TW201938154A - O-phenoxy and o-benzyloxypropylamino derivatives having activity against pain - Google Patents

O-phenoxy and o-benzyloxypropylamino derivatives having activity against pain Download PDF

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TW201938154A
TW201938154A TW107143316A TW107143316A TW201938154A TW 201938154 A TW201938154 A TW 201938154A TW 107143316 A TW107143316 A TW 107143316A TW 107143316 A TW107143316 A TW 107143316A TW 201938154 A TW201938154 A TW 201938154A
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羅薩萊斯 卡門 阿爾曼薩
布爾納多 瑪麗亞 維吉里
沙爾瑪 蒙妮卡 阿隆索
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西班牙商艾斯提夫製藥股份有限公司
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Abstract

The present invention relates to o-phenoxy and o-benzyloxypropylamino derivatives having pharmacological activity towards the [alpha]2[delta]□ subunit, in particular the [alpha]2[delta]-1 subunit, of the voltage-gated calcium channel, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

Description

具有抗疼痛活性之鄰苯氧基及鄰苄氧基丙胺基衍生物O-phenoxy and o-benzyloxypropylamine derivatives with anti-pain activity

本發明係關於具有針對電壓閘控鈣通道之全部α2 δ子單元之藥理學活性的化合物，且更特定言之，係關於具有此藥理學活性之鄰苯氧基及鄰苄氧基丙胺基衍生物，關於製備此類化合物之方法，關於包含其之醫藥組合物，且關於其在療法中之用途，尤其用於治療疼痛。The present invention relates to compounds having pharmacological activity against all α 2 δ subunits of voltage-gated calcium channels, and more particularly, to o-phenoxy and o-benzyloxypropylamine groups having this pharmacological activity Derivatives, with regard to methods of preparing such compounds, with regard to pharmaceutical compositions comprising them, and with regard to their use in therapy, especially for the treatment of pain.

對疼痛之恰當控制構成重要挑戰，此係因為目前可獲得之治療在許多情況下僅提供適度改善，使許多患者無法得到舒解(Turk, D.C., Wilson, H.D., Cahana, A.; 2011;Lancet ; 377; 2226-2235)。疼痛以約20%之流行率估計值影響大部分群體，且特定言之在慢性疼痛之情況下，其發病率由於群體老化而增加。另外，疼痛與共病(諸如抑鬱症、焦慮症及失眠)明確相關，該等共病導致重要生產力損失及社會經濟負擔(Goldberg, D.S., McGee, S.J.; 2011;BMC Public Health ; 11; 770)。現有疼痛療法包括非類固醇消炎藥(NSAID)、類鴉片促效劑、鈣離子通道阻斷劑及抗抑鬱劑，但其在安全率方面遠非最佳。其全部展示有限之功效及妨礙其尤其在慢性情況中使用之一系列次要作用。Proper control of pain poses an important challenge because the currently available treatments provide only modest improvement in many cases, preventing many patients from being relieved (Turk, DC, Wilson, HD, Cahana, A .; 2011; Lancet 377; 2226-2235). Pain affects most of the population with an estimated prevalence of about 20%, and in particular in the case of chronic pain, its incidence increases due to population aging. In addition, pain is clearly associated with comorbidities, such as depression, anxiety, and insomnia, which cause significant productivity losses and socioeconomic burdens (Goldberg, DS, McGee, SJ; 2011; BMC Public Health ; 11; 770) . Current pain therapies include nonsteroidal anti-inflammatory drugs (NSAIDs), opioid agonists, calcium channel blockers, and antidepressants, but they are far from optimal in terms of safety. All of them exhibit limited efficacy and a series of secondary effects that prevent their use, especially in chronic situations.

電壓閘控鈣通道(VGCC)為身體內許多關鍵功能所需要的。已描述電壓閘控鈣通道之不同亞型(Zamponi等人, Pharmacol Rev. 2015 67:821-70)。VGCC經由不同子單元，即α1 (Cav α1 )、β (Cav β)、α2 δ (Cav α2 δ)及γ (Cav γ)之相互作用進行組裝。α1 子單元為通道複合物之關鍵性多孔形成性單元，負責Ca2+ 傳導及Ca2+ 內流之產生。α2 δ、β及γ子單元為輔助的，但對於通道調控極為重要，此係因為其增加α1 子單元在質膜中之表現以及調節其功能，從而產生不同細胞類型中之功能多樣性。基於其生理及藥理學特性，視通道形成性CaV α子單元而定，VGCC可細分為低電壓活化之T型(Cav 3.1、Cav 3.2及Cav 3.3)及高電壓活化之L型(Cav 1.1至Cav 1.4)、N型(Cav 2.2)、P/Q型(Cav 2.1)及R型(Cav 2.3)。此五個子類別全部見於中樞及周邊神經系統中。經由此等VGCC之活化來對細胞內鈣進行調控必然在以下中起作用：1)神經傳遞質釋放，2)膜退極化及超極化，3)酶活化及失活，及4)基因調控(Perret及Luo, Neurotherapeutics. 2009 6:679-92；Zamponi等人, 2015 同前文獻；Neumaier等人, Prog Neurobiol. 2015 129:1-36.)。大量數據已明確指示VGCC涉及介導各種疾病病況，包括疼痛處理。已開發出與不同鈣通道亞型及子單元相互作用之藥物。目前之治療劑包括靶向L型Cav 1.2鈣通道之藥物(特定言之，1,4-二氫吡啶)，其廣泛用於治療高血壓。T型(Cav 3)通道為乙琥胺之目標，其廣泛用於失神性癲癇症。N型(Cav 2.2)鈣通道之肽阻斷劑齊考諾肽(Ziconotide)已批准用作頑固性疼痛之治療。(Perret及Luo, 2009, 同前文獻；Vink及Alewood, Br J Pharmacol. 2012 167:970-89.)。Voltage-gated calcium channels (VGCC) are required for many key functions in the body. Different subtypes of voltage-gated calcium channels have been described (Zamponi et al., Pharmacol Rev. 2015 67: 821-70). VGCC is assembled through the interaction of different subunits, namely α 1 (Ca v α 1 ), β (Ca v β), α 2 δ (Ca v α 2 δ), and γ (Ca v γ). The α 1 subunit is a key porous forming unit of the channel complex and is responsible for Ca 2+ conduction and Ca 2+ influx generation. The α 2 δ, β, and γ subunits are auxiliary, but are extremely important for channel regulation. This is because it increases the expression of the α 1 subunit in the plasma membrane and regulates its function, resulting in functional diversity in different cell types. . Based on its physiological and pharmacological properties, depending on the channel-forming Ca V α subunit, VGCC can be subdivided into low-voltage activated T-types (Ca v 3.1, Ca v 3.2, and Ca v 3.3) and high-voltage activated L-types (Ca v 1.1 to Ca v 1.4), N type (Ca v 2.2), P / Q type (Ca v 2.1), and R type (Ca v 2.3). These five subcategories are all found in the central and peripheral nervous systems. The regulation of intracellular calcium by such activation of VGCC must play a role in: 1) neurotransmitter release, 2) membrane depolarization and hyperpolarization, 3) enzyme activation and inactivation, and 4) genes Regulation (Perret and Luo, Neurotherapeutics. 2009 6: 679-92; Zamponi et al., 2015 ibid .; Neumaier et al., Prog Neurobiol. 2015 129: 1-36.). Large amounts of data have clearly indicated that VGCC is involved in mediating various disease conditions, including pain management. Drugs have been developed that interact with different calcium channel subtypes and subunits. Current therapeutic agents include drugs that target L-type Ca v 1.2 calcium channels (specifically, 1,4-dihydropyridine), which are widely used to treat hypertension. The T-type (Ca v 3) channel is the target of ethosuccinine, which is widely used in alopecia epilepsy. Ziconotide, a peptide blocker of type N (Ca v 2.2) calcium channels, has been approved for the treatment of refractory pain. (Perret and Luo, 2009, ibid .; Vink and Alewood, Br J Pharmacol. 2012 167: 970-89.).

