺基乙醯基)吼咯啶-2-基]曱基} (2- {[2-(3-氟 苯基)乙基]胺基}-6-(1-甲基。比唑-4-基)(3-吼啶基))甲醯胺 0.587 M+H 494.3 N-{[(2R)-l-(3-胺基丙醯基)吼咯啶-2-基]甲基} (2- {[2-(3-氟 苯基)乙基]胺基}-6-(1-甲基吡唑-4-基)(3-吼啶基))甲醯胺 0.351 M+H 508.3 N-{[(2R)-l-(4-胺基丁醯基)吼咯啶-2-基]曱基} (2- {[2-(3-氟 苯基)乙基]胺基甲基吡唑-4-基)(3-吡啶基))曱醯胺 0.515 M+H 418.2 N-((2S&gt;2_胺基丙基)(6_(2_氰基苯基)-2- {[2-(3·氟苯基)乙基] 胺基}(3-吡啶基))曱醯胺 9.572 M+H 589.4 2-[(第三丁氧基）羰基胺基ρΝ_{2·[(6·(2-氰基苯基）_ 2-{[2_(3_氟苯基）乙基]胺基}(3-吼啶基))羰基胺基]-第三丁 基}乙醯胺 0.194 M+H 617.4 4-[(第三丁氧基）羰基胺基]_Ν-{2_[(6_(2-氰基苯基)-2_{[2-(3_氟苯基)乙基]胺基}(3-吼啶基))幾基胺基]-第三丁 240 200823188 IC50 算數平均 離子 m/z 化學名稱 -基}丁醯胺 N-{(1 S)-2-[(6-(2_ 氰基苯基)-2-{[2·(3_ 氟苯基)乙基]胺基}(3-口比啶基))幾基胺基]-異丙基H-[(第三丁氧基)羰基胺基]丁 2.019 M+H 603.3 醯胺 N-[((2R)-l]5-[(第三丁氧基)羰基胺基]戊醯基}吡咯啶-2-基)甲基](6-(2-氰基苯基)-2-{[2-(3-說苯基)乙基]胺基}(3-吼 2.94 M+H 643.4 啶基))甲醯胺 2-胺基-Ν-{2_[(6·(2•氰基苯基)-2-{[2_(3·氟苯基)乙基;|胺基} 0.32 M+H 489.3 (3-0比咬基))幾基胺基]-第三丁基}乙醯胺 4_胺基-Ν-{2-[(6_(2-氰基苯基)-2-{[2_(3-敗苯基)乙基]胺基} 0.277 M+H 517.3 (3-°比啶基))羰基胺基]-第三丁基} 丁醯胺 N-{[(m)-l-(N-曱基胺甲醯基)吡咯啶-2-基]甲基}(6- (2-氰 0.307 M+H 501.1 基苯基)-2-{[2-(3_1苯基)乙基]胺基}(3-吼啶基))甲醯胺 (2R)-2-{[(6_(2·氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基} (P比 0.101 M+H 502.2 σ定基))幾基胺基]甲基}°比洛咬繞酸曱酉旨 N-{(1 S)-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3- 1.459 M+H 475.2 吡啶基))羰基胺基]-異丙基}-2-胺基乙醯胺 N-{(1 S)-2_[(6-(2_ 氰基苯基)-2_{[2-(3-氟苯基)乙基]胺基}(3- 3.56 M+H 503.2 吡啶基))羰基胺基]-異丙基}各胺基丙醯胺 N-{[(2R)-l-(5_胺基戊醯基)吼咯啶-2-基]曱基} (6- (2-氰基 0.099 M+H 543.3 苯基)-2-{|&gt;(3-氟苯基)乙基]胺基} (P比啶基))曱醯胺 N-{(2S)-2-[(甲基磺醯基）胺基]丙基}(6-(2-氰基苯基)- 1.215 M+H 496.1 2_ {|&gt;(3-氟苯基)乙基]胺基} (3_吼啶基))甲醯胺 (2R)-2-{[(6-(2-氰基苯基)-2_{[2-(3_說苯基)乙基]胺基} (3-吼 0.027 M+H M+H- 531.2 啶基))羰基胺基]甲基}吡咯啶羧酸2-胺基乙基酯 N-[(2S)_2_(曱基胺基）丙基](6-(2-氰基苯基)-2-{[2-(3-氟苯 0.944 Me 432.2 基)乙基]胺基} (3-吼啶基))甲醯胺 N-((2R)-2-胺基丙基)(6-(2_氰基苯基)-2- {[2-(3-氟苯基)乙基] 0.399 M+H 418.2 胺基}(3-吡啶基))甲醯胺 &gt;H(2 R)_2-(甲基胺基)丙基](6-(2-氰基苯基)-2-{[2- (3-氟苯 1.89 M+H 432.2 基)乙基]胺基}(3-吼啶基))甲醯胺 5.84 M+H 510.2 N-{(2S)-2-[曱基(甲基磺醯基)胺基]丙基}(6-(2-氰基苯基)- 241 200823188 IC50 算數平均 1.333 7.071 2.312 5.916 0.049 3.677 3.246 6.826 0.041 0.204 0.71 0.152 0.012 0.025 離子 m/z M+H 496.2 M+H 510.2 M+H 575.3 M+H 589.3 M+H 603.3 M+H 617.4 M+H 489.2 M+H 517.3 M+H 475.2 M+H 503.2 M+H 517.2 M+H 489.2 M+H 449.1 M+H 501.2 化學名稱 2-{[2-(3_氟苯基)乙基]胺基}(3-n比啶基))甲醯胺 N-{(2R)-2-[(曱基磺醯基）胺基]丙基}(6-(2-氰基苯 基)-2-{[2_(3-氟苯基)乙基]胺基}(3-吡啶基))甲醯胺 N-{(2R)-2-[曱基（甲基磺醯基）胺基]丙基}(6-(2-氰基苯 基)-2-{[2_(3-氟苯基)乙基]胺基}(3-。比啶基))曱醯胺 N-{(lR)-2-[(6-(2-氰基苯基)-2_{[2-(3-氟苯基)乙基]胺基}(3-°比啶基))羰基胺基]-異丙基}-2-[(第三丁氧基)羰基胺基]乙 醯胺 N-{(1R)_2_[(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吡啶基))羰基胺基]-異丙基}-2-[(第三丁氧基)羰基胺基]-N-曱基乙醯胺 N-{(1 R)-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-吼啶基))羰基胺基]-異丙基}-4-[(第三丁氧基)羰基胺 基]丁醯胺 Ν·{(1 R)-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-吼啶基))羰基胺基]-異丙基}-4-[(第三丁氧基)羰基胺 基]-N-甲基丁醯胺 N-{(lS)_2_[(6-(2-氰基苯基)-2-{[2-(3-敗苯基)乙基]胺基}(3-α比π定基))&gt;炭基胺基]-異丙基}-2-胺基-N-甲基乙酿胺 N-{(1S)-2-[(6_(2-氰基苯基)-2-{[2-(3_ 氟苯基)乙基]胺基}(3-吡啶基))羰基胺基]-異丙基}-4-胺基_N-甲基丁醯胺 N-{(1R)-2_[(6-(2_ 氰基苯基)-2-{[2-(3_ 氟苯基)乙基]胺基}(3_ 吡啶基))羰基胺基]-異丙基}-2-胺基乙醯胺 N-{(1R)-2-[(6_(2·氰基苯基)1{[2-(3-氟苯基)乙基]胺基}(3-吡啶基))羰基胺基]-異丙基}-4-胺基丁醯胺 N-{(1 R)-2-[(6-(2-氰基苯基）-2-{[2-(3-氟苯基）乙基]胺 基}(3-°比σ定基))幾基胺基]-異丙基}-4-胺基-N-曱基丁醢胺 N-{(1 R)-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-吼°定基))獄基胺基]-異丙基}-2-胺基-N-甲基乙酸胺 〇氟-2-{[2_〇氟苯基）乙基]胺基}-6_(1-甲基吼唑-4-基)(3-吡啶基))-Ν-(3-ϋ比啶基曱基)曱醯胺 N-{[(2R)-l-(2-胺基乙醯基)吼咯咬-2-基]曱基}(6_ (2-氰基苯 242 200823188 IC50 算數平均 離子 m/z 化學名稱 0.029 M+H 528.2 基)·2·{[2_(3_氟苯基)乙基]胺基}(3_Π比啶基))曱醯胺 N-{[(2R)-l-(4-胺基丁醯基)吡咯啶-2-基]甲基}(6- (2-氰基苯 基)-2-{[2-(3_氟苯基)乙基]胺基}(3-°比唆基))曱醯胺 0.042 M+H 515.2 N-{[(2R)-l-(3-胺基丙基)-5-氧基。比咯啶-2-基]甲基} (6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))曱 醯胺 0.044 M+H 417.1 (2-{[2-(3-氟苯基)乙基]胺基}-6-吼唑-4-基(3』比啶基))-N-(3-吡啶基曱基)曱醯胺 6.265 M+H 424.2 {6-(3-甲基苯基)-2-[(2-(2·吼啶基）乙基）胺基](3-吼啶 基)}-N-(3-n比啶基甲基)甲醯胺 0.915 M+H 428.2 {6-(3-氟苯基）_2-[(2-(2- η比啶基）乙基）胺基](3·吼啶 基)}-Ν-(3-吡啶基甲基)曱醯胺 2.992 M+H 435.2 {6-(3-氰基苯基)-2-[(2-(2-η比啶基）乙基）胺基](3-吼啶 基)}·Ν-(3-吡啶基曱基)曱醯胺 14.933 M+H 440.2 {6-(3-甲氧基苯基)-2-[(2-(2-吼啶基）乙基）胺基](3-吼啶 基)}-N-(3-吡啶基甲基)曱醯胺 0.79 M+H 426.1 {6-(3-經基苯基）-2-[(2-(2-ϋ比咬基）乙基）胺基](3- 〇比σ定 基)}-Ν-(3-吡啶基甲基)曱醯胺 1.967 M+H 444.1 {6-(3-氣苯基）-2-[(2-(2- ^比σ定基）乙基）胺基](3·。比咬 基)}-Ν-(3-吼啶基曱基)曱醯胺 5.927 M+H 478.1 {2·[(2·(2-。比啶基)乙基)胺基]各[3_(三氟曱基)苯基](3-。比啶 基)}-Ν-(3』比啶基甲基)甲醯胺 12.404 M+H 453.2 {6-[3-(二甲基胺基)苯基]-2-[(2-(2^比啶基）乙基)胺基](3_,比 啶基)}-Ν·(3-吡啶基甲基)甲醯胺 1.321 M+H 428.1 {6-(2-氟苯基）-2-[(2-(2-吼咬基）乙基）胺基](3-。比啶 基)}-N-(3-吼啶基甲基)曱醯胺 4.438 M+H 444.1 {6-(2-氣苯基）-2-[(2-(2-咕咬基）乙基）胺基](3-吼啶 基)}-N-(3-吼啶基甲基)曱醯胺 11.031 M+H 424.2 {6-(2-曱基苯基)-2-[(2-(2-。比咬基）乙基）胺基](3- η比啶 基)}-Ν-(3·σΛ°^基曱基)甲醯胺 17.936 M+H 440.2 {ό-(2-曱氧基苯基)-2-[(2普°比σ定基）乙基）胺基](3“比啶 基)}-Ν-(3-吼啶基甲基)曱醯胺 243 200823188 IC50 算數平均 離子 m/z 化學名稱 {6-(2-氰基苯基)-2-[(2-(2-处啶基）乙基_)胺基](3-吼啶 0.46 M+H 435.2 基)}-N-(3-吼啶基甲基)曱醯胺 {2-[(2-(2-。比淀基）乙基）胺基]-6-(2-σ塞吩基）(3- °比σ定 0.797 M+H 416.1 基)}-Ν-(3-吡啶基曱基)曱醯胺 {2-[(2-(2-。比啶基）乙基）胺基]-6-(3-噻吩基）(3-吼啶 0.414 M+H 416.1 基)}-N-(3-吼啶基曱基)甲醯胺 {6-(4-羥基苯基）-2-[(2-(2-吡啶基）乙基）胺基](3-吡啶 0.586 M+H 426.1 基)}-N-(3-吡啶基曱基)甲醯胺 {6-(2-羥基苯基）-2-[(2-(2-吼啶基）乙基）胺基](3-吼啶 2.17 M+H 426.1 基)}-N-(3-吡啶基甲基)曱醯胺 {6-(4-乙基苯基）-2-[(2-(2- °比σ定基）乙基）胺基](3- °比〇定 2.792 M+H 438.2 基)}-Ν-(3-吼啶基曱基)曱醯胺 Ν-(4-{6-[(2-(2-吼啶基）乙基)胺基]·5-[Ν-(3-吼啶基曱基)胺 1.221 M+H 467.2 甲醯基]-2-吼啶基}苯基)乙醯胺 {6-(4-甲基(2-噻吩基))-2-[(2-(2-吡啶基）乙基)胺基](3-吡啶 0.344 M+H 430.1 基)}-N-(3-吡啶基曱基)曱醯胺 {6-(4-甲基(3-噻吩基))-2_[(2-(2』比啶基)乙基)胺基](3』比啶 4.063 M+H 430.1 基)}-N-(3 ^比啶基甲基)曱醯胺 {6-(2,3-二甲基苯基)-2-[(2-(2-吼啶基）乙基)胺基](3-。比啶 6.945 M+H 438.2 基)}-N-(3-吡啶基曱基)曱醯胺 {6-(2,5-二甲基苯基)-2-[(2-(2-n比啶基）乙基）胺基](3-u比啶 13.588 M+H 438.2 基)}-N-(3-吡啶基曱基)曱醯胺 {6-(2,4-二甲基苯基)-2-[(2-(2^比啶基）乙基）胺基](3-吼啶 3.964 M+H 438.2 基)}-N-(3-吡啶基曱基)曱醯胺 {6-(3,5-二甲基苯基)-2-[(2-(2-。比啶基）乙基)胺基](3-u比啶 10.138 M+H 438.2 基)}-N-(3-吡啶基曱基)曱醯胺 {6-(3,4-二甲基苯基)-2-[(2-(2 j比啶基）乙基）胺基](3-吼啶 3.38 M+H 438.2 基)}-N-(3-吡啶基曱基)甲醯胺 (2-{[2-(4-氟苯基)乙基]胺基}-6-苯基(3-啦啶基))-N- (3-u比啶 1.609 M+H 427.2 基曱基)甲醯胺 (2-{[2-(4-氯苯基)乙基]胺基}-6-苯基(3-吼啶基))-N- (3』比啶 6.677 M+H 443.1 基曱基)曱醯胺 244 200823188 IC50 算數平均 離子 m/z 化學名稱 (2-{[2-(3-氣苯基)乙基]胺基}-6-苯基(3-吼啶基))朴（3』比咬 0.349 M+H 443.1 基甲基)甲醯胺 (2-{|&gt;(3-甲氧基苯基）乙基]胺基卜6-苯基(3-吡啶基))K3- 0.269 M+H 439.1 吡啶基甲基)曱醯胺 (2-{[2-(3-氣苯基)乙基]胺基}·6-苯基(3-η比啶基))斗（3』比唆 0.063 M+H 427.1 基甲基)曱醯胺 (2-{[2-(2_氣苯基)乙基]胺基}-6-苯基(3』比啶基))-Ν- (34咬 0.16 M+H 443.1 基甲基)曱醯胺 (2-{[2-(2-甲氧基苯基)乙基]胺基}-6·苯基(3』比啶基))·Ν-(3** 0.98 M+H 439.1 吼。定基甲基)甲醯胺 (2-{[2-(2-甲基苯基）乙基]胺基}-6-苯基(3-吡啶基))-Ν-(3-吡 0.326 M+H 423.1 啶基甲基)甲醯胺 (2-{[2_(2-氟苯基)乙基]胺基}-6-苯基(3-吼啶基))-Ν-(3』比咬 0.107 M+H 427.1 基甲基)曱醯胺 (2-{[2-(2,6-二氟苯基)乙基]胺基}-6-苯基(3-吼啶基))-Ν-(3- 0.288 M+H 445.1 吡啶基甲基)甲醯胺 (2-{Ρ-(3,5-二氟苯基)乙基]胺基}-6-苯基(3-口比啶基))-Ν-(3- 0.055 M+H 445.1 吡啶基甲基)甲醯胺 (2-{[2-(3,4-二氟苯基)乙基]胺基}-6·苯基(3-吼啶基))-Ν-(3- 0.521 M+H 445.2 。比啶基甲基)甲醯胺 (2-{[2-(2,5-二氟苯基)乙基]胺基}-6-苯基(3-吼啶基))-Ν-(3- 0.079 M+H 445.2 吡啶基甲基)曱醯胺 [6-苯基-2-({2-[3-(三氟甲基）苯基]乙基）胺基)(3-吼啶 8.254 M+H 477.2 基)]-Ν-(3·咕啶基曱基)甲醯胺 (2-{[2-(3-氟苯基)乙基]胺基}-6-(4-甲基(2-噻吩基))(3』比啶 0.148 M+H 447.2 基))-Ν-(3-«比啶基曱基)曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(3-噻吩基）(3-吡啶 0.048 M+H 433.1 基))-N-(3-吼啶基甲基)甲醯胺 (2-{[2-(2-氰基苯基)乙基]胺基}-6-苯基(3-。比啶基))-N-(3-口比 0.26 M+H 443.1 啶基曱基)甲醯胺 (2- {[2-(3-氰基苯基)乙基]胺基} -6-苯基(3-°比β定基))-Ν-(3·σ比 4.649 M+H 434.1 啶基曱基)甲醯胺 245 200823188 IC50 算數平均 離子 m/z 化學名稱 36.722 M+H 425.1 (2-{[2-(4-羥基苯基)乙基]胺基}-6-_苯基(3』比啶基))· Ν·(3·σ比 啶基甲基)甲醯胺 2.431 M+H 425.1 (2-{[2-(2·羥基苯基)乙基]胺基}各苯基(3』比啶基))_ Ν-(3-σ比 啶基曱基)曱醯胺 27.106 M+H 424.1 (2-{[2-(4-胺基苯基)乙基]胺基Η-苯基(3』比啶基))· Ν·(3』比 啶基曱基)曱醯胺 11.492 M+H 452.1 3-[2-({6-苯基-3-[Ν-(3-吼啶基甲基)胺甲醯基1冬°比啶基}胺 基)乙基]苯甲醯胺 0.04 M+H 451.1 (2-{[2-(3,5-二氟苯基）乙基]胺基}-6-(3-噻吩基)(3-°比啶 基))-N-(3-吼啶基甲基)甲醯胺 0.119 M+H 465.1 (2-{[2-(3,5-二氟苯基）乙基]胺基}各(4-甲基(2-噻吩基))(3-°比啶基))-N-(3-°比啶基曱基)曱醯胺 0.041 M+H 470.1 (2-{[2-(3,5-二氣苯基）乙基]胺基}-6-(2-氰基苯基）（3_°比啶 基))-N-(3-叱啶基曱基)甲醯胺 0.137 M+H 433.1 (2-{[2·(3-氟苯基）乙基]胺基}-6-(2-噻吩基）(3-吼啶 基))-N-(3-吡啶基甲基)甲醯胺 0.097 M+H 451.1 (2-{[2-(3,5-二氟苯基）乙基]胺基}-6-(2-噻吩基)(3-吼啶 基))-N-(3-吼啶基甲基)甲醯胺 28.097 M+H 467.2 3-[2-({6-苯基-3-[N-(3-吼啶基甲基)胺曱醯基]-2-吼啶基}胺 基)乙基]苯甲酸甲酯 16.384 M+H 470.2 2-(6-{[2-(3-氟苯基)乙基]胺基}-5-[N-(3-啦啶基甲基)胺曱醯 基]-2-吡啶基)苯甲醯胺 0.198 M+H 445.2 (6-(4-氟苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-(3-吼啶基甲基)甲醯胺 21.862 M+H 453.2 3-[2-({6-苯基-3-[N-(3-吡啶基甲基)胺曱醯基]-2-吡啶基}胺 基)乙基]苯甲酸 1.383 M+H 479.1 (6-(2-氯-4-氟苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-。比π定 基))-Ν-(3-吼啶基甲基)曱醯胺 0.138 M+H 463.1 (2-{[2-(3,5-二氟苯基）乙基]胺基卜6-(4-氟苯基)(3_。比啶 基))-Ν-(3-吼啶基甲基)曱醯胺 0.038 M+H 470.1 (6_(2_氰基冰敗苯基)-2_{[2_(3-氟苯基）乙基]胺基}(3-η比啶 基))-Ν-(3-吼啶基甲基)曱醯胺 246 200823188 IC50 算數平均 離子 m/z 化學名稱 (6-(2-氯-6-氟苯基)-2-{[2-(3-氟苯基）乙基；i胺基}(3·吡啶 0.54 M+H 479.1 基))-Ν-(3-吼啶基甲基)曱醯胺 (6-(2-氯-5-甲氧基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3_吡啶 2.005 M+H 491.1 基))-N-(3-吼啶基甲基)曱醯胺 (6_(2·氰基甲氧基苯基)-2-{[2_(3_敗苯基)乙基]胺基}(3-°比 0.041 M+H M+氯 482.1 啶基吡啶基甲基)曱醯胺 (6-(2_氰基-6-氟苯基)·2·{[2_(3-默苯基)乙基]胺基比咬 0.086 Η 470.1 基))-N-(3-吼啶基甲基)曱醯胺 (6-(2- 1苯基）-2-{[2-(3-氣苯基）乙基]胺基}(3- η比咬 0.139 M+H 445.1 基))-Ν-(3·吼啶基甲基)甲醯胺 (2-{[2-(2, 3-二氟苯基）乙基]胺基}-6-(2_氰基苯基)(3-吡啶 0.022 M+H 470.1 基))-N-(3-吼啶基甲基)曱醯胺 (6-(2-氯-5-氟苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-ϋ比嗅 1.327 M+H 479.1 基))-Ν-(3-吼啶基甲基)甲醯胺 (6_(2_氰基氟苯基)-2_{[2-(3_就苯基）乙基]胺基}(3-吼啶 0.053 M+H 470.1 基))-Ν-(3-吼啶基曱基)甲醯胺 (6-(3-氟苯基）-2-{[2-(3-氟苯基）乙基]胺基}(3_ σ比啶 0.157 M+H 445.1 基》-Ν-(3-吼啶基甲基)甲醯胺 (6-[2-(氰基曱基)苯基]-2-{[2_(3-氟苯基)乙基]胺基}(3-吼啶 16.392 M+H 466.2 基))_Ν-(3·η比啶基甲基)甲醯胺 (2-{[2_(3-氟苯基)乙基]胺基}_6_[3_(經基甲基)(2-嗟吩基)](3- 2.245 M+H 463.1 σ比啶基))-Ν-(3-吡啶基曱基)曱醯胺 (2-{[2_(3-氟苯基)乙基]胺基}-6-(5-曱醯基(3_噻吩基))(3』比 0.098 M+H 461.1 啶基))-Ν-(3-吡啶基曱基)甲醯胺 (2-{[2-(3-氟苯基)乙基]胺基}各[5-(經基曱基)(3-噻吩基)](3- 0.073 M+H 463.1 σ比啶基))-Ν-(3-σ比啶基曱基)曱醯胺 (6-(2-氯-4-甲基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3_ϋ比σ定 2.078 M+H 475.1 基))-Ν-(3-吼啶基甲基)曱醯胺 (6-(2-氰基冬甲基苯基)冬{[2-(3-氟苯基)乙基]胺基}(34匕啶 0.996 M+H 466.2 基))-Ν-(3』比啶基曱基)曱醯胺 (2-{[2-(3-氟苯基)乙基]胺基}各[Η經基曱基)苯基](3』比唆 0.281 M+H 457.1 基))-Ν-(3-吼啶基甲基)甲醯胺 247 200823188 IC50 算數平均離子 m/z 5.719 Μ+Η 471.2 78.064 Μ+Η 419.1 1. 185 Μ+Η 491.1 12.904 Μ+Η 475.2 5.022 Μ+Η 475.2 4.812 Μ+Η 434.1 1.209 Μ+Η 581.2 0.008 Μ+Η 456.1 0.043 Μ+Η 446.1 0.032 Μ+Η 460.1 2.148 Μ+Η 458.2 0.336 Μ+Η 458.2 0.572 Μ+Η 515.2 3.874 Μ+Η 529.2 0.755 Μ+Η 515.2 1.261 Μ+Η 529.2 化學名稱 (2-{[2·(3-氟苯基)乙基]胺基}-6-[3-(甲氧基曱基)苯基](3』比 啶基吼啶基甲基)甲醯胺 (6-(1Η-1，2,3,4-四唑基)冬{[2-(3-敗苯基)乙基]胺基}(3』比 啶基;吡啶基甲基)甲醯胺 (6·[2-氯4㈣基甲基)苯基]_2-{[2_(3-敗苯基)乙基]胺基}(3- ϋ比啶基))-Ν-(3-σ比啶基甲基)曱醯胺 (2R)-2-胺基-4-[(6-(2-氰基苯基&gt;2·{[2-(3-氟苯基）乙基]胺 基}(3-吡啶基))羰基胺基]-Ν-曱基丁醯胺 (2S)-2-胺基-4-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-咐啶基))羰基胺基]-Ν·甲基丁醯胺 Ν-(3-胺基-2-羥基丙基)(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙 基]胺基}(3-吡啶基))甲醯胺 N-[(2-{[(第三丁氧基）羰基胺基]曱基}(3-吨啶基)）曱 基](6-(2-氰基苯基)-2_{[2_(3-氟苯基)乙基]胺基}(3-吼啶基)) 甲醯胺 N-{[2-(胺基甲基)(3-吼啶基)]甲基}(2-{[2-(3-氟苯基）乙基] 胺基}-6-苯基(3-吼啶基))甲醯胺 N-{[2-(胺基甲基)(3-吼啶基)]甲基}(2-{[2-(3-氟苯基）乙基] 胺基}_6_吡唑-3-基(3-吡啶基X)甲醯胺 N-{[2-(胺基甲基)(3-吼啶基)]曱基}(2-{[2-(3-氟苯基）乙基] 胺基}-6-(1-曱基口比。坐-3-基)(3-口比。定基))曱酸胺 N-[((3R)(3-派啶基))曱基](6-(2-氰基苯基)-2-{[2-(3-氟苯基） 乙基]胺基}(3-吡啶基)）曱醯胺 (6-(2-氰基苯基)·2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-Ν-(4-哌啶基曱基)曱醯胺 Ν-{[1-(2-胺基乙醯基)(4-哌啶基)]甲基}(6-(2-氰基苯 基)-2_{[2-(3_敗苯基)乙基]胺基}(3-吼啶基))曱醯胺 Ν-{[1-(3-胺基丙醯基)(4-哌啶基)]甲基}(6-(2-氰基苯 基)-2_{[2-(3_敗苯基)乙基]胺基}(3-吼啶基))甲醯胺 N-{[(3S)-l-(2-胺基乙醯基)(3-哌啶基)]曱基}(6-(2_氰基苯 基)-2_{[2-(3_氟苯基)乙基]胺基}(3』比啶基))甲醯胺 N-{[(3S)-l-(3-胺基丙醯基)(3-略σ定基)]甲基}(6-(2-氰基苯 248 200823188 IC50 算數平均 離子 m/z 化學名稱 基)-2-{[2_(3·氟苯基)乙基]胺基}(3』比啶基))甲醯胺· N-[(l-乙醯基(4-哌啶基))曱基](6-(2-氰基苯基)冬{[2-(3•氟 1.696 M+H 500.3 苯基)乙基]胺基}(3-吡啶基))甲醯胺 N-[((3S)-1-乙醯基（3-旅。定基））甲基](6-(2-氰基苯 10.729 M+H 500.3 基)·2·{[2·(3-氟苯基)乙基]胺基)(3·吼唆基))甲醯胺 Ν-{[1-(4-胺基丁醯基)(4-哌啶基)]甲基}(6-(2-氰基苯 6.009 M+H 543.3 基)_2_{|&gt;(3-氟苯基)乙基]胺基}(3·批啶基))甲醯胺 4-{[(6-(2_氰基苯基)-2-{[2-(3_氟苯基)乙基]胺基比啶基) 2.13 M+H 516.3 羰基胺基]曱基}哌啶羧酸曱酯 N-[((2R)(2·哌啶基))曱基](6-(2_氰基苯基)-2-{[2_(3_氟苯基) 1.159 M+H 458.3 乙基]胺基}(3-吡啶基))甲醯胺 N-{[(2R)-l-(2-胺基乙醯基)(2-哌啶基)]甲基}(6-(2-氰基苯 0.092 M+H 515.3 基)·2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 Ν-{[(2R)-1-(3-胺基丙醯基)(2-哌啶基)]甲基}(6-(2-氰基苯 0.155 M+H 529.2 基)-2_ {[2_(3 -氟苯基)乙基]胺基} (3 - η比咬基))甲酷胺 N-{[(2R)-l-(4-胺基丁醯基)(2-哌啶基)]甲基}(6-(2-氰基苯 0.083 M+H 543.2 基)-2_{[2·(3-氟苯基)乙基]胺基}(3』比咬基))甲酸胺 N-[((2R)-1-乙醯基（2·哌啶基））甲基](6-(2-氰基苯 2.676 M+H 500.2 基)-2_{[2_(3-氟苯基)乙基]胺基}(3』比啶基))甲醯胺 (2R)-2-{[(6_(2-氰基苯基)-2·{[2-(3-氟苯基)乙基]胺基}(3_σ比 4.282 M+H 516.3 啶基))羰基胺基]甲基}哌啶羧酸曱酯 N-({(2R)-l-[(3_胺基丙基)石黃酸基](2-π辰σ定基)}曱基)(6_(2_氰 0.37 M+H 579.2 基苯基)-2-{[2_(3_氟苯基)乙基]胺基吼啶基))甲醯胺 N-[((2R)-1-甲基(2_ 哌啶基))甲基](6·(2-氰基苯基)-2-{[2_(3_ 0.488 M+H 472.2 氟苯基)乙基]胺基}(3-°比。定基))甲驢胺 N-{[(2R)-l-((2R)_2,3c胺基丙醯基)(2·哌啶基)]甲基}(6-(2- 0.161 M+H 544.3 氰基苯基)-2-{[2_(3-氟苯基)乙基微基}(3_吡啶基))曱醯胺 N-{[(2R)-1-((2R)_2,4^胺基丁醯基)(2-哌啶基)]曱基}(6-(2_ 0.399 M+H 558.3 氰基苯基)·2_{[2_(3-氣苯基)乙基]胺基}(3-吼啶基))曱醯胺 N-{[(2R)-1-((2R)_2,5-二胺基戊醯基)(2-哌啶基)]曱基}(6-(2_ 0.456 M+H 572.2 氰基苯基)-2-{[2_(3·氟苯基)乙基]胺基}(3_吼啶基))曱醯胺 0.178 M+H 565.2 N-({(2R)-l-[(2-胺基乙基)磺醯基](2-哌啶基)}甲基)(6-(2-氰 249 200823188 IC50 算數平均 離子 m/z 化學名稱 0.048 M+H 572.3 基苯基)-2-{[2-(3-敗苯基)乙基]胺基}(3-°比唆基))曱醢胺 N-{[(m)小((2S)-2,5-二胺基戊醯基)(2-哌啶基)]曱基}(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 0.052 M+H 529.3 N-{[(2R)-l-((2S)-2-胺基丙醯基)(2-哌啶基)]曱基}(6-(2-氰基 苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比啶基))甲醯胺 0.261 M+H 529.2 N-{[(2R)-l-((2R)-2-胺基丙醯基)(2-哌啶基)]曱基}(6-(2-氰 基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 2.691 M+H 564.1 (2R)-2-{[(6-(2-氰基苯基)·2-{[2-(3-氟苯基)乙基]胺基}(3-口比 啶基))羰基胺基]甲基}哌啶羧酸2-氯乙基酯 0.091 M+H 545.2 (2R)-2-{[(6-(2-氰基苯基)-2-脚_氟苯基）乙基]胺 基}(3-吡啶基))羰基胺基]甲基}哌啶羧酸2-胺基乙基酯 0.023 M+H 547.2 N-{[(2R)-l-(4-胺基丁醯基户比咯啶-2-基]曱基}(2-{[2-(3,5-二 氟苯基)乙基]胺基}-6-(2-氰基苯基)(3-吼啶基))甲醯胺 0.133 M+H 515.3 N-{[(2R)-l-(4-胺基丁醯基)吼咯啶-2-基]曱基}{6-(2-氰基苯 基)-2-[(2-環己-1-稀基乙基)胺基](3-吼啶基)}曱醯胺 3.56 M+H 506.2 3-{[3-(N-{[(2R)-l-(4-胺基丁醯基)吼咯啶-2-基]甲基}胺甲 醯基)-6-(2-氰基苯基)(2-吼啶基)]胺基}-N，N-二甲基丙醯胺 0.062 M+H 511.2 N-{[(2R)-l-(4-胺基丁醯基)。比咯啶-2-基]甲基}{6-(2-氰基苯 基)-2-[(2-苯基乙基)胺基](3』比啶基)}曱醯胺 8.167 M+H 519.2 N-{[(2R)-l-(4-胺基丁醯基)吼咯啶-2-基]曱基}{6-(2-氰基苯 基)-2-[(2-(2H-3,4,5,6-四氫哌喃斗基)乙基)胺基](3-吼啶基)} 曱醯胺 2.038 M+H 519.2 N-{[(2R)-l-(4-胺基丁醯基户比咯啶-2-基]曱基}{6-(2-氰基苯 基)-2·[(2-(2 H-3,4,5,6-四氫哌喃-2-基）乙基)胺基](3-吼啶 基)}曱醯胺 0.059 M+H 530.2 N-{[(2R)-l-((2S)-2,3-二胺基丙醯基）吼咯啶-2-基]甲 基}(6-(2-氰基苯基)_2-{[2-(3-氣苯基)乙基]胺基}(3』比啶基)) 曱醯胺 0.193 M+H 545.2 N_{[(2R)-l-((2S)-2-胺基-3-曱氧基丙醯基)吼咯啶-2-基]甲 基}(6-(2-氰基苯基)·2-{[2-(3-敗苯基)乙基]胺基咐啶基)) 甲醯胺 0.173 M+H 531.2 N-{[(2R)小((2S)-2-胺基-3-羥基丙醯基）吼咯啶-2-基]甲 250 200823188 IC50 算數平均離子 m/z 化學名稱 基}(6_(2_氰基苯基)-2-{[2_(3_氟苯基)乙基]胺基}(3』比咬基)) 甲醯胺 0.014 Μ+Η 464.1 Ν-{[2·(胺基甲基)(3』比啶基)]甲基}(5-氟-2-{[2-(3-敗苯基) 乙基]胺基}-6-σ比峻-3-基(3_σ比σ定基))甲醯胺 0.108 Μ+Η 484.1 N-{[(2R)-l-(2-胺基乙醯基）ϋ比咯啶-2-基]甲基}(5-氟 _2-{[2-(3-氟苯基）乙基]胺基比唾冬基（3_σ比咬 基)）甲醯胺 0.269 Μ+Η 514.1 N-{[(2R)-l-((2S)-2_胺基-3-羥基丙醯基）吡咯啶-2-基]甲基}(5-敦-2- {[2-(3-氟苯基）乙基]胺基卜6-吼唾 -3-基(3·吡啶基)）曱醯胺 0.314 Μ+Η Μ+Η 498.2 N-{[(2R)-l-((2S)-2-胺基丙醯基）吡咯啶冬基]曱 基}(5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-吼唑-3-基 (3-吡啶基)）曱醯胺 0.169 Μ+Η 512.1 N-{[(2R)-l-(4-胺基丁醯基）响咯啶-2-基]甲基}(5-氟 -2-{[2-(3-氟苯基）乙基]胺基}-6-°比唾-3-基（3-°比。定 基)）甲酸胺 0.92 Μ+Η 428.1 {6_(2_氰基苯基)-2_[(2-氧雜戊環-2-基乙基)胺基](3-吼σ定 基)}-Ν-(3-吼啶基甲基)曱醯胺 0.398 Μ+Η 415.1 N-((2R)-2-胺基丙基）(5-氟-2-{[2-(3-氟苯基）乙基]胺 基}-6-(1_曱基吼唑-4-基)(3-σ比啶基))曱醯胺 1.754 Μ+Η 572.2 N-{(1 R)_2-[(5_氟-2-{[2-(3_氟苯基)乙基]胺基}各(1·曱基0比 唑斗基)(3-吡啶基))羰基胺基]-異丙基}冬[(第三丁氧基邊 基胺基]乙醯胺 0.076 Μ+Η 472.3 N-{(lR)-2-[(5-氣-2-{[2-(3-氟苯基）乙基]胺基}-6-(1·甲基 η 比 唑斗基)(3-吡啶基))幾基胺基]-異丙基}-2-胺基乙醯胺 0.027 Μ+Η 455.1 N-[((2R)-5·氧基°比略咬_2_基)甲基](5·氟_2_{[2_(3_氟苯基)乙 基]胺基Η-(1-甲基吡唑_4_基)(3-吡啶基))曱醯胺 1.804 Μ+Η 272.3 N-{(1S)_2_[(5-氟-2·{[2-(3_氟苯基）乙基]胺基}各(1_曱基^比 唑冰基)(3-吼啶基)博基胺基]-異丙基卜2-胺基乙醯胺 0.197 Μ+Η 473.1 N-{(lR)_2-[(5-說-2-{[2_(3_氟苯基）乙基]胺基}各(1_甲基。比 σΚ基)(3_吼。定基))幾基胺基]-異丙基卜2-經基乙隨胺 0.1 Μ+Η 600.2 N-{(lR)_2-[(5_氟-2_{[2-(3_氟苯基)乙基]胺基}各(1_曱基,比 251 200823188 IC50 算數平均 0.116 2.328 8.211 0.443 0.251 1.002 0.122 0.024 0.648 0.636 0.121 2.264 0.115 0.285XII is tested on 4-((R)-2-((6-(2-cyanophenyl)-2-(2-(tetrahydro-2H-pyran-2-yl)ethylamino)) Amino) fluorenyl) π 嘻唆 嘻唆 ) -4- ) ) ) -4- -4- -4- 47 47 47 47 47 47 47 47 47 47 47 47 47 Me Me Me Me Me Me Me 加入 加入 加入 加入 加入 加入TMSI (72 mg, 0·36 mmol). The mixture was stirred at room temperature for 2 hours and purified by RP-HPLC using acetonitrile and a mixture of &lt;RTI ID=0.0&gt;&&&&&&&&&&&&&&&& -(2.Cyanophenyl)-2-(2-(tetrahydro-2H-piperidin-2-yl)ethylamino)nicotinamide (36 226 200823188 mg, 77%). LRMS (M +H+) m/z 519.3. Example 13 The following compounds were synthesized and tested using a procedure similar to that described herein. IC50 arithmetic mean ion m/z chemical name 3.123 M+H 359.2 {6-phenyl-2-[( 2-(2-σ ratio base) ethyl)amino](3-π ratio π-decyl)}-N-prop-2-enylamine 6.747 M+H 346.2 N-methyl (2-{ [2-(3-Methylphenyl)ethyl]aminobiphenyl 6-phenyl (3_σ-pyridyl))carhamamine 18.628 M+H 332.2 Ν-methyl {6-phenyl-2-[( 2-phenylethyl)amino](3_,pyridyl)}mercaptoamine 1.062 M+H 358.2 {6-phenyl-2-[(2-phenylethyl)amino](3-吼Pyridyl)}-Ν-prop-2-enylcarbinamine 3.74 M+H 372,3 (2^2-(3-methylphenyl)ethyl]amino}_6_phenyl (3_. ratio Bite base))-Ν-prop-2-enylcarbamamine 27.729 M+H 333.2 Ν-fluorenyl {6-phenyl·2-[(2_(2·pyridyl)ethyl)amino](3) -Acridine )}Metamine 1.564 M+H 409.2 Ν-phenylhydrazino {6-phenyl·2_[(2-(2-acridinyl)ethyl)amino](3′′pyridinyl)}carboxamide 0.151 M+H 409.2 {ό-phenyl-2_[(2_phenylethyl)amino](3′′ 口 定 ))}_Ν_(3′′ 咬 甲基 甲基 13 13 13 13 13.296 M+H 361.3 Ν-(mercaptoethyl){卜phenyl_2_[(2_(2_,pyridyl)ethyl)amino](3_吼.定)) decylamine 0.463 M+H 410.1 {6_Benzene Base 1[(2-(2-pyridyl)ethyl)amino](3_0-pyridyl)}(2′′°°-methyl)carbamamine 1.29 M+H 410.2 {ό-phenyl-2_ [(2·(2_pyridyl)ethyl)amino](3_σ-pyridyl)}(冬°比咬基曱)carbamamine 5.373 M+H 396.2 {ό-phenyl-2_[( 2_(2-.pyridyl)ethyl)amino](indenidinyl)}-Ν-(3-σ*σ定227 200823188 IC50 arithmetic mean ion m/z chemical name 7.189 M+H 396.2 basis) Methionamine·{Phenyl hydrazide [(2-(2-pyridyl)ethyl)amino](3_♦)}-N-(2-Acridine)carbamamine 5.209 M+H 396.2 { 6_phenyl-2·[(2-(2-acridinyl)ethyl)amino](3′′pyridyl)}-N-(4′pyridyl)carhamamine 1.721 M+H 415.2 { Phenyl-2-[[2(2-acridinyl)ethyl)amino](3) ratio啶 ))}-N-〇 吩 曱 曱 曱醯 0.6 0.6 0.6 0.683 M+H 415.2 {6_phenyl-2-[(2-(2_π-pyridyl)ethyl)amino]pyridinyl) W3·Thienyl fluorenyl)carbamamine 11.022 M+H 403.3 N-(oxapenta-2-ylindenyl){6-phenyl-2-[(2-indolyl)ethyl Amino](3·σ-pyridyl))decylamine 6.821 M+H 403.2 N-[((2S)oxalanyl)-yl]{6_phenyl_2-[(2- (2"pyridinyl)ethyl)amino](3"-specific base)}mercaptoamine 65.098 M+H 518.2 2_[({6_phenyl_2_[(2-(2)-pyridyl) Ethyl)amino]pyridinyl}carbonylamino)methyl]morphincarboxylic acid tert-butyl ester 96.68 M+H 458.3 N-[(l-ethinyl(4-piperidinyl))methyl] Phenyl 2 -[(2_(2-0-pyridyl)ethyl)amino]] (3-° ratio) 曱醯amine 48.434 M+H 458.3 N-[(l-ethylidene) _ piperidinyl)) fluorenyl] {6_phenyl-2_[(2-(2^pyridyl)ethyl)amino](3·σ-pyridyl)} decylamine 43.709 M+H 416.3 {6·Phenyl-2-[(2_(2-acridinyl)ethyl)amino](3_acridinyl)}(4-piperidylhydrazinyl)carbamamine 0.532 M+H 413.2 {2-[(2-cyclohex-1-ethylideneethyl)amino]-6-phenyl (3-° ratio ° base)}-Ν-(3-σ-pyridylmethyl) formamide 5.68 9 M+H 423.3 {6_phenyl_2_[(3-phenylpropyl)amino](3-σ ratio)>-Ν-(3-σ1^σ疋yl) guanamine 2.792 M+H 395.2 {ό-phenyl[benzylamino](3-pyridyl)}-indole-(3-acridinylmethyl)decylamine 4.897 M+H 400.2 Ν-( 1,3 -carbazol-2-ylindenyl){6-phenyl-2-[(2-(2-acridinyl)ethyl)amino](3-pyridyl)}carbamimid 6.148 M+H 399.1 Ν-(imidazol-2-ylindenyl){6-phenyl-2·[(2-(2-. Bipyridyl)ethyl)amino](3-pyridyl)}carbamamine 15.715 M+H 444.3 N-[((2S)-1-ethylindolyl σ-pyridin-2-yl)indolyl] {6-Phenyl-2-[(2-(2. acridine 228 200823188 IC50 arithmetic mean ion m/z chemical name 26.904 M+H 444.3 base) ethyl)amino]] (3-° thiol)} Indoleamine N-[((3R)-1.Ethyl)pyrrolidyl-3-yl)indolyl]{6-phenyl-2-[(2-(2-acridinyl)ethyl) Amino](3-pyridyl)}decylamine 25.159 M+H 444.3 N-[((3S)-1-Ethylpyrrolidino-3-yl)methyl]{6-phenyl-2-[ (2-(2-Pyridyl)ethyl)amino](3-pyridyl)}carbamamine 1.335 M+H 390.2 2-({6-phenyl-2-[(2-phenylethyl)) Methylamino-3-pyridinyl}carbonylamino)acetate 11.377 M+H 347.1 [6-phenyl-2-(propylamino)(3-.pyridyl)]-N-(3 -acridinyl fluorenyl) guanamine 2.484 M+H 375.2 {2-[(3-mercaptobutyl)amino]-6-phenyl(3-pyridyl)}-N-(3-pyridyl Methyl) decylamine 1.854 M+H 415.3 {2-[(2-cyclohexylethyl)amino]-6-phenyl(3-acridinyl)}-N-(3-acridinylmethyl) ) guanamine 20.292 M+H 494.3 fluorenyl fluorenyl) (3-. chinyl) methyl} {6-phenyl-2-[(2-(2-)-ethyl)ethyl Amino](3-pyridyl)}decylamine 18.23 M+H 416.3 2-(Aminomethyl)piperidinyl 6-phenyl-2-[(2-(2-acridinyl)ethyl) Amino](3-pyridyl)one 21.154 M+H 458.3 Ν-{[1-({6-phenyl-2-[(2-(2-)acyl)ethyl)amino]-3 -acridinyl}carbonyl)-2·piperidinyl]fluorenyl}acetamide 22.226 M+H 494.3 2-{[(methylsulfonyl)amino]indolyl}piperidinyl 6-phenyl- 2-[(2-(2-pyridyl)ethyl)amino](3-acridinyl)one 1.298 M+H 413.2 N-[(l-fluorenylcarbazol-5-yl)methyl]{ 6-phenyl-2-[(2-(2-acridinyl)ethyl)amino](3-pyridyl)}decylamine 2.733 M+H 413.2 N-[(l-decylpyrazole- 3-yl)methyl]{6-phenyl-2-[(2-(2)pyridyl)ethyl)amino](3-pyridyl)}decylamine 0.711 M+H 399.2 {6- Phenyl-2-[(2-(2-acridinyl)ethyl)amino](3-acridinyl)}-N-(carbazol-3-ylmercapto)carbamamine 0.836 M+H 400.2 N-(iso-opoisole-5-ylindenyl){6-phenyl-2-[(2-(2-acridinyl)ethyl)amino](3-pyridyl)}decylamine 62.553 M+H 402.3 N-[((3S) fluoren-3-yl)methyl]{6-phenyl-2-[(2-(2-). Pyridyl)ethyl)amino](3-acridinyl)} decylamine 53.616 M+H 402.3 N-[((m-pyrrolidyl)-yl)]{6-phenyl-2- [(2-(2-Acryl)ethyl)amino](3-pyridyl)}carbamamine 229 200823188 IC50 arithmetic mean ion m/z chemical name 5.245 M+H 423.3 {6_benef·2 :[(2_本基ethyl)amino](3·π ratio decyl)}-Ν·(2_(2-τϊ ratio σ定基) Ethyl) decylamine 3.093 M+H 423.2 {6·Benzene ·····((2-phenylethyl)amino](ρ ratio) ν-(2-(3-° ratio) ethyl) decylamine 0.486 M+H 389.2 Ν-甲Benzyl-2-({6-phenyl-2-[(2-phenylethyl)amino]] (3-17 to 0-based)}]-phenylamino)acetamide 30.309 M+H 403.3 Ν,Ν - Dimercapto-2-({6-phenyl-2-[(2-phenylethyl)amino](3-pyridylcarbonylamino)acetamide 0.81 M+H 375.2 formate methyl) Phenyl 2 -[(2-phenylethyl)amino]pyrene)amine oxime 22.145 M+H 430.3 (2][2-(2-oxypiperidinyl)ethyl]amine }_6·Phenyl(3′′pyridinyl))-Ν-(3-pyridylmethyl)decylamine 20.145 M+H 430.3 (2-{[2-(1-methyl(4-) )) ethyl]amino}-6-phenyl (3-σ ratio), -Ν-(3-pyridylfluorenyl)曱醯0.149 M+H 415.2 {Phenyl-2-[[2-(2-thienyl)ethyl)amino](3"pyridinyl)}- Ν-(3-acridinylmethyl)anthracene Amine 32.174 M+H 413.2 (2-{[2-(1-methylimidazolidinyl)ethyl]amino}-6-phenyl(3-indole))-N-(3-pyridyl) Methionine 0.294 M+H 399.2 {2-[(2-(2-furyl)ethyl)amino]-6-phenyl(3·acridinyl)}-N-(3-acridine Methyl)carbendazim 4.835 M+H 389.2 [(oxapentan-2-ylmethyl)amino]-6-phenyl(3-acridinyl)}-N-(3-port ratio ° Stationary methyl)carbamamine 7.122 M+H 405.2 d(2-(l,3-dioxolan-2-yl)ethyl)amino]-6-phenyl(3-acridinyl)}- N-(3-pyridylfluorenyl)carbamamine 30.307 M+H 413.3 仏[(3^Mizolylpropyl)amino]phenyl(3-pyridyl)}-N-(3·pyridyl) Methyl) anthraquinone 37.33 M+H 418.3 "2-[(2-morpholin-4-ylethyl)amino]-6-phenyl(3-pyridyl)}-N-(3-pyridyl) Mercapto)carbamamine 20.164 M+H 425.2 to phenyl-2-[(2-phenoxyethyl)amino](3′′pyridinyl)}-N-(3′′pyridylfyl) Entrained amine 28.307 M+H 453.2 {2-[(2-(2H-benzo[3,4-d]l,3-dioxocyclopentenyl)ethyl)amino]·6-phenyl ( 3 比 pyridine Aminopyridylmethyl)guanamine 230 200823188 IC50 arithmetic mean ion m/z Chemical name - (2-{[2-(2-oxyimidazolidinyl)ethyl]aminobiphenyl 6-phenyl (3 -pyridine 70.65 M+H Χ)-Ν·(3_pyridylmethyl)methalinoxypyrrolidinyl)ethyl]amino}-6-p henyl (3-pyridine 10.62 M+H 416.2 ))-N-(3_Pyridylmethyl)methanoamine {2-[(2-imidazol-4-ylethyl)amino]-6-phenyl(3-°pyridinyl)}-N -(3-n-pyridyl 9.766 M+H 399.2-methyl) decylamine (2-{[(hydroxycyclohexyl)decyl]amino}ylphenyl(3-pyridyl))-N-(3 -pyridine 7.811 M+H 417.3 methyl group decylamine (2-{[2-(3,5-dimethyloxazol-4-yl)ethyl]amino}-6-phenyl (3- Acridine 5.941 M+H 427.2 base))-N-(3-pyridylmethyl)decylamine (2-{[2-(3,5-didecyloxazolyl)ethyl]amino}- 6-phenyl (3-. Bispin 6.833 M+H 427.2 base))-N-(3-acridinylmethyl)carbenamide (2-{[2-(2-phenylphenyl)ethyl]amino}-6-(2 -cyanophenyl)(3-acridine 0.028 M+H 468.2 base))-N-(3-pyridylfluorenyl)formamide (6-(2-cyanophenyl)-2-{[2 -(2-mercaptophenyl)ethyl]amino}(3-acridine 0.076 M+H 448.2 base))-N-(3-.pyridylhydrazino)decylamine (6-(2- Cyanophenyl)-2-{[2-(2-fluorophenyl)ethyl]amino}(3-acridine 0.028 M+H 452.2))-N-(3-pyridylmethyl)methyl Indoleamine (6-(2-cyanophenyl)-2-{[2-(2-cyanophenyl)ethyl]amino}(3-u-pyridyl 0.044 M+H 458.2))-N -(3-Acridinemethyl)guanamine {6-(2-cyanophenyl)-2-[(2-(2-thienyl)ethyl)amino](3-.pyridyl 0.029 M+H 440.2 base)}-N-(3-pyridylfluorenyl) decylamine {6-(2-cyanophenyl)-2-[(2-(2-furyl)ethyl)amine (3- η pyridine 0.065 M+H 424.2 】)-Ν-(3-acridinyl fluorenyl)carbamamine (2-{[2-(3-fluoropyridyl))ethyl]amine }--6-phenyl (3-pyridine 1.479 M+H group))-N-(3-pyridylmethyl)formamide (2-{[2-(3-methylphenyl)ethyl] Amino}-6-phenyl(3-pyridyl))-N-(3-pyridin 0.45 M+H 423.3 pyridine Indoleamine (6-(2-cyanophenyl)-2-{[2-(2-hydroxyphenyl)ethyl]amino} (3-acridine 0.38 M+H 450.1)) -N-(3-pyridylmethyl)decylamine N-{[2-(aminomethyl)(3-σ-pyridyl)]fluorenyl} {6"bisazol-4-yl-2- [(2-(2-port ratio 1.238 M+H 429.1 pyridine)ethyl)amino](3-pyridyl)}carbamamine 231 200823188 IC50 arithmetic mean ion m/z chemical name N-{(lR) -2-[(5·Fluor-2·{Ι&gt;(3-fluorophenyl)·2·Leptylethyl]amino}-6-port ratio 嗤冬基(3_° ratio of base))#炭Amino]-isopropyl}-2-[(tatabutoxy)carbonyl 14.214 M+H 574.3 aminoamino]acetamide {5-fluoro-6-oxazol-4-yl-2-[ (2-σ-pyrazolylethyl)amino](3-acridine 0.211 M+H 407.3 base)}-Ν-(3-acridinylmethyl)carbamamine N-[(lR)-2- ({5-Fluoro-6-pyrazol-4-yl-2-[(2-pyrazolylethyl)amino](3_pyrid 4.635 M+H 430.3 pyridine)}carbonylamino)_isopropyl 4-aminoacetamide (6-(2-cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl]amino} (3- ° 唆0.604 M+H 520.1 base))-N-{[6-(trifluoromethyl)(24 pyridine)]methyl}carboxamide (6-(2-cyanophenyl)-2-{[2-(3- Fluorophenyl)ethyl]amino}(3-bite 1.497 M+H 520.1 base))-N-{[5-(trifluoromethyl)(2-pyridyl)]methyl}decylamine (6-(2-cyanophenyl)-2-{[2-(3- Fluorophenyl)ethyl]amino}(3-吼唆0.603 M+H 520.1 base))-N-{[3-(trifluoromethyl)(2-pyridyl)]decyl}nonanylamine N -[(6·chloro(P-pyridyl))indenyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl) 1.789 M+H 486.1 ethyl]amino }(3-pyridyl))carzamide (6-(2-cyano(3-thienyl))-2-{[2-(3-fluorophenyl)ethyl]amino}(3·- Biscridium 0.033 M+H 458.1 base))-N-(3-acridinyl mercapto)carboxamide (2E)-3-(2-{[2-(3-fluorophenyl)ethyl]amine }-6-phenyl(3-acridinyl))-N- 57.378 M+H 376.1 mercaptoprop-2-enylamine (6-(2-cyanophenyl)-2-{[2-( 3-fluorophenyl)ethyl]amino}(3-acridine 0.298 M+H 481.2 base))-N-{[6-(decylamino)(3-acridinyl)]indenyl}曱Indoleamine N-{[6-(dimethylamino)(3-indolyl)]indenyl}(6-(2-cyanobenzene 30.234 M+H 495.2 yl)-2-{[2_( 3-fluorophenyl)ethyl]amino}(3_acridinyl))decylamine (2-{[2_(3-fluorophenyl)ethyl]amino}-4-(hydroxyindenyl) -6-phenyl (3-. Bis pyridine 59.114 M+H 457.2 base))-N-(3-acridinylmethyl)carbamamine N-[(5.amino(2·.pyridyl))indenyl](6_(2_ Cyanophenyl)-2_{|&gt;(3-fluorobenzene 0.021 M+H 467.1 yl)ethyl]amino}(3-pyridyl))carboxamide (2-{[2-(3-fluoro) Phenyl)ethyl]amino}-5-(hydroxymethyl)-6-phenyl(3-acridine 0.625 M+H 457.1))-N-(3·pyridylfluorenyl)decylamine ( 2-{[2-(3-fluorophenyl)ethyl]amino}-6-phenyl-5-[N-(3-acridinylmethyl) 55.988 M+H 561.2 Aminyl] 3-pyridyl))-N-(3-pyridylfluorenyl)formamide 0.428 M+H 482.2 (5-(2-diazotrisin 2-azavinyl)-2-{[2-(3 -fluorophenyl)ethyl]amino}-6-benzene 232 200823188 IC50 arithmetic mean ion m/z chemical name group (3-pyridyl))-&gt; 1-(3-°pyridinyl) hydrazine Indoleamine (5-(aminomethyl)-2-{[2·(3-fluorophenyl)ethyl]amino}-6-phenyl (3-acridine 8.904 M+H 456.1 base))- Ν-(3-Acridinesulfanyl)carbenamide (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-methylpyrazole-3-yl) (3)bipyridine 0.04 M+H 431.2 base))-Ν-(3-pyridylmethyl)carbamamine-({6_[3,3-bis(dimethylamino)-2-aza) Prop-2-enyl](2-perpenopyridine )}methyl)(6-(2-cyanophenyl)-2-{[2·(3-fluorophenyl)ethyl]amino}(3-acridinyl)) 0.285 M+H 579.2 A Indole 2-(6-{[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}-34 acridine 1.189 M+Na 603.2 ) carbonylamino]mercapto}-2-pyridyl)acetic acid tert-butyl ester Ν-{[4-(aminomethyl)(3- rididinyl)]methyl}(6-(2-cyano) Benzene 0.401 M+H 481.1 yl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl)) decylamine N-{[3-(aminomethyl) (4-Acridine)] fluorenyl}(6-(2-cyanobenzene 0.056 M+H 481.1 yl)-2_{[2_(3-fluorophenyl)ethyl]amino}(3-吼Pyridyl)) decylamine (5-bromo-2-{[2-(3-fluorophenyl)ethyl]amino} each bisazol-4-yl (3-acridine 0.021 M+H 497.1 ))_N_(3-Acridinesulfanyl)carbenamide (5-&gt;Smelly-2-{[2-(3-)-yl)ethyl]aminoindenyl group 0°°-4-yl (3- 0.023 M+H 509.1 pyridyl))-N-(3-pyridylmethyl)carbamamine (6-(5-cyanooxazol-4-yl)-2-{[2-( 3-fluorophenyl)ethyl]amino}(3-咕°0.105 M+H 442.1 base))-N-(3-acridinylfluorenyl) decylamine (5-cyano-2-{ [2-(3·Fluorophenyl)ethyl]amino}-6-(1-indolylcarbazole-4- 0.021 M+H 456.1 (3-Acridine))-N-(3-acridinylmethyl)decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6------- 3-yl (3" is pyridine))-N-(3- 0.124 M+H 417.1. Pyridylmethyl)carbamamine (6-(3-cyano-1 -methyloxazol-4-yl)-2-{[2-(3-fluorophenyl)ethyl]amine 0.047 M+ H 456.1 yl}(3-acridinyl))-N-(3-acridinylmethyl)decylamine (6-(5-yl-1-yl^^°-4-yl)- 2-{[2-(3-Phenylphenyl)ethyl]month female 0.02 M+H 456.1 base}(3-pyridyl))-N-(3-pyridylmethyl)carbamamine 2-[( 2-{[2-(3-Fluorophenyl)ethyl]amino}-6-oxazol-4-yl(3-acridinyl)carbonylcarbonyl 0.328 M+H 397.0 Amino]-N-曱Ethyl acetamide 2-[(2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-methyloxazol-4-yl) (3-° ratio 0.35 M+ H 411.1 pyridine))carbonylamino]-indole-mercaptoacetamide 233 200823188 IC50 arithmetic mean ion m/z chemical name 0.021 M+H 465.1 (5-chloro-2_{[2-(3-fluorophenyl) Ethyl]amino}-6-(l-methyloxazol-4-yl)(3-pyridyl))-N-(3-pyridylmethyl)formamide 0.604 M+H 536.1 N- {[6-(Aminomethyl)(2-acridinyl)]methyl}(5-indifferent 2-{[2·(3-fluorophenyl)ethyl]amino}-6-phenyl (3-pyridyl)) decylamine 2.725 M+Na 606.1 Ν-[(Η2·[(Tertibutoxy)carbonylamino]ethyl}carbazole-3-yl)methyl](6-Ο Cyanophenyl)_2·{[2-(3·methoxyphenyl)ethyl] Amino} (3_° to pyridine)) formamide 2.2 M+H 584.2 Ν-[(1-{2-[(Tertibutoxy)carbonylaminoethyl}oxazol-5-yl) A (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_acridinyl))carhamamine 0.296 M+H 484.1 Ν- {[1-(2-Aminoethyl)oxazol-3-yl]fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl] Amino}(3"pyridinyl))decylamine 0.032 M+H 484.1 Ν- {[ 1 -(2-Aminoethyl)pyrazol-5-yl]fluorenyl} (6-(2-cyanide) Phenyl)-2-{[2_(3-fluorophenyl)ethyl]amino}(3-acridinyl)) decylamine 0.136 M+H 460.1 N-{[6-(amino fluorenyl) (2"pyridinyl)]methyl}(2-{[2_(3-fluorophenyl)ethyl]aminobiphenyl 6-(1-methylpyrazoledongyl)(3-pyridyl))indole Indoleamine 0.121 M+H 446.1 N-{[6-(aminomethyl)(2′′pyridyl)]methyl}(2-{|&gt;(3-fluorophenyl)ethyl]amino} -6-pyrazol-4-yl(3-pyridyl))carbenamide 0.027 M+H 539.1 N-{[6-(aminomethyl)(2-. (5-bromo-2-{[2-(3-fluorophenyl)ethyl]amino) 6-(1-methylpyrazol-4-yl) (3-oxime) Pyridyl)) decylamine 0.013 M+H 458.1 N-[((2R)-5-oxyindoleridin-2-yl)methyl](6-(2-cyanophenyl)-2·{ [2·(3-fluorophenyl)ethyl]amino}(3-acridinyl))carbenamide 0.133 M+H 458.1 N-[((2S)-5-oxyn-pyrrolidine-2 -yl)methyl](6-(2-cyanophenyl)-2-{[2-(3·fluorophenyl)ethyl]amino}(3′′pyridyl))carbamamine 16.552 M +H 541.1 N-{3-[(5S)-5-(2-diazo-2-azaethyl)-2-oxo ° ratio slightly propyl] propyl} (6-(2-cyanide) Phenyl))-2_{[2-(3-phenylphenyl)ethyl]amino}(3-acridinyl)) decylamine 4.516 M+H 615.2 N-[((2S)-l-{ 3-([Tertidinoxy)carbonylamino]propyl 5-yloxypyrrolidin-2-yl)indenyl](6-(2-cyanophenyl)-2-{[2- (3-fluorophenyl)ethyl]amino}(3-pyridyl))carbenamide 0.917 M+H 501.1 N-{[(2S)-l-(2-aminoethyl)-5-oxygen base. (b-pyridin-2-yl]fluorenyl}(6-(2-cyanophenyl)2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl)) Methionine 234 200823188 IC50 arithmetic mean ion m/z chemical name 0.431 M+H 515.2 N-{[(2S)-l-(3-aminodiyl)·5·oxypyrrolidinyl]fluorenyl} 6-(2-Cyanophenyl)_2· {[2-(3-fluorophenyl)ethyl]amino} (3′′ aryl))carboxylic acid amine 11.658 M+H 515.1 N-{3-[ (5S)_5_(fe-based fluorenyl)_2_oxyn η 洛洛基]propyl)(6·(2_ylphenyl)-2_{[2_(3-fluorophenyl)ethyl]amine }} (3-吼 基)) carbamide 0.11 M+H 501.1 N-{[(2R)-l-(2-aminoethyl hydrazine-oxypyrrolidinyl) fluorenyl} (6_( 2_cyanophenyl)-2_{[2_(3-fluorophenyl)ethyl]amino}(3-exoBridinyl))carbenamide 5.621 M+H 541.2 N-{3-[(5R )-5_(2·diazoazinyl)_2_oxyindole succinate]propyl}(6-(2-cyanophenyl)-2_{[2-(3·fluorophenyl) Ethyl]amino}(3·acridinyl)) decylamine 4.951 M+H 515.1 N**{H(5R)-5-(aminomethyl)_2*»oxypyrene ]propyl}(6_(2.Cyanophenyl)-2-{[i-(3-fluorophenyl)ethyl]amino}(3_acridinyl))carbenamide 17.87 M+H 501.1 N-{2-[(5S)-5·(Aminomethyl)-2 -oxyanthracene π ϋ ] ]] ethyl}(6-(2-cyanophenyl)·2·{[2·(3-fluorophenyl)ethyl]amino}(3· acridinyl) )) guanamine 19.454 M+H 501.1 N-{2-[(5R)-5_(aminomercapto)_2-oxy σ-pyridyl]ethylenyl phenyl)-2-{[2_ (3·Merphenyl)ethyl]amino}(3′′pyridinyl))carbamamine 0.355 M+H 423.1 N-[((2R)-5-oxyπpyrrolidinyl)methyl ](2_{[2-(3-fluorophenyl)ethyl]amino}-6-°boxazol-3-yl(3-pyridyl))decylamine 0.156 M+H 437.1 Team [((211 -5-oxy-l-roxylpyridinyl)indenyl](2_{[2_(3-fluorophenyl)ethyl]amino}-6-(1-methylpyrazolyl) (3-pyridyl) )) decylamine 0.439 M+H 444.0 (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))- N-(pyrrolidin-2-ylmethyl)formamide 0.119 M+H 423.1 N-[((m)-5-oxyπ-pyridyl-2-yl)indenyl](2_{[2_( 3-fluorophenyl)ethyl]aminopyrazole_4_ylpyridinyl))carbamamine 4.834 M+H 587.1 N-[(l-{2_[(dibutyloxy))&gt; Amino]ethyl}oxime. Methyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl)) decylamine 2.082 M+H 601.2 N_[(M3-[(Tertidinoxy)carbonylamino]propyl}pyrrolidin-2-yl)indenyl](6-(2-cyanophenyl)-2-{[ 2-(3-fluorophenyl)ethyl;|amino}(3^pyridyl)carbamamine 0.758 M+H 487.1 Ν-{[1-(2-aminoethyl)pyrrolidine winter base]曱基}(6 cyanophenyl) winter {[2-〇fluorophenyl)ethyl]amino}(3′′pyridyl)) decylamine 3.502 M+H 501.2 Ν-{[1-( 4-aminobutyl) σ-pyrrolidine 1 yl] fluorenyl} (6_(2-cyanobenzene 235 200823188 IC50 arithmetic mean ion m/z chemical name base)_2_ {[2-(3-fluorophenyl) Ethyl]amino}(3-pyridyl))guanamine 2-({(2S)-2-amino-3-[(6-(2-cyanophenyl)-2-{[2 -(3-fluorophenyl)ethyl]0.913 M+H M+H- 505.1 Amino}(3-pyridyl))carbonylaminoljpropyl}amino)acetate oxime 2-({(2S)) 2-Amino-3·[(2·{[2-(3-fluorophenyl)ethyl]amino)-6-(1-methyl 10.852 OMe 452.3 pyrazol-4-yl)(3- Pyridyl))carbonylamino]propyl}aminoacetic acid methyl ester N_[((2S)_6-oxypipedino)indolyl](2·{[2_(3_1phenyl)ethyl]amine 16.026 M+H 438.2 yl}-6-pyrazol-4-yl(3-pyridyl))decylamine N-[((2S)-6-oxypiped-2-yl)indolyl](6-(2- Cyanophenyl)-2-{[2-(3-fluoro0.819 M+H M+H- 473.1 phenyl)ethyl]amino}(3′′pyridinyl))carbenamide N-[(( 2R)-4-{3-[(Tertibutoxy)carbonylamino]propyl}-6-oxypiped-2-yl)indenyl](6-(2-cyanophenyl)- 2-{[2-(3-fluorophenyl)ethyl]amine 9.536 Boc 530.2 base}(3-pyridyl)) decylamine N-[((2S)_6_oxypipecol 1) fluorenyl ](2-{[2-(3-1phenyl)ethyl]amine 13.056 M+H 452.1 base}-6-(1-methylpyrazol-4-yl)(3-pyridyl))曱醯Amine N-[((2S)-6-oxypiperidinyl) fluorenyl](2_p_(3-fluorophenyl)ethyl]amine 6.391 M+H 438.1 yl}-6-pyrazol-3-yl (3-n-pyridyl)) indoleamine N-{[(2R)_4-(3-aminopropyl)-6-oxypiperidinyl-2-yl]indenyl}(6-(2- Cyano group 4.522 M+H 530.2 phenyl)·2-{[2_(3_ phenyl)ethyl]amino}(3-π-pyridyl)) decylamine N-{[(2RH-(2) -aminoethyl)-6-oxypiped-2-yl]fluorenyl}(6-(2-cyano 8.4722 M+H 516.2 phenyl)-2_{[2_(3-fluorophenyl) (amino)(3_pyridyl)) decylamine N-[((2R)_6-oxypipedin-2-yl)indolyl]cyanophenyl) 0.155 M+H 473.1 fluorophenyl)ethyl]amino} (3-° thiol)) decylamine N][(2S)-4_(2-aminoethyl)oxypene曱 }}}(6·(2·cyano0.623 M+H 515.2 phenyl)-2-{[2_(3-fluorophenyl)ethyl]aminopyridinyl))carbenamide N][( 2S&gt;4-(3-Aminopropyl)_6_oxyπ bottom plough_2_yl]methyl}(6_(2_cyano 2.809 M+H 530.2 phenyl)·2-{[2_(3 -Fluorophenyl)ethyl]aminopyridinyl amide group ({(211)-1-[4-(1,3-dioxybenzo[c]oxazoline-2-yl)) Base]_5_oxyl 0 to ° each bit-2-yl}fluorenyl) (6_(2-cyanophenyl sheet {[2_(3-fluorophenyl)ethyl)amine 0.376 M+H 659.2 base} (3-bite base)) A test group ({(211)-1-[5-(1,3-dioxybenzo[c]oxazolyl))pentyl]_5-oxyindole Pyridin-2-yl}methyl)(6-(2-cyanophenyl)_2-{[2-(3-fluorophenyl)ethyl]amine 0.266 M+H 673.2 base}(3_吼吼基)) anthraquinone 236 200823188 IC50 arithmetic mean ion m/z chemical name (2R)_2_{[(6-(2-cyanophenyl)-2_{[2_(3-fluorophenyl)ethyl]amine } (3) ratio 1.933 M+H 544.2 pyridine))carbonylamino]methyl}pyrrolidinecarboxylic acid tert-butyl ester N-{[(2R)-l-(4-aminobutyl)-5-oxygen Pyridoxine -2-yl]methyl}(6-(2-cyanyl 0.0517 M+H 529.2 basic)-2 &lt;~{[2-(3-fluorophenyl)ethyl]amino} (3-τσ ratio σ base)) formamide Ν-{[(2Κ&gt;1·〇aminopentyl)-5_ Oxy-α-pyrrolidyl]fluorenyl}(6_(2-cyanide). 039 M+H 543. 2 basic group) 2 - {[2_(3-fluorophenyl)ethyl]amino} (3-indolyl group)) decanoic acid N-[((m))pyridinyl)] 6-(2_Cyanophenyl)·2·^#•Fluorobenzene 0. 1738 M+H 444. 1 yl)ethyl]amino}(3_pyridyl))carboxamide (2-{[2-(3-fluorophenyl)ethyl]amino}-6-indol-4-yl (3 - ° than bite base)) - 0. 034 M+H 406. 1 N-(pyrazol-3-ylmethyl)decylamine (2-{[2_(3·fluorophenyl)ethyl]aminoindolyl σ-biazole _4_yl) (3_σ-pyridyl 0. 031 M+H 420. 1 base))-indole-dodezol-3-ylmethyl) anthraquinone (2-{[2-(3-fluorophenyl)ethyl]amino}·6-indol-3-yl (3 -吼σ定基))- 0. 092 M+H 406. 1 Ν-(pyrazol-3-ylmercapto)carbamamine N-[((2R)-l-{4-[(t-butoxy)carbonylamino]butanyl}pyridinyl)methyl ](6_(2_Cyanophenyl)_2_{[2-(3.fluorophenyl)ethyl]amino}(3- 0. 432 M+H 629. 2 pyridyl)) decylamine N-{[(2R)-l-(3-aminopropionyl)oxaridin-2-yl]fluorenyl}(6-(2-cyanobenzene 0. 047 M+H 515. 2 base)-2·{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))carbenamide-{[1-(3-aminopropyl)carbazole -3-yl]fluorenyl}(6-(2-cyanophenyl) 0. 065 M+H 498. 2 -2-{[2-(3·fluorophenyl)ethyl]amino}(3-acridinyl))carbenamide-{[1-(3-aminopropyl-butyrazole-3) -yl]fluorenyl}(2-{[2-(3-fluorophenyl)ethyl] 2. 686 M+H 477· 1 Aminopyridylpyrazol-4-yl)(3-pyridyl)) amidoxime-{[1-(3-aminopropyl)oxazol-3-yl]anthracene Base}(2-{[2_(3-fluorophenyl)ethyl] 3. 764 M+H 463. 2 Amino}-6-pyrazol-3-yl(3-pyridyl))carbenamide-{[1-(3-aminopropylbisazol-5-yl]methyl}(2-{ [2_(3_fluorophenyl)ethyl] 0. 228 M+H 477. 2 Aminobi 6-(1-decylpyrazol-4-yl)(3-pyridyl))carbenamide-{[1-(3-aminopropyl)oxazol-5-yl]anthracene Base}(2-{[2_(3-fluorophenyl)ethyl] 0. 462 M+H 463. 2 Amino}-6-pyrazol-3-yl(3-pyridyl))carbenamide N-[((2R)-l-{2-[(t-butoxy)carbonylamino]ethyl }吼吼吼啶-2-yl)methyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-indolepyridinyl 3 . 691 M+H 587. 2 base)) guanamine 237 200823188 IC50 arithmetic mean ion m/z chemical name 1. 341 M+H 601. 2 N-[((2R)-l-{3-[(Tertidinoxy)carbonylamino]propyl}°pyrrolidin-2-yl)indenyl](6-(2-cyanobenzene) Base)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-exidinyl)) decylamine. 705 M+H 487. 2 N-{[(2R)-l-(2-Aminoethyl-2-bromo-2-yl]indolyl}(6-(2-cyanophenyl)-2-{[2-(3 -Fluorophenyl)ethyl]amino}(3"pyridinyl))carboxamide 1. 389 M+H 501. 2 N_ {[(2R)-1 -(3 _Aminopropylbutyrrolidin-2-yl]indolyl} (6-(2-cyanophenyl)-2-{[2_(3_fluorine) Phenyl)ethyl]amino}(3"pyridinyl))decylamine 11. 966 M+H 549. 2 Ν-[(1-{2·[(Tertidinoxy)carbonylamino]ethyl}°pyrazol-3-yl)methyl](2-{[2_(3-fluorophenyl)) Amino]-6-carbazolyl (3_°-pyridyl))carhamamine 1. 488 M+H 449. 1 Ν-{[1-(2-Aminoethylbisoxazol-3-yl)indolyl}(2-{[2_(3-fluorophenyl)ethyl]amino}-6-pyrazole-4 -yl (3-pyridyl) decylamine 5. 506 M+H 449. 2 Ν][1-(2-Aminoethyl)oxazol-3-yl]fluorenyl}(2-{[2-(3-fluorophenyl)ethyl]amino}-6-pyrazole- 3-yl(3-pyridyl))carhamamine 0. 634 M+H 449. 2 Aminoethyl carbazol-5-yl]methyl}(2-{[2_(3-fluorophenyl)ethyl]amino}-6-oxazol-3-yl (3-pyridyl) Methotrexate 862 M+H 463. 2 Ν-{[1-(2-Aminoethyl carbazol-3-yl)methyl}(2-{[2_(3-fluorophenyl)ethyl]amino}-6-(1- Methylpyrazol-4-yl)(3-pyridyl))carhamamine 0. 313 M+H 463. 3 N- {[ 1-(2-Aminoethyl)oxazol-5-yl]indenyl}(2- {[2-(3-fluorophenyl)ethyl]amino}-6-(1 -decylpyrazol-4-yl)(3-pyridyl))carhamamine 0. 318 M+H 530. 3 N-{[(2R)-l-(3-Aminopropyl)-6-oxypiperidinyl]methyl}(6-(2-cyanophenyl)-2-{[2_( 3.·Phenylphenyl)ethyl]amino}(3′′pyridinyl))decylamine 3. 562 M+H 509. 3 N-{[(2R)-l-(3-Aminopropyl)-6-oxypiped-2-yl]methyl}(2][2-(3-fluorophenyl)ethyl] Amino}-6-(1-mercaptopyrazolyl) (3-pyridyl))carboxylic acid amine 2. 343 M+H 495. 3 N-{[(2R)-l-(3-Aminopropyl)oxycarbonyl-4-yl]methyl}(2_{1&gt;(3-fluorophenyl)ethyl]amino} -6-pyrazol-4-yl (3′′pyridinyl))carhamamine 9. 627 M+H 495. 3 N-{[(2R)-l-(3-Aminopropyl)·6-oxypiped-2-yl]methyl}(2][2-(3-fluorophenyl)ethyl]amine }}-6-carbazol-3-yl (3′′pyridinyl))carhamamine 0. 119 M+H 486. 2 N-[((2R)-1-ethylindolyl σ Ρ Ρ σ -2- -2-yl)methyl](6-(2-cyanyl basic) _2-{[2-(3-fluorophenyl) Ethyl]amino} (3_σ-pyridyl)) decylamine 1. 448 M+H 522. 2 N-{[(2R)-l-(indolylsulfonyl carbaryl-2-bromo-2-yl)indolyl}(6-(2-cyanophenyl)·2_{[2-(3-fluoro Phenyl)ethyl]amino}(3′′pyridyl))carbamamine 238 200823188 IC50 arithmetic mean ion m/z chemical name 0. 214 M+H 458. 3 N-[((2R)-1-methyloxaridin-2-yl)indolyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl) Amino](3-acridinyl))carbenamide 2. 049 Μ 472. 2 N-[((2R)-1,1-dimethylmethylpyridin-2-yl)methyl](6-(2-cyanophenyl)-2_{[2_(3·fluorophenyl) Ethyl]amino}(3-acridinyl)) decylamine 11. 341 Μ+Η 695. 3 N-[((2R)-l-{[3-(l,3·dioxybenzo[c]oxalin-2-yl)propyl]sulfonyl)&gt; )methyl](6-(2-cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))decylamine. 071 Μ+Η 551. 3 N-( {(2R)-H(2-Aminoethyl)sulfonyl]oxaridin-2-yl}methyl) (6·(2·cyanophenyl)-2·{[2 -(3.Fluorophenyl)ethyl]amino}(3"pyridinyl))carhamamine 0. 234 Μ+Η 565. 3 N-({(2R)-l-[(3-Aminopropyl)sulfonyl)-p-pyridin-2-yl}indenyl) (6-(2-Hydrylphenyl)-2·{ [2-(3-Phenylphenyl)ethyl]amino}(3-ϋΐ^σ定基))carbamamine 1. 406 Μ+Η 463. 1 Ν-{[1-(3-Aminopropyl)oxazol-3yl]methyl}(2-{[2-(3-fluorophenyl)ethyl]amino}-6-pyrazole 4-yl(3-pyridyl))carhamamine 0. 095 Μ+Η 463. 1 Ν-{[1-(3-Aminopropyl)oxazol-5-yl]methyl}(2-{[2·(3-fluorophenyl)ethyl]amino}-6-pyrazole 4-yl(3-pyridyl))carboxamide 1. 342 Μ+Η 594. 3 N-[((2R)-l-{3-[(Tertidinoxy)carbonylamino]propyl}-5-oxyindole-2-yl)indenyl](2_{[2 -(3-Fluorophenyl)ethyl]amino}-6-(1-methyloxazol-4-yl)(3-pyridyl))carbenamide 2. 127 Μ+Η 578. 4 Ν-{[1-(3-Aminopropyl)-5-oxypyrrolidin-2-yl]fluorenyl}(6- {1-[(didecylamino)(dimercapto) Methyl]pyrazolyl}-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))carboxamide 0. 29 Μ+Η 494. 3 N-{[(2R)-l-(3-Aminopropyl)-5-oxyindole-2-yl]methyl} (2_{[2-(3·fluorophenyl)ethyl) Aminomethylpyrrolidino)(3-acridinyl))carbenamide 4. 64 Μ+Η 523. 3 (2R)-2-{[(2_{[2-(3-Oxophenyl)ethyl]amino)indolyl π than 〇--4_yl)(3-pyridyl))carbonylamino]indolyl } pyrrolidinecarboxylic acid third vinegar 0. 966 Μ+Η 480. 2 N-{[(2R)-l-(3-Aminopropyl)-5-oxyπpyrrole-2-yl]methylindole 2_{[2·(3-fluorophenyl)ethyl] Amino group -6-° ratio ° sitting base (3_° ratio 11 base)) decylamine 0. 518 Μ+Η 615. 3 N-[((2R)-H3_[(Tertidinoxy)carbonylamino]propyl}-5-oxypyrrolidine 239 200823188 IC50 arithmetic mean ion m/z chemical name 0. 666 M+H 432. 2-2-yl)methyl](6-(2-lactyl)-2][2-(3-murbenyl)ethyl]amino}(3_pyridyl))carbenamide-( 2-amino-2-methylpropyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl) ) formic acid amine 746 M+H 409. 2 N-[((2R) fluorenyl)methyl](2-{[2_(3_fluorophenyl)ethyl]amino}·6-π ratio 0 sitting _4_ base (3-σ More than bite base)) guanamine 3. 185 M+H 423. 2 N-[((2R))pyridinyl)methyl](2-{[2_(3·fluorophenyl)ethyl]amino}-6-(1-methylpyrazol-4-yl) (3-pyridyl))carhamamine 1. 473 M+H 510. 3 (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3- π-pyridyl))-N-{2-methyl- 2_[(decylsulfonyl)amino]propyl}decylamine 5. 532 M+H 580. 3 N-[((2R)-l-{2-[(Tertidinoxy)carbonylamino]ethyl)p-pyridin-2-yl)indenyl](2-{[2-(3) -Fluorophenyl)ethyl]amino}-6-(1-indolylcarbazol-4-yl)(3-pyridyl))decylamine 5. 026 M+H 594. 3 N-[((2R)-l-{3-[(Tertidinoxy)carbonylamino]propanyl}pyridin-2-yl)methyl](2-{[2-(3) -fluorophenyl)ethyl]amino}-6-(1-methyloxazol-4-yl)(3-acridinyl))carboxamide 3. 651 M+H 608. 3 N-[((2R)-l-{4-[(Tertidinoxy)carbonylamino]butanyl}pyrrolidin-2-yl)methyl](2-{[2-(3·Fluorine) Phenyl)ethyl]amino}-6-(1-indolylcarbazol-4-yl)(3-acridinyl))carboxamide 0. 581 M+H 480. 3 N-{[(2R)-l-(2-Aminoethyl)indolyl-2-yl]fluorenyl} (2-{[2-(3-fluorophenyl)ethyl]amino) }-6-(1-methyl.bizozol-4-yl)(3-acridinyl))carbenamide 0. 587 M+H 494. 3 N-{[(2R)-l-(3-Aminopropionyl)oxaridin-2-yl]methyl} (2-{[2-(3-fluorophenyl)ethyl]amino) }-6-(1-methylpyrazol-4-yl)(3-acridinyl))carhamamine 0. 351 M+H 508. 3 N-{[(2R)-l-(4-Aminobutyryl)oxaridin-2-yl]fluorenyl} (2-{[2-(3-fluorophenyl)ethyl]aminomethyl) Pyrazol-4-yl)(3-pyridyl))decylamine 0. 515 M+H 418. 2 N-((2S&gt;2_Aminopropyl)(6-(2-cyanophenyl)-2-{[2-(3.fluorophenyl)ethyl]amino}(3-pyridyl) ) guanamine 9. 572 M+H 589. 4-2-[(Tertibutoxy)carbonylamino]ρΝ_{2·[(6·(2-cyanophenyl)_ 2-{[2_(3-fluorophenyl)ethyl]amino}( 3-acridinyl))carbonylamino]-t-butyl}acetamido 0. 194 M+H 617. 4- 4-[(Tertibutoxy)carbonylamino]-Ν-{2_[(6-(2-cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl]amino}( 3-acridinyl)) benzylamino]-third butyl 240 200823188 IC50 arithmetic mean ion m/z chemical name - amide} butylamine N-{(1 S)-2-[(6-(2_ cyanide) Phenyl)-2-{[2·(3-fluorophenyl)ethyl]amino}(3-hydroxypyridyl))aminoamino]-isopropyl H-[(t-butoxy) )carbonylamino]butyl 2. 019 M+H 603. 3 indoleamine N-[((2R)-l]5-[(t-butoxy)carbonylamino]pentanyl}pyrrolidin-2-yl)methyl](6-(2-cyanobenzene) Base)-2-{[2-(3-phenylene)ethyl]amino}(3-吼2. 94 M+H 643. 4 pyridine))carbendazim 2-amino-indole-{2_[(6·(2•cyanophenyl)-2-{[2_(3·fluorophenyl)ethyl;|amino}} 0 . 32 M+H 489. 3 (3-0 to bite)) alkylamino]-tert-butyl}acetamidine 4_amino-indole-{2-[(6-(2-cyanophenyl)-2-{[ 2_(3-phenylphenyl)ethyl]amino} 0. 277 M+H 517. 3 (3-°-pyridyl))carbonylamino]-t-butyl}butanamine N-{[(m)-l-(N-nonylaminomethylindenyl)pyrrolidin-2-yl] Methyl}(6-(2-cyanide 0. 307 M+H 501. 1ylphenyl)-2-{[2-(3_1phenyl)ethyl]amino}(3-acridinyl))carbenamide (2R)-2-{[(6_(2·cyanobenzene) Base)-2-{[2-(3-fluorophenyl)ethyl]amino} (P vs. 0. 101 M+H 502. 2 σ定基)) arylamino]methyl} ° piroxime acid 曱酉 N-{(1 S)-2-[(6-(2-cyanophenyl)-2-{[2 -(3-fluorophenyl)ethyl]amino}(3- 1. 459 M+H 475. 2 pyridyl))carbonylamino]-isopropyl}-2-aminoacetamide N-{(1 S)-2_[(6-(2-cyanophenyl)-2_{[2-(3 -fluorophenyl)ethyl]amino}(3- 3. 56 M+H 503. 2 pyridyl))carbonylamino]-isopropyl}-aminopropylamine N-{[(2R)-l-(5-aminopentenyl)oxaridin-2-yl]fluorenyl} (6-(2-Cyano 0. 099 M+H 543. 3 phenyl)-2-{|&gt;(3-fluorophenyl)ethyl]amino} (P-pyridyl)) decylamine N-{(2S)-2-[(methylsulfonyl) Amino]propyl}(6-(2-cyanophenyl)- 1. 215 M+H 496. 1 2_ {|&gt;(3-Fluorophenyl)ethyl]amino} (3_acridinyl))carbenamide (2R)-2-{[(6-(2-cyanophenyl)- 2_{[2-(3_ phenyl)ethyl]amino} (3-吼0. 027 M+H M+H- 531. 2 pyridine))carbonylamino]methyl}pyrrolidinecarboxylic acid 2-aminoethyl ester N-[(2S)_2_(decylamino)propyl](6-(2-cyanophenyl) -2-{[2-(3-fluorobenzene 0. 944 Me 432. 2 yl)ethyl]amino} (3-acridinyl))carinamide N-((2R)-2-aminopropyl)(6-(2-cyanophenyl)-2- {[ 2-(3-fluorophenyl)ethyl] 0. 399 M+H 418. 2 Amino}(3-pyridyl))carbamamine&gt;H(2R)_2-(methylamino)propyl](6-(2-cyanophenyl)-2-{[2- (3-fluorobenzene 1. 89 M+H 432. 2 yl)ethyl]amino}(3-acridinyl))carboxamide 5. 84 M+H 510. 2 N-{(2S)-2-[indolyl(methylsulfonyl)amino]propyl}(6-(2-cyanophenyl)- 241 200823188 IC50 arithmetic mean 1. 333 7. 071 2. 312 5. 916 0. 049 3. 677 3. 246 6. 826 0. 041 0. 204 0. 71 0. 152 0. 012 0. 025 ion m/z M+H 496. 2 M+H 510. 2 M+H 575. 3 M+H 589. 3 M+H 603. 3 M+H 617. 4 M+H 489. 2 M+H 517. 3 M+H 475. 2 M+H 503. 2 M+H 517. 2 M+H 489. 2 M+H 449. 1 M+H 501. 2 Chemical name 2-{[2-(3-fluorophenyl)ethyl]amino}(3-n-pyridyl))carinamide N-{(2R)-2-[(indolylsulfonyl) Amino]propyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))carboxamide N-{ (2R)-2-[indolyl(methylsulfonyl)amino]propyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine }}(3-.pyridyl))guanamine N-{(lR)-2-[(6-(2-cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl) Amino}(3-°-pyridyl))carbonylamino]-isopropyl}-2-[(tatabutoxy)carbonylamino]acetamide N-{(1R)_2_[(6 -(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))carbonylamino]-isopropyl}-2-[( Third butoxy)carbonylamino]]-N-mercaptoacetamide N-{(1 R)-2-[(6-(2-cyanophenyl)-2-{[2-(3- Fluorophenyl)ethyl]amino}(3-acridinyl)carbonylamino]-isopropyl}-4-[(tatabutoxy)carbonylamino]butanamine Ν·{(1 R)-2-[(6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))carbonylamino]- Isopropyl}-4-[(Tertidinoxy)carbonylamino]-N-methylbutyramine N-{(lS)_2_[(6-(2-cyanophenyl)-2-{ [2-(3-phenylene) B Amino}(3-α to π-based))&gt;Carboaminol]-isopropyl}-2-amino-N-methylethanoamine N-{(1S)-2-[(6_ (2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))carbonylamino]]-isopropyl}-4-amino]N -methylbutanamine N-{(1R)-2_[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_pyridyl)) Carbonylamino]-isopropyl}-2-aminoacetamide N-{(1R)-2-[(6-(2.cyanophenyl)1{[2-(3-fluorophenyl)) Amino](3-pyridyl))carbonylamino]-isopropyl}-4-aminobutanamine N-{(1 R)-2-[(6-(2-cyanophenyl) -2-{[2-(3-fluorophenyl)ethyl]amino} (3-° ratio σ-based)) arylamino]-isopropyl}-4-amino-N-fluorenyl Butylated amine N-{(1 R)-2-[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}}(3-吼° Basement)) Prison Amino]-isopropyl}-2-amino-N-methylacetic acid amine fluorofluoro-2-{[2_〇fluorophenyl)ethyl]amino}-6_(1- Methyloxazol-4-yl)(3-pyridyl))-indole-(3-indolylpyranyl) decylamine N-{[(2R)-l-(2-aminoethenyl) ) 吼 bite-2-yl] fluorenyl} (6_ (2-cyanobenzene 242 200823188 IC50 arithmetic mean ion m / z chemical name 0. 029 M+H 528. 2 base)····{[2_(3_fluorophenyl)ethyl]amino}(3_abridinyl)) decylamine N-{[(2R)-l-(4-aminobutylidene)pyrrole Pyridin-2-yl]methyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-° thiol))曱Guanamine 0. 042 M+H 515. 2 N-{[(2R)-l-(3-Aminopropyl)-5-oxyl. Bilobidine-2-yl]methyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl)) Guanamine 0. 044 M+H 417. 1 (2-{[2-(3-Fluorophenyl)ethyl]amino}-6-oxazol-4-yl(3′′pyridinyl))-N-(3-pyridylfluorenyl)fluorene Indoleamine 265 M+H 424. 2 {6-(3-Methylphenyl)-2-[(2-(2.acridinyl)ethyl)amino](3-acridinyl)}-N-(3-n-pyridyl) Methyl)carbamamine 0. 915 M+H 428. 2 {6-(3-Fluorophenyl)_2-[(2-(2- η-pyridyl)ethyl)amino](3·acridinyl)}-Ν-(3-pyridylmethyl) Guanamine 992 M+H 435. 2 {6-(3-Cyanophenyl)-2-[(2-(2-η-pyridyl)ethyl)amino](3-acridinyl)}·Ν-(3-pyridylhydrazine Base amine 933 M+H 440. 2 {6-(3-Methoxyphenyl)-2-[(2-(2-acridinyl)ethyl)amino](3-acridinyl)}-N-(3-pyridyl) Base guanamine 0. 79 M+H 426. 1 {6-(3-Phenylphenyl)-2-[(2-(2-indenyl)ethyl)amino](3-indole σ-based)}-Ν-(3-pyridyl) Methyl) guanamine 967 M+H 444. 1 {6-(3-Phenylphenyl)-2-[(2-(2-^ σ 定定)ethyl)amino](3·. than dimethyl)}-Ν-(3-acridinyl) Sulfhydryl 927 M+H 478. 1 {2·[(2·(2-.pyridyl)ethyl)amino][3_(trifluoromethyl)phenyl](3-.pyridyl)}-Ν-(3) ratio Pyridylmethyl)carbamamine 12. 404 M+H 453. 2 {6-[3-(Dimethylamino)phenyl]-2-[(2-(2^pyridyl)ethyl)amino](3_,pyridyl)}-Ν·(3 -pyridylmethyl)carbamamine 1. 321 M+H 428. 1 {6-(2-Fluorophenyl)-2-[(2-(2-indolyl)ethyl)amino](3-.pyridyl)}-N-(3-acridinyl) Base amine 438 M+H 444. 1 {6-(2-Phenylphenyl)-2-[(2-(2-indolyl)ethyl)amino](3-acridinyl)}-N-(3-acridinylmethyl)曱醯amine 11. 031 M+H 424. 2 {6-(2-Mercaptophenyl)-2-[(2-(2-)-yl)ethyl)amino](3- η-pyridyl)}-Ν-(3·σΛ° ^基基基)carbamamine 17. 936 M+H 440. 2 {ό-(2-decyloxyphenyl)-2-[(2 °β 定定)ethyl)amino](3"pyridyl)}-Ν-(3-acridinylmethyl)曱醯amine 243 200823188 IC50 arithmetic mean ion m/z chemical name {6-(2-cyanophenyl)-2-[(2-(2- hexyl)ethyl)amino](3- Acridine 0. 46 M+H 435. 2 base)}-N-(3-acridinylmethyl)decylamine {2-[(2-(2-)-butyl)ethyl)amino]-6-(2-σ-sepeno ) (3- ° ratio σ is set to 0. 797 M+H 416. 1 base)}-Ν-(3-pyridylfluorenyl) decylamine {2-[(2-(2-)pyridyl)ethyl)amino]-6-(3-thienyl)(3) - acridine 0. 414 M+H 416. 1 base)}-N-(3-acridinylfluorenyl)formamide {6-(4-hydroxyphenyl)-2-[(2-(2-pyridyl)ethyl)amino](3) -pyridine 0. 586 M+H 426. 1 base)}-N-(3-pyridylfluorenyl)formamide {6-(2-hydroxyphenyl)-2-[(2-(2-acridinyl)ethyl)amino](3) - Acridine 2. 17 M+H 426. 1 base)}-N-(3-pyridylmethyl)decylamine {6-(4-ethylphenyl)-2-[(2-(2- ° σ 定)ethyl)amino] (3-° ratio setting 2. 792 M+H 438. 2 ))}-Ν-(3-acridinyl fluorenyl) amidoxime-(4-{6-[(2-(2-acridinyl)ethyl)amino]]5-[Ν- (3-Acridinesulfonyl)amine 1. 221 M+H 467. 2-Mercapto]-2-acridinyl}phenyl)acetamido{6-(4-methyl(2-thienyl))-2-[(2-(2-pyridyl)ethyl)amine Base] (3-pyridine 0. 344 M+H 430. 1 base)}-N-(3-pyridylfluorenyl) decylamine {6-(4-methyl(3-thienyl))-2_[(2-(2)pyridyl)ethyl)amine Base] (3) than pyridine 4. 063 M+H 430. 1 base)}-N-(3^pyridylmethyl)decylamine {6-(2,3-dimethylphenyl)-2-[(2-(2-acridinyl)ethyl) Amino] (3-. than pyridine 6. 945 M+H 438. 2))-N-(3-pyridylfluorenyl)guanamine {6-(2,5-dimethylphenyl)-2-[(2-(2-n-pyridyl)ethyl) Amino](3-u-pyridyl 13. 588 M+H 438. 2))-N-(3-pyridylfluorenyl)guanamine {6-(2,4-dimethylphenyl)-2-[(2-(2^pyridyl)ethyl)amine Base] (3-acridine 3. 964 M+H 438. 2))-N-(3-pyridylfluorenyl)guanamine {6-(3,5-dimethylphenyl)-2-[(2-(2-)pyridyl)ethyl) Amino](3-u-pyridinyl 10. 138 M+H 438. 2 base)}-N-(3-pyridylfluorenyl) decylamine {6-(3,4-dimethylphenyl)-2-[(2-(2 j-pyridyl)ethyl)amine Base] (3-acridine 3. 38 M+H 438. 2))-N-(3-pyridylfluorenyl)formamide (2-{[2-(4-fluorophenyl)ethyl]amino}-6-phenyl(3-lysyl) )-N- (3-u-bipyridine 1. 609 M+H 427. 2-mercapto)carbamamine (2-{[2-(4-chlorophenyl)ethyl]amino}-6-phenyl(3-acridinyl))-N- (3′′pyridyl 6 . 677 M+H 443. 1 mercapto) guanamine 244 200823188 IC50 arithmetic mean ion m/z chemical name (2-{[2-(3-phenylphenyl)ethyl]amino}-6-phenyl (3-acridinyl) )) Park (3) than bite 0. 349 M+H 443. 1 benzyl)carbamamine (2-{|&gt;(3-methoxyphenyl)ethyl]aminobiphenyl 6-phenyl(3-pyridyl)) K3- 0. 269 M+H 439. 1 pyridylmethyl)decylamine (2-{[2-(3-phenylphenyl)ethyl]amino}·6-phenyl(3-η-pyridyl)) bucket (3′′ 唆0 . 063 M+H 427. 1 benzyl) decylamine (2-{[2-(2- phenylphenyl)ethyl]amino}-6-phenyl (3 比 pyridine))-Ν- (34 bite 0. 16 M+H 443. 1 benzyl) decylamine (2-{[2-(2-methoxyphenyl)ethyl]amino}-6-phenyl (3 比pyridyl))·Ν-(3** 0. 98 M+H 439. 1 吼. Stationary methyl) formamide (2-{[2-(2-methylphenyl)ethyl]amino}-6-phenyl(3-pyridyl))-indole-(3-pyridinium 0. 326 M+H 423. 1 pyridinemethyl)carbamamine (2-{[2_(2-fluorophenyl)ethyl]amino}-6-phenyl(3-acridinyl))-oxime-(3) than bite 0 . 107 M+H 427. 1-ylmethyl)decylamine (2-{[2-(2,6-difluorophenyl)ethyl]amino}-6-phenyl(3-acridinyl))-indole-(3- 0. 288 M+H 445. 1 pyridylmethyl)carbamamine (2-{Ρ-(3,5-difluorophenyl)ethyl]amino}-6-phenyl(3-hydroxypyridyl))-Ν-(3 - 0. 055 M+H 445. 1 pyridylmethyl)carbamamine (2-{[2-(3,4-difluorophenyl)ethyl]amino}-6-phenyl(3-acridinyl))-indole-(3 - 0. 521 M+H 445. 2 . Pyridylmethyl)carbamamine (2-{[2-(2,5-difluorophenyl)ethyl]amino}-6-phenyl(3-acridinyl))-indole-(3 - 0. 079 M+H 445. 2 pyridylmethyl)guanamine [6-phenyl-2-({2-[3-(trifluoromethyl)phenyl)ethyl)amino) (3-acridine 8. 254 M+H 477. 2 base)]-Ν-(3· acridinehydrazinyl)carbamamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(4-methyl(2- Thienyl)) (3) is more than pyridine. 148 M+H 447. 2 base))-Ν-(3-«pyridinyl) decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(3-thienyl)( 3-pyridine 0. 048 M+H 433. 1 base))-N-(3-acridinylmethyl)carbamamine (2-{[2-(2-cyanophenyl)ethyl]amino}-6-phenyl (3-. ratio Pyridyl))-N-(3-port ratio 0. 26 M+H 443. 1 pyridyl hydrazino)carboxamide (2- {[2-(3-cyanophenyl)ethyl]amino} -6-phenyl (3-° ratio β base))-Ν-(3· σ ratio 4. 649 M+H 434. 1 pyridinyl)carbamamine 245 200823188 IC50 arithmetic mean ion m/z chemical name 36. 722 M+H 425. 1 (2-{[2-(4-Hydroxyphenyl)ethyl]amino}-6--phenyl (3′′pyridinyl))·Ν·(3·σ-pyridylmethyl) formamidine Amine 431 M+H 425. 1 (2-{[2-(2.hydroxyphenyl)ethyl]amino}}phenyl (3 比 pyridine)) Ν (-(3-σ-pyridyl fluorenyl) decylamine 27. 106 M+H 424. 1 (2-{[2-(4-Aminophenyl)ethyl]aminoindole-phenyl(3′′pyridinyl))·Ν·(3′′ 啶pyridinyl) decylamine 11. 492 M+H 452. 1 3-[2-({6-phenyl-3-[indole-(3-acridinylmethyl)aminemethanyl 1 milylpyridyl}amino)ethyl]benzamide 0.5. 04 M+H 451. 1 (2-{[2-(3,5-Difluorophenyl)ethyl]amino}-6-(3-thienyl)(3-°pyridinyl))-N-(3-acridine) Methyl)carbamamine 0. 119 M+H 465. 1 (2-{[2-(3,5-difluorophenyl)ethyl]amino}(4-methyl(2-thienyl))(3-°pyridyl))-N-( 3-°-pyridyl fluorenyl) guanamine 0. 041 M+H 470. 1 (2-{[2-(3,5-diphenyl)ethyl]amino}-6-(2-cyanophenyl)(3_°pyridyl))-N-(3-叱Pyridylcarbyl)carbamamine 0. 137 M+H 433. 1 (2-{[2·(3-fluorophenyl)ethyl]amino}-6-(2-thienyl)(3-acridinyl))-N-(3-pyridylmethyl)- Guanamine 0. 097 M+H 451. 1 (2-{[2-(3,5-Difluorophenyl)ethyl]amino}-6-(2-thienyl)(3-acridinyl))-N-(3-acridinyl) Methyl)carbamamine 28. 097 M+H 467. 2 3-[2-({6-Phenyl-3-[N-(3-acridinylmethyl))indolyl]-2-acridinyl}amino)ethyl]benzoic acid methyl ester 16 . 384 M+H 470. 2 2-(6-{[2-(3-Fluorophenyl)ethyl]amino}-5-[N-(3-oxaridinylmethyl)amine fluorenyl]-2-pyridyl)benzene Formamide 0. 198 M+H 445. 2(6-(4-Fluorophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))-N-(3-acridinylmethyl) ) methotrexate 21. 862 M+H 453. 2 3-[2-({6-phenyl-3-[N-(3-pyridylmethyl)amine fluorenyl]-2-pyridyl}amino)ethyl]benzoic acid 1. 383 M+H 479. 1 (6-(2-Chloro-4-fluorophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-. π-based))-Ν-(3- Acridine methyl) guanamine 0. 138 M+H 463. 1 (2-{[2-(3,5-Difluorophenyl)ethyl]aminobi 6-(4-fluorophenyl)(3_.pyridyl))-indole-(3-acridinyl) Methyl) guanamine 0. 038 M+H 470. 1 (6_(2_Cyano-acylphenyl)-2_{[2_(3-fluorophenyl)ethyl]amino}(3-η-pyridyl))-indole-(3-acridinyl) Base guanamine 246 200823188 IC50 arithmetic mean ion m/z chemical name (6-(2-chloro-6-fluorophenyl)-2-{[2-(3-fluorophenyl)ethyl; i-amino }(3·pyridine 0. 54 M+H 479. 1 base))-Ν-(3-acridinylmethyl)decylamine (6-(2-chloro-5-methoxyphenyl)-2-{[2-(3-fluorophenyl)) Amino group} (3_pyridine 2. 005 M+H 491. 1 base))-N-(3-acridinylmethyl)decylamine (6-(2·cyanomethoxyphenyl)-2-{[2_(3_phenyl)ethyl]amino }(3-° ratio 0. 041 M+H M+ chlorine 482. 1 pyridine pyridylmethyl) decylamine (6-(2-cyano-6-fluorophenyl)·2·{[2_(3-merylphenyl)ethyl]amino group than bite 0. 086 Η 470. 1 base))-N-(3-acridinylmethyl)decylamine (6-(2- 1phenyl)-2-{[2-(3-phenylphenyl)ethyl]amino} ( 3- η than bite 0. 139 M+H 445. 1 base))-Ν-(3· acridinemethyl)carbamamine (2-{[2-(2, 3-difluorophenyl)ethyl]amino}-6-(2-cyano) Phenyl) (3-pyridine 0. 022 M+H 470. 1 base))-N-(3-acridinylmethyl)decylamine (6-(2-chloro-5-fluorophenyl)-2-{[2-(3-fluorophenyl)ethyl] Amino group} 327 M+H 479. 1 base))-Ν-(3-acridinylmethyl)formamidine (6-(2-cyanofluorophenyl)-2_{[2-(3_phenylene)ethyl]amino}( 3-acridine 0. 053 M+H 470. 1 base))-Ν-(3-acridinylfluorenyl)formamide (6-(3-fluorophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}( 3_ σ is pyridine 0. 157 M+H 445. 1 》-Ν-(3-Acridinemethyl)carbamamine (6-[2-(cyanoindolyl)phenyl]-2-{[2-(3-fluorophenyl)ethyl]amine Base} (3-acridine 16. 392 M+H 466. 2 base))_Ν-(3·η-pyridylmethyl)carbamamine (2-{[2_(3-fluorophenyl)ethyl]amino}_6_[3_(ylamino)(2-嗟 基 ))]] (3- 2. 245 M+H 463. 1 σ pyridine group))-Ν-(3-pyridylfluorenyl) decylamine (2-{[2_(3-fluorophenyl)ethyl]amino}-6-(5-fluorenyl) 3_Thienyl)) (3) is 0. 098 M+H 461. 1 pyridyl))-indole-(3-pyridylfluorenyl)carzamide (2-{[2-(3-fluorophenyl)ethyl]amino} each [5-(yl fluorenyl) ( 3-thienyl)](3- 0. 073 M+H 463. 1 σ pyridine group))-Ν-(3-σ-pyridyl fluorenyl) decylamine (6-(2-chloro-4-methylphenyl)-2-{[2-(3-fluorobenzene) Ethyl]amino]} (3_ϋ ratio σ2. 078 M+H 475. 1 base))-Ν-(3-acridinylmethyl)decylamine (6-(2-cyano-t-methylphenyl) winter {[2-(3-fluorophenyl)ethyl]amine }(34匕啶0. 996 M+H 466. 2 base))-Ν-(3′′-pyridylfluorenyl) decylamine (2-{[2-(3-fluorophenyl)ethyl]amino} each [Η 曱 曱 phenyl) phenyl] (3) than 唆0. 281 M+H 457. 1 base))-Ν-(3-acridinylmethyl)formamide 247 200823188 IC50 arithmetic mean ion m/z 5. 719 Μ+Η 471. 2 78. 064 Μ+Η 419. 1 1.  185 Μ+Η 491. 1 12. 904 Μ+Η 475. 2 5. 022 Μ+Η 475. twenty four. 812 Μ+Η 434. 1 1. 209 Μ+Η 581. 2 0. 008 Μ+Η 456. 1 0. 043 Μ+Η 446. 1 0. 032 Μ+Η 460. 1 2. 148 Μ+Η 458. 2 0. 336 Μ+Η 458. 2 0. 572 Μ+Η 515. twenty three. 874 Μ+Η 529. 2 0. 755 Μ+Η 515. twenty one. 261 Μ+Η 529. 2 Chemical name (2-{[2·(3-fluorophenyl)ethyl]amino}-6-[3-(methoxyindolyl)phenyl](3′′pyridyl acridinylmethyl Methionine (6-(1Η-1,2,3,4-tetrazolyl) winter {[2-(3-phenylphenyl)ethyl]amino}(3′′pyridinyl; pyridyl Methylamine (6·[2-chloro-4-(tetra)ylmethyl)phenyl]_2-{[2_(3-phenylphenyl)ethyl]amino}(3-indolyl))-Ν- (3-σ-pyridylmethyl)decylamine (2R)-2-amino-4-[(6-(2-cyanophenyl)&gt;2·{[2-(3-fluorophenyl)) Ethyl]amino}(3-pyridyl))carbonylamino]-indole-mercaptobutylamine (2S)-2-amino-4-[(6-(2-cyanophenyl)-2 -{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))carbonylamino]-indole·methylbutylideamine-(3-amino-2-hydroxypropane (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))carbenamide N-[(2-{ [(Tertidinoxy)carbonylamino]mercapto}(3-tonidyl))indenyl](6-(2-cyanophenyl)-2_{[2_(3-fluorophenyl)B Amino](3-acridinyl))carboxamide N-{[2-(aminomethyl)(3-acridinyl)]methyl}(2-{[2-(3-fluoro) Phenyl)ethyl]amino}-6-phenyl(3-acridinyl))carbenamide N-{[2-(aminomethyl)(3-acridinyl)]methyl}(2 -{[2- (3-fluorophenyl)ethyl]amino}_6-pyrazol-3-yl(3-pyridyl X)carbenamide N-{[2-(aminomethyl)(3-acridinyl) ]] thiol}(2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-indolyl ratio. Sodium-3-yl) (3-port ratio. Base)) N-[((3R)(3-Pyridinyl))indenyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine (3-pyridyl)) decylamine (6-(2-cyanophenyl)·2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl) )-Ν-(4-piperidinyl indenyl) amidoxime-{[1-(2-aminoethyl)(4-piperidinyl)]methyl}(6-(2-cyano) Phenyl)-2_{[2-(3-phenylphenyl)ethyl]amino}(3-acridinyl))indoline-{[1-(3-aminopropyl)-(4) -piperidinyl)]methyl}(6-(2-cyanophenyl)-2_{[2-(3-phenylphenyl)ethyl]amino}(3-acridinyl))carboxamide N-{[(3S)-l-(2-aminoethenyl)(3-piperidinyl)]fluorenyl}(6-(2-cyanophenyl)-2_{[2-(3_ Fluorophenyl)ethyl]amino}(3′′pyridinyl)methaneamine N-{[(3S)-l-(3-aminopropionyl)(3-slightly sigma)]methyl }(6-(2-cyanobenzene 248 200823188 IC50 arithmetic mean ion m/z chemical name base)-2-{[2_(3·fluorophenyl)ethyl]amino}(3′′pyridinyl)) Formamide · N- [(l-Ethyl (4-piperidinyl)) fluorenyl] (6-(2-cyanophenyl) winter {[2-(3•Fluoric 1. 696 M+H 500. 3 phenyl)ethyl]amino}(3-pyridyl))carboxamide N-[((3S)-1-ethenyl (3-But.))methyl](6-(2- Cyanobenzene 729 M+H 500. 3 ))·2·{[2·(3-fluorophenyl)ethyl]amino)(3·fluorenyl))carbenamide-{[1-(4-aminobutylidene) (4- Piperidinyl)]methyl}(6-(2-cyanobenzene) 009 M+H 543. 3 base)_2_{|&gt;(3-fluorophenyl)ethyl]amino}(3·ridinyl))carbamidine 4-{[(6-(2-cyanophenyl)-2- {[2-(3-Fluorophenyl)ethyl]aminopyridinyl) 2. 13 M+H 516. 3 carbonylamino]hydrazino}piperidinecarboxylic acid oxime ester N-[((2R)(2·piperidinyl))indenyl](6-(2-cyanophenyl)-2-{[2_( 3_fluorophenyl) 1. 159 M+H 458. 3 ethyl]amino}(3-pyridyl))carbenamide N-{[(2R)-l-(2-aminoethenyl)(2-piperidinyl)]methyl}(6- (2-cyanobenzene 0. 092 M+H 515. 3-yl)·2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))carbenamide-{[(2R)-1-(3-aminopropyl) Mercapto)(2-piperidinyl)]methyl}(6-(2-cyanobenzene). 155 M+H 529. 2 base)-2_ {[2_(3-fluorophenyl)ethyl]amino} (3 - η ratio), carboamine N-{[(2R)-l-(4-aminobutylidene) (2-piperidinyl)]methyl}(6-(2-cyanobenzene). 083 M+H 543. 2 base)-2_{[2·(3-fluorophenyl)ethyl]amino}(3′′ 咬 )))) carboxylic acid amine N-[((2R)-1-ethenyl (2·piperidine) Base)) methyl](6-(2-cyanobenzene) 676 M+H 500. 2 base)-2_{[2_(3-fluorophenyl)ethyl]amino}(3′′pyridinyl))carbenamide (2R)-2-{[(6-(2-cyanophenyl) -2·{[2-(3-Fluorophenyl)ethyl]amino} (3_σ ratio 4. 282 M+H 516. 3 pyridine))carbonylamino]methyl}piperidinecarboxylic acid oxime ester N-({(2R)-l-[(3-aminopropyl)-retinyl)] (2-π σ σ determinate) }曱基)(6_(2_cyanoquinone 0. 37 M+H 579. 2ylphenyl)-2-{[2_(3-fluorophenyl)ethyl]aminopyridinyl))carinamide N-[((2R)-1-methyl(2_piperidinyl)) Methyl](6·(2-cyanophenyl)-2-{[2_(3_ 0. 488 M+H 472. 2 fluorophenyl)ethyl]amino} (3-° ratio. base)) formamide N-{[(2R)-l-((2R)_2,3caminopropionyl) (2. Pyridyl)]methyl}(6-(2- 0. 161 M+H 544. 3 cyanophenyl)-2-{[2_(3-fluorophenyl)ethylmicro}}(3_pyridyl))guanamine N-{[(2R)-1-((2R)_2, 4^Aminobutyryl)(2-piperidinyl)]fluorenyl}(6-(2_ 0. 399 M+H 558. 3 cyanophenyl)·2_{[2_(3-phenylphenyl)ethyl]amino}(3-acridinyl)) decylamine N-{[(2R)-1-((2R)_2 ,5-diaminopentenyl)(2-piperidinyl)]fluorenyl}(6-(2_ 0. 456 M+H 572. 2 cyanophenyl)-2-{[2_(3·fluorophenyl)ethyl]amino}(3_acridinyl)) decylamine 0. 178 M+H 565. 2 N-({(2R)-l-[(2-Aminoethyl)sulfonyl](2-piperidinyl)}methyl)(6-(2-cyanide 249 200823188 IC50 arithmetic mean ion m/ z Chemical name 0. 048 M+H 572. 3-ylphenyl)-2-{[2-(3-phenylphenyl)ethyl]amino} (3-° thiol)) decylamine N-{[(m) small((2S)- 2,5-diaminopentenyl)(2-piperidinyl)]fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl] Amino}(3-acridinyl))carhamamine 0. 052 M+H 529. 3 N-{[(2R)-l-((2S)-2-aminopropenyl)(2-piperidinyl)]fluorenyl}(6-(2-cyanophenyl)-2-{ [2-(3-Fluorophenyl)ethyl]amino}(3′′pyridinyl))carboxamide 0. 261 M+H 529. 2 N-{[(2R)-l-((2R)-2-aminopropenyl)(2-piperidinyl)]fluorenyl}(6-(2-cyanophenyl)-2-{ [2-(3-Fluorophenyl)ethyl]amino}(3-acridinyl)) decylamine 2. 691 M+H 564. 1 (2R)-2-{[(6-(2-Cyanophenyl)·2-{[2-(3-fluorophenyl)ethyl]amino}(3-hydroxypyridyl)carbonyl Amino]methyl}piperidinecarboxylic acid 2-chloroethyl ester 0. 091 M+H 545. 2(2R)-2-{[(6-(2-Cyanophenyl)-2-pin-fluorophenyl)ethyl]amino}(3-pyridyl))carbonylamino]methyl}piperidin 2-aminoethyl pyridine carboxylic acid 0. 023 M+H 547. 2 N-{[(2R)-l-(4-Aminobutyrydylpyrrolidin-2-yl]indolyl}(2-{[2-(3,5-difluorophenyl)ethyl]amine }}-6-(2-cyanophenyl)(3-acridinyl))carhamamine 0. 133 M+H 515. 3 N-{[(2R)-l-(4-Aminobutyryl)oxaridin-2-yl]fluorenyl}{6-(2-cyanophenyl)-2-[(2-cyclohexyl-) 1-diethylethyl)amino](3-acridinyl)}guanamine 3. 56 M+H 506. 2 3-{[3-(N-{[(2R)-l-(4-Aminobutylidene))pyridin-2-yl]methyl}amine-methylmethyl)-6-(2-cyanobenzene) () 2-(2-acridinyl)]amino}-N,N-dimethylpropanamide 0. 062 M+H 511. 2 N-{[(2R)-l-(4-Aminobutenyl). Bilpyridin-2-yl]methyl}{6-(2-cyanophenyl)-2-[(2-phenylethyl)amino](3′′pyridyl)}decylamine 8. 167 M+H 519. 2 N-{[(2R)-l-(4-Aminobutyryl)oxaridin-2-yl]fluorenyl}{6-(2-cyanophenyl)-2-[(2-(2H-) 3,4,5,6-tetrahydropiperidinyl)ethyl)amino](3-acridinyl)} guanamine 2. 038 M+H 519. 2 N-{[(2R)-l-(4-Aminobutyrydinylpyrrolidin-2-yl]indenyl}{6-(2-cyanophenyl)-2·[(2-(2 H) -3,4,5,6-tetrahydropiperidin-2-yl)ethyl)amino](3-acridinyl)}decylamine. 059 M+H 530. 2 N-{[(2R)-l-((2S)-2,3-Diaminopropionyl)oxaridin-2-yl]methyl}(6-(2-cyanophenyl)_2 -{[2-(3-Phenylphenyl)ethyl]amino}(3′′pyridinyl)) decylamine. 193 M+H 545. 2 N_{[(2R)-l-((2S)-2-Amino-3-methoxypropenyl)-indolyl-2-yl]methyl}(6-(2-cyanophenyl) )·2-{[2-(3-phenylene)ethyl]aminopyridinyl))carhamamine 0. 173 M+H 531. 2 N-{[(2R) small ((2S)-2-amino-3-hydroxypropionyl)-indolyl-2-yl]-250 200823188 IC50 arithmetic mean ion m/z chemical name base} (6_ (2_Cyanophenyl)-2-{[2_(3-fluorophenyl)ethyl]amino}(3" than butyl))carbamamine. 014 Μ+Η 464. 1 Ν-{[2·(Aminomethyl)(3′′pyridinyl)]methyl}(5-fluoro-2-{[2-(3-phenylphenyl)ethyl]amino}-6 -σ ratio -3--3-yl (3_σ ratio σ base)) formamidine 0. 108 Μ+Η 484. 1 N-{[(2R)-l-(2-Aminoethyl)p-pyrrolidin-2-yl]methyl}(5-fluoro_2-{[2-(3-fluorophenyl)) Ethyl]amino group is more than salicyl (3_σ than bite)) formamide 0. 269 Μ+Η 514. 1 N-{[(2R)-l-((2S)-2_Amino-3-hydroxypropionyl)pyrrolidin-2-yl]methyl}(5-敦-2- {[2-( 3-fluorophenyl)ethyl]aminopurine 6-indole-3-yl(3.pyridyl))decylamine. 314 Μ+Η Μ+Η 498. 2 N-{[(2R)-l-((2S)-2-aminopropenyl)pyrrolidinyl]yl]}(5-fluoro-2-{[2-(3-fluorophenyl)) Ethyl]amino}-6-oxazol-3-yl(3-pyridyl))decylamine. 169 Μ+Η 512. 1 N-{[(2R)-l-(4-Aminobutylidene)rrolo-2-yl]methyl}(5-fluoro-2-{[2-(3-fluorophenyl)ethyl] Amino}-6-° than sial-3-yl (3-° ratio. base)) formic acid amine. 92 Μ+Η 428. 1 {6_(2_Cyanophenyl)-2_[(2-oxapentan-2-ylethyl)amino](3-吼σ定基)}-Ν-(3-acridinylmethyl) ) guanamine 0. 398 Μ+Η 415. 1 N-((2R)-2-aminopropyl)(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-mercaptocarbazole- 4-yl)(3-σ-pyridyl))indolide 1. 754 Μ+Η 572. 2 N-{(1 R)_2-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino} each (1. fluorenyl 0-pyridyl) (3- Pyridyl))carbonylamino]-isopropyl} winter [(t-butoxycarbonylamino)acetamide 0. 076 Μ+Η 472. 3 N-{(lR)-2-[(5-Gas-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1·methylηpyrazole) ( 3-pyridyl))alkylamino]-isopropyl}-2-aminoacetamide 0. 027 Μ+Η 455. 1 N-[((2R)-5.oxyl ratio slightly biting 2_yl) methyl](5·fluoro_2_{[2_(3_fluorophenyl)ethyl]aminopurine-(1 -methylpyrazole_4_yl)(3-pyridyl))guanamine 1. 804 Μ+Η 272. 3 N-{(1S)_2_[(5-fluoro-2·{[2-(3-fluorophenyl)ethyl]amino} each (1_fluorenyl)pyrazole-based (3-acridine) Base) benzylamino]-isopropyl bromide 2-aminoacetamide 0. 197 Μ+Η 473. 1 N-{(lR)_2-[(5-say-2-{[2_(3-fluorophenyl)ethyl]amino} each (1_methyl. σ Κ Κ) (3_吼. )) alkylamino]-isopropylbutene 2-perylene with amine 0. 1 Μ+Η 600. 2 N-{(lR)_2-[(5-fluoro-2_{[2-(3-fluorophenyl)ethyl]amino} each (1_fluorenyl), 251 200823188 IC50 arithmetic mean 0. 116 2. 328 8. 211 0. 443 0. 251 1. 002 0. 122 0. 024 0. 648 0. 636 0. 121 2. 264 0. 115 0. 285