Cav 1及Cav 2子族含有輔助α2 δ子單元，其為加巴噴諾(gabapentinoid)藥物之治療目標，在某些癲癇及慢性神經病性疼痛中具有價值。迄今為止，存在四種已知α2 δ子單元，其各自由獨特獨特編碼並且均具有剪接變異體。各α2 δ蛋白質由單一信使RNA編碼，且進行轉譯後裂解，且隨後藉由二硫鍵連接。現已選殖編碼α2 δ子單元之四個基因。α2 δ-1最初選殖自骨胳肌肉，且展示相當廣泛之分佈。隨後，α2 δ-2及α2 δ-3選殖自腦部。最近鑑別出之子單元α2 δ-4在很大程度上為非神經元的。人類α2 δ-4蛋白質序列與人類α2 δ-1、α2 δ-2及α2 δ-3子單元分別共有30%、32%及61%一致性。所有α2 δ子單元之基因結構類似。所有α2 δ子單元均展示若干剪接變異體(Davies等人, Trends Pharmacol Sci. 2007 28:220-8.；Dolphin AC, Nat Rev Neurosci. 2012 13:542-55.，Biochim Biophys Acta. 2013 1828:1541-9.)。The Ca v 1 and Ca v 2 subfamilies contain auxiliary α 2 δ subunits, which are therapeutic targets of gabapentinoid drugs and have value in certain epilepsy and chronic neuropathic pain. To date, there are four known α 2 δ subunits, each of which is uniquely and uniquely encoded and each has a splice variant. Each α 2 δ protein is encoded by a single messenger RNA, is post-translationally cleaved, and is subsequently linked by a disulfide bond. Four genes encoding the α 2 δ subunit have been cloned. α 2 δ-1 was originally selected from skeletal muscle and showed a fairly wide distribution. Subsequently, α 2 δ-2 and α 2 δ-3 were selected from the brain. The recently identified subunit α 2 δ-4 is largely non-neuronal. The human α 2 δ-4 protein sequence shares 30%, 32%, and 61% identity with the human α 2 δ-1, α 2 δ-2, and α 2 δ-3 subunits, respectively. The genetic structure of all α 2 δ subunits is similar. All α 2 δ subunits display several splice variants (Davies et al., Trends Pharmacol Sci. 2007 28: 220-8 .; Dolphin AC, Nat Rev Neurosci. 2012 13: 542-55., Biochim Biophys Acta. 2013 1828 : 1541-9.).

Cav α2 δ-1子單元可能在神經病性疼痛發生中起重要作用(Perret及Luo, 2009, 同前文獻；Vink及Alewood, 2012, 同前文獻)。生化數據已指示，在與神經病性疼痛發生相關之神經損傷之後，Cav α2 δ-1而非Cav α2 δ-2子單元在脊椎背角及DRG (背根神經節)中明顯上調。另外，阻斷傷害誘導之DRG Cav α2 δ-1子單元軸索傳輸至中樞突觸前末梢減輕神經受傷之動物中的觸摸痛，表明DRG Cav α2 δ-1子單元升高促進神經病性觸摸痛。The Ca v α 2 δ-1 subunit may play an important role in the occurrence of neuropathic pain (Perret and Luo, 2009, ibid .; Vink and Alewood, 2012, ibid.). Biochemical data have indicated that after neurological injury associated with the occurrence of neuropathic pain, Ca v α 2 δ-1 and not Ca v α 2 δ-2 subunits are significantly upregulated in the spinal dorsal angle and DRG (dorsal root ganglia). . In addition, blocking the injury-induced transmission of DRG Ca v α 2 δ-1 subunit axonal cords to central presynaptic endings alleviates tactile pain in animals with nerve injury, suggesting that the increase in DRG Ca v α 2 δ-1 subunit promotes Neuropathic touch pain.

Cav α2 δ-1子單元(及Cav α2 δ-2，而非Cav α2 δ-3及Cav α2 δ-4子單元)為加巴噴丁之結合位點，該加巴噴丁在患者及動物模型中具有抗觸摸痛/痛覺過敏特性。因為傷害誘導之Cav α2 δ-1表現與神經病性疼痛發生及維持相關，且已知各種鈣通道促進脊椎突觸神經傳遞及DRG神經元可激發性，傷害誘導之Cav α2 δ-1子單元上調可能促進神經病性疼痛之起始及維持，該促進藉由改變VGCC在DRG神經元及其中樞末梢之亞群中的特性及/或分佈，因此調節背角中之可激發性及/或突觸神經可塑性來進行。針對Cav α2 δ-1子單元之鞘內反義寡核苷酸可阻斷神經損傷誘導之Cav α2 δ-1上調且預防觸摸痛發作而保留已建立之觸摸痛。The Ca v α 2 δ-1 subunit (and Ca v α 2 δ-2 instead of Ca v α 2 δ-3 and Ca v α 2 δ-4 subunits) is the binding site of gabapentin, which is in the patient And animal models have anti-touch pain / hyperalgesia properties. Because the damage-induced Ca v α 2 δ-1 expression and neuropathic pain related to and maintained, and the various calcium channels are known to promote spinal synaptic neurotransmission and DRG neuron excitability, injury-induced Ca v α 2 δ- The upregulation of subunit 1 may promote the initiation and maintenance of neuropathic pain. This promotion modifies the characteristics and / or distribution of VGCC in DRG neurons and their subgroups of central peripherals, thus regulating excitability and And / or synaptic nerve plasticity. Intrathecal antisense oligonucleotides targeting the Ca v α 2 δ-1 subunit can block nerve injury-induced Ca v α 2 δ-1 upregulation and prevent the onset of touch pain while retaining established touch pain.

如上文所提及，VGCC之α2 δ子單元形成加巴噴丁及普瑞巴林(pregabalin)之結合位點，該加巴噴丁及普瑞巴林為抑制性神經傳遞質GABA之結構性衍生物，但其不結合於GABAA、GABAB或苯二氮受體或改變動物腦製劑中之GABA調控。加巴噴丁及普瑞巴林與Cav α2 δ子單元之結合引起多種神經傳遞質之鈣依賴性釋放減少，從而導致對神經病性疼痛控制之功效及耐受性。加巴噴諾亦可藉由抑制突觸發生來降低可激發性(Perret及Luo, 2009, 同前文獻；Vink及Alewood, 2012, 同前文獻，Zamponi等人, 2015, 同前文獻)。As mentioned above, the α 2 δ subunit of VGCC forms the binding site of gabapentin and pregabalin, which are structural derivatives of the inhibitory neurotransmitter GABA, but they do not bind GABAA, GABAB or benzodiazepine receptors or alter GABA regulation in animal brain preparations. The combination of gabapentin and pregabalin with the Ca v α 2 δ subunit caused a decrease in calcium-dependent release of various neurotransmitters, resulting in efficacy and tolerance for neuropathic pain control. Gabapentin can also reduce excitability by inhibiting synapse generation (Perret and Luo, 2009, ibid .; Vink and Alewood, 2012, ibid., Zamponi et al. 2015, ibid.).

因此，本申請案係關於具有針對電壓閘控鈣通道之α2 δ-1子單元之活性以治療慢性疼痛的優勢。Therefore, the present application is related to the advantage of having the activity of the α 2 δ-1 subunit for voltage-gated calcium channels to treat chronic pain.

以此方式，本發明係關於作用機制暗示功效及耐受性比加巴噴諾(普瑞巴林及加巴噴丁)更好之化合物(電壓閘控鈣通道之α2 δ子單元(尤其α2 δ-1子單元)的阻斷劑)。In this way, the present invention is a compound (the α 2 δ subunit (especially the α 2 δ- 1 subunit)).

因此，仍需要尋找在疼痛治療中具有替代性或改良之藥理學活性的化合物，其有效且展示所需選擇性，且具有良好「可用藥性」特性，亦即與投藥、分佈、代謝及排泄相關之良好醫藥特性。Therefore, there is still a need to find compounds that have alternative or improved pharmacological activities in pain treatment, which are effective and exhibit the required selectivity, and have good "usable" properties, that is, related to administration, distribution, metabolism, and excretion Good medical properties.

本發明之作者已發現一系列展示針對電壓閘控鈣通道之α2 δ子單元(尤其α2 δ-1子單元)之藥理學活性的化合物，從而產生用於治療疼痛之創新、有效及替代性解決方案。The authors of the present invention have discovered a series of compounds demonstrating the pharmacological activity of the α 2 δ subunit (especially the α 2 δ-1 subunit) of voltage-gated calcium channels, resulting in innovative, effective, and alternative treatments for pain Sexual solution.

鑒於目前可獲得之療法及臨床實踐的現有結果，本發明提供與疼痛治療相關之解決方案。此主要藉由提供本發明化合物來達成，該等化合物結合於電壓閘控鈣通道之α2 δ子單元，尤其α2 δ-1子單元。In view of the current results of currently available therapies and clinical practices, the present invention provides solutions related to pain treatment. This is mainly achieved by providing the compounds of the invention, which are bound to the α 2 δ subunit, especially the α 2 δ-1 subunit of the voltage-gated calcium channel.

在本發明中鑑別由式(I)涵蓋的結構上不同之鄰苯氧基及鄰苄氧基丙胺基衍生物家族，其具有針對電壓閘控鈣通道之α2 δ子單元(尤其α2 δ-1子單元)之藥理學活性，由此藉由提供此類化合物來解決上文鑑別替代性或改良之疼痛治療的問題。In the present invention, the structurally different ortho-phenoxy and o-benzyloxypropylamino derivative families covered by formula (I) are identified, which have α 2 δ subunits (especially α 2 δ) for voltage-gated calcium channels -1 subunit), thereby solving the above problem of identifying alternative or improved pain treatments by providing such compounds.

本發明之主要目標係有關具有結合於電壓閘控鈣通道之α2 δ子單元(尤其α2 δ-1子單元)之活性的化合物，其用於疼痛治療。The main object of the present invention is a compound having an activity of α 2 δ subunit (especially α 2 δ-1 subunit) bound to a voltage-gated calcium channel for use in pain treatment.

由於本發明旨在提供充當電壓閘控鈣通道之α2 δ子單元(尤其α2 δ-1子單元)之配位體的化合物或一系列化學相關化合物，故極佳實施例為該化合物的以Ki 表示之結合對應於以下標度：
Ki (α2 δ-1)較佳＜ 10000 nM，更佳＜ 5000 nM，甚至更佳＜ 500 nM或甚至更佳＜ 100 nM。Since the present invention aims to provide a compound or a series of chemically related compounds that serve as ligands for the α 2 δ subunit (especially α 2 δ-1 subunit) of a voltage-gated calcium channel, an excellent embodiment is that of the compound The combination denoted by K i corresponds to the following scale:
K i (α 2 δ-1) is preferably <10000 nM, more preferably <5000 nM, even more preferably <500 nM or even more preferably <100 nM.

在一個主要態樣中，本發明係有關通式(I)化合物，

其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 、X、Y1 、Y2 及n如下文在詳細說明中所定義。In one main aspect, the invention relates to compounds of general formula (I),

Wherein R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , X, Y 1 , Y 2 and n are as defined in the detailed description below.

本發明之另一個目標涉及用於製備通式(I)化合物之方法。Another object of the present invention relates to a method for preparing a compound of general formula (I).

本發明之再另一個目標涉及中間化合物用於製備通式(I)化合物之用途。Yet another object of the present invention relates to the use of intermediate compounds for the preparation of compounds of general formula (I).

本發明之一個目標亦為一種包含式(I)化合物之醫藥組合物。It is also an object of the present invention to provide a pharmaceutical composition comprising a compound of formula (I).

最後，本發明之一個目標為化合物作為藥劑之用途，且更特定言之，用於治療疼痛及疼痛相關病狀之用途。Finally, an object of the present invention is the use of the compound as a medicament, and more specifically, the use for the treatment of pain and pain-related conditions.

在本發明中鑑別由式(I)涵蓋的結構上不同之鄰苯氧基及鄰苄氧基丙胺基衍生物家族，其具有針對電壓閘控鈣通道之α2 δ子單元(尤其α2 δ-1子單元)之藥理學活性，由此藉由提供此類化合物來解決上文鑑別替代性或改良之疼痛治療的問題。In the present invention, the structurally different ortho-phenoxy and o-benzyloxypropylamino derivative families covered by formula (I) are identified, which have α 2 δ subunits (especially α 2 δ) for voltage-gated calcium channels -1 subunit), thereby solving the above problem of identifying alternative or improved pain treatments by providing such compounds.

本發明之主要目標係有關具有結合於電壓閘控鈣通道之α2 δ子單元(尤其α2 δ-1子單元)之活性的化合物，其用於疼痛治療。The main object of the present invention is a compound having an activity of α 2 δ subunit (especially α 2 δ-1 subunit) bound to a voltage-gated calcium channel for use in pain treatment.

由於本發明旨在提供充當電壓閘控鈣通道之α2 δ子單元(尤其α2 δ-1子單元)之配位體的化合物或一系列化學相關化合物，故極佳實施例為該化合物的以Ki 表示之結合對應於以下標度：
Ki (α2 δ-1)較佳＜ 10000 nM，更佳＜ 5000 nM，甚至更佳＜ 500 nM或甚至更佳＜ 100 nM。Since the present invention aims to provide a compound or a series of chemically related compounds that serve as ligands for the α 2 δ subunit (especially α 2 δ-1 subunit) of a voltage-gated calcium channel, an excellent embodiment is that of the compound The combination denoted by K i corresponds to the following scale:
K i (α 2 δ-1) is preferably <10000 nM, more preferably <5000 nM, even more preferably <500 nM or even more preferably <100 nM.

在其更廣態樣中，本發明係有關通式(I)化合物，

其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
p為0、1、2、3、4或5；
q為0、1、2、3、4或5；
Y1 為-C(R10 R10 ' )-；
其中R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 及R10 ' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
Y2 為-C(R10 '' R10 ''' )-；
其中R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 '' 及R10 ''' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
n為0或1；
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基。In its broader aspect, the invention relates to compounds of general formula (I),

among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
p is 0, 1, 2, 3, 4 or 5;
q is 0, 1, 2, 3, 4 or 5;
Y 1 is -C (R 10 R 10 ' )-;
Wherein R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
Alternatively, R 10 and R 10 ′ may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
Y 2 is -C (R 10 '' R 10 ''')-;
Wherein R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted the substituted C 2-6 alkynyl group;
Alternatively, R 10 '' and R 10 '''may form a substituted or unsubstituted cycloalkyl group with the carbon atom they are attached;
n is 0 or 1;
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
R 5 'is selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non-substituted C 2-6 alkynyl group.

本發明之此等化合物視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。These compounds of the present invention optionally take the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (Preferably, the enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之此等化合物視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽。In another embodiment, the compounds of the present invention optionally take the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or At least two stereoisomers (preferably, enantiomers and / or diastereomers) in the form of a mixture at any mixing ratio, or their corresponding salts.

在一個特定實施例中，若X係選自-[CH2 ]p C(O)N(Rz )[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -，則q為1、2、3、4或5。In a specific embodiment, if X is selected from-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q -, Then q is 1, 2, 3, 4 or 5.

在另一個特定實施例中，若X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -及-[CH2 ]p N(Rz )C(O)[CH2 ]q -，則q為0、1、2、3、4或5；而若X係選自-[CH2 ]p C(O)N(Rz )[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -，則q為1、2、3、4或5。In another specific embodiment, if X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) C (O) [CH 2 ] q- , then q is 0, 1, 2 , 3, 4 or 5; and if X is selected from-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- , then q is 1, 2, 3, 4 or 5.

在一個特定實施例中，排除以下化合物：
。In a particular embodiment, the following compounds are excluded:
.

在另一個實施例中，本發明化合物為通式(I)化合物

其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
p為0、1、2、3、4或5；
q為0、1、2、3、4或5；
Y1 為-C(R10 R10 ' )-；
其中R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 及R10 ' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
Y2 為-C(R10 '' R10 ''' )-；
其中R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 '' 及R10 ''' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
n為0或1；
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
其中R2 中之芳基或雜環基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
其中，
R3 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR31 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR31 R31 ' ；
其中R3 中之環烷基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R31 、-OR31 、-NO2 、-NR31 R31 ' 、-NR31 C(O)R31 ' 、-NR31 S(O)2 R31 ' 、-S(O)2 NR31 R31 ' 、-NR31 C(O)NR31 ' R31 '' 、-SR31 、-S(O)R31 、-S(O)2 R31 、-CN、鹵烷基、鹵烷氧基、-C(O)OR31 、-C(O)NR31 R31 ' 、-OCH2 CH2 OR31 、-NR31 S(O)2 NR31 ' R31 '' 及-C(CH3 )2 OR31 ；
其中R31 、R31 ' 及R31 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR32 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR32 R32 ' ；
其中R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
其中
亦處於R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR51 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR51 R51 ' ；
其中亦處於如R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜芳基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R51 、-OR51 、-NO2 、-NR51 R51 ' 、-NR51 C(O)R51 ' 、-NR51 S(O)2 R51 ' 、-S(O)2 NR51 R51 ' 、-NR51 C(O)NR51 ' R51 '' 、-SR51 、-S(O)R51 、-S(O)2 R51 、-CN、鹵烷基、鹵烷氧基、-C(O)OR51 、-C(O)NR51 R51 ' 、-OCH2 CH2 OR51 、-NR51 S(O)2 NR51 ' R51 '' 及-C(CH3 )2 OR51 ；
及/或經一或多個選自以下之取代基取代：經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜環基；
其中R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
R5 ' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR52 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR52 R52 ' ；
其中R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之烷基、烯基或炔基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、-OR13 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR13 R13 ' ；
其中R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之芳基、雜環基或環烷基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R14 、-OR14 、-NO2 、-NR14 R14 ' 、-NR14 C(O)R14 ' 、-NR14 S(O)2 R14 ' 、-S(O)2 NR14 R14 ' 、-NR14 C(O)NR14 ' R14 '' 、-SR14 、-S(O)R14 、-S(O)2 R14 、-CN、鹵烷基、鹵烷氧基、-C(O)OR14 、-C(O)NR14 R14 ' 、-OCH2 CH2 OR14 、-NR14 S(O)2 NR14 ' R14 '' 及-C(CH3 )2 OR14 ；
其中R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of the invention is a compound of general formula (I)