離子 M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H m/z 化學名稱 • 唑斗基)(3-吡啶基))羰基胺基]-異丙基}-4-[(第三丁氧基)羰 基胺基]丁醯胺 N-{(lR)_2-[(5-氟-2·{[2-(3_ 氟苯基)乙基]胺基}-6-(1-甲基 口比 500.3 唑斗基)(3-吼啶基))羰基胺基]-異丙基}-4-胺基丁醯胺 N-{(2R)-2-[(2-甲氧基乙基)胺基]丙基}(5-氟-2-{[2-(3-氟苯 473 · 1 基)乙基]胺基}-6-(1-甲基吡唑斗基)(3-吡啶基))曱醯胺 N-{(2R)-2-[(第三丁氧基)羰基胺基]丙基}(5-氟-2-{[2-(3-氟 5〇1 · 1 苯基)乙基]胺基}各吡唑斗基(3-吡啶基))曱醯胺 乂((211)-2-胺基丙基)(5-氟-2-{|&gt;(3-氟苯基）乙基]胺基}-6- 401.1 吡唑-4-基(3-吡啶基))曱醯胺 N-{(lR)_2-[(5-氟-2_{[2-(3·氟苯基)乙基]胺基甲基吼 457·1 唑斗基)(3-吡啶基))羰基胺基]-異丙基}乙醯胺 N-{(2R)-2_[(曱基磺醯基)胺基]丙基}(5·氟-2_{[2-(3-氟苯基) 493 · 1 乙基]胺基甲基吡唑-4-基)(3-吡啶基))曱醯胺 N-{(lR)-2-[(5_氟-2-{[2_(3_氟苯基）乙基]胺基}_6-吼唑冰基 459· 1 (3_吼啶基))羰基胺基]-異丙基卜2-胺基乙醯胺 (5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-吼唑-4-基(3- η比啶 43 5 · 1基))-Ν-(2-吡啶基曱基)曱醯胺 N-{(2R)-2-[(2_羥基乙基)胺基]丙基}(5_氣ip#-氟苯基) 459·2 乙基]胺基}-6_(1-曱基吡唑冰基)(3-吡啶基))甲醯胺 N-{(2R)_2-[(胺曱醯基曱基)胺基]丙基}(5_氟ip#-氟苯 472· 1 基)乙基]胺基卜6_(1_甲基吡唑冰基χ3—吡啶基》曱醯胺 N-{(1 R)-2-[(5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-(1·甲基吡 唾-4-基)(3-u比啶基》羰基胺基]-異丙基卜2_(二曱基胺基）乙 500.2 醯胺 N-{(1 R)-2-[(5-氟-2-{[2-(3-氟苯基)乙基]胺基}-6-(1-曱基吡 °坐·4-基)(3_吼啶基))羰基胺基]-異丙基}(2S)-2-[(第三丁氧 602.2基)幾基胺基]-3-經基丙驢胺 N-{(1 R)-2-[(5-氟-2-{[2-(3-氟苯基)乙基]胺基甲基吡 唾-4-基)(3-吡啶基))羰基胺基]-異丙基}(2S)-2-胺基-3-羥基 502.2 丙醯胺 500.2 N-{(lR)-2-[(5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-(1-甲基吡 252 200823188 IC50 算數平均 離子 m/z 化學名稱 峻-4-基定基))幾基胺基]-異丙基}-2-胺基-2-曱基丙盤 胺 N-((lR)-l-{[(5-氟-2-{[2-(3-氟苯基)乙基]胺基}-6-(1-曱基口比 唑-4-基)(3-吡啶基))羰基胺基]曱基}丙基)-2-[(第三丁氧基) 3.04 M+H 586.3 羰基胺基]乙醯胺 N-((lR)-l-{[(5-氟-2-{[2-(3-氟苯基)乙基]胺基}-6-(1·甲基口比 0.131 M+H 486.2 唑-4-基)(3-吼啶基))羰基胺基]曱基}丙基)-2-胺基乙醯胺 N-((1R)-1_{[(5-氟-2-{[2-(3·氟苯基)乙基]胺基}-6-吼唑冰基 (3-吼啶基))羰基胺基]曱基}丙基)_2-[(第三丁氧基)羰基胺 4.323 M+H 572.3 基]乙醯胺 N-((lR)-l-{[(5-氟-2-{[2-(3-氟苯基)乙基]胺基}-6』比唑基 0.16 M+H 472.2 (3-吡啶基))羰基胺基]甲基}丙基)-2-胺基乙醯胺 N-{(lR)-2-[(5-氟-2-{[2-(3-氟苯基)乙基]胺基}-6-(1-甲基吼 0.131 M+H 486.2 唑-4-基)(3-吼啶基))羰基胺基]-異丙基}(2S)-2-胺基丙醯胺 N-((2R)-3-羥基-2-甲基丁基)(5-氟-2-{[2-(3-氟苯基)乙基]胺 0.283 M+H 444.2 基}-6-(1-甲基吼峻-4-基)(3-n比唆基))甲醯胺 Ν-{[2·(胺基甲基）(3-吼啶基）]甲基}(6-(2-氰基苯 0.006 M+H 481.1 基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比啶基))甲醯胺 Ν·{[2_(胺基甲基)(3_。比啶基)]甲基}(2][2-(3·氟苯基）乙基] 0.024 M+H 446.3 胺基}-6-吡唑-4-基(3-吡啶基))甲醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-啦啶 0.024 M+H 452.1 基))-N-(3-吼啶基甲基)甲醯胺 {6-苯基-2-[(2-(2-吼啶基)乙基)胺基](3-吼啶基)}-N-(3-吼啶 0.512 M+H 410.1 基曱基)曱醯胺 {6-(3,4-二氟苯基)-2-[(2-(2-吼啶基）乙基）胺基](3-σ比啶 1.206 M+H 446.1 基)}-Ν-(3-吼啶基曱基)曱醯胺 {6-(4_氟苯基）-2_[(2-(2-吼啶基）乙基）胺基](3- °比啶 1.045 M+H 428.2 基)}-Ν-(3-吼啶基曱基)甲醯胺 {6-(4-氣苯基）-2-[(2-(2- ^比σ定基）乙基）月女基](3- °比σ疋 0.629 M+H 444.1 基)}·Ν-(3-吼啶基曱基)曱醯胺 {6-(4-甲基苯基)-2-[(2·(2-吼啶基）乙基）胺基)(3-σ比啶 0.677 M+H 424.2 基)}·Ν-(3-吼啶基曱基)曱醯胺 253 200823188 IC50 算數平均 離子 m/z 化學名稱 1.935 M+H 435.1 {6-(4-氰基苯基&gt;2-[(2-(2-u比啶基）乙基）胺基](3-峨啶 基)}-N-(3』比啶基曱基)甲醯胺 1.063 M+H 440.1 {6-(4-甲氧基苯基)-2-[(2·(2-吼咬基）乙基）胺基](3- °比唆 基)}-Ν-(3-ΰ比啶基曱基)甲醯胺 2.43 M+H 440.2 {6-[4-(羥基甲基)苯基]-2-[(2-(2-吼啶基）乙基)胺基](34匕啶 基)}-Ν-(3』比啶基曱基)甲醯胺 3.375 M+H 478.1 {6-(3,4-二氯苯基)·2_[(2-(2- °比σ定基）乙基）胺基](3_ °比σ定 基)}-Ν-(3-吡啶基曱基)甲醯胺 2.285 M+H 478.1 {2-[(2-(2-吼啶基）乙基)胺基]-6-[4-(三氟甲基)苯基](34匕啶 基)}-Ν-(3』比啶基曱基)曱醯胺 0.989 M+H 468.1 4-{6-[(2-(2-°比咬基)乙基)胺基定基甲基)胺甲酷 基]-2-吡啶基}苯曱酸曱酯 0.809 M+H 453.2 {6-[4·(二曱基胺基)苯基]-2-[(2·(2_°比啶基)乙基)胺基](3』比 啶基)}-Ν-(3-σ比啶基曱基)甲醯胺 2.133 M+H 452.1 {6-(4-乙醯基苯基)-2-[(2-(2-吼啶基）乙基）胺基](3- °比啶 基)}-N-(3^比啶基甲基)甲醯胺 2.187 M+H 410.1 {6-苯基-2_[(2_(3·σ比唆基)乙基)胺基](3_°比°定基定 基曱基)甲醯胺 18.274 M+H 454.1 4·{6-[(2-(2_σΛσ定基)乙基)胺基]-ΗΝ_(3-σ比ϋ定基曱基)胺曱酿 基]-2-吼啶基}苯曱酸 19.129 M+H 411.1 义(3_°比。定基甲基）{6-(3_σΛσ定基)-2_[(2_(2-°比σ定基）乙基)胺 基](3-吡啶基)}甲醯胺 6.557 M+H 411.1 Ν-(3』比啶基曱基){6-(4_。比啶基)-2-[(2_(2_°比°定基）乙基)胺 基](3-吡啶基)}甲醯胺 5.379 M+H 411.2 Ν-(3-σ比啶基曱基){6-(2-°比啶基)-2-[(2-(2』比°定基）乙基)胺 基](3-吡啶基)}曱醯胺 2.538 M+H 453.1 4-{6-[(2-(2-吼啶基)乙基)胺基]-5-[Ν-(3_°比咬基甲基)胺曱酸 基]-2-吡啶基}苯曱醯胺 1.942 M+H 425.1 {2-[(2-經基-2-苯基乙基)胺基]各苯基(3』比咬基)}善(3』比 啶基甲基)甲醯胺 5.342 M+H 436.1 {2-[(2-(2-叱啶基）乙基)胺基]各(2-乙烯基苯基）（3_°比咬 基)}-N-(3-吼啶基曱基)甲醯胺 254 200823188 IC50 算數平均 離子 m/z 化學名稱 84.495 M+H 454.2 {6·[2-(甲氧基甲基)苯基]-2-[(2-(2-吡啶基)乙基)胺基](3-口比 啶基)}-N-(3-吡啶基甲基)甲醯胺 8.751 M+H 438.2 {6-(2-曱醯基苯基)-2-[(2·(2-吼啶基）乙基）胺基](3-n比啶 基)}-Ν-(3-吼啶基曱基)曱醯胺 0.559 M+H 443.2 (2-{[2-(3_氟苯基）-2-羥基乙基]胺基}-6-苯基（3-吡啶 基))-N-(3-吼啶基曱基)甲醯胺 0.339 M+H 468.2 (6-(2-氰基苯基)·2-{[2-(3-氤苯基)-2-羥基乙基]胺基}(3-吼唆 基))-N-(3-吡啶基甲基)甲醯胺 8.662 M+H 417.1 {2-[(2-(2-吼啶基）乙基）胺基]各(1，3-噻唑-2·基)(3-吼啶 基)}-N-(3-吼啶基甲基)曱醯胺 2.53 M+H 414.2 {6-(1-曱基°比唑-4-基)-2-[(2-(2-°比啶基）乙基)胺基](3-吼啶 基)}-N-(3-吼啶基甲基)甲醯胺 39.528 M+H 322.1 [3-(胺基曱基)-6-苯基(2_吼啶基)P-(3_氟苯基)乙基]胺 0.534 M+H 463.1 (6-(3,4-二氟苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-Ν-(3·批啶基甲基)甲醯胺 0.28 M+H 458.1 (6-(5-氣基(2-σ塞吩基))-2- {[2_(3 -氟本基）乙基]胺基} (3 - °比σ定 基))-Ν-(3-吼啶基甲基)曱醯胺 0.052 M+H 461.1 (2-{[2-(3-氟苯基)乙基]胺基}各(5-曱醯基(2-噻吩基))(3』比 啶基))-Ν-(3-吡啶基曱基)曱醯胺 0.783 M+H 461.1 (2-{[2-(3-氟苯基)乙基]胺基}各(3_曱醯基(2_噻吩基))(3·吼 啶基))-Ν-(3-°比啶基甲基)曱酸胺 1.482 M+H 461.1 (2-{[2-(3-氟苯基)乙基]胺基}-6-(2-曱醯基(3_噻吩基))(3_ 口比 啶基))-N-(3-u比啶基甲基)甲醯胺 30.616 M+H 699.2 [2-{[2-(3-氟苯基）乙基]胺基}各(6_{[2-(3·氟苯基）乙基]胺 基}-5-[N-(3-吼啶基曱基）胺甲醯基](2-ϋ比啶基))(3-吼啶 基)]-Ν-(3_σΛσ定基甲基)曱酷胺 1.567 M+H 463.1 (2-{[2-(3-氟苯基)乙基]胺基}-6_1&gt;濟基甲基)(3_噻吩基)](3-吡啶基))_Ν-(3-ϋ比啶基曱基)曱醯胺 49.792 M+H 418.1 (2-{[2-(3_氟苯基)乙基]胺基}各口寻。坐冬基比啶基))-Ν-(3-吡啶基甲基)甲醯胺 0.178 M+H 475.1 (6-(5-乙醯基(2-噻吩基))-2_{|&gt;(3-敦苯基）乙基]胺基}〇°比 啶基))-Ν-(3·°比啶基甲基)曱酸胺 255 200823188 IC50 算數平均 離子 m/z 化學名稱 55.694 M+H 462.1 (卜[3-(胺基甲基）（2_噻吩基)]-2-{[2-(3_氟苯基)-乙基]胺 基}(3-吡啶基))-Ν-(3·吡啶基甲基)曱醯胺 0.415 M+H 477.1 (2·{[2_(3_氟苯基)乙基]胺基}-6-[5-(羥基乙基)(2_噻吩基)](3_ 吡啶基))-Ν-(3-吡啶基曱基)曱醯胺 0.014 M+H 458.1 (6-(4-氰基(3 -嘍吩基))-2- {[2·(3 -氣苯基)乙基]胺基}(3-。比咬 基))-Ν-(3-吡啶基曱基)曱醯胺 2.698 M+H 462.1 (6_[5-(胺基甲基)(2-噻吩基)]-2-{|&gt;(3-氟苯基)乙基]胺基}(3-吡啶基))-N-(3-。比啶基曱基)曱醯胺 0.323 M+H 481.2 N-{[5-(胺基曱基）(3-吼啶基）]曱基}(6-(2-氰基苯 基{[2-(3 -氟苯基)乙基]胺基} (3-0比°定基))曱酿胺 0.081 M+H 482.1 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3·吼啶 基))-N-{[5-(羥基曱基)(3-吼啶基)]甲基}甲醯胺 2.715 M+H 579.2 Ν·({5_[3,3-雙(二甲基胺基)_2_氮雜丙-2-烯基](3-吡啶基)}曱 基)(6-(2-氰基苯基)-2_{[2_(3-氟苯基)乙基]胺基}(3-吼啶基)) 甲醯胺 0.624 M+H 481.1 Ν-{[3-(胺基曱基）(2-。比啶基）]曱基}(6-(2-氰基苯 基)-2·{[2_(3_氟苯基)乙基]胺基}(3』比啶基))曱醯胺 2.437 M+H 824.3 (6_(2_氰基苯基)-2-{[2-(3_氟苯基）乙基]胺基}(3-吼啶基))-Ν-[(3-{[(6_(2-氰基苯基)-2-{[2_(3-氟苯基）乙基]胺基}(3-口比 啶基))羰基胺基]曱基}(2-吼啶基))曱基]曱醯胺 70.994 M+H 442.1 Ν-[(2-{[2-(3_氟苯基)乙基]胺基}-6-苯基(3-吼啶基))曱基](3- 吡啶基胺基)甲醯胺 0.512 M+H 486.1 (5-氯-6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-(3-吼啶基甲基)甲醯胺 2.653 M+H 531 (5-溴-6-(2-氰基苯基)-2-{〇(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-(3』比啶基曱基)曱醯胺 0.318 M+H 477.1 (5-氰基-6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基} (3-。比 啶基))-N-(3-吼啶基曱基）曱醯胺 0.072 M+H 486.1 N-[(2_氯(3』比啶基))曱基](6-(2-氰基苯基)-2-{[2-(3_氟苯基) 乙基]胺基}(3-吡啶基))曱醯胺 0.013 M+H 510.1 N-({2-[(2-胺基乙基)胺基](3-吼啶基)}曱基)(6-(2-氰基苯 基)-2_{[2-(3·氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 256 200823188 IC50 算數平均 離子 m/z 化學名稱 0.088 M+H 453.1 (2_{[2-(3·氟苯基）乙基]胺基}_5·氧基茚基并[3,2-b]II比咬冬 基)-N-(3-吼啶基甲基)甲醯胺 0.029 M+H 472 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3- σ比咬 基))-Ν-[(6-氧基〇哌啶基))甲基]甲醯胺 0.877 M+H 629.2 Ν-[(Η3-[(第三丁氧基)羰基胺基]丙基氧基(2_哌唆基)) 甲基](6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3_^唆 基))甲醯胺 0.025 M+H 529.2 Ν-{[1-(3·胺基丙基)_6_氧基(2_派咬基)]曱基}(卜(2_氰基苯 基)-2_{|&gt;(3-氟苯基)乙基]胺基}(3_π比唆基))甲醯胺 1.024 M+H 458.2 N-[((2S)(2-哌啶基))曱基](6-(2-氰基苯基)-2-{[2·(3-氟苯基) 乙基]胺基}(3-°比淀基))甲醯胺 16.979 M+H 615.2 N-[((2S)-l-{2_[(第三丁氧基)羰基胺基]乙酸基泊雇。定基)) 曱基](6_(2_氰基苯基)_2_ {[2_(3·氣苯基)乙基]胺基} (3 -。比唆 基))甲醯胺 0.074 M+H 515.2 N-{[(2S)-l-(2-胺基乙酸基)(2-旅咬基)]曱基}(6-(2-氰基苯 基)-2-{[2-(3·氟苯基)乙基]胺基}(3_吼啶基))曱醯胺 8.636 M+H 629.2 N-[((2S)-1-{H(第三丁氧基)羰基胺基]丙醯基}(2·哌啶基)） 甲基](6-(2-氰基苯基)-2-{[2-(3_氟苯基)乙基]胺基}(3_σ比啶 基))曱醯胺 0.109 M+H 529.2 N-{[(2S)-l-(3-胺基丙醯基)(2-哌啶基)]甲基}(6-(2-氰基苯 基)-2_{[2_(3-氟苯基)乙基]胺基}(3_σ比π定基))甲酸胺 1.632 M+H 536.3 Ν-{[(2S)· 1-(甲基磺醯基)(2-哌啶基)]甲基} (6-(2-氰基苯 基)-2_{[2-(3_氟苯基)乙基]胺基}(3』比σ定基))曱醯胺 0.015 M+H 472.2 N-[((2R)-6-氧基（2-哌啶基））曱基](6-(2-氰基苯 基)-2_{[2-(3_氟苯基)乙基]胺基}(3·吼啶基))曱醯胺 0.392 M+H 629.4 N-[((2R)-1-{H(第三丁氧基)羰基胺基]丙基卜6-氧基(2-哌 啶基))甲基](6-(2-氰基苯基)-2-{|&gt;(3-氟苯基)乙基]胺基}(3_ 吡啶基))甲醯胺 0.026 M+H 529.2 N-{[(2R)-l-(3-胺基丙基)各氧基(2-哌啶基)]甲基}(6- (2-氰 基苯基)-2_([2_(3-就苯基)乙基]胺基}(3-°比咬基))曱醯胺 1.974 M+H 458.1 N-[((3S)(3-哌啶基))曱基](6-(2-氰基苯基)-2-{[2-(3-敗苯基） 乙基]胺基}(3_吡啶基))曱醯胺 257 200823188 IC50 算數平均 離子 m/z 化學名稱 0.696 M+H 500.3 N-[((3R)-1-乙酸基（3·哌啶基））曱-基](6-(2-氰基苯 基)-2-{[2_(3-氟苯基)乙基]胺基}(3』比啶基))甲醯胺 0.718 M+H 516.3 (3R)-3-{[(6_(2-氰基苯基)-2-{[2-(3-氣苯基)乙基]胺基}(3』比 啶基))羰基胺基]甲基}哌啶羧酸甲酯 0.199 M+H 615.4 N-[((3RH-{2_[(第三丁氧基)羰基胺基]乙醯基}(3_娘啶基)) 曱基](6-(2-氰基苯基)-2_{[2·(3-氟苯基)乙基]胺基}(3-啦啶 基))曱醯胺 3.79 M+H 629.4 N-[((m)-l-{3-[(第三丁氧基)羰基胺基]丙醯基}(3-旅啶基》 甲基](6_(2_氰基苯基)-2_{|&gt;(3-氟苯基)乙基]胺基}(3-π比啶 基))曱醯胺 6.161 M+H 643.4 &gt;H((3R)-l-{4_[(第三丁氧基)羰基胺基]丁醯基}(3_派啶基)) 甲基](6_(2_氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比啶 基))曱醯胺 0.246 M+H 615.4 N-{[(3R)-l-(2-胺基乙醯基)(3-哌啶基)]曱基}(6-(2-氰基苯 基)-2-{[2_(3_敗苯基)乙基]胺基)(3_〇比咬基))曱驢胺 0.173 M+H 629.5 N-{[(3R)-l-(3-胺基丙醯基)(3-哌啶基)]甲基}(6-(2-氰基苯 基)_2_ {[2_(3 -氟苯基)乙基]胺基} (3 -吼唆基))曱醯胺 0.512 M+H 543.3 N-{[(3R)-l-(4-胺基丁醯基)(3-哌啶基)]甲基}(6-(2-氰基苯 基)·2- {[2_(3 - IL苯基)乙基]胺基} (3 - °比咬基))曱醯胺 0.791 M+H 673.3 N-( {(2R)-1 - [4_(1，3·二氧基苯并[c]唆琳 基)丁基]-6-氧基 (2-哌啶基)}曱基)(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺 基}(3-吡啶基))曱醯胺 0.032 M+H 543.2 N-{[(2R)-l-(4_胺基丁基)-6-氧基(2·旅唆基)]曱基}(6-(2-氰 基苯基)-2-{|&gt;(3-氟苯基)乙基]胺基}(3_吼啶基))曱醯胺 5.537 M+H 523.2 1^-[((38,48,211，511)-3,4,5,6-四|^基(215-3,4,5,6-四氫11辰喃-2- 基))曱基](6普氰基苯基)_2· {[2·(3·氟苯基)乙基]胺基} (3_ϋ比 啶基))甲醯胺 13.202 M+H 533.2 2-[5-(N-{[(2R)-l-(3-胺基丙基)-5-氧基吡咯啶基]甲基}胺 曱酸基)-6-{[2-(3_氟苯基)乙基]胺基卜:^如定基]苯甲酸胺 3.262 M+H 615.2 N-[2-((2R)-2-{[(6-(2-氰基苯基)-2-{[2-(3_ 氟苯基）乙基]胺 基}(3』比啶基))幾基胺基]甲基}吡略啶基)(1 S)-l-曱基氧 基乙基](第三丁氧基)曱醯胺 258 200823188 IC50 算數平均 離子 m/z 化學名稱 0.053 M+H 515.2 N-{[(2R)-l-((2S)-2-胺基丙醯基)吼咯啶-2-基]曱基}(6-(2-氰 基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 3.94 M+H 615.2 N-[(lR)-2-((2R)-2-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基] 胺基}(3-吡啶基))羰基胺基]曱基}吡咯啶基)-1-曱基-2-氧基 乙基](第三丁氧基)曱醯胺 0.166 M+H 515.2 N-{[(2R)-H(2R)-2-胺基丙醯基)吼咯啶-2-基]曱基}(6-(2-氰 基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比啶基))曱醯胺 0.052 M+H 558.2 N-{[(2R)-l-((2S)-2,5-二胺基戊醯基）吼咯啶-2-基]甲 基}(6-(2_氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比啶基)) 曱醯胺 0.046 M+H 451.1 队[(2-氯(3-吼啶基)）甲基](2-{[2-(3-氟苯基）乙基]胺 基}-6-(1-曱基吡唑-4-基)(3-吡啶基))甲醯胺 0.129 M+H 489.2 N-({2-[(3_胺基丙基)胺基](3-吼啶基)}甲基)(2-{[2-(3-氟苯 基)乙基]胺基}-6-吡唑-4-基(3-吡啶基))甲醯胺 0.122 M+H 475.1 N-({2-[(2-胺基乙基)胺基](3·啦啶基)}甲基)(2-{[2-(3-氟苯 基)乙基]胺基}-6-啦唑-4-基(3-吼啶基))曱醯胺 1.459 M+H 541.3 (2R)-2-{[(5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6·(1-甲基吼唑 -4-基)(3-吡啶基))羰基胺基]甲基}吡咯啶羧酸第三丁酯 0.275 M+H 441.1 义[((21〇吼咯啶-2-基）曱基](5_氟-2-{[2-(3-氟苯基）乙基]胺 基曱基吡唑-4-基)(3-啦啶基)）曱醯胺 0.625 M+H 598.3 N-[((2 R)小{2-[(第三丁氧基)羰基胺基]乙醯基}吡咯啶-2-基）甲基](5_氟-2-{[2_(3-氟苯基）乙基]胺基}-6-(1•曱基吼唑 -4·基)(3-吼啶基))甲醯胺 0.065 M+H 476.1 (2·{[2-(3-氟苯基）乙基]胺基}-6-吡唑-4-基（3-吡啶基))-N-({2-[(2-羥基乙基)胺基](3-吡啶基)}甲基)甲醯胺 0.488 M+H 564.2 N-[(2-{[(第三丁氧基）羰基胺基]曱基}(3-σ比啶基)）曱 基](5-氟-2-{[2-(3-氟苯基）乙基]胺基卜6-吼唑-4-基(3-°比啶 基))甲醯胺 0.012 M+H 464.1 Ν-{[2·(胺基甲基)(3』比啶基)]甲基}(5_氟_2_{[2-(3-氟苯基） 乙基]胺基}-6-吡唑-4-基(3-吡啶基))曱醯胺 1.079 M+H 584.2 N-[((2R)-l-{2_[(第三丁氧基)羰基胺基]乙醯基咯啶冬 基）甲基](5_氟-2-{[2-(3-氟苯基)乙基]胺基}-6-吼唑-4-基(3- 259 200823188 IC50 算數平均 離子 m/z 化學名稱 -吡啶基))甲醯胺 . * N-{[(2R)-l-(2-胺基乙酿基）σ比洛淀-2-基]甲基}(5-亂 -2-{[2-(3-氟苯基）乙基]胺基}-6-α比唑-4-基(3-吼啶基)）甲醯 0.061 M+H 484.1 胺 N-[((2R)-l-{3-[(第三丁氧基)羰基胺基]丙醯基}吼咯啶-2-基）甲基](5_氣-2-{[2-(3-氣苯基）乙基]胺基}-6-°比唾-4-基(3- 0.98 M+H 598.3 。比。定基))甲驢胺 N-{[(2R)-1_(3-胺基丙醯基）吼咯啶-2-基]甲基}(5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-吼唑-4-基(3-吼啶基))甲 0.09 M+H 498.2 醯胺 N-[((2R)-1 - {4-[(第三丁氧基）羰基胺基]丁醯基}吼咯啶 -2-基）甲基](5-氟-2-{[2·(3-氟苯基）乙基]胺基}-6-吼唑-4-基 0.75 M+H 612.2 (3-吡啶基))甲醯胺 N-{[(2R)-l-(4-胺基丁醯基）吼咯啶-2-基]曱基}(5-氟 -2-{[2-(3-氟苯基）乙基]胺基}-6-吼唑-4-基(3-吼啶基)）曱醯 0.047 M+H 512.2 胺 义[((211户比咯啶-2-基）甲基](5-氟-2-{[2-(3-氟苯基）乙基]胺 0.394 M+H 427.1 基}-6』比唑-4-基(3-吼啶基》曱醯胺 N-[((2R)-l-{3-[(第三丁氧基)羰基胺基]丙基}-5-氧基啦咯啶 -2-基）甲基](5_氟-2-{[2-(3-氟苯基）乙基]胺基}-6-°比°坐-4-基 0.354 M+H 598.2 (3-吡啶基))甲醯胺 N-{[(2R)-l-(3-胺基丙基)-5-氧基吼17各σ定-2-基]曱基} (5-氟 -2-{[2-(3-氟苯基）乙基]胺基}-6-°比°圭·4-基(3-°比°定基)）甲酿 0.066 M+H 498.1 胺 Ν-(胺甲醯基曱基)(5-氟_2_ {[2-(3·氟苯基)乙基]胺基卜6_π比 0.14 M+H 401.1 唑-4-基(3·吼啶基))曱醯胺 2-[(5-氟-2-{[2_(3_氟苯基）乙基]胺基}-6_°比°坐-4-基(3-外匕0定 0.065 M+H 415 基))羰基胺基]-Ν-曱基乙醯胺 N-[((2R)-l-{(2S)_2-[(第三丁氧基)幾基胺基]·3-經基丙酸胺} σ比咯啶基）甲基](5_氣-2-{[2-(3-氟苯基)乙基]胺基}« 1.001 M+H 614.3 唑-4-基(3-吡啶基))甲醯胺 0.059 M+H 514.1 Ν- {[(2R)-1 -((2S)-2-胺基-3-羥基丙醯基）σ比咯啶-2-基]甲 260 200823188 IC50 算數平均 離子 m/z 化學名稱 基} (5-氟-2- {[2-(3 =氟苯基）乙基]胺基} -6- °比σ坐-4-基(3 -吼咬 基))甲醯胺 Ν-[(2-{[(第三丁氧基）羰基胺基]甲基}(3-α比啶基)）曱 基](5-氟-2_{[2-(3_氟苯基)乙基]胺基}_6_(2-吼啶基）0·吼啶 3.665 M+H 575.2 基))甲醯胺 Ν-{[2_(胺基曱基)(3-吼啶基)]曱基}(5-氟-2_{[2-(3·氟苯基) 0.066 M+H 475.1 乙基]胺基}-6-(2-吡啶基)(3-吡啶基))曱醯胺 (5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-(1-甲基吼唑-4-基)(3- 0.381 M+H 430.1 σ比啶基))-N-(2-羥基-2-甲基丙基)甲醯胺 (5-氣-2-{[2-(3-氣苯基）乙基]胺基}-6-(1-甲基°比0坐-4-基)(3_ 0.224 M+H 444.1 σ比啶基))-N-(3-羥基-2,2-二甲基丙基)曱醯胺 N-((2R)-2_甲基；氧基丁基)(5-氟-2-{[2-(3_氟苯基)乙基]胺 0.109 M+H 442.2 基}-6-(1-曱基。比唾-4-基)(3-吼咬基))甲酸胺 N-((2R)-3-羥基-2,3-二曱基丁基)(5-氟-2-{[2-(3-氟苯基）乙 1.225 M+H 458.1 基]胺基}-6·(1-甲基吡唑-4-基)(3-吡啶基))甲醯胺 2-[(第三丁氧基)羰基胺基]乙酸2-((2R)-2-{[(5-氟-2-{[2-(3- 氟苯基)乙基]胺基}-6-(1-曱基吨唑-4-基)(3-吼啶基))羰基胺 0.191 M+H 642.2 基]甲基}氮。旦基)-2-氧基乙基酯 2-胺基乙酸2-((2R)-2-{[(5-氟-2-{[2-(3·氟苯基）乙基]胺 基}-6-(1-曱基°比唾-4-基）（3-σΛσ定基))幾基胺基]曱基}氮口旦 0.045 M+H 542.2 基)-2-氧基乙基西旨 二甲基磷酸2-((2R)-2-{[(5_氟-2-{[2-(3-氟苯基）乙基]胺 基}-6-(1-曱基吼唑-4-基）（3-吼啶基))羰基胺基]甲基}氮。旦 0.4 M+H 593.2 基)-2-氧基乙基酯 (2-{[2-(3-氟苯基)乙基]胺基}-6-[5-(羥基曱基)(2-售吩基)](3_ 0.041 M+H 463.1 °比啶基))-N-(3-吼啶基曱基)曱醯胺 N-({2-[(3-胺基丙基)胺基](3-吼啶基)}曱基)(6-(2-氰基苯 0.017 M+H 基)-2-{[2_(3_氟苯基)乙基]胺基}(3』比啶基))曱醯胺 (5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6·-比唑-4-基(3-吼啶 0.018 M+H 基))_N-(3-呢啶基甲基)曱醯胺 N-{[(2R)-l-(2-胺基乙醯基）吼咯啶-2-基]甲基}(5_氟 0.066 M+H -2-{[2-(3-氟苯基）乙基]胺基}-6-(1-曱基吼唑-4-基)(3-吼啶 261 200823188 IC50 算數平均 離子 m/z 化學名稱 基))甲醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基H-甲基(3』比啶 1.076 M+H 466.2 基))-N-(3-吼啶基甲基)甲醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 16.894 M+H 537.2 基))-N-[(6-嗎啉基(3_°比啶基))曱基]甲醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 66.631 M+H 521.2 基))-N-[(6』比咯啶基(3』比啶基))曱基]曱醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 1.752 M+H 536.2 基))-N-[(6-哌畊基(3-n比啶基))甲基]曱醯胺 N-{[6-(4-乙醯基哌畊基)(3-σ比啶基)]甲基}(6-(2-氰基苯 7.747 M+H 578.2 基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比啶基))曱醯胺 Ν-[(6_溴(2_吼啶基))甲基](6-(2-氰基苯基)冬{[2-(3-氟苯基) 0.233 M+H 530.1 乙基]胺基}(3-吡啶基))甲醯胺 2-[(2-{[2-(3-氟苯基）乙基]胺基}-6-[5-(羥基曱基)(2-噻吩 0.254 M+H 443.1 基)](3-吼啶基))羰基胺基]-N-甲基乙醯胺 N-(2-胺曱醯基乙基)(2-{[2-(3-氟苯基）乙基]胺基}-6-[5-(羥 0.549 M+H 443.1 基曱基)(2-噻吩基)](3-吼啶基))甲醯胺 (2-{[2_(3_氟苯基)乙基]胺基卜6-[5_(羥基曱基)(2-嗟吩基))(3- 0.045 M+H 463.1 σ比啶基))-N-(2-吡啶基甲基)甲醯胺 N-(胺曱醯基曱基)(2-{[2·(3_氟苯基)乙基]胺基卜6_[5_(羥基 0.496 M+H 429.1 曱基)(2_σ塞吩基)](3_σ比咬基))曱酸胺 2-[(6-(2_氰基苯基氟苯基)乙基]胺基}(3』比啶基)) 24.88 M+H 496.1 羰基胺基]-Ν-(曱基磺醯基)乙醯胺 胺基甲基)環己基]甲基氰基苯基)_2][2-(3-氟 0.352 M+H 486.2 苯基)乙基]胺基}(3_吼啶基))曱醯胺 Η(6-(2_氰基苯基)-2-{[2-(3_氟苯基)乙基]胺基卜啶基) 11.631 M+H 472.1 羰基胺基]環戊烷甲醯胺 (6-(2-氰基苯基)_2-{[2-(3-氟苯基）乙基]胺基}(3^比啶 16.178 M+H 473.2 基))-N-〇旅畊基乙基)曱醯胺 (6-(2-氰基苯基峰{[2_(3-氟苯基）乙基]胺基}(3-。比啶 0.266 M+H 467.1 基))-N-〇吡畊I基乙基)曱醯胺 0.026 M+H 453.1 (6-(2-氰基苯基)_2-{[2_(3_氟苯基）乙基]胺基}(&gt; σ比啶 262 200823188 IC50 算數平均 離子 m/z 化學名稱 基))-N中比畊-2-基甲基)甲醯胺 · N-((lS)-5-胺基-1-胺甲醯基戊基)(6-(2-氰基苯基)-2-{[2-(3- 4.421 M+H 489.1 氟苯基)乙基]胺基}(3』比啶基))曱醯胺 N-(3-胺基-1-胺曱醯基丙基)(6-(2-氰基苯基)-2-{[2-(3-氟苯 1.906 M+H 461.1 基)乙基]胺基} (3-吡啶基))曱醯胺 N-{(1 R)-l-胺曱醯基-5-[(苯基曱氧基)羰基胺基]戊基}(6-(2- 58.8 M+H 623.2 氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 N-(4-胺基-1·胺曱醯基丁基)(6-(2-氰基苯基)-2-{[2-(3-氟本 0.59 M+H 475.1 基)乙基]胺基} (3-吡啶基))曱醯胺 N-((lR)-5-胺基-1-胺甲醯基戊基)(6-(2-氰基苯基)-2-{[2-(3- 1.28 M+H 489.1 氟苯基)乙基]胺基}(3-吡啶基))甲醯胺 N-({6-[(2-胺基乙基)胺基](2-吼啶基)}甲基)(6-(2-氰基苯 0.007 M+H 510.1 基)-2-{[2-(3-氟苯基)乙基]胺基)(3-吡啶基))曱醯胺 N-({6-[(3-胺基丙基)胺基](2-吼啶基)}甲基)(6-(2-氰基苯 0.005 M+H 524.2 基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 N-{(4R)-4-胺曱醯基-4-[(6-(2-氰基苯基)-2-{[2_(3-氟苯基)乙 19.6 M+H 609.1 基]胺基}(3-n比啶基))羰基胺基]丁基}(苯基甲氧基)甲醯胺 N-((lS)-4-胺基-1·胺甲醯基丁基）(6-(2-氰基苯 5.404 M+H 475.1 基)-2_{[2-(3_氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 N-((lR)-4-胺基-1-胺甲醯基丁基)(6-(2-氰基苯基)-2-{[2-(3- 7.413 M+H 475.1 氟苯基)乙基]胺基}(3·吡啶基))曱醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3- °比啶 0.963 M+H 444.1 基))-N-(吡咯啶-3-基甲基)甲醯胺 Ν-{[1-(2-胺基乙驢基）σ比p各σ定-3-基]甲基}(6-(2-氣基苯 0.203 M+H 501.1 基)-2-{[2-(3-1苯基)乙基]胺基}(3』比啶基))曱醯胺 Ν-{[1-(3-胺基丙醯基）π比咯啶_3_基]甲基}(6-(2-氰基苯 0.27 M+H 515.1 基)-2_{[2-(3_氟苯基)乙基]胺基}(3·吼啶基))甲醯胺 Ν-{[1-(4-胺基丁酿基）。比嘻咬_3_基]甲基}(6-(2-氰基苯 0.433 M+H 529.1 基)-2-{[2_(3_氟苯基)乙基]胺基}(3』比啶基))曱醯胺 N-[(l-乙醯基吡咯啶-3-基)曱基](6-(2-氰基苯基)-2- {[2-(3·氟 0.334 M+H 486.1 苯基)乙基]胺基}(3-°比〇定基))曱酸胺 4.787 M+H 501.2 Ν-{[1-(3-胺基丙基）σ比p各咬_3_基]甲基}(6-(2-氰基苯 263 200823188 IC50 算數平均 離子 m/z 化學名稱 ―基)-2_{[2-(3-氟苯基)乙基]胺基}(3』比啶基))甲酸胺， N-(3-胺基-2-胺甲醯基丙基)(6-(2-氰基苯基)-2-{[2-(3·氟苯 6.654 M+H 460.5 基)乙基]胺基}(3_ϋ比咬基))甲酸胺 (2][2-(3-1苯基）乙基]胺基}-6-(1_甲基°比唑斗基)(3_°比啶 1.236 M+H 452.3 基))-Ν-[(6-氧基哌畊-2-基)甲基]甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6- °比唑冬基（3-吼啶 0.973 M+H 438.3 基))-Ν-[(6-氧基哌畊-2-基)甲基]甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-σ比唑-5-基（3-σ比啶 6.954 M+H 438.3 基：))-Ν-[(6-氧基哌畊_2_基)甲基]甲醯胺 (6-(2-氰基苯基)_2-{[2-(3-氟苯基）乙基]胺基}(3_ °比啶 2.565 M+H 551.1 基))-N-{[4-(甲基磺醯基)-6·氧基哌畊-2-基]曱基}甲醯胺 N-[(4-乙酿基-6-氧基旅_-2-基）曱基](6-(2-氰基苯 1.635 M+H 515.1 基)冬{[2_(3-氟苯基)乙基]胺基}(3』比啶基))甲醯胺 (6-(2-氰基苯基)-2-{[2·(3-氟苯基）乙基]胺基}(3- ϋ比啶 0.037 M+H 487.1 基))-Ν-[(4·曱基-6-氧基哌畊-2-基)甲基]甲醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3- °比啶 0.866 M+H 461.2 基))-N-{2-[(曱基胺基)羰基胺基j乙基}甲醯胺 Ν-(2· {[(2-胺基乙基）磺醯基]胺基}乙基)(6-(2-氰基苯 1.548 M+H 511.2 基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比啶基))曱醯胺 N-[((2S)吼咯啶-2-基）曱基](6-(2-氰基苯基)-2-{[2-(3-氟苯 4.569 M+H 444.2 基)乙基]胺基}(3-吡啶基))甲醯胺 2-胺基-Ν·{2-[(6·(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 1.23 M+H 461.2 基}(3-吡啶基))羰基胺基]乙基}乙醯胺 3-胺基-Ν-{2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 4.325 M+H 475.2 基}(3』比啶基))羰基胺基]乙基}丙醯胺 4-胺基-N_ {2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 1.265 M+H 489.2 基}(3-1〇比°定基))幾基胺基]乙基} 丁酸胺 2-[(第三丁氧基)羰基胺基]-N-{2_[(6-(2-氰基苯基)-2·{[2-(3- 氟苯基）乙基]胺基}(3-吼啶基))羰基胺基]乙基}-Ν-曱基乙 15.303 M+H 575.3 醯胺 4-[(第三丁氧基)羰基胺基]-Ν·{2-[(6_(2-氰基苯基)-2-{[2-(3- 3.883 M+H 603.3 氟苯基）乙基]胺基}(3-吼啶基))羰基胺基]乙基}-Ν-甲基丁 264 200823188 IC50 算數平均 離子 m/z 化學名稱 醯胺 - N-{[(2S)-l-(2-胺基乙醯基)吼咯啶-2-基]甲基}(6-(2-氰基苯 0.995 M+H 501.2 基)-2-{[2-(3_氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 N_{[(2S)-l-(3-胺基丙醯基)吼咯啶-2-基]甲基}(6-(2-氰基苯 1.856 M+H 515.2 基)-2_{[2-(3_氟苯基)乙基]胺基}(3·吼啶基))甲醯胺 N-{[(2S)-l-(4-胺基丁醯基)吼咯啶-2-基]曱基}(6-(2-氰基苯 1.27 M+H 529.3 基)-2_{[2_(3-氟苯基)乙基]胺基}(3』比啶基))曱醯胺 2-胺基-N-{2-[(6-(2-氰基苯基)-2-{[2·(3-氟苯基）乙基]胺 1.374 M+H 475.2 基}(3-吡啶基))羰基胺基]乙基}-Ν-曱基乙醯胺 3-胺基-1^-{2-[(6-(2-氣基苯基)-2-{[2-(3-氟苯基）乙基]胺 1.775 M+H 489.2 基}(3-吡啶基))羰基胺基]乙基}-Ν-甲基丙醯胺 4·胺基-Ν-{2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 1.2 M+H 503.2 基}(3-吡啶基))羰基胺基]乙基}-N-曱基丁醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 1.385 M+H 496.2 基))-N-{2·[曱基(甲基磺醯基)胺基]乙基}甲醯胺 3-胺基-N-(2-胺基乙基)-2-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯 13.725 M+H 504.2 基)乙基]胺基}(3_吡啶基))羰基胺基]甲基}丙醯胺 N-(2-羰基胺基-2-甲基丙基)(6-(2-氰基苯基)-2-{[2-(3-氟苯 0.151 M+H 460.2 基)乙基]胺基}(3-。比啶基))曱醯胺 N-((2S)·2·胺基各羥基丙基)(6_(2_氰基苯基)冬{[2-(3-1苯 1.588 M+H 434.3 基)乙基]胺基}(3_吡啶基))曱醯胺 N-((lS)-l-{[(6-(2_ 氰基苯基)-2-{[2_(3_ 氟苯基)乙基]胺基}(3- 0.249 M+H 491.1 吡啶基))羰基胺基]曱基}-2-經基乙基)-2-胺基乙醯胺 2-胺基乙酸(2S)-2-(2-胺基乙醯基胺基)-3-[(6-(2-氰基苯 基)-2-{[2_(3-1苯基)乙基]胺基}(3-π比啶基》幾基胺基]丙基 5.705 M+H 548.3 N-((lR)-l-{[(6-(2-氰基苯基)-2-{[2-(3- 1 苯基）乙基]胺 0.441 M+H 504.2 基}(3_吼啶基))幾基胺基]曱基}冬甲基丙基)-2-經基乙醯胺 N-((l R)-l-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 0.939 M+H 503.3 基}(3-°比啶基))羰基胺基]曱基}_2_曱基丙基)-2-胺基乙醯胺 N-((2R)-2-胺基-4-曱基戊基)(6-(2-氰基苯基)-2·{[2-(3-氟苯 1.237 M+H 460.3 基)乙基]胺基}(3_吼°定基))曱酸胺 265 200823188 IC50 算數平均 離子 m/z 化學名稱 1.169 M+H 518.2 N-((lR)-l-{[(6-(2-氛基苯基)-2-{[2-(3-氣苯基）乙基]胺 基}(3·吡啶基))羰基胺基]甲基}-3-甲基丁基)-2-羥基乙醯胺 0.913 M+H 517.2 N-((lR)-l-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-吡啶基))羰基胺基]曱基}-3-曱基丁基)-2-胺基乙醯胺 12.554 M+H 490.2 N-((lR)-2-胺基小{[(6-(2-氰基苯基)冬{[2_(3_氟苯基)乙基] 胺基}(3_吡啶基))羰基胺基]曱基}乙基)-2-胺基乙醯胺 10.561 M+H 491.2 N-(( 1 R)-2-胺基-1 - {[(6_(2·氰基苯基)-2_ {[2_(3 -氟苯基)乙基] 胺基}(3-吡啶基))羰基胺基]甲基}乙基)-2-羥基乙醯胺 0.352 M+H 458.3 N-((3R)-2-氧基(3-旅淀基))(6-(2-氰基苯基)-2-{[2·(3-氟苯 基)乙基]胺基}(3-°比啶基))甲醯胺 17.307 M+H 423.1 {2-[((2R)-2-苯基丙基)胺基]-6-苯基(3·吼啶基)}-Ν-(3·-比啶 基曱基)曱醯胺 0.564 M+H 432.1 N-(胺甲醯基乙基)(6_(2_氰基苯基)-2-{[2-(3-氟苯基)乙基]胺 基}(3-吼啶基))甲醯胺 0.532 M+H 432.1 N-((1R)-1-胺甲醯基乙基)(6-(2-氰基苯基)-2-{[2_(3-氟苯基) 乙基]胺基}(3-吡啶基))甲醯胺 6.98 M+H 447.1 (23)-2-[(6-(2_氰基苯基)-2_{[2-(3-氟苯基）乙基]胺基}(3-n比 啶基))羰基胺基]丙酸曱酯 0.743 M+H 447.1 (2R)-2_[(6_(2-氰基苯基)-2_{[2_(3-氟苯基）乙基]胺基}(3』比 啶基))羰基胺基]丙酸甲酯 0.101 M+H 433.1 2-[(6_(2-氰基苯基)·2_ {[2-(3_氟苯基)乙基]胺基)-3·-比啶基) 羰基胺基]乙酸曱酯 1.083 M+H 405.1 (6-(2·氣基本基)-2·{[2-(3_氟苯基）乙基]胺基}(3_。比η定 基))-Ν-(2-羥基乙基)甲醯胺 0.238 M+H 419.1 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3- η比咬 基))-Ν-(2-曱氧基乙基)曱醯胺 4.222 M+H 432.1 义[2_(二甲基胺基）乙基](6_(2·氰基苯基)-2-{[2_(3-氟苯基) 乙基]胺基}(3_吡啶基))曱醯胺 42.246 M+H 518.1 Ν-{2_[(第三丁氧基)-Ν-曱基羰基胺基]乙基}(6_(2_氰基苯 基)-2_ {[2_(3_就苯基)乙基]胺基} (3_α比ϋ定基))曱酿胺 4.455 M+H 418.1 (6-(2-氰基苯基)-2-{[2-(3-氣苯基）乙基]胺基}(3·。比π定 基))-N-[2_(曱基胺基)乙基]曱酸胺 266 200823188 IC50 算數平均 離子 m/z 化學名稱 N-(3-胺基丙基)(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 0.994 M+H 418.1 基}(3-吡啶基))甲醯胺 (2S)-2- [(6-(2-氰基苯基)-2- {[2·(3 -氟苯基）乙基]胺基} (3 -σ比 0.985 M+H 446.1 啶基))羰基胺基]-Ν-甲基丙醯胺 (2R)-2-[(6_(2_氰基苯基)-2_{[2-(3_氟苯基）乙基]胺基}(3_ 口比 1.273 M+H 446.1 啶基))羰基胺基]-N-曱基丙醯胺 N_{2-[(6_(2-氰基苯基)-2_{[2_(3-1苯基)乙基]胺基}_3·吼啶 0.958 M+H 446.1 基)羰基胺基]乙基}乙醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼淀 1.118 M+H 462.1 基))-N-[2_(曱氧基羰基胺基)乙基]甲醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3·。比唆 0.326 M+H 482.1 基))-N-{2_[(甲基磺醯基)胺基]乙基}曱醯胺 H(6-(2_氰基苯基)-2_{[2·(3-氟苯基)乙基]胺基}·3-吼啶基) 4.792 M+H 461.1 羰基胺基]丙酸乙酯 4-[(6_(2-氰基苯基)-2_{[2_(3-氟苯基)乙基]胺基}_3』比啶基) 0.713 M+H 461.1 羰基胺基]丁酸曱酯 H(6-(2_氰基苯基)-2-{[2-(3·氟苯基)乙基]胺基}(3』比啶基)) 0.34 M+H 446.1 羰基胺基]-N-甲基丙醯胺 4-[(6_(2_氰基苯基)-2-{[2_(3-氟苯基)乙基]胺基}(3-吼啶基)) 2.956 M+H 460.1 羰基胺基]-N-甲基丁醯胺 N-(3_胺甲醯基丙基)(6_(2_氰基苯基)-2-{[2-(3-氟苯基)乙基] 0.185 M+H 446.1 胺基}(3-吡啶基))曱醯胺 4-[(6-(2_氰基苯基)-2-{[2_(3-敗苯基)乙基]胺基定基) 0.627 M+H 447.1 羰基胺基]丁酸 Ν-(2-胺基乙基)(6-(2-氰基苯基)-2-{[2-(3_氟苯基）乙基]胺 2.637 M+H 404.1 基}(3-吼啶基))甲醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-σ比〇定 2.108 M+H 469.1 基))-Ν-[(4_氟苯基)曱基]曱醯胺 (6-(2-氰基苯基)-2-{[2-(3_氟苯基）乙基]胺基}(3-啦啶 0.968 M+H 476.1 基))-N-[(4_氰基苯基)甲基]曱醯胺 N-[(3,4-二氟苯基)曱基](6-(2-氰基苯基)-2-{[2-(3-敦苯基)乙 1.981 M+H 487.1 基]胺基}(3-吡啶基))甲醯胺 267 200823188 IC50 算數平均 離子 m/z 化學名稱 1.02 M+H 448.1 N-((1S)-1-胺曱醯基-2-羥基乙基)(6-(2-氰基苯基)-2_{p-(3-氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 0.318 M+H 419.1 (6-(2-氰基苯基)-2-{[2·(3-氟苯基）乙基]胺基}(3-吨啶 基))-Ν-(3-羥基丙基)甲醯胺 0.396 M+H 433.1 (6-(2-氰基苯基)-2·{[2-(3-氟苯基）乙基]胺基)(3·吼啶 基))-14-(3-曱氧基丙基)曱醯胺 4.177 M+H 463.1 (2S)-2-[(6-(2_氰基苯基)-2_{[2_(3-氟苯基）乙基]胺基}(3-口比 啶基))羰基胺基]-3-羥基丙酸曱酯 0.513 M+H 463.1 (2R)-2-[(6-(2-氣基苯基)-2-{[2-(3·氟苯基）乙基]胺基}(3-°比 啶基))羰基胺基]-3-羥基丙酸曱酯 1.121 M+H 462.1 (2S)-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-口比 啶基))羰基胺基]-3-羥基-N-曱基丙醯胺 0.544 M+H 462.1 (2R)_2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-口比 啶基))羰基胺基]-3-羥基-N-曱基丙醯胺 0.029 M+H 452.1 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基》-N-(2-吼啶基甲基）甲醯胺 24.295 M+H 465.1 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-[(4-曱基苯基)曱基]曱醯胺 0.426 M+H 466.1 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-[(6-曱基(3-啦啶基))曱基]甲醯胺 0.054 M+H 466.1 (6-(2-氣基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-。比ϋ定 基))-Ν-[(6-甲基(2-吼啶基))曱基]曱醯胺 0.291 M+H 466.1 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-(2-(2-u比啶基)乙基)曱醯胺 0.15 M+H 466.1 (6-(2-氰基苯基)-2_{[2-(3·氟苯基）乙基]胺基}(3-吼啶 基))-N-(2-(3-吼啶基)乙基)甲醯胺 0.026 M+H 467.1 N-[(6-胺基(3-。比啶基)）甲基)(6-(2-氰基苯基)-2-{[2-(3-氟苯 基）乙基]胺基}(3-n比啶基))甲醯胺 8.099 M+H 482.1 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 基))-N-[(6-曱氧基(3-吡啶基))曱基]曱醯胺 0.022 M+H 466.1 (6-(2-氣基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3- °比σ定 基))-Ν-[(2-曱基(3-吼啶基))甲基]甲醯胺 268 200823188 IC50 算數平均 離子 m/z 化學名稱 0.022 M+H 467.1 N-[(2-胺基(3_-σ比啶基))甲基](6-(2·氰基苯基)-2-{[2·(3-氟苯 基)乙基j胺基}(3-吼啶基))甲醯胺 0.087 M+H 482.1 (6·(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-。比啶 基))-N-[(2-甲氧基(3』比啶基))甲基]甲醯胺 0.021 M+H 470.1 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-此σ定 基))-Ν-[(1-羥基(2』比啶基))甲基]甲醯胺 0.019 M+H 470.1 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-他啶 基))-N-[(l-羥基(3-吼啶基))甲基]甲醯胺 3.064 M+H 501.1 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-峨啶 基))-N-|&gt;(4-甲基哌畊基)丙基]曱醯胺 0.136 M+H 415.1 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3· °比啶 基))-N-(環丙基曱基)甲醯胺 9.309 M+H 489.1 N-[2-(二甲基胺基）乙基]-2-[(6-(2-氰基苯基)·2·{[2-(3-氟苯 基)乙基]胺基}(3-吡啶基))羰基胺基]乙醯胺 2.07 M+H 462.1 2-[(6_(2·氰基苯基)-2-{[2-(3_氟苯基)乙基]胺基}(3』比啶基)） 羰基胺基]-Ν-(2-羥基乙基)乙醯胺 12.17 M+H 489.1 Ν-(2-胺甲醯基乙基)-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙 基]胺基}(3-吡啶基))羰基胺基]乙醯胺 9.666 M+H 490.1 3-{2·[(6-(2-氰基苯基)-2·{[2·(3-氟苯基)乙基]胺基比啶 基)羰基胺基]乙醯基胺基}丙酸 9.876 M+H 575.1 Ν-{3-[(第三丁氧基）羰基胺基]丙基}-2-[(6-(2-氰基苯 基)-2_{[2_(3·氟苯基)乙基]胺基}(3_吼啶基))羰基胺基]乙醯 胺 12.22 M+H 503.1 义[3-(二甲基胺基)丙基]-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯 基)乙基]胺基}(3_吡啶基))羰基胺基]乙醯胺 5.836 M+H 476.1 2-[(6_(2_氰基苯基)-2-{[2-(3_氟苯基)乙基]胺基}(3-吼啶基)） 羰基胺基]-Ν-(3-羥基丙基)乙醯胺 65.469 M+H 575.1 Ν-{2-[(第三丁氧基)-Ν-甲基羰基胺基]乙基}-2-[(6-(2-氰基 苯基)-2- {[2_(3-氣苯基)乙基]胺基} (3 -吼咬基))幾基胺基]乙 酿胺 11.096 M+H 475.1 2-[(6_(2_氰基苯基)-2-{[2-(3_敗苯基)乙基]胺基}(3·π比啶基)） 罗炭基胺基]-Ν-[2_(曱基胺基)乙基]乙醯胺 269 200823188 IC50 算數平均 離子 m/z 化學名稱 (2S)-3-胺基-2·[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 2.318 M+H 462.1 基}(3-吡啶基))羰基胺基]丙酸甲酯 N-((lS)-2-胺基-1·胺甲醯基乙基）(6-(2-氰基苯 0.816 M+H 447.1 基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 (2S)-3-[(第三丁氧基）羰基胺基]-2-[(6-(2-氰基苯 30.417 M+H 548.1 基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吡啶基))羰基胺基]丙酸 (2S)-3-[(第三丁氧基）羰基胺基]-2-[(6-(2-氰基苯 基)-2·{[2-(3-氟苯基)乙基]胺基}(3』比啶基))羰基胺基]-Ν-甲 43.598 M+H 561.1 基丙醯胺 (28)各胺基-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 3.454 M+H 461.1 基}(3-吡啶基))羰基胺基]-Ν-曱基丙醯胺 (2S)-3-胺基-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 23.721 M+H 475.1 基}(3-吡啶基))羰基胺基]-Ν，Ν-二曱基丙醯胺 (2S)-3-胺基-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 11.072 M+H 448.1 基}(3^比啶基))羰基胺基]丙酸 (2S)-2-胺基各[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 0.619 M+H 462.1 基} (3-吡啶基))羰基胺基]丙酸曱酯 (2S)-2-(乙醯基胺基)-3-[(6-(2-氰基苯基)-2- {[2-(3-氟苯基)乙 1.639 M+H 504.1 基]胺基}(3-吡啶基))羰基胺基]丙酸曱酯 N-((2S)-2-胺基-2-胺甲醯基乙基）(6-(2-氰基苯 0.669 M+H 447.1 基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比啶基))甲醯胺 N-{(1 S)-l-胺甲酷基-2-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基) 2.629 M+H 489.1 乙基]胺基}(3-吡啶基))羰基胺基]乙基}乙醯胺 (2S)-2_胺基-3-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 2.318 M+H 461.1 基}(3-吡啶基))羰基胺基]-Ν-曱基丙醯胺 (2S)-2-胺基-3-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 8.179 M+H 475.1 基}(3-吡啶基))羰基胺基]-N，N-二甲基丙醯胺 (2S)-2-胺基-3-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 9.758 M+H 448.1 基}(3-吡啶基))羰基胺基]丙酸 (2S)-2-(乙酿基胺基)-3-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙 5.554 M+H 503.1 基]胺基}(3-吡啶基》羰基胺基]-N-甲基丙醯胺 2.384 M+H 462.1 (2R)-3-胺基·2-[(6-(2-氰基苯基)·2-{[2-(3-氟苯基）乙基]胺 270 200823188 IC50 算數平均 離子 m/z 化學名稱 基}(3·吡啶基))羰基胺基]丙酸曱酯 · N-((lR)-2-胺基-1-胺甲醯基乙基)(6-(2_氰基苯基)_2_{[2_(3- 0.538 M+H 447.1 氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 (2R)-3-胺基-2-[(6·(2·氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 0.274 M+H 461.1 基}(3-吼啶基))羰基胺基]-Ν-甲基丙醯胺 (2R)-2-胺基-3-[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 2.29 M+H 462.1 基}(3-吡啶基))羰基胺基]丙酸曱酯 N-((2R)-2-胺基-2-胺曱醯基乙基)(6-(2-氰基苯基)-2-{[2-(3- 0.321 M+H 447.1 氟苯基)乙基]胺基}(3-吡啶基))曱醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-ΰ比啶 0.04 M+H 442.1 基))-Ν-(1，3-哼唑-2-基曱基)甲醯胺 Ν-[(6-氰基(3-吼啶基))甲基](2][2-(3-氟苯基)乙基]胺基卜6_ 1.245 M+H 452.1 苯基(3-吡啶基))甲醯胺 Ν-{[6·(胺基甲基)(3-吼啶基)]甲基}(2-{[2-(3-氟苯基)乙基] 0.42 M+H 456.1 胺基}-6-苯基(3-吼啶基))甲醯胺 2-胺基-l-(2-{[2-(3-氟苯基)乙基]胺基}-6-苯基(3-吼啶基))乙 52.451 M+H 352.1 -1-醇 N-{[4-(胺基甲基）(2-吼啶基）]曱基}(6-(2-氰基苯 0.598 M+H 481.1 基)·2_ { [2_(3 -氟苯基)乙基]胺基} (3 - °比σ定基))曱酸胺 Ν-[(5-{[(第三丁氧基）羰基胺基]曱基}(2-啦啶基)）甲 基](6_(2·氰基苯基)-2-{[2_(3_氟苯基)乙基]胺基}(3-吼啶基)) 68.638 M+H 581.1 曱醯胺 Ν-{[5-(胺基甲基）(2-吼啶基）]甲基}(6-(2-氰基苯 0.515 M+H 481.1 基)_2_ {|&gt;(3 -敗苯基)乙基]胺基} (3 -咖定基))曱驢胺 N-{[4-(胺基曱基)(2-吼啶基)]甲基}(2-{[2_(3_氟苯基)乙基] 1.215 M+H 456.1 胺基}-6-苯基(3-吡啶基))曱醯胺 Ν-{[5·(胺基甲基)(2·。比啶基)]曱基}(2-{[2-(3-氟苯基)乙基] 1.061 M+H 456.1 胺基}-6_苯基(3-吼啶基))甲醯胺 (6·(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 0.021 M+H 442.1 基))-Ν-(異坐基曱基)甲驢胺 2-{|&gt;(2-{[2_(3-氟苯基)乙基]胺基}-6_苯基(3-π比啶基))-2-羥 51.566 M+H 409.1 基乙基]胺基}乙醯胺 271 200823188 IC50 算數平均 離子 m/z 化學名稱 15.082 M+H 438.1 乙基-2-{[2-(2-{[2-(3-氟苯基）乙基]胺基}-6-苯基(3」比啶 基))-2-羥基乙基]胺基}乙酸乙酯 19.362 M+H 443.1 1-(2-{[2-(3-氟苯基)乙基]胺基}-6-苯基(3-吼啶基))-2-[(2-吼 啶基曱基)胺基]乙-1-醇 0.416 M+H 432.1 N-(4-胺基丁基)(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-吡啶基))甲醯胺 0.154 M+H 446.1 N-(5-胺基戊基)(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-吡啶基))曱醯胺 1.244 M+H 460.1 N-(6-胺基己基)(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3·吡啶基))曱醯胺 0.032 M+H 495.1 N-{2-[6-(胺基曱基）(2-吼啶基）]乙基}(6-(2-氰基笨 基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 0.252 M+H 470.1 N-{2-[6-(胺基甲基)(2-吼啶基)]乙基}(2-{[2-(3-氟笨基）乙 基]胺基}-6-苯基(3-吡啶基))甲醯胺 0.011 M+H 495.1 N-{[6-(2-胺基乙基）(2-吼啶基）]曱基}(6-(2-氰基笨 基)-2-{[2-(3-氟苯基)乙基]胺基}(3-n比啶基))甲醯胺 0.024 M+H 470.1 N-{[6-(2-胺基乙基)(2-啦啶基)]甲基}(2-{[2-(3-氟苯基）乙 基]胺基}-6-苯基(3-吡啶基))甲醯胺 1.62 M+H 448.1 N-[2-(2-胺基eth氧基）乙基](6-(2-氰基苯基)-2_{[2-(3-氟笨 基)乙基]胺基}(3_吡啶基))曱醯胺 0.037 M+H 482.1 (6-(2-氰基苯基)_2-{[2-(3-氟苯基）乙基]胺基}(3ib σ定 基))-Ν-{[6-(羥基甲基)(2-吼啶基)]甲基}甲醯胺 0.012 M+H 480.1 N-{[3-(胺基曱基)苯基]曱基}(6-(2·氰基苯基)-2-{[2-(3-氟笨 基)乙基]胺基}(3-吡啶基))甲醯胺 0.532 M+H 446.1 2_[(6_(2-氰基苯基)_2·{[2-(3-氟苯基)乙基]胺基}(3』比啶基)) 羰基胺基]-N，N-二甲基乙醯胺 0.444 M+H 447.1 N-{2-[(2-胺基乙基)胺基]乙基}(6-(2_氰基苯基)-2-{[2-(3-氣 苯基)乙基]胺基}(3-。比啶基))甲醯胺 0.014 M+H 472.1 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-。比咬 基))-N-[(2-氧基(3-哌啶基))曱基]曱醯胺 0.015 M+H 44M (6-(2-氰基苯基)_2-{[2-(3-氟苯基）乙基]胺基}(3-。比咬 基))-N十比唑_3_基曱基)曱醯胺 272 200823188 IC50 算數平均 離子 m/z 化學名稱 (6-(2-氰基苯基)-2-{[2-·(3-氟苯基）乙基]胺基}(3_ °比啶 0.032 M+H 455.1 基))-Ν-[(1·曱基叫^坐-3-基)甲基]甲St胺 N-{[4·(胺基甲基)苯基]曱基}(6-(2-氰基苯基)_2-{[2-(3-氟苯 0.277 M+H 480.1 基)乙基]胺基}(3·^比啶基))甲醯胺 N-[(6-{[(2-胺基乙基)胺基]甲基}(2-。比啶基))曱基](6-(2-氰 0.019 M+H 524.1 基苯基)_2·{[2-(3-說苯基)乙基]胺基}(3』比啶基))曱醯胺 6- {[(6-(2-氰基苯基)-2- {[2-(3-氟苯基)乙基]胺基}-3』比啶基) 0.064 M+H 510.1 羰基胺基]曱基}吡啶-2-羧酸曱酯 6-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}-3-吨啶基) 0.047 M+H 496.1 羰基胺基]甲基}吡啶-2-羧酸 6-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}-3_σ比啶基) 0.06 M+H 495.1 羰基胺基]甲基}吡啶-2-曱醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3 j比啶 0.031 M+H 455.1 基))-Ν-[(1-曱基吼嗤-5-基)曱基]曱酿胺 Ν-(1-{2-[(第三丁氧基）羰基胺基]乙基}-2-氧基(3-哌啶 基))(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3^比啶 15.254 M+H 601.1 基))曱醯胺 N-[l-(2-胺基乙基）-2-氧基（3-哌啶基）](6-(2-氰基苯 18.531 M+H 501.1 基)-2_{[2_(3-氟苯基)乙基]胺基}(3』比啶基))甲醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3- %啶 基))·Ν-(2_{2-氧基_3-[(苯基甲氧基)幾基胺基]旅σ定基}乙基) 11.834 M+H 635.1 甲醯胺 Ν-[2-(3-胺基-2-氧基哌啶基）乙基](6-(2-氰基苯 2.95 M+H 501.1 基)-2_{[2-(3_氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 N-{[2-(胺基甲基)苯基]甲基}(6-(2-氰基苯基)-2-{[2-(3-氟苯 0.024 M+H 480.1 基)乙基]胺基}(3·吡啶基：))曱醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3-吼啶 0.032 M+H 458.1 基))-N-[(2_氧基吼咯啶_3·基)曱基]曱醯胺 Ν-[(2· {2-[(第三丁氧基）羰基胺基]乙基}(3-吼啶基)）曱 基](6-(2-氰基苯基)-2_{[2_(3-氟苯基)乙基]胺基}(Ρ比啶基)) 0.47 M+H 595.1 曱醯胺 0.006 M+H 495.1 ν_([2-(2-胺基乙基）(3-吼啶基）]甲基}(6-(2-氰基苯 273 200823188 IC50 算數平均 離子 m/z 化學名稱 基)-2_{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 N-{2-[3-(胺基甲基χ2-吼啶基乙基氰基苯 0.31 M+H 495.1 基)_2-{[2-(3_氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 N-((3S)·2-氧基π比咯啶士基)(6-(2-氰基苯基)-2·{[2-(3-氟苯 3.246 M+H 444.1 基)乙基]胺基}(3』比啶基))曱醯胺 (6-(2-氰基苯基)·2_{[2-(3·氟苯基）乙基]胺基}(3- °比啶 0.059 M+H 516.1 基))-N-{[1-(2-經基乙基)-2-氧基(3-哌啶基)]甲基}甲醯胺 Ν-{[1-(2-胺基乙基)-2-氧基(3-哌啶基)]曱基}(6-(2-氰基苯 0.031 M+H 515.1 基)_2-{|&gt;(3-氟苯基)乙基]胺基}(3-吼淀基))曱醯胺 (6-(2-氰基苯基)_2-{[2_(3-氟苯基）乙基j胺基}(3-吼啶 基))-Ν-{[1-(3-重氮-3-氮雜丙-3-烯基)-2-氧基(3-哌啶基)]曱 0.412 M+H 541.1 基}甲醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3- °比啶 基))-N-{[3-(3-重氮-3-氮雜丙-3-烯基)-2-氧基(3-哌啶基)]甲 15.844 M+H 541.1 基}曱醯胺 N-[((2 R)哌畊·2_基)曱基](6_(2_氰基苯基)_2-{[2-(3-氟苯基) 12.204 M+H 459.1 乙基]胺基}〇吡啶基))甲醯胺 N-[((2R)-1-曱基哌畊-2-基）曱基](6-(2-氰基苯基)-2-{[2-(3- 15.724 M+H 473.1 氟苯基)乙基]胺基)(3』比。定基))曱聽胺 N-[((2R)-1-乙醯基哌畊-2-基）甲基](6-(2-氰基苯 7.437 M+H 501.1 基)-2-{[2_(3_氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 N-{[(2R)-l-(乙基磺醯基）哌π井_2_基]甲基}(6-(2-氰基苯 16.793 M+H 551.1 基)-2·{[2-(3-氟苯基)乙基]胺基}(3-。比啶基))甲醯胺 (2R)-2-{[(6_(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3_吼 11.602 M+H 517.1 啶基))羰基胺基]甲基}哌畊羧酸曱酯 N-[((2S)-1-乙醯基-4-曱基哌畊-2-基）甲基](6-(2-氰基苯 6.789 M+H 515.1 基)-2-{[2_(3-氟苯基)乙基]胺基}(3-。比啶基))甲醯胺 (2S)-2-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比 10.062 M+H 531.1 啶基))羰基胺基]曱基}-4-曱基哌畊羧酸甲酯 N-{[(2R)-l-(2-胺基乙酿基)σ辰π井基]甲基}(6-(2-氰基苯 2.775 M+H 516.1 基)_2· {[2_(3_氟苯基)乙基]胺基} (3』比淀基))曱醯胺 4.893 M+H 530.1 N-{[(2R)-l-(3-胺基丙醯基)哌畊-2-基]甲基}(6-(2-氰基苯 274 200823188 IC50 算數平均 離子 m/z 化學名稱 基)_2_{[2-(3-氟苯基)乙基]胺基比啶基))甲醯胺 N-{[(2R)-l-(4·胺基丁醯基)σ辰牛基]甲基}(6_(2_鼠基苯 5.475 M+H 544.1 基)-2_{[2-(3_氟苯基)乙基]胺基比啶基))甲醯胺 N-{[(2S)-l-(2_胺基乙酿基)曱基略口井_2_基]曱基}(6-(2_策 1.283 M+H 530.1 基苯基)-2-{[2-(3·氟苯基)乙基]胺基}(3』比啶基))曱醯胺 N-{[(2S)-l-(3_胺基丙酸基)斗曱基旅。井-2·基]曱基}(6_(2_氰 2.393 M+H 544.1 基苯基)-2-{〇(3·說苯基)乙基]胺基}(3_0比唆基))甲酸胺 N-{[(2S)-l-(4-胺基丁醯基)冰甲基哌基]甲基}(6_(2_氰 2.322 M+H 558.1 基苯基)-2-{[2-(3·氟苯基)乙基]胺基}(3』比啶基))甲醯胺 N· {[(2S)_4-(2-胺基乙醯基)哌畊-2-基]甲基} (6普氰基苯 8.885 M+H 516.1 基)-2-{[2-(3-就苯基)乙基]胺基}(3』比啶基))曱醯胺 N_ {[(2SH-(3-胺基丙醯基)哌畊-2-基]甲基}(6-0氰基苯 11.197 M+H 530.1 基)_2_{[2-(3-氟苯基)乙基]胺基}(3』比啶基))曱醯胺 N- {[(2S)-4-(4_胺基丁醯基)哌σ井冬基]甲基}(6_(2_氰基苯 12.397 M+H 544.1 基)_2_{[2-(3-敗苯基)乙基]胺基}(3-吼啶基))甲醯胺 N-{[(2SH-(2_胺基乙醯基)小甲基哌畊-2-基]曱基}(6_(2_氰 6.97 M+H 530.1 基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3-叱啶基))甲醯胺 N-{[(2S)-4_(3-胺基丙醢基)小甲基旅11井-2-基]甲基}(6_(2_氰 16.962 M+H 544.1 基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3_吼啶基))甲醯胺 N-{[(2S&gt;4-(4-胺基丁醯基)小甲基哌畊-2_基]甲基}(6_(2_氰 6.717 M+H 558.1 基苯基)-2_{[2_(3-氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 2-(6-(2-氰基苯基)-2- {[2-(3-氟苯基）乙基]胺基)(3- °比啶 13.156 M+H 466.1 基))-N-(3_u比啶基曱基)乙醯胺 N-[((2S)-1，4_二乙醯基娘口井基）甲基](6-(2_ IL基笨 17.175 M+H 543.1 基)-2_{[2_(3-氟苯基)乙基]胺基}(3·。比啶基))曱醯胺 N-[((2S)_4-甲基旅u井_2_基)甲基](6-(2-氰基苯基)-2-{[2_(3~氟 2.92 M+H 473.1 苯基)乙基]胺基}(3-吡啶基))曱醯胺 乂[((2幻氮也2-基）曱基](6-(2-氰基苯基)_2_{|&gt;(3-氟苯基） 0.413 M+H 430.1 乙基]胺基}(3_°比啶基))曱醯胺 (2R)-2_{[(6-(2-氰基苯基)-2-{[2_(3-氟苯基)乙基]胺基}(3』比 0.073 M+H 488.1 啶基))羰基胺基]甲基)氮咀羧酸甲酯 0.248 M+H 437.1 (2-{[2_(3-氟苯基）乙基]胺基}-6-(1-甲基吼唑-冬基)(3_σ比啶 275 200823188 IC50 算數平均 離子 m/z 化學名稱 基))-N-[(2_氧基吡咯啶-3-基)甲基]甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基}·6-吼唑-4-基（3-吼啶 0.18 M+H 423.1 基))-Ν-[(2-氧基吡咯啶-3-基)曱基]甲醯胺 N-{[(2 R)-l-(2-經基乙酿基)σ比略σ定-2-基]甲基}(6-(2-氣基苯 0.116 M+H 502.1 基)-2-{[2-(3-氟苯基)乙基]胺基}(3-扯啶基))曱醯胺 4-((2R)-2-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 0.657 M+H 558.1 基}(3-吡啶基))羰基胺基]甲基}吡咯啶基)-4-氧基丁酸曱酯 N][(2R)-l-(4-羥基丁醯基户比咯啶-2-基]甲基}(6-(2-氰基苯 0.085 M+H 530.1 基)-2-{[2-(3_氟苯基)乙基]胺基)(3』比啶基))甲醯胺 N-{[(2R)-l-(2-氧基乙醯基比咯啶-2-基]曱基}(2-{[2-(3·氟 1.784 M+H 481.1 笨基)乙基]胺基甲基吡唑-4-基)(3-吡啶基))甲醯胺 4-((2R)-2-{[(2-{[2-(3-氟苯基)乙基]胺基}冬(1-甲基吼唑-4- 3.935 M+H 537.1 基)(3-吡啶基))羰基胺基]甲基}吡咯啶基)-4-氧基丁酸曱酯 N-{[(2R)-l-(4-經基丁 醯基)σ比tJ各σ定-2-基]甲基}(2-{[2-(3-1 1.456 M+H 509.1 苯基)乙基]胺基}-6-(1-曱基吡唑-4-基)(3-吼啶基))甲醯胺 N-[((2R)小乙醯基氮吸-2-基）甲基](6-(2-氰基苯 0.043 M+H 472.1 基)-2-{[2·(3_氟苯基)乙基]胺基}(3』比啶基))甲醯胺 N-{[(2R)-1 -(甲基磺醯基）氮咀-2-基]甲基}(6-(2-氰基苯 1.524 M+H 508.1 基)-2-{[2-(3·氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 N-{[(2R)-1 -(2-胺基乙醯基）氮哩-2-基]甲基}(6-(2-氰基苯 0.044 M+H 487.1 基)-2-{ [2-(3-氟苯基)乙基]胺基吡啶基))甲醯胺 N-{[(2R)-l-(3-胺基丙醯基）氮吸-2-基]甲基}(6-(2-氰基苯 0.045 M+H 501.1 基)-2_{[2-(3-氟苯基)乙基]胺基}(3-。比啶基))曱醯胺 N-{[(2R)-1 -(4-胺基丁醯基）氮。旦·2·基]甲基}(6-(2-氰基苯 0.025 M+H 515.1 基K2-{[2_(3·氟苯基)乙基]胺基}(3』比啶基))甲醯胺 N-{[(2R)-l-(2-羥基乙醯基）氮π旦-2-基]甲基}(6-(2·氰基苯 0.04 M+H 488.1 基)-2-{[2_(3_氟苯基)乙基]胺基}(3-。比啶基))甲醯胺 4-((2R)-2-{ [(6-(2-氰基苯基)-2-{[2-(3-氣苯基）乙基]胺 0.519 M+H 544.1 基}(3_°比啶基))幾基胺基]甲基}氮咀基)斗氧基丁酸甲酯 N-{[(2R)-1 -(4-羥基丁醯基）氮。旦-2-基]甲基}(6-(2-氰基苯 0.06 M+H 516.1 基)-2-{[2_(3_氟苯基)乙基]胺基}(3-π比淀基))甲醯胺 2.501 M+H 472.1 N-(氮雜全氫氮呼-2-基曱基)(6-(2-氰基苯基)-2-{[2-(3-氟苯 276 200823188 IC50 算數平均 離子 m/z 化學名稱 0.248 M+H 529.1 基)乙基]胺基}(3_°比啶基))曱醯胺 Ν-{[1-(2-胺基乙醯基)氮雜全氫氮呼-2-基]甲基}(6-(2-氰基 苯基)-2-{[2-(3-氟苯基)乙基]胺基}(34啶基))甲醯胺 0.256 M+H 543.1 N-{[H3-胺基丙醯基)氮雜全氫氮呼-2-基J甲基}(6-(2-氰基 苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 0.383 M+H 557.1 N-{[1 -(4-胺基丁醯基)氮雜全氫氮呼-2-基]甲基}(6·(2-氰基 苯基)-2-{[2_(3-氟苯基)乙基]胺基}(3·吼啶基))甲醯胺 0.104 M+H 615.1 N-[(l-{3-[(第三丁氧基)羰基胺基]丙基}-2-氧基吡咯啶-3· 基)甲基](6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吼 啶基))甲醯胺 0.382 M+H 515.1 Ν-{[1-(3-胺基丙基)-2-氧基吼咯啶-3-基]甲基}(6-(2-氰基苯 基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比啶基))曱醯胺 0.589 M+H 580.1 Ν-[(1-{3·[(第三丁氧基)羰基胺基J丙基}-2-氧基吼咯啶-3-基)甲基](2-{[2-(3-氟苯基)乙基]胺基卜6-吼唑-4-基(3-吼啶 基))甲醯胺 3.125 M+H 480.1 N-{[1 -(3-胺基丙基)-2-氧基吡咯啶-3-基J曱基}(2-{[2-(3-氟 苯基)乙基]胺基}-6-吡唑·4_基(3-吡啶基))甲醯胺 0.699 M+H 594.1 Ν_[(ΗΗ(第三丁氧基)羰基胺基]丙基氧基吡咯啶-3· 基）曱基](2·{[2-(3-氟苯基）乙基]胺基}_6-(1-曱基吡唑-4-基)(3_°比啶基))曱醯胺 5.504 M+H 494.1 Ν-{[1-〇胺基丙基)-2_氧基吼咯啶-3-基]甲基}(2-{[2-(3-氟 本基)乙基]胺基}·6-(1-甲基咖坐基)(3-^比咬基))甲醯胺 3.167 M+H 509.1 (2Κ&gt;2-{[(2·{[2·(3-氟苯基)乙基]胺基}如比唑冬基(3·σ比啶 基))幾基胺基]曱基}°比略咬緩酸第三丁酉旨 1.185 M+H 467.1 N-{[(2R)-l-(2-羥基乙醯基)吡咯啶丨基j曱基}(2_{[2-(3-氟 本基)乙基]胺基}-6-吼嗤-4-基比咬基))曱醯胺 0.095 M+H 486.1 (6&lt;2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3- σ比啶 基))-Ν·[(7_氧雜全氫氣呼·2_基)甲基]甲酿胺 0.687 M+H 451.1 (2-{[2-(3·氟本基）乙基]胺基卜&amp; 0比。坐冰基（3_。比唆 基))-N-[〇氧雜全氫氮呼基)曱基]甲醯胺 0.603 M+H 465.1 (2-{[2_(3-1本基）乙基]胺基}·6_(1_曱基π比嗤·4·基)(3·ϋ比σ定 基))-N-[(7-氧雜全氫氮呼基)曱基]曱醯胺 277 200823188 IC50 算數平均 離子 m/z 化學名稱 N-[(l-{3-[(第三丁氧基)羰基胺基]丙基卜7-氧雜全氫氮呼-2-基)甲基](6-(2·氰基苯基)-2-{|&gt;(3-氟苯基)乙基]胺基}(3-吼 17.15 M+H 643.1 啶基))甲醯胺 Ν-{[1-(3-胺基丙基）-7-氧雜全氫氮呼 (oxoazaperhydroepin)-2-基]曱基}(6-(2-氰基苯基)-2·{[2-(3- 0.273 M+H 543.1 氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 N-{[(2R)-l-(4_羥基丁醯基)吡咯啶基]曱基)(242-(3-氟 0.963 M+H 495.1 苯基)乙基]胺基}-6-°比嗤-4-基(3-咖定基))甲醯胺 N-{[(2R)-l-(2-經基乙醯基)氮α旦_2·基]曱基氟苯 基)乙基]胺基經基曱基)(2·噻吩基)](3-。比啶基))甲醯 2.541 M+H 499.1 胺 N-{[(2R)-l-(2,3·二羥基丙醯基)氮咀-2-基]甲基}(6-(2-氰基 0.051 M+H 518.1 苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3-η比咬基))曱醯胺 (2R)-2- {[(2- {[2-(3 -氟苯基）乙基]胺基} «吐-4-基(3 - °比咬 0.525 M+H 495.1 基))羰基胺基]甲基}氮°旦竣酸第三丁酯 N-[((2R)氮哩冬基)甲基](2-{[2-(3-氟苯基)乙基]胺基}各口比 5.442 M+H 395.1 唑-4-基(3-吡啶基))甲醯胺 N-[2-((2R)-2-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-吼啶基))羰基胺基]曱基}氮。旦基羥基甲 2.482 M+H 617.1 基)-2-氧基乙基](第三丁氧基)曱醯胺 N-{[(2R)-l-((2S)-2-胺基-3-羥基丙醯基）氮哩-2-基]甲 基}(6-(2·氰基苯基)-2-{[2-(3_1苯基)乙基]胺基砂u比啶基)) 0.088 M+H 517.1 曱醯胺 N-[(lR)-2-((m)-2-{[(6-(2·氰基苯基)-2-{[2-(3-氣苯基)乙基] 胺基}(3-°比0定基))幾基胺基]曱基}氮11且基)小(經基甲基)_2_ 0.439 M+H 617.1 氧基乙基](第三丁氧基)曱醯胺 N-{[(2R)-l-((2 R)-2-胺基-3-羥基丙醯基）氮咀-2-基]曱 基}(6-(2-氰基苯基)-2-{[2-(3-氟苯基)乙基]胺基}(3』比啶基)) 0.083 M+H 517.1 曱醯胺 N-[2-((2R)-2-{[(6-(2-氰基苯基)_2-{[2-(3-氣苯基）乙基]胺 基}(3^比啶基))羰基胺基]甲基丨氮。旦基)(1§)小(3-胺基丙 1.349 M+H 644.1 基)-2·氧基乙基](第三丁氧基)甲醯胺 278 200823188 IC50 算數平均 離子 m/z 化學名稱 N-{[(2R)-1-((2S)-2,5-二胺基戊醯基)氮咀-2-基]甲基}(6-(2_ 0.274 M+H 544.1 氰基苯基)-2-{[2_(3_氟苯基)乙基]胺基}(34啶基))甲醯胺 N-{[(2R)-l-(2·羥基乙醯基)氮吸I基]曱基}(2-{[2-(3-氟苯 0.559 M+H 453.1 基)乙基]胺基}-6-吡唑-4-基(3-吡啶基))甲醯胺 N-[((2R)-l-{2-[(第三丁氧基)羰基胺基]乙醯基}氮吸·2·基) 甲基](2-{[2_(3_氟苯基)乙基]胺基}-6-吼唑斗基(3_°比啶基)) 2.989 M+H 552.1 曱醯胺 N-{[(2R)-l-(2-胺基乙醯基)氮。旦-2-基]甲基}(2-{[2-(3-氟苯 0.562 M+H 452.1 基)乙基]胺基}-6-吡唑-4-基(3-吨啶基))曱醯胺 N-[(6-溴(2-吼啶基))甲基](2-{[2-(3-氟苯基)乙基]胺基}-6-口比 0.117 M+H 494.0 唑-4-基(3-吼啶基))甲醯胺 Ν·({6-[(3-胺基丙基)胺基](2-吼啶基)}曱基)(2-{[2-(3-氟苯 0.018 M+H 489.1 基)乙基]胺基}-6-吼唑-4-基(3-吼啶基))甲醯胺 Ν-({6-[(2-胺基乙基)胺基](2-吼啶基)}曱基)(2-{[2·(3-氟苯 0.02 M+H 475.1 基)乙基]胺基}-6·吡唑-4-基(3-吡啶基))曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-吼唑-4-基（3-吼啶 0.039 M+H 476.1 基))-Ν-({6-[(2·羥基乙基)胺基](2-吼啶基)}甲基)曱醯胺 (2R)-2-{[(2-{[2-(3-氟苯基）乙基]胺基}-6-处唑·4-基(3-吼啶 0.245 M+H 453.1 基))幾基胺基]甲基}氮0旦魏酸曱酯 N-[((2R)小{3-[(第三丁氧基)羰基胺基]丙醯基}吡咯啶-2-基)曱基](5·氣·2-{[2-(3_氟苯基)乙基]胺基}_6_(1-曱基。比。圭 0.505 M+H 612.1 _4-基)(3-吡啶基))曱醯胺 N-{[(2R)-l-(3-胺基丙醯基）咕咯啶-2-基]曱基}(5_ 氟_2_{[2-(3_氟苯基)乙基]胺基甲基。比。坐基)(3·υ比。定 0.07 M+H 512.1 基))曱醯胺 N-[((2R)-l-{4-[(第三丁氧基)羰基胺基]丁醯基}吡咯咬冬 基）甲基](5_氟-2-{[2-(3·氟苯基)乙基]胺基}_6_(1-曱基σ比唑 0.483 M+H 626.1 冰基)(3-吡啶基))甲醯胺 N_{[(2R)-l-(4-胺基丁醯基）吼咯啶-2-基]甲基}(孓氟 •2-{[2_(3-氟苯基）乙基]胺基}_6_(1-甲基吼唑斗基)(3』比咬 0.087 M+H 526.1 基))曱醯胺 0.388 M+H 578.1 Ν-[(2-{[(第三丁氧基）羰基胺基]曱基}(3-u比啶基)）曱基] 279 200823188 IC50 算數平均 離子 m/z 化學名稱 (5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-(1-曱基吼唑-4-基)(3- 吡啶基))甲醯胺 N-{[2-(胺基甲基)(3-咕啶基)]甲基}(5-氟-2-{[2-(3-氟苯基) 0.012 M+H 478.1 乙基]胺基}-6-(1-曱基咐吐-4-基)(3-吡啶基))曱醯胺 N-[((2R)-l-{3-[(第三丁氧基)羰基胺基]丙基}-5-氧基吼咯啶 基)曱基](5-氟-2-{[2-(3_氟苯基)乙基]胺基H-(l-甲基吼 0.322 M+H 612.1 唑-4-基)(3-吡啶基))曱醯胺 N-{[(2R)-l-(3-胺基丙基)-5•氧基吼咯啶-2-基]曱基}(5-氟 -2-{[2-(3-氟苯基）乙基]胺基}-6-(1-曱基吼唑-4-基)(3^比啶 0.079 M+H 512.1 基))甲醯胺 N-{[(2R)-1 -(2,3-二羥基丙醯基户比咯啶-2-基]甲基}(5-氟 -2·{[2-(3-氟苯基）乙基]胺基}-6-(1-曱基吼唑-4-基)(3-吼啶 0.143 M+H 529.1 基))曱醯胺 (2- { 〇(3-氟苯基）乙基]胺基卜6-[ 1-(2-羥基乙基）吼唑-4- 0.972 M+H 461.1 基](3-吼啶基))-N-(3-吼啶基曱基)曱醯胺 (2R)-2-{[(6-(2-氰基苯基)-5-氟-2-{[2-(3-氟苯基）乙基]胺 9.038 M+H 562.1 基}(3-吡啶基))羰基胺基]曱基}吡咯啶羧酸第三丁酯 N-[((2R)吼咯啶-2-基）曱基](6-(2-氰基苯基)-5-氟-2-{[2-(3- 0.103 M+H 462.1 氟苯基)乙基]胺基)(3-吼啶基))曱醯胺 N-[(2-{[(第三丁氧基）羰基胺基]甲基}(3-吼啶基)）甲 基](2-{[2-(3-氟苯基）乙基]胺基}-6-[1-(2-羥基乙基)吼唑-4- 14.993 M+H 590.1 基](3-吡啶基))曱醯胺 N-{[2-(胺基曱基)(3-。比啶基)]甲基}(2-{[2-(3-氟苯基)乙基] 0.707 M+H 490.1 胺基}-6-[1-(2-羥基乙基户比唑-4-基](3-吼啶基))甲醯胺 N-[(2-{[(第三丁氧基）羰基胺基]甲基}(3-吼啶基)）曱基] (6-(2-氰基苯基)-5-氟-2-{[2-(3-氟苯基）乙基]胺基}(3-n比啶 5.358 M+H 599.1 基))曱醯胺 N-{[2-(胺基曱基)(3-吼啶基)]曱基}(6-(2-氰基苯基)-5-氟 0.006 M+H 499.1 •2-{[2-(3_氟苯基)乙基]胺基}(3』比啶基))甲醯胺 N-[((2R)· 1 - {2-[(第三丁氧基)羰基胺基]乙醯基”比咯啶-2- 基）甲基](6-(2-氰基苯基)-5-氟-2-{[2-(3-氟苯基）乙基]胺 2.786 M+H 619.1 基}(3-吡啶基))甲醯胺 280 200823188 IC50 算數平均 離子 m/z 化學名稱 0.04 M+H 519.1 N-{[(2R)-l-(2-胺基乙醯基)吡咯啶-2·基]甲基}(6_(2_氰基苯 基&gt;5-氟-2-{[2-(3_l苯基)乙基]胺基}(3』比啶基))甲醯胺 2.771 M+H 633.1 N-[((2R)-l-{3-[(第三丁氧基)羰基胺基]丙醯基}°比咯啶-2· 基）曱基](6-(2-氰基苯基)-5-氟-2-{[2-(3-氟苯基）乙基]胺 基泊-10!^定基))甲酸胺 0.042 M+H 533.1 N-{[(2R)-l-(3-胺基丙醯基吼咯啶-2-基]甲基)(6-(2-氰基苯 基)-5-氟-2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 1.059 M+H 647.1 N-[((2R)-l-{4-[(第三丁氧基)羰基胺基]丁醯基比咯啶-2-基）曱基](6-(2-氰基苯基)-5-氟-2-{[2-(3-氟苯基）乙基]胺 基}(3-吡啶基))甲醯胺 0.038 M+H 547.1 N-{[(2R)-l-(4-胺基丁醯基户比咯啶_2_基]曱基}(6-(2-氰基苯 基)-5-氟-2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))甲醯胺 0.845 M+H 633.1 N-[((2R)-l-{3-[(第三丁氧基)羰基胺基]丙基}-5-氧基吼咯啶 -2-基）甲基](6-(2-鼠基苯基)-5-氟-2-{[2-(3-氟苯基)乙基]胺 基}(3-吡啶基))甲醯胺 0.042 M+H 533.1 N-{[(2R)-l-(3-胺基丙基)·5-氧基吼咯啶-2-基]曱基}(6-(2-氰 基苯基)-5-氟-2-{[2-(3-氟苯基）乙基]胺基)(3-吼啶基))曱醯 胺 0.11 M+H 550.1 N-{[(2R)-l-(2,3-二羥基丙醯基)°比咯啶-2-基]甲基}(6·(2-氰 基苯基)_5_氟-2-Ρ-(3-氟苯基)乙基]胺基}(3』比啶基))曱醯 胺 1.953 M+H 612.1 N-[2-((2R)-2-{[(5-氟-2-{[2-(3-氟苯基)乙基]胺基}-6-(1-甲基 °比唑-4-基)(3-吼啶基))羰基胺基]曱基}°比咯啶基）（1 S)-l-甲 基-2-氧基乙基](第三丁氧基)甲醯胺 0.099 M+H 512.1 N-{[(2R)-l-((2S)-2-胺基丙醯基）η比咯啶_2_基]曱基}(5-氟 -2-{[2-(3-氟苯基）乙基]胺基}-6-(1-曱基吼唑-4-基)(3-°比啶 基))曱醯胺 19.6 M+H 755.4 N-[((2R)-l-{(2S)-2,5-雙[(第三丁氧基)羰基胺基]戊醯基}。比 咯啶基）曱基](5-氟-2-{[2_(3-氟苯基）乙基]胺基}各(1-甲 基吡唑-4-基)(3-吡啶基))甲醯胺 0.078 M+H 555.1 N][(2R)-l-((2s)-2,5-二胺基戊醯基户比咯啶-2-基]甲基}(5-氟_2-{[2_(3-氟苯基)乙基]胺基}_6_(1_甲基吼ϋ坐基)(3-σ比σ定 281 200823188 IC50 算數平均 離子 m/z 化學名稱 基))甲醯胺 N-l&gt;((2R)-2-{[(5-氟-2-{[2-(3-就苯基)乙基]胺基曱基 σ比唑-4-基)(3-吼啶基))羰基胺基]甲基咯啶基）（18)小(羥 1.195 M+H 628.1 基甲基)冬氧基乙基](第三丁氧基)曱醯胺 N-{[(2R)-l-((2S)-2-胺基-3-羥基丙醯基）°比咯啶-2-基]甲 基}(5-鼠-2-{[2·(3-1苯基）乙基]胺基曱基α比ϋ坐_4_ 0.072 M+H 528.1 基)〇吡啶基))甲醯胺 4-((2R)_2_{[(5-氟-2_{[2-(3·氟苯基）乙基]胺基}_6·(1_ 曱基吼 唑斗基)(3-咣啶基》羰基胺基]甲基}吡咯啶基)斗氧基丁酸 0.534 M+H 555.1 曱酯 N_{[(2R)-l-(4-羥基丁醯基）吡咯啶-2-基]曱基}(5-氣-2-{[2-(3-氣苯基)乙基]胺基}-6-(1-甲基11比11坐-4-基)(3-11比咬 0.245 M+H 527.1 基))甲醯胺 N-[(2-{[(第三丁氧基）羰基胺基]甲基}(3-吼啶基)）甲 基](5-氰基-2-{[2-(3-氟苯基）乙基]胺基}-6-(1 -甲基吨唑 0.75 M+H 585.1 -4-基)(3-吡啶基))甲醯胺 N-{[2-(胺基甲基)(3·-比啶基)]甲基}(5-氰基-2-{[2-(3-氟苯 0.05 M+H 485.1 基)乙基]胺基}-6-(1-曱基吡唑冰基)(3-吡啶基))甲醯胺 N-[3-((5R)-5-{[(5-氰基-2-{[2-(3-氟苯基)乙基]胺基}-6-(1-曱 基吼唑-4-基)(3-咕啶基))羰基胺基]曱基}-2-氧基吼咯啶基） 1.15 M+H 619.1 丙基](第三丁氧基)曱醯胺 N_{[(2R)-l-(3-胺基丙基)-5-氧基啦咯啶-2-基]曱基}(5-氰基 -2-{[2-(3-氟苯基）乙基]胺基卜6-(1-甲基吼唑-4-基)(3-ΰ比啶 0.31 M+H 519.1 基))甲醯胺 C2R)-2-{[(5-氰基_2-{[2-(3_氟苯基)乙基]胺基}-6_(1-曱基°比 2.518 M+H 548.1 唑斗基)(3-吡啶基))羰基胺基]曱基}吡咯啶羧酸第三丁酯 N-[((2R)%b咯啶-2-基）甲基](5_氰基-2-{[2-(3-氟苯基）乙基] 0.281 M+H 448.1 胺基}-6-(1-甲基吡唑-4-基)(3-吡啶基))甲醯胺 N-[((2R)-1 - {4-[(第三丁氧基)羰基胺基j 丁醯基}吡咯啶-2- 基)曱基](5-氰基-2-{[2-(3_氟苯基）乙基]胺基}-6·(1-曱基。比 1.613 M+H 633.2 唑-4-基)(3-吡啶基))曱醯胺 0.211 M+H 533.2 N-{[(2R)-l-(4-胺基丁醯基）σ比咯啶-2-基]甲基}(5-氰基 282 200823188 IC50 算數平均 離子 m/z 化學名稱 -2 - {[2-(3-氟苯基）乙基]胺基}·6-(1-曱基吼唑-4-基)(3-吼啶 基))曱醯胺 Ν-[(2·{[(第三丁氧基）羰基胺基]甲基}(3-吼啶基)）甲 基](2-{[2-(3-氟苯基）乙基]胺基}-5-曱基-6-(1-甲基吼唑-4- 1.122 M+H 574.1 基)(3-吡啶基))甲醯胺 Ν·{[2_(胺基甲基)(3』比啶基)J曱基}(2·{[2-(3-氟苯基)乙基] 0.129 M+H 474.1 胺基}-5-甲基-6-(1-曱基吡唑-4-基)(3-吡啶基))曱醯胺 N-[((2R)-l-{3-[(第三丁氧基)羰基胺基]丙基}-5-氧基吼咯啶 -2-基)甲基](2-{[2-(3_氟苯基)乙基]胺基}-5-曱基-6-(1-甲基 1.461 M+H 608.2 吡唑-4-基)(3-吡啶基))曱醯胺 Ν·{[(2 R)-l-(3-胺基丙基）-5-氧基吼咯啶-2-基]甲 基}(2-{[2-(3_氟苯基）乙基]胺基}-5-曱基-6-(1-甲基吼唑-4- 0.577 M+H 508.2 基)(3-吡啶基))甲醯胺 (2R)-2-{[(2-{[2-(3-氟苯基)乙基]胺基}-5-曱基-6-(1-曱基吼 3.702 M+H 537.1 唑-4-基)(3-吡啶基))羰基胺基]曱基}吡咯啶羧酸第三丁酯 N-[((2R)吼咯啶-2-基)曱基](2-{[2-(3-氟苯基)乙基j胺基}-5- 0.901 M+H 437.1 甲基-6-(1-曱基0比〇坐-4·基)(3-σ比咬基))曱酿胺 N-[((2R)-l-{4-[(第三丁氧基)羰基胺基]丁醯基}吡咯啶-2-基）甲基](2-{[2-(3-氟苯基)乙基]胺基}-5-甲基-6-(1-曱基吼 2.265 M+H 622.3 唑-4-基)(3-吡啶基))曱醯胺 N-{[(2R)-l-(4-胺基丁醯基)吼咯啶-2·基]曱基}(2-{[2-(3-氟 苯基)乙基]胺基}-5-曱基-6-0曱基吼唑-4-基)(3-吼啶基))甲 0.381 M+H 522.2 醯胺 (2R)-2-{[(5-氰基-2·{[2·(3-氟苯基)乙基]胺基}-6-吼唑-4-基 6.407 M+H 534.1 (3-吡啶基))羰基胺基]甲基}吡咯啶羧酸第三丁酯 N-[((2R)。比咯啶I基）曱基](5_氰基氟苯基)乙基] 0.624 M+H 434.1 胺基}-6-吡唑-4-基(3·吡啶基))甲醯胺 N-[((2R)-l-{4_[(第三丁氧基)羰基胺基]丁醯基},比咯啶冬 基)曱基Ο氰基_2-{[2-(3-氟苯基)乙基]胺基}-6-。比唑·4·基(3- 3.421 M+H 619.2 吡啶基))甲醯胺 N-{[(2R)-l-(4·胺基丁醯基）吼咯啶-2-基曱基}(5-氰基 0.359 M+H 519.2 -2-{[2-(3·氟苯基）乙基]胺基吼唑冬基(3-吼啶基))曱醯 283 200823188 IC50 算數平均離子 m/z 化學名稱 - -N-[((2R)-l-{3-[(第三丁氧基)羰基胺基]丙基}-5-氧基吡咯啶 3.506 M+H 605.1 -2-基)甲基](5_氰基-2-{[2-(3_氟苯基)乙基]胺基}-6』比唑-4-基(3-吼啶基))甲醯胺 0.735 M+H 505.1 N-{[(2R)-l-(3-胺基丙基)·5-氧基吼咯啶-2-基J甲基}(5-氰基 -2-{[2-(3-氟苯基）乙基]胺基}-6-η比唑-4-基(3-吼啶基))甲醯 胺 1.003 M+H 571.1 Ν-[(2-{[(第三丁氧基）羰基胺基]曱基}(3-吼啶基)）甲 基](5-氰基苯基)乙基]胺基]^-。比唾冬基(3-σ比淀 基))甲醯胺 0.058 M+H 471.1 Ν-{[2-(胺基曱基)(3-。比啶基)]曱基}(5-氰基-2·{[2·(3·氟苯 基)乙基]胺基}-6-吡唑-4-基(3-吡啶基))曱醯胺 4.252 M+H 595.2 Ν-[(2-{[(第三丁氧基）羰基胺基]曱基}(3·-比啶基)）曱基 j(6-(2_亂基苯基)-2-{[2-(3_氟苯基）乙基]胺基}·5-曱基(3-口比 啶基))甲醯胺 0.158 M+H 495.2 Ν-{[2-(胺基甲基）(3-吼咬基）]曱基}(6-(2-氰基苯 基)_2_ {[2_(3_氟苯基)乙基]胺基}_5·曱基(3_吡啶基))甲醯胺 5.372 M+H 629.2 N-[3-((5R)-5-{[(6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺 基}-5-甲基(3-吡啶基))羰基胺基]曱基}·2_氧基吡咯啶基)丙 基](第三丁氧基)甲醯胺 1.226 M+H 529.1 N_{[(2R)-l-(3-胺基丙基)_5_氧基吡咯啶-；2-基J甲基}(6_(2-氰 基苯基)-2-{[2·〇1苯基)乙基]胺基}-5-甲基(3-σ比咬基))曱 醯胺 15.521 M+H 389.0 5_氯-2-{[2-(3_氟苯基)乙基]胺基卜6_(1_曱基^比峻冰基户比咬 _3-羧酸甲酯 0.414 M+H 594.1 Ν-[(2_{[(第二丁氧基博基胺基]曱基}〇°比咬基))曱基](5_ 氣-2_{[2_(3-氟苯基)乙基]胺基曱基吡唑_4_基)…比咬 基))甲醯胺 0.03 M+H 494.0 Ν-{[2·(胺基甲基)(3』比啶基)]曱基}(5·氯_2_{[2-(3-氟苯基) 乙基]胺基}-6-(1-甲基吼唑冰基)(3』比啶基))甲醯胺 0.443 M+H 628.2 N-[((2 R)-l-{3-[(第三丁氧基)羰基胺基]丙基氧基呲咯 咬基)曱基](5_氯_2_{[2_(3-氟苯基)乙基]胺基}各(1-甲基 200823188 IC50 算數平均 離子 m/z 化學名稱 0.16 M+H 528.1 吡唑-4-基)(3-吡啶基))甲醯胺 N-{[(2R)-l-(3-胺基丙基)-5·氧基吡咯啶-2-基]曱基}(5-氯 2-{[2-(3-氟苯基）乙基]胺基}-6-(1-曱基啦唑斗基)(3-咐啶 基))甲醯胺 1.601 M+H 557.1 (2R)-2-{[(5—氣-2·{[2·(3-氟苯基）乙基]胺基}·6_(1-曱基σ比唑 -4-基)(3-σ比咬基))幾基胺基]曱基}σ比洛咬羧酸第三丁酯 0.167 M+H 457.1 N-[((m户比咯啶基）曱基](5_氯-2-{[2-(3_氣苯基)乙基]胺 基曱基啦唑-4-基)(3-吼啶基))曱醯胺 0.683 M+H 642.2 N-[((2R)-l-{4_[(第三丁氧基)羰基胺基]丁醯基}吡咯啶冬 基)甲基](5_氯-2_{[2·(3· 1苯基)乙基]胺基}-6_(1-曱基σ比嗤 -4-基)(3-σ比咬基))曱醯胺 0.047 M+H 542.1 Ν·{[(2Κ&gt;1-(4-胺基丁醯基）吼咯啶-2-基]曱基}(5-氯 { 〇(3 -氟苯基）乙基]胺基} _6_( 1 -曱基吼唾-4-基)(3 -σ比口定 基))甲醯胺 4.501 M+H 515.2 Ν-{3-[(第三丁氧基)羰基胺基]丙基}(5-氟-2-{[2-(3·敗苯基) 乙基]胺基}·6_(1-甲基°比唾冬基)(3-°比咬基))曱醯胺 3.957 M+H 415.1 Ν·(3-胺基丙基)(5_說-2-{[2_(3_氟苯基）乙基]胺基&gt;6_(1-曱 基吡唑-4-基)(3-吡啶基))曱醯胺 0.1 M+H 458.1 (2R)-H(5-氟-2-{[2-(3-氟苯基)乙基]胺基}-6-(1-曱基。比唑冰 基)(3-吡啶基))羰基胺基]-2-甲基丙酸曱酯 3.841 M+H 444.1 (2R)-H(5_氟_2-{[2-(3_氟苯基)乙基]胺基曱基σ比唑冬 基)(3·吡啶基))羰基胺基]-2-甲基丙酸 0.768 M+H 572.2 2-[(第三丁氧基)羰基胺基]_Ν]3_[(5_氟·2·{[2_(3_氟苯基)乙 基]胺基}-6_(1-曱基吡唑冰基)(3•吡啶基))叛基胺基]丙基} 乙醯胺 2.494 M+H 472.1 2-胺基-Ν-{3-[(5-氟-2-{[2-(3-氟苯基)乙基]胺基}-6-(1-曱基 °比唾冰基)(3』比啶基))幾基胺基]丙基}乙醯胺 2.617 M+H 457.1 N-{H(5_H{[2-(3-氟苯基）乙基]胺基}-6-(1-曱基吼唑-4-基)冬吼啶基)羰基胺基]丙基}乙醯胺 0.05 M+H 430.1 N-((2R)_3-經基冬曱基丙基)(5·氟么{[2·(3·氟苯基)乙基]胺 基}_6-〇甲基吡唑冰基)〇吡啶基))甲醯胺 0.089 M+H 443.1 N-((2R)_2_胺曱醯基丙基)(5H{[2_(3·氟苯基）乙基]胺 285 200823188 IC50 算數平均 離子 m/z 化學名稱 - 基}-6-(1-曱基吡唑-4-基)(3-吡啶基))甲醯胺 0.13 M+H 457.1 (2R)_3_[(5·氟-2-{[2-(3-氟苯基)乙基]胺基}-6-(1·曱基吼唑1 基)(3·吡啶基))羰基胺基]-2-曱基-N-甲基丙醯胺 0.024 M+H 424.1 (5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-吼唑-4-基(3- °比啶 基))-N-(吡唑-3-基甲基)曱醯胺 0.02 M+H 438.1 (5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-(1-甲基吼唑冬基)(3-吡啶基))-N-(吡唑-3-基曱基)甲醯胺 0.118 M+H 455.2 N-((2R)-4-重氮-2-甲基-4-氮雜丁-4-烯基)(5-氟-2-{[2-(3-氟 苯基)乙基]胺基}-6-(1-甲基吡唑-4-基)(3-吡啶基))甲醯胺 10.538 M+H 412.1 5-氟-2-{[2-(3-氟苯基)乙基]胺基}-6-(1-甲基吼唑-4-基)(3』比 啶基）3-甲基氮咀基酮 1.05 M+H 429.2 队((28)-3-胺基-2_甲基丙基)(5-氣-2-{[2-(3-氟苯基)乙基]胺 基}-6-(1-甲基吡唑-4-基)(3-吡啶基))曱醯胺 0.373 M+H 586.5 N-{(2R)-3-[(5·氣-2_{[2-(3-氟苯基）乙基]胺基}-6-(1-甲基口比 唑-4-基)(3^比啶基))羰基胺基]-2-曱基丙基}-2-[(第三丁氧 基)羰基胺基]乙醯胺 0.152 M+H 486.2 N-{(2R)-3-[(5-氟-2_{[&gt;(3-氟苯基）乙基]胺基}-6-(1-甲基口比 唑斗基)(3-吼啶基))羰基胺基]-2-曱基丙基}-2-胺基乙醯胺 0.105 M+H 487.1 N-{(2R)-3-[(5-氟 _2-{[2_(3-氟苯基)乙基]胺基}-6-(1-甲基口 比 唑-4-基)(3-吼啶基))羰基胺基]-2-甲基丙基}-2·羥基乙醯胺 0.525 M+H 527.1 (2R)-2-{[(5-氟_2-{[2-(3-氟苯基）乙基]胺基曱基σ比唑 基)(3-°比咬基))羰基胺基]曱基}氮°旦魏酸第三丁商旨 1.582 M+H 427.1 N-[((2R)氮口旦-2-基）曱基](5-氟-2- {[2-(3-氟苯基）乙基]胺 基}-6-(1-甲基吼唑-4-基)(3』比啶基))曱醯胺 0.436 M+H 584.3 N-[((2R)-l-{2-[(第三丁氧基)羰基胺基]乙醯基}氮吸-2-基) 曱基](5·氟-2-{[2_(3-氟苯基）乙基]胺基}-6-(1-曱基吼唑冬 基)(3-吡啶基))甲醯胺 0.05 M+H 484.1 n_{[(2R)小(2-胺基乙醯基）氮°旦-2-基]曱基}(5-氣-2-{[2-(3-氟苯基)乙基]胺基}各(1-曱基吼唑斗基)(3-u比啶基))曱醯胺 0.122 M+H 612.3 N-[((2R)-l-{4_[(第三丁氧基)羰基胺基]丁醯基}氮。旦基) 曱基J(5-氟-2-{[2_(3-氟苯基）乙基]胺基}-6·(1-甲基吡唑斗 基)(3-u比啶基))甲醯胺 286 200823188 IC50 算數平均 離子 m/z 化學名稱 N-{[(2R)-l-(4:胺基丁 醯基)氮祖·2-基]曱基}(5_ 氟:2_{[2-(3- 0.04 M+H 512.1 氟苯基)乙基]胺基}-6_(1-甲基吼τι坐-4-基)(3』比淀基))甲醯胺 N-{[(m)-i-(2-羥基乙醯基)氮。且_2_基]甲基}(5-氟_2_{[2-(3- 0.047 M+H 485.2 氟苯基)乙基]胺基}-6·(1-甲基。比。坐_4_基)(3_υ比π定基))甲醯胺 (2S)-3-[(5_氟-2_ {[2_(3_氣苯基)乙基]胺基卜6-(1 -曱基°比峻-4_ 0.141 M+H 458.1 基)(3-咕啶基))羰基胺基；1-2-甲基丙酸曱酯 N-((2S)_3-hyd r氧基曱基丙基χ5_氟-2-{[2-(3-氟苯基)乙 0.09 M+H 430.1 基]胺基曱基吡唑-4-基)(3-吡啶基))甲醯胺 N-((2R)·3-羥基_2_甲基丙基)(5-就_2- {[2-(3-氟苯基)乙基]胺 0.059 M+H 416.1 基}-6-0比唾-4-基(3-0比咬基))曱酿胺 (2R)-3-[(5_氟-2·{[2-(3·氟苯基)乙基]胺基比唆冬基(3_ 口比 0.073 M+H 444.1 啶基))羰基胺基]-2-甲基丙酸甲酯 (2R)-3_[(6-(2_氰基苯基)-2-{[2-(3-敗苯基）乙基]胺基}(3_吼 0.186 M+H 461.1 σ定基))幾基胺基]-2-曱基丙酸曱酉旨 N-((2R)-3-羥基-2-曱基丙基)(6-(2-氰基苯基)-2-{[2-(3-氟苯 0.061 M+H 433.2 基)乙基]胺基}(3-吼啶基))曱醯胺 N-[(2,2-二甲基(1，3-二噁烷-5-基))甲基](5-氟-2-{[2-(3-氟苯 2.226 M+H 486.2 基)乙基]胺基曱基σ比嗅-4-基)(3-σΛσ定基))甲酸胺 (5-氟-2-{[2-(3-氟苯基）乙基]胺基}-6-(1-甲基吼唑斗基)(3- 0.134 M+H 446.2 σ比咬基))-N-[3-|^i基-2-(¾基曱基)丙基]甲驢胺 N-[(2,2-二甲基(I，3-二噁烷 I 基))曱基](5-氟 _2-{[2_(3-氟苯 0.927 M+H 472.2 基)乙基]胺基}-6-吼唑-4·基(3 ^比啶基))曱醯胺 (5-氟-2-{[2-(3-氟苯基）乙基]胺基卜6-啦唑-4-基(3-吼啶 0.215 M+H 432.2 基))-N-[3_羥基_2_(羥基甲基)丙基]曱醯胺 N-[(2,2-二甲基（1，3-二噁烷-5-基)）甲基](6-(2-氰基苯 1.023 M+H 489.2 基)-2-{[2-(3-氟苯基)乙基]胺基}(3-吼啶基))曱醯胺 (6-(2-氰基苯基)-2-{[2-(3-氟苯基）乙基]胺基}(3- η比啶 0.209 M+H 449.2 基))-Ν-[3-羥基-2-(羥基曱基)丙基]曱醯胺 (2R)-2_{[(5_氟_2-{[2-(3-氟苯基）乙基]胺基}-6-(卜曱基u比唑 0.117 M+H 472.1 -4-基)(3』比啶基))羰基胺基]甲基} 丁酸甲酯 义((21〇-2-乙基-3-羥基丙基)(5-氟-2-{[2-(3-氟苯基)乙基]胺 0.039 M+H 444.1 基}-6-(1-甲基吼唑-4-基)(3』比啶基))曱醯胺 287 200823188 IC50 算數平均 離子 m/z 化學名稱 0.117 M+H 458.1 (2R)-2-{[(5·氟-2:{[2_(3-氟苯基)乙基]胺基丨各吼唾冰基(3_ 吡啶基))羰基胺基]曱基} 丁酸甲酯 0.052 M+H 430.1 N-((2R)_2-乙基羥基丙基)(5-氟冬{[2-(3·氟苯基)乙基]胺 基}-6-吡唑-4·基(3-吼啶基))甲醯胺 90.761 M+H 559.2 (2R)-2_[(第三丁氧基)羰基胺基]-3·[(5-氣-2_{[2_(3_氟苯基) 乙基]胺基卜6_(1·甲基吡唑斗基)(3-吡啶基))幾基胺基]丙酸 曱酯 0.568 M+H 459.2 (2R)_2_胺基-3-[(5_氣-2· {[2_(3_氟苯基)乙基]胺基}·6_(1_曱基 吡唑斗基)(3_吡啶基))羰基胺基]丙酸甲酯 25.925 M+H 531.2 N-((lR)-l-{[(5·氟-；2-{[2-(3-氟苯基)乙基]胺基}·6_(ι·甲基外匕 唑斗基)(3·α比啶基))幾基胺基]曱基}_2_經基乙基)(第三丁氧 基)曱醯胺 1.258 M+H 431.2 N-((2R)-：2-胺基·3_經基丙基)(5·說-；2- {[2_(3_氟苯基)乙基]胺 基}-6-(1-曱基0比〇坐-4-基)(3-σ比咬基))甲酿胺 57.166 M+H 517.2 Ν-(( 1 R)-1 - {[(5_ 氟 _2_ {[2_(3 -氟苯基)乙基]胺基} 坐-4-基 (3-吡啶基))羰基胺基]甲基}-2-羥基乙基)(第三丁氧基)曱醯 胺 1.825 M+H 417.2 N-((2R)_2_胺基_3·輕基丙基)(5_氟·2-{[2_(3_氟苯基)乙基]胺 基}-6-吡唑-4-基(3-吼啶基))甲醯胺 0.307 M+H 432.1 Ν-(2,3-二經基丙基)(5-氟-2-{[2-(3-氟苯基)乙基]胺基}_6_(μ 甲基吡唑-4-基)(3-吡啶基))甲醯胺 0.448 M+H 418.1 N-(2，3-二經基丙基）（5-氟-2-{[2-(3-氟苯基)乙基]胺基}_6一 吡唑-4-基(3-吡啶基))甲醯胺 86.027 M+H 336.1 (2R)-3-{[2-胺基-5-|L-6-(l-曱基°比。坐-4-基)(3-π比σ定基)]幾基 胺基}-2-甲基丙酸曱酯 0.141 M+H 513.1 N-{[(2R)-l-(2*·經基甲基丙醒基）氮。旦_2—基]曱基}(5·氟 -2-{[2_(3-氟苯基）乙基]胺基}-6_(1-曱基。比唑_4·基)(3』比咬 基))甲醯胺 0.289 M+H 513.1 (2R)-2-{[(5-氟-2-{[2-(3-氟苯基）乙基]胺基}各,比唑斗基 (3-〇比咬基))魏基胺基]曱基}氮°旦叛酸第三丁西旨 0.046 M+H 471.1 N_{[(2R)-l-(2-^ 基乙酸基)氮口旦-2-基]曱基}(5_ 氣 _2_{[2-(3_ 氟苯基)乙基]胺基}-6-°比°坐冰基(3』比咬基))曱酸胺 200823188 IC50 算數平均 離子 m/z 化學名稱 N-[((2R)氮。旦-2-基）甲基](5-i-2-{[2-(3-氟苯基）乙基]胺 0.466 M+H 413.1 基}-6-|7比°坐-4-基(3-0比°定基))甲醯胺 N-{[6-(胺基曱基）（2-咐啶基)]甲基}(2-{[2-(3-氟苯基)乙基] 0.019 M+H 456.1 胺基)-6-苯基(3·°比啶基))曱醯胺 N-{[6-(胺基甲基）(2-ϋ比啶基）]甲基}(6-(2-氰基苯 0.009 M+H 481.1 基)-2-([2-(3-氟苯基)乙基]胺基}(3-0比啶基))曱醯胺 N-(胺甲醯基甲基)(6-(2-氰基苯基)-2-{[2_(3-氟苯基)乙基]胺 0.104 M+H 418.1 基}(3-吡啶基))甲醯胺 N-(2-胺甲醯基乙基)(6-(2-氰基苯基)-2- {[2-(3-氟苯基)乙基] 0.099 M+H 432.1 胺基}(3-吡啶基))甲醯胺 2-[(6-(2-氰基苯基)-2-{[2-(3_氟苯基)乙基]胺基}(3-ϋ比咬基)) 0.102 M+H 432.1 羰基胺基]-Ν-甲基乙醯胺 N-((3S)-2-氧基(3-哌啶基))(6-(2·氰基苯基)-2-{[2-(3-5-氟苯 5.614 M+H 458.1 基)乙基]胺基}(3-10比唆基))曱酉胜胺 實例14 :Ion M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H m/z Chemical Name • Oxazole (3-pyridyl))carbonylamino]-isopropyl}-4-[(tatabutoxy)carbonylamino]butanamine N-{(lR)_2-[(5-fluoro) -2·{[2-(3-fluorophenyl)ethyl]amino}-6-(1-methyl-port ratio 500. 3 oxazolyl)(3-acridinyl))carbonylamino]-isopropyl}-4-aminobutyric acid N-{(2R)-2-[(2-methoxyethyl)amine (i-propyl}(5-fluoro-2-{[2-(3-fluorophenyl473·1yl)ethyl]amino}-6-(1-methylpyrazol) (3-pyridyl) )) indoleamine N-{(2R)-2-[(tatabutoxy)carbonylamino]propyl}(5-fluoro-2-{[2-(3-fluoro5〇1 · 1 benzene) Ethyl]amino}amino}pyrazolyl (3-pyridyl)) amidoxime ((211)-2-aminopropyl) (5-fluoro-2-{|&gt;(3- Fluorophenyl)ethyl]amino}-6- 401. 1 pyrazol-4-yl(3-pyridyl))decylamine N-{(lR)_2-[(5-fluoro-2_{[2-(3)fluorophenyl)ethyl]aminomethyl吼457·1 oxazolidine)(3-pyridyl))carbonylamino]-isopropyl}acetamidamine N-{(2R)-2_[(fluorenylsulfonyl)amino]propyl}( 5·Fluoro-2_{[2-(3-fluorophenyl) 493 · 1 ethyl]aminomethylpyrazol-4-yl)(3-pyridyl))decylamine N-{(lR)- 2-[(5-fluoro-2-{[2_(3-fluorophenyl)ethyl]amino}_6-indazole ice-based 459· 1 (3-acridinyl))carbonylamino]-isopropyl Kebu 2-aminoacetamide (5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-oxazol-4-yl (3- η-pyridyl 43 5 · 1 base))-Ν-(2-pyridylfluorenyl)guanamine N-{(2R)-2-[(2-hydroxyethyl)amino]propyl} (5_ gas ip#-fluorine Phenyl) 459·2 ethyl]amino}-6-(1-mercaptopyrazole yl) (3-pyridyl))carinamide N-{(2R)_2-[(aminopurinyl) Amino]propyl}(5_fluoroip#-fluorobenzene472·1yl)ethyl]aminobib 6_(1_methylpyrazole glacial guanidine 3-pyridyl) decylamine N-{(1) R)-2-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1·methylpyran-4-yl)(3-u ratio Pyridyl"carbonylamino]-isopropylbenzene 2_(didecylamino)ethyl 500. 2 indoleamine N-{(1 R)-2-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-mercaptopyran 4-yl)(3_acridinyl))carbonylamino]-isopropyl}(2S)-2-[(third butoxy 602. 2-yl)aminoamino]-3-ylpropionamine N-{(1 R)-2-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino) Methylpyran-4-yl)(3-pyridyl))carbonylamino]-isopropyl}(2S)-2-amino-3-hydroxy 502. 2 propylamine 500. 2 N-{(lR)-2-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-methylpyridinium 252 200823188 IC50 arithmetic mean ion m/z chemical name -4--4-yl group)) benzylamino]-isopropyl}-2-amino-2-mercaptopropanol N-((lR)-l-{[(5- Fluor-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-indolyl portyrazole-4-yl)(3-pyridyl))carbonylamino]indolyl }propyl)-2-[(t-butoxy) 3. 04 M+H 586. 3 carbonylamino]acetamide N-((lR)-l-{[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1·A Base ratio is 0. 131 M+H 486. 2 oxazol-4-yl)(3-acridinyl))carbonylamino]mercapto}propyl)-2-aminoacetamide N-((1R)-1_{[(5-fluoro-2- {[2-(3.Fluorophenyl)ethyl]amino}-6-indazole-based (3-acridinyl)carbonylamino]]indenyl}propyl)_2-[(third butoxide) Carboxylamine 323 M+H 572. 3-yl]acetamide N-((lR)-l-{[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6"-pyrazolyl group 16 M+H 472. 2(3-Pyridinyl))carbonylamino]methyl}propyl)-2-aminoacetamide N-{(lR)-2-[(5-fluoro-2-{[2-(3- Fluorophenyl)ethyl]amino}-6-(1-methyloxime. 131 M+H 486. 2 oxazol-4-yl)(3-acridinyl))carbonylamino]-isopropyl}(2S)-2-aminopropionamine N-((2R)-3-hydroxy-2-methyl Butyl) (5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amine 0. 283 M+H 444. 2 base}-6-(1-methylindol-4-yl)(3-n-pyrylyl))carbenamide-{[2·(aminomethyl)(3-acridinyl)] Methyl}(6-(2-cyanobenzene). 006 M+H 481. 1 yl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3′′pyridinyl))carbenamide·{[2_(aminomethyl)(3_.pyridinium) Base)]methyl}(2][2-(3.fluorophenyl)ethyl]. 024 M+H 446. 3 Amino}-6-pyrazol-4-yl(3-pyridyl))carbenamide (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl) Amino} (3-picidine 0. 024 M+H 452. 1 base))-N-(3-acridinylmethyl)methanoamine {6-phenyl-2-[(2-(2-acridinyl)ethyl)amino](3-acridinyl) )}-N-(3-Acridine 0. 512 M+H 410. 1 mercapto) guanamine {6-(3,4-difluorophenyl)-2-[(2-(2-acridinyl)ethyl)amino](3-σ-pyridyl 1. 206 M+H 446. 1 base)}-Ν-(3-acridinylfluorenyl) decylamine {6-(4-fluorophenyl)-2_[(2-(2-acridinyl)ethyl)amino](3) - ° than pyridine 1. 045 M+H 428. 2 ))}-Ν-(3-acridinyl fluorenyl)methanoamine {6-(4-carbophenyl)-2-[(2-(2-)pyridine)ethyl) ] (3- ° ratio σ疋0. 629 M+H 444. 1 base)}·Ν-(3-acridinylfluorenyl) decylamine {6-(4-methylphenyl)-2-[(2·(2-acridinyl)ethyl)amino) (3-σ ratio pyridine 0. 677 M+H 424. 2 base)}·Ν-(3-acridinylfluorenyl) guanamine 253 200823188 IC50 arithmetic mean ion m/z chemical name 1. 935 M+H 435. 1 {6-(4-cyanophenyl)2-[(2-(2-u-pyridyl)ethyl)amino](3-acridinyl)}-N-(3′′pyridyl) Mercapto) 063 M+H 440. 1 {6-(4-methoxyphenyl)-2-[(2·(2-吼)ethyl)amino](3- ° 唆 ))}-Ν-(3-ΰ ratio Pyridylcarbyl)carbamamine 2. 43 M+H 440. 2 {6-[4-(Hydroxymethyl)phenyl]-2-[(2-(2-acridinyl)ethyl)amino](34 acridine)}-Ν-(3′′ pyridine Carbenylamine 375 M+H 478. 1 {6-(3,4-Dichlorophenyl)·2_[(2-(2-° ratio σ-decyl)ethyl)amino]] (3_° ratio σ base)}-Ν-(3-pyridyl group Mercapto) 285 M+H 478. 1 {2-[(2-(2-Acridine)ethyl)amino]-6-[4-(trifluoromethyl)phenyl](34 acridine)}-Ν-(3) ratio Acridine-based guanamine 0. 989 M+H 468. 1 4-{6-[(2-(2-°2-bito)ethyl)amino-based methyl)aminocarbyl]-2-pyridyl}benzoate oxime ester 0. 809 M+H 453. 2 {6-[4·(Didecylamino)phenyl]-2-[(2·(2-pyridyl)ethyl)amino](3′′pyridinyl)}-Ν-(3 - σ-pyridyl fluorenyl) carbamide 2. 133 M+H 452. 1 {6-(4-Ethylphenyl)-2-[(2-(2-acridinyl)ethyl)amino](3- °pyridyl)}-N-(3^pyridinium Methyl)carbamamine 2. 187 M+H 410. 1 {6-phenyl-2_[(2_(3·σ 唆 ))ethyl)amino]] (3 ° ° ° ° base thiol) meglumine 18. 274 M+H 454. 1 4·{6-[(2-(2_σΛσ定基)ethyl)amino]-ΗΝ_(3-σ ϋ 曱 曱 ) ) ) ) ) ) ] ] ] ] ] 19. 19. 19. 19. 19. 19. 19. 19. 19. 129 M+H 411. 1 (3_° ratio. base methyl) {6-(3_σΛσ定基)-2_[(2_(2-° ratio σ定基)ethyl)amino]](3-pyridyl)}carbamamine 6. 557 M+H 411. 1 Ν-(3′′-pyridyl fluorenyl) {6-(4_.pyridyl)-2-[(2_(2_°°°定基)ethyl)amino](3-pyridyl)}carbendide Amine 379 M+H 411. 2 Ν-(3-σ-pyridylhydrazino) {6-(2-°-pyridyl)-2-[(2-(2′′)-)ethyl)amino](3-pyridyl) } guanamine 2. 538 M+H 453. 1 4-{6-[(2-(2-Acridine)ethyl)amino]-5-[Ν-(3_° ratio dimethylmethyl)amine decanoic acid]-2-pyridyl}benzene Guanamine 942 M+H 425. 1 {2-[(2-Phenyl-2-phenylethyl)amino] each phenyl (3′′ than bite)} good (3′′ pyridylmethyl) formamide 5. 342 M+H 436. 1 {2-[(2-(2-Acridine)ethyl)amino] each (2-vinylphenyl) (3_° ratio), -N-(3-acridinyl) Formamide 254 200823188 IC50 arithmetic mean ion m/z chemical name 84. 495 M+H 454. 2 {6·[2-(Methoxymethyl)phenyl]-2-[(2-(2-pyridyl)ethyl)amino](3-hydroxypyridyl)}-N-(3 -pyridylmethyl)carbamamine 8. 751 M+H 438. 2 {6-(2-Mercaptophenyl)-2-[(2·(2-acridinyl)ethyl)amino](3-n-pyridyl)}-Ν-(3-acridine) Alkylamine 559 M+H 443. 2 (2-{[2-(3-fluorophenyl)-2-hydroxyethyl]amino}-6-phenyl(3-pyridyl))-N-(3-acridinylindolyl) A Guanamine 0. 339 M+H 468. 2 (6-(2-Cyanophenyl)·2-{[2-(3-indolyl)-2-hydroxyethyl]amino}(3-indenyl))-N-(3- Pyridylmethyl)carbamamine 8. 662 M+H 417. 1 {2-[(2-(2-Acridine)ethyl)amino]](1,3-thiazol-2-yl)(3-acridinyl)}-N-(3-acridinyl) Methyl) guanamine 2. 53 M+H 414. 2 {6-(1-indolylpyrazol-4-yl)-2-[(2-(2-pyridyl)ethyl)amino](3-acridinyl)}-N-( 3-Acridinemethyl)carbamamine 39. 528 M+H 322. 1 [3-(Aminoguanidino)-6-phenyl(2-acridinyl)P-(3-fluorophenyl)ethyl]amine 0. 534 M+H 463. 1 (6-(3,4-difluorophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))-indole-(3·pen pyridine Methyl)carbamamine 0. 28 M+H 458. 1 (6-(5-alkyl(2-σ-sepyl))-2-{[2_(3-fluorocarbyl)ethyl]amino} (3 - ° ratio σ base))-Ν-( 3-acridinylmethyl) decylamine 0. 052 M+H 461. 1 (2-{[2-(3-fluorophenyl)ethyl]amino} each (5-fluorenyl (2-thienyl))(3′′pyridinyl))-Ν-(3-pyridine Alkylamine 783 M+H 461. 1 (2-{[2-(3-fluorophenyl)ethyl]amino} each (3-fluorenyl (2-thienyl))(3·acridinyl))-Ν-(3-° Pyridylmethyl) decanoic acid amine 482 M+H 461. 1 (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(2-indolyl (3-thienyl))(3_pronyl))-N-(3 -u-pyridylmethyl)carbamamine 30. 616 M+H 699. 2 [2-{[2-(3-Fluorophenyl)ethyl]amino} each (6_{[2-(3.fluorophenyl)ethyl]amino}-5-[N-(3- Acridine-ylamino)aminomethyl]](2-indolyl))(3-acridinyl)]-anthracene-(3_σΛσ-decylmethyl)anthracene 1. 567 M+H 463. 1 (2-{[2-(3-fluorophenyl)ethyl]amino}-6_1&gt; benzylmethyl)(3_thienyl)](3-pyridyl))_Ν-(3-ϋ ratio Acridine-based guanamine 49. 792 M+H 418. 1 (2-{[2-(3-fluorophenyl)ethyl]amino} each of the ostomy. Sodium carbazyl))-Ν-(3-pyridylmethyl)carbamamine 0. 178 M+H 475. 1 (6-(5-Ethyl (2-thienyl))-2_{|&gt;(3-Denylphenyl)ethyl]amino}〇°pyridinyl))-Ν-(3·° Bipyridylmethyl) decanoic acid 255 200823188 IC50 arithmetic mean ion m/z chemical name 55. 694 M+H 462. 1 (Bu [3-(Aminomethyl)(2_thienyl)]-2-{[2-(3-fluorophenyl)-ethyl]amino}(3-pyridyl))-Ν- (3·pyridylmethyl)decylamine 0. 415 M+H 477. 1 (2·{[2_(3_fluorophenyl)ethyl]amino}-6-[5-(hydroxyethyl)(2_thienyl)](3_pyridyl))-Ν-(3- Pyridyl fluorenyl decylamine 0. 014 M+H 458. 1 (6-(4-cyano(3-indolyl))-2-{[2·(3-(phenylphenyl)ethyl]amino}}(3-. than bityl))-Ν-( 3-pyridyl fluorenyl) guanamine 2. 698 M+H 462. 1 (6-[5-(aminomethyl)(2-thienyl)]-2-{|&gt;(3-fluorophenyl)ethyl]amino}(3-pyridyl))-N-( 3-.pyridyl fluorenyl) guanamine 0. 323 M+H 481. 2 N-{[5-(aminomercapto)(3-acridinyl)]fluorenyl}(6-(2-cyanophenyl{[2-(3-fluorophenyl)ethyl]amino) } (3-0 than ° base)) 曱 amine 0. 081 M+H 482. 1 (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3·acridinyl))-N-{[5-(hydroxyindole) () 3-(aziridinyl)]methyl}carbamamine 2. 715 M+H 579. 2 Ν·({5_[3,3-bis(dimethylamino)_2_azapropan-2-enyl](3-pyridyl)}indenyl)(6-(2-cyanophenyl) -2_{[2_(3-fluorophenyl)ethyl]amino}(3-acridinyl))carhamamine 0. 624 M+H 481. 1 Ν-{[3-(Aminomethyl)(2-.pyridyl)]fluorenyl}(6-(2-cyanophenyl)-2·{[2_(3_fluorophenyl)B Amino group] (3 比 pyridine group)) decylamine 2. 437 M+H 824. 3 (6_(2_Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))-Ν-[(3-{[(6_) (2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-hydroxypyridyl))carbonylamino]indenyl}(2-acridinyl)曱基] guanamine 70. 994 M+H 442. 1 Ν-[(2-{[2-(3_Fluorophenyl)ethyl]amino}-6-phenyl(3-acridinyl))indenyl](3-pyridylamino)formamidine Amine 0. 512 M+H 486. 1 (5-chloro-6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))-N-(3- Acridine methyl)carbamamine 2. 653 M+H 531 (5-Bromo-6-(2-cyanophenyl)-2-{indole(3-fluorophenyl)ethyl]amino}(3-acridinyl))-N-( 3 比 啶 曱 曱 曱醯 曱醯 曱醯 0 0 0. 318 M+H 477. 1 (5-Cyano-6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3-.pyridyl))-N-( 3-acridinyl fluorenyl) guanamine 0. 072 M+H 486. 1 N-[(2-chloro(3′′-pyridyl))indenyl](6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3-pyridyl)) decylamine 0. 013 M+H 510. 1 N-({2-[(2-Aminoethyl)amino](3-acridinyl)}indenyl)(6-(2-cyanophenyl)-2_{[2-(3· Fluorophenyl)ethyl]amino}(3-acridinyl))decylamine 256 200823188 IC50 arithmetic mean ion m/z chemical name 0. 088 M+H 453. 1 (2_{[2-(3·Fluorophenyl)ethyl]amino}_5·oxyindolyl[3,2-b]II than dimethylidene)-N-(3-acridinyl) Carbenamide 0. 029 M+H 472 (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3- σ ratio), -Ν-[( 6-oxypiperidinyl))methyl]carbamamine 0. 877 M+H 629. 2 Ν-[(Η3-[(Tertibutoxy)carbonylamino]propyloxy(2_piperidinyl))methyl](6-(2-cyanophenyl)-2-{[ 2-(3-Fluorophenyl)ethyl]amino}(3_^indolyl))carboxamide 0. 025 M+H 529. 2 Ν-{[1-(3·Aminopropyl)_6_oxy (2_ aryl)] fluorenyl}(Bu(2_cyanophenyl)-2_{|&gt;(3-Fluorine Phenyl)ethyl]amino}(3_π-indenyl))carhamamine 1. 024 M+H 458. 2 N-[((2S)(2-piperidinyl))indenyl](6-(2-cyanophenyl)-2-{[2·(3-fluorophenyl)ethyl]amino} (3-° ratio of base)) formamide 16. 979 M+H 615. 2 N-[((2S)-l-{2_[(Tertidinoxy)carbonylamino]acetic acid). Basement)) 曱]](6_(2_cyanophenyl)_2_ {[2_ (3·Phenylphenyl)ethyl]amino} (3 -. fluorenyl)) formamide 0. 074 M+H 515. 2 N-{[(2S)-l-(2-Aminoacetic acid) (2-Benyl)] fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3 · Fluorophenyl)ethyl]amino} (3_ acridine) decylamine 8. 636 M+H 629. 2 N-[((2S)-1-{H(Tertidinoxy)carbonylamino]propanyl}(2·piperidinyl))methyl](6-(2-cyanophenyl) -2-{[2-(3-fluorophenyl)ethyl]amino}(3_σ-pyridyl)) decylamine. 109 M+H 529. 2 N-{[(2S)-l-(3-Aminopropenyl)(2-piperidinyl)]methyl}(6-(2-cyanophenyl)-2_{[2_(3- Fluorophenyl)ethyl]amino} (3_σ ratio π-based)) formic acid amine 1. 632 M+H 536. 3 Ν-{[(2S)· 1-(methylsulfonyl)(2-piperidinyl)]methyl} (6-(2-cyanophenyl)-2_{[2-(3_fluoro) Phenyl)ethyl]amino}(3" than sigma)) decylamine. 015 M+H 472. 2 N-[((2R)-6-oxy(2-piperidinyl))indenyl](6-(2-cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl Amino} (3 · acridinyl)) decylamine 0. 392 M+H 629. 4 N-[((2R)-1-{H(Tertidinoxy)carbonylamino]propyl 6-oxy(2-piperidinyl))methyl](6-(2-cyano) Phenyl)-2-{|&gt;(3-fluorophenyl)ethyl]amino}(3_pyridyl))carboxamide 0. 026 M+H 529. 2 N-{[(2R)-l-(3-Aminopropyl)oxy (2-piperidinyl)]methyl}(6-(2-cyanophenyl)-2_([2_( 3- phenyl)ethyl]amino} (3-° ratio), decylamine 1. 974 M+H 458. 1 N-[((3S)(3-piperidinyl))indenyl](6-(2-cyanophenyl)-2-{[2-(3-phenylphenyl)ethyl]amino} (3_pyridyl)) guanamine 257 200823188 IC50 arithmetic mean ion m/z chemical name 0. 696 M+H 500. 3 N-[((3R)-1-Acetyl(3·piperidinyl))fluorenyl](6-(2-cyanophenyl)-2-{[2_(3-fluorophenyl)-B Amino group (amino acid) (3) pyridine group) carbenamide 0. 718 M+H 516. 3(3R)-3-{[(6_(2-Cyanophenyl)-2-{[2-(3-phenylphenyl)ethyl]amino}(3′′pyridyl)carbonylamino Methyl} piperidine carboxylate 0. 199 M+H 615. 4 N-[((3RH-{2_[(Tertidinoxy)carbonylamino]]indolyl}(3_Nantyl))indolyl](6-(2-cyanophenyl)-2_ {[2·(3-Fluorophenyl)ethyl]amino}(3-lideridyl))guanamine 3. 79 M+H 629. 4 N-[((m)-l-{3-[(Tertidinoxy)carbonylamino]propanyl}(3-Bedenyl)methyl](6_(2-cyanophenyl) -2_{|&gt;(3-Fluorophenyl)ethyl]amino}(3-π-pyridyl)) decylamine 6. 161 M+H 643. 4 &gt;H((3R)-l-{4_[(Tertidinoxy)carbonylamino]butanyl}(3-p-pyridinyl))methyl](6-(2-cyanophenyl)-2 -{[2-(3-Fluorophenyl)ethyl]amino}(3′′pyridinyl))decylamine. 246 M+H 615. 4 N-{[(3R)-l-(2-Aminoethyl)(3-piperidinyl)]fluorenyl}(6-(2-cyanophenyl)-2-{[2_(3 _ phenyl) ethyl] amino) (3 〇 咬 咬 base)) guanamine 0. 173 M+H 629. 5 N-{[(3R)-l-(3-Aminopropionyl)(3-piperidinyl)]methyl}(6-(2-cyanophenyl)_2_ {[2_(3-fluoro) Phenyl)ethyl]amino} (3-indenyl)) decylamine. 512 M+H 543. 3 N-{[(3R)-l-(4-aminobutylidene)(3-piperidinyl)]methyl}(6-(2-cyanophenyl)·2- {[2_(3 - IL) Phenyl)ethyl]amino} (3 - ° than bite)) guanamine 0. 791 M+H 673. 3 N-( {(2R)-1 - [4_(1,3·dioxybenzo[c]indolyl)butyl]-6-oxy(2-piperidinyl)}indenyl) 6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))decylamine. 032 M+H 543. 2 N-{[(2R)-l-(4_Aminobutyl)-6-oxy(2.)] fluorenyl}(6-(2-cyanophenyl)-2-{ |&gt;(3-Fluorophenyl)ethyl]amino}(3_acridinyl)) decylamine 5. 537 M+H 523. 2 1^-[((38,48,211,511)-3,4,5,6-tetra](yl)(215-3,4,5,6-tetrahydro 11-butyl-2-yl)) fluorenyl (6 cyanophenyl)_2· {[2·(3·fluorophenyl)ethyl]amino} (3_ϋpyridinyl))carbamamine 13. 202 M+H 533. 2 2-[5-(N-{[(2R)-l-(3-Aminopropyl)-5-oxypyrrolidinyl]methyl}amine decanoic acid)-6-{[2-( 3_fluorophenyl)ethyl]aminopurine: ^ as a base] benzoic acid amine 3. 262 M+H 615. 2 N-[2-((2R)-2-{[(6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}}} Base)) arylamino]methyl}pyridinyl)(1 S)-l-decyloxyethyl](t-butoxy)decyl 258 200823188 IC50 arithmetic mean ion m/z chemistry Name 0. 053 M+H 515. 2 N-{[(2R)-l-((2S)-2-aminopropionyl)oxaridin-2-yl]fluorenyl}(6-(2-cyanophenyl)-2-{ [2-(3-Fluorophenyl)ethyl]amino}(3-acridinyl))carboxamide 3. 94 M+H 615. 2 N-[(lR)-2-((2R)-2-{[(6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3-pyridyl))carbonylamino]]hydrazino}pyrrolidinyl)-1-indolyl-2-oxyethyl](t-butoxy)decylamine 0. 166 M+H 515. 2 N-{[(2R)-H(2R)-2-aminopropionyl)oxaridin-2-yl]fluorenyl}(6-(2-cyanophenyl)-2-{[2 -(3-Fluorophenyl)ethyl]amino}(3"pyridinyl))decylamine. 052 M+H 558. 2 N-{[(2R)-l-((2S)-2,5-Diaminopentenyl)-indolyl-2-yl]methyl}(6-(2-cyanophenyl)- 2-{[2-(3-Fluorophenyl)ethyl]amino}(3′′pyridinyl)) decylamine. 046 M+H 451. 1 team [(2-chloro(3-acridinyl))methyl](2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-mercaptopyrazole-4 -yl)(3-pyridyl))carhamamine 0. 129 M+H 489. 2 N-({2-[(3-Aminopropyl)amino](3-acridinyl)}methyl)(2-{[2-(3-fluorophenyl)ethyl]amino} -6-pyrazol-4-yl(3-pyridyl))carhamamine 0. 122 M+H 475. 1 N-({2-[(2-Aminoethyl)amino](3·oxaridinyl)}methyl)(2-{[2-(3-fluorophenyl)ethyl]amino} -6-oxazol-4-yl (3-acridinyl)) decylamine 1. 459 M+H 541. 3 (2R)-2-{[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-methyloxazol-4-yl) (3 -pyridyl))carbonylamino]methyl}pyrrolidinecarboxylic acid tert-butyl ester 0. 275 M+H 441. 1 义[((21〇吼rrolidin-2-yl)indolyl](5-fluoro-2-{[2-(3-fluorophenyl)ethyl]aminopurinylpyrazol-4-yl) (3-oxaridinyl)) guanamine 0. 625 M+H 598. 3 N-[((2 R) small {2-[(t-butoxy)carbonylamino]ethyl)pyrrolidin-2-yl)methyl](5_fluoro-2-{[2_( 3-fluorophenyl)ethyl]amino}-6-(1•mercaptoindole-4.yl)(3-acridinyl))carboxamide 0. 065 M+H 476. 1 (2·{[2-(3-Fluorophenyl)ethyl]amino}-6-pyrazol-4-yl(3-pyridyl))-N-({2-[(2-hydroxyethyl) Amino](3-pyridyl)}methyl)carbenamide 0. 488 M+H 564. 2 N-[(2-{[(Tertidinoxy)carbonylamino]indolyl}(3-σ-pyridyl))indolyl](5-fluoro-2-{[2-(3-fluoro) Phenyl)ethyl]aminobi b 6-oxazol-4-yl (3-pyridyl)carboxamide 0. 012 M+H 464. 1 Ν-{[2·(Aminomethyl)(3′′pyridyl)]methyl}(5_fluoro_2_{[2-(3-fluorophenyl)ethyl]amino}-6- Pyrazol-4-yl (3-pyridyl) decylamine 1. 079 M+H 584. 2 N-[((2R)-l-{2_[(Tertidinoxy)carbonylamino]ethinylpyridinyl)methyl](5_fluoro-2-{[2-(3- Fluorophenyl)ethyl]amino}-6-oxazol-4-yl (3-259 200823188 IC50 arithmetic mean ion m/z chemical name-pyridyl)) formamide.  * N-{[(2R)-l-(2-Aminopropyl) σpyrrol-2-yl]methyl}(5-ran-2-{[2-(3-fluorophenyl)) Ethyl]amino}-6-α-pyrazol-4-yl(3-acridinyl))carboxamide. 061 M+H 484. 1 Amine N-[((2R)-l-{3-[(Tertidinoxy)carbonylamino]propanyl}-pyridin-2-yl)methyl](5_气-2-{ [2-(3-Phenylphenyl)ethyl]amino}-6-° than sal-4-yl (3- 0. 98 M+H 598. 3 . ratio. Basement))carbamide N-{[(2R)-1_(3-aminopropionyl)oxaridin-2-yl]methyl}(5-fluoro-2-{[2-(3-fluoro) Phenyl)ethyl]amino}-6-oxazol-4-yl(3-acridinyl)). 09 M+H 498. 2 indoleamine N-[((2R)-1 - {4-[(t-butoxy)carbonylamino]butanyl}pyridin-2-yl)methyl](5-fluoro-2-{[ 2. (3-Fluorophenyl)ethyl]amino}-6-oxazol-4-yl. 75 M+H 612. 2(3-Pyridinyl))carbenamide N-{[(2R)-l-(4-aminobutylidene)-pyridin-2-yl]fluorenyl}(5-fluoro-2-{[2- (3-Fluorophenyl)ethyl]amino}-6-oxazol-4-yl (3-acridinyl)) oxime. 047 M+H 512. 2 amine sense [((211 phenylpyrrolidin-2-yl)methyl](5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amine) 394 M+H 427. 1 base}-6"pyrazol-4-yl(3-acridinyl)nonylamine N-[((2R)-l-{3-[(t-butoxy)carbonylamino]propyl} -5-oxy-hlrolidine-2-yl)methyl](5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-°°°坐-4- Base 0. 354 M+H 598. 2 (3-pyridyl))carinamide N-{[(2R)-l-(3-aminopropyl)-5-oxyindole 17 σ σ-2-yl] fluorenyl} (5- Fluor-2-{[2-(3-fluorophenyl)ethyl]amino}-6-° ratio 圭··· 4-base (3-° ratio ° base)) 066 M+H 498. 1 Amine Ν-(Aminomethyl fluorenyl) (5-fluoro_2_ {[2-(3·fluorophenyl)ethyl]amino) 6_π ratio 0. 14 M+H 401. 1 oxazol-4-yl (3 · acridine)) decylamine 2-[(5-fluoro-2-{[2_(3-fluorophenyl)ethyl]amino}}__°°°- 4-base (3-external 匕0 fixed 0. 065 M+H 415 base))carbonylamino]-indole-mercaptoacetamide N-[((2R)-l-{(2S)_2-[(t-butoxy)amino)] 3-glycosylamine} σpyrrolidyl)methyl](5_gas-2-{[2-(3-fluorophenyl)ethyl]amino}« 1. 001 M+H 614. 3 oxazol-4-yl (3-pyridyl))carhamamine 0. 059 M+H 514. 1 Ν- {[(2R)-1 -((2S)-2-amino-3-hydroxypropenyl) σ-pyridin-2-yl]- 260 200823188 IC50 arithmetic mean ion m/z chemical name base } (5-fluoro-2-{[2-(3=fluorophenyl)ethyl]amino} -6- ° ratio σ sit-4-yl (3-anthraquinone)) formamide Ν-[ (2-{[(Tertidinoxy)carbonylamino]methyl}(3-α-pyridyl))indenyl](5-fluoro-2_{[2-(3-fluorophenyl)ethyl) Amino}_6_(2-acridinyl)0. acridine 3. 665 M+H 575. 2 base)) formamide Ν-{[2_(aminomercapto)(3-acridinyl)] fluorenyl}(5-fluoro-2_{[2-(3·fluorophenyl) 0. 066 M+H 475. 1 ethyl]amino}-6-(2-pyridyl)(3-pyridyl))decylamine (5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino} -6-(1-methyloxazol-4-yl) (3- 0. 381 M+H 430. 1 σ pyridine group))-N-(2-hydroxy-2-methylpropyl) formamide (5-gas-2-{[2-(3-phenylphenyl)ethyl]amino}- 6-(1-methyl ° is 0 to -4-base) (3_ 0. 224 M+H 444. 1 σ pyridine group))-N-(3-hydroxy-2,2-dimethylpropyl) decylamine N-((2R)-2-methyl; oxybutyl) (5-fluoro- 2-{[2-(3-fluorophenyl)ethyl]amine 0. 109 M+H 442. 2 base}-6-(1-indenyl.pyran-4-yl)(3-indolyl))sodium formate N-((2R)-3-hydroxy-2,3-didecylbutyl) (5-fluoro-2-{[2-(3-fluorophenyl)ethyl 1. 225 M+H 458. 1 yl]amino}-6-(1-methylpyrazol-4-yl)(3-pyridyl))carinamide 2-[(tatabutoxy)carbonylamino]acetic acid 2-(( 2R)-2-{[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-indolyloxazol-4-yl)(3-吼) Pyridyl))carbonylamine 0. 191 M+H 642. 2 base] methyl} nitrogen. Danyl)-2-oxoethyl ester 2-aminoacetic acid 2-((2R)-2-{[(5-fluoro-2-{[2-(3.fluorophenyl)ethyl]amino) }-6-(1-fluorenyl ° than sal-4-yl) (3-σΛσ-based)) alkylamino]fluorenyl}nitrogen} 045 M+H 542. 2-yl)-2-oxoethyl dimethyl 2-((2R)-2-{[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino) }-6-(1-mercaptooxazol-4-yl)(3-acridinyl))carbonylamino]methyl}nitrogen. 4 M+H 593. 2-yl)-2-oxoethyl ester (2-{[2-(3-fluorophenyl)ethyl]amino}-6-[5-(hydroxyindenyl)(2-phenyl) (3_ 0. 041 M+H 463. 1 ° ratio pyridine))-N-(3-acridinyl fluorenyl) decylamine N-({2-[(3-aminopropyl)amino](3-acridinyl)} fluorenyl )(6-(2-cyanobenzene 0. 017 M+H group)-2-{[2_(3-fluorophenyl)ethyl]amino}(3′′pyridyl))guanamine (5-fluoro-2-{[2-(3- Fluorophenyl)ethyl]amino}-6--bizozol-4-yl (3-acridine 0. 018 M+H group))_N-(3-octidylmethyl)decylamine N-{[(2R)-l-(2-aminoethenyl)oxaridin-2-yl]methyl }(5_Fluor 0. 066 M+H -2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-indolylcarbazole-4-yl)(3-acridine 261 200823188 IC50 arithmetic mean ion m/z chemical name base)) formamide (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine H-methyl (3′′ pyridine) 1. 076 M+H 466. 2))-N-(3-Acridinemethyl)carbamamine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3-Acridine 16. 894 M+H 537. 2)))-N-[(6-morpholinyl(3_~pyridyl))indolyl]carbamamine (6-(2-cyanophenyl)-2-{[2-(3-fluoro) Phenyl)ethyl]amino}(3-acridine 66. 631 M+H 521. 2)))-N-[(6"pyrrolidyl(3"pyridinyl))indolyl]nonanamine (6-(2-cyanophenyl)-2-{[2-(3- Fluorophenyl)ethyl]amino}(3-acridine 1. 752 M+H 536. 2 base))-N-[(6-piperidinyl(3-n-pyridyl)methyl]decylamine N-{[6-(4-ethylhydrazine) (3-σ ratio) Pyridyl)]methyl}(6-(2-cyanobenzene) 747 M+H 578. 2-yl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3′′pyridinyl)) amidoxime-[(6-bromo(2-acridinyl))- (6-(2-cyanophenyl) winter {[2-(3-fluorophenyl) 0. 233 M+H 530. 1 ethyl]amino}(3-pyridyl))carboxamide 2-[(2-{[2-(3-fluorophenyl)ethyl]amino}-6-[5-(hydroxyindenyl) ) (2-thiophene 0. 254 M+H 443. 1 base)](3-acridinyl))carbonylamino]-N-methylacetamide N-(2-aminomercaptoethyl)(2-{[2-(3-fluorophenyl)) Ethyl]amino}-6-[5-(hydroxyl. 549 M+H 443. (ylthio)(2-thienyl)](3-acridinyl))carboxamide (2-{[2_(3-fluorophenyl)ethyl]aminobi 6-[5_(hydroxy fluorenyl) )(2-nonyl))(3- 0. 045 M+H 463. 1 σ pyridine group))-N-(2-pyridylmethyl)carbamamine N-(amine fluorenyl) (2-{[2·(3-fluorophenyl)ethyl]amino group Bu 6_[5_(hydroxy 0. 496 M+H 429. 1 fluorenyl) (2_σsecenyl)] (3_σ ratio bite)) decanoic acid 2-[(6-(2-cyanophenylfluorophenyl)ethyl]amino}(3′′pyridyl) )) twenty four. 88 M+H 496. 1 carbonylamino]-indole-(fluorenylsulfonyl)acetamide aminomethyl)cyclohexyl]methylcyanophenyl)_2][2-(3-fluoro 0. 352 M+H 486. 2 phenyl)ethyl]amino}(3_acridinyl)) amidoxime (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl] Aminopyridinyl) 11. 631 M+H 472. 1 carbonylamino]cyclopentanecarbamamine (6-(2-cyanophenyl)_2-{[2-(3-fluorophenyl)ethyl]amino} (3^pyridyl 16. 178 M+H 473. 2 base))-N-〇 〇 耕 乙基 ethyl) decylamine (6-(2-cyanophenyl peak {[2_(3-fluorophenyl)ethyl)amino} (3-. 0. 266 M+H 467. 1 base))-N-pyridinium I-ethyl) decylamine 0. 026 M+H 453. 1 (6-(2-Cyanophenyl)_2-{[2_(3-fluorophenyl)ethyl]amino} (&gt; σ pyridine 262 200823188 IC50 arithmetic mean ion m/z chemical name base)) -N in the ratio of cumyl-2-ylmethyl)carhamamine·N-((lS)-5-amino-1-amine-mercaptopentyl)(6-(2-cyanophenyl)-2 -{[2-(3- 4. 421 M+H 489. 1 fluorophenyl)ethyl]amino}(3′′pyridinyl))decylamine N-(3-amino-1-amine-mercaptopropyl)(6-(2-cyanophenyl) -2-{[2-(3-fluorobenzene 1. 906 M+H 461. 1 yl)ethyl]amino} (3-pyridyl)) decylamine N-{(1 R)-l-amine fluorenyl-5-[(phenyl decyloxy)carbonylamino]pentyl }(6-(2- 58. 8 M+H 623. 2 cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl)) decylamine N-(4-amino-1.amine oxime Benzyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorobenz. 59 M+H 475. 1 yl)ethyl]amino} (3-pyridyl)) decylamine N-((lR)-5-amino-1-amine-mercaptopentyl) (6-(2-cyanophenyl) )-2-{[2-(3- 1. 28 M+H 489. 1 fluorophenyl)ethyl]amino}(3-pyridyl))carboxamide N-({6-[(2-aminoethyl)amino](2-acridinyl)}methyl) (6-(2-cyanobenzene 0. 007 M+H 510. 1-yl)-2-{[2-(3-fluorophenyl)ethyl]amino)(3-pyridyl))decylamine N-({6-[(3-aminopropyl)amino) ](2-Aridinyl)}methyl)(6-(2-cyanobenzene). 005 M+H 524. 2-yl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))decylamine N-{(4R)-4-amineindolyl-4- [(6-(2-Cyanophenyl)-2-{[2_(3-fluorophenyl)ethyl 19. 6 M+H 609. 1 yl]amino}(3-n-pyridyl))carbonylamino]butyl}(phenylmethoxy)carbamamine N-((lS)-4-amino-1.aminecarbamyl Butyl) (6-(2-cyanobenzene) 404 M+H 475. 1 yl)-2_{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl)) decylamine N-((lR)-4-amino-1-aminecarboxamidine Butyl)(6-(2-cyanophenyl)-2-{[2-(3- 7. 413 M+H 475. 1 fluorophenyl)ethyl]amino}(3·pyridyl))decylamine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine Base} (3- ° than pyridine 0. 963 M+H 444. 1 base))-N-(pyrrolidin-3-ylmethyl)carbamamine-{[1-(2-aminoethenyl) σ ratio p σ -3--3-methyl]methyl} 6-(2-carbobenzene 0. 203 M+H 501. 1 base)-2-{[2-(3-1phenyl)ethyl]amino}(3′′pyridinyl)) amidoxime-{[1-(3-aminopropionyl)π Bilobidine _3_yl]methyl}(6-(2-cyanobenzene 0. 27 M+H 515. 1 yl)-2_{[2-(3-fluorophenyl)ethyl]amino}(3·acridinyl))carbamamine Ν-{[1-(4-aminobutyryl). Than bite _3_yl]methyl}(6-(2-cyanobenzene 0. 433 M+H 529. 1 yl)-2-{[2_(3-fluorophenyl)ethyl]amino}(3′′pyridinyl))indoleamine N-[(l-ethylidenepyrrolidin-3-yl)indole (6-(2-cyanophenyl)-2-{[2-(3·fluorine 0. 334 M+H 486. 1 phenyl)ethyl]amino} (3-° 〇 基 base)) decanoic acid amine 4. 787 M+H 501. 2 Ν-{[1-(3-Aminopropyl)σ ratio p bit _3_yl]methyl}(6-(2-cyanobenzene263 200823188 IC50 arithmetic mean ion m/z chemical name-based -2[{2-(3-fluorophenyl)ethyl]amino}(3"pyridyl))carboxylic acid amine, N-(3-amino-2-aminemethylmercaptopropyl) (6 -(2-cyanophenyl)-2-{[2-(3·fluorobenzene) 6. 654 M+H 460. 5-yl)ethyl]amino}(3_ϋ 咬))) carboxylic acid amine (2][2-(3-1 phenyl)ethyl]amino}-6-(1-methyl-pyridyl) ) (3_° than pyridine 1. 236 M+H 452. 3 base))-Ν-[(6-oxypiped-2-yl)methyl]carbamamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6- ° Bizodazole (3-acridine 0. 973 M+H 438. 3))-Ν-[(6-oxypiped-2-yl)methyl]carbamamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-σ Biazo-5-yl (3-σ-pyridyl 6. 954 M+H 438. 3 base:))-Ν-[(6-oxypiperidin-2-yl)methyl]carbamamine (6-(2-cyanophenyl)_2-{[2-(3-fluorophenyl) ) ethyl]amino} (3_ ° than pyridine 2. 565 M+H 551. 1 base))-N-{[4-(methylsulfonyl)-6.oxypipedin-2-yl]decyl}carbenamide N-[(4-ethyl-branched-6-oxyl) Brigade _-2-base) thiol] (6-(2-cyanobenzene) 635 M+H 515. 1 base) winter {[2_(3-fluorophenyl)ethyl]amino}(3′′pyridinyl))carboxamide (6-(2-cyanophenyl)-2-{[2·( 3-fluorophenyl)ethyl]amino}(3-indenylpyridinium 0. 037 M+H 487. 1 base))-Ν-[(4·decyl-6-oxypiped-2-yl)methyl]carbenamide (6-(2-cyanophenyl)-2-{[2-( 3-fluorophenyl)ethyl]amino} (3- ° than pyridine 0. 866 M+H 461. 2)))-N-{2-[(decylamino)carbonylaminojethyl}carbamimidoxime-(2·{[(2-aminoethyl)sulfonyl]amino} Base) (6-(2-cyanobenzene) 548 M+H 511. 2-yl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3′′pyridyl))indoleamine N-[((2S)-pyridin-2-yl)indole (6-(2-cyanophenyl)-2-{[2-(3-fluorobenzene) 569 M+H 444. 2-yl)ethyl]amino}(3-pyridyl))carbamamine 2-amino-indole {2-[(6·(2-cyanophenyl)-2-{[2-(3) -fluorophenyl)ethyl]amine 1. 23 M+H 461. 2 base}(3-pyridyl))carbonylamino]ethyl}acetamido 3-amino-indole-{2-[(6-(2-cyanophenyl)-2-{[2-( 3-fluorophenyl)ethyl]amine 4. 325 M+H 475. 2 base}(3′′-pyridyl))carbonylamino]ethyl}propanamine 4-amino-N_ {2-[(6-(2-cyanophenyl)-2-{[2-( 3-fluorophenyl)ethyl]amine 1. 265 M+H 489. 2 base}(3-1〇 ratio° base)) arylamino]ethyl}butyric acid amine 2-[(tatabutoxy)carbonylamino]-N-{2_[(6-(2- Cyanophenyl)-2·{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))carbonylamino]ethyl}-fluorene-fluorenylethyl 15. 303 M+H 575. 3 decylamine 4-[(tatabutoxy)carbonylamino]-Ν·{2-[(6_(2-cyanophenyl)-2-{[2-(3- 3. 883 M+H 603. 3 fluorophenyl)ethyl]amino}(3-acridinyl))carbonylamino]ethyl}-fluorene-methylbutyl 264 200823188 IC50 arithmetic mean ion m/z chemical name decylamine - N-{[ (2S)-l-(2-Aminoethyl) fluorenyl-2-yl]methyl}(6-(2-cyanobenzene). 995 M+H 501. 2-yl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))carbenamide N_{[(2S)-l-(3-aminopropionamidine Base) 吼 吼 啶 -2- 基 基 基 甲基 甲基 6 6 6 6 6 6 6 6 6 856 M+H 515. 2 yl)-2_{[2-(3-fluorophenyl)ethyl]amino}(3·acridinyl))carbenamide N-{[(2S)-l-(4-aminobutylidene) Ethrolidin-2-yl]fluorenyl}(6-(2-cyanobenzene) 27 M+H 529. 3-yl)-2_{[2_(3-fluorophenyl)ethyl]amino}(3′′pyridinyl))guanamine 2-amino-N-{2-[(6-(2-cyanide) Phenyl)-2-{[2·(3-fluorophenyl)ethyl]amine 1. 374 M+H 475. 2 base}(3-pyridyl))carbonylamino]ethyl}-indole-mercaptoacetamide 3-amino-1^-{2-[(6-(2-carbylphenyl)-2) -{[2-(3-Fluorophenyl)ethyl]amine 1. 775 M+H 489. 2 base}(3-pyridyl))carbonylamino]ethyl}-indole-methylpropanamide 4·amino-indole-{2-[(6-(2-cyanophenyl)-2- {[2-(3-Fluorophenyl)ethyl]amine 1. 2 M+H 503. 2 base}(3-pyridyl))carbonylamino]ethyl}-N-mercaptobutylamine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)) Ethyl]amino}(3-acridine 1. 385 M+H 496. 2 base))-N-{2·[indolyl(methylsulfonyl)amino]ethyl}mercaptoamine 3-amino-N-(2-aminoethyl)-2-{[( 6-(2-cyanophenyl)-2-{[2-(3-fluorobenzene 13. 725 M+H 504. 2-yl)ethyl]amino}(3-pyridyl))carbonylamino]methyl}propanamine N-(2-carbonylamino-2-methylpropyl)(6-(2-cyano) Phenyl)-2-{[2-(3-fluorobenzene 0. 151 M+H 460. 2 yl)ethyl]amino}(3-.pyridyl)) decylamine N-((2S)·2·amino group hydroxypropyl)(6_(2-cyanophenyl) winter {[ 2-(3-1 benzene 1. 588 M+H 434. 3-yl)ethyl]amino}(3_pyridyl))decylamine N-((lS)-l-{[(6-(2-cyanophenyl)-2-{[2_(3_ fluorobenzene) Ethyl]amino]} (3- 0. 249 M+H 491. 1 pyridyl))carbonylamino]mercapto}-2-ylethyl)-2-aminoacetamide 2-aminoacetic acid (2S)-2-(2-aminoethenylamino) -3-[(6-(2-cyanophenyl)-2-{[2_(3-1phenyl)ethyl]amino}(3-π-pyridyl)-ylamino]propyl 5 . 705 M+H 548. 3 N-((lR)-l-{[(6-(2-Cyanophenyl)-2-{[2-(3- 1 phenyl)ethyl]amine 0. 441 M+H 504. 2 base}(3_acridinyl))alkylamino]mercapto}m-methylpropyl)-2-carbylamine N-((l R)-l-{[(6-(2) -Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine 0. 939 M+H 503. 3-yl}(3-°-pyridyl))carbonylamino]mercapto}_2-mercaptopropyl)-2-aminoacetamide N-((2R)-2-amino-4-indenyl Pentyl)(6-(2-cyanophenyl)-2·{[2-(3-fluorobenzene) 237 M+H 460. 3 yl)ethyl]amino}(3_吼°定)) decanoic acid 265 200823188 IC50 arithmetic mean ion m/z chemical name 1. 169 M+H 518. 2 N-((lR)-l-{[(6-(2-Actylphenyl)-2-{[2-(3-phenylphenyl)ethyl]amino}(3·pyridyl)) Carbonylamino]methyl}-3-methylbutyl)-2-hydroxyacetamidine 0. 913 M+H 517. 2 N-((lR)-l-{[(6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl)) Carbonylamino] fluorenyl}-3-mercaptobutyl)-2-aminoacetamide 12. 554 M+H 490. 2 N-((lR)-2-amino group small {[(6-(2-cyanophenyl) winter {[2_(3-fluorophenyl)ethyl]amino}} (3-pyridyl)) Carbonylamino]mercapto}ethyl)-2-aminoacetamide 10. 561 M+H 491. 2 N-(( 1 R)-2-Amino-1 - {[(6_(2· cyanophenyl)-2_ {[2_(3-fluorophenyl)ethyl]amino}}(3-pyridine Base)) carbonylamino]methyl}ethyl)-2-hydroxyacetamidine 0. 352 M+H 458. 3 N-((3R)-2-oxy(3-teledecyl))(6-(2-cyanophenyl)-2-{[2·(3-fluorophenyl)ethyl]amino } (3-° pyridine group)) formazan 17. 307 M+H 423. 1 {2-[((2R)-2-phenylpropyl)amino]-6-phenyl(3· acridine)}-indole-(3·-pyridylfluorenyl) decylamine 0 . 564 M+H 432. 1 N-(Aminomethylhydrazineethyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl)) A Guanamine 0. 532 M+H 432. 1 N-((1R)-1-amine-mercaptoethyl)(6-(2-cyanophenyl)-2-{[2_(3-fluorophenyl)ethyl]amino}(3- Pyridyl)) formamide 6. 98 M+H 447. 1 (23)-2-[(6-(2-Cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl]amino}(3-n-pyridyl)carbonylamino ] decyl propionate 0. 743 M+H 447. 1 (2R)-2_[(6_(2-cyanophenyl)-2_{[2_(3-fluorophenyl)ethyl]amino}(3′′pyridinyl))carbonylamino]propanoic acid Ester 0. 101 M+H 433. 1 2-[(6_(2-Cyanophenyl)·2_ {[2-(3-fluorophenyl)ethyl]amino)-3·-pyridinyl)carbonylamino]acetate oxime 1. 083 M+H 405. 1 (6-(2······························· Guanamine 0. 238 M+H 419. 1 (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3- η ratio), -Ν-(2-methoxyl) Ethyl) decylamine 4. 222 M+H 432. 1[2_(Dimethylamino)ethyl](6-(2·cyanophenyl)-2-{[2_(3-fluorophenyl)ethyl]amino}(3_pyridyl)) Guanamine 42. 246 M+H 518. 1 Ν-{2_[(Tertidinoxy)-fluorenylcarbonylamino]ethyl}(6-(2-cyanophenyl)-2_ {[2_(3_phenyl)ethyl] Amino group (3_α than hydrazide)) an amine 4. 455 M+H 418. 1 (6-(2-Cyanophenyl)-2-{[2-(3-phenylphenyl)ethyl]amino} (3·. π-based))-N-[2_(decylamine) Ethyl] decanoic acid amine 266 200823188 IC50 arithmetic mean ion m/z chemical name N-(3-aminopropyl)(6-(2-cyanophenyl)-2-{[2-(3- Fluorophenyl)ethyl]amine 0. 994 M+H 418. 1 base}(3-pyridyl))carboxamide (2S)-2-[(6-(2-cyanophenyl)-2-{[2·(3-fluorophenyl)ethyl]amino) } (3 -σ ratio 0. 985 M+H 446. 1 pyridine))carbonylamino]-indole-methylpropanamide (2R)-2-[(6-(2-cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl]] Amino group} (3_ mouth ratio 1. 273 M+H 446. 1 pyridine))carbonylamino]-N-mercaptopropionamide N_{2-[(6-(2-cyanophenyl)-2_{[2_(3-1phenyl)ethyl]amino} _3·吼吼0. 958 M+H 446. 1 yl)carbonylamino]ethyl}acetamidamine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3-吼1) . 118 M+H 462. 1 base))-N-[2_(decyloxycarbonylamino)ethyl]carbenamide (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl) Amine base} (3·. than 唆0. 326 M+H 482. 1 base))-N-{2_[(methylsulfonyl)amino]ethyl}decylamine H(6-(2-cyanophenyl)-2_{[2·(3-fluorophenyl) Ethyl]amino}·3-acridinyl) 4. 792 M+H 461. 1 carbonylamino]ethyl propionate 4-[(6-(2-cyanophenyl)-2_{[2_(3-fluorophenyl)ethyl]amino}_3"-pyridyl) 0. 713 M+H 461. 1 carbonylamino] decanoic acid decyl ester H (6-(2-cyanophenyl)-2-{[2-(3.fluorophenyl)ethyl]amino}(3′′pyridinyl)) 0 . 34 M+H 446. 1 carbonylamino]-N-methylpropionamide 4-[(6-(2-cyanophenyl)-2-{[2_(3-fluorophenyl)ethyl]amino}(3-acridine) Base)) 2. 956 M+H 460. 1 carbonylamino]-N-methylbutyramine N-(3-aminomethylpropyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)-ethyl Base] 0. 185 M+H 446. 1 Amino}(3-pyridyl))guanamine 4-[(6-(2-cyanophenyl)-2-{[2_(3-phenylphenyl)ethyl]amino group). 627 M+H 447. 1 carbonylamino]butyric acid Ν-(2-aminoethyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine 2. 637 M+H 404. 1-yl}(3-acridinyl))carbenamide (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3-σ ratio Set 2. 108 M+H 469. 1 base))-Ν-[(4-fluorophenyl)indolyl]decylamine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine Base} (3- lysidine 0. 968 M+H 476. 1 base))-N-[(4-cyanophenyl)methyl]decylamine N-[(3,4-difluorophenyl)indenyl](6-(2-cyanophenyl)- 2-{[2-(3-Denylphenyl) B. 981 M+H 487. 1 yl]amino}(3-pyridyl))carbamamine 267 200823188 IC50 arithmetic mean ion m/z chemical name 1. 02 M+H 448. 1 N-((1S)-1-Amidino-2-hydroxyethyl)(6-(2-cyanophenyl)-2_{p-(3-fluorophenyl)ethyl]amino} (3-Acridine))carbamamine 0. 318 M+H 419. 1 (6-(2-Cyanophenyl)-2-{[2·(3-fluorophenyl)ethyl]amino}(3-tonpyridyl))-indole-(3-hydroxypropyl) Formamide 0. 396 M+H 433. 1 (6-(2-Cyanophenyl)-2·{[2-(3-fluorophenyl)ethyl]amino)(3·acridinyl))-14-(3-decyloxypropane Base amine 177 M+H 463. 1 (2S)-2-[(6-(2-Cyanophenyl)-2_{[2_(3-fluorophenyl)ethyl]amino}(3-cyclopyridyl)carbonylamino] 3-hydroxypropionate oxime ester 0. 513 M+H 463. 1 (2R)-2-[(6-(2-carbophenyl)-2-{[2-(3.fluorophenyl)ethyl]amino}(3-°pyridyl))carbonylamine ]]-3-hydroxypropionate oxime ester 1. 121 M+H 462. 1 (2S)-2-[(6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-cyclopyridyl)carbonylamine 3-hydroxy-N-mercaptopropylamine 0. 544 M+H 462. 1 (2R)_2-[(6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-hydroxypyridyl))carbonylamino ]-3-hydroxy-N-mercaptopropionamide 0. 029 M+H 452. 1 (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl)-N-(2-acridinylmethyl) ) methotrexate 24. 295 M+H 465. 1 (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))-N-[(4-mercaptobenzene) Alkylamine 426 M+H 466. 1 (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))-N-[(6-fluorenyl) 3-oxaridinyl))indolyl]carbamamine 0. 054 M+H 466. 1 (6-(2-carbophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-.pyridinyl))-Ν-[(6-methyl) (2-Acridine)) fluorenyl] guanamine 0. 291 M+H 466. 1 (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))-N-(2-(2-u) Bipyridyl)ethyl) decylamine 0. 15 M+H 466. 1 (6-(2-Cyanophenyl)-2_{[2-(3.fluorophenyl)ethyl]amino}(3-acridinyl))-N-(2-(3-acridine) Base) ethyl)carbamamine 0. 026 M+H 467. 1 N-[(6-Amino(3-.pyridyl))methyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine Base} (3-n-pyridyl) carbenamide 8. 099 M+H 482. 1 (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))-N-[(6-decyloxy) (3-pyridyl)) fluorenyl] decylamine 0. 022 M+H 466. 1 (6-(2-carbophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3- ° ratio σ base))-Ν-[(2-fluorenyl) (3-Acridine))methyl]carbamamine 268 200823188 IC50 arithmetic mean ion m/z chemical name 0. 022 M+H 467. 1 N-[(2-Amino (3_-σ-pyridyl))methyl](6-(2·cyanophenyl)-2-{[2·(3-fluorophenyl)ethyljamine }}(3-acridinyl))carbamamine 0. 087 M+H 482. 1 (6·(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-.pyridyl))-N-[(2-methoxy) (3 比 pyridine group)) methyl] carbamide 0. 021 M+H 470. 1 (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-this σ-decyl))-Ν-[(1-hydroxy(2)比 pyridine group)) methyl] formamide 0. 019 M+H 470. 1 (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-heptinyl))-N-[(l-hydroxy(3) - aridinyl)) methyl] formamide 3. 064 M+H 501. 1 (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))-N-|&gt;(4-A Isopropyl] propyl] guanamine 0. 136 M+H 415. 