among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
p is 0, 1, 2, 3, 4 or 5;
q is 0, 1, 2, 3, 4 or 5;
Y 1 is -C (R 10 R 10 ' )-;
Wherein R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
Alternatively, R 10 and R 10 ′ may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
Y 2 is -C (R 10 '' R 10 ''')-;
Wherein R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted the substituted C 2-6 alkynyl group;
Alternatively, R 10 '' and R 10 '''may form a substituted or unsubstituted cycloalkyl group with the carbon atom they are attached;
n is 0 or 1;
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
Wherein, if an aryl or heterocyclic group in R 2 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
among them,
If an alkyl, alkenyl or alkynyl group as defined in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: -OR 31 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 31 R 31 ' ;
Wherein, if the cycloalkyl group in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 31 , -OR 31 , -NO 2 , -NR 31 R 31 ' , -NR 31 C (O) R 31 ' , -NR 31 S (O) 2 R 31 ' , -S (O) 2 NR 31 R 31 ' , -NR 31 C (O) NR 31 ' R 31 '' , -SR 31 , -S (O) R 31 , -S (O) 2 R 31 , -CN, haloalkyl, haloalkoxy, -C (O) OR 31 , -C (O) NR 31 R 31 ' ,- OCH 2 CH 2 OR 31 , -NR 31 S (O) 2 NR 31 ' R 31 '' and -C (CH 3 ) 2 OR 31 ;
Wherein R 31, R 31 'and R 31' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
If an alkyl, alkenyl or alkynyl group as defined in R 3 ′ is substituted, it is substituted with one or more substituents selected from: -OR 32 , halogen, -CN, haloalkyl, haloalkoxy And -NR 32 R 32 ' ;
Wherein R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
Where alkyl, alkenyl or alkynyl in alkylaryl, alkylheteroaryl or alkylcycloalkyl as defined in R 5 is substituted, it is substituted by one or more of the following Group substitution: -OR 51 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 51 R 51 ' ;
Where cycloalkyl, aryl or heteroaryl, which is also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R 5 is substituted, it is selected from one or more selected from The following substituents are substituted: halogen, -R 51 , -OR 51 , -NO 2 , -NR 51 R 51 ' , -NR 51 C (O) R 51 ' , -NR 51 S (O) 2 R 51 ' , -S (O) 2 NR 51 R 51 ' , -NR 51 C (O) NR 51 ' R 51 '' , -SR 51 , -S (O) R 51 , -S (O) 2 R 51 , -CN , Haloalkyl, haloalkoxy, -C (O) OR 51 , -C (O) NR 51 R 51 ' , -OCH 2 CH 2 OR 51 , -NR 51 S (O) 2 NR 51 ' R 51 '' And -C (CH 3 ) 2 OR 51 ;
And / or substituted with one or more substituents selected from: substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted Or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheterocyclyl;
Wherein R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
among them
If an alkyl, alkenyl or alkynyl group as defined in R 5 ' is substituted, it is substituted with one or more substituents selected from -OR 52 , halogen, -CN, haloalkyl, haloalkoxy And -NR 52 R 52 ' ;
Wherein R 52 and R 52 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
Alkyl, alkenyl, or alkynyl that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group if substituted and the substitution is not otherwise defined, is selected from one or more selected from The following substituents are substituted: = O, -OR 13 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 13 R 13 ′ ;
Wherein R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
If an aryl, heterocyclyl, or cycloalkyl group that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group is substituted and the substitution is not otherwise defined, it is substituted by one or more Substituted by a substituent selected from: = O, halogen, -R 14 , -OR 14 , -NO 2 , -NR 14 R 14 ' , -NR 14 C (O) R 14 ' , -NR 14 S (O) 2 R 14 ' , -S (O) 2 NR 14 R 14 ' , -NR 14 C (O) NR 14 ' R 14 '' , -SR 14 , -S (O) R 14 , -S (O) 2 R 14 , -CN, haloalkyl, haloalkoxy, -C (O) OR 14 , -C (O) NR 14 R 14 ' , -OCH 2 CH 2 OR 14 , -NR 14 S (O) 2 NR 14 ' R 14 '' and -C (CH 3 ) 2 OR 14 ;
Wherein R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl, unsubstituted alkenyl group of C 2-6, unsubstituted C 2-6 alkynyl group of , Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic group;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明化合物為通式(I)化合物

其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
若X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -及-[CH2 ]p N(Rz )C(O)[CH2 ]q -，則q為0、1、2、3、4或5；而
若X係選自-[CH2 ]p C(O)N(Rz )[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -，則q為1、2、3、4或5；
p為0、1、2、3、4或5；
Y1 為-C(R10 R10 ' )-；
其中R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 及R10 ' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
Y2 為-C(R10 '' R10 ''' )-；
其中R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 '' 及R10 ''' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
n為0或1；
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
其中R2 中之芳基或雜環基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
其中，
R3 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR31 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR31 R31 ' ；
其中R3 中之環烷基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R31 、-OR31 、-NO2 、-NR31 R31 ' 、-NR31 C(O)R31 ' 、-NR31 S(O)2 R31 ' 、-S(O)2 NR31 R31 ' 、-NR31 C(O)NR31 ' R31 '' 、-SR31 、-S(O)R31 、-S(O)2 R31 、-CN、鹵烷基、鹵烷氧基、-C(O)OR31 、-C(O)NR31 R31 ' 、-OCH2 CH2 OR31 、-NR31 S(O)2 NR31 ' R31 '' 及-C(CH3 )2 OR31 ；
其中R31 、R31 ' 及R31 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR32 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR32 R32 ' ；
其中R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
其中
亦處於R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR51 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR51 R51 ' ；
其中亦處於如R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜芳基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R51 、-OR51 、-NO2 、-NR51 R51 ' 、-NR51 C(O)R51 ' 、-NR51 S(O)2 R51 ' 、-S(O)2 NR51 R51 ' 、-NR51 C(O)NR51 ' R51 '' 、-SR51 、-S(O)R51 、-S(O)2 R51 、-CN、鹵烷基、鹵烷氧基、-C(O)OR51 、-C(O)NR51 R51 ' 、-OCH2 CH2 OR51 、-NR51 S(O)2 NR51 ' R51 '' 及-C(CH3 )2 OR51 ；
及/或經一或多個選自以下之取代基取代：經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜環基；
其中R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
R5 ' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR52 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR52 R52 ' ；
其中R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之烷基、烯基或炔基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、-OR13 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR13 R13 ' ；
其中R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之芳基、雜環基或環烷基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R14 、-OR14 、-NO2 、-NR14 R14 ' 、-NR14 C(O)R14 ' 、-NR14 S(O)2 R14 ' 、-S(O)2 NR14 R14 ' 、-NR14 C(O)NR14 ' R14 '' 、-SR14 、-S(O)R14 、-S(O)2 R14 、-CN、鹵烷基、鹵烷氧基、-C(O)OR14 、-C(O)NR14 R14 ' 、-OCH2 CH2 OR14 、-NR14 S(O)2 NR14 ' R14 '' 及-C(CH3 )2 OR14 ；
其中R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of the invention is a compound of general formula (I)