1 (6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3·° ratio pyridine))-N-(cyclopropyl fluorenyl) ) methotrexate 9. 309 M+H 489. 1 N-[2-(Dimethylamino)ethyl]-2-[(6-(2-cyanophenyl)·2·{[2-(3-fluorophenyl)ethyl]amino) }(3-Pyridinyl))carbonylamino]acetamide 2. 07 M+H 462. 1 2-[(6_(2·Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3′′pyridinyl))carbonylamino]-Ν-( 2-hydroxyethyl)acetamide 12. 17 M+H 489. 1 Ν-(2-Aminomethylmethyl)-2-[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}} -pyridyl))carbonylamino]acetamide 9. 666 M+H 490. 1 3-{2·[(6-(2-Cyanophenyl)-2·{[2·(3-fluorophenyl)ethyl]aminopyridinyl)carbonylamino]ethinylamino }Protein 9. 876 M+H 575. 1 Ν-{3-[(Tertibutoxy)carbonylamino]propyl}-2-[(6-(2-cyanophenyl)-2_{[2_(3·fluorophenyl)ethyl) Amino}(3_acridinyl))carbonylamino]acetamide 12. 22 M+H 503. 1[3-(Dimethylamino)propyl]-2-[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3_pyridyl))carbonylamino]acetamide 5. 836 M+H 476. 1 2-[(6_(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))carbonylamino]-Ν-( 3-hydroxypropyl)acetamide 65. 469 M+H 575. 1 Ν-{2-[(Tertibutoxy)-fluorenyl-methylcarbonylamino]ethyl}-2-[(6-(2-cyanophenyl)-2- {[2_(3- Phenyl phenyl)ethyl]amino} (3 - carbyl)) arylamino] arylamine 11. 096 M+H 475. 1 2-[(6_(2_Cyanophenyl)-2-{[2-(3-phenylphenyl)ethyl]amino}(3·π-pyridyl)) carbylamino]- Ν-[2_(decylamino)ethyl]acetamide 269 200823188 IC50 arithmetic mean ion m/z chemical name (2S)-3-amino-2·[(6-(2-cyanophenyl) -2-{[2-(3-Fluorophenyl)ethyl]amine 2. 318 M+H 462. 1 base}(3-pyridyl))carbonylamino]methyl propionate N-((lS)-2-amino-1.aminemethylmercaptoethyl)(6-(2-cyanobenzene). 816 M+H 447. 1-yl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))decylamine (2S)-3-[(t-butoxy)carbonylamine Base]-2-[(6-(2-cyanobenzene) 30. 417 M+H 548. 1-yl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))carbonylamino]propionic acid (2S)-3-[(t-butoxy) Carbonylamino]-2-[(6-(2-cyanophenyl)-2·{[2-(3-fluorophenyl)ethyl]amino}(3′′pyridyl)carbonylamino ]-Ν-甲43. 598 M+H 561. 1 propyl amide (28) each amino-2-[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine 3. 454 M+H 461. 1 yl}(3-pyridyl))carbonylamino]]-fluorenyl-mercaptopropylamine (2S)-3-amino-2-[(6-(2-cyanophenyl)-2-{[ 2-(3-Fluorophenyl)ethyl]amine 23. 721 M+H 475. 1 base}(3-pyridyl))carbonylamino]-indole, indole-dimercaptopropanamide (2S)-3-amino-2-[(6-(2-cyanophenyl)-2 -{[2-(3-Fluorophenyl)ethyl]amine 11. 072 M+H 448. 1 base}(3^pyridyl))carbonylamino]propionic acid (2S)-2-amino group [(6-(2-cyanophenyl)-2-{[2-(3-fluorobenzene) Ethyl)amine 619 M+H 462. (yl)(3-pyridyl))carbonylamino]propionate (2S)-2-(ethinylamino)-3-[(6-(2-cyanophenyl)-2-{ [2-(3-fluorophenyl)ethyl 1. 639 M+H 504. 1-yl]amino}(3-pyridyl))carbonylamino]propionic acid decyl N-((2S)-2-amino-2-aminemethylaminoethyl)(6-(2-cyano) Benzene 0. 669 M+H 447. 1 yl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3′′pyridinyl))carbenamide N-{(1 S)-l-aminecarboyl-2 -[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)) 629 M+H 489. 1 ethyl]amino}(3-pyridyl))carbonylamino]ethyl}acetamidamine (2S)-2-amino-3-[(6-(2-cyanophenyl)-2- {[2-(3-Fluorophenyl)ethyl]amine 2. 318 M+H 461. 1 yl}(3-pyridyl))carbonylamino]]-fluorenyl-mercaptopropylamine (2S)-2-amino-3-[(6-(2-cyanophenyl)-2-{[ 2-(3-Fluorophenyl)ethyl]amine 8. 179 M+H 475. 1 base}(3-pyridyl))carbonylamino]-N,N-dimethylpropanamide (2S)-2-amino-3-[(6-(2-cyanophenyl)-2 -{[2-(3-Fluorophenyl)ethyl]amine 9. 758 M+H 448. 1 base}(3-pyridyl))carbonylamino]propionic acid (2S)-2-(ethylamino)-3-[(6-(2-cyanophenyl)-2-{[2 -(3-fluorophenyl)ethyl 5. 554 M+H 503. 1 yl]amino}(3-pyridyl)carbonylamino]-N-methylpropanamide 2. 384 M+H 462. 1 (2R)-3-Amino·2-[(6-(2-cyanophenyl)·2-{[2-(3-fluorophenyl)ethyl]amine 270 200823188 IC50 arithmetic mean ion m/ z Chemical name group}(3·pyridyl))carbonylamino]ylidene propionate·N-((lR)-2-amino-1-aminemethylaminoethyl)(6-(2-cyano) Phenyl)_2_{[2_(3- 0. 538 M+H 447. 1 fluorophenyl)ethyl]amino}(3-acridinyl))carboxamide (2R)-3-amino-2-[(6·(2·cyanophenyl)-2-{[ 2-(3-Fluorophenyl)ethyl]amine 0. 274 M+H 461. 1-yl}(3-acridinyl))carbonylamino]-indole-methylpropanamide (2R)-2-amino-3-[(6-(2-cyanophenyl)-2-{ [2-(3-Fluorophenyl)ethyl]amine 2. 29 M+H 462. 1-yl}(3-pyridyl))carbonylamino]propionate decanoate N-((2R)-2-amino-2-amineindolylethyl)(6-(2-cyanophenyl) -2-{[2-(3- 0. 321 M+H 447. 1 fluorophenyl)ethyl]amino}(3-pyridyl))decylamine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine Base} (3-ΰ比pyridine0. 04 M+H 442. 1 base))-Ν-(1,3-oxazol-2-ylindenyl)carbamamine-[(6-cyano(3-acridinyl))methyl](2][2-( 3-fluorophenyl)ethyl]amino group 6_ 1. 245 M+H 452. 1 phenyl(3-pyridyl))carbenamide-{[6·(aminomethyl)(3-acridinyl)]methyl}(2-{[2-(3-fluorophenyl)) Ethyl] 0. 42 M+H 456. 1 Amino}-6-phenyl(3-acridinyl))carboxamide 2-aminol-l-(2-{[2-(3-fluorophenyl)ethyl]amino}-6- Phenyl (3-acridinyl)) b. 451 M+H 352. 1-1-Alcohol N-{[4-(Aminomethyl)(2-acridinyl)]fluorenyl}(6-(2-cyanobenzene) 598 M+H 481. 1 base)·2_ { [2_(3-fluorophenyl)ethyl]amino} (3 - ° ratio σ base)) Amidoxime-[(5-{[(t-butoxy)carbonylamine) (曱2-yl}(2-piperidinyl))methyl](6-(2.cyanophenyl)-2-{[2_(3-fluorophenyl)ethyl]amino}(3-acridine Base)) 68. 638 M+H 581. 1 amidoxime Ν-{[5-(aminomethyl)(2-acridinyl)]methyl}(6-(2-cyanobenzene 0. 515 M+H 481. 1 base)_2_ {|&gt;(3-aminophenyl)ethyl]amino} (3 - gayl)) guanamine N-{[4-(aminoindenyl)(2-acridinyl) ]methyl}(2-{[2_(3_fluorophenyl)ethyl] 1. 215 M+H 456. 1 Amino}-6-phenyl(3-pyridyl))indoline {-{[5·(Aminomethyl)(2·.pyridyl)]indenyl}(2-{[2- (3-fluorophenyl)ethyl] 1. 061 M+H 456. 1 Amino}-6-phenyl(3-acridinyl))carbenamide (6·(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine }(3-吼吼0. 021 M+H 442. 1 base))-Ν-(iso-ylhydrazino)carbamamine 2-{|&gt;(2-{[2_(3-fluorophenyl)ethyl]amino}-6-phenyl (3- Π-pyridyl))-2-hydroxyl. 566 M+H 409. 1 ethethyl]amino}acetamide 271 200823188 IC50 arithmetic mean ion m/z chemical name 15. 082 M+H 438. 1 ethyl-2-{[2-(2-{[2-(3-fluorophenyl)ethyl]amino}-6-phenyl(3"pyridyl))-2-hydroxyethyl] Amino} ethyl acetate 19. 362 M+H 443. 1 1-(2-{[2-(3-Fluorophenyl)ethyl]amino}-6-phenyl(3-acridinyl))-2-[(2-acridinylfluorenyl)amine Base] ethyl-1-ol 0. 416 M+H 432. 1 N-(4-Aminobutyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))- Guanamine 0. 154 M+H 446. 1 N-(5-Aminopentyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))indole Guanamine 244 M+H 460. 1 N-(6-Aminohexyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3·pyridyl))曱醯Amine 0. 032 M+H 495. 1 N-{2-[6-(Aminoguanidino)(2-acridinyl)]ethyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl) Ethyl]amino}(3-acridinyl))carhamamine 0. 252 M+H 470. 1 N-{2-[6-(Aminomethyl)(2-acridinyl)]ethyl}(2-{[2-(3-fluorophenyl)ethyl]amino}-6-benzene Base (3-pyridyl))carhamamine 0. 011 M+H 495. 1 N-{[6-(2-Aminoethyl)(2-acridinyl)]fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl) Ethyl]amino}(3-n-pyridyl)carboxamide 0. 024 M+H 470. 1 N-{[6-(2-Aminoethyl)(2-piperidinyl)]methyl}(2-{[2-(3-fluorophenyl)ethyl]amino}-6-benzene (3-pyridyl))carhamamine 1. 62 M+H 448. 1 N-[2-(2-Aminoethoxy)ethyl](6-(2-cyanophenyl)-2_{[2-(3-fluorophenyl)ethyl]amino}(3 _Pyridinyl)) decylamine 0. 037 M+H 482. 1 (6-(2-Cyanophenyl)_2-{[2-(3-fluorophenyl)ethyl]amino}(3ib σ-decyl))-Ν-{[6-(hydroxymethyl)( 2-acridinyl)]methyl}carbamamine 0. 012 M+H 480. 1 N-{[3-(Aminomethyl)phenyl]fluorenyl}(6-(2.cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3-pyridyl))carhamamine 0. 532 M+H 446. 1 2_[(6_(2-cyanophenyl)_2·{[2-(3-fluorophenyl)ethyl]amino}(3′′pyridinyl))carbonylamino]-N,N-di Methylacetamide 0. 444 M+H 447. 1 N-{2-[(2-Aminoethyl)amino]ethyl}(6-(2-cyanophenyl)-2-{[2-(3-phenylphenyl)ethyl]amine Base} (3-.pyridyl))carbamamine 0. 014 M+H 472. 1 (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-. than butyl))-N-[(2-oxyl) (3-piperidinyl)) fluorenyl] guanamine 0. 015 M+H 44M (6-(2-Cyanophenyl)_2-{[2-(3-fluorophenyl)ethyl]amino}(3-. than butyl))-N-decabine _ 3_ylmercapto)guanamine 272 200823188 IC50 arithmetic mean ion m/z chemical name (6-(2-cyanophenyl)-2-{[2-·(3-fluorophenyl)ethyl]amine Base} (3_ ° is more than pyridine 0. 032 M+H 455. 1 base))-Ν-[(1·曱基叫^坐-3-yl)methyl]methyl st-amine N-{[4·(aminomethyl)phenyl]fluorenyl}(6-(2 -Cyanophenyl)_2-{[2-(3-fluorobenzene 0. 277 M+H 480. 1 yl)ethyl]amino}(3·^pyridyl))carboxamide N-[(6-{[(2-aminoethyl)amino]methyl}(2-.pyridyl) )) 曱基](6-(2-cyanide 0. 019 M+H 524. 1 phenyl))_2·{[2-(3-]phenyl)ethyl]amino}(3′′pyridinyl))decylamine 6-{[(6-(2-cyanophenyl) -2- {[2-(3-Fluorophenyl)ethyl]amino}-3"-pyridyl) 0. 064 M+H 510. 1 carbonylamino]hydrazino}pyridine-2-carboxylic acid oxime ester 6-{[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino group }-3- tons of pyridine) 0. 047 M+H 496. 1 carbonylamino]methyl}pyridine-2-carboxylic acid 6-{[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}- 3_σ pyridine group) 0. 06 M+H 495. 1 carbonylamino]methyl}pyridin-2-decylamine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3 j ratio Acridine 0. 031 M+H 455. 1 base))-Ν-[(1-indolyl-5-yl)indenyl] anthraquinone-(1-{2-[(t-butoxy)carbonylamino]ethyl}- 2-oxy(3-piperidinyl))(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3^pyridinyl 15. 254 M+H 601. 1 base)) decylamine N-[l-(2-aminoethyl)-2-oxy(3-piperidinyl)](6-(2-cyanobenzene) 18. 531 M+H 501. 1 base)-2_{[2_(3-fluorophenyl)ethyl]amino}(3′′pyridinyl))carboxamide (6-(2-cyanophenyl)-2-{[2- (3-fluorophenyl)ethyl]amino}(3-% pyridine)) Ν-(2_{2-oxy_3-[(phenylmethoxy)alkylamino] brigade }Ethyl) 11. 834 M+H 635. 1 Methionamine Ν-[2-(3-Amino-2-oxypiperidinyl)ethyl](6-(2-cyanobenzene) 2. 95 M+H 501. 1 base)-2_{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))carinamide N-{[2-(aminomethyl)phenyl]methyl }(6-(2-Cyanophenyl)-2-{[2-(3-fluorobenzene 0. 024 M+H 480. 1 yl)ethyl]amino}(3·pyridyl:)) decylamine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine }(3-吼吼0. 032 M+H 458. 1 base))-N-[(2-oxyindoleridinyl-3-yl)indolyl] amidoxime-[(2·{2-[(t-butoxy)carbonylamino)ethyl }(3-Aridinyl))indenyl](6-(2-cyanophenyl)-2_{[2_(3-fluorophenyl)ethyl]amino}(indenidinyl)). 47 M+H 595. 1 guanamine 0. 006 M+H 495. 1 ν_([2-(2-Aminoethyl)(3-acridinyl)]methyl}(6-(2-cyanobenzene 273 200823188 IC50 arithmetic mean ion m/z chemical name base)-2_{ [2-(3-Fluorophenyl)ethyl]amino}(3-acridinyl))decylamine N-{2-[3-(aminomethylχ2-acridinylethylcyanobenzene) 0. 31 M+H 495. 1 yl)_2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl)) decylamine N-((3S)·2-oxyπ-pyrrolidinyl (6-(2-cyanophenyl)-2·{[2-(3-fluorobenzene) 246 M+H 444. 1 yl)ethyl]amino}(3′′pyridinyl))decylamine (6-(2-cyanophenyl)·2_{[2-(3·fluorophenyl)ethyl]amino} (3- ° than pyridine 0. 059 M+H 516. 1 base))-N-{[1-(2-transethylethyl)-2-oxy(3-piperidinyl)]methyl}carbamamine-{[1-(2-amino) ))-2-oxo(3-piperidinyl)]fluorenyl}(6-(2-cyanobenzene). 031 M+H 515. 1 base)_2-{|&gt;(3-fluorophenyl)ethyl]amino}(3-indole)) decylamine (6-(2-cyanophenyl)_2-{[2_( 3-fluorophenyl)ethylj-amino}(3-acridinyl))-indole-{[1-(3-diazo-3-azaprop-3-enyl)-2-oxy ( 3-piperidinyl)]曱0. 412 M+H 541. 1 }}carbamamine (6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3- ° pyridine))-N-{ [3-(3- Diazo-3-azapropan-3-enyl)-2-oxy(3-piperidinyl)]-methyl 15. 844 M+H 541. 1 base} guanamine N-[((2 R)pipedyl 2) fluorenyl](6_(2-cyanophenyl)_2-{[2-(3-fluorophenyl) 12. 204 M+H 459. 1 ethyl]amino}pyridinyl))carinamide N-[((2R)-1-indolylpiperidin-2-yl)indenyl](6-(2-cyanophenyl)-2 -{[2-(3- 15. 724 M+H 473. 1 fluorophenyl)ethyl]amino) (3 』.. base)) 曱amine N-[((2R)-1-ethylhydrazinopiperidin-2-yl)methyl](6-(2) -Cyanobenzene 7. 437 M+H 501. 1-yl)-2-{[2_(3-fluorophenyl)ethyl]amino}(3-acridinyl))carbenamide N-{[(2R)-l-(ethylsulfonyl) Piper pi well_2_yl]methyl}(6-(2-cyanobenzene) 793 M+H 551. 1 base)-2·{[2-(3-fluorophenyl)ethyl]amino}(3-.pyridyl))carbenamide (2R)-2-{[(6-(2-cyano) Phenyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3_吼11. 602 M+H 517. 1 pyridine))carbonylamino]methyl}piperidine carboxylic acid oxime ester N-[((2S)-1-ethylindol-4-ylpiperidin-2-yl)methyl](6-( 2-cyanobenzene 6. 789 M+H 515. 1 base)-2-{[2_(3-fluorophenyl)ethyl]amino}(3-.pyridyl))carboxamide (2S)-2-{[(6-(2-cyano) Phenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3) is 10. 062 M+H 531. 1 pyridine))carbonylamino]mercapto}-4-mercaptopiperidinic acid methyl ester N-{[(2R)-l-(2-aminoethylidene) σ chen π well base] methyl }(6-(2-Cyanobenzene 2. 775 M+H 516. 1 base)_2· {[2_(3_fluorophenyl)ethyl]amino} (3) than decyl)) decylamine 4. 893 M+H 530. 1 N-{[(2R)-l-(3-Aminopropyl)piperidin-2-yl]methyl}(6-(2-cyanobenzene 274 200823188 IC50 arithmetic mean ion m/z chemical name Base)_2_{[2-(3-Fluorophenyl)ethyl]aminopyridinyl))carbenamide N-{[(2R)-l-(4.aminobutanyl) σ辰牛基] Base}(6_(2_murine benzene 5. 475 M+H 544. 1 yl)-2_{[2-(3-fluorophenyl)ethyl]aminopyridinyl)carboxamide N-{[(2S)-l-(2-aminoethyl) fluorenyl Slightly well _2_基]曱基}(6-(2_策1. 283 M+H 530. 1 phenyl))-2-{[2-(3.fluorophenyl)ethyl]amino}(3′′pyridyl))decylamine N-{[(2S)-l-(3_amine Propionate based brigade base brigade. Well-2·base] sulfhydryl} (6_(2_cyanide 2. 393 M+H 544. 1 phenyl)-2-(〇(3· phenyl)ethyl]amino}(3_0 thiol))carboxylic acid amine N-{[(2S)-l-(4-aminobutylidene) ice Methylpiperidyl]methyl}(6_(2-cyanide). 322 M+H 558. 1 phenyl))-2-{[2-(3.fluorophenyl)ethyl]amino}(3′′pyridinyl))carboxamide N· {[(2S)_4-(2-amino) Ethyl)piperidin-2-yl]methyl} (6 cyanobenzene) 885 M+H 516. 1 yl)-2-{[2-(3-p-phenyl)ethyl]amino}(3′′pyridinyl))decylamine N_ {[(2SH-(3-Aminopropyl))piperidin Till-2-yl]methyl}(6-0 cyanobenzene 11. 197 M+H 530. 1 base)_2_{[2-(3-fluorophenyl)ethyl]amino}(3′′pyridyl))indoleamine N- {[(2S)-4-(4-aminobutylidene)) σ井冬基]Methyl}(6_(2_cyanobenzene12. 397 M+H 544. 1 yl)_2_{[2-(3-phenylene)ethyl]amino}(3-acridinyl))carbenamide N-{[(2SH-(2-aminoethyl fluorenyl)) Benzyl-2-yl] fluorenyl} (6_(2_cyanide). 97 M+H 530. 1 phenyl)-2-([2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))carboxamide N-{[(2S)-4_(3-amino) Propionyl) small methyl breeze 11 well-2-yl] methyl} (6_(2_cyanide 16. 962 M+H 544. 1 phenyl))-2-{[2-(3-fluorophenyl)ethyl]amino}(3_acridinyl))carbenamide N-{[(2S&gt;4-(4-amino group)醯醯基)Small methyl peptin-2_yl]methyl}(6_(2_cyanide 6. 717 M+H 558. 1 phenyl))-2_{[2_(3-fluorophenyl)ethyl]amino}(3-acridinyl))guanamine 2-(6-(2-cyanophenyl)-2- {[2-(3-Fluorophenyl)ethyl]amino) (3- ° than pyridine 13. 156 M+H 466. 1 base))-N-(3_u-pyridylhydrazino)acetamide N-[((2S)-1,4_diethyl fluorenyl) methyl](6-(2_IL-based) 17. 175 M+H 543. 1 base)-2_{[2_(3-fluorophenyl)ethyl]amino}(3·.pyridyl))indoleamine N-[((2S)_4-methyl brigade u well_2_ Methyl](6-(2-cyanophenyl)-2-{[2_(3~fluoro. 92 M+H 473. 1 phenyl)ethyl]amino}(3-pyridyl))indoline oxime [((2,3-naphthyl-2-yl)indolyl](6-(2-cyanophenyl)_2_{|&gt ;(3-fluorophenyl) 0. 413 M+H 430. 1 ethyl]amino} (3_° pyridine)) decylamine (2R)-2_{[(6-(2-cyanophenyl)-2-{[2_(3-fluorophenyl)) Amino group} (3) is more than 0. 073 M+H 488. 1 pyridine))carbonylamino]methyl)methyl sulfonate methyl ester 0. 248 M+H 437. 1 (2-{[2_(3-fluorophenyl)ethyl]amino}-6-(1-methylcarbazole-winter) (3_σ-pyridyl 275 200823188 IC50 arithmetic mean ion m/z chemical name base ))-N-[(2-oxypyrrolidin-3-yl)methyl]carbenamide (2-{[2-(3-fluorophenyl)ethyl]amino}·6-carbazole- 4-based (3-acridine 0. 18 M+H 423. 1 base))-Ν-[(2-oxypyrrolidin-3-yl)indolyl]carbamamine N-{[(2 R)-l-(2-ylamino) σ ratio σ Dec-2-yl]methyl}(6-(2-carbylbenzene). 116 M+H 502. 1-yl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-taxidyl))guanamine 4-((2R)-2-{[(6-(2) -Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amine 0. 657 M+H 558. 1 base}(3-pyridyl))carbonylamino]methyl}pyrrolidinyl)-4-oxobutanoate N][(2R)-l-(4-hydroxybutanylpyrrolidine-2 -yl]methyl}(6-(2-cyanobenzene 0. 085 M+H 530. 1-yl)-2-{[2-(3-fluorophenyl)ethyl]amino)(3′′pyridinyl))carbenamide N-{[(2R)-l-(2-oxyethyl) Indylpyrrolidin-2-yl]fluorenyl}(2-{[2-(3·Fluoride 1. 784 M+H 481. 1 stupid)ethyl]aminomethylpyrazol-4-yl)(3-pyridyl))carbenamide 4-((2R)-2-{[(2-{[2-(3-fluoro) Phenyl)ethyl]amino} Winter (1-methylcarbazole-4- 3. 935 M+H 537. 1()(3-pyridyl))carbonylamino]methyl}pyrrolidinyl)-4-oxobutanoate N-{[(2R)-l-(4-pyridinyl)σ ratio tJ Each σ -2--2-yl]methyl}(2-{[2-(3-1 1. 456 M+H 509. 1 phenyl)ethyl]amino}-6-(1-indolylpyrazol-4-yl)(3-acridinyl))carbenamide N-[((2R) succinyl) 2-yl)methyl](6-(2-cyanobenzene). 043 M+H 472. 1 base)-2-{[2·(3_fluorophenyl)ethyl]amino}(3′′pyridinyl))carboxamide N-{[(2R)-1 -(methylsulfonyl) Nitrogen-2-yl]methyl}(6-(2-cyanobenzene) 524 M+H 508. 1-yl)-2-{[2-(3.fluorophenyl)ethyl]amino}(3-acridinyl))carbenamide N-{[(2R)-1 -(2-aminoethyl Indenyl)azin-2-yl]methyl}(6-(2-cyanobenzene). 044 M+H 487. 1 base)-2-{[2-(3-fluorophenyl)ethyl]aminopyridinyl))carinamide N-{[(2R)-l-(3-aminopropionyl) nitrogen -2-yl]methyl}(6-(2-cyanobenzene). 045 M+H 501. 1 yl)-2_{[2-(3-fluorophenyl)ethyl]amino}(3-.pyridyl))p-amine N-{[(2R)-1 -(4-aminobutyryl) )nitrogen.丹·2·yl]methyl}(6-(2-cyanobenzene 0. 025 M+H 515. 1 base K2-{[2_(3·fluorophenyl)ethyl]amino}(3′′pyridinyl))carboxamide N-{[(2R)-l-(2-hydroxyethyl)nitrogen π旦-2-yl]methyl}(6-(2·cyanobenzene 0. 04 M+H 488. 1 yl)-2-{[2_(3-fluorophenyl)ethyl]amino}(3-.pyridyl))carbenamide 4-((2R)-2-{ [(6-(2) -Cyanophenyl)-2-{[2-(3-phenylphenyl)ethyl]amine 0. 519 M+H 544. 1 base} (3_° pyridine group)) benzylamino]methyl}azanthyl) oxobutanoic acid methyl N-{[(2R)-1 -(4-hydroxybutanyl) nitrogen. Dan-2-yl]methyl}(6-(2-cyanobenzene) 06 M+H 516. 1 base)-2-{[2_(3_fluorophenyl)ethyl]amino} (3-π ratio decyl)) formamide 2. 501 M+H 472. 1 N-(aza-perhydroazino-2-ylindenyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorobenzene) 276 200823188 IC50 arithmetic mean ion m/z chemistry Name 0. 248 M+H 529. 1 yl)ethyl]amino}(3_°pyridyl)) amidoxime-{[1-(2-aminoethenyl)azahydrohydrogenyl-2-yl]methyl}( 6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(34 pyridine))carboxamide 0. 256 M+H 543. 1 N-{[H3-Aminopropenyl) aza-perhydroazin-2-yl J-methyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorobenzene) Ethyl]amino]amino}(3-acridinyl))carboxamide 0. 383 M+H 557. 1 N-{[1 -(4-Aminobutylidene) aza-perhydroazin-2-yl]methyl}(6·(2-cyanophenyl)-2-{[2_(3-fluorobenzene) Ethyl]amino]amino}(3·acridinyl))carboxamide 0. 104 M+H 615. 1 N-[(l-{3-[(Tertidinoxy)carbonylamino]propyl}-2-oxypyrrolidin-3yl)methyl](6-(2-cyanophenyl) -2-{[2-(3-Fluorophenyl)ethyl]amino}(3-acridinyl))carboxamide 0. 382 M+H 515. 1 Ν-{[1-(3-Aminopropyl)-2-oxopyrrolidin-3-yl]methyl}(6-(2-cyanophenyl)-2-{[2-( 3-fluorophenyl)ethyl]amino} (3′′ pyridine)) decylamine 0. 589 M+H 580. 1 Ν-[(1-{3·[(Tertidinoxy)carbonylamino)Jpropyl}-2-oxindyrridin-3-yl)methyl](2-{[2-(3) -Fluorophenyl)ethyl]aminobi b 6-oxazol-4-yl (3-acridinyl))carboxamide 3. 125 M+H 480. 1 N-{[1 -(3-Aminopropyl)-2-oxypyrrolidin-3-ylJ-yl}}-(2-{[2-(3-fluorophenyl)ethyl]amino} -6-pyrazole·4_yl(3-pyridyl))carhamamine 0. 699 M+H 594. 1 Ν_[(ΗΗ(t-butoxy)carbonylamino]propyloxypyrrolidine-3·yl)indenyl](2·{[2-(3-fluorophenyl)ethyl]amino} _6-(1-decylpyrazol-4-yl) (3_° pyridine)) decylamine 5. 504 M+H 494. 1 Ν-{[1-Prolylpropyl)-2-oxoindrolridin-3-yl]methyl}(2-{[2-(3-fluorobenzyl)ethyl]amino} 6-(1-methyl-based sitting base) (3-^ than biting base)) formazan 3. 167 M+H 509. 1 (2Κ&gt;2-{[(2·{[2·(3-fluorophenyl)ethyl]amino}} such as, for example, carbazolyl (3·σ-pyridyl))alkylamino] fluorenyl} ° is slightly more bitter than the third bite 185 M+H 467. 1 N-{[(2R)-l-(2-hydroxyethyl)pyrrolidinyl j-yl}(2_{[2-(3-fluorobenzyl)ethyl]amino}-6-吼嗤-4-base ratio bite base)) guanamine 0. 095 M+H 486. 1 (6 &lt;2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3- σ-pyridyl))-Ν·[(7_oxagen full hydrogen · 2_yl)methyl]cartoamine 0.687 M+H 451.1 (2-{[2-(3·fluoro)ethyl]amino)b &amp; 0 ratio. Sitting on ice base (3_. ))-N-[〇 oxahydrohydrohexyl) fluorenyl]carbamamine 0.603 M+H 465.1 (2-{[2_(3-1 benzyl)ethyl]amine}·6_(1_曱基π比嗤·4·基)(3·ϋ ratio σ定基))-N-[(7-oxaperhydroazino)indolyl]phthalamide 277 200823188 IC50 arithmetic mean ion m/z chemistry Name N-[(l-{3-[(Tertidinoxy)carbonylamino]propyl 7-oxaperhydroazin-2-yl)methyl](6-(2·cyanobenzene) Base)-2-{|&gt;(3-fluorophenyl)ethyl]amino}(3-吼17.15 M+H 643.1 pyridine))carbamamine-{[1-(3-aminopropyl) (7)-oxo-hydrogen nitrogen (oxoazaperhydroepin)-2-yl]fluorenyl}(6-(2-cyanophenyl)-2·{[2-(3- 0.273 M+H 543.1 fluorobenzene) Ethyl]amino]amino}(3-acridinyl))carboxamide N-{[(2R)-l-(4-hydroxybutyryl)pyrrolidinyl]indenyl)(242-(3-fluoro0.963) M+H 495.1 Phenyl)ethyl]amino}-6-° than 嗤-4-yl (3-cadinyl))carbamide N-{[(2R)-l-(2-aminopyridyl) base Nitrogen α _2 · · · · 氟 氟 氟 氟 · · 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯 醯-{[(2R)-l-(2,3·dihydroxypropionyl)azin-2-yl]methyl}(6-(2-cyano0.051 M+H 518.1 phenyl)-2-{ [2-(3-Fluorophenyl)ethyl]amino}(3-η ratio), decylamine (2R)-2- {[(2-{[2-(3-fluorophenyl)) Ethyl]amino} «T--4-yl (3 - ° ratio biting 0.525 M+H 495.1 base)) carbonylamino]methyl}nitrogen decanoic acid tert-butyl N-[((2R) nitrogen哩冬基)methyl](2-{[2-(3-fluorophenyl)ethyl]amine} each mouth ratio 5.442 M+H 395.1 oxazol-4-yl (3-pyridyl))carboxamide N-[2-((2R)-2-{[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}} Base))carbonylamino]mercapto}nitrogen.danylhydroxymethyl 2.482 M+H 617.1 yl)-2-oxoethyl](t-butoxy)decylamine N-{[(2R)-l -((2S)-2-amino-3-hydroxypropionyl)azin-2-yl]methyl}(6-(2.cyanophenyl)-2-{[2-(3_1phenyl) Ethyl]amine-based sand u-pyridyl)) 0.088 M+H 517.1 decylamine N-[(lR)-2-((m)-2-{[(6-(2·cyanophenyl)) -2-{[2-(3-Phenylphenyl)ethyl]amino} (3-° ratio 0 base)) arylamino] fluorenyl }Nitrate 11 and yl) small (transmethyl)_2_ 0.439 M+H 617.1 oxyethyl](t-butoxy)decylamine N-{[(2R)-l-((2 R)- 2-amino-3-hydroxypropionyl)azin-2-yl]fluorenyl}(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl] Amino}(3′′-pyridyl)) 0.083 M+H 517.1 Indoleamine N-[2-((2R)-2-{[(6-(2-cyanophenyl)_2-{[2- (3-Acephenyl)ethyl]amino}(3^pyridyl))carbonylamino]methylindole nitrogen. Danyl) (1§) small (3-aminopropane 1.349 M+H 644.1 yl)-2.oxyethyl](t-butoxy)carbamamine 278 200823188 IC50 arithmetic mean ion m/z chemical name N-{[(2R)-1-((2S)-2,5-diaminopentenyl)azepin-2-yl]methyl}(6-(2_ 0.274 M+H 544.1 cyanophenyl) )-2-{[2_(3_fluorophenyl)ethyl]amino}(34 pyridine))carboxamide N-{[(2R)-l-(2·hydroxyethyl fluorenyl) nitrogen (2-{[2-(3-fluorobenzene 0.559 M+H 453.1))ethyl]amino}-6-pyrazol-4-yl(3-pyridyl))carbenamide N -[((2R)-l-{2-[(Tertibutoxy)carbonylamino]ethyl)}azinyl-2-yl)methyl](2-{[2_(3_fluorophenyl) Ethyl]amino}-6-indazole (3_° pyridine)) 2.989 M+H 552.1 guanamine N-{[(2R)-l-(2-aminoethenyl) nitrogen . -2--2-yl]methyl}(2-{[2-(3-fluorobenzene 0.562 M+H 452.1 yl)ethyl]amino}-6-pyrazol-4-yl (3-ton pyridine) ) indoleamine N-[(6-bromo(2-indolyl))methyl](2-{[2-(3-fluorophenyl)ethyl]amino}-6-port ratio 0.117 M+ H 494.0 oxazol-4-yl(3-acridinyl))carboxamide Ν·({6-[(3-aminopropyl)amino](2-acridinyl)}indenyl) (2- {[2-(3-Fluorobenzene 0.018 M+H 489.1 yl)ethyl]amino}-6-oxazol-4-yl(3-acridinyl))carbenamide-({6-[( 2-Aminoethyl)amino](2-acridinyl)}indenyl)(2-{[2·(3-fluorobenzene 0.02 M+H 475.1 yl)ethyl]amino}-6·pyridyl Zyridin-4-yl(3-pyridyl))decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-oxazol-4-yl (3-acridine 0.039) M+H 476.1 base))-Ν-({6-[(2·hydroxyethyl)amino](2-acridinyl)}methyl)decylamine (2R)-2-{[(2- {[2-(3-Fluorophenyl)ethyl]amino}-6-oxazole·4-yl (3-acridine 0.245 M+H 453.1 base)) benzylamino]methyl}nitrogen N-[((2R) small {3-[(t-butoxy)carbonylamino]propenyl}pyrrolidin-2-yl)indolyl](5·气·2-{[ 2-(3-Fluorophenyl)ethyl]amino}_6_(1-indenyl. Ratio. Gui 0.505 M+H 612.1 _4-yl) (3-pyridyl)) Indoleamine N-{[( 2R)-l-(3-Aminopropionyl)oxaridin-2-yl]fluorenyl}(5-fluoro-2-{{2-(3-fluorophenyl)ethyl]aminomethyl. . sitting base) (3 · υ ratio. set 0.07 M + H 512.1 base)) guanamine N-[((2R)-l-{4-[(t-butoxy)carbonylamino]butanyl}pyrrole Bite winter base) methyl](5_fluoro-2-{[2-(3.fluorophenyl)ethyl]amino}_6_(1-mercapto-sigma-pyrazole 0.483 M+H 626.1 ice-based) (3 -pyridyl))carboxamide N_{[(2R)-l-(4-aminobutylidene)-fluoren-2-yl]methyl}(孓fluoro•2-{[2_(3-fluorophenyl) ) ethyl]amino}_6_(1-methylindazole) (3) than biting 0.087 M+H 526.1 base)) guanamine 0.388 M+H 578.1 Ν-[(2-{[(third Butoxy)carbonylamino]mercapto}(3-u-pyridyl))indenyl] 279 200823188 IC50 arithmetic mean ion m/z chemical name (5-fluoro-2-{[2-(3-fluorobenzene) Ethyl]amino}-6-(1-indolylcarbazol-4-yl)(3-pyridyl))carbenamide N-{[2-(aminomethyl)(3-acridine) Base]]methyl}(5-fluoro-2-{[2-(3-fluorophenyl)0.012 M+H 478.1 ethyl]amino}-6-(1-indolylpyt-4-yl) (3-pyridyl)) decylamine N-[((2R)-l-{3-[(tatabutoxy)carbonylamino]propyl}-5-oxypyrrolidyl) fluorenyl ](5-fluoro-2-{[2 -(3_fluorophenyl)ethyl]amino H-(l-methylhydrazine 0.322 M+H 612.1 oxazol-4-yl)(3-pyridyl))decylamine N-{[(2R)- L-(3-Aminopropyl)-5•oxyoxaridin-2-yl]fluorenyl}(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino} -6-(1-mercaptooxazol-4-yl) (3^pyridinium 0.079 M+H 512.1 base))carbamamine N-{[(2R)-1 -(2,3-dihydroxypropionamidine) Alkyl bromidino-2-yl]methyl}(5-fluoro-2·{[2-(3-fluorophenyl)ethyl]amino}-6-(1-indolylcarbazole-4- (3-(Acridine 0.143 M+H 529.1 base)) decylamine (2-{ 〇(3-fluorophenyl)ethyl]aminopyr-6-[ 1-(2-hydroxyethyl)carbazole -4- 0.972 M+H 461.1 yl](3-acridinyl))-N-(3-acridinylfluorenyl) decylamine (2R)-2-{[(6-(2-cyanobenzene) 5-)-fluoro-2-{[2-(3-fluorophenyl)ethyl]amine 9.038 M+H 562.1 base}(3-pyridyl))carbonylamino]]indenyl}pyrrolidinecarboxylic acid Tributyl ester N-[((2R))-pyridin-2-yl)indenyl](6-(2-cyanophenyl)-5-fluoro-2-{[2-(3- 0.103 M+H 462.1 Fluorophenyl)ethyl]amino)(3-acridinyl))decylamine N-[(2-{[(t-butoxy)carbonylamino]methyl}(3-acridinyl) )) methyl](2-{[2-(3-fluorophenyl)ethyl]amino}-6-[1-(2-hydroxyethyl)carbazole-4- 14.993 M+H 590.1 base](3-pyridyl))guanamine N-{[2-(aminoindenyl)(3-. Pyridyl)]methyl}(2-{[2-(3-fluorophenyl)ethyl] 0.707 M+H 490.1 Amino}-6-[1-(2-hydroxyethyl carbazole-4 -yl](3-acridinyl))carbenamide N-[(2-{[(t-butoxy)carbonylamino]methyl}(3-acridinyl))indolyl] (6- (2-cyanophenyl)-5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino} (3-n-pyridinium 5.358 M+H 599.1)) decylamine N -{[2-(Aminoguanidino)(3-acridinyl)]fluorenyl}(6-(2-cyanophenyl)-5-fluoro0.006 M+H 499.1 •2-{[2-( 3-fluorophenyl)ethyl]amino}(3′′pyridinyl))carboxamide N-[((2R)· 1 — {2-[(t-butoxy)carbonylamino] acetamidine] "Byrrolidin-2-yl)methyl](6-(2-cyanophenyl)-5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amine 2.786 M+H 619.1 base}(3-pyridyl))formamide 280 200823188 IC50 arithmetic mean ion m/z chemical name 0.04 M+H 519.1 N-{[(2R)-l-(2-aminoethenyl)pyrrolidine -2·yl]methyl}(6_(2_cyanophenyl)5-fluoro-2-{[2-(3_lphenyl)ethyl]amino}(3′′pyridinyl))carboxamidine Amine 2.771 M+H 633.1 N-[((2R)-l-{3-[(Tertidinoxy)carbonylamino]propanyl}°pyrrolidine-2·yl)indenyl](6- (2-cyanophenyl)-5-fluoro-2-{[2-(3-fluorophenyl) Ethyl]aminopoline-10!^-based)) formic acid amine 0.042 M+H 533.1 N-{[(2R)-l-(3-aminopropionylfluorenyl-2-yl]methyl) 6-(2-Cyanophenyl)-5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))carhamamine 1.059 M+H 647.1 N-[((2R)-l-{4-[(Tertidinoxy)carbonylamino]butanylpyrrolidin-2-yl)indenyl](6-(2-cyanophenyl)-5 -Fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))carhamamine 0.038 M+H 547.1 N-{[(2R)-l-(4- Aminobutyridinylpyrrolidino-2-yl]fluorenyl}(6-(2-cyanophenyl)-5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino} (3-Acridine))carbamamine 0.845 M+H 633.1 N-[((2R)-l-{3-[(Tertidinoxy)carbonylamino]propyl}-5-oxyanthracene (rheptidin-2-yl)methyl](6-(2-n-phenylphenyl)-5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl) )) Myramine 0.042 M+H 533.1 N-{[(2R)-l-(3-Aminopropyl)·5-oxyindolindin-2-yl]indenyl}(6-(2- Cyanophenyl)-5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino)(3-acridinyl))decylamine 0.11 M+H 550.1 N-{[( 2R)-l-(2,3-dihydroxypropionyl)°pyrrolidin-2-yl]methyl}(6·(2-cyanophenyl)_5_fluoro-2-indole-(3- fluorine Phenyl)ethyl]amino}(3′′pyridyl))decylamine 1.953 M+H 612.1 N-[2-((2R)-2-{[(5-fluoro-2-{[2- (3-fluorophenyl)ethyl]amino}-6-(1-methylpyrazole-4-yl)(3-acridinyl))carbonylamino]indenyl}°pyrrolidyl) (1 S)-l-Methyl-2-oxoethyl](t-butoxy)carbamamine 0.099 M+H 512.1 N-{[(2R)-l-((2S)-2-amine (1,5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-indenyl hydrazide) Zin-4-yl) (3-°-pyridyl) guanamine 19.6 M+H 755.4 N-[((2R)-l-{(2S)-2,5-bis[(T-butoxy) )carbonylamino]pentanyl}. (r-pyridyl) fluorenyl](5-fluoro-2-{[2_(3-fluorophenyl)ethyl]amino}(1-methylpyrazol-4-yl)(3-pyridyl) Methionine 0.078 M+H 555.1 N][(2R)-l-((2s)-2,5-diaminopentenyl carbaryl-2-yl]methyl}(5-fluoro_ 2-{[2_(3-fluorophenyl)ethyl]amino}_6_(1_methylindole) (3-σ ratio σ 281 200823188 IC50 arithmetic mean ion m/z chemical name base)) Formamidine N-l&gt;((2R)-2-{[(5-fluoro-2-{[2-(3-p-phenyl)ethyl]aminoindolyl σ-pyrazol-4-yl)( 3-acridinyl))carbonylamino]methylpyridinyl)(18) small (hydroxyl 1.195 M+H 628.1 methyl)towoxyethyl](t-butoxy)decylamine N- {[(2R)-l-((2S)-2-amino-3-hydroxypropionyl))pyrrolidin-2-yl]methyl}(5-rat-2-{[2·(3 -1 phenyl)ethyl]amino fluorenyl α is ϋ4_ 0.072 M+H 528.1 〇)pyridyl))carbamamine 4-((2R)_2_{[(5-fluoro-2_{[ 2-(3·Fluorophenyl)ethyl]amino}_6·(1_ fluorenyl oxazole) (3-Acridineyl)carbonylamino]methyl}pyrrolidinyl)butoxybutyric acid 0.534 M+H 555.1 oxime ester N_{[(2R)-l-(4-hydroxybutylidene)pyrrolidin-2-yl]fluorenyl}(5-gas-2-{[2-(3-phenylene)) Amino group}- 6-(1-methyl 11 to 11-position-4-yl) (3-11 than 0.245 M+H 527.1 base)) formazan N-[(2-{[(t-butoxy)carbonylamine) Methyl}(3-acridinyl))methyl](5-cyano-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-methyl ton Azole 0.75 M+H 585.1 -4-yl)(3-pyridyl))carboxamide N-{[2-(aminomethyl)(3·-pyridyl)]methyl}(5-cyano) -2-{[2-(3-fluorobenzene 0.05 M+H 485.1 yl)ethyl]amino}-6-(1-mercaptopyrazole yl) (3-pyridyl))carboxamide N- [3-((5R)-5-{[(5-Cyano-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-indolylcarbazole-4- (3-(Acridine))carbonylamino]]indolyl}-2-oxohydrazinyl) 1.15 M+H 619.1 propyl](t-butoxy)decylamine N_{[(2R )-l-(3-Aminopropyl)-5-oxyloxaridin-2-yl]fluorenyl}(5-cyano-2-{[2-(3-fluorophenyl)ethyl] Aminobi 6-(1-methyloxazol-4-yl)(3-indolepyridinium 0.31 M+H 519.1 base))carbamide C2R)-2-{[(5-cyano-2-{ [2-(3-Fluorophenyl)ethyl]amino}-6-(1-indenyl ratio: 2.518 M+H 548.1 oxazolidine) (3-pyridyl))carbonylamino]indenyl}pyrrolidine N-butyl carboxylic acid N-[((2R)%b-bromo-2-yl)methyl](5-cyano-2-{[2-(3-fluorophenyl)) ] 0.281 M+H 448.1 Amino}-6-(1-methylpyrazol-4-yl)(3-pyridyl))carbenamide N-[((2R)-1 - {4-[( Tributoxy)carbonylaminoj-butanyl}pyrrolidin-2-yl)indenyl](5-cyano-2-{[2-(3-fluorophenyl)ethyl]amino}-6(( 1-mercapto. Ratio 1.613 M+H 633.2 oxazol-4-yl)(3-pyridyl)) decylamine 0.211 M+H 533.2 N-{[(2R)-l-(4-aminobutylidene) σ-pyrrolidine-2 -yl]methyl}(5-cyano 282 200823188 IC50 arithmetic mean ion m/z chemical name-2 - {[2-(3-fluorophenyl)ethyl]amino}·6-(1-indenyl) (oxazol-4-yl)(3-acridinyl)) amidoxime-[(2·{[(t-butoxy)carbonylamino]methyl}(3-acridinyl))methyl (2-{[2-(3-fluorophenyl)ethyl]amino}-5-fluorenyl-6-(1-methylcarbazole-4- 1.122 M+H 574.1) (3-pyridine Base))carbamamine {·{[2_(aminomethyl)(3′′pyridyl)J 曱}}(2·{[2-(3-fluorophenyl)ethyl] 0.129 M+H 474.1 Amino}-5-methyl-6-(1-mercaptopyrazole-4-yl)(3-pyridyl))decylamine N-[((2R)-l-{3-[(third Butoxy)carbonylamino]propyl}-5-oxyindole-2-yl)methyl](2-{[2-(3-fluorophenyl)ethyl]amino}-5- Mercapto-6-(1-methyl 1.461 M+H 608.2 pyrazol-4-yl)(3-pyridyl)) amidoxime·{[(2 R)-l-(3-aminopropyl -5-oxypurridin-2-yl]methyl}(2-{[2-(3-fluorophenyl)ethyl]amino}-5-mercapto-6-(1-methyl Carbazole-4-0.577 M+H 508.2 base)(3-pyridyl))carbenamide (2R -2{[(2-{[2-(3-fluorophenyl)ethyl]amino}}-5-fluorenyl-6-(1-indolyl 吼3.702 M+H 537.1 azole-4-yl (3-pyridyl))carbonylamino]]hydrazino}pyrrolidinecarboxylic acid tert-butyl ester N-[((2R))pyridin-2-yl)indenyl](2-{[2-(3) -fluorophenyl)ethylj-amino}-5-0.901 M+H 437.1 methyl-6-(1-indolyl 0 to sputum-4·yl) (3-sigma ratio) N-[((2R)-l-{4-[(Tertidinoxy)carbonylamino]butanyl}pyrrolidin-2-yl)methyl](2-{[2-(3-fluorophenyl) Ethyl]amino}-5-methyl-6-(1-indolyl ruthenium 2.265 M+H 622.3 oxazol-4-yl)(3-pyridyl)) decylamine N-{[(2R)- 1-(4-Aminobutanyl)pyrrolidin-2-yl]indenyl}(2-{[2-(3-fluorophenyl)ethyl]amino}-5-fluorenyl-6-0曱(oxazol-4-yl)(3-acridinyl))methyl 0.381 M+H 522.2 decylamine (2R)-2-{[(5-cyano-2·{[2·(3-fluorophenyl) Ethyl]amino}-6-oxazol-4-yl 6.407 M+H 534.1 (3-pyridyl))carbonylamino]methyl}pyrrolidinecarboxylic acid tert-butyl ester N-[((2R) . Bilobidine I-based fluorenyl](5-cyanofluorophenyl)ethyl] 0.624 M+H 434.1 Amino}-6-pyrazol-4-yl(3·pyridyl))carboxamide N- [((2R)-l-{4_[(Tertidinoxy)carbonylamino]butanyl},pyrrolidinyl)indolyl cyano-2-({2-(3-fluorophenyl)) Ethyl]amino}-6-. Butyrazole·4·yl (3- 3.421 M+H 619.2 pyridyl))carboxamide N-{[(2R)-l-(4·aminobutylidene)-pyridin-2-ylindenyl} -cyano 0.359 M+H 519.2 -2-{[2-(3·fluorophenyl)ethyl]aminocarbazole-m-yl (3-acridinyl)) 曱醯 283 200823188 IC50 arithmetic mean ion m/z Chemical name - -N-[((2R)-l-{3-[(Tertidinoxy)carbonylamino)propyl}-5-oxypyrrolidine 3.506 M+H 605.1 -2-yl) A (5-cyano-2-{[2-(3-fluorophenyl)ethyl]amino}-6"pyrazol-4-yl(3-acridinyl))carbenamide 0.735 M+ H 505.1 N-{[(2R)-l-(3-Aminopropyl)·5-oxyindole-2-yl J-methyl}(5-cyano-2-{[2-(3) -fluorophenyl)ethyl]amino}-6-η-pyrazol-4-yl(3-acridinyl)carbamidine 1.003 M+H 571.1 Ν-[(2-{[(3rd butoxide) Carboxyamino] fluorenyl}(3-acridinyl))methyl](5-cyanophenyl)ethyl]amino]^-. More than salicyl (3-σ ratio decyl)) formamide 0.058 M+H 471.1 Ν-{[2-(amino fluorenyl)(3-.pyridyl)] fluorenyl}(5-cyano) -2·{[2·(3·Fluorophenyl)ethyl]amino}-6-pyrazol-4-yl(3-pyridyl))decylamine 4.252 M+H 595.2 Ν-[(2- {[(Tertidinoxy)carbonylamino]indolyl}(3·-pyridyl))indenyl j(6-(2_ranylphenyl)-2-{[2-(3_fluoro Phenyl)ethyl]amino}·5-fluorenyl (3-hydroxypyridyl)carboxamide 0.158 M+H 495.2 Ν-{[2-(aminomethyl)(3-anthracene)曱]}(6-(2-cyanophenyl)_2_ {[2_(3_fluorophenyl)ethyl]amino}_5·decyl (3_pyridyl))carbenamide 5.372 M+H 629.2 N-[3-((5R)-5-{[(6-(2-Cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}-5-A (3-pyridyl))carbonylamino]indenyl}.2-oxypyrrolidinyl)propyl](t-butoxy)carbamamine 1.226 M+H 529.1 N_{[(2R)-l -(3-aminopropyl)_5-oxypyrrolidine-;2-ylJmethyl}(6-(2-cyanophenyl)-2-{[2·〇1phenyl)ethyl]amine }}-5-methyl (3-σ ratio), guanamine 15.521 M+H 389.0 5_chloro-2-{[2-(3-fluorophenyl)ethyl]aminopyr 6_(1 _曱基^比峻冰基户比 bit_3-carboxymethyl ester 0.414 M+H 594.1 Ν-[(2_{[(2nd-butoxy-ylamino)] yl)}〇° 咬 base)) 曱]](5_气-2_{[2_(3-fluorophenyl)ethyl]amine曱 曱 吡 _ _ _ ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) Chloro 2_{[2-(3-fluorophenyl)ethyl]amino}-6-(1-methylcarbazole-based) (3′′pyridinyl))carbenamide 0.443 M+H 628.2 N -[((2 R)-l-{3-[(Tertidinoxy)carbonylamino]propyloxy fluorenyl) thiol](5_chloro_2_{[2_(3-fluoro Phenyl)ethyl]amino} each (1-methyl 200823188 IC50 arithmetic mean ion m/z chemical name 0.16 M+H 528.1 pyrazol-4-yl) (3-pyridyl))carbenamide N-{ [(2R)-l-(3-Aminopropyl)-5.oxypyrrolidin-2-yl]indenyl}(5-chloro2-{[2-(3-fluorophenyl)ethyl] Amino}-6-(1-indolyloxazolyl)(3-acridinyl))carbenamide 1.601 M+H 557.1 (2R)-2-{[(5-gas-2·{[2 ·(3-Fluorophenyl)ethyl]amino}·6_(1-indolyl σ-pyrazol-4-yl) (3-σ ratio thiol)) benzylamino] sulfhydryl} σ Tert-butyl carboxylic acid 0.167 M+H 457.1 N-[((m-pyrrolidyl)indolyl](5-chloro-2-{[2-(3-)-phenyl)ethyl]aminoindole Benzazole-4-yl)(3-吼Base)) decylamine 0.683 M+H 642.2 N-[((2R)-l-{4_[(t-butoxy)carbonylamino]butanyl}pyrrolidinyl)methyl](5-chloro- 2_{[2·(3·1 phenyl)ethyl]amino}-6_(1-indolyl σ than 嗤-4-yl) (3-σ ratio thiol)) decylamine 0.047 M+H 542.1 Ν·{[(2Κ&gt;1-(4-Aminobutyryl)oxaridin-2-yl]fluorenyl}(5-chloro{ 〇(3-fluorophenyl)ethyl]amino} _6_( 1 -曱 吼 吼 -4- -4-yl) (3 - σ 比 定 ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) -2-{[2-(3·phenylene)ethyl]amino}·6_(1-methyl-rheptylpyryl) (3-° ratio), guanamine 3.957 M+H 415.1 Ν·(3-Aminopropyl)(5_say-2-{[2_(3-fluorophenyl)ethyl]amino]&gt;6-(1-indolylpyrazol-4-yl)(3- Pyridyl)) decylamine 0.1 M+H 458.1 (2R)-H (5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-indenyl). Bis-zolyl)(3-pyridyl))carbonylamino]-2-methylpropionate oxime 3.841 M+H 444.1 (2R)-H(5_fluoro_2-{[2-(3_fluoro) Phenyl)ethyl]amino fluorenyl σ-r-oxazolidine (3·pyridyl))carbonylamino]-2-methylpropanoic acid 0.768 M+H 572.2 2-[(Tertidinoxy)carbonyl Amino]_Ν]3_[(5_fluoro·2·{[2_(3_fluorophenyl)ethyl]amino}-6-(1-mercaptopyrazole) (3•pyridyl)) Aminoamine]propyl} acetamamine 2.494 M+H 472.1 2-amino-indole-{3-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino} -6-(1-mercapto-pyrrolidyl) (3"pyridinyl))aminoamino]propyl}acetamidamine 2.617 M+H 457.1 N-{H(5_H{[2-(3 -fluorophenyl)ethyl]amino}-6-(1-indolylcarbazol-4-yl)-indolinyl)carbonylamino]propyl}acetamide 0.05 M+H 430.1 N-(( 2R)_3- via carbaryl propyl) (5·fluorom {{2·(3·fluorophenyl)ethyl]amino}_6-indolemethylpyrazole yl) pyridyl)) Indoleamine 0.089 M+H 443.1 N-((2R)_2-aminomercaptopropyl) (5H{[2_(3·fluorophenyl)ethyl]amine 285 200823188 IC50 arithmetic mean ion m/z chemical name - }}-6-(1-decylpyrazol-4-yl)(3-pyridyl))carbenamide 0.13 M+H 457.1 (2R)_3_[(5· -2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1·indolylcarbazole 1 yl)(3·pyridyl))carbonylamino]-2-indolyl- N-methylpropionamide 0.024 M+H 424.1 (5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-oxazol-4-yl (3- ° ratio Pyridyl))-N-(pyrazol-3-ylmethyl)decylamine 0.02 M+H 438.1 (5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}- 6-(1-methylcarbazole-tungyl)(3-pyridyl))-N-(pyrazol-3-ylmercapto)carbamamine 0.118 M+H 455.2 N-((2R)-4-Heavy Nitro-2-methyl-4-azabut-4-enyl)(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-methyl Pyrazol-4-yl)(3-pyridyl))carbenamide 10.538 M+H 412.1 5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1 -methyloxazol-4-yl)(3"pyridinyl)3-methylazolyl ketone 1.05 M+H 429.2 team ((28)-3-amino-2-methylpropyl) (5 -Gas-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(1-methylpyrazol-4-yl)(3-pyridyl))decylamine 0.373 M+ H 586.5 N-{(2R)-3-[(5·Gas-2_{[2-(3-fluorophenyl)ethyl]amino}-6-(1-methyl-portazole-4-yl) (3^pyridyl))carbonylamino]-2-mercaptopropyl}-2-[(tatabutoxy)carbonylamino]acetamide 0.152 M+H 486.2 N-{(2R) -3 -[(5-fluoro-2_{[&gt;(3-fluorophenyl)ethyl]amino}-6-(1-methyl-portpyrazolyl)(3-acridinyl))carbonylamino ]-2-mercaptopropyl}-2-aminoacetamide 0.105 M+H 487.1 N-{(2R)-3-[(5-fluoro_2-{[2_(3-fluorophenyl)) Amino]-6-(1-methyl-portyrazole-4-yl)(3-acridinyl))carbonylamino]-2-methylpropyl}-2-hydroxyacetamidine 0.525 M +H 527.1 (2R)-2-{[(5-fluoro_2-{[2-(3-fluorophenyl)ethyl]aminoindolyl σ-pyrazolyl) (3-° ratio) Carbonylamino] fluorenyl}nitrogen levulinic acid third butyl business 1.582 M+H 427.1 N-[((2R)azan-2-yl)indenyl](5-fluoro-2-{[2 -(3-fluorophenyl)ethyl]amino}-6-(1-methyloxazol-4-yl)(3′′pyridinyl))decylamine 0.436 M+H 584.3 N-[(( 2R)-l-{2-[(Tertidinoxy)carbonylamino]ethenyl}azul-2-yl)indenyl](5·fluoro-2-{[2_(3-fluorophenyl) Ethyl]amino}-6-(1-mercaptocarbazole-tungyl)(3-pyridyl))carbenamide 0.05 M+H 484.1 n_{[(2R) small (2-aminoethyl fluorenyl) (5-gas-2-{[2-(3-fluorophenyl)ethyl]amino} each (1-mercaptoindole) (3- U-pyridyl)) decylamine 0.122 M+H 612.3 N-[((2R)-l-{4_[(T-butoxy)carbonylamine Base] Danyl) fluorenyl J(5-fluoro-2-{[2_(3-fluorophenyl)ethyl]amino}-6-(1-methylpyrazolyl) (3-u-pyridyl) )carbamamine 286 200823188 IC50 arithmetic mean ion m/z chemical name N-{[(2R)-l-(4:aminobutylidene) nitrogen progenitor 2-yl]fluorenyl}(5_ fluorine: 2_{[2 -(3- 0.04 M+H 512.1 fluorophenyl)ethyl]amino}-6-(1-methyl吼τι坐-4-yl) (3′′ aryl))carbenamide N-{[( m)-i-(2-hydroxyethyl)nitrogen. And _2_yl]methyl}(5-fluoro_2_{[2-(3- 0.047 M+H 485.2 fluorophenyl)ethyl]amino}-6·(1-methyl. Ratio. Sitting _ 4_base) (3_υ ratio π base)) formamide (2S)-3-[(5_fluoro-2_ {[2_(3_-phenylphenyl)ethyl]amino)b 6-(1-indolyl) ° ratio-4_ 0.141 M+H 458.1 base) (3-acridinyl))carbonylamino; 1-2-methylpropionate N-((2S)_3-hyd roxymercaptopropyl χ5_Fluoro-2-{[2-(3-fluorophenyl)ethyl 0.09 M+H 430.1 yl]aminomercaptopyrazol-4-yl)(3-pyridyl))carbenamide N-(( 2R)·3-hydroxy-2-methylpropyl)(5-is_2-{[2-(3-fluorophenyl)ethyl]amine 0.059 M+H 416.1 base}-6-0 than saliva- 4-based (3-0 ratio bite base)) an amine (2R)-3-[(5-fluoro-2.{[2-(3.fluorophenyl)ethyl])amino group 3_ mouth ratio 0.073 M+H 444.1 pyridine))carbonylamino]-2-methylpropanoic acid methyl ester (2R)-3_[(6-(2-cyanophenyl)-2-{[2-( 3- phenyl)ethyl]amino}(3_吼0.186 M+H 461.1 σ定)) arylamino]-2-mercaptopropanoate N-((2R)-3-hydroxyl -2-mercaptopropyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorobenzene 0.061 M+H 433.2 yl)ethyl]amino}(3-acridinyl) )) indoleamine N-[(2,2-dimethyl(1,3-dioxan-5-yl))methyl](5-fluoro-2- {[2-(3-Fluorobenzene 2.226 M+H 486.2 yl)ethyl]amino fluorenyl σ olvis-4-yl)(3-σΛσ定基))carboxylic acid amine (5-fluoro-2-{[2 -(3-fluorophenyl)ethyl]amino}-6-(1-methyloxazolidine) (3- 0.134 M+H 446.2 σ ratio bite))-N-[3-|^i N-[(2,2-dimethyl(I,3-dioxanyl))indenyl](5-fluoro_2-{ [2_(3-fluorobenzene 0.927 M+H 472.2 yl)ethyl]amino}-6-carbazole-4·yl (3^pyridyl)) decylamine (5-fluoro-2-{[2 -(3-fluorophenyl)ethyl]aminobiphenyl 6-oxazol-4-yl (3-acridine 0.215 M+H 432.2 base))-N-[3_hydroxy_2_(hydroxymethyl)propyl N-[(2,2-dimethyl(1,3-dioxan-5-yl))methyl](6-(2-cyanobenzene 1.023 M+H 489.2)) 2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl))decylamine (6-(2-cyanophenyl)-2-{[2-(3) -fluorophenyl)ethyl]amino}(3- ηpyridinium 0.209 M+H 449.2 base))-indole-[3-hydroxy-2-(hydroxyindenyl)propyl]decylamine (2R)- 2_{[(5_Fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}-6-(diphenyl]pyrazine 0.117 M+H 472.1 -4-yl)(3′′ pyridine Base))carbonylamino]methyl}butyric acid methyl ester ((21〇-2-ethyl-3-hydroxypropyl)(5-fluoro-2-) {[2-(3-Fluorophenyl)ethyl]amine 0.039 M+H 444.1 yl}-6-(1-methyloxazol-4-yl)(3′′pyridinyl))decylamine 287 200823188 IC50 arithmetic mean ion m/z chemical name 0.117 M+H 458.1 (2R)-2-{[(5·fluoro-2:{[2_(3-fluorophenyl)ethyl]amine 丨 吼 吼 吼 吼 基(3_pyridyl))carbonylamino]mercapto}methyl butyrate 0.052 M+H 430.1 N-((2R)_2-ethylhydroxypropyl)(5-fluorodong{[2-(3·fluorobenzene) Ethyl]amino]amino}-6-pyrazole-4.yl(3-acridinyl))carbenamide 90.761 M+H 559.2 (2R)-2_[(Tertibutoxy)carbonylamino] -3·[(5-Gas-2_{[2_(3_fluorophenyl)ethyl]aminobib 6_(1·methylpyrazolyl)(3-pyridyl))alkylamino]propyl Acid oxime ester 0.568 M+H 459.2 (2R)_2_Amino-3-[(5_气-2· {[2_(3_fluorophenyl)ethyl]amino}·6_(1_曱-ylpyridyl) (3-(pyridyl))carbonylamino]methylpropionate 25.925 M+H 531.2 N-((lR)-l-{[(5·fluoro-; 2-{[2-(3- Fluorophenyl)ethyl]amino}·6_(ι·methyl-outazole) (3·α-pyridyl))alkylamino]mercapto}_2_ylidylethyl) (third Butoxy)guanamine 1.258 M+H 431.2 N-((2R)-:2-Amino-3_yl-propyl)(5·说-;2- {[2_(3_fluorophenyl) Ethyl]amino}-6-(1-indolyl 0 to 〇-4-yl) (3-σ ratio thiol)) arylamine 57.166 M+H 517.2 Ν-(( 1 R)-1 - {[(5_ fluoro_2_ {[2_(3-fluorophenyl)ethyl]amino}]-4-yl(3-pyridyl))carbonylamino]methyl}-2-hydroxyethyl) (Third butoxy) decylamine 1.825 M+H 417.2 N-((2R)_2_Amino_3·light propyl) (5-fluoro·2-{[2_(3_fluorophenyl)) Ethyl]amino}-6-pyrazol-4-yl(3-acridinyl))carbenamide 0.307 M+H 432.1 Ν-(2,3-dipropylpropyl)(5-fluoro-2 -{[2-(3-fluorophenyl)ethyl]amino}_6_(μmethylpyrazol-4-yl)(3-pyridyl))carhamamine 0.448 M+H 418.1 N-(2, 3-dipropylpropyl)(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}_6-pyrazol-4-yl(3-pyridyl))carboxamide 86.027 M+H 336.1 (2R)-3-{[2-Amino-5-|L-6-(l-fluorenyl) ratio. -4-yl)(3-π ratio σ-based)] benzylamino}-2-methylpropionate 0.141 M+H 513.1 N-{[(2R)-l-(2*· Methyl propyl ketone) nitrogen. _2_2-yl] fluorenyl}(5·fluoro-2-{[2_(3-fluorophenyl)ethyl]amino}-6-(1-indenyl.pyrazole_4·yl)(3』 Specific bite base)) methotrexate 0.289 M+H 513.1 (2R)-2-{[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino} each, azole (3- 〇 咬 ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) ) Nitrogen-2-yl]fluorenyl}(5_gas_2_{[2-(3-fluorophenyl)ethyl]amino}-6-° ratio ° sitting on ice base (3" than bite base)) Acid amine 200823188 IC50 arithmetic mean ion m/z chemical name N-[((2R) nitrogen.dan-2-yl)methyl](5-i-2-{[2-(3-fluorophenyl)ethyl Amine 0.466 M+H 413.1 base}-6-|7 ratio ° sit-4-yl (3-0 ratio ° base)) formamide N-{[6-(aminomercapto) (2-acridine) Base]]methyl}(2-{[2-(3-fluorophenyl)ethyl] 0.019 M+H 456.1 Amino)-6-phenyl (3·°-pyridyl))decylamine N- {[6-(Aminomethyl)(2-indolyl)]methyl}(6-(2-cyanobenzene 0.009 M+H 481.1 yl)-2-([2-(3-fluorobenzene) Ethyl]amino}amino}(3-0-pyridyl))decylamine N-(aminomethylmethyl)(6-(2-cyanophenyl)-2-{[2_(3- Fluorophenyl)ethyl]amine 0.104 M+H 418.1 base}(3-pyridyl)) Methionine N-(2-aminoformamidoethyl)(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl] 0.099 M+H 432.1 Amino }(3-pyridyl))carbendazim 2-[(6-(2-cyanophenyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-indole ratio Benton base)) 0.102 M+H 432.1 carbonylamino]-indole-methylacetamide N-((3S)-2-oxy(3-piperidinyl))(6-(2·cyanophenyl) -2-{[2-(3-5-fluorobenzene 5.614 M+H 458.1 yl)ethyl]amino} (3-10 fluorenyl)) acesulfame amine Example 14:

2-(3-氟苯乙基胺基)-N十比啶-3-基曱基）-6十比咯啶小基）菸鹼醯胺2-(3-Fluorophenethylamino)-N-decapyridin-3-ylindenyl)-6-decapyridinyl) Nicotinamide

CICI

將2,6-二氯菸鹼酸（19.2 g，0.1 mol)、N，N’-羰基二咪唑 (CDI，17·8 g，0.11 mmol)及 THE (1 L)混合物於 60oC 攪拌 289 200823188 30分鐘並冷卻至室溫。於混合物中加入3-胺基甲基σ比口定 (10·2 mL，0·1 mol)及 DIEA(21 mL, 0·12 mol)。將反應混合 物於室溫攪拌4小時，並以EtOAc稀釋。將有機層以 H20、鹽水清洗，以Na2S04乾燥。將有機溶液濃縮，得 到2,6-二氯-N·(吡啶-3_基曱基)菸鹼醯胺(20.5 g，73%)。 LRMS (M+H+) m/z 282.0 ； (M+2+H+) m/z 283.9 ^Mix 2,6-dichloronicotinic acid (19.2 g, 0.1 mol), N,N'-carbonyldiimidazole (CDI, 17·8 g, 0.11 mmol) and THE (1 L) mixture at 60 ° C 289 200823188 30 Minutes and cooled to room temperature. 3-Aminomethyl σ was added to the mixture (10·2 mL, 0.11 mol) and DIEA (21 mL, 0·12 mol). The reaction mixture was stirred at room temperature for 4 h and diluted with EtOAc. The organic layer was washed with H.sub.2, brine and dried over Na2SO. The organic solution was concentrated to give 2,6-dichloro-N.(pyridin-3-ylmercapto)nicotinamide (20.5 g, 73%). LRMS (M+H+) m/z 282.0 ; (M+2+H+) m/z 283.9^

將2,6-二氯-N-(吡啶_3-基曱基)菸鹼醯胺(20·4 g，72.3 mmol)、3-氟苯乙基胺（li.i g，79·5 mmol)、K2CO3(20g 145 ίο mm〇l)及DMF(200 mL)混合物於100°C攪拌10小時。將 • 混合物以乙酸乙酯稀釋(2 X 300 mL)並以飽和的氯化銨、 碳酸氫鈉及鹽水清洗。將有機層組合、乾燥(MgS04)並濃 縮。將殘餘物以矽膠層析純化，得到6_氯-2-(3-氟苯乙基 &amp;c基)_N十比唆-3-基甲基）於驗隨胺（12.6 g，46%)。LRMS 15 (M+H+) m/z 385.1 °2,6-Dichloro-N-(pyridine-3-ylmercapto)nicotinium amide (20·4 g, 72.3 mmol), 3-fluorophenethylamine (li.ig, 79·5 mmol) A mixture of K2CO3 (20 g 145 ίο mm〇l) and DMF (200 mL) was stirred at 100 ° C for 10 hours. The mixture was diluted with ethyl acetate (2 x 300 mL) and washed with saturated aqueous ammonium chloride, sodium bicarbonate and brine. The organic layers were combined, dried (MgS04) and concentrated. The residue was purified by chromatography to give 6-chloro-2-(3-fluorophenethyl &amp;cyl)-N-de-indol-3-ylmethyl) as the amine (12.6 g, 46%) . LRMS 15 (M+H+) m/z 385.1 °

將6氣2-(3-氣本乙基胺基)_Ν-(σ比咬-3-基曱基)於驗 酿胺（50 mg，〇·13 mmol)及吡咯啶（94 mg，1.3 mmol)置於密 封試管中並150°C於加熱10分鐘。LC/MS顯示反應完全。 將粗產物以MeOH稀釋、過濾並使用乙腈和h2〇混合物 290 20 200823188 於RP-HPLC上純化，得到2_(3_氟苯乙基胺基)_N个比啶_3_6 gas 2-(3-carbylethylamino)_Ν-(σ ratio -3-yl fluorenyl) to the amine (50 mg, 〇·13 mmol) and pyrrolidine (94 mg, 1.3 mmol) Place in a sealed tube and heat at 150 ° C for 10 minutes. LC/MS showed the reaction was complete. The crude product was diluted with MeOH, filtered and purified using EtOAc EtOAc EtOAc EtOAc EtOAc EtOAc

， 基曱基)_6十比咯啶_!_基)於鹼醯胺(20.2 mg，37%)。LRMS (Μ +H+) m/z 420.2。 5 實例15 :, base ))) _6 decapyridinyl _! _ base) in the base amide (20.2 mg, 37%). LRMS (Μ +H+) m/z 420.2. 5 Example 15:

2-(3-象苯乙基胺基)-6-(環物烯)-N-(2-曱基胺基|基曱基)终鹼醯胺 广細 Cl2-(3-Phenylethylamino)-6-(cycloalkenyl)-N-(2-decylamino)-ylindenyl decylamine amide

將酸6-氯-2-(3-氟苯乙基胺基）菸鹼酸（12 g，42 10 mmol) ^ DIPEA (0.69 mL5 4.2 mmol) , HBTU (16 4 2 mmol)及DMF (7 mL)混合物於室溫下攪拌。將胺(3=胺基 甲基)口比咬-2-基）甲基胺曱酸第三丁醋(〇9 g，38 於DMF (3·5 mL)加到將反應混合物中並於室溫攪拌直到 反應完成。將混合物以EtOAc稀釋並以jj2〇、1MNa〇H、 15 鹽水清洗並乾燥(Na2S〇4)。將有機溶液濃縮，並以Et0Ac 及己烧混合物藉由矽膠層分析純化，得到（3_((6_氯_2_(3一 氟苯乙基胺基)菸驗醯胺基）甲基)吡啶_2_基）曱美胺甲 三丁酯（0.9 g，46%)。LC/MS (M+H+) m/z 514 ^ 291 2008231886-Chloro-2-(3-fluorophenethylamino)nicotinic acid (12 g, 42 10 mmol) ^ DIPEA (0.69 mL 5 4.2 mmol), HBTU (16 4 2 mmol) and DMF (7 mL) The mixture was stirred at room temperature. Add amine (3 = aminomethyl) mouth to bite-2-yl) methylamine citrate third butan vinegar (〇9 g, 38 in DMF (3 · 5 mL) was added to the reaction mixture and in the chamber The mixture was stirred with EtOAc and diluted with EtOAc EtOAc (EtOAc). (3_((6-Chloro-2_(3-fluorophenethylamino)) acetamino)methyl)pyridin-2-yl)imumamine tributyl ester (0.9 g, 46%) was obtained. LC/MS (M+H+) m/z 514 ^ 291 200823188

將（3-((6-氯_2-(3 -氟苯乙基胺基)終鹼醯胺基）曱基户比 咬-2-基）甲基胺曱酸第三丁酯（〇Λ 〇 g，〇」9 _〇1)、肆（三苯 基膦）!巴（0) (0.045 g，0.039 mmol)、K2C03 (0.081 g，0.59 5 mmo1)、環戊烯-1·基硼酸（〇·〇26 g，〇·23 mmol)及 NMP (0·2 mL)密封於試管中並以150cC微波3〇分鐘。將反應混合 物經由矽膠塞以EtOAc過濾，以h20、鹽水清洗，以乾 燥(NajO4)並濃縮，得到(3_((6_環戊烯基_2_(3_氟苯乙基胺 基）菸鹼醯胺基）曱基）吡啶-2-基）曱基胺曱酸第三丁酯。 ίο LC/MS (M+H+) m/z 546.2。(3-((6-Chloro-2-(3-fluorophenethylamino))))) 曱 户 -2- -2- -2- -2- -2- -2- -2- -2- 第三 第三 第三 第三〇g,〇"9 _〇1), 肆 (triphenylphosphine)! Bar (0) (0.045 g, 0.039 mmol), K2C03 (0.081 g, 0.59 5 mmo1), cyclopentene-1·ylboronic acid ( 〇·〇26 g, 〇·23 mmol) and NMP (0.2 mL) were sealed in a test tube and microwaved at 150 ° C for 3 minutes. The reaction mixture was filtered through EtOAc EtOAc (EtOAc) eluting NajO4) and concentrated to give (3_((6-cyclopentenyl-2-(3-fluorophenethylamino))nicotinoylamino)indolyl)pyridin-2-yl)decylamine decanoic acid Butyl ester. ίο LC/MS (M+H+) m/z 546.2.

將(3-((6-環環戊烯基-2-(3-氟苯乙基胺基)菸鹼醯胺基) 曱基)吡啶-2-基）曱基胺曱酸第三丁酯溶於MeOH(l mL)中 並於室溫攪拌。逐滴加入HC1/二噁烷(4M, 2 mL)並攪拌直 15 到反應完全。將反應混合物濃縮，並以EtOAc稀釋，以 飽和的碳酸氫鈉、鹽水清洗並乾燥(Na2S04)。將有機層濃 縮，並使用乙腈和H20混合物於RP-HPLC上純化，得到 N-((2-(胺基甲基”比唆-3-基）曱基)-6-環戊烯基-2-(3-氟苯 乙基胺基)菸鹼醯胺之固體(〇·〇26 g，25%)。LC/MS (M+H+) m/z 446.2 0 292 20 200823188 實例16 :(3-((6-Cyclopentenyl-2-(3-fluorophenethylamino))nicotinium)amino)pyridin-2-yl)decylamine decanoic acid tert-butyl ester Dissolved in MeOH (1 mL) and stirred at rt. Add HC1/dioxane (4M, 2 mL) dropwise and stir until the reaction is complete. The reaction mixture was concentrated with EtOAc (EtOAc m. The organic layer was concentrated and purified on RP-HPLC using acetonitrile and H20 to give N-((2-(aminomethyl) </RTI> <RTIgt; -(3-Fluorophenethylamino)nicotinium amide solid (〇·〇26 g, 25%). LC/MS (M+H+) m/z 446.2 0 292 20 200823188 Example 16:

4-(6_(3·氟苯乙基胺基)-5-(吼啶-3-基甲基胺甲醯基）σ比啶-2· 基)-5,6-二氫吡啶-1(2Η)-羧酸甲酯4-(6-(3·Fluorophenethylamino)-5-(acridin-3-ylmethylaminemethanyl) σ-pyridin-2·yl)-5,6-dihydropyridine-1 ( 2Η)-carboxylic acid methyl ester

將2,6-二氯-Ν十比啶_3_基甲基)菸鹼醯胺(234 mg，0·6 mmol)、4-(4,4,5,5、四曱基-l53,2-二氧雜戊硼烷_2_基)_5,6_ 二氫吼咬-1(2Η)-羧酸第三丁酯（234 mg，0.75 mmol)、 ίο Pd(PPh3)4(69 mg· 〇 〇6 mm〇i)、k2C03(249 mg，1.8 mmol) 及DMF(6 mL)混合物於15〇〇c微波中攪拌i小時，然後 濃縮至乾。將殘餘物溶於Et〇Ac_Me〇H (9 :丨，1〇 mL)、 經由矽膠包過濾。將混合物濃縮，接著使用乙腈和H2〇 混合物於RP-HPLC上純化，得到4-(6-(3-氟苯乙基胺 15 基）_5十比啶各基曱基胺曱醯基）吼啶-2-基）-5,6-二氫吼啶 _1(211)-叛酸第三丁酯之淡黃色固體(24〇111§，75%)。1^]^ (M+H+) m/z 532.2 ° 293 2008231882,6-Dichloro-indolylpyridinyl-3-ylmethyl)nicotinamide (234 mg, 0.6 mmol), 4-(4,4,5,5, tetradecyl-l53, 2-Dioxaborolan-2-yl)_5,6-dihydrobite-1(2Η)-carboxylic acid tert-butyl ester (234 mg, 0.75 mmol), ίο Pd(PPh3)4 (69 mg· A mixture of 〇〇6 mm〇i), k2C03 (249 mg, 1.8 mmol) and DMF (6 mL) was stirred in a 15 〇〇c microwave for one hour and then concentrated to dryness. The residue was dissolved in Et EtOAc (EtOAc: EtOAc) The mixture was concentrated and then purified on RP-HPLC using acetonitrile and a mixture of H.sub.2 to afford 4-(6-(3-fluorophenethylamine 15 yl) </ </ </ </ </ 2-yl)-5,6-dihydroacridine_1 (211)-tartrate tartrate pale yellow solid (24 〇 111 §, 75%). 1^]^ (M+H+) m/z 532.2 ° 293 200823188

於4-(6-(3-氟苯乙基胺基)-5十比啶-3-基曱基胺曱醯基) 吡啶-2-基）-5,6·二氫吡咬-1(2H)-羧酸第三丁酯（200 mg， 0.377 mmol)之MeOH (8 mL)溶液中於〇°C及於氮氣壓下 5 加入HC1(2.0 mL，8 mmol, 4 Μ之二噁烷溶液）。將反應混 合物於室溫攪拌4小時。LC/MS顯示反應完成。將反應 混合物減壓濃縮，得到2_(3_氟苯乙基胺基)-Ν-(吼啶-3-基 曱基)-6-(1，2,3,6-四氫吡啶-4-基)菸鹼醯胺，將其用於下個 步驟不需進一步純化。LRMS (Μ +Η+) m/z 444.2。4-(6-(3-Fluorophenethylamino)-5-decapyrid-3-ylmercaptoamine fluorenyl)pyridin-2-yl)-5,6·dihydropyridyl-1 2H)-Dicarboxylic acid tert-butyl ester (200 mg, 0.377 mmol) in MeOH (8 mL) EtOAc (2 mL) ). The reaction mixture was stirred at room temperature for 4 hours. LC/MS showed the reaction was completed. The reaction mixture was concentrated under reduced pressure to give &lt;RTIgt;&quot;&quot;&quot;&quot;&quot;&quot;&quot;&quot;&quot;&quot&&&&&&&&&&&&&&&&&& Nicotinamide, which was used in the next step without further purification. LRMS (Μ +Η+) m/z 444.2.

10 &quot;丨 於 4 (69 mg，0.128 mmol)、DIEA (111 pL，0.640 mmol) 及DCM (2 mL)混合物中於0°C逐滴加入氯曱酸曱酯（12 μ。0.154 mmol)。將混合物於室溫攪拌〇·5小時。將混合 物濃縮，接著使用乙腈和H20混合物於RP-HPLC上純 15 化’得到4-(6-(3-氟苯乙基胺基)-5-(0比咬-3-基曱基胺甲酸 基）吼。定-2-基）-5,6-二氮°比咬-1(2H)-叛酸曱酉旨（33 mg， 53%) 〇 LRMS (M+H+) m/z 490.2。 294 200823188 實例17 使用類似文中所述之製程，合成並試驗下表之化合10 &quot; 曱 曱 chlorohydrazide (12 μ. 0.154 mmol) was added dropwise at 0 °C in a mixture of 4 (69 mg, 0.128 mmol), DIEA (111 pL, 0.640 mmol) and DCM (2 mL). The mixture was stirred at room temperature for 5 hours. The mixture was concentrated, then purified by RP-HPLC using acetonitrile and a mixture of H20 to afford 4-(6-(3-fluorophenethylamino)-5-(0-bito-3-ylmercaptoaminecarboxylic acid吼). -2--2-yl)-5,6-diazepine ratio bite-1 (2H)-rebel acid (33 mg, 53%) 〇LRMS (M+H+) m/z 490.2. 294 200823188 Example 17 Synthesize and test the combination of the following table using a process similar to that described in the text

物。 IC50 算數平均離子 0.3713 M+H 3.7733 M+H 11.4467 M+H 3.4375 M+H 71.3315 M+H 1.4612 M+H 0.3107 M+H 64.7725 M+H 47.5598 M+H 75.0803 M+H 5.4042 M+H m/z化學名稱 (2·{[2-(3-氟笨基）乙基]胺基}-6-哌啶基(3-&lt;咬 434.2基))-Ν-(3-吡啶基甲基）甲醯胺 N-{[(3S)-l-(6-{[2-(3-氟苯基）乙基]胺 S}-5-[N-(3-nH：^基甲基）胺曱酿基](2-0比°定基))σ比 491 ·2 °各唆-3-基]曱基}乙醯胺 (6-((3R)-3-羥基π比咯啶基)-2-{[2-(3-氟苯基）乙基] 402.2胺基}(3-吡啶基))·Ν·(胺曱醯基甲基）甲醯胺 2-[(6-((3R)-3-羥基吼咯啶基)-2-{[2-(3-氟苯基）乙 416.2基]胺基}(3-呢啶基))羰基胺基]-N-甲基乙醯胺 (6-((3R)-3-羥基吼咯啶基)-2-{[2-(3-氟苯基）乙基] 373.2胺基}(3·吡啶基))-N，N-二甲基甲醯胺 N-(胺曱醯基曱基)(2-{[2-(3-氟苯基）乙基]胺 386.2基}-6-吡咯啶基（3-吡啶基)）曱醯胺 (6-[(3R)-3-(羥基甲基)吼咯啶基]-2-{[2-(3-氟苯基) 450.2乙基]胺基}(3^比啶基》-N-(3_吡啶基甲基）甲醯胺 (6-{(3S)-3-[(曱基胺基）甲基]吼咯啶 基卜2-{[2·(3·氟苯基）乙基]胺基}(3-吼啶 463.2基))-Ν-(3-吡啶基甲基）甲醯胺 N-{[(3R)-l-(6-{[2-(3-氟苯基）乙基]胺 基}-5-[&gt;1-(3-吡啶基曱基）胺曱醯基](2-0比啶基))&quot;比 505.2咯啶基]甲基}-Ν·甲基乙醯胺 (6-{(3S)-3-[(二曱基胺基）甲基]吡咯啶 基卜2-{[2-(3-敗苯基）乙基]胺基}(3-咕啶 477.3基))-N-(3-吡啶基甲基）甲醯胺 448.1 (2-{[2-(3-氟苯基）乙基胺基}-6-(2-氧基哌啶基)(3- 295 200823188 IC50 算數平均 16.8833 0.243 1.5893 0.5329 4.5555 0.1306 15.9209 1.0159 0.3825 29.6559 6.9699 59.8594 0.4705 59.7576 離子 m/z化學名稱 吼啶基))-Ν-(3·°比啶基曱基）甲醯胺 Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η (6-[(3S)-3-(胺基甲基)0比咯啶基]·2-{[2-(3·氟苯基) 449.2乙基]胺基}(3-吡啶基))-Ν-(3-吡啶基曱基）曱醯胺 Ν-[(6-胺基(3』比啶基)）甲基](2-{[2·(3-氟苯基）乙 435.2基]胺基}-6-吡咯啶基(3-吡啶基)）曱醯胺 Ν-(2-胺曱醯基乙基)(2-{[2-(3-氟苯基）乙基]胺 400.2基}-6-吡咯啶基（3-吡啶基)）曱醯胺 (6-((3R)-3-羥基吼咯啶基)·2-{[2-(3-氟苯基）乙基] 436.2胺基}(3-吡啶基))-Ν-(3-吡啶基曱基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(2-氧基吼咯啶 434.1基）(3_吡啶基))-Ν-(3-吡啶基甲基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-η比咯啶基(3^比啶 420.2基))-Ν-(3-吡啶基甲基）甲醯胺 (6-((3R)-3-羥基吼咯啶基)-2-{[2-(3-氟苯基）乙基] 416.2胺基}(3-吡啶基))-N-(2-胺曱醯基乙基）甲醯胺 (6-((38)-3-經基°比洛咬基)-2-{[2-(3-氟苯基）乙基] 436.2胺基}(3-吡啶基))-N-(3-吡啶基甲基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-[4-(羥基甲基)娘 464.2啶基](3-吡啶基))-N-(3-吡啶基曱基）甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基卜6-(5-羥基1氧基0展 464.2啶基）(3-吡啶基))-N-(3-吡啶基甲基）甲醯胺 (2-{[2-(3-敗苯基）乙基]胺基}-6-(3-氧基娘啡 449.2基）(3·。比啶基))-N-(3-°比啶基甲基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(4-曱基派畊 449.2基）(3-〇比唆基))-&gt;^-(3-°比°定基曱基）曱酿胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-[4-(2-羥基乙基） 478.2哌啶基](3-吡啶基))-N-(3-吡啶基曱基）甲醯胺 4-(6-{[2-(3-氟苯基）乙基]胺基}-5-[Ν-(3·^σ定基甲 基）胺曱醯基](2-吼啶基))-3-氧基哌畊羧酸第三丁 549.2 S| 296 200823188 IC50 算數平均 70.7815 53.3561 0.4654 0.3292 0.1539 28.4133 67.7779 1.1721 32.8026 14.3105 1.5042 0.3268 0.0146Things. IC50 arithmetic mean ion 0.3713 M+H 3.7733 M+H 11.4467 M+H 3.4375 M+H 71.3315 M+H 1.4612 M+H 0.3107 M+H 64.7725 M+H 47.5598 M+H 75.0803 M+H 5.4042 M+H m/ Zchemical name (2·{[2-(3-fluorophenyl)ethyl]amino}-6-piperidinyl (3-&lt;biting 434.2))-indole-(3-pyridylmethyl) Formamide N-{[(3S)-l-(6-{[2-(3-fluorophenyl)ethyl]amine S}-5-[N-(3-nH:^ylmethyl)amine Brewing base] (2-0 ratio ° base)) σ ratio 491 · 2 ° each 唆-3-yl] fluorenyl} acetamide (6-((3R)-3-hydroxyπpyrrolidyl)- 2-{[2-(3-fluorophenyl)ethyl] 402.2amino}(3-pyridyl))·Ν·(Amidinomethyl)carbamamine 2-[(6-((3R) )-3-hydroxypyridinyl)-2-{[2-(3-fluorophenyl)ethyl 416.2-yl]amino}(3-oxaridinyl))carbonylamino]-N-methylacetamidine Amine (6-((3R)-3-hydroxypyridinyl)-2-{[2-(3-fluorophenyl)ethyl] 373.2 Amino}(3·pyridyl))-N,N- Dimethylmethaneamine N-(amine fluorenyl) (2-{[2-(3-fluorophenyl)ethyl]amine 386.2 yl}-6-pyrrolidinyl (3-pyridyl)) Indoleamine (6-[(3R)-3-(hydroxymethyl)oxaridinyl]-2-{[2-(3-fluorophenyl) 450.2ethyl]amino}(3^pyridyl) 》-N-(3_pyridyl Methionamine (6-{(3S)-3-[(decylamino)methyl]-pyridinyl) 2-{[2·(3·fluorophenyl)ethyl]amino}(3) - acridine 463.2))-Ν-(3-pyridylmethyl)carbamamine N-{[(3R)-l-(6-{[2-(3-fluorophenyl)ethyl]amine }-5-[&gt;1-(3-pyridylfluorenyl)amine fluorenyl](2-0-pyridyl))&quot;Specific 505.2-pyridinyl]methyl}-oxime-methylacetamide (6-{(3S)-3-[(didecylamino)methyl]pyrrolidinyl) 2-{[2-(3-phenylphenyl)ethyl]amino}(3-acridine 477.3 Base))-N-(3-pyridylmethyl)carbamamine 448.1 (2-{[2-(3-fluorophenyl)ethylamino}-6-(2-oxypiperidinyl) ( 3- 295 200823188 IC50 The arithmetic average is 16.8833 0.243 1.5893 0.5329 4.5555 0.1306 15.9209 1.0159 0.3825 29.6559 6.9699 59.8594 0.4705 59.7576 Ion m/z chemical name acridinyl))-Ν-(3·°pyridinyl)carbamamine Μ+ Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η Μ+Η (6-[(3S)-3- (aminomethyl) 0-r-hexidyl]·2-{[2-(3·fluorophenyl) 449.2ethyl]amino}(3-pyridyl))-fluorene-(3-pyridylfluorenyl) Amidoxime-[(6-amino(3"pyridyl))methyl](2-{[2·(3-fluoro) Ethyl)435.2-amino]amino}-6-pyrrolidinyl(3-pyridyl)) amidoxime-(2-aminomercaptoethyl)(2-{[2-(3-fluorophenyl) Ethyl]amine 400.2-based}-6-pyrrolidinyl(3-pyridyl))decylamine (6-((3R)-3-hydroxypyridinyl)·2-{[2-(3- Fluorophenyl)ethyl] 436.2amino}(3-pyridyl))-indole-(3-pyridylfluorenyl)decylamine (2-{[2-(3-fluorophenyl)ethyl)amine -6--6-(2-oxopurine 434.1) (3-pyridyl))-indole-(3-pyridylmethyl)decylamine (2-{[2-(3-fluorophenyl) Ethyl]amino}-6-η-pyridyl (3^pyridyl 420.2))-indole-(3-pyridylmethyl)carbenamide (6-((3R)-3-hydroxyindole) (rhoidyl)-2-{[2-(3-fluorophenyl)ethyl] 416.2amino}(3-pyridyl))-N-(2-aminodecylethyl)carbenamide (6 -((38)-3-carbylpyrazine)-2-{[2-(3-fluorophenyl)ethyl] 436.2amino}(3-pyridyl))-N-(3- Pyridylmethyl)decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-[4-(hydroxymethyl)anthene 464.2 pyridine] (3-pyridyl) -N-(3-pyridylfluorenyl)carbamamine (2-{[2-(3-fluorophenyl)ethyl)amino) 6-(5-hydroxyloxy 0-existing 464.2 pyridine) (3-pyridyl))-N-(3-pyridyl A ) A Amides (2 - {[2- (3-phenyl defeat) ethyl] amino} -6- (3-yl group Mother coffee 449.2) (3 ·. Bisyl))-N-(3-°-pyridylmethyl)decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(4-mercapto Plowing 449.2 Å) (3-〇 唆 )))-&gt;^-(3-° ratio ° 曱 曱 base) 曱 amine (2-{[2-(3-fluorophenyl)ethyl]amine }-6-[4-(2-hydroxyethyl) 478.2 piperidinyl](3-pyridyl))-N-(3-pyridylfluorenyl)carbamamine 4-(6-{[2-( 3-fluorophenyl)ethyl]amino}-5-[Ν-(3·^σ定基 methyl)amine fluorenyl](2-acridinyl))-3-oxypitricin三丁549.2 S| 296 200823188 IC50 arithmetic average 70.7815 53.3561 0.4654 0.3292 0.1539 28.4133 67.7779 1.1721 32.8026 14.3105 1.5042 0.3268 0.0146

離子 M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H m/z 化學名稱 (2-{[2·(3-氟苯基)乙基]胺基}-6-(2-氧基哌畊 449.1基）(3-吡啶基))-Ν-(3·吡啶基曱基）曱醯胺 (2-{[2-(3_氟苯基）乙基]胺基}-6-(2-氧基哌啶 385.1基）(3-吡啶基))-Ν，Ν·二甲基甲醯胺 (6-[(3S)-3-(hyd r氧基曱基）口比咯啶基]-2-{[2-(3-氣 苯基）乙基]胺基}(3-°比啶基))-Ν-(3-吼啶基甲基）曱 450.2醯胺 2-[(2-{[2-(3-氟苯基）乙基]胺基}-6-°比洛咬基(3-U比 400.2啶基))羰基胺基]-Ν-曱基乙醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(3-η比咯啶基)(3-418.1吡啶基))-Ν-(3-吡啶基曱基）曱醯胺 (6-((3S)-3-胺基吼咯啶基)-2-{[2-(3-氟苯基）乙基] 435.2胺基}(3-n比唆基))_N-(3-°比唆基甲基）曱酸胺 N-[(3R)-l-(6-{[2-(3-氟苯基）乙基]胺 S}-5-[N-(3-吼啶基甲基）胺甲醯基](2-吡啶基）)吡 506.2咯啶-3-基](二曱基胺基）曱醯胺 (6-氮σ旦基-2-{[2-(3-氟苯基）乙基]胺基}(3-η比σ定 406.2基))-Ν-(3-ϋ比咬基曱基）甲酿胺 {2-[(2-(2-°比咬基）乙基）胺基]-6-°比洛咬基（3-η比唆 403.2基）}-Ν-(3-σΛσ定基曱基）曱酿胺 {6_(4·曱基哌啶基)_2_[(2·(2』比啶基）乙基)胺基](3_ 431.2 °比σ定基）}σ定基曱基）曱酿胺 (2-{[2_(3_氟苯基）乙基]胺基}-6-(1，3-十圭琳_2-420.1基）(3-吼。定基))-Ν-(3-°比咬基曱基）甲酿胺 (6-((3R)-3-羥基吼咯啶基)_2-{[2-(3-氟苯基）乙基] 胺基}(3_°比啶基))-N-{[2_(胺基甲基)(3_π比啶基)]曱 465.2基}甲醯胺 Ν-{[2-(胺基甲基）(3-吼啶基)]甲基}(6-環戊烯 446·2基_2-{[2-(3·氟笨基）乙基]胺基丨仏^比^定基)）曱醢胺 297 200823188 IC50 算數平均 離子 m/z 化學名稱 - (6-((3S)-3-氟吼咯啶基)-2-{[2-(3-氟苯基）乙基]胺 0.0882 M+H 467.1 基}(3-吼啶基))-N-{[2-(胺基甲基)(3-吼啶基)]曱 基}甲醯胺 0.0313 M+H 467.1 (6-((3R)-3-氟吼咯啶基)-2-{[2-(3-氟苯基）乙基]胺 基}(3-吨啶基))-N-[2-(胺基曱基）(3·-比啶基)]甲基} 曱醯胺 0.0656 M+H 463.2 N-{[2-(胺基曱基)(3-吼啶基)]甲基}(2-{[2-(3-氟苯 基）乙基]胺基卜6_哌啶基（3-吡啶基)）曱醯胺 0.0297 M+H 449.1 N-{[2-(胺基曱基)(3^比啶基)]曱基}(2-{[2-(3-氟苯 基）乙基]胺基卜6-吼咯啶基（3-吼啶基））甲醯胺 12.277 M+H 493.2 N-[(3S)-l-(6-([2-(3-氟苯基）乙基]胺 基}-5-[义(3^比啶基甲基）胺甲醯基](2-。比啶基))。比 咯啶-3-基]曱氧基曱醯胺 0.6271 M+H 470.2 4-(6-{[2-(3-氟苯基）乙基]胺基}-5-{Ν-[(Ν·曱基胺 甲醯基）曱基]胺甲醯基}-2-吼啶基）-1，2,5,6-四氫 吼啶羧酸曱酯 4.5022 M+H 493.2 N-[(3R)-l-(6-{[2-(3-氟苯基）乙基]胺 基}-5-[N-(3吡啶基曱基）胺曱醯基](2-吡啶基))吡 咯啶-3-基]曱氧基曱醯胺 13.1958 M+H 417.1 {6-哌啶基-2-[(2-(2-吼啶基）乙基）胺基](3-n比啶 基）}-N-(3-吡啶基甲基）甲醯胺 35.5447 M+H 435.2 (6-((3R)-3-胺基吼咯啶基)-2-{[2-(3-氟苯基）乙基] 胺基}(3-咣啶基))-N-(3-吡啶基甲基）曱醯胺 0.6872 M+H 432.2 (2-{[2-(3-氟苯基）乙基]胺基}-6-(1，2,5,6-四氫啦啶 基）(3/比啶基）)-N-(3-啦啶基曱基）曱醯胺 0.2341 454.1 (5 -氯ι-2-{[2-(3 -亂苯基）乙基]胺基定基 (3-吼啶基）)-N-(3-咕啶基曱基）曱醯胺 0.1649 445.1 (5 -氣基-2-{[2-(3 -氟苯基）乙基]胺基}-6-σΛ^σ定基 (3-吼啶基）)-Ν-(3-吼啶基曱基）甲醯胺 21.1565 477.1 2-(6-{[2-(3-氟苯基）乙基]胺基}-5-[Ν-(3-吼啶基曱 基）胺曱醯基]-2-吼啶基）-2-咪唑啉羧酸曱酯 298 200823188Ion M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H M+H m/z Chemical name (2-{[ 2-(3-fluorophenyl)ethyl]amino}-6-(2-oxypiped 449.1-) (3-pyridyl))-indole-(3·pyridylfluorenyl)decylamine 2-{[2-(3-fluorophenyl)ethyl]amino}-6-(2-oxypiperidine 385.1)(3-pyridyl))-indole, Ν·dimethylformamide (6-[(3S)-3-(hyd roxyindolyl)-p-pyridyl]-2-{[2-(3-phenylphenyl)ethyl]amino} (3-° pyridine) Base))-Ν-(3-acridinylmethyl)phosphonium 450.2 decylamine 2-[(2-{[2-(3-fluorophenyl)ethyl]amino}-6-° piroxime (3-U ratio 400.2 pyridine))carbonylamino]-indole-mercaptoacetamide (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(3-n ratio (rhoidyl)(3-418.1pyridyl))-indole-(3-pyridylfluorenyl)decylamine (6-((3S)-3-aminopyrrolidinyl)-2-{[2- (3-fluorophenyl)ethyl] 435.2 amino}}(3-n-indenyl))_N-(3-°-pyridylmethyl)decanoic acid N-[(3R)-l-(6- {[2-(3-Fluorophenyl)ethyl]amine S}-5-[N-(3-acridinylmethyl)aminecarboxylidene](2-pyridyl)pyridine 506.2-rhodin-3 -yl](didecylamino)guanamine (6-nitrosyl-denyl-2-{[2-(3-fluorophenyl)ethyl]amino} (3-η ratio σ 406.2 base))-Ν-(3-ϋ 咬 曱 base) 甲 { { { { [ [ [ [ 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 2- 3-η比唆403.2基)}-Ν-(3-σΛσ定基基基) anthraquinone {6_(4·曱-ylpiperidinyl)_2_[(2·(2′′pyridyl)ethyl)amine Base](3_431.2 ° ratio σ base)} σ定基曱 base) an amine (2-{[2_(3_fluorophenyl)ethyl]amino}-6-(1,3- 十圭琳_ 2-420.1 base) (3-oxime. base))-Ν-(3-° ratio thiol thiol) amide (6-((3R)-3-hydroxypyridinyl)_2-{[2 -(3-fluorophenyl)ethyl]amino}(3_°pyridyl))-N-{[2-(methylamino)(3_π-pyridyl)]曱465.2}}Amidoxime- {[2-(Aminomethyl)(3-acridinyl)]methyl}(6-cyclopentene 446·2 base_2-{[2-(3·fluorophenyl)ethyl]amine丨仏^比^定基)) guanamine 297 200823188 IC50 arithmetic mean ion m/z chemical name - (6-((3S)-3-fluoropyridinyl)-2-{[2-(3-fluoro Phenyl)ethyl]amine 0.0882 M+H 467.1 base}(3-acridinyl))-N-{[2-(aminomethyl)(3-acridinyl)]decyl}carbamamine 0.0313 M+H 467.1 (6-((3R)-3-fluoropyridinyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3-tonyl))-N -[2-(曱 ))) (3·-pyridyl)]methyl} guanamine 0.0656 M+H 463.2 N-{[2-(aminomercapto)(3-acridinyl)]methyl}(2- {[2-(3-Fluorophenyl)ethyl]aminopyr-6-piperidinyl(3-pyridyl))decylamine 0.0297 M+H 449.1 N-{[2-(Aminoguanidino) 3^pyridinyl)]fluorenyl}(2-{[2-(3-fluorophenyl)ethyl]aminobi-6-oxaridinyl (3-acridinyl))carbenamide 12.277 M+ H 493.2 N-[(3S)-l-(6-([2-(3-fluorophenyl)ethyl]amino}-5-[yi(3^pyridylmethyl)aminemethanyl] (2-. Bipyridyl)). Biloxidin-3-yl]nonyl decylamine 0.6271 M+H 470.2 4-(6-{[2-(3-fluorophenyl)ethyl]amino}-5-{Ν-[(Ν曱 胺 胺 曱 曱 曱 ] ] ] ] ] 4.5 4.5 4.5 4.5 4.5 4.5 4.5 4.5 4.5 4.5 4.5 4.5 4.5 4.5 022 022 022 022 022 022 022 022 022 022 022 022 022 022 022 022 022 022 022 022 022 022 022 022 -l-(6-{[2-(3-Fluorophenyl)ethyl]amino}-5-[N-(3-pyridylfluorenyl)amine fluorenyl](2-pyridyl))pyrrole Pyridin-3-yl]decyloxyguanamine 13.19958 M+H 417.1 {6-piperidinyl-2-[(2-(2-acridinyl)ethyl)amino](3-n-pyridyl) }-N-(3-Pyridylmethyl)carbamamine 35.5447 M+H 435.2 (6-((3R)-3-Aminopyrrolidinyl)-2-{[2-(3-fluorobenzene) Ethyl]ethyl]amino}(3-acridinyl))-N-(3-pyridylmethyl)decylamine 0.6872 M+H 432.2 (2-{[2-(3-fluorophenyl)) Amino}-6-(1,2,5,6-tetrahydrolylpyridyl)(3/pyridyl))-N-(3-lysylcarbenyl)nonylamine 0.2341 454.1 (5 -chlorom-2-{[2-(3-disorganophenyl)ethyl]amino-based (3-acridinyl))-N-(3-acridinylfluorenyl) decylamine 0.1649 445.1 (5 - gas-based 2-{[2-(3-fluorophenyl)ethyl]amino}-6-σΛ^σ-based (3-acridinyl))-fluorene-(3-acridinylfluorenyl) Formamide 21.1565 477.1 2-(6-{[2-(3-Fluorophenyl)ethyl]amino}-5-[Ν-(3-acridinyl)indolyl]-2-indolyl) -2-imidazolium carboxylate 298 200823188

IC50 算數平均離子 0.4347 0.1186 0.023 6.7754 M+H 0.1249 M+H 0.4299 M+H 10.5122 M+H 2.148 M+H 4.4109 M+H 1.8243 M+H 0.1001 M+H 0.637 M+H m/z化學名稱 (6-(l-氰基(2-τ米唑啉-2_基))-2_{[2-(3-氟苯基）乙 444·1基]胺基}(3·η比唆基))-N-(3-u比唆基曱基）曱醯胺 N-{[(2R)-1-(3-胺基丙基)-5-氧基咐^各唆-2-基]曱 基}(5-氟-2-{[2-(3-氣苯基）乙基]胺基}_6-11比洛咬基 501.2 (3-°比°定基)）甲酸胺 (6-((3R)_3_氟吼咯啶基)-5-氟-2-{[2_(3-氟苯基）乙 基]胺基}(3·-比啶基))-N-{[2-(胺基曱基)(3_,比啶 485.1基)]曱基}曱醯胺 (6-((3R)-3-羥基吼咯啶基)·5_氟_2_{[2气3_氟苯基） 乙基]胺基}(3_η比α定基))-Ν·[(2_{[(第三丁氧基）魏 583·1基胺基]曱基}(3_吡啶基)）曱基]甲醯胺 (6-((3R)-3-羥基吼咯啶基)-5_氟_2-{[2-(3-氟苯基） 乙基]胺基}(3-吼啶基))-Ν-{[2·(胺基曱基)(3_吼啶 483.1基)]甲基}曱醯胺 (6-(1-乙醯基(4-ΐ，2,556-四氫吼啶基）)-2-{[2-(3-氟 本基）乙基]胺基}(3-°比°定基）)-Ν-(3-σΛ^基曱基）甲 474.2醯胺 (2-{[2-(3-氟苯基）乙基]胺基卜6-(4-1，2,5,6-四氫〇比 432·2啶基）(3_吡啶基))-Ν-(3-吡啶基曱基）曱醯胺 4-(6-{[2-(3-氟苯基）乙基]胺基}-5耶-(3_0比啶基曱 基）胺甲醯基]-2-吡啶基）-l，2,5,6-四氫吼啶羧酸第 532.2三丁醋 (6-環戊基-2-{[2-(3-氟苯基）乙基]胺基}(3^比啶 419.2基))-N-(3-u比啶基曱基）曱醯胺 (6-(1，4-二氧雜螺基[45]癸烯冬基)_2_{[2_(3_氟 苯基）乙基]胺基}(3-°比°定基))-Ν-(3-σ&amp;。定基曱基）曱 489·2醯胺 4-(6-{[2-(3_氟苯基）乙基]胺基比啶基曱 基）Jk曱醯基]-2-吼啶基）-1，2,5,6-四氫吼啶羧酸曱 490.2 酯 (6-環戊-1-烯基-2-{[2_(3-氟苯基）乙基]胺基}(3_〇比 417.2啶基))-N-(3-吡啶基曱基）曱醯胺 299 200823188IC50 arithmetic mean ion 0.4347 0.1186 0.023 6.7754 M+H 0.1249 M+H 0.4299 M+H 10.5122 M+H 2.148 M+H 4.4109 M+H 1.8243 M+H 0.1001 M+H 0.637 M+H m/z Chemical name (6 -(l-Cyano(2-τ imiazolin-2-yl))-2_{[2-(3-fluorophenyl)ethyl 444.1]amino}(3·η 唆 ))) -N-(3-u 唆 曱 曱 曱醯) decylamine N-{[(2R)-1-(3-aminopropyl)-5-oxyanthracepin-2-yl] fluorenyl }(5-fluoro-2-{[2-(3-Phenylphenyl)ethyl]amino}_6-11 piroxime 501.2 (3-° ratio ° base)) formic acid amine (6-((3R) )_3_Fluoropyridinyl)-5-fluoro-2-{[2_(3-fluorophenyl)ethyl]amino}(3·-pyridinyl))-N-{[2-(amine (3,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,, Ethyl]amino}(3_η比α定基))-Ν·[(2_{[(Tertidinoxy)Wei 583·1 ylamino] fluorenyl}(3_pyridyl)) fluorenyl] Methionamine (6-((3R)-3-hydroxypyridinyl)-5-fluoro_2-{[2-(3-fluorophenyl)ethyl]amino}(3-acridinyl) )-Ν-{[2·(Aminoguanidino)(3_acridine 483.1)]methyl}decylamine (6-(1-ethylindenyl)- 4-indole, 2,556-tetrahydroacridinyl ))-2-{[2-(3-Fluorobenzyl)ethyl]amine Base}(3-° ratio ° base))-Ν-(3-σΛ^yl fluorenyl)-474.2 decylamine (2-{[2-(3-fluorophenyl)ethyl)aminophenyl 6-( 4-1,2,5,6-tetrahydroindole ratio 432·2 pyridine)(3_pyridyl))-indole-(3-pyridylfluorenyl) decylamine 4-(6-{[2- (3-fluorophenyl)ethyl]amino}-5 y-(3_0-pyridylhydrazinyl)amine carbaryl]-2-pyridyl)-l,2,5,6-tetrahydroacridine carboxylate Acid No. 532.2 Tributyl vinegar (6-cyclopentyl-2-{[2-(3-fluorophenyl)ethyl]amino} (3^pyridyl 419.2))-N-(3-u-bipyridine Amidoxime (6-(1,4-dioxaspiro[45]decene), 2_{[2_(3-fluorophenyl)ethyl]amino} (3-° ratio) °定定))-Ν-(3-σ&amp;. 定基曱基)曱489·2 guanamine 4-(6-{[2-(3-fluorophenyl)ethyl]aminopyridinyl) Jk fluorenyl-2-pyridyl)-1,2,5,6-tetrahydroacridine carboxylic acid hydrazine 490.2 ester (6-cyclopent-1-enyl-2-{[2_(3-fluoro Phenyl)ethyl]amino}(3_〇 ratio 417.2 pyridine))-N-(3-pyridylfluorenyl) decyl 299 200823188

IC50 算數平均離子 15.099 M+H 0.6709 M+H 8.243 M+H 4.1699 M+H 0.1169 M+H 3.3223 M+H 0.4518 M+H 0.2947 M+H 4.3572 M+H 5.7696 M+H 56.4278 M+H 0.3084 M+H m/z化學名稱 N-{(lR)-2-[(5-氟-2-{[2-(3-氟苯基）乙基]胺 基卜6_ϋ比咯啶基（3-n比啶基))羰基胺基]-異丙 561.2基卜2-[(第三丁氧基）羰基胺基]乙醯胺 (2-{[2-(3-氟苯基）乙基]胺基卜6-(4-氧基環己-1-蝉 445.1基)(3·-比啶基))冰(3_吡啶基曱基）曱醯胺 (6-((3R)-3-氟η比咯啶基)_5_氟-2_{[2-(3_氟苯基）乙 基]胺基}(3-吡啶基第三丁氧基）羰基 585·2胺基]曱基}(3-吡啶基)）曱基]曱醯胺 (6-環己基-2-{[2-(3-氟苯基）乙基]胺基}(3 比咬 433.2基))-Ν-(3-吡啶基曱基）甲醯胺 (6-環己·1-烯基_2_{[2_(3_氟苯基）乙基]胺基}(3_〇比 431.2唆基))-Ν-(3-吡啶基甲基）甲醯胺 N-[((2R)_1_{3_[(第三丁氧基）羰基胺基]丙 基}-5_氧基吡咯啶1基）曱基](5_氣·2][2-(夂氟苯 601.2基）乙基]胺基}冬。比略啶基(3-ϋ比啶基)）甲醯胺 (6-[1-(Ν，Ν-二曱基胺曱醯基）(4-1，2,5,6-四氫0比0定 基)]_2_{[2-(3-氟苯基）乙基]胺基}(3-吼啶 503·2基))-Ν-(3-吼啶基曱基）曱醯胺 (5-溴-2-{[2-(3-氟苯基）乙基]胺基}-6-。比咯咬基 498.1 (3-吡啶基）)-N-(3-吡啶基甲基）曱醯胺 土 (2_{[2-(3-氟苯基）乙基]胺基卜6_(1-甲基 (4-1，2,5,6-四氫吡啶基）)(3-吡啶基）)-Ν-(3。比咬某 446.2曱基）曱醯胺 &amp; 4-(6_{[2-(3·氟苯基）乙基]胺基}-5-[N〇b定基f 基）胺曱醯基]-2-°比啶基）-1，4,5,6-四氫。比啶竣IC50 arithmetic mean ion 15.099 M+H 0.6709 M+H 8.243 M+H 4.1699 M+H 0.1169 M+H 3.3223 M+H 0.4518 M+H 0.2947 M+H 4.3572 M+H 5.7696 M+H 56.4278 M+H 0.3084 M +H m/z chemical name N-{(lR)-2-[(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino)b 6-indolepyridyl (3-n Pyridyl))carbonylamino]-isopropyl 561.2-based 2-[(tatabutoxy)carbonylamino]acetamide (2-{[2-(3-fluorophenyl)ethyl]amine 6b (6-((3R)-3-fluoro)比r-pyridinyl)_5_fluoro-2_{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl-tert-butoxy)carbonyl 585·2-amino]indenyl} 3-pyridyl))indenyl]decylamine (6-cyclohexyl-2-{[2-(3-fluorophenyl)ethyl]amino} (3 bites 433.2))-Ν-(3 -pyridylmercapto)carbamamine (6-cyclohexan-1-altyl-2-{{2_(3-fluorophenyl)ethyl]amino} (3_〇 ratio 431.2 唆))-Ν- (3-pyridylmethyl)formamidine N-[((2R)_1_{3_[(Tertidinoxy)carbonylamino]propyl}-5-oxypyrrolidine 1yl)indenyl]( 5_气·2][2-(fluorenylfluorophenyl 601.2-yl)ethyl]amino} Winter. Bilidine (3-ϋ ratio Base))carbamide (6-[1-(Ν,Ν-didecylamine fluorenyl) (4-1,2,5,6-tetrahydro 0 to 0 base)]_2_{[2-( 3-fluorophenyl)ethyl]amino}(3-acridinium 503.2))-indole-(3-acridinylfluorenyl) decylamine (5-bromo-2-{[2-( 3-fluorophenyl)ethyl]amino}-6-. Specific butyl group 498.1 (3-pyridyl))-N-(3-pyridylmethyl) decylamine (2_{[2-( 3-fluorophenyl)ethyl]aminobiphenyl 6-(1-methyl(4-1,2,5,6-tetrahydropyridyl))(3-pyridyl))-oxime-(3. than bite a certain 446.2 mercapto) guanamine &amp; 4-(6_{[2-(3·fluorophenyl)ethyl]amino}-5-[N〇b-decylf-yl)amine fluorenyl]-2- ° pyridine group-1,4,5,6-tetrahydrogen. Biidine

490.2 酯 _文 T (2-{[2-(3-氟苯基）乙基]胺基}-6-(2-味唾琳_2_ 419.1基)(3-吡啶基）)-N-(3-吡啶基曱基）曱醯胺 义{[(211)-1-(4-胺基丁8藍基）1[?比略咬-2-基]甲基}(5 氟-2-{[2-(3-氟苯基）乙基]胺基}-6-11比略1(1 515.2 咬基））甲酸胺 300 200823188490.2 Ester_T-(2-{[2-(3-fluorophenyl)ethyl]amino}-6-(2-flavorin_2_419.1-yl)(3-pyridyl))-N-( 3-pyridyl fluorenyl) decylamine {[(211)-1-(4-aminobutyl 8 yl) 1 [? 略 略 -2- -2-yl] methyl} (5 fluoro-2-{ [2-(3-Fluorophenyl)ethyl]amino}-6-11 ratio 1 (1 515.2 biting)) formic acid amine 300 200823188

IC50 算數平均離子 8.5545 M+H 0.212 M+H 13.6492 M+H 0.0259 M+H 1.7993 6.8551 1.3219 0.1973 M+H 6.3961 M+H 48.4841 M+H 1.5317 M+H 23.1246 M+H m/z 化學名稱 第三丁氧基）幾基胺基]丁醯基}吡 嘻啶基）甲基](5·氟·2_{[2-(3-氟苯基）乙基]胺 615.3基}-6-吡咯啶基（3-吡啶基)）甲醯胺 &amp;{[(211)-1-(2-胺基乙醯基）吡咯啶-2-基]甲基}(5-氟-2-{[2-(3-氣苯基）乙基]胺基}-6-°比嘻淀基（3-11比 487.2啶基)）曱醯胺 N-[((2R)-l-{2_[(第三丁氧基）幾基胺基]乙醯基}0比 洛啶-2-基）甲基](5-氟-2-U2-(3-氟苯基）乙基]胺 587·3基}-6-吡咯啶基（3-吡啶基））甲醯胺 Ν-{[2-(胺基曱基)(3-吼啶基)]甲基}(5_氟 -2-{[2-(3-氟苯基）乙基]胺基}-6-°比洛唆基(3-°比啶 467.1基)）甲醯胺 N-[((2 R)吼哈咬-2-基）曱基](5-氟-2-{[2-(3-氟苯 430 基）乙基]胺基}-6-°比洛《定基（3-吼α定基)）甲酿胺 (2R)_2-{[(5-默·2_{〇(3-氟苯基）乙基]胺基}_6-口比 口各啶基（3-吼啶基))羰基胺基]曱基}吡咯啶羧酸第 530.2三丁酯 N-{[2-(胺基曱基）(3-u比啶基)]甲基}(6_環丙基_5-氟_2_{[2·(3-氟苯基）乙基]胺基}(3_吼啶基)）曱醯 438.1 胺 N-{(lR)-2-[(5-氟-2-{[2-(3-氟苯基）乙基]胺 基}-6-吼咯啶基（3·吡啶基))羰基胺基&gt;異丙 461.2基}-2·胺基乙醯胺 (2-{[2-(3-氟苯基）乙基]胺基}_6-[1-(曱基磺醯 基）(4-1，2,5,6-四氫口比咬基）](3-口比咬基）)-义(3-口比口定 510.2基曱基）曱醯胺 [4-(6-{[2-(3_氟苯基）乙基]胺基}_5_[Ν_(3_σ比啶基 曱基）胺曱醯基](2-η比啶基))旅畊基]_Ν，Ν_二甲基 506.2甲醯胺 4-(6_{[2-(3-氟苯基）乙基]胺基}-5-[Ν-(3-σ比啶基曱 493.2基）胺甲醯基]-2-吡啶基）哌畊羧酸曱酯 435.2 (6-(3-胺基吼咯啶基)-2-{[2-(3-氟苯基）乙基]胺 301 200823188 IC50 算數平均離子 2.6652 M+H 10.5355 M+H 8.2504 M+H 9.4962 M+H 18.4756 M+H 75.9885 M+H 1.062 M+H 3.6861 M+H 5.6018 M+H 2.968 M+H 0.9312 M+H 0.2133 M+H 2.4916 M+H 0.274 m/z 化學名稱 一 基}(3_吡啶基))-N-(3-吡啶基甲基）甲醯胺 (2-{[2-(3-氣本基）乙基]胺基}-6_嗎淋-4-基（3_u比咬 436.2基))-N-(3-吼啶基甲基）曱醯胺 (H(2R)-2-(經基甲基)σ比咯啶基]_2-{[2-(3遗苯 基）乙基]胺基}(3-吼啶基))-Ν-(3-σ比啶基甲基）甲 450.2醯胺 2-[(6-((3S)_3-羥基吼咯啶基)_2-{[2-(3-氟苯基）乙 416.1基]胺基}(3-吡啶基))羰基胺基]_N_甲基乙醯胺 2-[(2_ {[2-(3-氟苯基）乙基]胺基羥基哌咬 430.1基）(3_吡啶基）)羰基胺基]_N_甲基乙醯胺 (第三丁氧基)_Ν-[1-(6-{[2-(3_氟苯基）乙基]胺 基卜5-[N-(3-吼啶基曱基）胺甲醯基](2-吼啶基))0比 535.2咯啶-3-基]曱醯胺 (6-[(3R)-3-(二曱基胺基）吼咯啶基]_2_{[2_(3•氣苯 基）乙基]胺基}(3-吡啶基))-N-(3-吡啶基曱基）甲 463.2醯胺 2-[(6_((3S)-3-氟吡咯啶基)_2][2-(3_氟苯基）乙基] 418.1胺基}(3-吡啶基）)羰基胺基]_N_曱基乙醯胺 2-[(6-((3R)_3-羥基吡咯啶基)·2-{[2_(3-氟苯基）乙 416.1基]胺基}(3-吡啶基）)羰基胺基&gt;队曱基乙醯胺 2-[1-(6-{|&gt;(3-氟苯基）乙基]胺基卜5_价(3』比咬 478.2基曱基）胺曱醢基]-2-u比咬基）吼17各。定_3·基]乙酸 (2 {[2 (3-鼠本基）乙基]胺基}_6-(3-(4-°比咬基）〇比 497·2咯啶基)(3_吼啶基))專(3_吼啶基甲基）甲醯胺 2·[(6_(3,3-二氟吡咯啶基&gt;2_{[2_(3_氟苯基）乙基] 436.1胺基}(3-吡啶基）)羰基胺基]_Ν_甲基乙醯胺 Ν-{[6-(胺基曱基)(2-吼啶基)]曱基}(2_{[2-(3·氟苯 449.2基）乙基]胺基}-6-°比略咬基（3-α比咬基））甲酿胺 (2-{[2-(3-氟苯基）乙基]胺基}_6-[3、(三氟甲基”比 488·2咯啶基](3-吡啶基）)-Ν-(3_吡啶基甲基）甲醯胺 (6-(3,3-二氟吼咯啶基)_2_{[2_(3·氟苯基）乙基]胺 456.1基}(3-°比。定基))-1(3-°比咬基甲基）甲醯胺 302 200823188 IC50 算數平均 離子 m/z 化學名稱 N‘{[6-(胺基甲基)(2』比啶基)]甲基}(2-{[2-(3·氟苯 0.3336 M+H 463.2 基）乙基]胺基}-6-哌啶基(3-吡啶基)）甲醯胺 (6-((3S)-3-羥基啦咯啶基)-2-{[2-(3-氟苯基）乙基] 胺基}(3-吼啶基))-Ν·{[6-(胺基曱基)(2-吼啶基)] 3.0712 M+H 465.1 甲基}甲醯胺 (6-((3R)-3-羥基°比咯啶基)-2-{[2-(3-氟苯基）乙基] 胺基}(3·吼啶基))-N-{[6-(胺基曱基)(2-n比啶基)] 2.2162 M+H 465.2 甲基}甲醯胺 (6-((3 R)-3-氟吼咯啶基)-2-{[2·(3-氟苯基）乙基] 0.1066 M+H 438.2 胺基}(3-吼啶基))·Ν-(3-吼啶基曱基）甲醯胺 (6-[4-(胺基甲基)哌啶基]-2-{[2-(3·氟苯基）乙基] 39.1112 M+H 463.2 胺基}(3-吡啶基))-Ν-(3-吡啶基甲基）甲醯胺 2-[(2-{|；2-(3-氟苯基）乙基]胺基}·6-哌啶基(3-°比啶 1.1175 M+H 414.2 基))羰基胺基]-Ν-曱基乙醯胺 (2-{[2-(3-氟苯基）乙基]胺基卜6-[3-(甲基磺醯基） 11.54 M+H 498.2 °比咯啶基](3-吡啶基))-Ν-(3-吼啶基甲基）甲醯胺 (6-[(2S)-2-(甲氧基甲基户比咯啶基]-2-{[2-(3-氟苯 基）乙基]胺基}(3-吼啶基))-Ν-(3-吼啶基甲基）甲 67.3028 M+H 464.2 醯胺 (第三丁氧基)-Ν-{[1-(6-{[2-(3-氟苯基）乙基]胺 基}-5-[&gt;^-(3-〇比咬基曱基）胺曱驢基](2-10比。定 4.5603 M+H 563.3 基))(4-哌啶基)]甲基}曱醯胺 (第三丁氧基)-Ν-[1-(6-{[2-(3-氟苯基）乙基]胺 &amp;}-5_[N-(3-吼啶基甲基)胺甲醯基](2-π比啶 16.3821 M+H 549.2 基))(4-哌啶基)]曱醯胺 (2-{[2-(3-1苯基）乙基]胺基}-6-(4-羥基-4-苯基哌 16.6585 M+H 526.2 啶基）(3-吡啶基）)-N-(3-吡啶基曱基）曱醯胺 1(6-(1:2-(3-氟苯基）乙基]胺基}-5-[队(3^比啶基甲 1.5586 M+H 506.2 基）胺甲酿基]-2-吼咬基）派啶-4-致酸乙酯 (6-((3S)-3-氟吼咯啶基)-2-{[2·(3-氟苯基）乙基]胺 0.4307 M+H 438.2 基}(3-吡啶基))-Ν-(3-吡啶基甲基）曱醯胺 11.0012 M+H 491.2 (2_{[2-(3-氟苯基）乙基]胺基卜6_[4·(ν-曱基胺甲 303 200823188 IC50 算數平均 離子 m/z 化學名稱 醯基)哌啶基](3··吼啶基))-N-(3-批啶基曱基）甲醯-胺 (2-{[2-(3-氣苯基）乙基]胺基}-6-(4-經基娘咬 0.7562 M+H 450.2 基)(3·吼啶基))-N-(3-吼啶基甲基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-哌畊基(3-吼啶 31.7978 M+H 435.2 基))-N-(3-啦啶基甲基）甲醯胺 (6-((3S)-3-羥基哌啶基)-2-{[2-(3_氟苯基）乙基]胺 0.5153 M+H 450.2 基}(3-吡啶基))-N-(3-吡啶基曱基）曱醯胺 Ν·[1-(6-{[2-(3-氟苯基）乙基]胺基}-5-[N-(3-吼啶 20.7136 M+H 477.2 基甲基）胺甲醯基]-2-吡啶基）吡咯啶-3-基]乙醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-[2-(羥基甲基)嗎 7.2059 M+H 466.2 啉-4-基](3-吼啶基))-N-(3-吡啶基曱基）甲醯胺 (6-[(3S)-3-(曱基胺基）吨咯啶基]-2-{[2-(3-氟苯 基）乙基]胺基}(34b啶基))-N-(3-吼啶基曱基）曱 59.5321 M+H 449.2 醯胺 (2-{[2-(3-氟苯基）乙基]胺 基} -6-(1，4-thiazaperhydroin-4-基）(3-°比淀 1.5743 M+H 452.1 基))-N-(3-。比啶基甲基）甲醯胺 (6-(1，1 -二氧基（1,4-thiazaperhydroin-4-基))-2-{[2·(3-氟苯基）乙基]胺基}(3』比啶 29.8736 M+H 484.2 基))-Ν-(3-吼啶基曱基）甲醯胺 (6-(4-乙酿基σ辰σ井基)-2-{[2-(3 - 1苯基）乙基]胺 8.5678 M+H 477.2 基}(3』比啶基))-N-(3-吡啶基甲基）曱醯胺 (2 _{[2_ (3-氟本基）乙基]胺基σ定基ϋ辰σ定 29.7341 M+H 517.3 基）(3-吡啶基))-Ν-(3-吡啶基甲基）曱醯胺 4_(6-{[2-(3-氟苯基）乙基]胺基比啶基曱 3.1634 M+H 507.2 基）胺曱醯基]-2-。比°定基）旅η井叛酸乙酉旨 304 200823188 實例18 :IC50 arithmetic average ion 8.5545 M+H 0.212 M+H 13.6492 M+H 0.0259 M+H 1.7993 6.8551 1.3219 0.1973 M+H 6.3961 M+H 48.4841 M+H 1.5317 M+H 23.1246 M+H m/z Chemical name third Butoxy)aminoamino]butanyl}pyridinyl)methyl](5.fluoro.2_{[2-(3-fluorophenyl)ethyl]amine 615.3-based}-6-pyrrolidinyl ( 3-pyridyl))carbamamine &amp;{[(211)-1-(2-aminoethyl)pyrrolidin-2-yl]methyl}(5-fluoro-2-{[2-( 3-oxophenyl)ethyl]amino}-6-° than hydrazine (3-11 vs. 487.2 pyridine)) guanamine N-[((2R)-l-{2_[(third) Oxy)aminoamino]ethinyl}0-pyridin-2-yl)methyl](5-fluoro-2-U2-(3-fluorophenyl)ethyl]amine 587·3 base}- 6-pyrrolidinyl(3-pyridyl))carbenamide-{[2-(aminomercapto)(3-acridinyl)]methyl}(5_fluoro-2-{[2-( 3-fluorophenyl)ethyl]amino}-6-°biprodyl (3-° ratio pyridine 467.1))carbamamine N-[((2 R)吼habit-2-yl)曱(5-fluoro-2-{[2-(3-fluorophenyl) 430-yl)ethyl]amino}-6-°Pilo"-based (3-吼α-based) amide (2R)_2 -{[(5-默·2_{〇(3-fluorophenyl)ethyl]amino}_6-portyl acyl (3-oxime) Pyridyl))carbonylamino]mercapto}pyrrolidinecarboxylic acid 530.2 tributyl ester N-{[2-(aminomercapto)(3-u-pyridyl)]methyl}(6-cyclopropyl _5-fluoro_2_{[2·(3-fluorophenyl)ethyl]amino}(3_acridinyl))曱醯438.1 Amine N-{(lR)-2-[(5-fluoro- 2-{[2-(3-Fluorophenyl)ethyl]amino}-6-oxaridinyl (3·pyridyl))carbonylamino group&gt;isopropyl 461.2-based}-2-aminoethyl hydrazine Amine (2-{[2-(3-fluorophenyl)ethyl]amino}_6-[1-(indolylsulfonyl) (4-1,2,5,6-tetrahydro port ratio bite base) )](3-port ratio bite base))--(3-port specific ratio 510.2 fluorenyl) decylamine [4-(6-{[2-(3-fluorophenyl)ethyl]amino) }_5_[Ν_(3_σ-pyridyl)indolyl](2-η-pyridyl)) bridging base]_Ν,Ν_dimethyl 506.2 formamide 4-(6_{[2-( 3-fluorophenyl)ethyl]amino}-5-[Ν-(3-σ-pyridylpurine 493.2-yl)amine-carbamoyl]-2-pyridyl)-peptidyl carboxylic acid oxime ester 435.2 (6- (3-Aminopyrrolidyl)-2-{[2-(3-fluorophenyl)ethyl]amine 301 200823188 IC50 arithmetic mean ion 2.6652 M+H 10.5355 M+H 8.2504 M+H 9.4962 M+H 18.4756 M+H 75.9885 M+H 1.062 M+H 3.6861 M+H 5.6018 M+H 2.968 M+H 0.9312 M+H 0.2133 M+H 2.4916 M+H 0.274 m/z Chemical name-based}(3_pyridyl))-N-(3-pyridylmethyl)carbamamine (2-{[2-(3-carbyl)ethyl) Amino}-6-oxalin-4-yl (3_u ratio bit 436.2))-N-(3-acridinylmethyl)decylamine (H(2R)-2-(radiomethyl) σ Bilobidyl]_2-{[2-(3)phenyl)ethyl]amino}(3-acridinyl))-indole-(3-σ-pyridylmethyl)methyl 450.2 guanamine 2- [(6-((3S)_3-hydroxypyrrolidyl)_2-{[2-(3-fluorophenyl)ethyl 416.1-yl]amino}(3-pyridyl))carbonylamino]]_N_A Ethyl acetamide 2-[(2_{[2-(3-fluorophenyl)ethyl]amino) hydroxypiperidine 430.1 yl)(3-pyridyl))carbonylamino]]N-methylacetamide Third butoxy)-Ν-[1-(6-{[2-(3-fluorophenyl)ethyl]amino) 5-[N-(3-acridinylindolyl)amine-methyl] (2-Acridine))0 to 535.2-bromo-3-yl]decylamine (6-[(3R)-3-(didecylamino)pyridinyl]_2_{[2_(3• Phenyl)ethyl]amino}(3-pyridyl))-N-(3-pyridylfluorenyl)methyl 463.2 decylamine 2-[(6-((3S)-3-fluoropyrrolidinyl)) ][2-(3-Fluorophenyl)ethyl] 418.1amino}(3-pyridyl))carbonylamino]]N-mercaptoacetamide 2-[(6-((3R)_3-hydroxypyrrole) Acridine)·2-{[2_ (3-Fluorophenyl)ethyl 416.1-yl]amino}(3-pyridyl))carbonylamino group&gt;Teamyl acetamide 2-[1-(6-{|&gt;(3-fluorophenyl) Ethyl]aminopurine 5_valent (3" than the biting 478.2 fluorenyl) amidino]-2-u than the bite) 吼17 each. _3·yl]acetic acid (2 {[2 (3-murine)ethyl]amino}}_6-(3-(4-° ratio)) 497 497 497 497 497 497 497 Acridinyl))-(3_acridinylmethyl)carbamamine 2·[(6_(3,3-difluoropyrrolidinyl)&gt;2_{[2_(3_fluorophenyl)ethyl] 436.1 Amino}(3-pyridyl))carbonylamino]-Ν-methylacetamido-{[6-(aminomercapto)(2-acridinyl)]fluorenyl}(2_{[2- (3. fluorobenzene 449.2 yl) ethyl]amino} -6-° ratio slightly biting (3-α ratio bite base)) urethane (2-{[2-(3-fluorophenyl)ethyl) Amino}_6-[3, (trifluoromethyl) to 488. 2 halpyridyl] (3-pyridyl))-indole-(3-pyridylmethyl)carbamidine (6-(3, 3-difluoropyridinyl)_2_{[2_(3.fluorophenyl)ethyl]amine 456.1 yl} (3-° ratio. base))-1 (3-° ratio dimethyl group) formazan Amine 302 200823188 IC50 arithmetic mean ion m/z chemical name N'{[6-(aminomethyl)(2"pyridyl)]methyl}(2-{[2-(3·fluorobenzene 0.3336 M+ H 463.2 yl)ethyl]amino}-6-piperidinyl(3-pyridyl))carbenamide (6-((3S)-3-hydroxylahydropyridinyl)-2-{[2-( 3-fluorophenyl)ethyl]amino}(3-acridinyl))-Ν·{[6-(aminoindenyl)(2-acridinyl)] 3.0712 M+H 465.1 Methyl} Formamide (6-((3R)-3-hydroxylpyrrolidyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3· acridinyl))-N -{[6-(aminomercapto)(2-n-pyridyl)] 2.2162 M+H 465.2 methyl}carbamamine (6-((3 R)-3-fluoropyridinyl)-2 -{[2·(3-fluorophenyl)ethyl] 0.1066 M+H 438.2 Amino}(3-acridinyl))·Ν-(3-acridinylhydrazino)carbenamide (6-[ 4-(Aminomethyl)piperidinyl]-2-{[2-(3.fluorophenyl)ethyl] 39.1112 M+H 463.2 Amino}(3-pyridyl))-Ν-(3- Pyridylmethyl)methaneamine 2-[(2-{|; 2-(3-fluorophenyl)ethyl]amino}·6-piperidinyl (3-° ratio pyridine 1.1175 M+H 414.2 ))carbonylamino]-indole-mercaptoacetamide (2-{[2-(3-fluorophenyl)ethyl)aminodi 6-[3-(methylsulfonyl) 11.54 M+H 498.2 °pyrrolidyl](3-pyridyl))-indole-(3-acridinylmethyl)carbenamide (6-[(2S)-2-(methoxymethyl)pyrrolidyl ]-2-{[2-(3-Fluorophenyl)ethyl]amino}(3-acridinyl))-indole-(3-acridinylmethyl)-methyl 67.3028 M+H 464.2 decylamine Third butoxy)-Ν-{[1-(6-{[2-(3-fluorophenyl)ethyl]amino}}-5-[&gt;^-(3-〇 咬 咬 base Amine thiol] (2-10 ratio. 4.5603 M+H 563.3 base))(4-piperidinyl)]methyl}decylamine (t-butoxy)-indole-[1-(6-{[2-(3-fluorophenyl)) Ethyl]amine &amp;}-5_[N-(3-acridinylmethyl)aminemethanyl](2-π-pyridyl 16.3821. M+H 549.2 base))(4-piperidinyl)]oxime Amine (2-{[2-(3-1phenyl)ethyl]amino}-6-(4-hydroxy-4-phenylpiped 16.655 M+H 526.2 pyridine)(3-pyridyl))- N-(3-pyridylfluorenyl)guanamine 1(6-(1:2-(3-fluorophenyl)ethyl]amino}-5-[team (3^pyridylyl 1.5586 M+ H 506.2 amide (amino) aryl]-2-indole) pyridin-4-acid ethyl ester (6-((3S)-3-fluoropyridinyl)-2-{[2·(3 -fluorophenyl)ethyl]amine 0.4307 M+H 438.2 base}(3-pyridyl))-indole-(3-pyridylmethyl)decylamine 11.0012 M+H 491.2 (2_{[2-(3 -fluorophenyl)ethyl]aminodibu 6_[4·(ν-decylamine A 303 200823188 IC50 arithmetic mean ion m/z chemical name fluorenyl) piperidinyl](3·· acridinyl))- N-(3-b-pyridylhydrazinyl)formamidine-amine (2-{[2-(3-phenylphenyl)ethyl]amino}-6-(4- via maiden bite 0.7562 M+H 450.2 (3. acridine))-N-(3-acridinylmethyl)decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-piped (3-Acridine 31.7978 M+H 435.2 base))-N-(3-Pyridinylmethyl)carbamidine (6-((3S)-3-hydroxypiperidinyl)-2-{[2- (3_fluorophenyl)ethyl]amine 0.5153 M+H 450.2 base}(3-pyridyl))-N-(3-pyridylfluorenyl) amidoxime·[1-(6-{[2 -(3-fluorophenyl)ethyl]amino}-5-[N-(3-acridine 20.7136 M+H 477.2-methyl)aminomercapto]-2-pyridyl)pyrrolidin-3- Ethylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-[2-(hydroxymethyl)?7.2059 M+H 466.2 phenyl-4-yl](3 -Aridyridyl))-N-(3-pyridylfluorenyl)carhamamine (6-[(3S)-3-(decylamino)torosidinyl]-2-{[2-(3 -fluorophenyl)ethyl]amino}(34b pyridine))-N-(3-acridinyl fluorenyl) hydrazine 59.5321 M+H 449.2 decylamine (2-{[2-(3-fluorophenyl) Ethyl]amino}-6-(1,4-thiazaperhydroin-4-yl) (3-° ratio 1.5743 M+H 452.1 base))-N-(3-. Pyridylmethyl)carbamamine (6-(1,1-dioxy(1,4-thiazaperhydroin-4-yl))-2-{[2·(3-fluorophenyl)ethyl]amine Base}(3" than pyridine 29.8736 M+H 484.2 base))-Ν-(3-acridinyl fluorenyl)methanoamine (6-(4-ethyl-branched σ σ σ well base)-2-{[ 2-(3 -1phenyl)ethyl]amine 8.5678 M+H 477.2 base}(3"pyridinyl))-N-(3-pyridylmethyl)decylamine (2 _{[2_ (3 -Fluorophenyl)ethyl]amino sigma-based ϋ σ 2 29.7341 M+H 517.3 base) (3-pyridyl))-Ν-(3-pyridylmethyl) decylamine 4_(6-{[ 2-(3-Fluorophenyl)ethyl]aminopyridinyl hydrazide 3.1634 M+H 507.2 yl)aminoindenyl]-2-. Than ° ° base) brigade η well rebel acid 酉 304 200823188 Example 18:

(E)-2-(3-氟苯乙基胺基)-6-(丙-1 ·烯基)·Ν-(σ比咬-3-基曱基）於驗醯胺(E)-2-(3-fluorophenethylamino)-6-(propan-1 alkenyl)·Ν-(σ ratio -3-ylindenyl)

5 將酸2,6-二氯菸鹼酸（19·2 g，0.1 mol)、Ν，Ν，-幾基二咪 唑(CDI，17·8 g，0.11 mmol)及 THE (1 L)混合物於 60oC 攪 拌30分鐘並冷卻至室溫。於混合物中加入胺基甲基吼 啶（10.2 mL, 0.1 mol)及 DIEA(21 mL，0·12 mol)。將反應混 合物於室溫攪拌4小時，並以EtOAc稀釋。將有機層以 ίο ^2〇、鹽水清洗，以Na2S04乾燥。將有機溶液濃縮，得到 2,6-二氯-N-(吡啶-3-基甲基)菸鹼醯胺(20.5 g，73%)。LRMS (M+H+) m/z 282·0 ; (M+2+H+) m/z 283·9。5 a mixture of acid 2,6-dichloronicotinic acid (19. 2 g, 0.1 mol), hydrazine, hydrazine, -monodiimidazole (CDI, 17·8 g, 0.11 mmol) and THE (1 L) Stir at 60oC for 30 minutes and cool to room temperature. Aminomethyl acridine (10.2 mL, 0.1 mol) and DIEA (21 mL, 0·12 mol) were added to the mixture. The reaction mixture was stirred at room temperature for 4 h and diluted with EtOAc. The organic layer was washed with brine, dried over Na 2 SO 4 . The organic solution was concentrated to give 2,6-dichloro-N-(pyridin-3-ylmethyl)nicotinamide (20.5 g, 73%). LRMS (M+H+) m/z 282·0; (M+2+H+) m/z 283·9.