among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
If X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) C (O) [CH 2 ] q- , then q is 0, 1, 2 , 3, 4 or 5; and if X is selected from-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- , then q is 1, 2, 3, 4 or 5;
p is 0, 1, 2, 3, 4 or 5;
Y 1 is -C (R 10 R 10 ' )-;
Wherein R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
Alternatively, R 10 and R 10 ′ may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
Y 2 is -C (R 10 '' R 10 ''')-;
Wherein R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted the substituted C 2-6 alkynyl group;
Alternatively, R 10 '' and R 10 '''may form a substituted or unsubstituted cycloalkyl group with the carbon atom they are attached;
n is 0 or 1;
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
Wherein, if an aryl or heterocyclic group in R 2 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
among them,
If an alkyl, alkenyl or alkynyl group as defined in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: -OR 31 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 31 R 31 ' ;
Wherein, if the cycloalkyl group in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 31 , -OR 31 , -NO 2 , -NR 31 R 31 ' , -NR 31 C (O) R 31 ' , -NR 31 S (O) 2 R 31 ' , -S (O) 2 NR 31 R 31 ' , -NR 31 C (O) NR 31 ' R 31 '' , -SR 31 , -S (O) R 31 , -S (O) 2 R 31 , -CN, haloalkyl, haloalkoxy, -C (O) OR 31 , -C (O) NR 31 R 31 ' ,- OCH 2 CH 2 OR 31 , -NR 31 S (O) 2 NR 31 ' R 31 '' and -C (CH 3 ) 2 OR 31 ;
Wherein R 31, R 31 'and R 31' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
If an alkyl, alkenyl or alkynyl group as defined in R 3 ′ is substituted, it is substituted with one or more substituents selected from: -OR 32 , halogen, -CN, haloalkyl, haloalkoxy And -NR 32 R 32 ' ;
Wherein R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
Where alkyl, alkenyl or alkynyl in alkylaryl, alkylheteroaryl or alkylcycloalkyl as defined in R 5 is substituted, it is substituted by one or more of the following Group substitution: -OR 51 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 51 R 51 ' ;
Where cycloalkyl, aryl or heteroaryl, which is also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R 5 is substituted, it is selected from one or more selected from The following substituents are substituted: halogen, -R 51 , -OR 51 , -NO 2 , -NR 51 R 51 ' , -NR 51 C (O) R 51 ' , -NR 51 S (O) 2 R 51 ' , -S (O) 2 NR 51 R 51 ' , -NR 51 C (O) NR 51 ' R 51 '' , -SR 51 , -S (O) R 51 , -S (O) 2 R 51 , -CN , Haloalkyl, haloalkoxy, -C (O) OR 51 , -C (O) NR 51 R 51 ' , -OCH 2 CH 2 OR 51 , -NR 51 S (O) 2 NR 51 ' R 51 '' And -C (CH 3 ) 2 OR 51 ;
And / or substituted with one or more substituents selected from: substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted Or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheterocyclyl;
Wherein R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
among them
If an alkyl, alkenyl or alkynyl group as defined in R 5 ' is substituted, it is substituted with one or more substituents selected from -OR 52 , halogen, -CN, haloalkyl, haloalkoxy And -NR 52 R 52 ' ;
Wherein R 52 and R 52 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
Alkyl, alkenyl, or alkynyl that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group if substituted and the substitution is not otherwise defined, is selected from one or more selected from The following substituents are substituted: = O, -OR 13 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 13 R 13 ′ ;
Wherein R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
If an aryl, heterocyclyl, or cycloalkyl group that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group is substituted and the substitution is not otherwise defined, it is substituted by one or more Substituted by a substituent selected from: = O, halogen, -R 14 , -OR 14 , -NO 2 , -NR 14 R 14 ' , -NR 14 C (O) R 14 ' , -NR 14 S (O) 2 R 14 ' , -S (O) 2 NR 14 R 14 ' , -NR 14 C (O) NR 14 ' R 14 '' , -SR 14 , -S (O) R 14 , -S (O) 2 R 14 , -CN, haloalkyl, haloalkoxy, -C (O) OR 14 , -C (O) NR 14 R 14 ' , -OCH 2 CH 2 OR 14 , -NR 14 S (O) 2 NR 14 ' R 14 '' and -C (CH 3 ) 2 OR 14 ;
Wherein R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl, unsubstituted alkenyl group of C 2-6, unsubstituted C 2-6 alkynyl group of , Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic group;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(I' )化合物

其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 、X及n如在詳細說明中所定義，
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I ' )

Where R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , X and n are as defined in the detailed description,
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(I' )化合物

其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
p為0、1、2、3、4或5；
q為0、1、2、3、4或5；
n為0或1；
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I ' )

among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
p is 0, 1, 2, 3, 4 or 5;
q is 0, 1, 2, 3, 4 or 5;
n is 0 or 1;
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(I' )化合物

其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
p為0、1、2、3、4或5；
q為0、1、2、3、4或5；
n為0或1；
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
其中R2 中之芳基或雜環基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
其中，
R3 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR31 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR31 R31 ' ；
其中R3 中之環烷基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R31 、-OR31 、-NO2 、-NR31 R31 ' 、-NR31 C(O)R31 ' 、-NR31 S(O)2 R31 ' 、-S(O)2 NR31 R31 ' 、-NR31 C(O)NR31 ' R31 '' 、-SR31 、-S(O)R31 、-S(O)2 R31 、-CN、鹵烷基、鹵烷氧基、-C(O)OR31 、-C(O)NR31 R31 ' 、-OCH2 CH2 OR31 、-NR31 S(O)2 NR31 ' R31 '' 及-C(CH3 )2 OR31 ；
其中R31 、R31 ' 及R31 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR32 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR32 R32 ' ；
其中R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 ' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
其中
亦處於R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR51 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR51 R51 ' ；
其中亦處於如R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜芳基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R51 、-OR51 、-NO2 、-NR51 R51 ' 、-NR51 C(O)R51 ' 、-NR51 S(O)2 R51 ' 、-S(O)2 NR51 R51 ' 、-NR51 C(O)NR51 ' R51 '' 、-SR51 、-S(O)R51 、-S(O)2 R51 、-CN、鹵烷基、鹵烷氧基、-C(O)OR51 、-C(O)NR51 R51 ' 、-OCH2 CH2 OR51 、-NR51 S(O)2 NR51 ' R51 '' 及-C(CH3 )2 OR51 ；
及/或經一或多個選自以下之取代基取代：經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜環基；
其中R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
R5 ' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR52 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR52 R52 ' ；
其中R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之烷基、烯基或炔基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、-OR13 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR13 R13 ' ；
其中R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之芳基、雜環基或環烷基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R14 、-OR14 、-NO2 、-NR14 R14 ' 、-NR14 C(O)R14 ' 、-NR14 S(O)2 R14 ' 、-S(O)2 NR14 R14 ' 、-NR14 C(O)NR14 ' R14 '' 、-SR14 、-S(O)R14 、-S(O)2 R14 、-CN、鹵烷基、鹵烷氧基、-C(O)OR14 、-C(O)NR14 R14 ' 、-OCH2 CH2 OR14 、-NR14 S(O)2 NR14 ' R14 '' 及-C(CH3 )2 OR14 ；
其中R14 、R14 ' 及R14 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I ' )

among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
p is 0, 1, 2, 3, 4 or 5;
q is 0, 1, 2, 3, 4 or 5;
n is 0 or 1;
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
Wherein, if an aryl or heterocyclic group in R 2 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
among them,
If an alkyl, alkenyl or alkynyl group as defined in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: -OR 31 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 31 R 31 ' ;
Wherein, if the cycloalkyl group in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 31 , -OR 31 , -NO 2 , -NR 31 R 31 ' , -NR 31 C (O) R 31 ' , -NR 31 S (O) 2 R 31 ' , -S (O) 2 NR 31 R 31 ' , -NR 31 C (O) NR 31 ' R 31 '' , -SR 31 , -S (O) R 31 , -S (O) 2 R 31 , -CN, haloalkyl, haloalkoxy, -C (O) OR 31 , -C (O) NR 31 R 31 ' ,- OCH 2 CH 2 OR 31 , -NR 31 S (O) 2 NR 31 ' R 31 '' and -C (CH 3 ) 2 OR 31 ;
Wherein R 31, R 31 'and R 31' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
If an alkyl, alkenyl or alkynyl group as defined in R 3 ′ is substituted, it is substituted with one or more substituents selected from: -OR 32 , halogen, -CN, haloalkyl, haloalkoxy And -NR 32 R 32 ' ;
Wherein R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 ' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
Where alkyl, alkenyl or alkynyl in alkylaryl, alkylheteroaryl or alkylcycloalkyl as defined in R 5 is substituted, it is substituted by one or more of the following Group substitution: -OR 51 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 51 R 51 ' ;
Where cycloalkyl, aryl or heteroaryl, which is also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R 5 is substituted, it is selected from one or more selected from The following substituents are substituted: halogen, -R 51 , -OR 51 , -NO 2 , -NR 51 R 51 ' , -NR 51 C (O) R 51 ' , -NR 51 S (O) 2 R 51 ' , -S (O) 2 NR 51 R 51 ' , -NR 51 C (O) NR 51 ' R 51 '' , -SR 51 , -S (O) R 51 , -S (O) 2 R 51 , -CN , Haloalkyl, haloalkoxy, -C (O) OR 51 , -C (O) NR 51 R 51 ' , -OCH 2 CH 2 OR 51 , -NR 51 S (O) 2 NR 51 ' R 51 '' And -C (CH 3 ) 2 OR 51 ;
And / or substituted with one or more substituents selected from: substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted Or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheterocyclyl;
Wherein R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
among them
If an alkyl, alkenyl or alkynyl group as defined in R 5 ' is substituted, it is substituted with one or more substituents selected from -OR 52 , halogen, -CN, haloalkyl, haloalkoxy And -NR 52 R 52 ' ;
Wherein R 52 and R 52 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
Alkyl, alkenyl, or alkynyl that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group if substituted and the substitution is not otherwise defined, is selected from one or more selected from The following substituents are substituted: = O, -OR 13 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 13 R 13 ′ ;
Wherein R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
If an aryl, heterocyclyl, or cycloalkyl group that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group is substituted and the substitution is not otherwise defined, it is substituted by one or more Substituted by a substituent selected from: = O, halogen, -R 14 , -OR 14 , -NO 2 , -NR 14 R 14 ' , -NR 14 C (O) R 14 ' , -NR 14 S (O) 2 R 14 ' , -S (O) 2 NR 14 R 14 ' , -NR 14 C (O) NR 14 ' R 14 '' , -SR 14 , -S (O) R 14 , -S (O) 2 R 14 , -CN, haloalkyl, haloalkoxy, -C (O) OR 14 , -C (O) NR 14 R 14 ' , -OCH 2 CH 2 OR 14 , -NR 14 S (O) 2 NR 14 ' R 14 '' and -C (CH 3 ) 2 OR 14 ;
Wherein R 14 , R 14 ' and R 14 ' are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, unsubstituted C 2-6 alkynyl, Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic groups;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(Ia )化合物

其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 、R6 、R6 ' 、X、Y1 、Y2 及n如在詳細說明中所定義，
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I a )

Wherein R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 6 , R 6 ′ , X, Y 1 , Y 2 and n are as defined in the detailed description,
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(Ia )化合物

其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
p為0、1、2、3、4或5；
q為0、1、2、3、4或5；
Y1 為-C(R10 R10 ' )-；
其中R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 及R10 ' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
Y2 為-C(R10 '' R10 ''' )-；
其中R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 '' 及R10 ''' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
n為0或1；
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I a )

among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
p is 0, 1, 2, 3, 4 or 5;
q is 0, 1, 2, 3, 4 or 5;
Y 1 is -C (R 10 R 10 ' )-;
Wherein R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
Alternatively, R 10 and R 10 ′ may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
Y 2 is -C (R 10 '' R 10 ''')-;
Wherein R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted the substituted C 2-6 alkynyl group;
Alternatively, R 10 '' and R 10 '''may form a substituted or unsubstituted cycloalkyl group with the carbon atom they are attached;
n is 0 or 1;
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(Ia )化合物

其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
p為0、1、2、3、4或5；
q為0、1、2、3、4或5；
Y1 為-C(R10 R10 ' )-；
其中R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 及R10 ' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
Y2 為-C(R10 '' R10 ''' )-；
其中R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 '' 及R10 ''' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
n為0或1；
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
其中R2 中之芳基或雜環基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
其中，
R3 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR31 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR31 R31 ' ；
其中R3 中之環烷基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R31 、-OR31 、-NO2 、-NR31 R31 ' 、-NR31 C(O)R31 ' 、-NR31 S(O)2 R31 ' 、-S(O)2 NR31 R31 ' 、-NR31 C(O)NR31 ' R31 '' 、-SR31 、-S(O)R31 、-S(O)2 R31 、-CN、鹵烷基、鹵烷氧基、-C(O)OR31 、-C(O)NR31 R31 ' 、-OCH2 CH2 OR31 、-NR31 S(O)2 NR31 ' R31 '' 及-C(CH3 )2 OR31 ；
其中R31 、R31 ' 及R31 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR32 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR32 R32 ' ；
其中R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
其中
亦處於R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR51 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR51 R51 ' ；
其中亦處於如R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜芳基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R51 、-OR51 、-NO2 、-NR51 R51 ' 、-NR51 C(O)R51 ' 、-NR51 S(O)2 R51 ' 、-S(O)2 NR51 R51 ' 、-NR51 C(O)NR51 ' R51 '' 、-SR51 、-S(O)R51 、-S(O)2 R51 、-CN、鹵烷基、鹵烷氧基、-C(O)OR51 、-C(O)NR51 R51 ' 、-OCH2 CH2 OR51 、-NR51 S(O)2 NR51 ' R51 '' 及-C(CH3 )2 OR51 ；
及/或經一或多個選自以下之取代基取代：經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜環基；
其中R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
R5 ' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR52 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR52 R52 ' ；
其中R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之烷基、烯基或炔基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、-OR13 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR13 R13 ' ；
其中R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之芳基、雜環基或環烷基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R14 、-OR14 、-NO2 、-NR14 R14 ' 、-NR14 C(O)R14 ' 、-NR14 S(O)2 R14 ' 、-S(O)2 NR14 R14 ' 、-NR14 C(O)NR14 ' R14 '' 、-SR14 、-S(O)R14 、-S(O)2 R14 、-CN、鹵烷基、鹵烷氧基、-C(O)OR14 、-C(O)NR14 R14 ' 、-OCH2 CH2 OR14 、-NR14 S(O)2 NR14 ' R14 '' 及-C(CH3 )2 OR14 ；
其中R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I a )

among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
p is 0, 1, 2, 3, 4 or 5;
q is 0, 1, 2, 3, 4 or 5;
Y 1 is -C (R 10 R 10 ' )-;
Wherein R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
Alternatively, R 10 and R 10 ′ may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
Y 2 is -C (R 10 '' R 10 ''')-;
Wherein R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted the substituted C 2-6 alkynyl group;
Alternatively, R 10 '' and R 10 '''may form a substituted or unsubstituted cycloalkyl group with the carbon atom they are attached;
n is 0 or 1;
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
Wherein, if an aryl or heterocyclic group in R 2 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
among them,
If an alkyl, alkenyl or alkynyl group as defined in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: -OR 31 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 31 R 31 ' ;
Wherein, if the cycloalkyl group in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 31 , -OR 31 , -NO 2 , -NR 31 R 31 ' , -NR 31 C (O) R 31 ' , -NR 31 S (O) 2 R 31 ' , -S (O) 2 NR 31 R 31 ' , -NR 31 C (O) NR 31 ' R 31 '' , -SR 31 , -S (O) R 31 , -S (O) 2 R 31 , -CN, haloalkyl, haloalkoxy, -C (O) OR 31 , -C (O) NR 31 R 31 ' ,- OCH 2 CH 2 OR 31 , -NR 31 S (O) 2 NR 31 ' R 31 '' and -C (CH 3 ) 2 OR 31 ;
Wherein R 31, R 31 'and R 31' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
If an alkyl, alkenyl or alkynyl group as defined in R 3 ′ is substituted, it is substituted with one or more substituents selected from: -OR 32 , halogen, -CN, haloalkyl, haloalkoxy And -NR 32 R 32 ' ;
Wherein R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
Where alkyl, alkenyl or alkynyl in alkylaryl, alkylheteroaryl or alkylcycloalkyl as defined in R 5 is substituted, it is substituted by one or more of the following Group substitution: -OR 51 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 51 R 51 ' ;
Where cycloalkyl, aryl or heteroaryl, which is also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R 5 is substituted, it is selected from one or more selected from The following substituents are substituted: halogen, -R 51 , -OR 51 , -NO 2 , -NR 51 R 51 ' , -NR 51 C (O) R 51 ' , -NR 51 S (O) 2 R 51 ' , -S (O) 2 NR 51 R 51 ' , -NR 51 C (O) NR 51 ' R 51 '' , -SR 51 , -S (O) R 51 , -S (O) 2 R 51 , -CN , Haloalkyl, haloalkoxy, -C (O) OR 51 , -C (O) NR 51 R 51 ' , -OCH 2 CH 2 OR 51 , -NR 51 S (O) 2 NR 51 ' R 51 '' And -C (CH 3 ) 2 OR 51 ;
And / or substituted with one or more substituents selected from: substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted Or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheterocyclyl;
Wherein R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
among them
If an alkyl, alkenyl or alkynyl group as defined in R 5 ' is substituted, it is substituted with one or more substituents selected from -OR 52 , halogen, -CN, haloalkyl, haloalkoxy And -NR 52 R 52 ' ;
Wherein R 52 and R 52 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
Alkyl, alkenyl, or alkynyl that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group if substituted and the substitution is not otherwise defined, is selected from one or more selected from The following substituents are substituted: = O, -OR 13 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 13 R 13 ′ ;
Wherein R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
If an aryl, heterocyclyl, or cycloalkyl group that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group is substituted and the substitution is not otherwise defined, it is substituted by one or more Substituted by a substituent selected from: = O, halogen, -R 14 , -OR 14 , -NO 2 , -NR 14 R 14 ' , -NR 14 C (O) R 14 ' , -NR 14 S (O) 2 R 14 ' , -S (O) 2 NR 14 R 14 ' , -NR 14 C (O) NR 14 ' R 14 '' , -SR 14 , -S (O) R 14 , -S (O) 2 R 14 , -CN, haloalkyl, haloalkoxy, -C (O) OR 14 , -C (O) NR 14 R 14 ' , -OCH 2 CH 2 OR 14 , -NR 14 S (O) 2 NR 14 ' R 14 '' and -C (CH 3 ) 2 OR 14 ;
Wherein R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl, unsubstituted alkenyl group of C 2-6, unsubstituted C 2-6 alkynyl group of , Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic group;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(Ia ' )化合物

其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 、R6 、R6 ' 、X及n如在詳細說明中所定義，
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I a ' )

Where R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 6 , R 6 ′ , X and n are as defined in the detailed description,
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(Ia ' )化合物

其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
p為0、1、2、3、4或5；
q為0、1、2、3、4或5；
n為0或1；
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I a ' )

among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
p is 0, 1, 2, 3, 4 or 5;
q is 0, 1, 2, 3, 4 or 5;
n is 0 or 1;
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(Ia ' )化合物