將2,6-二氯-Ν-(吡啶-3-基曱基)菸鹼醯胺(20.4 g，72·3 15 mmol)、3-氟苯乙基胺（11·1 g，79·5 mmol)、K2CO3(20 g 145 mmol)及DMF(200 mL)混合物於l〇〇°C攪拌l〇小時。將混 305 200823188 合物以乙酸乙酯（2 X 300 mL)稀釋，並以飽和的氯化銨、 碳酸氫鈉及鹽水清洗。將有機層組合，乾燥(MgS〇4)並濃 縮。將殘餘物以矽膠層析純化，得到所欲產物6_氯_2_(3_ 氟 苯乙基胺基）基甲 5 基)於驗酸胺（12.6 g，46%). LRMS (M+H+) m/z 385.1。2,6-Dichloro-indole-(pyridin-3-ylmercapto)nicotinium amide (20.4 g, 72·3 15 mmol), 3-fluorophenethylamine (11·1 g, 79·5 Mixture of mmol), K2CO3 (20 g 145 mmol) and DMF (200 mL) was stirred at 10 ° C for 1 hour. The mixed 305 200823188 was diluted with ethyl acetate (2 X 300 mL) and washed with saturated aqueous ammonium chloride, sodium bicarbonate and brine. The organic layers were combined, dried (MgS〇4) and concentrated. The residue was purified by silica gel chromatography to give the desired product 6-chloro-2-(3-fluorophenethylethylamino)methyl-5 as the acid amine (12.6 g, 46%). LRMS (M+H+) m/z 385.1.

將氯化物6-氯-2-(3-氟苯乙基胺基)-N-(吼啶各基甲基) 於驗驢胺（100 mg，0.260 mmol)、反式-1-丙稀-1-基石朋酸(27 ίο mg，0.312 mmol)、PdCl2(dppf)2(14 mg，0.026 mmol)、2N K2CO3(0.39 mL，0.78 mmol)及 ΤΗΕ(1·5 mL)混合物於 125°C攪拌30分鐘。將混合物經由矽膠墊過濾並以EtOAc 清洗。將濾液濃縮至乾並使用乙腈和H2〇混合物於 RP-HPLC上純化，得到（E)-2-(3-氟苯乙基胺基）各（丙小 15 烯基）-N-(吡啶-3-基曱基）菸鹼醯胺之淡黃色固體（59 mg， 86%)。LRMS (M+H+) m/z 391.2。 實例19 :Chloride 6-chloro-2-(3-fluorophenethylamino)-N-(acridinemethyl) was tested on decylamine (100 mg, 0.260 mmol), trans-1-propene- Mixture of 1-keshiponic acid (27 ίο mg, 0.312 mmol), PdCl 2 (dppf) 2 (14 mg, 0.026 mmol), 2N K2CO3 (0.39 mL, 0.78 mmol) and hydrazine (1.5 mL) at 125 ° C 30 minutes. The mixture was filtered through a pad of EtOAc and washed with EtOAc. The filtrate was concentrated to dryness and purified on RP-HPLC using acetonitrile and a mixture of H.sub.2, to afford (E)-2-(3-fluorophenethylamino) each (propenyl 15 alkenyl)-N-(pyridine- 3-methoxyindolyl nicotinamide light yellow solid (59 mg, 86%). LRMS (M+H+) m/z 391.2. Example 19:

306 200823188 2-(3-氟苯乙基胺基)-6-(氰基亞胺酰胺)-N十比啶-3-基甲基)菸鹼醯胺306 200823188 2-(3-Fluorophenethylamino)-6-(cyanoimidoamide)-N-depyridin-3-ylmethyl)nicotinate

將6-氯-2-(3-氟苯乙基胺基)-N-(吼啶-3-基曱基)菸鹼 酉龜胺（1·3 g，3.3 mmol)、NiBr2 (1·1 g，4.9 mmol)、NaCN (0.48 g，9·8 mmol)及NMP (6 mL)混合物於220°C攪拌1小時。 將反應混合物經由矽藻土以EtOAc過濾。將有機層以水、 鹽水清洗，以乾燥(Na2S04)並濃縮，得到腈6-氰基-2-(3-氟苯乙基胺基）-N-(吼啶-3-基甲基）菸鹼醯胺（0.85 g， 69%)。LC/MS (M+H+) m/z 376」。6-Chloro-2-(3-fluorophenethylamino)-N-(acridin-3-ylindenyl)nicotinamide (1·3 g, 3.3 mmol), NiBr2 (1·1) A mixture of g, 4.9 mmol), NaCN (0.48 g, 9·8 mmol) and NMP (6 mL) was stirred at 220 ° C for one hour. The reaction mixture was filtered with EtOAc over EtOAc. The organic layer was washed with water and brine, dried (Na.sub.2SO.sub.sub.sub.sub.sub.sub.sub.sssssssssssssssssssssssss Base decylamine (0.85 g, 69%). LC/MS (M+H+) m/z 376.

於以乾冰丙酮冷凝器固定之三頸圓底燒瓶中裝入腈 6-氰基-2-(3 -氟苯乙基胺基比咬-3-基曱基）於驗隨胺 (0·10 g，0.27 mmol)、EtOH (2 mL)並與 HCI(g)攪拌 20 分鐘。 然後將反應混合物濃縮至乾，得到6-(3-氟苯乙基胺 15 基)-5-(吡啶-3-基曱基胺曱醯基）曱吡啶亞胺酸乙酯。LC/MS (M+H+) m/z 422.1。A three-necked round bottom flask fixed in a dry ice acetone condenser was charged with a nitrile 6-cyano-2-(3-fluorophenethylamino group hexane-3-yl fluorenyl group) in the test amine (0·10). g, 0.27 mmol), EtOH (2 mL) and stirred with HCI (g) for 20 min. The reaction mixture was then concentrated to dryness to give 6-(3-fluorophenethylamine 15 yl)-5-(pyridin-3-ylmercaptoamine decyl) pyridine pyridine imidate. LC/MS (M+H+) m/z 4221.

將6-(3-氟苯乙基胺基&gt;5_卜比啶-3-基曱基胺甲醯基）曱 307 200823188 吡啶亞胺酸乙酯及NH3/MeOH(7N，0.76 mL)混合物於50oC •擾拌30分鐘1小時。將反應混合物濃縮至乾，得到6•曱 脒基-2-(3-氟苯乙基胺基)-N-(吼啶-3-基甲基）菸鹼醯胺。 LC/MS (M+H+) m/z 394.1。6-(3-Fluorophenethylamino)&gt;5-bubidin-3-ylmercaptoaminecarbazide) 307 200823188 Ethyl pyridine imidate and a mixture of NH3/MeOH (7N, 0.76 mL) At 50oC • Spoil for 30 minutes and 1 hour. The reaction mixture was concentrated to dryness to give &lt;RTI ID=0.0&gt;&gt;&&&&&&&&&&&& LC/MS (M+H+) m/z 394.1.

5 π 將6-曱脒基-2-(3-氟苯乙基胺基)-Ν-(吼啶-3-基曱基) 菸鹼醯胺（0.013 g，0.034 mmol)、CNBr(3N，0.017 mL，0.051 mmol)、DIPEA(0.0085 mL，0.051 mmol)之 DCM (0·10 mL) . 混合物於室溫下攪拌直到反應完全。將反應混合物於室溫 10 攪拌4小時，並以EtOAc稀釋濃縮至乾，並使用乙腈和 H20混合物藉由RP-HPLC純化，得到6-(N-氰基甲胨 基)-2-(3-氟苯乙基胺基十比咬-3-基曱基）於驗酿胺之固 體（0·0058 g5 41〇/〇)。LC/MS (M+H+) m/z 418.1。 15 實例20 使用類似文中所述之製程，合成及試驗下表之化合 物0 IC50 算數平均離子m/z 化學名稱 N-{[6-(胺基甲基)(2-σ比σ定基)]甲基}(2-{[2-(3-氟苯基）乙基]胺 7.3929 Μ+Η 457.1基}-5-(3-吼啶基)(3-吡啶基))甲醯胺 9.8364 Μ+Η 457·1 N-{[6-(胺基曱基）(2-吼啶基）]甲基}(2-{[2-(3-氟苯基）乙 308 200823188 IC50 算數平均離子5 π 6-Mercapto-2-(3-fluorophenethylamino)-indole-(acridin-3-ylindenyl) nicotinic acid amide (0.013 g, 0.034 mmol), CNBr (3N, 0.017 mL, 0.051 mmol), DIPEA (0.0085 mL, 0.051 mmol), DCM (0·10 mL). The mixture was stirred at room temperature until the reaction was completed. The reaction mixture was stirred at rt EtOAc (EtOAc) EtOAc (EtOAc m. The fluorophenethylamino group is a solid of the amine (0·0058 g5 41〇/〇). LC/MS (M+H+) m/z 418.1. 15 Example 20 Using the procedure described in the text, synthesize and test the compounds in the table below. IC50 arithmetic mean ion m/z chemical name N-{[6-(aminomethyl) (2-σ ratio σ base)] }}(2-{[2-(3-fluorophenyl)ethyl]amine 7.3929 Μ+Η 457.1 }}-5-(3-acridinyl)(3-pyridyl))carbenamide 9.8364 Μ+ 457 457·1 N-{[6-(aminomercapto)(2-acridinyl)]methyl}(2-{[2-(3-fluorophenyl)ethyl 308 200823188 IC50 arithmetic mean ion

17.7374 M+H 6.0282 M+H 12.683 M+H 17.7243 M+H 17.258 M+H 11.19 M+H 14.887 M+H 9.7159 M+H 11.8154 M+H 15.0424 M+H 16.0219 M+H 44.3072 M+H 55.0688 M+H 38.046 M+H 6.7378 M+H 70.3134 M+H 42.7772 M+H m/z 化學名稱 基]胺基} -5 - (4 -·吼°定基)(3』比咬基)）甲趨胺 N-{[6-(胺基曱基）(2-n比啶基）]曱基氟苯基）乙 46〇·1基]胺基甲基η比唾基)(3』比。定基)）曱醯胺 Ν-{[6-(胺基甲基）(2-吼啶基）]曱基}(5_(2-氰基苯 481.1基)-2-{[2-(3-氟苯基）乙基]胺基吡啶基甲醯胺 (5-氰基-2-{[2-(3-氟苯基）乙基；|胺基比啶基乃以乂孓口比 376.1啶基甲基）甲醯胺 (5-肩-2-{[2·(3-氟本基）乙基]胺基〉（3-0比σ定基）)_n_[(6-曱 455基(2-吼啶基)）甲基]甲醯胺 (5-漠-6-氯-2-{[2-(3-氟苯基）乙基]胺基}(3- σ比啶 465基))-Ν-(2-吼啶基曱基）甲醯胺 341 5-溴-2-{[2-(3-氟苯基）乙基]胺基}吡啶-3•羧酸 300.1 5-氰基-2-{[2·(3-氟苯基）乙基]胺基}吡啶羧酸曱酯 Ν-({6-[(1，3-二氧基苯并[c]唑琳基）曱基](2_吡啶基）}曱 59〇基)(5-&gt;臭-2-{[2-(3-氟苯基）乙基]胺基比啶基)）曱醯胺 (5备2-{[2-(3-氟苯基）乙基]胺基比啶基))善(2_吡啶 431基甲基）曱醯胺 Ν-{[6-(胺基曱基）(2』比啶基）]曱基}(5_漠_2_{[2_(3-氟苯 46〇基）乙基]胺基定基)）曱醯胺 n-{[6-(胺基甲基）〇比啶基）]曱基丨(2_{[2_(3_說苯基）乙 457.1基]胺基}-5-(2』比咬基)(3』比咬基)）甲醯胺 6-[(4-胺曱醯基丁基)胺基&gt;2|(3_ 389.2吡啶-3-羧酸甲酯 」 ； 5 [(6 {[2-(3-氟苯基）乙基]胺基卜5 &gt;比 493.2曱醯基吡口令装、、…甘Ί、τ ； ^ 土 W '疋基))胺基]-Ν，Ν-二曱基戊醯胺 479 2 5甲[:，其{[1^亂苯基)乙基]胺基}_5供(3-°比咬基曱基)胺 甲&amp;基](H定基))胺基]善曱基戊酿胺 465 2 基丁基）胺基]_2_ {[2-(3_ 苯基）乙基]胺 •土 }( 疋基）)-Ν-(3-π比啶基曱基）曱醯胺 479.2 土 #疋基))胺基]-N，N-二甲基丁醯胺 451·2 Μ3·胺甲酸基丙基）胺基]·2·{[2-(3·氟苯基）乙基]胺 309 200823188 IC5017.7374 M+H 6.0282 M+H 12.683 M+H 17.7243 M+H 17.258 M+H 11.19 M+H 14.887 M+H 9.7159 M+H 11.8154 M+H 15.0424 M+H 16.0219 M+H 44.3072 M+H 55.0688 M +H 38.046 M+H 6.7378 M+H 70.3134 M+H 42.7772 M+H m/z Chemical name base]Amino group -5 - (4 -·吼°定基) (3′′ than bite base)) N-{[6-(aminomercapto)(2-n-pyridyl)]nonylfluorophenyl)ethyl 46〇·1yl]aminomethyl η than spyryl) (3′′ ratio. Amidoxime-{[6-(aminomethyl)(2-acridinyl)]fluorenyl}(5-(2-cyanobenzene 481.1-yl)-2-{[2-(3-fluorobenzene) Ethyl]aminopyridylcarzamide (5-cyano-2-{[2-(3-fluorophenyl)ethyl;|aminopyridinyl) is a ratio of 376.1 pyridine Methylamine (5-shoulder-2-{[2·(3-fluorobenzyl)ethyl]amine> (3-0 to σ-based))_n_[(6-曱455-based (2-吼) Pyridyl))methyl]carbamamine (5-indol-6-chloro-2-{[2-(3-fluorophenyl)ethyl]amino}(3- σ-pyridyl 465))-Ν -(2-Acridinesulfanyl)carhamamine 341 5-bromo-2-{[2-(3-fluorophenyl)ethyl]amino}pyridine-3•carboxylic acid 300.1 5-cyano-2 -{[2·(3-Fluorophenyl)ethyl]amino}pyridine carboxylic acid oxime Ν-({6-[(1,3) -dioxybenzo[c]oxalyl)indolyl](2_pyridyl)}曱59〇yl)(5-&gt;Smelly-2-{[2-(3-fluorophenyl)ethyl Aminopyridinyl))guanamine (5-preparative 2-{[2-(3-fluorophenyl)ethyl]aminopyridinyl)) good (2_pyridyl 431-methyl) decylamine Ν-{[6-(Aminocarbonyl)(2′′pyridyl)]hydrazino}(5_漠_2_{[2_(3-fluorophenyl46〇yl)ethyl]amino group))曱Indole n-{[6-(aminomethyl)pyridinyl)]indolyl (2_{[2_(3_ phenyl)ethyl 457.1)]amino}-5-(2) than bite () is a carbamide 6-[(4-aminomercaptobutyl)amino group&gt;2|(3_389.2 pyridine-3-carboxylic acid methyl ester); 5 [(6 { [2-(3-Fluorophenyl)ethyl]aminopurine 5 &gt; than 493.2 mercapto-pyridyl, ..., kansin, τ; ^ soil W 'indenyl)) amino]-Ν, Ν - Dimercaptoguanamine 479 2 5 A [:, its {[1^ disordered phenyl)ethyl]amino}_5 for (3-° ratio thiol amide) amine A &amp; base] (H-based )) Amino] 曱 曱 戊 465 465 2 2 butyl butyl) amine] 2_ {[2-(3 phenyl) ethyl] amine • earth} (fluorenyl))-Ν-(3-π ratio Pyridyl yl) guanamine 479.2 疋#疋基))Amino]-N,N-dimethylbutyramine 451·2 Amine acid 3-yl propyl) amino] · 2 · {[2- (3-fluorophenyl) ethyl] amine 309 200823188 IC50

算數平均離子 4.919 M+H 49.2162 M+H 10.883 M+H 33.5035 M+H 53.412 M+H 13.9674 M+H 65.8061 M+H 5.6092 M+H 0.2309 M+H 10.5082 M+H 44.1181 M+H 4.3507 M+H 10.7731 M+H 0.7796 M+H 3.4457 M+H 33.9795 M+H m/z 化學名稱 基}(3-吡啶基))-N-(3-吡啶基曱基）甲醯胺 (6-(二曱基胺基）-2-{[2-(3-鼠苯基）乙基]胺基}(3-°比咬 394.1基))-N-(3-吡啶基曱基）曱醯胺 5- [(6-{[2-(3-氟苯基）乙基]胺基}-5-[N-(3-啦啶基曱基) 556.2胺甲醯基](2-吡啶基))胺基]-N-(3-吡啶基曱基）戊醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(曱基胺基）(3-吼啶 380.2基))-N-(3-吡啶基曱基）曱醯胺 N-(6-{[2-(3-氣苯基）乙基]胺基}-5-[N-(3-°比σ定基曱基） 422.2胺甲醯基](2-吡啶基))-Ν-甲基乙醯胺 Ν-(6_{[2-(3-氟苯基）乙基]胺基卜5-[Ν-(3-吼啶基曱基） 452.2胺甲醯基](2-吡啶基))-Ν-(2-羥基乙基）乙醯胺 6- {[2-(3-氟苯基）乙基]胺基}-5-[Ν-(3-吼啶基甲基）胺 394.1甲醯基]吡啶-2-甲醯胺 (6-氰基-2-{[2-(3-氟苯基）乙基]胺基}(3-。比啶 376.1基))-Ν-(3-啦啶基曱基）甲醯胺 2-{[2-(3-氟苯基）乙基]胺基}-6-[(3-。比啶基甲基）胺 457.1基](3-吼啶基))-Ν-(3-吼啶基甲基）曱醯胺 (6-[(氰基胺基）亞胺基甲基]-2-{[2-(3-氟苯基）乙基]胺 418.1基}(3-吡啶基))-Ν-(3-吡啶基甲基）甲醯胺 (6-((1Ζ)-1-甲基丙-1-烯基）-2-{[2-(3-氟苯基）乙基]胺 405·1基}(3-吼啶基))-Ν-(3-吡啶基曱基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-(Ν-曱基胺曱醯基）(3-408.1吡啶基）)-N-(3-吡啶基曱基）甲醯胺 6-{[2-(3-氟苯基）乙基]胺基}-5-[N-(3-吼啶基甲基）胺甲 409.1醯基]吡啶-2-羧酸甲酯 (2-{[2-(3-氟苯基）乙基]胺基}-6-[(2-吼啶基曱基）胺 457.2基](3-吡啶基))-N-(3-吡啶基曱基）曱醯胺 (6-((1Ε)丙-1-烯基）-5-溴-2-{[2-(3-氟苯基）乙基]胺 469 基}(3-吡啶基）)-N-(3-吡啶基甲基）曱醯胺 (2E)-3-(6-{[2-(3 -氣苯基）乙基]胺基}- 5-[N-(3-°比σ定基曱 449.1基）胺曱醯基](2-吡啶基））丁-2-烯酸甲酯 457.1 (2-{[2·(3-氟苯基）乙基]胺基}-6·[(4-吼啶基曱基）胺 310 200823188 IC50 算數平均離子Arithmetic Mean 4.919 M+H 49.2162 M+H 10.883 M+H 33.5035 M+H 53.412 M+H 13.9674 M+H 65.8061 M+H 5.6092 M+H 0.2309 M+H 10.5082 M+H 44.1181 M+H 4.3507 M+ H 10.7731 M+H 0.7796 M+H 3.4457 M+H 33.9795 M+H m/z Chemical name base}(3-pyridyl))-N-(3-pyridylfluorenyl) formamide (6-(two) Mercaptoamino)-2-{[2-(3-murophenyl)ethyl]amino} (3-° ratio bit 394.1))-N-(3-pyridylfluorenyl)guanamine 5 - [(6-{[2-(3-Fluorophenyl)ethyl]amino}-5-[N-(3-oxaridinyl)- 556.2-aminomethyl]-(2-pyridyl)) Amino]-N-(3-pyridylfluorenyl)pentanylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-(decylamino)(3-oxime) Acridine 380.2-based))-N-(3-pyridylfluorenyl)guanamine N-(6-{[2-(3-phenylphenyl)ethyl]amino}-5-[N-(3- ° σ 曱 曱 ) 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 42 -[Ν-(3-Acridinesulfanyl) 452.2 Aminomethylindenyl](2-pyridyl))-indole-(2-hydroxyethyl)acetamidamine 6- {[2-(3-fluorobenzene) Ethyl]amino}-5-[indolyl-(3-acridinylmethyl)amine 394.1-mercapto]pyridin-2-carboxamide (6-cyano- 2-{[2-(3-fluorophenyl)ethyl]amino}(3-.pyridyl 376.1))-indole-(3-oxaridinyl)carbamamine 2-{[2- (3-fluorophenyl)ethyl]amino}-6-[(3-.pyridylmethyl)amine 457.1-yl](3-acridinyl))-indole-(3-acridinylmethyl) Indoleamine (6-[(cyanoamino)iminomethyl]-2-{[2-(3-fluorophenyl)ethyl]amine 418.1-yl}(3-pyridyl))-oxime -(3-pyridylmethyl)formamide (6-((1Ζ)-1-methylprop-1-enyl)-2-{[2-(3-fluorophenyl)ethyl]amine 405 · 1-yl}(3-acridinyl))-indole-(3-pyridylfluorenyl) decylamine (2-{[2-(3-fluorophenyl)ethyl)amino}-6-( (Ν-mercaptoamine) (3-408.1 pyridyl))-N-(3-pyridylfluorenyl)carhamamine 6-{[2-(3-fluorophenyl)ethyl]amino} -5-[N-(3-Acridinemethyl)amine 409.19.1-yl]pyridine-2-carboxylic acid methyl ester (2-{[2-(3-fluorophenyl)ethyl]amino}- 6-[(2-Acridinesulfanyl)amine 457.2-yl](3-pyridyl))-N-(3-pyridylfluorenyl)decylamine (6-((1Ε)prop-1-enyl) )-5-bromo-2-{[2-(3-fluorophenyl)ethyl]amine 469 base}(3-pyridyl))-N-(3-pyridylmethyl)decylamine (2E) -3-(6-{[2-(3-Phenylphenyl)ethyl]amino}- 5-[N-(3-° ratio σ曱449.1)Aminoguanidino](2-pyridyl))but-2-enoic acid methyl ester 457.1 (2-{[2·(3-fluorophenyl)ethyl]amino}-6·[( 4-Acridinesulfonyl)amine 310 200823188 IC50 arithmetic mean ion

2.6522 M+H 0.3021 M+H 0.3608 M+H 0.3473 M+H 17.2629 M+H2.6522 M+H 0.3021 M+H 0.3608 M+H 0.3473 M+H 17.2629 M+H

5.1875 M+H5.1875 M+H

6.619 M+H6.619 M+H

14.9996 M+H14.9996 M+H

0.038 M+H0.038 M+H

17.9719 M+H17.9719 M+H

0.9273 M+H0.9273 M+H

73.03 M+H73.03 M+H

24.7905 M+H24.7905 M+H

0.0805 M+H0.0805 M+H

11.7073 M+H m/z 化學名稱 基](3-σ比咬基·))·Ν-(3-ϋ比咬基曱基）曱酿胺 6-{[2·(3-1苯基）乙基]胺基卜5-[Ν〇比哈发m 423.1醯基]吡啶-2-羧酸乙酯 土 基）胺甲 (6-((1Ε)丙-1-烯基)-2-{[2-(3-氟苯基）乙基 391.2啶基))-N-(3-吡啶基曱基）曱醯胺 丞}(3，匕 (6-(⑽丙小烯基）-5-氰基_2_{[2分氣笨基 416.1基}(3-吡啶基))-N-(3-吡啶基甲基）甲醯胺 &amp;暴]胺 (2-{[2-(3-氟苯基）乙基]胺基}_6_(2-曱基丙4 4〇5·2吡啶基))-N-(3·吡啶基曱基）甲醯胺 碲基）(夂 (6-[(二甲基胺基）亞胺基甲基泣收(3·氣 421.2胺基}(3-吡啶基）)-N-(3-吡啶基甲基）甲醉胺土）乙基] (6-[(1幻小（二甲基胺基氰基二 基]-2-{[2-(3-氟苯基）乙基]胺基}(3_,比啶基n 446.1啶基甲基）甲醯胺 H吧 6-{[2-(3-氟苯基）乙基]胺基}-5-[Ν_(3_吡啶美 393.1醯基]口比咬-2-曱脉 土 土）¾甲 2-Κ2-ί[2-(3-氣苯基）乙基]胺基卜5_苯基 407.1基胺基]-N-甲基乙醯胺 疋卷））¾ (，((1E)丙-1-烯基)-2-{[2-(3-氟苯基）乙基]胺基}(3一比 420.1啶基))-N-{[2-(胺基曱基）(3-吡啶基)]甲基}甲醯胺 2-[(5-(2-氰基苯基）-2_{[2_(3_氟苯基）乙基]胺基}(3^比 432·1啶基))羰基胺基]-N-甲基乙醯胺 (6-((1Ε)-3-甲氧基丙-1-烯基&gt;2_{[2_(3-氟苯基）乙基] 421.2基}(3-咄啶基》_N_(3-吡啶基甲基）甲醯胺 土 (6-(乙氧基乙基）_2-{[2-(3-氟苯基）乙基]胺基}(3_吼 423.2基))-N-(3-吡啶基曱基）曱醯胺 (6-乙酸基-2-{[2-(3-敗苯基）乙基]胺基}(3』比咬基）)_队( 393.1吡啶基甲基）曱醯胺 (6·((1Ε)丙-1-烯基）冬氟-2·{[2-(3_氟苯基）乙基]胺基}( 438.1吼啶基))_队{[2·(胺基曱基）(3-σ比啶基)]甲基}甲醯胺 (6·((1Ε)丙-1-烯基）-5-氟-2-{[2-(3-氟苯基）乙基]胺基}&lt; 538·2 °比咬基）)1[(2-{[(第三丁氧基）獄基胺基]曱基}(3』比 200823188 IC50 算數平均離子m/z 2.6897 M+H 398 26.8336 M+H 351.1 2.7696 M+H 419.2 8.1803 M+H 423.1 0.7025 M+H 421.2 13.0601 M+H 410.2 45.4109 M+H 424.2 7.6223 M+H 424.2 10.4821 M+H 438.2 11.0022 M+H 438.2 8.4659 M+H 424.2 化學名稱 基)）曱基]曱醯胺 - N-{[2-(胺基曱基）(3-σ比啶基）]甲基}(5-氟-2-{[2-(3-氟苯 基）乙基]胺基}(3^比啶基））甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基}(3-吡啶基）)-&gt;!-(3-吡啶基甲 基）甲醯胺 (6-(1，2-二曱基丙-1 -稀基）_2- {[2-(3 -氟本基）乙基]胺基}(3_ °比0定基）)-Ν-(3-σ比咬基曱基）甲醢胺 (2-{[2-(3-氟苯基）乙基]胺基卜6-(3-曱氧基丙基）(3_°比咬 基))-Ν-(3-ϋ比啶基甲基）甲醯胺 (6-(1-乙氧基乙稀基{[2-(3-氟苯基）乙基]胺基}(3-σΛσ定 基))_Ν-(3_σ比啶基甲基）甲酿胺 (2-{[2-(3-氟苯基）乙基]胺基卜6-[(2-經基乙基）胺基](3-。比 啶基))-Ν-(3-ϋ比啶基甲基）曱醯胺 (2-{[2-(3-氟苯基）乙基]胺基}-6-[(2·經基乙基）甲基胺 基](3』比啶基))-N-(34b淀基甲基）甲酸胺 (2-{[2-(3-氟苯基）乙基]胺基卜6-[(2-甲氧基乙基）胺基](3-。比咬基))-]^-(3-。比咬基甲基）曱胺 (2-R2-(3-氟苯基）乙基]胺基}-6-[(2_羥基丙基）曱基胺 基](3-吼啶基))斗(3-t定基甲基）甲醯胺 (2-{[2-(3-氟苯基）乙基]胺基IH(3_曱氧基丙基）胺基](3-吡°定基比咬基甲基）曱酸胺 (2-{[2-(3-氟苯基）乙基]胺基卜6-[(3**羥基丙基）胺基](3-11比 σ定基))·Ν-(3-σΐ^定基甲基）曱酿胺 實例21 :合成6-(2-氰基苯基)_4-(3-氟苯乙基胺基)-Ν十比 啶-3_基曱基)菸鹼醯胺 312 20082318811.7073 M+H m/z Chemical name base] (3-σ ratio bite base))·Ν-(3-ϋ ratio 咬 base group) 曱 amine 6-{[2·(3-1 phenyl) Ethyl]aminodibu 5-[Ν〇比哈发m 423.1 fluorenyl]pyridine-2-carboxylic acid ethyl ester) methamine (6-((1Ε)prop-1-enyl)-2-{ [2-(3-Fluorophenyl)ethyl 391.2 pyridine))-N-(3-pyridylfluorenyl) amidoxime] (3, 匕(6-((10))propenyl)-5- Cyano 2_{[2 gas-stirring 416.1-yl}(3-pyridyl)-N-(3-pyridylmethyl)carbamamine &amp; violent amines (2-{[2-(3- Fluorophenyl)ethyl]amino}_6_(2-mercaptopropan 4 4〇5·2 pyridinyl))-N-(3·pyridylfluorenyl)carbamamine fluorenyl) (夂-6-[ (Dimethylamino)imidomethyl weeping (3·gas 421.2 amino}}(3-pyridyl))-N-(3-pyridylmethyl)hydantoin)ethyl] (6 -[(1 xiaoxiao(dimethylaminocyanodiyl)-2-{[2-(3-fluorophenyl)ethyl]amino}(3_,pyridyl n 446.1 pyridinemethyl) Methionine H bar 6-{[2-(3-fluorophenyl)ethyl]amino}-5-[Ν_(3_pyridine US 393.1 fluorenyl) mouth bite -2- 曱 土 soil) 3⁄4 2-2-[2-(3-(phenyl)ethyl]amino) 5-phenyl- 407.1-amino]-N-methylacetamide 3⁄4 (,((1E)prop-1-enyl)-2-{[2-(3-fluorophenyl)ethyl]amino} (3 to 420.1 pyridine))-N-{[2 -(aminomercapto)(3-pyridyl)]methyl}carbenamide 2-[(5-(2-cyanophenyl)-2_{[2_(3-fluorophenyl)ethyl]amine }}(3^ ratio 432·1 pyridine))carbonylamino]-N-methylacetamide (6-((1Ε)-3-methoxyprop-1-enyl)<2_{[2_ (3-fluorophenyl)ethyl] 421.2-yl}(3-acridinyl)_N_(3-pyridylmethyl)carbammine (6-(ethoxyethyl)_2-{[2-( 3-fluorophenyl)ethyl]amino}(3_吼423.2))-N-(3-pyridylfluorenyl)decylamine (6-acetoxy-2-{[2-(3-) Phenyl)ethyl]amino}(3) than butyl))_team (393.1 pyridylmethyl) decylamine (6·((1Ε)prop-1-enyl) chlorofluoro-2·{[ 2-(3-Fluorophenyl)ethyl]amino}(438.1 aridinyl))_team {[2.(Aminomethyl)(3-σ-pyridyl)]methyl}carboxamide 6·((1Ε)prop-1-enyl)-5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}}&lt; 538·2 ° ratio bite base)) 1 [ (2-{[(Tertidinoxy)) Peptidyl] sulfhydryl}(3) is compared with 200823188 IC50 arithmetic mean ion m/z 2.6897 M+H 398 26.8336 M+H 351.1 2.7696 M+H 419.2 8.1803 M+ H 423.1 0.7025 M +H 421.2 13.0601 M+H 410.2 45.4109 M+H 424.2 7.6223 M+H 424.2 10.4821 M+H 438.2 11.0022 M+H 438.2 8.4659 M+H 424.2 Chemical name base)) fluorenyl] decylamine - N-{[2 -(aminoindenyl)(3-σ-pyridyl)]methyl}(5-fluoro-2-{[2-(3-fluorophenyl)ethyl]amino}(3^pyridyl) Methionine (2-{[2-(3-fluorophenyl)ethyl]amino}(3-pyridyl))-&gt;!-(3-pyridylmethyl)carhamamine (6- (1,2-dimercaptopropan-1 -succinyl)_2- {[2-(3-fluorophenyl)ethyl]amino}(3_° ratio 0 base))-Ν-(3-σ ratio咬 ) base) formazan (2-{[2-(3-fluorophenyl)ethyl]aminobiphenyl 6-(3-decyloxypropyl) (3_° than bite))-Ν- (3-indolylmethyl)carbamamine (6-(1-ethoxyethyl){[2-(3-fluorophenyl)ethyl]amino}(3-σΛσ定基))_Ν -(3_σ-pyridylmethyl)cartoamine (2-{[2-(3-fluorophenyl)ethyl)aminophenyl 6-[(2-ylethylethyl)amino](3-. Bisyl))-Ν-(3-indolylmethyl) decylamine (2-{[2-(3-fluorophenyl)ethyl]amino}-6-[(2· Ethyl)methylamino](3′′pyridinyl))-N-(34b butylmethyl)formic acid amine (2-{[2-(3-fluorophenyl)ethyl]amino)- 6- [(2-methoxyethyl)amino](3-. than butyl))-]^-(3-. than dimethylmethyl) decylamine (2-R2-(3-fluorophenyl) Ethyl]amino}-6-[(2-hydroxypropyl)decylamino](3-acridinyl))indole (3-t-decylmethyl)carbenamide (2-{[2-( 3-fluorophenyl)ethyl]amino IH(3-methoxypropyl)amino](3-pyridinyl butylmethyl) decanoic acid amine (2-{[2-(3-fluoro) Phenyl)ethyl]aminobib 6-[(3**hydroxypropyl)amino](3-11 σ stilyl))·Ν-(3-σΐ^定基methyl) anthraquinone Example 21 : Synthesis of 6-(2-cyanophenyl)_4-(3-fluorophenethylamino)-indolylpyridin-3-ylhydrazino)nicotinamide 312 200823188

一 土）4-(3-氟苯乙基胺基)_ν_(π比π定·3_基甲基）於驗酸胺a soil) 4-(3-fluorophenethylamino)_ν_(π ratio π定·3_ylmethyl)

於4,6_二氯菸鹼酸乙酯(2·2 g，10·0 mmol)及3_氟-苯基 5 乙基胺（1.5g，U.Ommol)之DMF(20 mL)溶液中於室溫^加 入K^COKUg，30 mmol)。將反應混合物於室溫下擾拌至 隔夜。將反應混合物過濾並減壓濃縮。將生成的殘餘物使 用乙腈及H2〇混合物於RP_HPL上純化，得到6_氯_4_(3一 氟苯乙基胺基)菸鹼酸乙酯（11 mg, 34%hLRMS (M+H4·) ίο m/z 323·0 〇In a solution of 4,6-dichloronicotinic acid ethyl ester (2·2 g, 10·0 mmol) and 3-fluoro-phenyl 5 ethylamine (1.5 g, U.Ommol) in DMF (20 mL) Add K^COKUg, 30 mmol) at room temperature. The reaction mixture was stirred at room temperature overnight. The reaction mixture was filtered and concentrated under reduced pressure. The resulting residue was purified on RP_HPL using acetonitrile and a mixture of H.sub.2 to afford ethyl 6-chloro-4-[(3-fluorophenethylamino) nicotinic acid ethyl ester (11 mg, 34% hLRMS (M+H4·) Οο m/z 323·0 〇

C02EtC02Et

hctb、ohHctb, oh

PdCI2dppf 於6_氯-4-(3_氟苯乙基胺基）菸驗酸乙酯（1.2 g，3.7 111111〇1)、2-氰基-苯基硼酸(1.18，7.4111111〇1)及1^2(^03(1.5运， 11·1 mmol)之 DMF(25 mL)混合物中加入 PdCl2.dppf(0.2 g, 15 0.37 mmol)。將反應混合物於1〇〇。〇下攪拌4h°LC/MS顯 示反應完成。將反應混合物過濾並將濾液濃縮。將生成的 313 200823188 殘餘物使用乙腈及H20混合物於RP-HPL上純化，得到 6-(2-氣基苯基)-4-(3^氟苯乙基胺基）於驗酸乙醋(500 mg， 34%)。LRMS (M+H+) m/z 389.0。PdCI2dppf on 6-chloro-4-(3-fluorophenethylamino) niacin acid ethyl ester (1.2 g, 3.7 111111〇1), 2-cyano-phenylboronic acid (1.18, 7.4111111〇1) and 1 PdCl2.dppf (0.2 g, 15 0.37 mmol) was added to a mixture of &lt;RTI ID=0.0&gt;&gt; MS showed the reaction was completed. The reaction mixture was filtered and the filtrate was concentrated. EtOAc EtOAc EtOAc EtOAc EtOAc Fluorophenethylamino) was tested in acid vinegar (500 mg, 34%). LRMS (M+H+) m/z 389.0.

5 於6-(2-氰基苯基)-4-(3-氟苯乙基胺基)於驗酸乙醋（1〇〇 mg，0.26 mmol)及 3-胺基甲基吼σ定(39 mg，0.36mmol)之曱 苯（1 mL)溶液中於室溫下加入AlMe3(0.2 mL，2M甲苯溶液， 0.39mmol)。將反應混合物於70°C攪拌至隔夜。將反應冷 • 卻、以飽和的NaHC03進行驟冷並以EtOAc稀釋。將有機 ίο 層分離，以鹽水清洗，以Na2S〇4乾燥並過濾。將濾液減壓 濃酸得到粗油狀物。將粗混合物使用乙腈及H20混合物於 RP-HPL上純化’得到6·(2-氛基苯基)-4-(3-氣苯乙基胺 基）-Ν-(ϋ比唆_3_基甲基）於驗酿胺（10 mg，8.6%)。LRMS (M+H+) m/z 452.0。 15 實例22 使用類似文中所述之製程，合成及試驗下表中之化合 物。 314 200823188 IC50 算數平均離子m/z 化挙名稱 (6-(2-氰基苯基）-4-{[2-(3- |L苯基）乙基]胺 2·02 M+H 452.1基}(3-0比°定基))-N-(3_o比〇定基曱基）甲醯胺 2·[(6-(2-氰基苯基）-4-{[2-(3-氟苯基）乙基]胺 48·426 Μ+Η 432.1基}〇吼啶基))幾基胺基]_Ν-甲基乙醯胺 [4-{[2-(3-氟苯基）乙基]胺基}-6-(2-{亞胺基[(3-口比 唆基曱基）胺基]曱基}苯基)(3-吼咬基)]-Ν-(3-σΛ咬 61.236 Μ+Η 560.2基甲基）甲醯胺 實例23 :在活體外劑量依賴平滑肌肌凝蛋白Ατρ酶調節 之模型 5 篩選分析係使用丙酮酸激酶及含有下列試劑之乳酸去 氫酶偶合ΑΤΡ酶分析來進行：PIPES鉀(50mM)、MgCl2(3 mM)、KCI (100 mM)、ΑΤΡ(0·15 mM)、DTT(l mM)、BSA(0.1 mg/ml)、NADH (0·5 mM)、ΡΕΡ(1·5 mM)、丙酮酸激酶(4 U/ml)、乳酸去氫酶(8 U/ml)及消泡劑（50 ppm)(所表示的濃 10 度為最終分析濃度）。於22°C藉由加入氫氧化鉀將PH調整 至6.80。以含有下列試劑之較敏感的丙酮酸激酶/山葵過氧 化酶/丙酮酸-氧化酶-偶合ATP酶分析進行最適化分析： PIPES 鉀（12 mM)、MgCl2(2 mM)、KC1(100 mM)、ΑΤΡ(0·15 mM)、BSA(0.05 mg/ml)、石舞酸_(2 mM)、amplex red(0.1 15 mM)、ΡΕΡ(0·1 mM)、丙酮酸激酶(4 U/ml)、山葵過氧化酶 (0·5 U/ml)、丙酮酸氧化酶(〇·5 u/ml)及消泡劑（50 ppm)(所 表示的濃度為最終分析濃度）。於22°C藉由加入氫氧化鉀 將pH調整至7.00。 315 2008231885 in 6-(2-cyanophenyl)-4-(3-fluorophenethylamino) in acid vinegar (1 〇〇 mg, 0.26 mmol) and 3-aminomethyl hydrazine A solution of 39 mg, 0.36 mmol) in benzene (1 mL) was added at room temperature to <RTI ID=0.0>#</RTI> <RTIgt; The reaction mixture was stirred at 70 ° C until overnight. The reaction was cooled, quenched with saturated NaHC03 and diluted with EtOAc. The organic layer was separated, washed with brine, dried over Na 2 EtOAc and filtered. The filtrate was concentrated under reduced pressure to give a crude oil. The crude mixture was purified by acetonitrile and H20 mixture on RP-HPL to give 6(2-aminophenyl)-4-(3-phenethylethylamino)-indole-(ϋ比唆_3_yl) Methyl) was tested on amine (10 mg, 8.6%). LRMS (M+H+) m/z 452.0. 15 Example 22 The compounds in the table below were synthesized and tested using procedures similar to those described herein. 314 200823188 IC50 arithmetic mean ion m/z 挙 name (6-(2-cyanophenyl)-4-{[2-(3- |L phenyl)ethyl]amine 2·02 M+H 452.1 }(3-0 ratio ° base))-N-(3_o 〇定基基基)carbamamine 2·[(6-(2-cyanophenyl)-4-{[2-(3-fluorobenzene) ))ethyl]amine 48·426 Μ+Η 432.1 〇吼} aridinyl)) arylamino] Ν-methyl acetamide [4-{[2-(3-fluorophenyl)ethyl] Amino}-6-(2-{imino[(3-hydroxypyranyl)amino]indolyl}phenyl)(3-indenyl)]-Ν-(3-σΛ bite 61.236 Μ+Η 560.2-methyl)carbamamine Example 23: Model for regulation of in vitro dose-dependent smooth muscle myosin Ατρ enzyme 5 Screening analysis using pyruvate kinase and lactic acid dehydrogenase coupled chymase assay with the following reagents Perform: PIPES potassium (50 mM), MgCl2 (3 mM), KCI (100 mM), sputum (0.15 mM), DTT (1 mM), BSA (0.1 mg/ml), NADH (0.5 mM), ΡΕΡ (1·5 mM), pyruvate kinase (4 U/ml), lactate dehydrogenase (8 U/ml), and defoamer (50 ppm) (concentrated by 10 degrees is the final assay concentration). The pH was adjusted to 6.80 by the addition of potassium hydroxide at 22 °C. Optimization analysis was performed with the more sensitive pyruvate kinase/wasabi peroxidase/pyruvate-oxidase-coupled ATPase assay containing the following reagents: PIPES potassium (12 mM), MgCl2 (2 mM), KC1 (100 mM) , ΑΤΡ (0·15 mM), BSA (0.05 mg/ml), Shisha _ (2 mM), amplex red (0.1 15 mM), ΡΕΡ (0·1 mM), pyruvate kinase (4 U/ml ), wasabi peroxidase (0.5 U/ml), pyruvate oxidase (〇·5 u/ml), and defoamer (50 ppm) (the concentration indicated is the final assay concentration). The pH was adjusted to 7.00 by the addition of potassium hydroxide at 22 °C. 315 200823188

針對此分析之蛋白質成份為已使用過量的1-乙基 二甲基胺基丙基]碳醯亞胺鹽酸鹽及N_經基破珀醯 亞胺與心肌或骨絡肌肌動蛋白化學交聯結合之雞脸平滑 肌肌凝蛋白次斷片-1。分析中交聯結合的平滑肌肌凝蛋白 5 之確切的濃度係以實驗來測定，藉由滴定達到所欲的ATP 水解速率。因為活性分子在各製備中的比例不同，所以蛋 白貝製備物間的濃度亦不同。 化合物劑量反應分析係藉由先各以含有PIPES、 MgCl2、KC1、ATP、BSA、石粦酸卸、amplex red、PEP、交 10 聯平滑肌肌凝蛋白（次斷片-l)、消泡劑及水之分析混合物 製備連續稀釋之試驗化合物，來進行。分析開始係加入等 體積含有Pipes鉀、MgCl2、KC卜BSA、磷酸鉀、丙酮酸 激酶、山葵過氧化酶、丙酮酸氧化酶、消泡劑及水之濃液。 ATP水解係藉由測量amplex red (激發光48〇 nm，發射光 15 615 nm)之螢光來監測。產生的劑量反應曲線係由4參數 方程式y:底點+ ((頂點-底點)/(1+((IC5G/x)AHill)))來凝 合。IQo係定義為Αχ?酶活性在介於劑量反應曲線的頂點 和底點間之中間值置時之濃度。 本文所述之特定化學品具有低於10 μΜ之1C% ;例 2〇 如，低於ΙμΜ。 當本气明已參照其特定的實施例來說明，熟習本項技 術者應了解在不悖離本發明之真實的精神及範圍下，可 做各種改變並可使用同等物取代。此外，可對本發明之目 標、精神和範圍做許多的修改以適應特定的狀況、物質、 316 200823188 材料之成份、製程、處理步驟或步驟。所有該等之修改係 希望在其所附的申請專利範圍之範疇下。 _The protein component for this analysis is an excess of 1-ethyldimethylaminopropyl]carbenium imide hydrochloride and N-trans-based cyanide and myocardial or skeletal muscle actin chemistry. Cross-linked chicken smooth muscle myosin sub-slice-1. The exact concentration of cross-linked smooth muscle myosin 5 in the assay was determined experimentally by titration to achieve the desired rate of ATP hydrolysis. Since the ratio of active molecules in each preparation is different, the concentration between the protein preparations is also different. The compound dose-response analysis was performed by first containing PIPES, MgCl2, KC1, ATP, BSA, saponin, amplex red, PEP, conjugated smooth muscle myosin (secondary fragment-l), defoamer and water. The assay mixture is prepared by preparing serially diluted test compounds. The analysis was started by adding equal volumes of Pipes Potassium, MgCl2, KC Bu BSA, Potassium Phosphate, Pyruvate Kinase, Wasabi Peroxidase, Pyruvate Oxidase, Antifoaming Agent and Water Concentrate. ATP hydrolysis was monitored by measuring the fluorescence of amplex red (excitation light 48 〇 nm, emission 15 15 615 nm). The resulting dose response curve is condensed by the 4-parameter equation y: bottom point + ((vertex - bottom point) / (1 + ((IC5G / x) AHill))). IQo is defined as the concentration of enzyme activity at an intermediate value between the apex and the bottom of the dose response curve. The specific chemicals described herein have a CC of less than 10 μΜ; Example 2 is, for example, less than ΙμΜ. While the present invention has been described with reference to the specific embodiments thereof, it will be understood by those skilled in the art that various changes may be made and the equivalents may be substituted without departing from the true spirit and scope of the invention. In addition, many modifications may be made to the subject matter, spirit, and scope of the invention to adapt to the particular conditions, materials, compositions, process, process steps or steps. All such modifications are intended to be within the scope of the appended claims. _

Claims (1)