其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
p為0、1、2、3、4或5；
q為0、1、2、3、4或5；
n為0或1；
R1 係選自-NR5 R' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
其中R2 中之芳基或雜環基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
其中，
R3 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR31 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR31 R31 ' ；
其中R3 中之環烷基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R31 、-OR31 、-NO2 、-NR31 R31 ' 、-NR31 C(O)R31 ' 、-NR31 S(O)2 R31 ' 、-S(O)2 NR31 R31 ' 、-NR31 C(O)NR31 ' R31 '' 、-SR31 、-S(O)R31 、-S(O)2 R31 、-CN、鹵烷基、鹵烷氧基、-C(O)OR31 、-C(O)NR31 R31 ' 、-OCH2 CH2 OR31 、-NR31 S(O)2 NR31 ' R31 '' 及-C(CH3 )2 OR31 ；
其中R31 、R31 ' 及R31 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR32 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR32 R32 ' ；
其中R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
其中
亦處於R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR51 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR51 R51 ' ；
其中亦處於如R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜芳基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R51 、-OR51 、-NO2 、-NR51 R51 ' 、-NR51 C(O)R51 ' 、-NR51 S(O)2 R51 ' 、-S(O)2 NR51 R51 ' 、-NR51 C(O)NR51 ' R51 ' 、-SR51 、-S(O)R51 、-S(O)2 R51 、-CN、鹵烷基、鹵烷氧基、-C(O)OR51 、-C(O)NR51 R51 ' 、-OCH2 CH2 OR51 、-NR51 S(O)2 NR51 ' R51 '' 及-C(CH3 )2 OR51 ；
及/或經一或多個選自以下之取代基取代：經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜環基；
其中R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
R5 ' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR52 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR52 R52 ' ；
其中R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之烷基、烯基或炔基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、-OR13 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR13 R13 ' ；
其中R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之芳基、雜環基或環烷基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R14 、-OR14 、-NO2 、-NR14 R14 ' 、-NR14 C(O)R14 ' 、-NR14 S(O)2 R14 ' 、-S(O)2 NR14 R14 ' 、-NR14 C(O)NR14 ' R14 '' 、-SR14 、-S(O)R14 、-S(O)2 R14 、-CN、鹵烷基、鹵烷氧基、-C(O)OR14 、-C(O)NR14 R14 ' 、-OCH2 CH2 OR14 、-NR14 S(O)2 NR14 ' R14 '' 及-C(CH3 )2 OR14 ；
其中R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I a ' )

among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
p is 0, 1, 2, 3, 4 or 5;
q is 0, 1, 2, 3, 4 or 5;
n is 0 or 1;
R 1 is selected from -NR 5 R ' and -NR 5 ' C (O) R 5 ;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
Wherein, if an aryl or heterocyclic group in R 2 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
among them,
If an alkyl, alkenyl or alkynyl group as defined in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: -OR 31 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 31 R 31 ' ;
Wherein, if the cycloalkyl group in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 31 , -OR 31 , -NO 2 , -NR 31 R 31 ' , -NR 31 C (O) R 31 ' , -NR 31 S (O) 2 R 31 ' , -S (O) 2 NR 31 R 31 ' , -NR 31 C (O) NR 31 ' R 31 '' , -SR 31 , -S (O) R 31 , -S (O) 2 R 31 , -CN, haloalkyl, haloalkoxy, -C (O) OR 31 , -C (O) NR 31 R 31 ' ,- OCH 2 CH 2 OR 31 , -NR 31 S (O) 2 NR 31 ' R 31 '' and -C (CH 3 ) 2 OR 31 ;
Wherein R 31, R 31 'and R 31' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
If an alkyl, alkenyl or alkynyl group as defined in R 3 ′ is substituted, it is substituted with one or more substituents selected from: -OR 32 , halogen, -CN, haloalkyl, haloalkoxy And -NR 32 R 32 ' ;
Wherein R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41 , R 41 ′ and R 41 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
Where alkyl, alkenyl or alkynyl in alkylaryl, alkylheteroaryl or alkylcycloalkyl as defined in R 5 is substituted, it is substituted by one or more of the following Group substitution: -OR 51 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 51 R 51 ' ;
Wherein R 5 also is defined as a cycloalkyl group of aryl, alkyl aryl or alkyl heteroaryl cycloalkyl group, an aryl group or heteroaryl group, if substituted, is substituted with one or more substituents selected from The following substituents are substituted: halogen, -R 51 , -OR 51 , -NO 2 , -NR 51 R 51 ' , -NR 51 C (O) R 51 ' , -NR 51 S (O) 2 R 51 ' , -S (O) 2 NR 51 R 51 ' , -NR 51 C (O) NR 51 ' R 51 ' , -SR 51 , -S (O) R 51 , -S (O) 2 R 51 , -CN, Haloalkyl, haloalkoxy, -C (O) OR 51 , -C (O) NR 51 R 51 ' , -OCH 2 CH 2 OR 51 , -NR 51 S (O) 2 NR 51 ' R 51 '' And -C (CH 3 ) 2 OR 51 ;
And / or substituted with one or more substituents selected from: substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted Or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheterocyclyl;
Wherein R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
among them
If an alkyl, alkenyl or alkynyl group as defined in R 5 ' is substituted, it is substituted with one or more substituents selected from -OR 52 , halogen, -CN, haloalkyl, haloalkoxy And -NR 52 R 52 ' ;
Wherein R 52 and R 52 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
Alkyl, alkenyl, or alkynyl that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group if substituted and the substitution is not otherwise defined, is selected from one or more selected from The following substituents are substituted: = O, -OR 13 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 13 R 13 ′ ;
Wherein R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
If an aryl, heterocyclyl, or cycloalkyl group that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group is substituted and the substitution is not otherwise defined, it is substituted by one or more Substituted by a substituent selected from: = O, halogen, -R 14 , -OR 14 , -NO 2 , -NR 14 R 14 ' , -NR 14 C (O) R 14 ' , -NR 14 S (O) 2 R 14 ' , -S (O) 2 NR 14 R 14 ' , -NR 14 C (O) NR 14 ' R 14 '' , -SR 14 , -S (O) R 14 , -S (O) 2 R 14 , -CN, haloalkyl, haloalkoxy, -C (O) OR 14 , -C (O) NR 14 R 14 ' , -OCH 2 CH 2 OR 14 , -NR 14 S (O) 2 NR 14 ' R 14 '' and -C (CH 3 ) 2 OR 14 ;
Wherein R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl, unsubstituted alkenyl group of C 2-6, unsubstituted C 2-6 alkynyl group of , Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic group;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(Ib )化合物
，
其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 、R6 、R6 ' 、X、Y1 、Y2 及n如下文在詳細說明中所定義，
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I b )
,
Wherein R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 6 , R 6 ′ , X, Y 1 , Y 2 and n are as defined in the detailed description below,
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(Ib )化合物

其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
p為0、1、2、3、4或5；
q為0、1、2、3、4或5；
Y1 為-C(R10 R10 ' )-；
其中R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 及R10 ' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
Y2 為-C(R10 '' R10 ''' )-；
其中R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 '' 及R10 ''' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
n為0或1；
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I b )

among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
p is 0, 1, 2, 3, 4 or 5;
q is 0, 1, 2, 3, 4 or 5;
Y 1 is -C (R 10 R 10 ' )-;
Wherein R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
Alternatively, R 10 and R 10 ′ may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
Y 2 is -C (R 10 '' R 10 ''')-;
Wherein R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted the substituted C 2-6 alkynyl group;
Alternatively, R 10 '' and R 10 '''may form a substituted or unsubstituted cycloalkyl group with the carbon atom they are attached;
n is 0 or 1;
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(Ib )化合物

其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
p為0、1、2、3、4或5；
q為0、1、2、3、4或5；
Y1 為-C(R10 R10 ' )-；
其中R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 及R10 ' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
Y2 為-C(R10 '' R10 ''' )-；
其中R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 '' 及R10 ''' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
n為0或1；
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
其中R2 中之芳基或雜環基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
其中，
R3 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR31 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR31 R31 ' ；
其中R3 中之環烷基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R31 、-OR31 、-NO2 、-NR31 R31 ' 、-NR31 C(O)R31 ' 、-NR31 S(O)2 R31 ' 、-S(O)2 NR31 R31 ' 、-NR31 C(O)NR31 ' R31 '' 、-SR31 、-S(O)R31 、-S(O)2 R31 、-CN、鹵烷基、鹵烷氧基、-C(O)OR31 、-C(O)NR31 R31 ' 、-OCH2 CH2 OR31 、-NR31 S(O)2 NR31 ' R31 '' 及-C(CH3 )2 OR31 ；
其中R31 、R31 ' 及R31 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR32 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR32 R32 ' ；
其中R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
其中
亦處於R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR51 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR51 R51 ' ；
其中亦處於如R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜環基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R51 、-OR51 、-NO2 、-NR51 R51 ' 、-NR51 C(O)R51 ' 、-NR51 S(O)2 R51 ' 、-S(O)2 NR51 R51 ' 、-NR51 C(O)NR51 ' R51 '' 、-SR51 、-S(O)R51 、-S(O)2 R51 、-CN、鹵烷基、鹵烷氧基、-C(O)OR51 、-C(O)NR51 R51 ' 、-OCH2 CH2 OR51 、-NR51 S(O)2 NR51 ' R51 '' 及-C(CH3 )2 OR51 ；
及/或經一或多個選自以下之取代基取代：經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜環基；
其中R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
R5 ' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR52 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR52 R52 ' ；
其中R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之烷基、烯基或炔基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、-OR13 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR13 R13 ' ；
其中R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之芳基、雜環基或環烷基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R14 、-OR14 、-NO2 、-NR14 R14 ' 、-NR14 C(O)R14 ' 、-NR14 S(O)2 R14 ' 、-S(O)2 NR14 R14 ' 、-NR14 C(O)NR14 ' R14 '' 、-SR14 、-S(O)R14 、-S(O)2 R14 、-CN、鹵烷基、鹵烷氧基、-C(O)OR14 、-C(O)NR14 R14 ' 、-OCH2 CH2 OR14 、-NR14 S(O)2 NR14 ' R14 '' 及-C(CH3 )2 OR14 ；
其中R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I b )