200823188 十、申請專利範圍： •至少一種選自式X化合物及其醫藥上可接受鹽類之化學 品200823188 X. Patent application scope: • At least one chemical selected from the group consisting of a compound of formula X and a pharmaceutically acceptable salt thereof 式X 其中 W1係選自N及CR6，真w2係選自N及CR4，其 限制條件為W1及W2二者不玎皆為N ; R1及R4係獨立地選自氫、氰基、鹵基、羥基、疊 氮基、硝基、磺醯基、亞磺醯基、硫烷基、視需要經 取代之烧乳基、視需要經取代之酿氧基、視需要經取 代之胺基羰基氧基、視需要經取代之芳基氧基、視需 要經取代之雜芳基氧基、視需要經取代之雜環烷基氧 基、視需要經取代之烷氧基羰基、視需要經取代之烷 基、視需要經取代之烯基、視需要經取代之炔基、視 需要經取代之芳基氧基、視需要經取代之芳基、視需 要經取代之雜芳基、視需要經取代之雜環烷基、視需 要經取代之胺基、視需要經取代之醯基、視需要經取 代之胺基羰基及/見需要經取代之carbamin〇d〇yl ; Z1係選自氫、視需要經取代之芳基、視需要經取 代之雜芳基、視需要經取代之環絲、視需要經取代 318 200823188 之雜環烧基、氰基、視需要經取代之烷基、視需要經 取代之醯基、視需要經取代之烷氧基羰基、視需要經 取代之胺基、視需要經取代之胺基羰基、視需要經取 代之曱脒基、視需要經取代之烧氧基、視需要經取代 之芳基氧基、視需要經取代之雜芳基氧基、視需要經 取代之雜環烷基氧基、視需要經取代之烯基、視需要 經取代之炔基、磺醯基、亞磺醯基及硫烷基； z2係選自氳、視需要經取代之曱脒基、羧基、視 需要經取代之烷氧基羰基、視需要經取代之醯基、視 需要經取代之烯基、視需要經取代之烷基、視需要經 取代之雜環烷基、視需要經取代之雜芳基及視需要經 取代之胺基魏基； 15 z係選自氫、i素及視需要經取代之燒基； r3係選自氳及視需要經取代之烷基；及 R係返自虱、視需要經取代之醯基、視需要經取 代之烷基、氰基、_基、疊氮基、視需要經取代之胺 基、視需要經取代之烷氧基羰基、視需要經取代之胺 基獄基、續醯基、亞磺醯基及硫烧基。 2·至少一種如申請專利範圍第1項之化學品，其中該式χ 化合物係選自式I化合物，Wherein W1 is selected from N and CR6, and true w2 is selected from N and CR4, the limitation is that both W1 and W2 are N; R1 and R4 are independently selected from hydrogen, cyano, and halo. , hydroxy, azido, nitro, sulfonyl, sulfinyl, sulfanyl, substituted calcined base, optionally substituted oxy, optionally substituted carbonyl carbonyl a substituted aryloxy group, optionally substituted heteroaryloxy group, optionally substituted heterocycloalkyloxy group, optionally substituted alkoxycarbonyl group, optionally substituted Alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryloxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted a heterocycloalkyl group, an optionally substituted amino group, an optionally substituted thiol group, an optionally substituted aminocarbonyl group, and/or a substituted carbamin 〇d〇yl; Z1 is selected from the group consisting of hydrogen and hydrogen. Substituted aryl groups, optionally substituted heteroaryl groups, optionally substituted cyclofilaments, optionally substituted 318 200823188 Heterocyclic alkyl, cyano, optionally substituted alkyl, optionally substituted fluorenyl, optionally substituted alkoxycarbonyl, optionally substituted amine, optionally substituted amine Alkylcarbonyl, optionally substituted fluorenyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted heterocycloalkane a oxy group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, a sulfonyl group, a sulfinyl group, and a sulfanyl group; the z2 group is selected from the group consisting of an anthracene, an optionally substituted thiol group, a carboxyl group, Optionally substituted alkoxycarbonyl, optionally substituted fluorenyl, optionally substituted alkenyl, optionally substituted alkyl, optionally substituted heterocycloalkyl, optionally substituted An aryl group and an optionally substituted amino group; the 15 z is selected from the group consisting of hydrogen, i, and optionally substituted alkyl; the r3 is selected from the group consisting of hydrazine and optionally substituted alkyl; and the R is derived from Anthracene, substituted alkyl group, optionally substituted alkyl, cyano group, _ group, stack Group, optionally substituted the amine group, the optionally substituted alkoxycarbonyl groups, optionally substituted amine group of prison group, continued acyl, sulfinyl group and burning sulfur group. 2. A chemical according to the first aspect of the invention, wherein the hydrazine compound is selected from the group consisting of a compound of formula I, 319 20 200823188 其中 R1及R4係獨立地選自氫、氰基、鹵基、羥基、疊 氮基、硝基、磺醯基、亞績醯基、硫烧基、視需要經 取代之烧氧基、視需要經取代之酿氧基、視需要經取 5 代之胺基羰基氧基、視需要經取代之芳基氧基、視需 要經取代之雜务基氧基、視需要經取代之雜環烧基氧 基、視需要經取代之烷氧基羰基、視需要經取代之烷 基、視需要經取代之烯基、視需要經取代之炔基、視 需要經取代之芳基氧基、視需要經取代之芳基、視需 10 要經取代之雜芳基、視需要經取代之雜環烷基、視需 要經取代之胺基、視需要經取代之醯基、視需要經取 代之胺基幾基及視需要經取代之carbaminodoyl ; Z1係選自視需要經取代之芳基及視需要經取代之 雜芳基； 15 Z2係選自氫、視需要經取代之曱肺基、羧基、視 需要經取代之烷氧基羰基、視需要經取代之醯基、視 需要經取代之烯基、視需要經取代之烷基、視需要經 取代之雜環烷基、視需要經取代之雜芳基及視需要經 取代之胺基羰基； 2〇 Z3係選自氫及視需要經取代之烧基；及 R3係選自氫及視需要經取代之烷基。 3. 至少一種如申請專利範圍第2項之化學品，其中該式I 化合物係選自式II化合物， 320 200823188319 20 200823188 wherein R1 and R4 are independently selected from the group consisting of hydrogen, cyano, halo, hydroxy, azido, nitro, sulfonyl, fluorenyl, thiol, optionally substituted alkoxy , if necessary, substituted oxy-oxyl group, if necessary, 5 times of aminocarbonyloxy group, optionally substituted aryloxy group, optionally substituted hydroxy group, substituted as needed a cycloalkyloxy group, an optionally substituted alkoxycarbonyl group, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted aryloxy group, Optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, optionally substituted amine, optionally substituted thiol, optionally substituted Amino group and optionally substituted carbaminodoyl; Z1 is selected from an optionally substituted aryl group and optionally substituted heteroaryl group; 15 Z2 is selected from hydrogen, optionally substituted silicyl group, carboxyl group Substituted alkoxycarbonyl group, optionally substituted sulfhydryl group, depending on A substituted alkenyl group, optionally substituted alkyl group, optionally substituted heterocycloalkyl group, optionally substituted heteroaryl group, and optionally substituted aminocarbonyl group; 2〇Z3 system selected from hydrogen And optionally substituted alkyl; and R3 is selected from the group consisting of hydrogen and optionally substituted alkyl. 3. At least one chemical as claimed in claim 2, wherein the compound of formula I is selected from the group consisting of a compound of formula II, 320 200823188 式II 其中 R1及R4係獨立地選自氫、視需要經取代之醯基、 視需要經取代之烷基、氰基、豳基、疊氮基、視需要 經取代之胺基、視需要經取代之烷氧基羰基、視需要 經取代之胺基羰基、磺醯基、亞磺醯基及硫烷基； Z1為視需要經取代之芳基； Z2係選自氩、視需要經取代之曱肺基、羧基、祝 需要經取代之烷氧基羰基、視需要經取代之醯基、祝 需要經取代之烯基、視需要經取代之烷基及視需要經 取代之胺基羰基； Z3係選自視需要經取代之芳烷基及視需要經取代 之雜芳烷基；及 R3係選自氫及視需要經取代之烷基。 4·至少一種如申請專利範圍第3項之化學品，其中z2係選 自羧基、視需要經取代之烷氧基羰基、視需要經取代之 醯基、視需要經取代之烯基及視需要經取代之烷基。 5.至少了種如申請專利範圍第4項之化學品，其中z2為羧 基、視需要經取代之哌啶基羰基、視需要經取代之吡啶 基幾基、視需要經取代之低碳燒基、視需要經取代之低 321 200823188 碳烯基及低碳烷氧基羰基。 • 6·至少一種如申請專利範圍第5項之化學品，其中z2係選 自（2-(N-乙醯基胺基甲基)派啶小基）魏基；（2_胺基甲基 旅咬-1-基)羰基；1-羥基_2-胺基_乙基；2-((曱基磺醯胺基) 5 甲基)派&quot;定小基羰基；2-(甲基胺基幾基）乙烯基；2十比啶 -3-基甲基)-2H-三唑-5-基；胺基甲基；羧基；甲氧基羰 基；吡啶-2-基羰基；吡啶_3_基羰基；及吡啶_4_基羰基。 7·至少一種如申請專利範圍第3至6項中任一項之化學 品，其中R3係選自氫及视需要經取代之低碳烷基。 ίο 8·至少一種如申请專利範圍第7項之化學品，其中R3係選 自氫及低碳烧基。 • 9.至少一種如申請專利範圍第8項之化學品，其中R3係選 . 自氫及甲基。 10·至少-種如申請專利範圍第9項之化學品，其中r3為氣。 15 11·至少-種如申請專利範圍第2項之化學品，其中22為 -C(0)NR2R5’其中R2係、選自視需要經取代之烧基及視需 要經取代之城基，而V細自氫及視需要經取代之乾 基。 12. 至少-種如申請專利範圍第3至u項中任一項之化學 20 品，其中R4係選自氫、氰基、鹵基、疊氮基、視需要趣 取代之胺基羰基及視需要經取代之烷基。 13. 至少-種如申請專利範圍帛12項之化土學品，其中尺4係 選自氫、氰基、氯、漠、氣、疊氮基、視需要經取代文 烧基胺基叛基及視需要經取代之甲其^ 322 200823188 14. 至少一種如申請專利範圍第π項之化學品，其中以係 -選自氫、氰基、m氮基K3—基甲基胺基幾 基、胺基甲基及羥基甲基。 15. 至少一種如申請專利範園第14項之化學品，其中^為 5 氫。 16. 至少一種如申請專利範園第Ui15項中任一項之化學 品，其中R2係選自視需要經取代之曱基、視需要經取代 之乙基、視需要經取代之丙基、視需要經取代之丁基、 視需要經取代之戊基、祝需要經取代之己基、視需要經 〇 取代之環丙基、視需要經取代之環戊基及視需要經取代 之環己基，其中各視需要經取代之基團係視需要經一、 二或三個由下列選出之基團取代：視需要經取代之芳 基、視需要經取代之雜芳基、視需要經取代之雜環炫基、 視需要纽取代之環烧基、視需要經取代之胺基幾基、視 5 需要經取代之胺基、羥基、羧基、視需要經取代之烷氧 基幾基及視需要經取代之烧氧基。 17·至少一種如申請專利範園第16項之化學品，其中尺2係 ‘自甲基和乙基，其中甲基和乙基基團係視需要經一或 3 二個由下列選出之基團取代：視需要經取代之芳基、視 需要經取代之雜芳基、視需要經取代之雜環烷基、視需 要經取代之環烷基、視需要經取代之胺基羰基、視需要 經取代之胺基、羥基、羧基、視需要經取代之烷氧基羰 基及視需要經取代之烷氧基。 18 石 •至少—種如申請專利範圍第Π項之化學品，其中R2係 323 200823188 選自 (1-(2-胺基乙基)-1Η·吼唑·3_基）甲基；（1-(曱基磺醯基)哌 咬-3-基）甲基；（1-乙醯基派咬-3-基）曱基；（1-乙酿基外匕咯 啶-2_基）曱基；(1H-咪唑-2-基）甲基；(1H-吡唑-3-基）曱基； (1-曱基·1Η_吡唑-3-基）甲基；（1-曱基-1H_吡唑-5-基）曱 基；（2-(胺基羰基）乙基胺基)羰基甲基；（2-(胺基曱基户比 啶-3-基）甲基；（2-(羧基）乙基胺基)羰基甲基；（2_(二甲基 胺基）乙基胺基)羰基曱基；(2-(羥基）乙基胺基)羰基曱基； (2-(甲基胺基）乙基胺基)羰基曱基；(2-(N-曱基-N-(第三丁 氧基羰基)-胺基）乙基胺基)羰基曱基；（2-氧基哌啶-3-基） 甲基；（3-(二曱基胺基）丙基胺基)羰基曱基；（3-(羥基）乙 基胺基）羰基曱基；（3-(第三丁氧基羰基胺基）丙基胺基） 羰基曱基；（4-(胺基曱基户比啶-2-基）曱基；（5-(胺基甲基） 吼啶-2-基）曱基；（6-((1，3_二氧基異吲哚啉-2_基）曱基)吼 11 疋基）甲基，（6_(2_胺基乙基胺基）°比咬-2-基）曱基； (6-(3-胺基丙基胺基)吼咬-2-基）曱基；（6-(胺基曱基)η比咬 -2-基）曱基；（6-(羥基曱基)吡啶-2-基）曱基；（6-溴吡啶-2-基）甲基；（曱基磺醯胺基)幾基曱基；（吼啶-2_基）乙基胺 基；1-(2-(第三丁氧基羰基胺基）乙基)-lH-吼唑-3-基甲 基；1-(2·(第三丁氧基羰基胺基）乙基)-lH-吼唑-5_基曱 基；1-(胺基羰基)-2-(胺基)-乙-1-基；1-(胺基羰基)-3-(胺 基）-丙基，1 -(胺基獄基）-4-(胺基）-丁基，1 -(胺基叛 基)-4_(苯曱基氧基羰基胺基)_戊基；1_(胺基羰基)-5-(胺 基)-戊基；1-(胺基羰基）乙-1-基；1-(羧基基)-2-(胺基)-乙 324 200823188 1-基，1_(一曱基胺基幾基）_2-(胺基）_乙_ι_基；(經 基)-2-(胺基羰基甲基胺基）乙_1_基；1_(經基)_2—_(乙氧基幾 基甲基胺基）乙-1-基；1-(羥基)-2-(吼啶-2-基甲基胺基）乙 -1-基’ 1-(甲乳基緩基)-2-(胺基)-乙-1-基；ι_(曱氧基罗炭 5 基弟二丁乳基艘基胺基)-乙-1-基；ι_(曱氧基幾基) 乙-1_基；1-(甲基胺基羰基)-2-(胺基)-乙小基(2 〇cc); 1-(甲基胺基幾基）乙-1-基；1-胺基魏基-2-經基-乙_1_基； 1- 甲氧基魏基-2-經基-乙-1-基；2-(2-胺基乙氧基）乙基； 2- (2-胺基乙基)-吼咬-6-基甲基；2-(2-胺基乙基胺基）乙 ίο 基；2_(3_氟苯基）乙基；2_(3_曱氧基羰基）乙基；2-(6-(胺 基曱基户比咬-2-基）乙基；2-(乙醯基胺基）乙基；2-(胺基) 乙基；2-(胺基羰基)-2-(乙醯基胺基)-乙-1-基；2_(胺基幾 基)-2-(胺基)-乙-1-基；2-(胺基叛基）乙基；2-(胺基曱基) 口比口定-5-基曱基，2-(叛基)-2-(胺基)-乙-1-基；2-(二甲基胺 15 基）乙基；2-(二曱基胺基幾基)-2-(胺基)ϋ基；2-(乙氧 基叛基）乙基，2-(甲氧基幾基)-2-(乙蕴基胺基)_乙_ι_基； 2-(甲氧基叛基)-2-(胺基)-乙-1-基；2-(曱氧基幾基胺基) 乙基，2-(甲基胺基）乙基，2_(曱基胺基幾基)_2_(乙酿基 胺基)-乙-1-基；2-(曱基胺基羰基)-2-(胺基卜乙^•基；2_(甲 20 基磺醯胺基）乙基；2-(曱氧基羰基)_2-(胺基)_乙4_基； 2-(N-(第三丁氧基羰基)-N-(曱基)-胺基）乙基；2_(派啡小 基）乙基；2-(吼+2_基）乙基；2十比啶_2_基）乙基；2_(口比 唆-3-基）乙基；2-(第三丁氧基魏基胺基曱基)τι比咬_3_基曱 基；2-(第三丁氧基羰基胺基曱基)吡啶-6-基曱基；2_(三 325 200823188 氟甲基比啶-6-基甲基；2-胺基吼啶-3-基甲基；2-胺基 吨啶-5-基甲基；2-氯吡啶_5_基甲基；2-氰基吼啶_5_基甲 基；2-羥基-3-胺基·丙小基；2-羥基乙基；2-甲氧基乙小 基’ 2-曱氧基σ比咬_3_基曱基；2-曱氧基ϋ比π定-5-基甲基； 2- 曱基u比啶-3-基曱基；2-曱基吡啶-5-基甲基；2-甲基口比 啶-6-基甲基·，3-(2-胺基乙基)環己基）曱基；3-(4_甲基哌 口井-l-基）丙基；3_(胺基)冬（曱基胺基羰基）丙基；3_(胺 基羰基）丙基；3-(胺基曱基)苯甲基；3_(胺基甲基)吼啶_2-基甲基；3-(甲氧基羰基）丙基；3_(甲基胺基羰基）丙基； 3- (三氟甲基)_π比啶-2-基甲基；3,4-二氟苯甲基；3-胺基甲 基吼啶-4-基甲基；3-胺基丙基；3-胺甲醯基環戊基；3-羧基丙基；3-羥基丙基；3-甲氧基丙基；4-(胺基甲基)_ °比啶-2-基甲基；4-(Ν，Ν-二曱基胺基）吡啶-3-基甲基； 4- (第三丁氧基羰基胺基)_嗎啉基甲基；4_胺基丁基；4_ 胺基甲基吼啶-3-基曱基；4-氰基苯曱基；4-氟苯曱基； 4-曱基胺基吼啶-3-基甲基；4-甲基苯曱基；4-嗎啉基吡 啶-3-基曱基；4-哌畊基吡啶-3-基甲基；5-((雙(二甲基胺 基）甲基月女基）甲基户比咬-3-基曱基；5-(胺基甲基)吼咬_2_ 基曱基；5-(胺基甲基)π比咬_3_基曱基；5_(經基曱基)π比咬 -3-基曱基；5_(第三丁氧基羰基胺基甲基)_σ比啶-2_基甲 基；5-(三氟甲基)-π比啶1基甲基；5_胺基戊基；5_胺基 口比啶-2-基甲基；6-((雙(二曱基胺基)伸曱基胺基）曱基)吡 啶-2-基）甲基；6-(4-乙醯基哌畊-1-基）吼啶_3_基甲基）； 6-(胺基甲基)吼啶-2-基）甲基；6-胺基己基；胺基羰基曱 326 200823188 基；苯甲基；環丙基曱基；二甲基胺基羰基曱基；異丙 基；異噚唑-5-基甲基；甲氧基羰基甲基；曱基；曱基胺 基羰基曱基；哼唑-2-基曱基；哌啶-4-基甲基；丙-2-烯-1-基；吡口井-2-基甲基；吡啶-2-基曱基；吡啶-2-基甲基-N-5 氧化物；吡啶-3-基曱基；吡啶-3-基曱基-N-氧化物；吡 ϋ定-4-基曱基，嗟吩-2-基曱基，及σ塞吩-3-基甲基。 19. 至少一種如申請專利範圍第3至18項中任一項之化學 品，其中Ζ3係選自-(CH2)rR2G，其中r係選自1、2及3， 且R2G係選自視需要經取代之芳基及視需要經取代之雜 10 芳基。 20. 至少一種如申請專利範圍第19項之化學品，其中Z3係 ' 選自2-(3-曱基苯基）乙基、2-(1Η-咪唑-4-基）乙基、2-(1- - 曱基-1H-咪唑-4-基）乙基、2-(2,3-二氟苯基）乙基、2-(2,5- 二氣苯基）乙基、2-(2,6-二鼠苯基）乙基、2-(2-鼠苯基）乙 15 基、2-(2-氧基苯基）乙基、2-(2-氣苯基）乙基、2-(2-經基 苯基）乙基、2-(2-曱氧基苯基）乙基、2-(2-甲基苯基）乙 基、2-(3-(三氟甲基）苯基）乙基、2-(3,4-二氟苯基）乙基、 2-(3,5-二氟苯基）乙基、2-(3,5-二曱基-1H-吡唑-1-基）乙 基、2-(3,5-二曱基-1H-吡唑-4-基）乙基、2-(3-胺曱醯基苯 2〇 基）乙基、2-(3-羧基苯基）乙基、2-(3-氰基苯基）乙基、2_(3_ 氣苯基)-2-(輕基)-乙基、2-(3-氣苯基）乙基、二-口-氣11比咬 -2-基）乙基、2_(3_曱氧基羰基苯基）乙基、2-(3-曱氧基苯 基）乙基、2-(3-曱基苯基）乙基、2-(4-胺基苯基）乙基、2-(4-氯苯基）乙基、2-(4-氟苯基）乙基、2-(4-羥基苯基）乙基、 327 10 15 20 200823188 基、2伤基）乙基、2_(咬喃2-基）乙 基）乙基、2十 土)乙基、2_(苯基）乙基、2十岐_2_ 基丙小基、3_im 土）乙基、2十塞吩_2_基）乙基、2-苯 基、吡啶-2-基τ:;，1:基)丙_1_基、3_苯基丙基、苯甲 21.至少-種如比咬·3_基甲基及嗟吩-3-基甲基。 2十比唆-2-基利範圍第2〇項之化學品，其中Ζ3為 夕種如申請專利範圍 品，其中Ζ1係撰白、目干 至21員中任—項之化學 取代之芳A H而要經—或二個由下列選出之基團 代之燒基、視1二ΐ基、經基、甲酸基、視需要經取 基、幾基、視:、，二代之烯基、視需要經取代之烧氧 之酿基、視^ 取代之烧氧基幾基、視需要經取代 基、視需^幾t、視需要經取代之胺 視需要經取代夕田^ %&lt;说基、視需要經取代之雜芳基、 23 5 /h _ _ 甲脒基及視需要經取代之磺醯基。 、登二如申請專利範圍第22項之化學品，其中Z1係 而要經—或二個由下列選出之基團取代之苯基： 虱自基、羥基、曱醯基、視需要經取代之低碳烷基、 ,¼，基、低碳烷氧基、羧基、視需要經取代之低碳烷 氧基，基、低碳醯基、二烷基胺基、乙醯基胺基、視需 要經氮基、芳烷基及雜芳烷基取代之甲脒基以及胺基羰 基。 24· ^少一種如申請專利範圍第23項之化學品，其中Z1係 k自本基、2-胺基叛基苯基、2-氟苯基、2·氯苯基、2- 328 200823188 羥基笨基、2-曱基苯基、2-曱氧基苯基、2-氰基苯基、2-氰基甲基笨基、2-乙烯基苯基、2-甲醯基苯基、_3,4-二氟 苯基、3-甲基苯基、3-氯苯基、3-氟苯基、3-氰基苯基、 3- 二曱基胺基苯基、3-曱氧基苯基、3-甲氧基甲基苯基、 5 3-羥基苯基、3-三氟曱基苯基、4-胺基羰基苯基、4-氟苯 基、4-氯苯基、4-曱基苯基、4-羥基苯基、4-氰基苯基、 4- 曱乳基苯基、4-輕基曱基苯基、4-二氣曱基苯基、4_ 曱氧基羰基苯基、4-二甲基胺基苯基、4-乙醯基苯基、 4-羧基苯基、4-乙基苯基、4-乙醯基胺基苯基、3,4-二氯 ίο 苯基、3,4-二氟苯基、2,3-二甲基苯基、2,5-二曱基苯基、 2,4-二甲基苯基、3,5-二甲基苯基、3,4-二甲基苯基、2-氮-4-氣-苯基、2-鼠基-4-氣-苯基、2-鼠-6-氣-苯基、2-氯 -4-曱乳基-苯基、2-鼠基-4-曱乳基-苯基、2-襄基-6-氣_ 苯基、2-氣-5-鼠-苯基、2-氣基-5-氣-苯基、2-氯-4-甲基 15 苯基、2-氯-4-羥基甲基-苯基、2-(N-(吼啶-3-基曱基）甲脒 基)苯基及2-氣基-4-曱基苯基。 25. 至少一種如申請專利範圍第3至24項中任一項之化學 品，其中R1係選自氫及視需要經取代之低碳烧基。 26. 至少一種如申請專利範圍第25項之化學品，其中R1係 20 選自氬及低碳烷基。 27. 至少一種如申請專利範圍第26項之化學品，其中R1係 選自氫及曱基。 28. 至少一種如申請專利範圍第2項之化學品，其中該式I 化合物係選自式III化合物 329 200823188Wherein R 1 and R 4 are independently selected from the group consisting of hydrogen, optionally substituted fluorenyl, optionally substituted alkyl, cyano, decyl, azide, optionally substituted amine, optionally Substituted alkoxycarbonyl, optionally substituted aminocarbonyl, sulfonyl, sulfinyl and sulfanyl; Z1 is an optionally substituted aryl; Z2 is selected from argon, optionally substituted Silicyl group, carboxyl group, wishing substituted alkoxycarbonyl group, optionally substituted fluorenyl group, wishing substituted alkenyl group, optionally substituted alkyl group and optionally substituted aminocarbonyl group; Z3 Is selected from the group consisting of an optionally substituted aralkyl group and optionally substituted heteroaralkyl; and R3 is selected from the group consisting of hydrogen and optionally substituted alkyl. 4. At least one chemical as claimed in claim 3, wherein z2 is selected from the group consisting of a carboxyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted thiol group, an optionally substituted alkenyl group, and optionally Substituted alkyl group. 5. At least one such as the chemical of claim 4, wherein z2 is a carboxyl group, optionally substituted piperidinylcarbonyl, optionally substituted pyridyl group, optionally substituted low carbon alkyl group , as required to replace the low 321 200823188 carboxyalkenyl and lower alkoxycarbonyl. • 6. At least one chemical as claimed in claim 5, wherein z2 is selected from the group consisting of (2-(N-ethylidinomethyl)methylpyridinyl)wei (; 2-aminomethyl) TB-1-yl)carbonyl; 1-hydroxy-2-amino-ethyl; 2-((fluorenylsulfonylamino) 5 methyl)pyry&quot; carboxylic acid; 2-(methylamine) Vinyl; 2 decathyridin-3-ylmethyl)-2H-triazol-5-yl; aminomethyl; carboxy; methoxycarbonyl; pyridin-2-ylcarbonyl; pyridine _3 a carbonyl group; and a pyridine-4-ylcarbonyl group. A chemical according to any one of claims 3 to 6, wherein R3 is selected from the group consisting of hydrogen and optionally substituted lower alkyl. Ίο 8· At least one of the chemicals of claim 7 wherein R3 is selected from the group consisting of hydrogen and low carbon. • 9. At least one chemical as claimed in item 8 of the patent application, in which R3 is selected from hydrogen and methyl. 10. At least - a chemical as claimed in claim 9 wherein r3 is gas. 15 11 · At least - a chemical as in claim 2, wherein 22 is -C(0)NR2R5' wherein R2 is selected from the group which is optionally substituted and optionally substituted. V is finely self-hydrogenated and optionally substituted. 12. At least one of the chemical products of any one of claims 3 to 5, wherein R4 is selected from the group consisting of hydrogen, cyano, halo, azide, optionally substituted aminocarbonyl and A substituted alkyl group is required. 13. At least - a variety of petrochemicals such as the scope of patent application ,12, wherein the rule 4 is selected from the group consisting of hydrogen, cyano, chlorine, desert, gas, azide, and optionally substituted arylamino And 322 200823188 14. At least one chemical as in the scope of claim π, wherein the system is selected from the group consisting of hydrogen, cyano, m-nitro K3-methylamino group, Aminomethyl and hydroxymethyl. 15. At least one chemical, such as patent application No. 14, wherein ^ is 5 hydrogen. 16. A chemical according to any one of the preceding claims, wherein R2 is selected from the group consisting of an optionally substituted thiol group, an optionally substituted ethyl group, an optionally substituted propyl group, and optionally A substituted butyl group, an optionally substituted pentyl group, a substituted hexyl group, a cyclopropyl group which is optionally substituted by hydrazine, a cyclopentyl group which may be optionally substituted, and a cyclohexyl group which may be optionally substituted, wherein Each of the optionally substituted groups may be substituted by one, two or three groups selected as follows: an optionally substituted aryl group, an optionally substituted heteroaryl group, optionally substituted heterocyclic ring. A thiol group, a ring-substituted group which is optionally substituted with a ring, an amine group which may be substituted as required, an amine group which needs to be substituted, a hydroxyl group, a carboxyl group, an alkoxy group which is optionally substituted, and optionally substituted Alkoxy groups. 17. At least one chemical as claimed in claim 16 wherein the rule 2 is 'from methyl and ethyl, wherein the methyl and ethyl groups are optionally selected from one or three of the following groups. Substituted: an optionally substituted aryl group, optionally substituted heteroaryl group, optionally substituted heterocycloalkyl group, optionally substituted cycloalkyl group, optionally substituted aminocarbonyl group, optionally substituted aminocarbonyl group, if desired Substituted amine group, hydroxyl group, carboxyl group, optionally substituted alkoxycarbonyl group and optionally substituted alkoxy group. 18石•At least—a chemical of the scope of the patent application, wherein R2 is 323 200823188 selected from (1-(2-aminoethyl)-1Η·carbazole-3-yl)methyl; -(fluorenylsulfonyl)piperidin-3-yl)methyl; (1-ethylindenyl-3-yl)indenyl; (1-ethyl-bromo-purine-2-yl) (1H-imidazol-2-yl)methyl; (1H-pyrazol-3-yl)indolyl; (1-indolyl-1Η-pyrazol-3-yl)methyl; (1-indenyl) -1H_pyrazol-5-yl)indenyl; (2-(aminocarbonyl)ethylamino)carbonylmethyl; (2-(aminomercaptopuridin-3-yl)methyl; 2-(carboxy)ethylamino)carbonylmethyl; (2-(dimethylamino)ethylamino)carbonylcarbonyl; (2-(hydroxy)ethylamino)carbonylindenyl; (2- (methylamino)ethylamino)carbonylcarbonyl; (2-(N-fluorenyl-N-(t-butoxycarbonyl)-amino)ethylamino)carbonylcarbonyl; (2- Oxypiperidin-3-yl)methyl; (3-(didecylamino)propylamino)carbonylindenyl; (3-(hydroxy)ethylamino)carbonylindenyl; (3-( Third butoxycarbonylamino)propylamino)carbonylcarbonyl; (4-(amino fluorenyl) (2-(aminomethyl) acridine-2-yl)indolyl; (6-((1,3-dioxyisoindoline-2-yl)anthracene)吼11 疋 )) methyl, (6-(2-aminoethylamino) ° 咬-2-yl) fluorenyl; (6-(3-aminopropylamino) 吼-2 -yl) fluorenyl; (6-(amino fluorenyl) η than butyl-2-yl) fluorenyl; (6-(hydroxyindenyl)pyridin-2-yl)indenyl; (6-bromopyridine-2 -yl)methyl; (fluorenylsulfonylamino) benzyl hydrazino; (acridin-2-yl)ethylamino; 1-(2-(t-butoxycarbonylamino)ethyl) -lH-carbazol-3-ylmethyl; 1-(2.(t-butoxycarbonylamino)ethyl)-lH-indazole-5-ylindenyl; 1-(aminocarbonyl)- 2-(Amino)-eth-1-yl; 1-(aminocarbonyl)-3-(amino)-propyl, 1-(amino-phenyl)-4-(amino)-butyl, 1-(Amino-reactive)-4-(phenylhydrazyloxycarbonylamino)-pentyl; 1-(aminocarbonyl)-5-(amino)-pentyl; 1-(aminocarbonyl)- 1-yl; 1-(carboxyl)-2-(amino)-ethane 324 200823188 1-yl, 1-(indolylamino)-2-(amino)-ethylidene; Base)-2-(aminocarbonylmethylamino)ethyl-1-yl; 1_(base) _2-((ethoxymethylmethylamino)ethyl-1-yl; 1-(hydroxy)-2-(acridin-2-ylmethylamino)ethyl-1-yl' 1-(A乳基基基)-2-(Amino)-eth-1-yl; ι_(曱 罗 罗 5 5 基 二 丁 艘 - - - - - - 乙 乙 ι ι ι ι ι ι ι Alkyl-1 -yl-l-(methylaminocarbonyl)-2-(amino)-ethyl small group (2 〇cc); 1-(methylaminomethyl)ethyl-1-yl ; 1-aminocarbyl-2-yl-ethyl-1-yl; 1-methoxyweiyl-2-yl-ethyl-1-yl; 2-(2-aminoethoxy) 2-(2-Aminoethyl)-anthracene-6-ylmethyl; 2-(2-aminoethylamino)ethyl; 2-(3-fluorophenyl)ethyl; 2_ (3_decyloxycarbonyl)ethyl; 2-(6-(amino fluorenyl)-yl-2-yl)ethyl; 2-(ethionylamino)ethyl; 2-(amino) Ethyl; 2-(aminocarbonyl)-2-(ethenylamino)-eth-1-yl; 2-(aminomethyl)-2-(amino)-eth-1-yl; 2- (amino thiol)ethyl; 2-(amino fluorenyl) phenoxyl-5-yl fluorenyl, 2-(inferior)-2-(amino)-eth-1-yl; 2- (dimethylamine 15 yl)ethyl; 2-(didecylamino)-2-(amino)indenyl; 2-(ethoxylated)ethyl, 2-(A 2-yl)-2-(ethylamino)-ethylidene; 2-(methoxy-reactive)-2-(amino)-eth-1-yl; 2-(decyloxy) Alkylamino)ethyl, 2-(methylamino)ethyl, 2-(indolylamino)_2-(ethenylamino)-eth-1-yl; 2-(decylamino) Carbonyl)-2-(aminophenylethyl); 2-(methyl 20-sulfonylamino)ethyl; 2-(decyloxycarbonyl)_2-(amino)-ethyl-4-yl; 2-( N-(Tertidinoxycarbonyl)-N-(indenyl)-amino)ethyl; 2-(p-pylinyl)ethyl; 2-(indol-2-yl)ethyl; _2 基 乙基 ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; Tributoxycarbonylamino-mercapto)pyridine-6-ylindenyl; 2_(three 325 200823188 fluoromethylpyridin-6-ylmethyl; 2-aminopyridin-3-ylmethyl; 2- Amino oxaridin-5-ylmethyl; 2-chloropyridine-5-ylmethyl; 2-cyanoacridine-5-ylmethyl; 2-hydroxy-3-amino-propanyl; 2- Hydroxyethyl; 2-methoxyethyl small group '2-methoxyl σ ratio bite _3_ fluorenyl; 2-decyloxy hydrazine ratio π--5-ylmethyl; 2- fluorenyl u ratio Pyridin-3-ylindenyl; 2-mercaptopyridine-5-ylmethyl 2-methyl-p-pyridin-6-ylmethyl·, 3-(2-aminoethyl)cyclohexyl)indenyl; 3-(4-methylpiperidin-l-yl)propyl; 3_ (amino) winter (decylaminocarbonyl)propyl; 3-(aminocarbonyl)propyl; 3-(aminoindenyl)benzyl; 3-(aminomethyl)acridin-2-yl 3-(methoxycarbonyl)propyl; 3-(methylaminocarbonyl)propyl; 3-(trifluoromethyl)-π-pyridin-2-ylmethyl; 3,4-difluorobenzoate 3-aminomethyl acridin-4-ylmethyl; 3-aminopropyl; 3-amine-methylmethylcyclopentyl; 3-carboxypropyl; 3-hydroxypropyl; 3-methoxy Propyl; 4-(aminomethyl)_ °pyridin-2-ylmethyl; 4-(anthracene, fluorenyl-didecylamino)pyridin-3-ylmethyl; 4- (third Oxycarbonylamino) morpholinomethyl; 4-aminobutyl; 4-aminomethyl acridine-3-ylindenyl; 4-cyanobenzoinyl; 4-fluorophenylindenyl; - mercaptoamino acridine-3-ylmethyl; 4-methylphenylindenyl; 4-morpholinylpyridin-3-ylindenyl; 4-piperidinylpyridin-3-ylmethyl; 5- ((bis(dimethylamino)methyl), methyl group, -3-yl fluorenyl group; 5-(aminomethyl), bite, _2, thiol group; 5-(amino group A) Base) π Ratio _3_ mercapto group; 5_(via fluorenyl) π ratio -3-yl fluorenyl; 5_(t-butoxycarbonylaminomethyl)_σpyridin-2-ylmethyl; -(trifluoromethyl)-π-pyridyl 1 -methyl; 5-aminopentyl; 5-aminolpyridin-2-ylmethyl; 6-((bis(didecylamino)) Nonylamino)mercapto)pyridin-2-yl)methyl; 6-(4-ethinylpiperidin-1-yl)acridine-3-ylmethyl); 6-(aminomethyl) Acridine-2-yl)methyl; 6-aminohexyl; aminocarbonyl 曱 326 200823188; benzyl; cyclopropyl fluorenyl; dimethylaminocarbonylcarbonyl; isopropyl; isoxazole -5-ylmethyl; methoxycarbonylmethyl; fluorenyl; decylaminocarbonylcarbonyl; oxazol-2-ylindenyl; piperidin-4-ylmethyl; prop-2-ene-1 -yl; pyridyl-2-ylmethyl; pyridin-2-ylindenyl; pyridin-2-ylmethyl-N-5 oxide; pyridin-3-ylindenyl; pyridin-3-ylindenyl -N-oxide; pyridin-4-ylindenyl, porphin-2-ylindenyl, and σ-secen-3-ylmethyl. The chemical according to any one of claims 3 to 18, wherein the Ζ3 is selected from the group consisting of -(CH2)rR2G, wherein the r is selected from 1, 2 and 3, and the R2G is selected from the group as needed. Substituted aryl and optionally substituted hetero 10 aryl. 20. At least one chemical according to claim 19, wherein the Z3 system is selected from the group consisting of 2-(3-mercaptophenyl)ethyl, 2-(1Η-imidazol-4-yl)ethyl, 2- (1- -indolyl-1H-imidazol-4-yl)ethyl, 2-(2,3-difluorophenyl)ethyl, 2-(2,5-diphenyl)ethyl, 2- (2,6-di-r-phenyl)ethyl, 2-(2-rhenylphenyl)ethyl 15-yl, 2-(2-oxyphenyl)ethyl, 2-(2-phenylphenyl)ethyl , 2-(2-Phenylphenyl)ethyl, 2-(2-decyloxyphenyl)ethyl, 2-(2-methylphenyl)ethyl, 2-(3-(trifluoromethyl) Phenyl)ethyl, 2-(3,4-difluorophenyl)ethyl, 2-(3,5-difluorophenyl)ethyl, 2-(3,5-diindolyl-1H -pyrazol-1-yl)ethyl, 2-(3,5-dimercapto-1H-pyrazol-4-yl)ethyl, 2-(3-aminoindenyl-2-yl)ethyl , 2-(3-carboxyphenyl)ethyl, 2-(3-cyanophenyl)ethyl, 2-(3-hydroxyphenyl)-2-(light-based)-ethyl, 2-(3- gas Phenyl)ethyl, di-oral-gas 11 butyl-2-yl)ethyl, 2-(3-hydroxycarbonylphenyl)ethyl, 2-(3-decyloxyphenyl)ethyl, 2-(3-mercaptophenyl)ethyl, 2-(4-aminophenyl)ethyl, 2-(4-chlorophenyl)ethyl , 2-(4-fluorophenyl)ethyl, 2-(4-hydroxyphenyl)ethyl, 327 10 15 20 200823188, 2, ethyl, 2-((2-yl)ethyl) Ethyl, 20 earth) ethyl, 2-(phenyl)ethyl, 2 decyl-2-ylpropanyl, 3_im)ethyl, 20-thenyl-2-yl)ethyl, 2-phenyl , pyridin-2-ylτ:;, 1: base) propyl-1-yl, 3-phenylpropyl, benzene 21. At least one species such as bis-methylamino and porphin-3-yl methyl. 210 唆-2-Kili range of the second item of the chemical, of which Ζ3 is the eve species such as the scope of the patent application, of which Ζ1 is a white, and the target is to 21 members - the chemical substitution of the aromatic AH And the group selected by the following - or two groups selected by the following are substituted, 1 dimethyl group, thiol group, formic acid group, optionally taken base, several groups, depending on:, second generation alkenyl, visual The substituted oxygen-burning base, the substituted alkoxy group, the substituent as needed, the amine which is optionally substituted, and the amine which is substituted as needed may be replaced by Xitian^%&lt; Substituted heteroaryl, 23 5 /h _ _ mercapto and optionally substituted sulfonyl. , as in the application for the chemical scope of the 22nd item of the chemical, in which Z1 is to be replaced by - or two of the following selected groups: 虱 from the base, hydroxyl, thiol, as needed Lower alkyl, 1⁄4, yl, lower alkoxy, carboxy, optionally substituted lower alkoxy, carbyl, lower fluorenyl, dialkylamino, ethionyl, on-demand A mercapto group substituted with a nitrogen group, an aralkyl group, and a heteroaralkyl group, and an aminocarbonyl group. 24· Less one chemical as in claim 23, wherein Z1 is k from the base, 2-amino thiophenyl, 2-fluorophenyl, 2-chlorophenyl, 2-328 200823188 hydroxyl Stupyl, 2-mercaptophenyl, 2-decyloxyphenyl, 2-cyanophenyl, 2-cyanomethylphenyl, 2-vinylphenyl, 2-methylnonylphenyl, _3 ,4-difluorophenyl, 3-methylphenyl, 3-chlorophenyl, 3-fluorophenyl, 3-cyanophenyl, 3-didecylaminophenyl, 3-decyloxybenzene , 3-methoxymethylphenyl, 5 3-hydroxyphenyl, 3-trifluorodecylphenyl, 4-aminocarbonylphenyl, 4-fluorophenyl, 4-chlorophenyl, 4- Nonylphenyl, 4-hydroxyphenyl, 4-cyanophenyl, 4-fluorenylphenyl, 4-light-based nonylphenyl, 4-dimethylnonylphenyl, 4-methoxycarbonylbenzene Base, 4-dimethylaminophenyl, 4-ethenylphenyl, 4-carboxyphenyl, 4-ethylphenyl, 4-ethylguanidinophenyl, 3,4-dichloro Phenyl, 3,4-difluorophenyl, 2,3-dimethylphenyl, 2,5-dimercaptophenyl, 2,4-dimethylphenyl, 3,5-dimethylbenzene Base, 3,4-dimethylphenyl, 2-nitro-4-a-phenyl, 2-nitriyl-4-a-phenyl, 2-murine-6-gas-phenyl, 2-chloro-4-hydrazino-phenyl, 2-muryl-4-indene-phenyl, 2-mercapto-6-a-phenyl, 2-gas-5-murine-phenyl, 2-carbyl-5-gas-phenyl, 2-chloro-4-methyl15 phenyl, 2-chloro-4-hydroxymethyl-phenyl, 2- (N-(Acridine-3-ylmercapto)methyl)phenyl and 2-aphthyl-4-mercaptophenyl. A chemical according to any one of claims 3 to 24, wherein R1 is selected from the group consisting of hydrogen and optionally substituted low carbon alkyl. 26. At least one chemical as claimed in claim 25, wherein the R1 system 20 is selected from the group consisting of argon and a lower alkyl group. 27. At least one chemical as claimed in claim 26, wherein R1 is selected from the group consisting of hydrogen and sulfhydryl. 28. At least one chemical of claim 2, wherein the compound of formula I is selected from the group consisting of a compound of formula III 329 200823188 式III 其中 R1及R4係獨立地選自氫、視需要經取代之醯基、 視需要經取代之烷基、氰基、鹵基、疊氮基、視需要經 取代之胺基、視需要經取代之烷氧基羰基、視需要經取 代之胺基羰基、磺醯基、亞磺醯基及硫烷基； Z1為視需要經取代之雜芳基； Z2係選自氫、視需要經取代之甲脒基、羧基、視需 要經取代之烧氧基羰基、視需要經取代之醯基、視需要 經取代之烯基、視需要經取代之烷基及視需要經取代之 胺基羰基； z係選自視需要經取代之芳院基及視需要經取代 之雜芳烷基；及 R3係選自氫及視需要經取代之烷基。 29 2S •主夕一種如申請專利範圍第28項之化學品，其中21係 k自1H-吼吨-3-基；1Η-σ比吐-4-基；1H_三唾_5_基· 1 甲基_1H_吡唑_4_基；1-曱基_m-吡唑-5-基；2-胺基甲爲 °塞吩-5-基；2-氰基噻吩冬基；2-曱醯基噻吩-3-基； 酿基噻吩-4-基；2H-吡咯-1(5H)-基；2-羥基甲基嗟吩一3_ 基，2-羥基曱基噻吩-4-基；2-羥基甲基噻吩-5-基；3_胺 330 200823188 基甲基σ塞吩-2基，3 -氣基-1 -曱基-1 Η-π比0坐-4-基，3-氧基 嗟_吩-4-基，3-曱酸基σ奏吩-2-基，3-經基甲基ϋ塞吩-2-基， 4- 甲基噻吩-2-基；4-曱基噻吩-3_基；5-(1-羥基乙-1-基)-17奏吩基，5-乙酿·基0奏吩-5-基，5-氣基-1Η-ϋ比唾-4-基， 5 5-氣基-1-曱基-1Η-ϋ比11 坐-4-基，5-氮基σ塞吩-2-基，5-曱酸 基噻吩-2-基；5-羥基曱基噻吩-2-基；異哼唑-4-基；吡啶 -2-基，12比ϋ定-3-基，ϋ比ϋ定-4-基，ϋ塞11 坐-2-基，ϋ塞吩-2-基， 及ϋ塞吩-3 -基。 30. 至少一種如申請專利範圍第29項之化學品，其中Ζ1係 ίο 選自1Η·吡唑-3-基；1Η-吡唑-4-基；1Η-三唑-5-基；1- 曱基-1Η-吡唑-4-基；1·曱基-1Η_吡唑-5-基；2-(羥基曱基) 噻吩-3-基；2,2’-二吡啶；2,3’-二吡啶；2,4’-二吡啶；2-氰基噻吩-3-基；2-曱醯基噻吩-3-基；3-(羥基曱基)噻吩 -2-基；3-氰基-1-曱基-1Η-吡唑-4-基；3-曱醯基噻吩-2-15 基，4-氣基嗟吩-3-基，4-甲基17塞吩-2-基，4-曱基σ塞吩-3- 基；5_(1_羥基乙基)噻吩-2-基；5-(胺基曱基)噻吩-2-基； 5- (羥基曱基)噻吩-2-基；5-(羥基曱基)噻吩-3-基；5-乙醯 基噻吩-2_基；5-氰基-1Η-吡唑-4-基；5-氰基-1-曱基-1Η-吡唑-4-基；5-氰基噻吩-2-基；5-曱醯基噻吩-2_基；5-甲 20 醯基噻吩-3-基；3-(胺基曱基)噻吩-2-基；異崎唑-4-基； σ泰U坐_2_基，。泰吩-2-基，及σ塞吩-3-基。 31. 至少一種如申請專利範圍第28至30項中任一項之化學 品，其中Ζ2係選自羧基、視需要經取代之烷氧基羰基、 視需要經取代之醯基、視需要經取代之烯基及視需要經 331 200823188 取代之烷基。 32. 至少一種如申請專利範圍第31項之化學品，其中Z2係 選自羧基、視需要經取代之哌啶基羰基、視需要經取代 之吡啶基羰基、視需要經取代之低礙烷基、視需要經取 5 代之低碳烯基及低碳烷氧基羰基。 33. 至少一種如申請專利範圍第32項之化學品，其中Z2係 選自2-(甲基胺基)-2-乳基乙基、2-胺基-2-乳基乙基、3_ 胺基-3-氧基丙基、（2-(N-乙醯基胺基曱基)哌啶-1-基）羰 基，（2-胺基甲基旅淀-1-基)_炭基，1-輕基-2-胺基-乙基， ίο 2-((曱基磺醯胺基）甲基)哌啶-1-基羰基；2-(甲基胺基羰 基）乙烯基；2-(吡啶-3-基曱基)-2H-三唑-5-基；胺基曱 基；羧基；曱氧基羰基；吼啶-2-基羰基；吡啶-3-基羰基； - 及^比17定-4-基援基。 34. 至少一種如申請專利範圍第28至33項中任一項之化學 15 品，其中R3係選自氫及視需要經取代之低碳烷基。 35. 至少一種如申請專利範圍第34項之化學品，其中R3係 選自氳及低碳烷基。 36. 至少一種如申請專利範圍第35項之化學品，其中R3係 選自氫及甲基。 20 3 7.至少一種如申請專利範圍第36項之化學品，其中R3為 氫。 38.至少一種如申請專利範圍第28項之化學品，其中Z2為 -C(0)NR2R5，其中R2係選自視需要經取代之烷基及視需 要經取代之環烧基；而R5係選自氫及視需要經取代之烧 332 200823188 基。 39.至少一種如申請專利範圍第28至38項中任一項之化學 品，其中R4係選自氫、氰基、鹵基、疊氮基、視需要經 取代之胺基数基及視需要經取代之炫基。 40·至少一種如申請專利範圍第39項之化學品，其中R4係 選自氫、亂基、氯、溴、氟、疊氮基、視需要經取代之 烧基胺基羰基及視需要經取代之甲基。 41·至少一種如申請專利範圍第4〇項之化學品，其中R4係 10 15 選自氫、氰基、氯、溴、疊氮基、，比啶_3_基甲基胺基羰 基、胺基甲基及羥基甲基。 42·至少一種如申請專利範圍第41項之化學品，其中R4為 43.至少 住別r堉寻利範圍第38至42項中任一項之化學 品’其中R2係選自視需要經取代之甲基、視需要經 之乙基m經取代之丙基、視需要經取代之丁美、 =要！取代之戊基、視需要經取代之己基 ： 之環己基，其中久視•要一，衣戊基及視而要經取代 二或三個由下：二取二之^ 基、視需要經取代之雜芳基、視需要經：之:取，之芳 視需要經取代之環烷基、視需要麫 烷基、 基羰基及視需要、經 取二燒視需要經取代之燒氧 至少-種如中請專利範圍第43項之化學品，其中, 333 44. 20 200823188 进自甲基及乙基，#中該甲基及乙基基團係視需要經一 戈们由下列返出之基風取代·視需要經取代之芳基、 ，需要經取代之雜芳基、視需要經取代之雜環烷基、視 需要經取代之環烷基、視需要經取代之胺基羰基、視需 要經取代之胺基、羥基、羧基、視需要經取代之烷氧基 羰基及視需要經取代之烷氧基。 45·至少一種如申請專利範圍第43項之化學品，其中^係 選自（1_(2-胺基乙基)_1H—吡唑各基）甲基；士（曱基磺醯 基)旅唆-3-基）甲基；（i_乙醯基旅嘴基）曱基；乙醯 基°比咯咬-2_基）曱基；（1H-咪嗤-2-基）甲基；（1HH3-基）甲基；（1_曱基_111』比。坐_3_基）甲基；（ι_曱基_ιη_π比口坐 -5-基）曱基；（2-(胺基羰基）乙基胺基)羰基甲基；（2_(胺基 甲基）吼唆各基）甲基；〇(羧基）乙基胺基）幾基曱基； (2-(二曱基胺基）乙基胺基)羰基曱基；(2_(羥基）乙基胺基） 羰基甲基；（2_(甲基胺基）乙基胺基）幾基曱基；（2-(Ν_ 曱基(第三丁氧基羰基)_胺基）乙基胺基)幾基曱基；（2_ 氧基哌啶-3-基）曱基；（3-(二甲基胺基）丙基胺基)羰基甲 基；（3-(羥基）乙基胺基)羰基曱基；（3_(第三丁氧基羰基 胺基）丙基胺基）羰基曱基；（4-(胺基甲基）吼咬基）曱 基；（5_(胺基曱基户比啶_2_基）甲基；（6_((1，3_二氧基異吲 哚啉-2-基）甲基)吼啶-2-基）甲基；（6_(2_胺基乙基胺基)u比 咬-2-基）曱基；（6-(3-胺基丙基胺基）π比咬_2_基）曱基； (6-(胺基曱基户比啶基）甲基；（6_(羥基曱基),比啶冬基） 甲基；（6-溴吼啶-2-基）甲基；（甲基磺醯胺基)幾基甲基； 334 200823188 (口比啶-2-基）乙基胺基；1-(2-(第三丁氧基羰基胺基）乙 基σ坐-3-基曱基，1-(2-(第二丁氧基辣基胺基）乙 基plH-utb12坐-5-基甲基，1-(胺基 &gt;炭基)-2-(胺基)-乙-1-基， 1-(胺基羰基)-3-(胺基)-丙基；1-(胺基羰基)-4-(胺基)-丁 5 基；1-(胺基羰基)-4-(苯曱基氧基羰基胺基)-戊基；1-(胺 基搂基）-5-(胺基)-戍基，1-(胺基搂基）乙-1-基，1-(叛 基)-2-(胺基)-乙-1-基，1-(二曱基胺基綠基)-2-(胺基)·乙 -1-基，1-(經基)-2-(胺基搂基曱基胺基）乙-1-基，1-(輕 基)-2-(乙氧基羰基曱基胺基）乙-1-基；1-(羥基)-2-(吼啶 1〇 -2-基曱基胺基）乙-1 -基，1 -(曱氧基綠基)-2-(胺基)-乙-1 - 基，1-(甲乳基綠基)-2-(第二丁乳基搂基胺基)-乙-1-基， 1- (曱氧基叛基）乙-1-基，1-(曱基胺基獄基)-2-(胺基)-乙 * -1 -基(2 occ)，1-(曱基胺基祿基）乙-1 -基，1 -胺基被基-2_ 羥基-乙-1-基；1-甲氧基羰基-2-羥基-乙-1-基；2-(2-胺基 15 乙乳基）乙基，2-(2-胺基乙基)-0比σ定-6-基甲基，2-(2-胺基 乙基胺基）乙基，2-(3-氣苯基）乙基，2-(3-甲乳基綠基）乙 基；2-(6-(胺基曱基)吼啶-2-基）乙基；2-(乙醯基胺基）乙 基，2-(胺基）乙基，2-(胺基祿基)-2-(乙酸基胺基)-乙-1-基，2-(胺基繞基)-2-(胺基)-乙-1-基，2-(胺基_炭基）乙基， 20 2-(胺基甲基户比啶-5-基曱基；2-(羧基)-2-(胺基)-乙-1-基； 2- (二曱基胺基）乙基；2-(二甲基胺基羰基)-2-(胺基)-乙-1-基；2-(乙氧基羰基）乙基；2-(曱氧基羰基)-2-(乙醯基胺 基)-乙-1-基；2-(曱氧基羰基)-2-(胺基)-乙-1-基；2-(曱氧 基幾基胺基）乙基，2-(曱基胺基）乙基，2-(曱基胺基幾 335 200823188 基)-2-(乙醯基胺基)-乙基；2-(曱基胺基羰基)_2_(胺 基）-乙-1-基；2-(甲基磺醯胺基）乙基；2_(曱氧基羰 基)_2_(胺基)_乙小基；2_(N_(第三丁氧基羰基)_N_(甲基)_ 胺基）乙基；2-(哌畊-1-基）乙基；比畊_2_基）乙基；2_(吼 啶-2-基）乙基；2-(吡啶-3_基）乙基；2-(第三丁氧基羰基胺 基曱基)吼啶-3-基甲基；2-(第三丁氧基羰基胺基曱基)。比 咬-6-基曱基；2-(三氟曱基)_吡啶_6•基曱基；胺基吡啶 -3-基甲基；2-胺基吡啶-5-基曱基；2-氯吡啶-5-基甲基； 2- 氰基咐^疋-5-基甲基；2-經基-3-胺基-丙-1-基；2-經基乙 基，2-曱氧基乙小基；2-甲氧基π比咬_3_基曱基；2-曱氧 基吡啶-5-基曱基；2-甲基吡啶-3-基甲基；2-甲基吡啶-5-基甲基；2_甲基吡啶_6_基曱基；3_(2_胺基乙基)環己基） 甲基；3-(4-曱基哌畊-1-基）丙基；3_(胺基)_3_(甲基胺基 幾基）丙-1-基；3_(胺基幾基）丙基；3-(胺基甲基）苯甲基； 3- (胺基甲基)吼啶-2-基曱基；3-(甲氧基羰基）丙基；3_(曱 基胺基羰基）丙基；3-(三氟甲基)-u比啶-2-基曱基；3,4-二 氟苯曱基；3-胺基曱基吡啶-4-基曱基；3-胺基丙基；3_ 胺曱酸基環戊基；3-羧基丙基；3-羥基丙基；3-曱氧基丙 基；4-(胺基曱基)_吡啶_2_基甲基；4-(N，N-二曱基胺基） 吼咬-3-基曱基；4-(第三丁氧基羰基胺基)-嗎啉基曱基； 4- 胺基丁基；4-胺基曱基π比啶_3_基曱基；4-氰基苯甲基； 4-氟苯曱基；4-曱基胺基π比啶_3_基甲基；4-曱基苯曱基； 4-嗎啉基吼啶-3-基曱基；4-哌畊基吼啶-3-基曱基；5-((雙 (一甲基胺基）甲基胺基）曱基)吼0定-3-基曱基；5-(胺基曱 336 200823188 基)吼啶-2-基甲基；5-(胺基甲基)吼啶-3-基甲基；5-(羥基 曱基)吡啶-3-基曱基；5-(第三丁氧基羰基胺基曱基：吡啶 -2-基甲基；5-(三氟甲基)^比啶-2-基曱基；5-胺基戊基； 5-胺基吼啶-2-基曱基；6-((雙（二曱基胺基)伸曱基胺基) 5 甲基户比啶_2_基）甲基；6-(4-乙醯基哌畊-1-基户比啶-3-基 曱基），6-(胺基曱基)σ比咬-2-基曱基，6-胺基己基，胺基 羰基甲基；苯曱基；環丙基甲基；二曱基胺基羰基曱基； 異丙基；異畤唑-5-基曱基；曱氧基羰基曱基；曱基；曱 基胺基羰基甲基；噚唑-2-基甲基；哌啶-4-基曱基；丙-2- 1〇 烯-1-基；吡畊-2-基曱基；吡啶-2-基曱基；吡啶-2-基甲 基氧化物；吡啶-3-基甲基；吡啶-3-基曱基-Ν-氧化物； 吡啶-4-基曱基；噻吩-2-基曱基；及噻吩-3-基曱基。 46. 至少一種如申請專利範圍第28至45項中任一項之化學 品，其中Ζ3係選自-(CH2)rR2G，其中r係選自1、2及3， 15 且R2G係選自視需要經取代之芳基及視需要經取代之雜 芳基。 47. 至少一種如申請專利範圍第46項之化學品，其中Z3係 選自2-(3-甲基苯基）乙基、2-(1Η-咪唑-4-基）乙基、2-(1-曱基-1H-咪唑-4-基）乙基、2-(2,3-二氟苯基）乙基、2-(2,5- 2〇 二氣苯基）乙基、2-(2,6-二氣苯基）乙基、2-(2-氯苯基）乙 基、2-(2-氰基苯基）乙基、2-(2-氟苯基）乙基、2-(2-羥基 苯基）乙基、2-(2-曱氧基苯基）乙基、2-(2-曱基苯基）乙 基、2-(3-(三氟曱基)苯基）乙基、2-(3,4-二氟苯基）乙基、 2-(3,5-二氟苯基）乙基、2-(3、5-二曱基-lH-u比唑-1-基）乙 337 200823188 =2-(3、5_—甲基_m_吡唑_4_基）乙基、印-胺甲醯基 笨基基、2_(3脅基苯基）乙基、2-(3_氰基苯基）乙基、 (氣苯基）2物基)_乙基、2_(3_氣苯基）乙基、2_(3_氣 口比=2-基）乙基、2_(3_甲氧基幾基苯基）乙基、2分甲氧 基苯基）乙基、2_(3_甲基苯基）乙基、2_(4_胺基苯基）乙 基、2_(4'氯苯基）乙基、2-(4-氟苯基）乙基、2普經基苯 基)乙基、2-(苯并⑷以，3]二氧環戊烯-5-基）乙基、2十夫喃 2^基）乙基、2-(經基)_2_(苯基）乙基、2_(苯基）乙基、2十比 疋^基）乙基、2十比唆基）乙基、2十塞吩士基）乙基、 ^苯基丙基、3-(ιΗ』米唾]-基)丙小基、3_苯基丙基、 本甲基H2-基Ψ基、吼咬！基曱基及0塞吩冬基甲 15 48·至/種如申請專利範圍第47項之化學品，其中z3係 選自^氟苯乙基、3,5_二氟苯乙基及2十比H基）乙基。、 49·至少一種如申請專利範圍第28至48項中任一項之化學 口口 ’其中R1係選自氫及視需要經取代之低碳烧基。 50 ·至少一種如申請專利範圍第奶項之化學品，其中“ 選自氫及低碳烷基。 〃 、Wherein R 1 and R 4 are independently selected from the group consisting of hydrogen, optionally substituted fluorenyl, optionally substituted alkyl, cyano, halo, azide, optionally substituted amine, optionally Substituted alkoxycarbonyl, optionally substituted aminocarbonyl, sulfonyl, sulfinyl and sulfanyl; Z1 is optionally substituted heteroaryl; Z2 is selected from hydrogen, optionally substituted a mercapto group, a carboxyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted fluorenyl group, an optionally substituted alkenyl group, an optionally substituted alkyl group, and an optionally substituted aminocarbonyl group; z is selected from the group consisting of a substituted aryl group and optionally a heteroarylalkyl group; and R3 is selected from the group consisting of hydrogen and optionally substituted alkyl. 29 2S • Main eve of a chemical as claimed in item 28 of the patent, in which 21 lines k from 1H-xanth-3-yl; 1Η-σ ratio to 4-yl; 1H_three-salt-5-based 1 methyl_1H_pyrazole_4_yl; 1-mercapto-m-pyrazol-5-yl; 2-aminomethyl is °Cent-5-yl; 2-cyanothiophene; 2 - mercaptothiophen-3-yl; arylthiophen-4-yl; 2H-pyrrole-1(5H)-yl; 2-hydroxymethyl porphin-3-yl, 2-hydroxydecylthiophen-4-yl ; 2-hydroxymethylthiophene-5-yl; 3-amine 330 200823188 benzyl σ thiophene-2-yl, 3-carbyl-1 -mercapto-1 Η-π ratio 0 -4- group, 3 -oxyindole-4-phen-4-yl, 3-decanoic acid σ-phen-2-yl, 3-ylmethyl oxenophen-2-yl, 4-methylthiophen-2-yl; 4- Nonylthiophene-3-yl; 5-(1-hydroxyethyl-1-yl)-17-phenanthryl, 5-ethyl-branched-yl-O-phenan-5-yl, 5-carbonyl-1Η-ϋpyr 4-yl, 5- 5-hydroxy-1-indolyl-1Η-ϋ ratio 11 -4-yl, 5-nitros-7-thiophen-2-yl, 5-nonanoylthiophen-2-yl; 5-hydroxymercaptothiophen-2-yl; isoxazol-4-yl; pyridin-2-yl, 12-pyridin-3-yl, indomethacin-4-yl, oxime 11 Base, oxime-2-yl, and oxime-3-yl. 30. At least one chemical as claimed in claim 29, wherein Ζ1 is ίο from 1 Ηpyrazol-3-yl; 1 Η-pyrazol-4-yl; 1 Η-triazol-5-yl; Mercapto-1Η-pyrazol-4-yl; 1·fluorenyl-1Η-pyrazol-5-yl; 2-(hydroxyindenyl)thiophen-3-yl; 2,2'-dipyridine; 2,3 '-Dipyridine; 2,4'-dipyridine; 2-cyanothiophen-3-yl; 2-mercaptothiophen-3-yl; 3-(hydroxyindenyl)thiophen-2-yl; 3-cyano曱-1-fluorenyl-1 Η-pyrazol-4-yl; 3-mercaptothiophene-2-15yl, 4-oxathiophen-3-yl, 4-methyl-17-phen-2-yl , 4-mercapto σ-cetin-3-yl; 5-(1-hydroxyethyl)thiophen-2-yl; 5-(aminoindenyl)thiophen-2-yl; 5-(hydroxyindenyl)thiophene- 2-yl; 5-(hydroxyindenyl)thiophen-3-yl; 5-ethenylthiophen-2-yl; 5-cyano-1indole-pyrazol-4-yl; 5-cyano-1-pyrene -l-pyrazol-4-yl; 5-cyanothiophen-2-yl; 5-nonylthiophen-2-yl; 5-methyl 20-decylthiophen-3-yl; 3-(amino hydrazine Thiophen-2-yl; isoxazol-4-yl; σ泰 U sits _2_ base. Tertiary-2-yl, and σ-cetin-3-yl. 31. A chemical according to any one of claims 28 to 30, wherein the oxime 2 is selected from the group consisting of a carboxyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted thiol group, and optionally substituted Alkenyl and alkyl substituted by 331 200823188 as needed. 32. At least one chemical according to claim 31, wherein Z2 is selected from the group consisting of a carboxyl group, an optionally substituted piperidinylcarbonyl group, an optionally substituted pyridylcarbonyl group, and optionally a substituted lower alkyl group. 5 generations of lower alkenyl and lower alkoxycarbonyl groups are taken as needed. 33. At least one chemical according to claim 32, wherein Z2 is selected from the group consisting of 2-(methylamino)-2-milylethyl, 2-amino-2-lactylethyl, 3-amine 3-yloxypropyl, (2-(N-ethylidinoaminoindolyl)piperidin-1-yl)carbonyl, (2-aminomethyl-tung-l-yl)-carbyl, 1-light-2-amino-ethyl, ίο 2-((fluorenylsulfonyl)methyl)piperidin-1-ylcarbonyl; 2-(methylaminocarbonyl)vinyl; 2- (pyridin-3-ylindenyl)-2H-triazol-5-yl;amino fluorenyl; carboxy; decyloxycarbonyl; acridine-2-ylcarbonyl; pyridin-3-ylcarbonyl; 17 1-4 base aid. 34. A chemical according to any one of claims 28 to 33, wherein R3 is selected from the group consisting of hydrogen and optionally substituted lower alkyl. 35. At least one chemical of claim 34, wherein R3 is selected from the group consisting of hydrazine and lower alkyl. 36. At least one chemical as claimed in claim 35, wherein R3 is selected from the group consisting of hydrogen and methyl. 20 3 7. At least one chemical as claimed in claim 36, wherein R3 is hydrogen. 38. At least one chemical according to claim 28, wherein Z2 is -C(0)NR2R5, wherein R2 is selected from an alkyl group optionally substituted and a cycloalkyl group optionally substituted; It is selected from hydrogen and optionally substituted 332 200823188. The chemical according to any one of claims 28 to 38, wherein R4 is selected from the group consisting of hydrogen, cyano, halo, azide, optionally substituted amino group and optionally Replace the dazzle. 40. At least one chemical as claimed in claim 39, wherein R4 is selected from the group consisting of hydrogen, chaotic, chloro, bromo, fluoro, azido, optionally substituted alkylaminocarbonyl and optionally substituted Methyl group. 41. At least one chemical of claim 4, wherein R4 is 10 15 selected from the group consisting of hydrogen, cyano, chloro, bromo, azide, pyridine-3-aminomethylcarbonyl, amine Methyl and hydroxymethyl. 42. At least one chemical as claimed in item 41 of the patent application, wherein R4 is 43. at least one of the chemicals of any of items 38 to 42 of the range of interest, wherein R2 is selected from the group as needed. The methyl group, the propyl group which is replaced by the ethyl group as needed, and the Dingmei which is replaced as needed, =! Substituted pentyl group, optionally substituted hexyl group: cyclohexyl group, of which long-term • one, pentyl group and visually substituted two or three by: two take two base, as needed Heteroaryl, if necessary: take, the aromatics need to be substituted cycloalkyl, optionally decyl, carbonyl and, if necessary, by the second burning, need to be substituted by burning oxygen at least For example, the chemical of the 43rd patent scope, in which 333 44. 20 200823188 is derived from methyl and ethyl, the methyl and ethyl groups in # are returned to the base by the following Substituted by the wind, optionally substituted aryl, substituted heteroaryl, optionally substituted heterocycloalkyl, optionally substituted cycloalkyl, optionally substituted aminocarbonyl, optionally Substituted amine group, hydroxyl group, carboxyl group, optionally substituted alkoxycarbonyl group and optionally substituted alkoxy group. 45. At least one chemical as claimed in claim 43 wherein ^ is selected from the group consisting of (1-(2-aminoethyl)_1H-pyrazole each) methyl; s(sulfonylsulfonyl) tourism -3-yl)methyl; (i_acetyl group) thiol; ethyl hydrazide ° bite - 2 yl) fluorenyl; (1H-imidin-2-yl) methyl; 1HH3-yl)methyl; (1_fluorenyl-111) ratio; sitting _3_yl) methyl; (ι_曱基_ιη_π than 5-nyl) fluorenyl; (2-(amino) Carbonyl)ethylamino)carbonylmethyl; (2-(aminomethyl)fluorenyl)methyl; fluorenyl (carboxy)ethylamino)methyl hydrazino; (2-(didecylamino) Ethylamino)carbonylcarbonyl group; (2-(hydroxy)ethylamino)carbonylmethyl; (2-(methylamino)ethylamino)methyl hydrazino; (2-(Ν- 曱 () Tertiary butoxycarbonyl)-amino)ethylamino)methylidene; (2-oxypiperidin-3-yl)indenyl; (3-(dimethylamino)propylamino) Carbonylmethyl; (3-(hydroxy)ethylamino)carbonylindenyl; (3-(t-butoxycarbonylamino)propylamino)carbonylindenyl; (4-(aminomethyl)anthracene Biting base 5-(Amino fluorenylbipyridyl-2-yl)methyl; (6-((1,3-dioxyisoindolin-2-yl)methyl)acridin-2-yl)methyl; (6-(2-aminoethylamino)u) than 2-yl) fluorenyl; (6-(3-aminopropylamino) π than _2-yl) fluorenyl; (6- (amino-based fluorenylpyridyl)methyl; (6-(hydroxyindenyl), pyridyl)methyl; (6-bromoacridin-2-yl)methyl; (methylsulfonamide) Alkylmethyl; 334 200823188 (orridin-2-yl)ethylamino; 1-(2-(t-butoxycarbonylamino)ethyl σ--3-ylindenyl, 1- (2-(Setrabutoxyalkylamino)ethyl plH-utb12 is a 5-methyl group, 1-(amino&gt;carbonyl)-2-(amino)-eth-1-yl , 1-(aminocarbonyl)-3-(amino)-propyl; 1-(aminocarbonyl)-4-(amino)-butan-5; 1-(aminocarbonyl)-4-(benzene Mercaptooxycarbonylamino)-pentyl; 1-(aminoindenyl)-5-(amino)-indenyl, 1-(aminoindenyl)ethyl-1-yl, 1-(rebel --2-(amino)-eth-1-yl, 1-(didecylamino)-(2-yl)-eth-1-yl, 1-(yl)-2-( Amino-mercaptoalkylamino)ethyl-1-yl, 1-(light)-2-(ethoxycarbonyldecylamino) Ethyl-1-yl; 1-(hydroxy)-2-(acridin-1in-2-yldecylamino)ethyl-1-yl, 1-(decyloxygreen)-2-(amino) -B-1 -yl, 1-(methyllacyl-green)-2-(second butyl-based decylamino)-eth-1-yl, 1-(decyloxy)ethyl-1- 1,1-(decylamine-based)-2-(amino)-ethyl*-yl-(2 occ), 1-(decylamino)-yl-yl, 1-amine 2-yl 2-hydroxy-ethyl-1-yl; 1-methoxycarbonyl-2-hydroxy-ethyl-1-yl; 2-(2-amino-15 ethyl lactyl)ethyl, 2-(2- Aminoethyl)-0 to sigma-6-ylmethyl, 2-(2-aminoethylamino)ethyl, 2-(3-phenylphenyl)ethyl, 2-(3-methyl Ethyl-based green)ethyl; 2-(6-(aminoindenyl)acridin-2-yl)ethyl; 2-(ethionylamino)ethyl, 2-(amino)ethyl, 2-(Amino-based)-2-(acetamidoamino)-eth-1-yl, 2-(amino-based)-2-(amino)-eth-1-yl, 2-(amine Ethyl-carbon-based ethyl, 20 2-(aminomethyl-carbidin-5-ylindenyl; 2-(carboxy)-2-(amino)-eth-1-yl; 2-(di) Ethylamino)ethyl; 2-(dimethylaminocarbonyl)-2-(amino)-eth-1-yl; 2-(ethoxycarbonyl)ethyl; 2-(decyloxycarbonyl) -2-(acetonitrile Amino)-ethyl-1-yl; 2-(decyloxycarbonyl)-2-(amino)-eth-1-yl; 2-(decyloxyamino)ethyl, 2-(曱Ethylamino)ethyl, 2-(fluorenylamino 335 200823188)-2-(ethenylamino)-ethyl; 2-(decylaminocarbonyl)_2-(amino)-B- 1-yl; 2-(methylsulfonylamino)ethyl; 2-(decyloxycarbonyl)_2-(amino)-ethylidene; 2_(N_(t-butoxycarbonyl)_N_(methyl) _ amino) ethyl; 2-(pipedino-1-yl)ethyl; specific cultivating _2-yl)ethyl; 2-(acridin-2-yl)ethyl; 2-(pyridine-3-yl Ethyl; 2-(t-butoxycarbonylaminoguanidino) acridine-3-ylmethyl; 2-(t-butoxycarbonylaminoindenyl). Ratio of -6-ylindenyl; 2-(trifluoromethyl)-pyridine-6-ylindenyl; aminopyridin-3-ylmethyl; 2-aminopyridin-5-ylindenyl; Chloropyridin-5-ylmethyl; 2-cyanoindole-5-ylmethyl; 2-yl-3-amino-propan-1-yl; 2-ylethyl, 2-oxo乙乙基基; 2-methoxy π ratio biting _3_ fluorenyl; 2-decyloxypyridin-5-ylindenyl; 2-methylpyridin-3-ylmethyl; 2-methylpyridine -5-ylmethyl; 2-methylpyridyl-6-ylindenyl; 3-(2-aminoethyl)cyclohexyl)methyl; 3-(4-indolylpiperidin-1-yl)propyl ; 3_(amino)_3_(methylamino)propyl-1-yl; 3-(amino)propyl; 3-(aminomethyl)benzyl; 3-(aminomethyl) Acridine-2-ylindenyl; 3-(methoxycarbonyl)propyl; 3-(decylaminocarbonyl)propyl; 3-(trifluoromethyl)-u-pyridin-2-ylindenyl 3,4-difluorophenylindenyl; 3-aminomercaptopyridin-4-ylindenyl; 3-aminopropyl; 3-aminocaproic acid cyclopentyl; 3-carboxypropyl; 3-hydroxyl Propyl; 3-methoxypropyl; 4-(aminoindenyl)-pyridine-2-ylmethyl; 4-(N,N-didecylamino) guan-3-ylindenyl; 4-(t-butoxycarbonylamino group )-morpholinylfluorenyl; 4-aminobutyl; 4-aminoindenyl π-pyridyl_3_ylindenyl; 4-cyanobenzyl; 4-fluorophenylindenyl; 4-fluorenyl Aminopyridinium-3-ylmethyl; 4-mercaptobenzoyl; 4-morpholinylacridin-3-ylindenyl; 4-piperidinyl acridine-3-ylindenyl; 5- ((bis(monomethylamino)methylamino)alkyl) 吼0 -3--3-indenyl; 5-(amino 曱 336 200823188 yl) acridin-2-ylmethyl; 5- ( Aminomethyl)acridin-3-ylmethyl; 5-(hydroxyindenyl)pyridin-3-ylindenyl; 5-(t-butoxycarbonylaminoindenyl:pyridin-2-ylmethyl 5-(trifluoromethyl)^pyridin-2-ylindenyl; 5-aminopentyl; 5-aminoacridin-2-ylindenyl; 6-((bis(didecylamino)曱 曱 胺 ) 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5 5曱 ) ) σ 咬 曱 曱 曱 曱 曱 , , , , , , 曱 曱 曱 曱 曱 曱 曱 曱 曱 曱 曱 曱 -2- 曱 -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- -2- Oxazol-5-ylindenyl; oximeoxycarbonyl fluorenyl; fluorenyl; decylaminocarbonylmethyl; oxazol-2-ylmethyl; piperidin-4-ylindenyl; - 1 nonen-1-yl; pyridin-2-ylindenyl; pyridin-2-ylindenyl; pyridin-2-ylmethyloxide; pyridin-3-ylmethyl; pyridin-3-ylindole a quinone-oxime-oxide; a pyridin-4-ylindenyl group; a thiophen-2-ylindenyl group; and a thiophen-3-ylindenyl group. 46. At least one of the claims 28 to 45 A chemical wherein the oxime 3 is selected from the group consisting of -(CH2)rR2G, wherein the r is selected from 1, 2 and 3, 15 and the R2G is selected from the group consisting of an optionally substituted aryl group and optionally substituted heteroaryl groups. 47. At least one chemical according to claim 46, wherein Z3 is selected from the group consisting of 2-(3-methylphenyl)ethyl, 2-(1Η-imidazol-4-yl)ethyl, 2-( 1-mercapto-1H-imidazol-4-yl)ethyl, 2-(2,3-difluorophenyl)ethyl, 2-(2,5- 2 fluorene diphenyl)ethyl, 2- (2,6-diphenyl)ethyl, 2-(2-chlorophenyl)ethyl, 2-(2-cyanophenyl)ethyl, 2-(2-fluorophenyl)ethyl, 2-(2-hydroxyphenyl)ethyl, 2-(2-decyloxyphenyl)ethyl, 2-(2-mercaptophenyl)ethyl, 2-(3-(trifluoromethyl) Phenyl)ethyl, 2-(3,4-difluorophenyl)ethyl, 2-(3,5-difluorophenyl)ethyl, 2-(3,5-dimercapto-lH-u Bizozol-1-yl)ethyl 337 200823188 = 2-(3,5_-methyl-m-pyrazole-4-yl)ethyl, im-amine-methylmethylidene, 2-(3 phenyl) Ethyl, 2-(3-cyanophenyl)ethyl, (oxyphenyl) 2yl)-ethyl, 2-(3-hydroxyphenyl)ethyl, 2_(3_port ratio=2- Ethyl, 2-(3-methoxyphenyl)ethyl, 2-methoxyphenyl)ethyl, 2-(3-methylphenyl)ethyl, 2-(4-aminobenzene) Ethyl, 2-(4' chlorophenyl)ethyl, 2-(4-fluorobenzene Ethyl, 2-Pyridylphenyl)ethyl, 2-(benzo(4),3]dioxol-5-yl)ethyl, 2,10-hydroxy-2-yl), 2 - (radio)_2_(phenyl)ethyl, 2_(phenyl)ethyl, 20 decyl)ethyl, 20 decyl)ethyl, 20 ketosyl)ethyl, ^Phenylpropyl, 3-(ιΗ"miso]-yl)propanyl, 3-phenylpropyl, benzyl H2-ylindenyl, bite! a sulfhydryl group, a thiophene ethyl group, a 3,5-difluorophenethyl group, and a phthalate, wherein the z3 is selected from the group consisting of fluorophenethyl, 3,5-difluorophenethyl and 20 H group based on ethyl. 49. A chemical mouth of any one of claims 28 to 48 wherein R1 is selected from the group consisting of hydrogen and optionally substituted low carbon alkyl. 50. At least one chemical as claimed in the patent application, wherein "selected from hydrogen and a lower alkyl group. 至少一種如申請專利範圍第 選自氫及甲基。 50項之化學品，其中Ri係 52·至少-種如申請專利範圍第51項之化學品，其中“ 氫。 至少一種如申請專利範圍第 化合物係選自式IV化合物 2項之化學品，其令該式j 338 53. 20 200823188At least one of the patent applications is selected from the group consisting of hydrogen and methyl. a chemical of 50, wherein R is 52. at least one of the chemicals of claim 51, wherein "hydrogen. At least one of the compounds of the patent application range is selected from the group 2 compound of formula IV, Let the formula j 338 53. 20 200823188 式IV 其中 R1及R4係獨立選自氫、視需要經取代之醯基、視 需要經取代之烷基、氰基、鹵基、疊氮基、視需要經取 代之胺基、視需要經取代之烷氧基羰基、視需要經取代 之胺基幾基、續醯基、亞確醯基及硫烧基；Z1係選自視 需要經取代之芳基及視需要經取代之雜芳基；Z2係選自 氫、羧基、視需要經取代之烷氧基羰基、視需要經取代 之醯基、視需要經取代之烯基、視需要經取代之烷基、 視需要經取代之甲脒基及視需要經取代之胺基羰基； Z3為視需要經取代之烷基；及 R3係選自氫及視需要經取代之烷基。 54·至少一種如申請專利範圍第53項之化學品，其中z2係 選自羧基、視需要經取代之烷氧基羰基、視需要經取代 之醯基、視需要經取代之烯基及視需要經取代之烷基。 55·至少一種如申請專利範圍第54項之化學品，其中z2係 選自羧基、視需要經取代之哌啶基羰基、視需要經取代 之吡啶基羰基、視需要經取代之吡啶基曱基羰基、視需 要經取代之低碳烷基、視需要經取代之低碳烯基及低碳 烷氧基羰基。 56·至少一種如申請專利範圍第55項之化學品，其中z2係 339 200823188 選自吡啶-3-基曱基羰基、（2-(N-乙醯基胺基甲基)哌啶-1-基）羰基；（2-胺基曱基哌啶-1-基）羰基1-羥基-2-胺基-乙基；2-((甲基磺醯胺基）曱基)哌啶-1-基羰基；2-(甲基 胺基羰基）乙烯基；2-(吡啶-3-基曱基)-2H-三唑-5-基曱 5 基；胺基甲基；羧基；曱氧基羰基；吼啶-2-基羰基；吼 ϋ定-3-基祿基，及吼11 定-4-基幾基。 57. 至少一種如申請專利範圍第53至56項中任一項之化學 品，其中R3係選自氫及視需要經取代之低碳烷基。 58. 至少一種如申請專利範圍第57項之化學品，其中R3係 10 選自氫及低碳烧基。 59. 至少一種如申請專利範圍第58項之化學品，其中R3係 選自氫及曱基。 ， 60.至少一種如申請專利範圍第59項之化學品，其中R3為 氫。 15 61.至少一種如申請專利範圍第53項之化學品，其中Ζ2為 -C(0)NR2R5,其中R2係選自視需要經取代之烷基及視需 要經取代之環烷基；而R5係選自氫及視需要經取代之烷 '基。 62. 至少一種如申請專利範圍第53至61項中任一項之化學 2〇 品，其中R4係選自氫、氰基、鹵基、疊氮基、視需要經 取代之胺基羰基及視需要經取代之烷基。 63. 至少一種如申請專利範圍第62項之化學品，其中R4係 選自氫、氰基、氯、溴、氟、疊氮基、視需要經取代之 烷基胺基羰基及視需要經取代之甲基。 340 200823188 64.至少一種如申請專利範圍第63項之化學品，其中R4係 -選自氫、氰基、氯、溴、疊氮基、吼啶_3_基甲基胺基羰 基、胺基甲基及羥基甲基。 65·至少一種如申請專利範圍第64項之化學品，其中R4為 5 氫。 66·至少一種如申請專利範圍第61至65項中任一項之化學 品，其中R5係選自氫及低碳烷基。 67·至少一種如申請專利範圍第66項之化學品，其中R5係 選自氫及甲基。 ίο 68·至少一種如申請專利範圍第67項之化學品，其中R5為 氫。 69·至少一種如申請專利範圍第61至68項中任一項之化學 * 品，其中R2係選自視需要經取代之曱基、視需要經取代 之乙基、視需要經取代之丙基、視需要經取代之丁基、 15 視需要經取代之戊基、視需要經取代之己基、視需要經 取代之環丙基、視需要經取代之環戊基及視需要經取代 之環己基，其中各視需要經取代之基團係視需要經一、 二或三個由下列選出之基團取代··視需要經取代之芳 基、視需要經取代之雜芳基、視需要經取代之雜環烷基、 20 視需要經取代之環烧基、視需要經取代之胺基羰基、視 需要經取代之胺基、羥基、羧基、視需要經取代之烷氧 基羰基及視需要經取代之烧氧基。 70·至少一種如申請專利範圍第69項之化學品，其中R2係 選自曱基及乙基，其中該曱基及乙基基團係視需要經一 341 200823188 ^個由下列選出之基團取代：視需要經取代之芳基、 ^要經取代之雜芳基、視需要經取代之雜環烧基、視 ^要經取代之環烷基、視需要經取代之胺基羰基、視需 要經取代之胺基、綠、縣、視需要經取代之烧氧基 71 10 15 20 竣基及視需要經取代之烷氧基。 至少種如申請專利範圍第70項之化學品，其中r2係 選自（1-(2-胺基乙基)_1H_吡唑_3_基）甲基；（丨_(甲基磺醯 基）旅啶-3-基）甲基；（ι_乙醯基旅啶_3_基）甲基；（〗_乙醯 基吼咯咬-2-基）曱基；（m_咪唑_2_基）甲基；（m-吡唑_3_ 基）甲基；（1_甲基-1H-吡唑l基）甲基；（1-甲基-1H-吡唑 -基）甲基；（2-(胺基羰基）乙基胺基)羰基甲基；（2兴胺 基甲基)σ比啶-3_基）甲基；（2_(羧基）乙基胺基)幾基甲基； (2-(二甲基胺基）乙基胺基)羰基甲基；(2-(羥基）乙基胺基） 幾基甲基；（2-(曱基胺基）乙基胺基)羰基曱基；（^(队甲 基-Ν-(第三丁氧基羰基)_胺基）乙基胺基）羰基曱基；（1 氣基哌啶-3-基）甲基；（3-(二甲基胺基）丙基胺基)羰基甲 基；（3-(羥基）乙基胺基)羰基曱基；（3-(第三丁氧基羰基 胺基）丙基胺基）羰基甲基；（4-(胺基甲基）吼啶-2-基）甲 基；（5-(胺基甲基)π比啶_2_基）曱基；（6-((1，3-二氧基異吲 木琳-2-基）甲基)υ比咬-2-基）甲基，（6-(2-胺基乙基胺基比 啶-2-基）甲基；（6-(3-胺基丙基胺基）吼啶-2-基）甲基； (&amp;(胺基甲基)吼啶士基）曱基；（6-(羥基·曱基)吼啶-2-基） 甲基；（6-溴吼啶-2-基）曱基；（甲基磺醯胺基)幾基甲基； 0比啶-2-基）乙基胺基；1_(2_(第三丁氧基羰基胺基）乙 342 200823188 基)_1Η-吡唑_3-基曱基；1-(2-(第三丁氧基羰基胺基）乙 基)-旧-吼嗤-5-基甲基；1_(胺基羰基)_2_(胺基卜乙小基； 1-(胺基羰基)-3-(胺基)-丙基；u(胺基羰基)_4_(胺基)_丁 基，1-(胺基羰基)-4-(苯曱基氧基羰基胺基)_戊基；丨_(胺 基羰基)-5_(胺基)_戊基；1_(胺基羰基）乙-1-基，· 1_(羧 基)_2-(胺基)-乙小基；丨_(二甲基胺基羰基)_2_(胺基乙 -1-基；Η皋基)-2-(胺基羰基曱基胺基）乙小基；丨_(羥 基)_2-(乙氧基羰基甲基胺基）乙-1-基；1-(羥基)-2-(吡啶 -2-基甲基胺基）乙_1_基；1_(甲氧基羰基)_2_(胺基)_乙-卜 基，1-(曱氧基羰基)-2-(第三丁氧基羰基胺基)_乙基； Η甲氧基羰基）乙_1_基；1_(甲基胺基羰基)_2_(胺基)_乙 基(2 〇CC) ; 1_(曱基胺基羰基）乙-1-基；1-胺基羰基_2_ 羥，-乙-1-基；；U甲氧基羰基_2_羥基_乙4_基；2_(2_胺基 乙氧基）乙基；2-(2-胺基乙基；)_吡啶_6_基甲基；2_(2_胺基 =基胺基）乙基；2·(3_氟苯基）乙基；2_(3_甲氧基幾基）乙 =，2-(6-(胺基甲基)。比咬_2_基）乙基；2_(乙酸基胺基）乙 :·’ 2-(胺基）乙基’· 2_(胺基幾基峰（乙醯基胺基)_乙小 土，2-(胺基·)_2_(胺基)_乙小基；h(胺基幾基)乙基； 胺基曱基)喊_5_基甲基；2_(__2_(胺基)心卜基； _(-曱基胺基）乙基；2仁甲基胺基幾基)_2_(胺基)_乙小 L，2~(乙氧基幾基）乙基；2-(甲氧基幾基)-2-(乙酿基胺 乙1基’ 2_(甲氧基羰基)_2_(胺基)_乙小基；2_(甲氧 =炭基胺乙基；2_(f基胺基）乙基；2_(甲基胺基幾 土 乙酿基胺基)_乙小基；2_(曱基胺基幾基)-2-(胺 343 200823188 基）-乙-1-基；2-(甲基磺醯胺基）乙基；(曱氧基羰 基)-2-(胺基)_乙_1_基；2-(N-(第三丁氧基羰基)_N_(甲基)_ 胺基）乙基；2-(哌畊-1-基）乙基；2十比畊-2-基）乙基；2-(吼 啶-2-基）乙基，2-(吡啶-3-基）乙基；2-(第三丁氧基羰基胺 基甲基户比淀各基曱基；2-(第三丁氧基羰基胺基曱基户比 咬-6-基曱基，2-(二氟曱基)定_6_基曱基；2-胺基π比π定 -3-基f基；2-胺基吡啶-5-基甲基；2-氯吡啶-5_基曱基； 2- 氰基峨啶-5-基甲基；2-羥基-3-胺基-丙-1-基；2-羥基乙 基；2-甲氧基乙_1_基；2-曱氧基σ比咬—3-基甲基；2-曱氧 基吡啶-5-基曱基；2-甲基吡啶_3_基甲基；2-甲基吡啶-5-基甲基；2_甲基吼啶_6_基甲基；胺基乙基)環己基） 甲基；3-(4-曱基哌畊-1-基）丙基；3_(胺基)-3_(甲基胺基 幾基)丙-1-基；3-(胺基幾基）丙基；3_(胺基曱基)苯曱基； 3- (胺基曱基)吼啶-2-基曱基；3-(曱氧基羰基）丙基；3_(甲 基胺基羰基）丙基；3-(三氟甲基)比啶_2_基甲基；3,4-二 氟苯曱基；3-胺基曱基吼啶-4-基甲基；3-胺基丙基；3-胺甲醯基環戊基；3-羧基丙基；3-羥基丙基；3-曱氧基丙 基；4_(胺基曱基)_吡啶_2_基甲基；4_(Ν，Ν_二甲基胺基） 吼咬-3-基曱基；4-(第三丁氧基羰基胺基)_嗎啉基曱基； 4- 胺基丁基；4-胺基曱基π比啶_3_基曱基；4_氰基苯曱基； 4_氟苯甲基；4-曱基胺基π比咬_3-基曱基；4-曱基苯曱基； 4-嗎啉基吡啶_3_基曱基；4-哌畊基吡啶_3_基曱基；5_((雙 (二曱基胺基）曱基胺基）甲基)吼啶-3_基甲基；5_(胺基甲 基户比&quot;定_2·基曱基；5_(胺基曱基)吼啶冬基曱基；5-(羥基 344 200823188 甲基)吼啶-3-基甲基；5-(第三丁氧基羰基胺基甲基)-吼啶 -2-基甲基，5-(二氣曱基)-0比σ定-2-基曱基；5_胺基戍基； 5-胺基^比ϋ定-2-基曱基，6-((雙（二甲基胺基)伸曱基胺基) 曱基）吼啶-2-基）甲基；6-(4-乙醯基哌畊-1-基）吼啶-3-基 5 甲基）；6-(胺基曱基)吼啶-2-基）甲基；6-胺基己基；胺基 羰基曱基；苯甲基；環丙基曱基；二曱基胺基羰基甲基； 異丙基；異噚唑-5-基曱基；曱氧基羰基甲基；曱基；甲 基胺基綠基甲基，^亏11 坐-2-基曱基，旅咬-4-基甲基，丙-2_ 烯-1-基；吡畊-2-基甲基；吡啶-2-基曱基；吼啶-2-基曱 ίο 基-N-氧化物；吡啶-3-基曱基；吡啶-3-基曱基-N-氧化物； 吡啶-4-基甲基；噻吩-2-基曱基；及噻吩-3-基曱基。 - 72.至少一種如申請專利範圍第71項之化學品，其中R2為 吡啶-3-基曱基。 73. 至少一種如申請專利範圍第53至72項中任一項之化學 15 品，其中Z3係選自-(CH2)rR2G，其中r係選自1、2及3， 且R2()係選自視需要經取代之雜環烧基及視需要經取代 之環烷基。 74. 至少一種如申請專利範圍第73項之化學品，其中Z3係 選自（四氫呋喃2-基甲基、1-羥基環己基曱基、2-(1，3-二 20 氧戊環-2-基）乙基、2-(1-曱基哌啶-4-基）乙基、2-(2-氧基 口米嗤^定-1-基）乙基、2-(2-氧基ϋ底ϋ定-1-基）乙基、2-(2-乳基 吡咯啶-1-基）乙基、2-環己-1-烯基乙基、2-環己基乙基及 2-嗎啉基乙基。 至少一種如申請專利範圍第53至74項中任一項之化學 345 75. 200823188 二’厂？係選自視需要經一或二個由下列選出之基團 、.代之方基、:.氰基、鹵基、瘦基、甲酿基、視需要經取 ί之ϊί:視ΐ要經取代之烯基、視需要經取代之烷氧 '視而要·取代之燒氧基幾基、視需要經取代 -监土、視需要經取代之胺基㈣、視需要經取代之胺 ς視需要經取代之雜環烧基、視需要經取代之雜芳 =視需要經取代之㈣基和視需要經取代之績酿基， Μ及 10 20 或二個由下列選出之基團取代之雜芳基：氛 =j、錄、Μ基、視需要經取代之烧基、視需 之烯基、視需要經取代之垸氧基、躲、視需 鰣：烷氧基羰基、視需要經取代之醯基、視需要 之胺基叛基、視需要經取代之雜環烷基、視需要 彳、之竑芳基、視需要經取代之甲肺基和視需要經取 代之磺醯基。 • 、種如申請專利範圍第乃項之化學品，其中ζι係 ，自視需要經-或二個由下列選出之基團取代之芳基： 氰基i基、羥基、甲醯基、視需要經取代之低碳烷基、 ^需要經取狀低麵基、視需要經取狀低碳烧氧 土羧基、視需要經取代之低碳烷氧基羰基、視需要經 取代之低碳酿基、視需要經取代之胺絲基、視需要經 取代之雜壞絲、視需要經取代之雜絲及視需要經烧 基取代之胺基，以及 視而要經一或二個由下列選出之基團取代之雜芳基：氰 346 200823188 基、鹵基、羥基、曱醯基、視需要經取代之低碳烷基、 視I要經取代之低碳烯基、視需要經取代_之低碳烷氧 基、羧基、視需要經取代之低碳烷氧基羰基、視需要經 取代之低碳醯基、視需要經取代之胺基羰基、視需要經 5 取代之雜環烷基、視需要經取代之雜芳基及視需要經烷 基取代之胺基。 77. 至少一種如申請專利範圍第76項之化學品，其中Z1係 選自苯基、1H-口比唑-3-基；1H-口比唑-4-基；1H-三唑-5-基；1-曱基-1H-吡唑-4_基；1_曱基-1H-吡唑-5-基；2_胺 ίο 基甲基噻吩-5-基；2-氰基噻吩-3-基；2-曱醯基噻吩-3- 基；2-甲醯基噻吩-4-基；2H-吡咯·1(5Η)_基；2-羥基甲基 ϋ塞吩-3-基，2-經基曱基ϋ泰吩-4-基，2-經基曱基ϋ塞吩-5-基；3-胺基曱基噻吩-2基；3-氰基-1-甲基-1Η-吡唑-4-基； 3-氣基11塞吩-4-基，3 -曱酿基ϋ塞吩-2-基，3 -經基甲基嗟吩 15 -2-基，4-曱基ϋ塞吩-2-基，4-甲基σ塞吩-3·基，5-(1 - ¾基乙 -1-基)-噻吩-2_基；5-乙醯基噻吩-5-基；5-氰基-1H-吡唑 -4-基；5-氰基-1-曱基-1H-吡唑-4-基；5-氰基噻吩-2-基； 5-曱醯基噻吩-2-基；5-羥基曱基噻吩-2-基；異畤唑i-4-基，ϋ比°定-2 -基，^比ϋ定-3 -基，0比^定-4 -基，0奏σ坐-2 -基，口秦 20 口分^口奏口分〇 78. 至少一種如申請專利範圍第53至77項中任一項之化學 品，其中R1係選自氫及視需要經取代之低碳烷基。 79. 至少一種如申請專利範圍第78項之化學品，其中R1係 選自氬及曱基。 347 200823188 8〇.至少-種如申請專利範圍帛79項之化學品，1中 &amp;0 八· 81.至少-種如申請專利範圍第}項之化學品，其中該式t 化合物係選自式V化合物Wherein R 1 and R 4 are independently selected from the group consisting of hydrogen, optionally substituted fluorenyl, optionally substituted alkyl, cyano, halo, azide, optionally substituted amine, optionally substituted An alkoxycarbonyl group, optionally substituted amino group, a fluorenyl group, an anthracene group and a thiol group; Z1 is selected from an optionally substituted aryl group and optionally substituted heteroaryl group; Z2 is selected from the group consisting of hydrogen, carboxyl, optionally substituted alkoxycarbonyl, optionally substituted indenyl, optionally substituted alkenyl, optionally substituted alkyl, optionally substituted formazan. And optionally substituted aminocarbonyl; Z3 is an optionally substituted alkyl; and R3 is selected from hydrogen and optionally substituted alkyl. 54. At least one chemical according to claim 53 wherein z2 is selected from the group consisting of a carboxyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted thiol group, an optionally substituted alkenyl group, and optionally Substituted alkyl group. 55. At least one chemical according to claim 54 wherein z2 is selected from the group consisting of a carboxy group, optionally substituted piperidinylcarbonyl, optionally substituted pyridylcarbonyl, optionally substituted pyridyl fluorenyl A carbonyl group, a substituted lower alkyl group, optionally a substituted lower alkenyl group and a lower alkoxycarbonyl group. 56. At least one chemical as claimed in claim 55, wherein z2 is 339 200823188 selected from pyridin-3-ylindenylcarbonyl, (2-(N-ethylidinomethyl)methylpiperidine-1- (2-aminomercaptopiperidin-1-yl)carbonyl 1-hydroxy-2-amino-ethyl; 2-((methylsulfonylamino)indolylpiperidin-1- 2-carbonyl group; 2-(methylaminocarbonyl)vinyl; 2-(pyridin-3-ylindenyl)-2H-triazol-5-ylindole-5;aminomethyl;carboxy; oxiranylcarbonyl Acridine-2-ylcarbonyl; hydrazin-3-ylsulfanyl, and hydrazinyl-4-yl. 57. A chemical according to any one of claims 53 to 56 wherein R3 is selected from the group consisting of hydrogen and optionally substituted lower alkyl. 58. At least one chemical as claimed in claim 57, wherein the R3 system 10 is selected from the group consisting of hydrogen and a low carbon alkyl group. 59. At least one chemical as claimed in claim 58 wherein R3 is selected from the group consisting of hydrogen and sulfhydryl. 60. At least one chemical as claimed in claim 59, wherein R3 is hydrogen. 15 61. At least one chemical according to claim 53 wherein Ζ2 is -C(0)NR2R5, wherein R2 is selected from an alkyl group optionally substituted and a cycloalkyl group optionally substituted; It is selected from the group consisting of hydrogen and optionally substituted alkane. 62. A chemical 2 product according to any one of claims 53 to 61, wherein R4 is selected from the group consisting of hydrogen, cyano, halo, azido, optionally substituted aminocarbonyl and A substituted alkyl group is required. 63. At least one chemical as claimed in claim 62, wherein R4 is selected from the group consisting of hydrogen, cyano, chloro, bromo, fluoro, azido, optionally substituted alkylaminocarbonyl and optionally substituted Methyl group. 340 200823188 64. At least one chemical according to claim 63, wherein R4 is selected from the group consisting of hydrogen, cyano, chloro, bromo, azide, acridine-3-ylaminocarbonyl, amine Methyl and hydroxymethyl. 65. At least one chemical as claimed in claim 64, wherein R4 is 5 hydrogen. 66. A chemical according to any one of claims 61 to 65 wherein R5 is selected from the group consisting of hydrogen and lower alkyl. 67. At least one chemical as claimed in claim 66, wherein R5 is selected from the group consisting of hydrogen and methyl. Ίο 68· At least one chemical as claimed in claim 67, wherein R5 is hydrogen. 69. A chemical product according to any one of claims 61 to 68, wherein R2 is selected from the group consisting of an optionally substituted thiol group, an optionally substituted ethyl group, optionally substituted propyl group. , optionally substituted butyl, 15 optionally substituted pentyl, optionally substituted hexyl, optionally substituted cyclopropyl, optionally substituted cyclopentyl and optionally substituted cyclohexyl Wherein each of the groups which are optionally substituted may be substituted by one, two or three groups selected by the following groups: optionally substituted aryl groups, optionally substituted heteroaryl groups, optionally substituted Heterocycloalkyl, 20 optionally substituted cycloalkyl, optionally substituted aminocarbonyl, optionally substituted amine, hydroxy, carboxy, optionally substituted alkoxycarbonyl and optionally Replace the alkoxy group. 70. At least one chemical according to claim 69, wherein R2 is selected from the group consisting of a fluorenyl group and an ethyl group, wherein the thiol group and the ethyl group are optionally selected from the group consisting of 341 200823188 Substitution: an optionally substituted aryl group, a heteroaryl group to be substituted, an optionally substituted heterocycloalkyl group, a cycloalkyl group to be substituted, an optionally substituted aminocarbonyl group, optionally Substituted amine group, green, county, or alkoxy group 71 10 15 20 decyl and optionally substituted alkoxy group as desired. At least the chemical of claim 70, wherein r2 is selected from (1-(2-aminoethyl)_1H-pyrazole-3-yl)methyl; (丨_(methylsulfonyl)旅 -3- -3-yl)methyl; (ι _ 醯 旅 _ _ _ _ _ _) methyl; (〗 〖 醯 醯 吼 吼 -2- 基 基 基 ; ; ; ; ;; (m_imidazole _2 (m)pyridylmethyl; (m-pyrazole-3-yl)methyl; (1-methyl-1H-pyrazoleyl)methyl; (1-methyl-1H-pyrazole-yl)methyl; (2-(Aminocarbonyl)ethylamino)carbonylmethyl; (2-aminomethyl) σ-pyridin-3-yl)methyl; (2-(carboxy)ethylamino)methylmethyl (2-(dimethylamino)ethylamino)carbonylmethyl; (2-(hydroxy)ethylamino)methylamino; (2-(decylamino)ethylamino) Carbonyl fluorenyl; (^(team methyl-Ν-(t-butoxycarbonyl)-amino)ethylamino)carbonylcarbonyl; (1 gas-piperidin-3-yl)methyl; (3 -(dimethylamino)propylamino)carbonylmethyl; (3-(hydroxy)ethylamino)carbonylindenyl; (3-(t-butoxycarbonylamino)propylamino) Carbonylmethyl; (4-(aminomethyl) acridine-2-yl)methyl; 5-(Aminomethyl)π-pyridinyl-2-yl)indenyl; (6-((1,3-diisoisoindolyl-2-yl)methyl)pyrene) Methyl, (6-(2-aminoethylaminobipyridin-2-yl)methyl; (6-(3-aminopropylamino)acridin-2-yl)methyl; And (aminomethyl) acridinyl) fluorenyl; (6-(hydroxyindolyl)acridin-2-yl)methyl; (6-bromoacridin-2-yl)indenyl; Methylsulfonylamino)methylidene; 0-pyridin-2-yl)ethylamino; 1-(2-(t-butoxycarbonylamino)ethyl 342 200823188))Η-pyrazole_3- Base group; 1-(2-(t-butoxycarbonylamino)ethyl)-old-indol-5-ylmethyl; 1-(aminocarbonyl)_2_(aminobiphenyl); -(aminocarbonyl)-3-(amino)-propyl; u(aminocarbonyl)_4-(amino)-butyl, 1-(aminocarbonyl)-4-(phenylhydrazyloxycarbonylamine ))-pentyl; 丨-(aminocarbonyl)-5-(amino)-pentyl; 1-(aminocarbonyl)eth-1-yl,·1-(carboxy)_2-(amino)-ethyl small ;丨_(dimethylaminocarbonyl)_2_(aminoethyl-1-yl;fluorenyl)-2-(aminocarbonylcarbonylamino)ethyl small group; 丨_(hydroxy)_2-(B Oxycarbonylmethylamino Ethyl-1-yl; 1-(hydroxy)-2-(pyridin-2-ylmethylamino)ethyl-1-yl; 1-(methoxycarbonyl)_2-(amino)-ethyl-b-yl, 1-(decyloxycarbonyl)-2-(t-butoxycarbonylamino)-ethyl; fluorenylmethoxycarbonyl)ethyl-1-yl; 1-(methylaminocarbonyl)_2-(amino) _Ethyl (2 〇CC); 1_(decylaminocarbonyl)ethyl-1-yl; 1-aminocarbonyl-2-hydroxyl, -ethyl-1-yl; Umethoxycarbonyl-2-hydroxyl Ethyl 4-yl; 2-(2-aminoethoxy)ethyl; 2-(2-aminoethyl;)-pyridine-6-ylmethyl; 2-(2-amino=ylamino) 2;(3-fluorophenyl)ethyl; 2-(3-methoxymethyl)ethyl=,2-(6-(aminomethyl). Specific bite 2_(yl)ethyl; 2_(acetoxyamino)ethyl:·' 2-(amino)ethyl'· 2_(aminol base peak (ethylideneamino)-B small earth, 2-(Amino)-_2-(amino)-ethylidene; h(amino)ethyl; aminoguanidino) _5-ylmethyl; 2_(__2_(amino)pyryl ; _(-decylamino)ethyl; 2, methylaminoamino)_2_(amino)-ethyl L, 2~(ethoxy)ethyl; 2-(methoxy ))-2-(i-bromoamine ethyl 1 yl ' 2 -(methoxycarbonyl) 2 -(amino)-ethyl small group; 2 - (methoxy = carbon amino amine ethyl; 2 - (f-amino) Base; 2_(methylaminocarbendyrylamino)-ethylidene; 2-(decylamino)-2-(amine 343 200823188)-ethyl-1-yl; 2-(A (sulfonylamino)ethyl; (decyloxycarbonyl)-2-(amino)-ethyl-1-yl; 2-(N-(t-butoxycarbonyl)_N_(methyl)-amino Ethyl; 2-(pipedino-1-yl)ethyl; 2 decyl-2-yl)ethyl; 2-(acridin-2-yl)ethyl, 2-(pyridin-3-yl) Ethyl; 2-(t-butoxycarbonylaminomethyl-methyl-pyrylene-based fluorenyl; 2-(t-butoxycarbonylamino fluorenyl phenyl-based -6-yl fluorenyl, 2- (difluorodecyl) _6_yl fluorenyl; 2-amino π ratio π-3-yl-f-yl; 2-aminopyridin-5-ylmethyl; 2-chloropyridin-5-ylindenyl; 2-cyano acridine -5-ylmethyl; 2-hydroxy-3-amino-propan-1-yl; 2-hydroxyethyl; 2-methoxyethyl-1-yl; 2-decyloxy σ ratio bite 3- Methyl; 2-methoxypyridine-5-ylindenyl; 2-methylpyridine-3-ylmethyl; 2-methylpyridin-5-ylmethyl; 2-methylacridine_6_ Methyl;aminoethyl)cyclohexyl)methyl; 3-(4-indolylpiperidin-1-yl)propyl; 3-(amino)-3_(methylamino)propyl-1 -yl; 3-(aminophenyl)propyl; 3-(aminoindenyl)phenylhydrazine; 3-(aminoindenyl)acridin-2-ylindenyl; 3-(decyloxycarbonyl) Propyl; 3-(methylaminocarbonyl)propyl; 3-(trifluoromethyl)pyridinyl-2-ylmethyl; 3,4-difluorobenzoinyl; 3-aminoindenyl acridine- 4-ylmethyl; 3-aminopropyl; 3-amineindolylcyclopentyl; 3-carboxypropyl; 3-hydroxypropyl; 3-methoxypropyl; 4-(aminothio) _pyridine-2-ylmethyl; 4_(Ν,Ν_dimethylamino) 吼-3-ylindenyl; 4-(t-butoxycarbonylamino)-morpholinyl fluorenyl; 4 - aminobutyl; 4-amino hydrazine π 比 啶 _ 3 3 ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; 4 4 4 4 4 4 4 4 4 4 4 4 4 4 4 π π π ; ; ; 4-morpholinylpyridine_3_ylindenyl; 4-piperidinylpyridine_3_ylindenyl; 5-((bis(didecylamino)decylamino)methyl)acridine-3_ Methyl group; 5_(aminomethyl group ratio &quot; _2 · · ; ;; 5 _ (amino fluorenyl) acridine hydrazino; 5- (hydroxy 344 200823188 methyl) acridine-3- Methyl group; 5-(t-butoxycarbonylaminomethyl)-acridin-2-ylmethyl, 5-(dihydroindenyl)-0-pyridin-2-ylindenyl; 5_ Amino fluorenyl; 5-amino group ϋ ϋ -2- -2-yl fluorenyl, 6-((bis(dimethylamino) decylamino) fluorenyl) acridine-2-yl)methyl 6-(4-Ethylpiperidin-1-yl)acridin-3-yl-5methyl); 6-(aminoindenyl)acridin-2-yl)methyl; 6-aminohexyl Aminocarbonylcarbonyl group; benzyl group; cyclopropyl fluorenyl group; dimercaptoaminocarbonylmethyl group; isopropyl group; isoxazol-5-ylindenyl group; oxime oxycarbonylmethyl group; fluorenyl group; Methylaminomethylmethyl, ^11 ketone-2-yl sulfhydryl, brigade-4-ylmethyl, propyl-2-eno-1-yl; pyridin-2-ylmethyl Pyridin-2-ylindenyl; acridine-2-yloxime ί-yl-N-oxide; pyridin-3-ylindenyl; pyridin-3-ylindenyl-N-oxide; pyridin-4-yl Thiophen-2-ylindenyl; and thiophen-3-ylindenyl. - 72. At least one chemical according to claim 71, wherein R2 is pyridin-3-ylindenyl. 73. A chemical product according to any one of claims 53 to 72, wherein Z3 is selected from the group consisting of -(CH2)rR2G, wherein r is selected from 1, 2 and 3, and R2() is selected Self-viewing requires a substituted heterocycloalkyl group and optionally substituted cycloalkyl groups. 74. At least one chemical according to claim 73, wherein Z3 is selected from the group consisting of (tetrahydrofuran 2-ylmethyl, 1-hydroxycyclohexylfluorenyl, 2-(1,3-di20-oxolane-2) -yl)ethyl, 2-(1-mercaptopiperidin-4-yl)ethyl, 2-(2-oxymethylpyrano-l-yl)ethyl, 2-(2-oxyl ϋ ϋ -1- -1-yl) ethyl, 2-(2-lacylpyrrolidin-1-yl)ethyl, 2-cyclohex-1-enylethyl, 2-cyclohexylethyl and 2- Morpholinylethyl. At least one of the chemistry of any one of claims 53 to 74 of the patent application 345 75. 200823188 The second 'factory' is selected from one or two groups selected by the following, as needed. The square base,: cyano group, halogen group, lean base, brewing base, as needed 经 ϊ : : : : : : : : 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基 烯基Alkoxy groups, optionally substituted-supervised, optionally substituted amino groups (IV), optionally substituted amines, disubstituted heterocyclic alkyl groups, optionally substituted heteroaryls as needed Substituted (iv) base and, if necessary, replaced by the base, Μ and 10 20 or two by Substituted heteroaryl group: atmosphere = j, recorded, fluorenyl, optionally substituted alkyl, optionally alkenyl, optionally substituted methoxy, hiding, as needed: alkoxy Alkylcarbonyl, optionally substituted thiol, optionally amino-based thiol, optionally substituted heterocycloalkyl, optionally hydrazine, aryl, optionally substituted alpha-lung and optionally Substituted sulfonyl group. • A chemical such as the scope of the patent application, in which ζι is a aryl group which is replaced by a group selected from the following: or a cyano group, a hydroxy group, A mercapto group, a lower alkyl group which is optionally substituted, a low-carbon alkoxycarbonyl group which is required to be taken in a low-base group, optionally taken in a low-carbon aerobic earth, and optionally substituted, if necessary Substituted low-carbon brewing base, optionally substituted amine silk base, optionally substituted heterochromic silk, optionally substituted filament and optionally substituted alkyl group, and optionally subjected to one or Two heteroaryl groups substituted by the following selected groups: cyanide 346 200823188, halo, hydroxy, a mercapto group, a substituted lower alkyl group, a lower alkenyl group to be substituted, a lower alkoxy group optionally substituted, a carboxyl group, a substituted lower alkoxycarbonyl group, Substituted lower carbon fluorenyl, optionally substituted aminocarbonyl, optionally substituted 5-heterocycloalkyl, optionally substituted heteroaryl, and optionally alkyl substituted amine. At least one chemical as claimed in claim 76, wherein Z1 is selected from the group consisting of phenyl, 1H-portobazol-3-yl; 1H-mouthbazol-4-yl; 1H-triazol-5-yl ; 1-mercapto-1H-pyrazole-4_yl; 1_mercapto-1H-pyrazol-5-yl; 2-amine ίο-methylthiophen-5-yl; 2-cyanothiophene-3- 2-mercaptothiophen-3-yl; 2-carboxenylthiophen-4-yl; 2H-pyrrole·1(5Η)-yl; 2-hydroxymethyloxime-3-yl, 2-曱 吩 -4--4-yl, 2-transmethyl hydrazino-5-yl; 3-aminomercaptothiophen-2-yl; 3-cyano-1-methyl-1 Η-pyridyl Zyridin-4-yl; 3-carbyl 11-cephen-4-yl, 3-mercapto-thioxan-2-yl, 3-carbylmethyl phenanthrene-15-2-yl, 4-mercaptopurine Cet-2-yl, 4-methyl sigma--3, 5 -(1 - 3⁄4ylethyl-1-yl)-thiophen-2-yl; 5-ethenylthiophen-5-yl; 5-cyano-1H-pyrazol-4-yl; 5-cyano-1 -mercapto-1H-pyrazol-4-yl; 5-cyanothiophen-2-yl; 5-mercaptothiophen-2-yl; 5-hydroxydecylthiophen-2-yl; isoxazole i- 4-base, ϋ ratio ° -2 - base, ^ ϋ -3 -3 - base, 0 to ^ -4 - base, 0 σ sit - 2 - base, mouth Qin 20 mouth ^ mouth mouth The chemical according to any one of claims 53 to 77, wherein R1 is selected from the group consisting of hydrogen and optionally substituted lower alkyl. 79. At least one chemical as claimed in claim 78, wherein R1 is selected from the group consisting of argon and sulfhydryl. 347 200823188 8〇. At least - a chemical such as the scope of application for patents, 79, 1 &amp; 0 VIII. 81. At least - a chemical of the scope of claim patent, wherein the compound of formula t is selected from Compound of formula V 式V 其中 R係k自氫、視需要經取代之醯基、視需要經取代 之烷基、氰基、齒基、疊氮基、視需要經取代之胺基、 視需要經取代之烷氧基羰基、視需要經取代之胺基羰 基、續醯基、亞續醯基及硫燒基； Z1係選自氫、視需要經取代之芳基、視需要經取代 之雜芳基、視需要經取代之環烷基、視需要經取代之雜 環烧基、氰基、視需要經取代之烧基、視需要經取代之 酿基、視需要經取代之烷氧基羰基、視需要經取代之胺 基、視需要經取代之胺基羰基、視需要經取代之甲脒基、 视需要經取代之烷氧基、視需要經取代之芳基氧基、視 需要經取代之雜芳基氧基、視需要經取代之雜環烷基氧 基、視需要經取代之烯基、視需要經取代之炔基、磺醯 基、亞續酿基及硫烧基； Z2係選自氫、視需要經取代之曱脒基、羧基、視需 348 200823188 要經取代之烷氧基羰基、視需要經取代之醯基、視需要 經取代之烯基、視需要經取代之烷基、視需要經取代之 雜環烷基、視需要經取代之雜芳基及視需要經取代之胺 基幾基； 5 z3係選自視需要經取代之烷基及視需要經取代之 雜芳烷基； R3係選自氫及視需要經取代之烷基；及 R係％自鼠、視需要經取代之酿基、視需要經取代 之烷基、氰基、i基、疊氮基、視需要經取代之胺基、 10 視需要經取代之烷氧基羰基、視需要經取代之胺基羰 基、磺醯基、亞磺醯基及硫烷基。 82·至少一種如申請專利範圍第81項之化學品，其中ζι係 選視需要經一、二或三個由下列選出之基團取代之苯 基：自i基、烷基、烷氧基、氰基及視需要經取代之醯 15 基。 83·至少—種如申請專利範圍第82項之化學品，其中Z1係 選自3，‘二氟苯基及2-氰基苯基。 84·至少一種如申請專利範圍第81至83項中任一項之化學 品’其中Z2係選自甲基胺基羰基、曱基胺基羰基曱基胺 20 基羰基、乙基胺基羰基、丙基胺基羰基及異丙基胺基羰 基’其中該甲基、乙基、丙基及異丙基基團係視需要經 一、二或三個由下列選出之基團取代：視需要經取代之 曱氧基、視需要經取代之乙氧基、視需要經取代之苯基 及視需要經取代之咄啶基。 349 200823188 85·至少一種如申請專利範圍第84項之化學品，其中Z1係 選自2-曱乳基乙-1-基胺基&gt;炭基_、苯甲基胺基幾基、異丙 基胺基綠基、0比唆-3-基甲基胺基綠基及。比唆-4-基甲基胺 基幾基。 5 86·至少一種如申請專利範圍第81至85項中任一項之化學 品，其中Z3係選自經一、二或三個獨立地由視需要經取 代之芳基及視需要經取代之雜芳基選出之基團取代之乙 基、曱基及丙基。 87.至少一種如申請專利範圍第86項之化學品，其中Z3係 1〇 選自經由視需要經取代之芳基及視需要經取代之雜芳基 選出之基團取代之乙基及甲基。 • 88.至少一種如申請專利範圍第87項之化學品，其中Z3係 選自2-(3-氣苯基）乙基、2-(3-曱基苯基）乙基、2-(吼唆-2-基）乙基、2-(3 -曱基苯基）乙基及ϋ比σ定-2-基甲基。 15 89.至少一種如申請專利範圍第81至88項中任一項之化學 品，其中R1係選自氫及視需要經取代之低碳烷基。 90. 至少一種如申請專利範圍第89項之化學品，其中R1係 選自氫及低碳烧基。 91. 至少一種如申請專利範圍第90項之化學品，其中R1係 20 選自氫及曱基。 92·至少一種如申請專利範圍第91項之化學品，其中R1為 氫。 93.至少一種如申請專利範圍第81至92項中任一項之化學 品，其中R3係選自氫及視需要經取代之低碳烷基。 350 200823188 94.至少一種如申請專利範圍第93項之化學品，其中R3係 選自氫及低碳烧基。 95·至少一種如申請專利範圍第94項之化學品，其中R3係 選自氫及曱基。 5 96.至少一種如申請專利範圍第95項之化學品，其中R3為 氳。 97.至少一種如申請專利範圍第81至96項中任一項之化學 品，其中R6係選自氳、氰基、鹵基、疊氮基、視需要 經取代之胺基羰基及視需要經取代之烷基。 1〇 98.至少一種如申請專利範圍第97項之化學品，其中R6係 選自氫、氰基、氯、溴、氟、疊氮基、視需要經取代之 烷基胺基羰基及視需要經取代之甲基。 99. 至少一種如申請專利範圍第98項之化學品，其中R6係 選自氮、氮基、氣、&gt;臭、豐氮基、°比咬-3-基甲基胺基幾 15 基、胺基曱基及經基甲基。 100. 至少一種如申請專利範圍第99項之化學品，其中R6為 氫。 101. 至少一種如申請專利範圍第1項之化學品，其中該式X 化合物係選自式VI化合物Wherein R is k from hydrogen, optionally substituted fluorenyl, optionally substituted alkyl, cyano, dentate, azide, optionally substituted amine, optionally substituted alkoxy a carbonyl group, an optionally substituted aminocarbonyl group, a fluorenyl group, a fluorenyl group, and a thiol group; the Z1 group is selected from the group consisting of hydrogen, an optionally substituted aryl group, an optionally substituted heteroaryl group, optionally Substituted cycloalkyl, optionally substituted heterocycloalkyl, cyano, optionally substituted alkyl, optionally substituted aryl, optionally substituted alkoxycarbonyl, optionally substituted Amino group, optionally substituted aminocarbonyl group, optionally substituted formazan group, optionally substituted alkoxy group, optionally substituted aryloxy group, optionally substituted heteroaryloxy group a heterocycloalkyloxy group optionally substituted, an alkenyl group optionally substituted, an alkynyl group optionally substituted, a sulfonyl group, a sulfenyl group, and a sulfur group; the Z2 group is selected from the group consisting of hydrogen and Substituted thiol, carboxyl, as needed 348 200823188 substituted alkoxycarbonyl, A substituted thiol group, an optionally substituted alkenyl group, an optionally substituted alkyl group, an optionally substituted heterocycloalkyl group, an optionally substituted heteroaryl group, and an optionally substituted amino group are required. 5 z3 is selected from an optionally substituted alkyl group and optionally substituted heteroarylalkyl group; R3 is selected from hydrogen and optionally substituted alkyl; and R is % from mouse, optionally substituted Alkyl, cyano, i-based, azido, optionally substituted amino, 10, optionally substituted alkoxycarbonyl, optionally substituted aminocarbonyl, Sulfonyl, sulfinyl and sulfanyl. 82. At least one chemical as claimed in claim 81, wherein the oxime is selected from the group consisting of one, two or three groups substituted by the group selected from the group consisting of i groups, alkyl groups, alkoxy groups, Cyano group and substituted 15 base as needed. 83. At least - a chemical as claimed in claim 82, wherein Z1 is selected from the group consisting of 3, 'difluorophenyl and 2-cyanophenyl. 84. A chemical according to any one of claims 81 to 83 wherein Z2 is selected from the group consisting of methylaminocarbonyl, mercaptoaminocarbonylcarbonylamine 20-based carbonyl, ethylaminocarbonyl, A propylaminocarbonyl group and an isopropylaminocarbonyl group wherein the methyl, ethyl, propyl and isopropyl groups are optionally substituted by one, two or three groups selected from the group consisting of: Substituted oxiranyl, optionally substituted ethoxy, optionally substituted phenyl and optionally substituted acridinyl. 349 200823188 85. At least one chemical according to claim 84, wherein Z1 is selected from the group consisting of 2-mercaptoethyl-1-ylamino group&gt; carbon-based, benzylamino-based, isopropyl Alkylamino group, 0-indol-3-ylmethylamino green group and. More than 唆-4-ylmethylamino group. The chemical according to any one of claims 81 to 85, wherein the Z3 is selected from the group consisting of one, two or three independently substituted aryl groups and optionally substituted The selected group of the heteroaryl group is substituted with an ethyl group, a thiol group and a propyl group. 87. At least one chemical according to claim 86, wherein the Z3 group is selected from the group consisting of an ethyl group substituted with an optionally substituted aryl group and optionally a substituted heteroaryl group. . • 88. At least one chemical as claimed in claim 87, wherein Z3 is selected from the group consisting of 2-(3-phenylphenyl)ethyl, 2-(3-mercaptophenyl)ethyl, 2-(吼Indole-2-yl)ethyl, 2-(3-indenylphenyl)ethyl and indolopyridyl-2-ylmethyl. The chemical according to any one of claims 81 to 88, wherein R1 is selected from the group consisting of hydrogen and optionally substituted lower alkyl. 90. At least one chemical as claimed in claim 89, wherein R1 is selected from the group consisting of hydrogen and a low carbon alkyl group. 91. At least one chemical as claimed in claim 90, wherein the R1 system 20 is selected from the group consisting of hydrogen and sulfhydryl. 92. At least one chemical as claimed in claim 91, wherein R1 is hydrogen. A chemical according to any one of claims 81 to 92, wherein R3 is selected from the group consisting of hydrogen and optionally substituted lower alkyl. 350. The method of claim 93, wherein the R3 is selected from the group consisting of hydrogen and a low carbon alkyl group. 95. At least one chemical as claimed in claim 94, wherein R3 is selected from the group consisting of hydrogen and sulfhydryl. 5 96. At least one chemical as claimed in claim 95, wherein R3 is hydrazine. 97. A chemical according to any one of claims 81 to 96, wherein R6 is selected from the group consisting of hydrazine, cyano, halo, azide, optionally substituted aminocarbonyl, and optionally Substituted alkyl. 1〇98. At least one chemical as claimed in claim 97, wherein R6 is selected from the group consisting of hydrogen, cyano, chloro, bromo, fluoro, azide, optionally substituted alkylaminocarbonyl, and optionally Substituted methyl group. 99. At least one chemical as claimed in claim 98, wherein R6 is selected from the group consisting of nitrogen, nitrogen, gas, &gt; odor, nitrogen-rich, butyl-3-ylmethylamino Amino fluorenyl and transmethyl. 100. At least one chemical as claimed in claim 99, wherein R6 is hydrogen. 101. At least one chemical of claim 1, wherein the compound of formula X is selected from the group consisting of a compound of formula VI 式VI 351 200823188 其中 R1及R4係獨立地選自氫、氰基、鹵基、羥基、疊 氮I基、硝基、續酿基、亞續酿基、硫烧基、視需要經取 代之烷氧基、視需要經取代之醯氧基、視需要經取代之 胺基幾基氧基、視需要經取代之芳基氧基、視需要經取 代之雜芳基氧基、視需要經取代之雜環烷基氧基、視需 要經取代之烷氧基羰基、視需要經取代之烷基、視需要 經取代之烯基、視需要經取代之炔基、視需要經取代之 芳基氧基、視需要經取代之芳基、視需要經取代之雜芳 基、視需要經取代之雜環烷基、視需要經取代之胺基、 視需要經取代之醯基、視需要經取代之胺基羰基及視需 要經取代之carbaminodoyl ; Z1係選自視需要經取代之環烧基及視需要經取代 之雜環烷基； Z2係選自氫、視需要經取代之曱脒基、羧基、視需 要經取代之烷氧基羰基、視需要經取代之醯基、視需要 經取代之烯基、視需要經取代之烷基、視需要經取代之 雜環烷基、視需要經取代之雜芳基及視需要經取代之胺 基幾基； Z3係選自卣基及視需要經取代之烷基；及 R3係選自氫及視需要經取代之烷基。 102·至少一種如申請專利範圍第1〇1項之化學品，其中z2係選 自羧基、視需要經取代之烷氧基羰基、視需要經取代之 酿基、視需要經取代之稀基及視需要經取代之燒基。 352 200823188 103·至少一種如申請專利範圍第1〇2項之化學品，其中z2係選 自羧基、視需要經取代之哌啶基羰基、視需要經取代之 吡啶基羰基、視需要經取代之低碳烷基、視需要經取代 之低碳烯基及低碳烷氧基羰基。 5 104·至少一種如申請專利範圍第103項之化學品，其中z2係選 自（2-(N-乙醯基胺基曱基)旅咬小基）幾基；（2_胺基甲基 娘唆-1·基)幾基；1_經基1胺基乙基；2_((曱基磺醯胺基) 甲基）辰疋小基夢厌基，2_(曱基胺基羰基）乙稀基；2-(π比口定 -3-基曱基)-2Η-三唑-5-基；胺基曱基；綾基；曱氧基羰 10 基；°比&quot;定1基羰基；吡啶_3_基羰基；及吡啶-4-基羰基。 105·至少一種如申請專利範圍第1〇1至1〇4項中任一項之化學 品’其中R3係選自氫及視需要經取代之低碳烷基。 106·至^ 一種如申請專利範圍第1〇5項之化學品，其中R3係選 自氫及低碳烷基。 15 1〇7·至少一種如申請專利範圍第1〇6項之化學品，其中R3係選 自氩及甲基。 1〇8·至少一種如申請專利範圍第107項之化學品，其中R3為 氫。 109·至少—種如申請專利範圍第ι〇ι項之化 20 -C(0)NR2rs ^ T ^ 婉、’其中R係選自視需要經取代之烷基及視需 經取代之環烷基；而R5係選自氫及視需要經取代之烷 基。 口、 種如申請專利範圍第ιοί至1〇9項中任一項之化學 阳，其中R4係選自氫、氰基、鹵基、疊氮基、視需要經 353 200823188 取代之胺基羰基及視需要經取代之烷基。 111·至少一種如申請專利範圍第11〇項之化學品，其中R4係選 自氫、氰基、氯、溴、氟、疊氮基、視需要經取代之烷 基胺基羰基及視需要經取代之曱基。 112·至少一種如申請專利範圍第ln項之化學品，其中R4係選 自氫、氰基、氯、溴、叠氮基“比咬冬基甲基胺基幾基、 胺基曱基及經基甲基。 113·至少一種如申請專利範圍第12項之化學品，其中r4係為 氫。 10 15 20 114·至^'一種如申请專利範圍第至113項中任一項之化學 品，其中R5係選自氫及低碳烷基。 115·至少一種如申請專利範圍第丨14項之化學品，其中R5係 自氫及甲基。 、 116·至少一種如申請專利範圍第ιΐ5項之化 氫- 117· —種如_請專利範圍第1G9至116項巾任-項之化學 中R係選自視需要經取代之甲基、視需要經取代 視需要經取代之丙基、視f要經取代之丁基、 =要峰代之戊基、視需要經取代之己基、視需要經 之=丙ί:需要經取代之環戊基及視需獅代 二二Γ列選出之基團取代：視需要經取代之芳 取代之雜芳基、視需要經取代之賴基、 視而要、、4代之魏基、視W峰叙 354 200823188 需要經取代之胺基、羥基、羧基、視需要經取代之烧氧 基羰基及視需要經取代之烷氧基。· 118·至少一種如申請專利範圍第117項之化學品，其中R2係選 自甲基及乙基，其中該曱基及乙基基團係視需要經一或 5 二個由下列選出之基團取代··視需要經取代之芳基、視 需要經取代之雜芳基、視需要經取代之雜環烷基、視需 要經取代之環烷基、視需要經取代之胺基羰基、視需要 經取代之胺基、羥基、羧基、視需要經取代之烷氧基幾 基及視需要經取代之烷氧基。 ίο 119·至少一種如申請專利範圍第118項之化學品，其中R2係選 自（H2-胺基乙基)-iH』比唑冬基）曱基；（1_(甲基磺醯基) • 旅淀基）甲基；（1-乙酿基旅°定-3-基）曱基；（1-乙酸基〇比 • 咯啶-2-基）甲基；（1Η-咪唑-2-基）曱基；（1Η-吡唑-3-基) 甲基，（1-曱基-1Η_σ比嗤-3-基）曱基；（1_曱基-1Η』比吐-5- 15 基）甲基，（2-(胺基幾基）乙基胺基）幾基甲基；（2-(胺基 甲基广比咬_3_基）甲基；（2_(羧基）乙基胺基）幾基曱基； (2-(—甲基胺基）乙基胺基)幾基甲基；(2-(經基）乙基胺基) 羰基甲基；（2-(曱基胺基）乙基胺基）羰基曱基；（2_(]^_曱 基(第三丁氧基羰基)_胺基）乙基胺基）羰基曱基；（2_ 20 氧基哌啶基）曱基；（3-(二甲基胺基）丙基胺基）羰基甲 基；（3-(羥基）乙基胺基)羰基曱基；（3_(第三丁氧基羰基 胺基）丙基胺基）幾基曱基；（4-(胺基甲基户比π定-2-基）曱 基；（5_(胺基甲基户比啶冬基）曱基；（6_((1，3_二氧基異吲 哚啉-2-基）甲基)π比啶_2_基）甲基；（6-(2_胺基乙基胺基)吼 355 200823188 咬-2-基）曱基；（6_(3_胺基丙基胺基）π比啶_2_基）曱基； (6_(胺基甲基)η比啶1基）曱基；（6_(經基曱基)吼咬_2-基) 曱基；（6-溴吼啶_2_基）甲基；（曱基磺醯胺基)幾基甲基； (吼啶-2-基）乙基胺基；丨_(2_(第三丁氧基羰基胺基）乙 基)-1Η-啦唑-3-基曱基；^(2-(第三丁氧基羰基胺基）乙 基)_1H』比嗤_5_基甲基；1-(胺基羰基)·2_(胺基)_乙_1-基； 1- (胺基羰基)-3-(胺基)_丙基；ι_(胺基羰基)_4_(胺基戶丁 基；1-(胺基羰基)-4-(苯曱基氧基羰基胺基)_戊基；ι_(胺 基羰基)-5-(胺基)_戊基；ι_(胺基羰基）乙基；ι_(羧氧 基(胺基)-乙_；[_基；ι_(二曱基胺基羰基)_2_(胺基)_乙 -1-基；1-(經基)_2-(胺基羰基曱基胺基）乙小基；μ(經 基)-2_(乙氧基羰基曱基胺基）乙基；ι_(羥基)_2_^比啶 -2-基甲基胺基）乙基；(曱氧基羰基)_2_(胺基 基；1-(曱氧基羰基)_2-(第三丁氧基羰基胺基)_乙_；μ基； Η甲氧基幾基）乙+基；！_(曱基胺基羰基(胺基)_乙 -1-基(2 occ) ; 曱基胺基羰基）乙基；丨_胺基羰基_2_ 輕基-乙-1-基，1_甲氧基羰基_2_羥基-乙小基；2_(2_胺基 乙氧基）乙基；2-(2-胺基乙基)_，比啶_6_基甲基；2_(2_胺基 乙基胺基）乙基；2_(3_氟苯基）乙基；2_(3_甲氧基幾基）乙 基2 (6 (私:基甲基）σ比咬-2-基）乙基；2-(乙酸基胺基）乙 基，2-(胺基）乙基；2_(胺基羰基)_2_(乙醯基胺基)_乙_^ 基；2-(胺基幾基叫胺基)_乙-1-基；2-(胺基幾基）乙基； 2_(胺基曱基)吼啶1基曱基；2_(缓基)_2_(胺基)_乙小基； 2- (二曱基胺基）乙基；2_(二甲基胺基羰基)_2_(胺基&gt; 乙_工_ 356 200823188 基；2-(乙氧基羰基）乙基；2_(甲氧基羰基)_2_(乙醯基胺 —基)-乙-1-基，2-(甲氧基羰基)_2_(胺基)_乙基；2_(甲氧 基罗厌基月女基）乙基；2-(甲基胺基）乙基；2_(曱基胺基幾 基)-2-(乙基胺基)ϋ基；2_(甲基胺基羰基)-2_(胺基)_ 乙-1-基；2-(曱基磺醯胺基）乙基；2气甲氧基羰基&gt;2_(胺 基)-乙-1-基；2-(Ν-(第三丁氧基羰基)_Ν_(甲基)_胺基）乙 基；2_(派口井小基）乙基；2十比α井-2-基）乙基；2-(吼啶-2-基）乙基；2-(吡啶-3-基）乙基；2-(第三丁氧基羰基胺基甲 基)吼啶-3-基甲基；2-(第三丁氧基羰基胺基曱基)σ比啶_6_ 基甲基；2-(三氟甲基)_吡啶-6-基曱基；2-胺基吡啶-3-基 甲基；2-胺基吡啶-5-基曱基；2-氯吡啶-5-基曱基；2-氰 基吡啶-5-基曱基；2-羥基-3-胺基-丙-1-基；2-羥基乙基； 甲氧基乙-1-基；2-曱氧基吡啶-3-基曱基；2-甲氧基口比 啶-5-基甲基；2-曱基吡啶-3-基曱基；2-曱基吡啶-5-基曱 基；2-曱基咐啶-6-基曱基；3-(2-胺基乙基)環己基）曱基； 3_(4_甲基哌畊-1-基）丙基；3-(胺基)-3-(曱基胺基羰基）丙 小基；3-(胺基羰基）丙基；3-(胺基甲基)苯曱基；3-(胺基 曱基户比啶-2-基甲基；3-(甲氧基羰基）丙基；3-(甲基胺基 羰基）丙基；3-(三氟曱基)j比啶-2-基甲基；3,4-二氟苯曱 基；3-胺基曱基吡啶-4-基甲基；3-胺基丙基；3-胺甲醯 基環戊基；3-羧基丙基；3-經基丙基；3-曱氧基丙基；4-(胺 基甲基)-吡啶-2-基曱基；4_(N，N-二曱基胺基）吼啶-3-基 曱基；4-(第三丁氧基羰基胺基)-嗎啉基曱基；4-胺基丁 基；4-胺基曱基吼啶-3-基曱基；4-氰基苯曱基；4_氟苯 357 200823188 甲基；4-曱基胺基吼啶-3-基曱基；4-曱基苯曱基；4-嗎 啉基吡啶-3-基甲基；4-哌畊基吡啶-3-基甲基；5-((雙(二 甲基胺基）甲基胺基）甲基）吼啶-3-基曱基；5-(胺基甲基) 。比啶-2-基曱基；5-(胺基曱基)吼啶-3-基甲基；5-(羥基曱 5 基）σ比ϋ定-3 -基曱基，5-(第二丁乳基搂基胺基曱基丨-吼咬 -2-基曱基，5-(二鼠曱基)-ϋ比σ定-2-基曱基，5-胺基戍基， 5-胺基吼啶-2-基曱基；6-((雙（二甲基胺基)伸甲基胺基) 曱基)吡啶-2-基曱基；6-(4-乙醯基哌啡-1-基)吼啶-3-基曱 基），6-(胺基曱基)0比σ定-2-基曱基，6-胺基己基，胺基援 ίο 基甲基；苯甲基；環丙基甲基；二甲基胺基羰基甲基； 異丙基，異ϋ亏唾-5 -基甲基，甲氧基幾基甲基，曱基，曱 ' 基胺基羰基曱基；噚唑-2-基甲基；哌啶-4-基曱基；丙-2- • 烯-1-基；吡畊-2-基曱基；吡啶-2-基甲基；吡啶-2-基曱 基-Ν-氧化物；吡啶-3-基曱基；吡啶-3-基甲基-Ν-氧化物； 15 °比ϋ定-4-基甲基，11 塞吩-2-基曱基，及嗟吩-3-基曱基。 120. 至少一種如申請專利範圍第101至119項中任一項之化學 品，其中ζ3係選自i基及視需要經取代之低碳烷基。 121. 至少一種如申請專利範圍第120項之化學品，其中Z3係選 自鹵基、視需要經取代之甲基、視需要經取代之乙基及 20 視需要經取代之丙基，其中該曱基、乙基及丙基基團係 視需要經一或二個由下列選出之基團取代：羥基、視需 要經取代之芳基、視需要經取代之雜芳基、視需要經取 代之雜環烷基、視需要經取代之環烷基及視需要經取代 之芳基氧基。 358 200823188 122.至少一種如申請專利範圍第121項之化學品，其中Z3係選 自2-(3-甲基苯基）乙基、（四氳呋喃2-基）甲基、1-羥基環 己基曱基、2-(1，3-二氧戊環-2-基）乙基、2·(1Η-咪唑_4_ 基）乙基、2-(1-曱基-1Η-咪唑-4-基）乙基、2·(1-甲基哌啶 5 -4-基）乙基、2_(2,3-二氣苯基）乙基、2-(2,5-二氣苯基）乙 基、2-(2,6-二氟苯基）乙基、2-(2-氯苯基）乙基、2-(2-氰基 苯基）乙基、2-(2 -氟苯基）乙基、2-(2-經基苯基）乙基、2-(2_ 甲氧基苯基）乙基、2-(2-曱基苯基）乙基、2-(2-氧基咪唑 0定-1-基）乙基、2-(2-乳基娘0定-1-基）乙基、2-(2-氧1基0比咯 1〇 咬-1_基）乙基、2-(3-(二氣曱基）苯基）乙基、2-(3，4-二氣苯 基）乙基、2-(3,5-二氟苯基）乙基、2-(3,5-二甲基-lH-u比唑 -1 -基）乙基，2-(3，5-二曱基-1 Η-%。坐-4-基）乙基、2-(3-胺曱 醢基苯基）乙基、2-(3-羧基苯基）乙基、2-(3-氰基苯基）乙 基、2-(3-氟苯基)-2-(羥基)-乙基、2-(3-氟苯基）乙基、2-(3-15 氟吡啶-2-基）乙基、2-(3-曱氧基羰基苯基）乙基、2-(3-曱 氧基苯基）乙基、2-(3-曱基苯基）乙基、2-(4-胺基苯基）乙 基、2-(4-氯苯基）乙基、2-(4-氟苯基）乙基、2-(4-羥基苯 基）乙基、2-(苯并[d][l，3]二氧環戊烯-5-基）乙基、2-(呋喃 2- 基）乙基、2-(羥基)-2-(苯基）乙基、2-(苯基）乙基、2-(吼 2〇 咬-2-基）乙基、2-(ϋ比17定-3-基）乙基、2-(ϋ塞吩-2-基）乙基、 2 -壞己-1 -細基乙基、2 -壞己基乙基、2 -嗎琳基乙基、2 _ 苯氧基乙基、2-苯基丙-1-基、3-(ΙΗ-咪唑-1-基）丙-1-基、 3- 苯基丙基、苯甲基、氯、異戊基、丙基、吼啶-2-基曱 基、吡啶-3-基曱基及噻吩-3-基甲基。 359 200823188 123·至少一種如申請專利範圍第122項之化學品，其中Z3係選 自2-(3-氟苯基）乙基及2-(π比唆_2_基）乙基。 124·至少一種如申請專利範圍第1〇1至123項中任一項之化學 品，其中Ζ1係選自環烷基及雜環烷基，其中各基團係視 5 需要經一或二個由下列選出之基團取代：氰基、i基、 羥基、曱醯基、視需要經取代之烷基、視需要經取代之 烯基、視需要經取代之烷氧基、羧基、視需要經取代之 烷氧基羰基、視需要經取代之醯基、視需要經取代之胺 基羰基、視需要經取代之胺基、視需要經取代之雜環烷 10 基、視需要經取代之雜芳基、視需要經取代之甲脒基及 視需要經取代之磺醯基。 • 125·至少一種如申請專利範圍第124項之化學品，其中Z1係選 - 自環烷基及雜環烷基，其中各基團係視需要經一或二個 由下列選出之基團取代：氰基、鹵基、羥基、曱醯基、 15 視需要經取代之低碳烷基、視需要經取代之低碳烯基、 視需要經取代之低碳烷氧基、羧基、視需要經取代之低 碳烷氧基羰基、視需要經取代之醯基、視需要經取代之 胺基羰基、視需要經取代之雜環烷基、視需要經取代之 雜芳基、視需要經取代之曱脒基及視需要經取代之磺醯 20 基。 126.至少一種如申請專利範圍第125項之化學品，其中Z1係選 自1-(2Η)-(曱氧基羰基)-3,4_二氫吼啶_4-基；1-(2Η)-(曱氧 基叛基)-5,6-二氫σ比咬-4-基；1-(2H)-(曱氧基曱基)-5,6-二 氫°比啶4-基；1_(2H)-(第三丁氧基羰基)-5,6-二氫吼啶-4- 360 200823188 基，1-(2Η)-5,6-二鼠吼^7定-4_基，1-(乙酿基)-4,5-二氮口米°坐 •2-基；1-(二甲基胺曱醯基)-1，.2,3,6-四氳吡啶-4-基；1-(曱 氧基曱基)_4,5_二氫咪唑-2-基；1-氰基-4,5-二氫-1H_咪唑 -2-基，1-曱基-1，2,3,6-四鼠吼12定-4-基，2-(乙酿基胺基甲 5 基）0比嘻淀-1 -基，2-(¾基甲基）嗎琳基，2-(經基曱基）11比 咯啶-1-基；2-(曱氧基曱基)吡咯啶-1-基；2H-吡咯-1(5H)-基；2-羥基嗎啉基；2-曱基-4-(第三丁氧基羰基)-哌畊-1-基，2-氧基-5-經基-旅咬基，2-氧基娘ϋ井基，2-氧基派唆 基；2-氧基吼咯啶基；3-(3,3-二甲基脲基)吡咯啶-1-基； 10 3-(胺基曱基）-σ比咯咬-1-基，3-(竣基曱基）-°比洛σ定基； 3- (二甲基胺基户比咯啶-1-基；3·(二曱基胺基曱基)-吼咯 σ定-1-基，3-(技基曱基比咯σ定-1-基，3-(曱乳基綠基胺基)_ 吡咯啶基；3-(甲基磺醯基)吡咯啶-1-基；3-(Ν-乙醯基-Ν- 甲基)-胺基曱基)-吡咯啶-1-基；3-(吡啶-4-基）吡咯啶-1-15 基；3-(第三丁氧基羰基胺基)-吼咯啶基；3-(三氟曱基） 吡咯啶-1-基；3,3-二氟吡咯啶基；3-乙醯基胺基吡咯啶 基，3 -胺基ϋ比洛ϋ定-1 -基，3 -氣ϋ比略^定-1 -基，3 -經基曱基 吼咯唆-1-基；3-經基吼嘻唆-1-基；3-曱氧基甲基吼洛口定 -1 -基，3-曱基胺基-吼洛ϋ定基，3-乳基娘ϋ井-1 -基，4-(乙酿 20 基)-哌畊-1-基；4-(胺基曱基)哌啶-1-基；4-(乙氧基羰基)- 娘π井-1-基，4-(乙乳基搂基)-ϋ底咬基，4-(曱氧基搂基)-派 畊-1-基；4-(甲基磺醯基)環己-1-烯基；4-(Ν，Ν-二曱基胺 基搂基)-派^井-1_基，4-(弟二丁乳基綠基胺基)-旅17定-1-基； 4- (第三丁氧基羰基胺基曱基)-哌啶-1-基；4,5-二氳-1Η- 361 200823188 咪唑-2-基；4,5-二氳崎唑-2-基；4-羥基-4-苯基哌啶-1-基； 4-技基乙基-旅咬-基，4-經基甲基-旅咬-基；4-輕基派咬 基；4-甲基胺基搂基-旅ϋ定基，4-甲基旅11井-1-基；4-曱基 哌啶基；4-氧基環己-1-烯基；5,6-二氫吡啶-1(2Η)-基； 氮哩基；環己-1-烯基；環己基；環戊-1-烯基；環戊基； 嗎琳基；旅σ井基；旅咬基；σ比咯σ定基；及嗟嗎淋基。 127. 至少一種如申請專利範圍第101至126項中任一項之化學 品，其中R1係選自氫及視需要經取代之低碳烷基。 10 15 128. 至少一種如申請專利範圍第127項之化學品，其中R1係選 自氫及低碳烧基。 129. 至少一種如申請專利範圍第128項之化學品，其中R1係選 自氫及甲基。 130. 至少一種如申請專利範圍第129項之化學品，其中R1為 氫。 131. 至少一種如申請專利範圍第1項之化學品，其中該式X化 合物係選自式VII化合物Formula VI 351 200823188 wherein R1 and R4 are independently selected from the group consisting of hydrogen, cyano, halo, hydroxy, azide I, nitro, holly, sulphur, thiol, optionally substituted alkane An oxy group, optionally substituted methoxy group, optionally substituted amino group oxy group, optionally substituted aryloxy group, optionally substituted heteroaryloxy group, optionally substituted Heterocycloalkyloxy, optionally substituted alkoxycarbonyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryloxy , optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, optionally substituted amine, optionally substituted thiol, optionally substituted amine Carbocarbonyl and optionally substituted carbaminodoyl; Z1 is selected from optionally substituted cycloalkyl and optionally substituted heterocycloalkyl; Z2 is selected from hydrogen, optionally substituted thiol, carboxyl, Substituted alkoxycarbonyl group, optionally substituted sulfhydryl group, depending on necessity Alkenyl group to be substituted, alkyl group optionally substituted, heterocycloalkyl group optionally substituted, heteroaryl group optionally substituted, and optionally substituted amino group; Z3 is selected from fluorenyl group And optionally substituted alkyl; and R3 is selected from the group consisting of hydrogen and optionally substituted alkyl. 102. A chemical according to any one of claims 1 to 1, wherein z2 is selected from the group consisting of a carboxyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted aryl group, an optionally substituted dilute group, and Substituted burnt base as needed. 352 200823188 103. At least one chemical according to claim 1, wherein z2 is selected from the group consisting of a carboxyl group, a substituted piperidinylcarbonyl group, an optionally substituted pyridylcarbonyl group, optionally substituted. Lower alkyl, optionally substituted lower alkenyl and lower alkoxycarbonyl. 5 104. At least one chemical as claimed in claim 103, wherein z2 is selected from the group consisting of (2-(N-ethyl decylamino fluorenyl) brittle base); (2-aminomethyl)唆-1·yl) aryl; 1 _ yl 1 aminoethyl; 2 _ ((fluorenyl sulfonylamino) methyl) 疋 疋 基 base, 2 _ (decylaminocarbonyl) a dilute group; a 2-(π-tert-but-3-ylindenyl)-2Η-triazol-5-yl group; an amine fluorenyl group; a fluorenyl group; an oxime oxycarbonyl group 10; a ratio of &quot;1 carbonyl; Pyridine-3-ylcarbonyl; and pyridin-4-ylcarbonyl. 105. A chemical according to any one of claims 1 to 1 to 4 wherein R3 is selected from the group consisting of hydrogen and optionally substituted lower alkyl. 106· to ^ A chemical as claimed in claim 1 , wherein R3 is selected from the group consisting of hydrogen and lower alkyl. 15 1〇7· At least one of the chemicals of the first and sixth aspects of the patent application, wherein R3 is selected from the group consisting of argon and methyl. 1〇8· At least one chemical as claimed in claim 107, wherein R3 is hydrogen. 109. At least - such as the patent application range ι 〇 之 ification 20 - C (0) NR2rs ^ T ^ 婉, 'where R is selected from the alkyl group optionally substituted and cycloalkyl as desired And R5 is selected from the group consisting of hydrogen and optionally substituted alkyl. Ordinary, such as the chemical cation of any one of the claims ιοί to 〇9, wherein R4 is selected from the group consisting of hydrogen, cyano, halo, azide, amino carbonyl substituted by 353 200823188, and An alkyl group which is optionally substituted. 111. At least one chemical according to claim 11 wherein R4 is selected from the group consisting of hydrogen, cyano, chloro, bromo, fluoro, azide, optionally substituted alkylaminocarbonyl, and optionally Replace the base. 112. At least one chemical as claimed in claim ln, wherein R4 is selected from the group consisting of hydrogen, cyano, chloro, bromo, azido, butylaminomethylamino, aminoguanidino and 113. A chemical according to claim 12, wherein the r4 is hydrogen. 10 15 20 114· to a chemical according to any one of claims 1 to 113, Wherein R5 is selected from the group consisting of hydrogen and lower alkyl. 115. At least one chemical as described in claim 14 of the patent application, wherein R5 is derived from hydrogen and methyl. 116, at least one of the applications of claim ι. Hydrogen - 117 · - _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ The butyl group to be substituted, the pentyl group to be substituted, the hexyl group to be substituted as needed, and the propyl group as needed: the group selected by the substituted cyclopentyl group and the lion group Substitution: Heteroaryl substituted by aryl as required, substituted lysine as needed, depending on, 4 generations Wei Ke, 视 W peak 354 200823188 A substituted amino group, a hydroxyl group, a carboxyl group, an optionally substituted alkoxycarbonyl group and an optionally substituted alkoxy group. 118. At least one of the patent applications A chemical of item 117, wherein R2 is selected from the group consisting of methyl and ethyl, wherein the thiol and ethyl groups are optionally substituted by one or two of the groups selected by the following: Substituted, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, optionally substituted cycloalkyl, optionally substituted aminocarbonyl, optionally substituted amine, hydroxy, carboxy And optionally substituted alkoxy groups. ίο 119. At least one chemical according to claim 118, wherein R2 is selected from (H2-aminoethyl) -iH"-pyrazolyl) fluorenyl; (1_(methylsulfonyl); lyophilized) methyl; (1-ethyl aryl-based -3-yl) fluorenyl; (1-acetic acid (1Η-imidazol-2-yl)indenyl; (1Η-pyrazol-3-yl)methyl, (1-indolyl-1Η_嗤-3-yl) fluorenyl; (1_mercapto-1 Η) than oxime-5- 15 yl) methyl, (2-(amino)ethylamino)methylidene; (2 -(aminomethylmethyl octa- _3_yl)methyl; (2-(carboxy)ethylamino) benzyl hydrazino; (2-(-methylamino)ethylamino) (2-(trans)ethylamino)carbonylmethyl; (2-(decylamino)ethylamino)carbonylindenyl; (2-(]^-indenyl (t-butoxy) Carbonyl)-amino)ethylamino)carbonylcarbonyl; (2-20 oxypiperidinyl)fluorenyl; (3-(dimethylamino)propylamino)carbonylmethyl; (3-( Hydroxy)ethylamino)carbonylcarbonyl; (3-(t-butoxycarbonylamino)propylamino) benzyl hydrazino; (4-(aminomethyl pyridyl-2-yl) Sulfhydryl; (5-(aminomethyl-methylpyridinyl)-yl); (6-((1,3-dioxyisoindolin-2-yl)methyl)π-pyridin-2-yl) Methyl; (6-(2-aminoethylamino) ruthenium 355 200823188 keto-2-yl) fluorenyl; (6-(3-aminopropylamino) π-pyridyl-2-yl) fluorenyl (6_(Aminomethyl) η than pyridine 1 yl) fluorenyl; (6_(via fluorenyl) hydrazine; _2-yl) fluorenyl; (6-bromoacridin-2-yl)methyl; (fluorenylsulfonylamino)methylidene; (acridin-2-yl)ethylamine; 丨_( 2-((t-butoxycarbonylamino)ethyl)-1Η-oxazol-3-ylindenyl; ^(2-(t-butoxycarbonylamino)ethyl)_1H" than 嗤_5_ Methyl; 1-(aminocarbonyl)·2_(amino)-ethyl-1-yl; 1-(aminocarbonyl)-3-(amino)-propyl; i-(aminocarbonyl)_4_( Aminobutyl butyl; 1-(aminocarbonyl)-4-(phenylhydrazinocarbonylcarbonyl)-pentyl; i-(aminocarbonyl)-5-(amino)-pentyl; ι-(amine Methylcarbonyl)ethyl; i-(carboxyoxy(amino)-ethyl); [-yl; i-(didecylaminocarbonyl)_2-(amino)-eth-1-yl; 1-(trans-base) _2-(Aminocarbonylcarbonylamino)ethyl small group; μ(trans)-2-((ethoxycarbonylguanidino)ethyl; ι_(hydroxy)_2_^pyridin-2-ylmethylamine Ethyl (ethyloxycarbonyl)_2-(amino group; 1-(decyloxycarbonyl)_2-(t-butoxycarbonylamino)-B-; μ group; fluorenylmethoxy group ) B + base;! _(decylaminocarbonyl(amino)-eth-1-yl(2 occ); mercaptoaminocarbonyl)ethyl; hydrazine-aminocarbonyl-2_light-ethyl-1-yl, 1-methyl Oxycarbonylcarbonyl-2-hydroxy-ethyl small group; 2-(2-aminoethoxy)ethyl; 2-(2-aminoethyl)-, pyridyl-6-ylmethyl; 2_(2_ Aminoethylamino)ethyl; 2_(3-fluorophenyl)ethyl; 2-(3-methoxymethyl)ethyl 2 (6 (private: ylmethyl) σ ratio -2- base Ethyl; 2-(acetamidoamino)ethyl, 2-(amino)ethyl; 2-(aminocarbonyl)_2-(ethinylamino)-ethyl-yl; 2-(amino group Amino group)-ethyl-1-yl; 2-(aminophenyl)ethyl; 2-(aminoindenyl)acridinyl 1 fluorenyl; 2_(suppressyl)_2_(amino)-B 2-(didecylamino)ethyl; 2-(dimethylaminocarbonyl)_2-(amino)&gt; B_work_356 200823188; 2-(ethoxycarbonyl)ethyl; 2_( Methoxycarbonyl)_2_(ethinylamine-yl)-eth-1-yl, 2-(methoxycarbonyl)_2-(amino)-ethyl; 2_(methoxy oxa ruthenyl) Ethyl; 2-(methylamino)ethyl; 2-(indolylamino)-2-(ethylamino)indenyl; 2-(methylaminocarbonyl)-2-(amino)_ B-1- ; 2-(indolylsulfonylamino)ethyl; 2 gas methoxycarbonyl &gt; 2 -(amino)-eth-1-yl; 2-(indole-(t-butoxycarbonyl)_Ν_(A Ethyl)-amino)ethyl; 2_(Peikou small base) ethyl; 2 decyl-α-2-yl)ethyl; 2-(acridin-2-yl)ethyl; 2-(pyridine 3-yl)ethyl; 2-(t-butoxycarbonylaminomethyl) acridine-3-ylmethyl; 2-(t-butoxycarbonylaminomethyl) σ-pyridine _6_ Methyl; 2-(trifluoromethyl)-pyridin-6-ylindenyl; 2-aminopyridin-3-ylmethyl; 2-aminopyridin-5-ylindenyl; 2-chloropyridine- 5-ylindenyl; 2-cyanopyridine-5-ylindenyl; 2-hydroxy-3-amino-propan-1-yl; 2-hydroxyethyl; methoxyethyl-1-yl; 2- Alkoxypyridin-3-ylindenyl; 2-methoxylpyridin-5-ylmethyl; 2-mercaptopyridine-3-ylindenyl; 2-mercaptopyridine-5-ylindenyl; 2-mercaptoacridin-6-ylindenyl; 3-(2-aminoethyl)cyclohexyl)indenyl; 3-(4-methylpipen-1-yl)propyl; 3-(amino --3-(decylaminocarbonyl)propanyl; 3-(aminocarbonyl)propyl; 3-(aminomethyl)phenylhydrazinyl; 3-(aminopurinylbipyridin-2- Methyl group; 3-(methoxycarbonyl)propyl 3-(methylaminocarbonyl)propyl; 3-(trifluoromethyl)j-pyridin-2-ylmethyl; 3,4-difluorobenzoinyl; 3-aminomercaptopyridine- 4-ylmethyl; 3-aminopropyl; 3-amineindolylcyclopentyl; 3-carboxypropyl; 3-propylpropyl; 3-methoxypropyl; 4-(aminomethyl) 4-pyridin-2-ylindenyl; 4-(N,N-didecylamino)acridin-3-ylindenyl; 4-(t-butoxycarbonylamino)-morpholinylfluorenyl 4-aminobutyl; 4-aminomercaptoacridin-3-ylindenyl; 4-cyanobenzoinyl; 4-fluorobenzene 357 200823188 methyl; 4-mercaptoaminopyridinium-3 -ylindenyl; 4-mercaptophenylhydrazino; 4-morpholinylpyridin-3-ylmethyl; 4-piperidinylpyridin-3-ylmethyl; 5-((bis(dimethylamino) Methylamino)methyl)acridin-3-ylindenyl; 5-(aminomethyl). Bis-2-ylindenyl; 5-(aminoindenyl)acridin-3-ylmethyl; 5-(hydroxyindole-5yl)σϋϋ定-3-ylindenyl, 5-(second Butyl-based mercaptoamine-based thiol-indole-2-yl sulfhydryl, 5-(dimural fluorenyl)-anthracene sigma-2-ylindolyl, 5-aminoindenyl, 5-amine Acridine-2-ylindenyl; 6-((bis(dimethylamino)methylamino) fluorenyl)pyridin-2-ylindenyl; 6-(4-ethinylpipenine- 1-yl)acridin-3-ylindenyl), 6-(aminoindenyl) 0-sigma-2-ylindenyl, 6-aminohexyl, aminylmethyl; benzyl Cyclopropylmethyl; dimethylaminocarbonylmethyl; isopropyl, isoindolyl-5-ylmethyl, methoxymethylmethyl, decyl, 曱'ylaminocarbonyl fluorenyl ; oxazol-2-ylmethyl; piperidin-4-ylindenyl; prop-2--2-en-1-yl; pyridin-2-ylindenyl; pyridin-2-ylmethyl; pyridine-2 - fluorenyl-hydrazine-oxide; pyridin-3-ylindenyl; pyridin-3-ylmethyl-indole-oxide; 15 ° ratio -4--4-ylmethyl, 11 cephen-2-yl Indenyl, and indole-3-ylindenyl. 120. A chemical according to any one of claims 101 to 119, wherein the oxime 3 is selected from the group consisting of i groups and optionally substituted lower alkyl groups. 121. At least one chemical as claimed in claim 120, wherein Z3 is selected from the group consisting of halo, optionally substituted methyl, optionally substituted ethyl and 20 optionally substituted propyl, wherein The thiol, ethyl and propyl groups are optionally substituted by one or two groups selected from the group consisting of hydroxyl groups, optionally substituted aryl groups, optionally substituted heteroaryl groups, optionally substituted Heterocycloalkyl, optionally substituted cycloalkyl and optionally substituted aryloxy. 358 200823188 122. At least one chemical according to claim 121, wherein Z3 is selected from the group consisting of 2-(3-methylphenyl)ethyl, (tetramethylenefuran-2-yl)methyl, 1-hydroxyl ring Hexyl fluorenyl, 2-(1,3-dioxolan-2-yl)ethyl, 2·(1Η-imidazolium-4-yl)ethyl, 2-(1-indolyl-1Η-imidazole-4- Ethyl, 2-(1-methylpiperidin-5-4-yl)ethyl, 2-(2,3-diphenyl)ethyl, 2-(2,5-diphenyl)ethyl , 2-(2,6-difluorophenyl)ethyl, 2-(2-chlorophenyl)ethyl, 2-(2-cyanophenyl)ethyl, 2-(2-fluorophenyl) Ethyl, 2-(2-phenylphenyl)ethyl, 2-(2-methoxyphenyl)ethyl, 2-(2-mercaptophenyl)ethyl, 2-(2-oxyl Imidazole 0-den-1-yl)ethyl, 2-(2-lactyl-n-l-yl)ethyl, 2-(2-oxo 1 yl 0-pyrene 1 -1-1 yl)ethyl , 2-(3-(dioxamethyl)phenyl)ethyl, 2-(3,4-diphenyl)ethyl, 2-(3,5-difluorophenyl)ethyl, 2- (3,5-Dimethyl-lH-u-pyrazol-1-yl)ethyl, 2-(3,5-dimercapto-1 Η-%. sit-4-yl)ethyl, 2-( 3-aminomercaptophenyl)ethyl, 2-(3-carboxyphenyl)ethyl, 2-(3-cyanide Phenyl)ethyl, 2-(3-fluorophenyl)-2-(hydroxy)-ethyl, 2-(3-fluorophenyl)ethyl, 2-(3-15 fluoropyridin-2-yl) Ethyl, 2-(3-decyloxycarbonylphenyl)ethyl, 2-(3-decyloxyphenyl)ethyl, 2-(3-indolylphenyl)ethyl, 2-(4- Aminophenyl)ethyl, 2-(4-chlorophenyl)ethyl, 2-(4-fluorophenyl)ethyl, 2-(4-hydroxyphenyl)ethyl, 2-(benzo[ d][l,3]dioxol-5-yl)ethyl, 2-(furan-2-yl)ethyl, 2-(hydroxy)-2-(phenyl)ethyl, 2-(benzene Ethyl, 2-(吼2〇2-yl)ethyl, 2-(indole ratio 17-but-3-yl)ethyl, 2-(decenophen-2-yl)ethyl, 2 - succinyl-1 - fine ethyl, 2-dehexylethyl, 2-cylinylethyl, 2 phenoxyethyl, 2-phenylpropan-1-yl, 3-(indole-imidazole -yl)propan-1-yl, 3-phenylpropyl, benzyl, chloro, isopentyl, propyl, acridine-2-ylindenyl, pyridin-3-ylindenyl and thiophene- 3-ylmethyl. 359 200823188 123. At least one chemical as claimed in claim 122, wherein Z3 is selected from the group consisting of 2-(3-fluorophenyl)ethyl and 2-(π-pyridin-2-yl)ethyl. The chemical according to any one of claims 1 to 1 wherein the oxime 1 is selected from the group consisting of a cycloalkyl group and a heterocycloalkyl group, wherein each group is required to undergo one or two Substituted by the following selected groups: cyano, i-group, hydroxy, fluorenyl, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxy, carboxy, optionally Substituted alkoxycarbonyl, optionally substituted fluorenyl, optionally substituted aminocarbonyl, optionally substituted amine, optionally substituted heterocycloalkanyl, optionally substituted heteroaryl A sulfonyl group which is substituted, optionally substituted, and optionally substituted. • 125. At least one chemical as claimed in claim 124, wherein Z1 is selected from the group consisting of a cycloalkyl group and a heterocycloalkyl group, wherein each group is optionally substituted by one or two groups selected from the group consisting of the following: : cyano, halo, hydroxy, fluorenyl, 15 as desired, substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, carboxy, optionally Substituted lower alkoxycarbonyl, optionally substituted fluorenyl, optionally substituted aminocarbonyl, optionally substituted heterocycloalkyl, optionally substituted heteroaryl, optionally substituted Sulfhydryl and sulfonate 20 bases as needed. 126. At least one chemical according to claim 125, wherein Z1 is selected from the group consisting of 1-(2Η)-(decyloxycarbonyl)-3,4-dihydroacridin-4-yl; 1-(2Η )-(decyloxy)-5,6-dihydroσ ratio -4-yl; 1-(2H)-(decyloxy)-5,6-dihydropyridin-4-yl ;1_(2H)-(Tertibutoxycarbonyl)-5,6-dihydroacridine-4- 360 200823188, 1-(2Η)-5,6-di sputum 77-7-based , 1-(ethyl aryl)-4,5-diaza methane ° sit-2-based; 1-(dimethylaminoindolyl)-1,.2,3,6-tetrapyridinium-4 -yl; 1-(decyloxyindenyl)-4,5-dihydroimidazol-2-yl; 1-cyano-4,5-dihydro-1H-imidazol-2-yl, 1-indolyl-1 , 2,3,6-tetra-purine 12-1,4-yl, 2-(ethenylamino-5-yl)0-pyridyl-1-yl, 2-(3⁄4-ylmethyl)morphinyl, 2-(via fluorenyl) 11-pyridin-1-yl; 2-(decyloxy)pyrrolidin-1-yl; 2H-pyrrole-1(5H)-yl; 2-hydroxymorpholinyl ; 2-mercapto-4-(t-butoxycarbonyl)-piped-l-yl, 2-oxo-5-carbyl-Benbityl, 2-oxanyl, 2-oxygen 2-hydroxypyridinyl; 3-(3,3-dimethylureido)pyrrolidin-1-yl; 10 3-(aminoindenyl)-σ ratio - , 3-(indolyl)-°Biro σ-based; 3-(Dimethylamine-based pyrrolidin-1-yl; 3-(didecylaminoindolyl)-pyrrole-s- 1-yl, 3-(technical 曱 比 比 σ σ -1- -1-yl, 3-(曱 基 绿 绿 绿 _)-pyrrolidinyl; 3-(methylsulfonyl)pyrrolidine-1- 3-(indole-ethenyl-indole-methyl)-aminomercapto)-pyrrolidin-1-yl; 3-(pyridin-4-yl)pyrrolidine-1-15yl; 3-( Third butoxycarbonylamino)-pyridridinyl; 3-(trifluoromethyl)pyrrolidin-1-yl; 3,3-difluoropyrrolidinyl; 3-ethylhydrazinopropylpyrrolidinyl , 3 -Aminopyrrolidine, l-decyl-1 -yl, 3 - gas enthalpy ratio -1 -yl, 3 -pyridylpyrrole-1-yl; 3-meridyl- 1-yl; 3-methoxyoxymethyl valoxolidine-1 -yl, 3-mercaptoamino-indolyl, 3-mercaptoin-1 -yl, 4-(ethyl 20 Base)-piperidin-1-yl; 4-(aminomercapto)piperidin-1-yl; 4-(ethoxycarbonyl)-nivine pi--1-yl, 4-(ethyllacyl fluorenyl) )- ϋ bottom bite, 4-(decyloxy fluorenyl)-pyrylene-1-yl; 4-(methylsulfonyl)cyclohex-1-enyl; 4-(Ν,Ν-二曱Amino-based fluorenyl)-Pei^ well-1_yl, 4-(di-butyl butyl-based green amino group )-Brigade 17-1,4-yl; 4-(Tertibutoxycarbonylaminomethyl)-piperidin-1-yl; 4,5-diin-1Η- 361 200823188 Imidazol-2-yl; 4 , 5-dioxazol-2-yl; 4-hydroxy-4-phenylpiperidin-1-yl; 4-ethylidene-Big bite-yl, 4-carbylmethyl-Brigade-Base ;4-light base-based bite group; 4-methylamino fluorenyl-tourism base, 4-methyl brigade 11 well-1-yl; 4-mercaptopiperidinyl; 4-oxycyclohexyl-1 -alkenyl; 5,6-dihydropyridine-1(2Η)-yl; hydrazinyl; cyclohex-1-enyl; cyclohexyl; cyclopent-1-enyl; cyclopentyl; morphine; Brigade σ well base; brigade bite base; σ ratio σ σ base; and 嗟 淋 基 base. 127. A chemical according to any one of claims 101 to 126, wherein R1 is selected from the group consisting of hydrogen and optionally substituted lower alkyl. 10 15 128. At least one of the chemicals of claim 127, wherein R1 is selected from the group consisting of hydrogen and low carbon. 129. At least one chemical as claimed in claim 128, wherein R1 is selected from the group consisting of hydrogen and methyl. 130. At least one chemical as claimed in claim 129, wherein R1 is hydrogen. 131. At least one chemical of claim 1, wherein the compound of formula X is selected from the group consisting of a compound of formula VII 其中 R1及R4係獨立地選自氫、氰基、鹵基、羥基、疊 氮基、硝基、磺醯基、亞磺醯基、硫烷基、視需要經取 代之烷氧基、視需要經取代之醯氧基、視需要經取代之 362 20 200823188 胺基幾，氧基、視需要經取代之芳基氧基、視需要經取 代之雜絲氧基、視需魏取代之雜環絲氧基、視需 要經取代之烧氧錢基、視f要經取代之縣、視需要 ，取，之縣、視需要魄代之絲、視需要經取代之 芳基氧基、視需要經取代之芳基、視需要經取代之雜芳 基、視而要經取代之雜環烷基、視需要經取代之胺基、 視需要經取代之醯基、視需要經取代之胺基縣及視需 要經取代之carbaminodoyl ; Z1係選自氫、氰基、視需要經取代之絲、視需要 經取代之醯基、視需要經取代之烷氧基羰基、視需要經 取代之胺基、視需要經取代之胺基羰基、視需要經取代 之甲脒基、視需要經取代之烷氧基、視需要經取代之芳 基氧基、視需要經取代之雜芳基氧基、視需要經取代之 雜環烷基氧基、視需要經取代之烯基、視需要經取代之 炔基、磺醯基、亞磺醯基及硫烷基； Z2係選自氫、視需要經取代之甲脒基、羧基、視需 要經取代之烷氧基羰基、視需要經取代之醯基、視需要 經取代之烯基、視需要經取代之烧基、視需要經取代之 雜環烷基、視需要經取代之雜芳基及視需要經取代之胺 基幾基； Z3係選自視需要經取代之烷基；及 R係選自氫及視需要經取代之炫基。 132·至少一種如申請專利範圍第131項之化學品，其中z2係選 自羧基、視需要經取代之烷氧基羰基、視需要經取代之 363 200823188 醯基、視需要經取代之烯基及視需要經取代之户 133·至少一種如申請專利範圍第132項之化學品，其=基^ 自羧基、視需要經取代之哌啶基羰基、视需^麫2係選 吡啶基羰基、視需要經取代之低碳烷基、视需^ =代之 之低碳烯基及低破燒氧基叛基。 ” 、、t取代 134·至少一種如申請專利範圍第133項之化學品，其中z2 ^ 自（2-(N-乙趨基胺基曱基户辰啶-1-基）幾基；係選 旅唆-1-基)獄基；1-經基-2-胺基-乙基；2-((甲基續 甲基)哌啶-1-基羰基；2-(曱基胺基羰基）乙埽基；f f 土） 10 15 冬基曱基）-2H-三唑冬基甲基；胺基曱基；声其/比&quot;疋 文，甲羞 基幾基；σ比咬-2-基魏基；吼唆-3-基叛基；及。比一 疋-4、基 基。 135·至少一種如申請專利範圍第131至134項中任— 〇 、之化學 品，其中R3係選自氫及視需要經取代之低碳燒基。 136·至少一種如申請專利範圍第135項之化學品，Α由^3〆 ，、r坟係選 自氫及低碳烷基。 其中R3係選 其中R3為 137·至少一種如申請專利範圍第136項之化學品 自氫及甲基。 138·至少一種如申請專利範圍第137項之化學品 氫。 139·至少一種如申請專利範圍第131項之化學品，其中Z2為 -C(0)NR2R5，其中R2係選自視需要經取代之烷基及視二 要經取代之環烷基；而R5係選自氫及視需要經取代之: 基。 70 364 20 200823188 140·至少一種如申請專利範圍第131至139項中任一項之化學 品，其中R4係選自氫、氰基、鹵基、疊氮基、視需要經 取代之胺基羰基及視需要經取代之烷基。 141·至少一種如申請專利範圍第14〇項之化學品，其中R4係選 5 自氫、氰基、氯、溴、氟、疊氮基、視需要經取代之烧 基胺基羰基及視需要經取代之甲基。 142·至少一種如申請專利範圍第ι41項之化學品，其中R4係選 自氫、氰基、氯、溴、疊氮基、吼啶_3_基曱基胺基羰基、 胺基甲基及羥基甲基。 ίο 143·至少一種如申請專利範圍第142項之化學品，其中R4為 氫。 ’ 144·至少一種如申請專利範圍第139至143項中任一項之化學 品，其中R5係選自氫及低碳烷基。 145·至少一種如申請專利範圍第144項之化學品，其中R5係琴 15 自氫及甲基。 其中R5為 146·至少一種如申請專利範圍第145項之化學品 氫。 147·至少一種如申請專利範圍第139至146項中任一項之化取 品，其中R2係選自視需要經取代之曱基、視需要緩取予 之乙基、視需要經取代之丙基、視需要經取代之丁代 視需要經取代之戊基、視需要經取代之己基、說霉二、 取代之環丙基、視需要經取代之環戊基及視需要 之壞己基’其中各視需要經取代之基團係視需要趣〜代 二或三個由下列選出之基團取代：視需要經取 、 1弋之芳 365 200823188 基、視需要經取代之雜芳基、視需要經取代之雜環烷基、 視需要經取代之環烷基、視需要經取代之胺基羰基、視 而要座取代之胺基、羥基、羧基、視需要經取代之烷氧 基幾基及視需要經取代之烷氧基。 5 14 8 ·至少一種如申請專利範圍第14 7項之化學品，其中R2係選 自甲基及乙基，其中該曱基及乙基基團係視需要經一或 二個由下列選出之基團取代··視需要經取代之芳基、視 需要經取代之雜芳基、視需要經取代之雜環烷基、視需 要經取代之環烷基、視需要經取代之胺基羰基、視需要 〇 經取代之胺基、羥基、羧基、視需要經取代之烷氧基羰 基及視需要經取代之烷氧基。 149·至少一種如申請專利範圍第148項之化學品，其中R2係選 白 (H2-胺基乙基•基）曱基；（1_(曱基磺醯基)哌 5 咬I基）甲基；（1-乙醯基哌啶各基）甲基；（1_乙醯基吼 u各咬I基）甲基；（1Η_咪唑_2_基）曱基；（m_吡唑_3_基） 甲基；（1-甲基-1Η-吡唑冬基）曱基；（1-曱基_111_吡唑-5_ 基）甲基；（2-(胺基羰基）乙基胺基)羰基曱基；（2_(胺基曱 基)吼唆-3-基）甲基；(2-(羧基）乙基胺基)羰基甲基；(2-(二 甲基胺基）乙基胺基)羰基曱基；（2_(羥基）乙基胺基)羰基 甲基；（2-(甲基胺基）乙基胺基）幾基甲基；（2_(Ν_曱基 Ν-(第二丁氧基裁基)_胺基）乙基胺基)幾基甲基；(2_氧基 哌啶-3-基）甲基；（3_(二曱基胺基）丙基胺基)羰基甲基； (3-(羥基）乙基胺基)羰基甲基；（3_(第三丁氧基羰基胺基） 366 200823188 丙基胺基）羰基甲基；（4-(胺基甲基）吼啶-2-基）曱基； (5-(胺基甲基户比啶-2-基）甲基；（6-((1,3-二氧基異吲哚啉 -2-基）甲基)0比17定-2-基）甲基，(6-(2-胺基乙基胺基)1[1比0定-2-基）曱基；（6-(3-胺基丙基胺基户比啶-2-基）甲基；（6-(胺基 5 曱基)吼啶-2-基）曱基；（6-(羥基曱基户比啶-2-基）甲基；（6- 溴吼啶-2-基）曱基；（甲基磺醯胺基)羰基曱基；（吨啶-2-基）乙基胺基；1-(2-(第三丁氧基幾基胺基）乙基)-1Η-σΛσ坐 -3-基曱基；1-(2-(第三丁氧基羰基胺基）乙基)-1Η-吼唑-5-基甲基，1 -(胺基綠基）-2-(胺基）-乙-1 -基，1 -(胺基緣 1〇 基)-3-(胺基)-丙基，1-(胺基搂基)-4-(胺基)-丁基，1-(胺 基幾基）-4-(苯曱基氧基獄基胺基）-戊基，1-(胺基幾 基)-5-(胺基)-戊基，1-(胺基被基）乙-1-基，1-(竣基)-2-(胺 , 基）-乙-1-基；1-(二曱基胺基羰基）-2-(胺基）-乙-1-基； 1- (羥基)-2-(胺基羰基曱基胺基）乙-1-基；1-(羥基)-2-(乙 15 氧基羰基曱基胺基）乙-1-基；1-(羥基)-2-(吼啶-2-基甲基 胺基）乙-1-基，1_(曱乳基綠基)-2-(胺基)-乙-1-基，1-(曱 氧基羰基)-2-(第三丁氧基羰基胺基)-乙-1_基；1-(曱氧基 羰基）乙-1-基；1-(甲基胺基羰基）-2·(胺基）-乙-1-基（2 occ) ; 1-(甲基胺基羰基）乙-1-基；1-胺基羰基-2-羥基-乙 2〇 -1-基，1-曱乳基綠基-2-輕基-乙-1-基，2-(2-胺基乙氧基） 乙基，2-(2-胺基乙基)-ϋ比咬-6-基曱基，2-(2-胺基乙基胺 基）乙基，2-(3-氣苯基）乙基，2-(3-曱氧基獄基）乙基， 2- (6-(胺基曱基)ϋ比σ定-2-基）乙基，2-(乙酿基胺基）乙基； 2-(胺基）乙基；2-(胺基羰基)-2-(乙醯基胺基)-乙-1-基； 367 200823188 2_(胺基羰基)_2·(胺基)_乙-1_基；2_(胺基羰基）乙基；2-(胺 基甲基)吼啶-5-基曱基；2-(羧基)-2-(胺基)-乙-1-基；2-(二 甲基胺基）乙基；2-(二甲基胺基羰基)-2-(胺基卜乙-丨―基； 2-(乙氧基羰基）乙基；2-(甲氧基羰基)-2-(乙醯基胺基)_ 乙小基；2_(甲氧基羰基)1(胺基)_乙小基；2_(甲氧基羰 基胺基）乙基；2-(甲基胺基）乙基；2-(甲基胺基羰 基)-2-(乙醯基胺基)-乙-1-基；2-(甲基胺基羰基）_2_(胺 基）-乙-1-基；2-(曱基石黃醯胺基）乙基；2-(曱氧基羰 基)_2_(胺基)-乙-1-基；2_(N_(第三丁氧基羰基)-N-(甲基)_ 胺基）乙基，2-(派η井-1-基）乙基；2十比σ井-2-基）乙基；2十比 啶-2-基）乙基；2-(。比啶-3-基）乙基；2-(第三丁氧基羰基 胺基曱基&gt; 比啶-3-基曱基；2-(第三丁氧基羰基胺基甲基） H6-基曱基；2-(三氟甲基)-吡啶_6_基甲基；2_胺基吼 咬-3-基曱基；2_胺基吡啶-5-基甲基；2-氯吡啶_5_基甲基； 2- 氰基吼啶-5-基甲基；2-羥基-3-胺基-丙-1-基；2-羥基 乙基；2-甲氧基乙-1-基；2-甲氧基吡啶_3_基曱基；2_甲 氧基吼啶-5-基曱基；2-曱基吡啶-3-基甲基；2-甲基吡啶 -5-基甲基；2-甲基吡啶-6-基甲基；3-(2-胺基乙基)環己 基）甲基，3_(4_甲基哌畊_1_基）丙基；3_(胺基)！（曱基胺 基羰基）丙-1-基，· 3-(胺基羰基）丙基；3-(胺基甲基）苯甲 基；3-(胺基曱基)吼啶_2_基曱基；3_(曱氧基羰基）丙基； 3- (甲基胺基幾基）丙基；3-(三氟甲基)_π比tr定_2_基曱基； 3,4_二氟苯甲基；3-胺基曱基吡啶_4_基曱基；3_胺基丙 基；3-胺甲醯基環戊基；3_羧基丙基；3_羥基丙基；3_ 368 200823188 甲氧基丙基；4-(胺基甲基)^比啶-2-基甲基；4-(N，N-二曱 基胺基）吼°定-3-基曱基_ ; 4-(第三丁氧基幾基胺基)-嗎·琳 基甲基；4-胺基丁基；4-胺基甲基吼啶-3-基甲基；4-氰 基苯甲基；4-氟苯曱基；4-曱基胺基吼啶-3-基曱基；4-5 曱基苯曱基；4-嗎啉基吡啶-3-基甲基；4-哌畊基吡啶-3- 基甲基；5_((雙(二甲基胺基）曱基胺基）曱基户比啶冬基甲 基；5-(胺基甲基）吡啶-2-基甲基；5-(胺基甲基)吡啶-3-基曱基，5-(經基曱基)σ比咬-3-基甲基；5-(第三丁氧基幾 基胺基曱基)-吼咬-2-基甲基；5-(三氟甲基)-σ比咬-2-基甲 10 基；5-胺基戊基；5_胺基。比啶—2-基曱基；6-((雙(二甲基 胺基)伸甲基胺基）曱基)吡啶-2-基）曱基；6-(4-乙醯基哌 畊小基)吼啶_3_基曱基）；6_(胺基甲基)。比啶-2_基）曱基； ' 胺基己基；胺基羰基曱基；苯甲基；環丙基甲基；二 曱基胺基羰基甲基；異丙基；異崎唑_5_基曱基；曱氧基 15 #炭基甲基；甲基；曱基胺基羰基甲基；呤唑-2-基曱基； 旅&quot;定·4_基甲基；丙-2-烯-1-基；吡畊-2-基曱基；吡啶-2_ 基甲基；σ比啶-2-基甲基-N-氧化物；吡啶-3-基曱基；吡 咬-3-基曱基_Ν_氧化物；吡啶_4_基甲基；噻吩-2_基曱基； 及噻吩-3-基甲基。 2〇 150·至少一種如申請專利範圍第131至139項中任一項之化 ^其中ζ3係選自視需要經取代之低碳烧基。 151·至少一種如申請專利範圍第150項之化學品，其中Ζ3係 延自視需要經取代之甲基、視需要經取代之乙基及視需 要、經取代之丙基，其中該曱基、乙基及丙基基團係視需 369 200823188 要經一或二個由下列選出之基團取代：羥基、視需要經 _取代之芳基、視需要經取代之靡芳基、視需要經取代之 雜環烷基、視需要經取代之環烷基及視需要經取代之芳 基氧基。 5 152.至少一種如申請專利範圍第151項之化學品，其中Z3係 選自2-(3-曱基苯基）乙基、（四氫呋喃2-基）甲基、1-羥基 環己基甲基、2-(1，3_二氧戊環-2-基）乙基、2-(1Η-咪唑-4-基）乙基、2-(1-曱基-1H-咪唑-4-基）乙基、2-(1-甲基哌啶 -4-基）乙基、2-(2,3-二氣苯基）乙基、2-(2,5_二氣苯基）乙 ίο 基、2-(2,6-二亂苯基）乙基、2-(2-氣苯基）乙基、2-(2-鼠基 苯基）乙基、2-(2-氟苯基）乙基、2-(2-羥基苯基）乙基、2-(2-• 甲氧基苯基）乙基、2-(2-甲基苯基）乙基、2-(2-氧基咪唑 ' 12定-1 -基）乙基、2-(2-乳基旅17定-1 -基）乙基、2-(2-乳基σ比洛 啶-1-基）乙基、2-(3-(三氟曱基）苯基）乙基、2-(3,4-二氟苯 15 基）乙基、2-(3,5-二氟苯基）乙基、2-(3,5-二曱基-1H-吼唑 -1 -基）乙基、2-(3，5-二曱基-1H-°比11 坐-4 -基）乙基、2-(3-胺 曱醯基苯基）乙基、2-(3_羧基苯基）乙基、2-(3-氰基苯基) 乙基、2-(3-氟苯基)-2-(羥基)-乙基、2-(3-氟苯基）乙基、 2-(3 -氣12比0定-2-基）乙基、2-(3 -曱乳基祿基苯基）乙基、2-(3-2〇 曱氧基苯基）乙基、2-(3-曱基苯基）乙基、2-(4-胺基苯基) 乙基、2-(4-鼠苯基）乙基、2-(4-鼠苯基）乙基、2-(4-¾基 苯基）乙基、2-(苯并[d][l，3]二氧環戊烯-5-基）乙基、2-(呋 喃2-基）乙基、2-(羥基)-2-(苯基）乙基、2-(苯基）乙基、2-(口比 啶-2-基）乙基、2-(吡啶-3-基）乙基、2-(噻吩-2-基）乙基、 370 200823188 2 5衣己-1-細基乙基、2_環己基乙基、2-嗎琳基乙基、2-苯氧基·乙基：2-苯基丙小基、3-(1Η-咪唑-1-基）丙-1-基、 3-苯基丙基、苯甲基、氯、異戊基、丙基、σ比咬_2_基曱 基、吼咬-3-基曱基及噻吩_3_基甲基。 5 10 15 153·至少一種如申請專利範圍第ι52項之化學品，其中ζ3係 選自2_0氟苯基）乙基及2-(吼啶-2_基）乙基。 154·至少一種如申請專利範圍第13ι至153項中任一項之化 學品’其中Ζ1係選自氰基、_基、視需要經取代之醯基、 視需要經取代之烯基、視需要經取代之烷氧基羰基、視 需要經取代之烷基、視需要經取代之胺基、視需要經取 代之胺基羰基及視需要經取代之甲脒基。 155·至少一種如申請專利範圍第154項之化學品，其中ζι係 运自基、沐基、烧氧基綠基、烧基、胺基、胺基纟炭美 及甲脒基，其中各基團係視需要經一或二個由下列選出 之基團取代：氰基、鹵基、羥基、甲醯基、視需 代之烧基、視需要經取代之稀基、視需要經取代之^&gt; t 基、敌基、視需要經取代之烧氧基幾基、視需要細取代 之醯基、視需要經取代之胺基羰基、視需要經取代之六 環烷基、視需要經取代之雜芳基、視需要經取代之甲= 基及視需要經取代之磺醯基。 /N 156·至少一種如申請專利範圍第155項之化學品，其中zl 〃 選自（5-氧基-四氫呋喃2-基）甲基胺基；（Ε)-Ν’-氰基&amp; 二甲基甲脒基；（Ζ)-4-(Ν-(2-羥基乙基)-Ν，Ν’-雙（甲气^ ^ 基）曱脒基）；（Z)-丁-2-烯-2-基；1-乙氧基乙七臭· 371 20 200823188 氧基乙細基，2-經基乙-1-基胺基2-曱乳基乙-1基胺基， . 2-甲基丙-1-烯基；3-(曱氧基羰基)-丙-2-烯-2-基;_ 3-(N，N- 二甲基胺基）羰基-丙-1-基胺基；3-胺基羰基-丙-1-基胺 基，3 -經基丙-1 -基胺基，3 -甲乳基-丙-1 -細基，3 -甲乳基 5 丙-1-基胺基；3-甲氧基丙基；3-曱基丁-2-烯-2-基；4-((吡 啶-3-基曱基）胺基羰基）丁基胺基；4-(N,N-二甲基胺基) 爹炭基-丁-1-基胺基，4-(N-曱基胺基）綠基-丁-1-基胺基； 4-胺基羰基-丁-1-基胺基；乙醯基；胺基羰基；曱脒基； 氯；氰基；二曱基胺基；乙氧基羰基；氫；曱氧基羰基； ίο 曱基胺基；N-(2-羥基乙基)-N-(乙醯基)-胺基；N-(2-羥基 乙基)-N-(曱基)-胺基；N-(2-羥基丙-1-基)-N-(曱基)-胺 基；N-(甲基)-胺基羰基；N_(吼啶-2-基曱基)胺基；N-(口比 . 啶-3-基曱基)胺基；N-(吡啶-4-基曱基)胺基；N，N-二甲基 曱脒基；N-氰基甲脒基；N-曱基-N-乙醯基胺基；及丙-1-15 稀基。 157. 至少一種如申請專利範圍第131至156項中任一項之化 $ 學品，其中R1係選自氫及視需要經取代之低碳烷基。 158. 至少一種如申請專利範圍第157項之化學品，其中R1 係選自氫及低碳烷基。 2〇 159.至少一種如申請專利範圍第158項之化學品，其中R1 係選自氫及曱基。 160. 至少一種如申請專利範圍第159項之化學品，其中R1 為氫。 161. —種醫藥上可接受之組合物，其係包含醫藥上可接受之 372 200823188 載劑及至少一種如申請專利範圍第i至16〇項中任一項 • 之化學品。 、 、 162·如申請專利範圍第161項之醫藥組合物，其中該組合物 係調配成選自錠劑、膠囊、散劑、液體、懸浮液、栓劑 5 及氣霧劑之型式。 163· —種包裝醫藥組合物，其係包含如申請專利範圍第 或162項之醫藥組合物及供使用組合物治療患有與平滑 肌肌凝蛋白或非肌肉肌凝蛋白有關疾病之病患之說明。 164·如申請專利範圍第163項之包裝醫藥組合物，其中該與 1〇 平滑肌肌凝蛋白有關之疾病係選自高血壓、氣喘、慢^ 阻塞性肺疾病（copd)氣喘、支氣管收縮性疾病、青光眼 # 及其他眼部適應症、尿失禁及其他膀胱功能失調、腸激 11 =症、早產、食迢蠕動異常、中風、蛛膜下腔出血、經 韵痙·手、勃起功能障礙及其他與平滑肌肌凝蛋白及/或非 15 肌肉肌凝蛋白有關之急性或慢性疾病和症狀。 165·種於哺乳動物中治療或減緩與平滑肌肌凝蛋白或非肌 肉肌凝蛋自有關疾病之方法，該方法包括料有此需要 =哺乳動物一治療上有效量之至少一種如申請專利範圍 第1至160項中任一項之化學品。 2〇 I%·如申請專利範圍第165項之方法，其中該與平滑肌机凝 蛋白有關之疾病係選自高血壓、氣喘、慢性阻塞性肺疾 病（⑶Pd)氣喘、支氣管收縮性疾病、青光眼及其他眼部 適應症、尿失禁及其他膀胱功能失調、腸激躁症、早產、 食逞蠕動異常、中風、蛛膜下腔出血、經前痙攣、勃起 373 200823188 功能障礙及其他與平滑肌肌凝蛋白及/或非肌肉肌凝蛋 白有關之急性或慢性疾病和症狀#。 . 200823188 七、指定代表圖： (一) 本案指定代表圖為：第（無）圖。 (二) 本代表圖之元件符號簡單說明： 無 八、本案若有化學式時，請揭示最能顯示發明特徵的化學式： 15Wherein R1 and R4 are independently selected from the group consisting of hydrogen, cyano, halo, hydroxy, azido, nitro, sulfonyl, sulfinyl, sulfanyl, optionally substituted alkoxy, optionally Substituted methoxy group, optionally substituted 362 20 200823188 Amino group, oxy group, optionally substituted aryloxy group, optionally substituted heterosilyl group, optionally substituted Wei substituted heterocyclic wire Oxygen, as needed, substituted oxygenated money base, county to be replaced by f, if necessary, taken, county, as needed, deuterated silk, as needed, substituted aryloxy, if necessary, replaced Aryl group, optionally substituted heteroaryl group, optionally substituted heterocycloalkyl group, optionally substituted amine group, optionally substituted thiol group, optionally substituted amine group county and A substituted carbaminodoyl; Z1 is selected from the group consisting of hydrogen, cyano, optionally substituted filaments, optionally substituted thiol groups, optionally substituted alkoxycarbonyl groups, optionally substituted amine groups, optionally as needed Substituted aminocarbonyl, optionally substituted formazan, optionally substituted alkane An oxy group, optionally substituted aryloxy group, optionally substituted heteroaryloxy group, optionally substituted heterocycloalkyloxy group, optionally substituted alkenyl group, optionally substituted alkyne a sulfonyl group, a sulfinyl group, a sulfinyl group, and a sulfanyl group; the Z2 group is selected from the group consisting of hydrogen, an optionally substituted formazan group, a carboxyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted thiol group, Alkenyl substituted, optionally substituted alkyl, optionally substituted heterocycloalkyl, optionally substituted heteroaryl, and optionally substituted amino group, if desired; Z3 is selected from the group consisting of A substituted alkyl group is required; and R is selected from the group consisting of hydrogen and optionally substituted thiol groups. 132. At least one chemical according to claim 131, wherein z2 is selected from the group consisting of a carboxyl group, an optionally substituted alkoxycarbonyl group, optionally substituted 363 200823188 fluorenyl, optionally substituted alkenyl group and A household which is substituted as needed 133. At least one chemical as described in claim 132, which is based on a carboxy group, optionally substituted piperidinylcarbonyl group, optionally as a pyridylcarbonyl group, A substituted lower alkyl group, a lower alkenyl group as desired, and a lower calcined oxy group are required. ”, t replace 134· at least one of the chemicals of the scope of claim 133, wherein z2 ^ from (2-(N-ethylhistylamino fluorenyl)-1-yl);唆-1-基) prison base; 1-transyl-2-amino-ethyl; 2-((methyl-methyl)piperidin-1-ylcarbonyl; 2-(decylaminocarbonyl) Ethyl hydrazide; ff soil) 10 15 mercaptopurine)-2H-triazole-m-methyl; amine thiol; acoustic/ratio&quot;疋文,甲羞基基基;σ ratio bite-2-魏 基 基 ; ; 及 及 ; ; ; ; 135 135 135 135 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少 至少Hydrogen and, if desired, a substituted low carbon alkyl group. 136. At least one chemical as claimed in claim 135, which is selected from the group consisting of hydrogen and a lower alkyl group. Wherein R3 is 137. at least one of the chemicals as claimed in claim 136, from hydrogen and methyl. 138. At least one chemical such as hydrogen in the scope of claim 137. 139. at least one of claims 131 Chemicals Z2 is -C(0)NR2R5, wherein R2 is selected from an optionally substituted alkyl group and a cycloalkyl group to be substituted; and R5 is selected from hydrogen and optionally substituted: a group. 70 364 20 The chemical according to any one of claims 131 to 139, wherein R4 is selected from the group consisting of hydrogen, cyano, halo, azide, optionally substituted aminocarbonyl, and optionally Substituted alkyl. 141. At least one chemical as claimed in claim 14 wherein R4 is selected from the group consisting of hydrogen, cyano, chloro, bromo, fluoro, azide, optionally substituted alkyl. Aminocarbonyl and optionally substituted methyl. 142. At least one chemical according to claim 41, wherein R4 is selected from the group consisting of hydrogen, cyano, chloro, bromo, azide, acridine _3_ a fluorenylaminocarbonyl group, an aminomethyl group, and a hydroxymethyl group. ίο 143. A chemical according to claim 142, wherein R4 is hydrogen. '144. At least one of claims 139 to 143 A chemical according to any one of the preceding claims, wherein R5 is selected from the group consisting of hydrogen and lower alkyl. 145. at least one For example, the chemical of the scope of claim 144, wherein R5 is a piano 15 from hydrogen and methyl. wherein R5 is 146. at least one chemical hydrogen as in claim 145. 147. at least one of the patent scope A compound according to any one of items 139 to 146, wherein R2 is selected from the group consisting of an optionally substituted thiol group, an ethyl group which is optionally taken up as needed, a propyl group which is optionally substituted, and a substituted butyl group as needed Substituted pentyl groups, optionally substituted hexyl groups, mildew, substituted cyclopropyl groups, optionally substituted cyclopentyl groups, and optionally hexyl groups, wherein each of the groups is substituted as desired If necessary, replace it with two or three groups selected by the following: as needed, 1 弋 芳 365 200823188, optionally substituted heteroaryl, optionally substituted heterocycloalkyl, A substituted cycloalkyl group, an optionally substituted aminocarbonyl group, an optionally substituted amino group, a hydroxyl group, a carboxyl group, an optionally substituted alkoxy group, and an optionally substituted alkoxy group are required. 5 14 8 · At least one chemical as claimed in claim 14 wherein R 2 is selected from the group consisting of methyl and ethyl, wherein the thiol and ethyl groups are optionally selected by one or two Substituent group substituted aryl group, optionally substituted heteroaryl group, optionally substituted heterocycloalkyl group, optionally substituted cycloalkyl group, optionally substituted aminocarbonyl group, An amine group, a hydroxyl group, a carboxyl group, an optionally substituted alkoxycarbonyl group, and an optionally substituted alkoxy group, if necessary. 149. At least one chemical as claimed in claim 148, wherein R2 is selected from the group consisting of (H2-aminoethyl) sulfhydryl; (1_(nonylsulfonyl)piperidin 5 bit I) methyl (1-ethylsulfonylpiperidine)methyl; (1_ethylhydrazine 吼u each bit I) methyl; (1Η_imidazole_2_yl) fluorenyl; (m_pyrazole_3 _ group) methyl; (1-methyl-1 Η-pyrazolyl) fluorenyl; (1-fluorenyl-111-pyrazole-5-yl)methyl; (2-(aminocarbonyl)ethylamine (2-(dimethylamino) carbonyl) (amino) carbonyl fluorenyl; (2-(hydroxy)ethylamino)carbonylmethyl; (2-(methylamino)ethylamino)methylidene; (2_(Ν_曱基Ν- (2nd-butoxyl group)-amino)ethylamino)methylidene; (2-oxypiperidin-3-yl)methyl; (3-(didecylamino)propylamine (carbonyl) methyl; (3-(hydroxy)ethylamino)carbonylmethyl; (3_(t-butoxycarbonylamino) 366 200823188 propylamino)carbonylmethyl; (4-(amino) Methyl) acridine-2-yl) fluorenyl (5-(Aminomethyl-bipyridin-2-yl)methyl; (6-((1,3-dioxyisoindol-2-yl)methyl)0 to 17 -2- Methyl, (6-(2-aminoethylamino) 1 [1-0-but-2-yl)indenyl; (6-(3-aminopropylamine-based pyridine-2- (6-(amino-5 fluorenyl)acridin-2-yl)indenyl; (6-(hydroxyindolylpyridin-2-yl)methyl; (6-bromoacridine- 2-yl) fluorenyl; (methylsulfonylamino)carbonyl fluorenyl; (ton-2-yl)ethylamino; 1-(2-(t-butoxyamino)ethyl -1Η-σΛσ sit-3-ylindenyl; 1-(2-(t-butoxycarbonylamino)ethyl)-1Η-indazol-5-ylmethyl, 1- (amino)-based -2-(amino)-ethyl-1-yl, 1-(amino-l-mercapto)-3-(amino)-propyl, 1-(aminomercapto)-4-(amino) )-butyl, 1-(aminomethyl)-4-(phenylhydrazolylphenyl)-pentyl, 1-(amino)-5-(amino)-pentyl, 1-(amino-based) ethyl-1-yl, 1-(indenyl)-2-(amine, yl)-eth-1-yl; 1-(didecylaminocarbonyl)-2-(amine ))-ethyl-1-yl; 1-(hydroxy)-2-(aminocarbonylcarbonylamino)ethyl-1-yl; 1-(hydroxy)-2-(ethyl 15 oxy Carbonyl decylamino) ethyl-1-yl; 1-(hydroxy)-2-(acridin-2-ylmethylamino)ethyl-1-yl, 1-(indolyl-based)-2-( Amino)-ethyl-1-yl, 1-(decyloxycarbonyl)-2-(t-butoxycarbonylamino)-ethyl-1-yl; 1-(decyloxycarbonyl)ethyl-1- 1-(methylaminocarbonyl)-2.(amino)-eth-1-yl(2 occ); 1-(methylaminocarbonyl)eth-1-yl; 1-aminocarbonyl- 2-hydroxy-ethyl-2-indol-1-yl, 1-indolyl-lacyl-green-2-pyryl-eth-1-yl, 2-(2-aminoethoxy)ethyl, 2-(2- Aminoethyl)-indole ratio bit-6-ylindenyl, 2-(2-aminoethylamino)ethyl, 2-(3-phenylphenyl)ethyl, 2-(3-oxime oxygen Ethyl, 2-(6-(aminomercapto)pyrene-pyridyl-2-yl)ethyl, 2-(ethionylamino)ethyl; 2-(amino)ethyl ; 2-(aminocarbonyl)-2-(ethinylamino)-eth-1-yl; 367 200823188 2-(aminocarbonyl)_2·(amino)-ethyl-1-yl; 2-(amino Carbonyl)ethyl; 2-(aminomethyl)acridin-5-ylindenyl; 2-(carboxy)-2-(amino)-eth-1-yl; 2-(dimethylamino) Ethyl; 2-(dimethylaminocarbonyl)-2-(amino-ethylidene-yl); 2-(ethoxycarbonyl)ethyl 2-(methoxycarbonyl)-2-(ethionylamino)-ethylidene; 2-(methoxycarbonyl)1(amino)-ethylidene; 2-(methoxycarbonylamino)ethyl 2-(methylamino)ethyl; 2-(methylaminocarbonyl)-2-(ethionylamino)-eth-1-yl; 2-(methylaminocarbonyl)_2_( Amino)-ethyl-1-yl; 2-(indolylxanthine)ethyl; 2-(decyloxycarbonyl)_2-(amino)-eth-1-yl; 2_(N_(third Oxycarbonyl)-N-(methyl)-amino)ethyl, 2-(pyryn-1-yl)ethyl; 2 deg σ well-2-yl)ethyl; 2 decapyridyl- 2-yl)ethyl; 2-(. Bispin-3-yl)ethyl; 2-(t-butoxycarbonylaminoindenyl)pyridin-3-ylindenyl; 2-(t-butoxycarbonylaminomethyl)H6- 2-mercapto group; 2-(trifluoromethyl)-pyridine-6-ylmethyl; 2-aminoglycine-3-ylindenyl; 2-aminopyridine-5-ylmethyl; 2-chloropyridine _5_ylmethyl; 2-cyanoacridin-5-ylmethyl; 2-hydroxy-3-amino-propan-1-yl; 2-hydroxyethyl; 2-methoxyethyl-1- 2-methoxypyridyl-3-ylhydrazino; 2-methoxyfluoridin-5-ylindenyl; 2-mercaptopyridin-3-ylmethyl; 2-methylpyridin-5-yl Methyl; 2-methylpyridin-6-ylmethyl; 3-(2-aminoethyl)cyclohexyl)methyl, 3-(4-methylpiperidine-1-yl)propyl; 3-(amine base)! (fluorenylaminocarbonyl)propan-1-yl, 3-(aminocarbonyl)propyl; 3-(aminomethyl)benzyl; 3-(aminoindenyl)acridin-2-yl Mercapto; 3_(decyloxycarbonyl)propyl; 3-(methylamino)propyl; 3-(trifluoromethyl)_π ratio tr~_2_ylindenyl; 3,4_2 Fluorobenzyl; 3-aminomercaptopyridine_4_ylindenyl; 3-aminopropyl; 3-amineindolylcyclopentyl; 3-carboxypropyl; 3-hydroxypropyl; 3_368 200823188 methoxypropyl; 4-(aminomethyl)^pyridin-2-ylmethyl; 4-(N,N-didecylamino)pyrene-3-ylindenyl _ ; 4 -(t-butoxymethylamino)-?-linylmethyl; 4-aminobutyl; 4-aminomethyl acridine-3-ylmethyl; 4-cyanobenzyl; 4-fluorophenylindenyl; 4-mercaptoaminopyridin-3-ylindenyl; 4-5 mercaptobenzoyl; 4-morpholinylpyridin-3-ylmethyl; 4-piperidinylpyridine -3-ylmethyl; 5-((bis(dimethylamino)decylamino)indolylpyridinylmethyl; 5-(aminomethyl)pyridin-2-ylmethyl; 5 -(aminomethyl)pyridin-3-ylindenyl, 5-(transmethyl fluorenyl) σ ratio -3-ylmethyl; 5-(t-butoxyaminoamino)- Bite-2-ylmethyl; 5-(trifluoromethyl)-σ ratio -2-ylmethyl 10 yl; 5-aminopentyl; 5-amino. Bipyridyl 2-ylindenyl; -((bis(dimethylamino)methylamino)indolyl)pyridin-2-yl)indolyl; 6-(4-ethylsulfonylpiperidine) acridine_3_ylindenyl ); 6_(aminomethyl). Bipyridin-2-yl) fluorenyl; 'aminohexyl; amine carbonyl fluorenyl; benzyl; cyclopropylmethyl; dimethylaminocarbonylcarbonyl; isopropyl; isoxazol _5_ Alkyl fluorenyl group; anthranyloxy group 15#carbylmethyl group; methyl group; mercaptoaminocarbonylcarbonylmethyl; oxazol-2-ylindenyl; british&quot;dine·4_ylmethyl; prop-2-ene -1-yl; pyridin-2-ylindenyl; pyridine-2-ylmethyl; σ-pyridin-2-ylmethyl-N-oxide; pyridin-3-ylindenyl; pyridyl-3-yl Indenyl_Ν_oxide; pyridine-4-ylmethyl; thiophene-2-ylindenyl; and thiophen-3-ylmethyl. 2〇 150· At least one of the methods of any one of claims 131 to 139 wherein ζ3 is selected from a low-carbon alkyl group which is optionally substituted. 151. At least one chemical as claimed in claim 150, wherein the oxime 3 is extended from a methyl group as desired, an optionally substituted ethyl group, and optionally a substituted propyl group, wherein the sulfhydryl group, Ethyl and propyl groups are required by 369 200823188 to be substituted by one or two groups selected from the group consisting of hydroxy, optionally substituted aryl, optionally substituted aryl, optionally substituted A heterocycloalkyl group, optionally substituted cycloalkyl, and optionally substituted aryloxy. 5 152. At least one chemical according to claim 151, wherein Z3 is selected from the group consisting of 2-(3-mercaptophenyl)ethyl, (tetrahydrofuran-2-yl)methyl, 1-hydroxycyclohexylmethyl , 2-(1,3-dioxolan-2-yl)ethyl, 2-(1Η-imidazol-4-yl)ethyl, 2-(1-indolyl-1H-imidazol-4-yl) Ethyl, 2-(1-methylpiperidin-4-yl)ethyl, 2-(2,3-diphenyl)ethyl, 2-(2,5-diphenyl)ethyl , 2-(2,6-disorganophenyl)ethyl, 2-(2-phenylphenyl)ethyl, 2-(2-m-phenylphenyl)ethyl, 2-(2-fluorophenyl) Ethyl, 2-(2-hydroxyphenyl)ethyl, 2-(2-•methoxyphenyl)ethyl, 2-(2-methylphenyl)ethyl, 2-(2-oxyl Imidazole '12-den-1-yl)ethyl, 2-(2-lacyl-based 17-decyl-1-yl)ethyl, 2-(2-lacyl-s-pyridin-1-yl)ethyl, 2 -(3-(Trifluoromethyl)phenyl)ethyl, 2-(3,4-difluorophenyl15-yl)ethyl, 2-(3,5-difluorophenyl)ethyl, 2-( 3,5-dimercapto-1H-indazole-1 -yl)ethyl, 2-(3,5-dimercapto-1H-° ratio 11 s--4-yl)ethyl, 2-(3- Amidinophenyl)ethyl, 2-(3-carboxyphenyl)ethyl, 2-(3-cyanobenzene Ethyl, 2-(3-fluorophenyl)-2-(hydroxy)-ethyl, 2-(3-fluorophenyl)ethyl, 2-(3- gas 12 to 0-but-2-yl) Ethyl, 2-(3-hydranyllacylphenyl)ethyl, 2-(3-2 decyloxyphenyl)ethyl, 2-(3-indolylphenyl)ethyl, 2- (4-Aminophenyl)ethyl, 2-(4-murophenyl)ethyl, 2-(4-murophenyl)ethyl, 2-(4--3-4-phenyl)ethyl, 2- (Benzo[d][l,3]dioxol-5-yl)ethyl, 2-(furan-2-yl)ethyl, 2-(hydroxy)-2-(phenyl)ethyl, 2-(phenyl)ethyl, 2-(oryridin-2-yl)ethyl, 2-(pyridin-3-yl)ethyl, 2-(thiophen-2-yl)ethyl, 370 200823188 2 5 hexyl-1-pyridylethyl, 2-cyclohexylethyl, 2-morphinylethyl, 2-phenoxyethyl: 2-phenylpropanyl, 3-(1Η-imidazole- 1-yl)propan-1-yl, 3-phenylpropyl, benzyl, chloro, isopentyl, propyl, σ ratio _2 yl thiol, guan-3-yl fluorenyl and thiophene _3_ylmethyl. 5 10 15 153. At least one chemical as claimed in claim 051, wherein ζ3 is selected from the group consisting of 2_0 fluorophenyl)ethyl and 2-(acridin-2-yl)ethyl. 154. A chemical according to any one of claims 13 to 153, wherein Ζ1 is selected from the group consisting of cyano, yl, optionally substituted thiol, optionally substituted alkenyl, optionally Substituted alkoxycarbonyl, optionally substituted alkyl, optionally substituted amine, optionally substituted aminocarbonyl, and optionally substituted formazan. 155. At least one chemical as claimed in claim 154, wherein ζι is transported from a base, a thiol group, an alkoxy green group, an alkyl group, an amine group, an amine group, and a carbaryl group, wherein each group The group is replaced by one or two groups selected by the following groups: cyano group, halogen group, hydroxyl group, methyl group, on-demand base, optionally substituted base, optionally substituted &gt; t group, dibasic group, optionally substituted alkoxy group, optionally substituted fluorenyl group, optionally substituted aminocarbonyl group, optionally substituted hexacycloalkyl group, optionally substituted Heteroaryl, optionally substituted methyl group and optionally substituted sulfonyl group. /N 156. At least one chemical as claimed in claim 155, wherein zl 〃 is selected from (5-oxy-tetrahydrofuran-2-yl)methylamino; (Ε)-Ν'-cyano &amp; Methyl formazan; (Ζ)-4-(Ν-(2-hydroxyethyl)-fluorene, Ν'-bis(methylhethane^) fluorenyl); (Z)-but-2-ene -2-yl; 1-ethoxyethyl seven odor · 371 20 200823188 oxyethyl, 2-ethylidene-1-ylamino 2-mercaptoethyl-1-ylamino, . 2-A 3-propen-1-enyl; 3-(decyloxycarbonyl)-prop-2-en-2-yl; 3-(N,N-dimethylamino)carbonyl-propan-1-ylamino 3-aminocarbonyl-propan-1-ylamino, 3-propenyl-1-ylamino, 3-methyllacyl-propan-1-decyl, 3-methyllacyl-5propan-1- 3-aminopropyl; 3-mercaptobut-2-en-2-yl; 4-((pyridin-3-ylindenyl)aminocarbonyl)butylamino; 4-( N,N-dimethylamino) anthracenyl-butan-1-ylamino, 4-(N-decylamino)-chloro-butan-1-ylamino; 4-aminocarbonyl-butyl -1-ylamino; ethyl hydrazide; aminocarbonyl; fluorenyl; chloro; cyano; dimercaptoamine; ethoxycarbonyl; hydrogen; oxiranyloxy; ίο decylamine N-(2-hydroxyethyl)-N-(ethionyl)-amino; N-(2-hydroxyethyl)-N-(indenyl)-amino; N-(2-hydroxypropan- 1-yl)-N-(indenyl)-amino; N-(methyl)-aminocarbonyl; N-(acridin-2-ylindenyl)amine; N-(mouth ratio. pyridine-3- Amino group; N-(pyridin-4-ylindenyl)amino group; N,N-dimethylindenyl; N-cyanomethylindenyl; N-fluorenyl-N-ethylidene Amine group; and propan-1-15 base. 157. At least one of the inventions of any one of claims 131 to 156, wherein R1 is selected from the group consisting of hydrogen and optionally substituted lower alkyl. 158. At least one chemical of claim 157, wherein R1 is selected from the group consisting of hydrogen and lower alkyl. 2〇 159. At least one chemical as claimed in claim 158, wherein R1 is selected from the group consisting of hydrogen and sulfhydryl. 160. At least one chemical as claimed in claim 159, wherein R1 is hydrogen. 161. A pharmaceutically acceptable composition comprising a pharmaceutically acceptable 372 200823188 carrier and at least one chemical as claimed in any one of claims i to 16 above. 162. The pharmaceutical composition of claim 161, wherein the composition is formulated in a form selected from the group consisting of a tablet, a capsule, a powder, a liquid, a suspension, a suppository 5, and an aerosol. 163. A packaged pharmaceutical composition comprising a pharmaceutical composition as claimed in claim 162 or a composition for treating a patient suffering from a disease associated with smooth muscle myosin or non-muscle myosin . 164. The packaged pharmaceutical composition according to claim 163, wherein the disease associated with 1〇 smooth muscle myosin is selected from the group consisting of hypertension, asthma, chronic obstructive pulmonary disease (COPD), asthma, and bronchoconstrictive disease. , glaucoma # and other eye indications, urinary incontinence and other bladder dysfunction, intestinal irritation 11 = syndrome, premature delivery, abnormal convulsions, stroke, subarachnoid hemorrhage, rhyme, hand, erectile dysfunction and others Acute or chronic diseases and conditions associated with smooth muscle myosin and/or non-15 muscle myosin. 165. A method of treating or slowing a disease associated with a smooth muscle myosin or a non-muscle muscle condensed egg in a mammal, the method comprising: requiring the mammal to have at least one therapeutically effective amount as claimed in the patent application A chemical of any of 1 to 160. 2〇I%· The method of claim 165, wherein the disease associated with smooth muscle lectin is selected from the group consisting of hypertension, asthma, chronic obstructive pulmonary disease ((3) Pd) asthma, bronchoconstrictive disease, glaucoma and Other ocular indications, urinary incontinence and other bladder dysfunction, irritable bowel syndrome, premature birth, abnormal convulsions, stroke, subarachnoid hemorrhage, anterior hernia, erection 373 200823188 Dysfunction and other smooth muscle myosin And/or non-muscular myosin-related acute or chronic diseases and symptoms#. 200823188 VII. Designation of Representative Representatives: (1) The representative representative of the case is: (No). (2) A brief description of the symbol of the representative figure: None 8. If there is a chemical formula in this case, please disclose the chemical formula that best shows the characteristics of the invention: 15 式X 4Formula X 4
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