among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
p is 0, 1, 2, 3, 4 or 5;
q is 0, 1, 2, 3, 4 or 5;
Y 1 is -C (R 10 R 10 ' )-;
Wherein R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
Alternatively, R 10 and R 10 ′ may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
Y 2 is -C (R 10 '' R 10 ''')-;
Wherein R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted the substituted C 2-6 alkynyl group;
Alternatively, R 10 '' and R 10 '''may form a substituted or unsubstituted cycloalkyl group with the carbon atom they are attached;
n is 0 or 1;
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
Wherein, if an aryl or heterocyclic group in R 2 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
among them,
If an alkyl, alkenyl or alkynyl group as defined in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: -OR 31 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 31 R 31 ' ;
Wherein, if the cycloalkyl group in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 31 , -OR 31 , -NO 2 , -NR 31 R 31 ' , -NR 31 C (O) R 31 ' , -NR 31 S (O) 2 R 31 ' , -S (O) 2 NR 31 R 31 ' , -NR 31 C (O) NR 31 ' R 31 '' , -SR 31 , -S (O) R 31 , -S (O) 2 R 31 , -CN, haloalkyl, haloalkoxy, -C (O) OR 31 , -C (O) NR 31 R 31 ' ,- OCH 2 CH 2 OR 31 , -NR 31 S (O) 2 NR 31 ' R 31 '' and -C (CH 3 ) 2 OR 31 ;
Wherein R 31, R 31 'and R 31' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
If an alkyl, alkenyl or alkynyl group as defined in R 3 ′ is substituted, it is substituted with one or more substituents selected from: -OR 32 , halogen, -CN, haloalkyl, haloalkoxy And -NR 32 R 32 ' ;
Wherein R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
Where alkyl, alkenyl or alkynyl in alkylaryl, alkylheteroaryl or alkylcycloalkyl as defined in R 5 is substituted, it is substituted by one or more of the following Group substitution: -OR 51 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 51 R 51 ' ;
Wherein a cycloalkyl, aryl or heterocyclic group which is also in an alkylaryl, alkylheteroaryl or alkylcycloalkyl group as defined in R 5 is substituted with one or more selected from The following substituents are substituted: halogen, -R 51 , -OR 51 , -NO 2 , -NR 51 R 51 ' , -NR 51 C (O) R 51 ' , -NR 51 S (O) 2 R 51 ' , -S (O) 2 NR 51 R 51 ' , -NR 51 C (O) NR 51 ' R 51 '' , -SR 51 , -S (O) R 51 , -S (O) 2 R 51 , -CN , Haloalkyl, haloalkoxy, -C (O) OR 51 , -C (O) NR 51 R 51 ' , -OCH 2 CH 2 OR 51 , -NR 51 S (O) 2 NR 51 ' R 51 '' And -C (CH 3 ) 2 OR 51 ;
And / or substituted with one or more substituents selected from: substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted Or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheterocyclyl;
Wherein R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
among them
If an alkyl, alkenyl or alkynyl group as defined in R 5 ' is substituted, it is substituted with one or more substituents selected from -OR 52 , halogen, -CN, haloalkyl, haloalkoxy And -NR 52 R 52 ' ;
Wherein R 52 and R 52 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
Alkyl, alkenyl, or alkynyl that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group if substituted and the substitution is not otherwise defined, is selected from one or more selected from The following substituents are substituted: = O, -OR 13 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 13 R 13 ′ ;
Wherein R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
If an aryl, heterocyclyl, or cycloalkyl group that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group is substituted and the substitution is not otherwise defined, it is substituted by one or more Substituted by a substituent selected from: = O, halogen, -R 14 , -OR 14 , -NO 2 , -NR 14 R 14 ' , -NR 14 C (O) R 14 ' , -NR 14 S (O) 2 R 14 ' , -S (O) 2 NR 14 R 14 ' , -NR 14 C (O) NR 14 ' R 14 '' , -SR 14 , -S (O) R 14 , -S (O) 2 R 14 , -CN, haloalkyl, haloalkoxy, -C (O) OR 14 , -C (O) NR 14 R 14 ' , -OCH 2 CH 2 OR 14 , -NR 14 S (O) 2 NR 14 ' R 14 '' and -C (CH 3 ) 2 OR 14 ;
Wherein R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl, unsubstituted alkenyl group of C 2-6, unsubstituted C 2-6 alkynyl group of , Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic group;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(Ib ' )化合物
，
其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 、R6 、R6 ' 、X及n如下文在詳細說明中所定義，
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I b ' )
,
Wherein R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 6 , R 6 ′ , X and n are as defined in the detailed description below,
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(Ib ' )化合物
，
其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
p為0、1、2、3、4或5；
q為0、1、2、3、4或5；
n為0或1；
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I b ' )
,
among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
p is 0, 1, 2, 3, 4 or 5;
q is 0, 1, 2, 3, 4 or 5;
n is 0 or 1;
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為通式(Ib ' )化合物
，
其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
p為0、1、2、3、4或5；
q為0、1、2、3、4或5；
n為0或1；
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
其中R2 中之芳基或雜環基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR2 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
其中，
R3 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR31 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR31 R31 ' ；
其中R3 中之環烷基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R31 、-OR31 、-NO2 、-NR31 R31 ' 、-NR31 C(O)R31 ' 、-NR31 S(O)2 R31 ' 、-S(O)2 NR31 R31 ' 、-NR31 C(O)NR31 ' R31 '' 、-SR31 、-S(O)R31 、-S(O)2 R31 、-CN、鹵烷基、鹵烷氧基、-C(O)OR31 、-C(O)NR31 R31 ' 、-OCH2 CH2 OR31 、-NR31 S(O)2 NR31 ' R31 '' 及-C(CH3 )2 OR31 ；
其中R31 、R31 ' 及R31 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR32 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR32 R32 ' ；
其中R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
其中
亦處於R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR51 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR51 R51 ' ；
其中亦處於如R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜芳基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R51 、-OR51 、-NO2 、-NR51 R51 ' 、-NR51 C(O)R51 ' 、-NR51 S(O)2 R51 ' 、-S(O)2 NR51 R51 ' 、-NR51 C(O)NR51 ' R51 '' 、-SR51 、-S(O)R51 、-S(O)2 R51 、-CN、鹵烷基、鹵烷氧基、-C(O)OR51 、-C(O)NR51 R51 ' 、-OCH2 CH2 OR51 、-NR51 S(O)2 NR51 ' R51 '' 及-C(CH3 )2 OR51 ；
及/或經一或多個選自以下之取代基取代：經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜環基；
其中R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
R5 ' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR52 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR52 R52 ' ；
其中R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 ' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之烷基、烯基或炔基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、-OR13 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR13 R13 ' ；
其中R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
亦處於烷基芳基、烷基雜環基或烷基環烷基中之芳基、雜環基或環烷基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R14 、-OR14 、-NO2 、-NR14 R14 ' 、-NR14 C(O)R14 ' 、-NR14 S(O)2 R14 ' 、-S(O)2 NR14 R14 ' 、-NR14 C(O)NR14 ' R14 '' 、-SR14 、-S(O)R14 、-S(O)2 R14 、-CN、鹵烷基、鹵烷氧基、-C(O)OR14 、-C(O)NR14 R14 ' 、-OCH2 CH2 OR14 、-NR14 S(O)2 NR14 ' R14 '' 及-C(CH3 )2 OR14 ；
其中R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound of general formula (I b ' )
,
among them
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
p is 0, 1, 2, 3, 4 or 5;
q is 0, 1, 2, 3, 4 or 5;
n is 0 or 1;
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
Wherein, if the aryl or heterocyclic group in R 2 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 2 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
among them,
If an alkyl, alkenyl or alkynyl group as defined in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: -OR 31 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 31 R 31 ' ;
Wherein, if the cycloalkyl group in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 31 , -OR 31 , -NO 2 , -NR 31 R 31 ' , -NR 31 C (O) R 31 ' , -NR 31 S (O) 2 R 31 ' , -S (O) 2 NR 31 R 31 ' , -NR 31 C (O) NR 31 ' R 31 '' , -SR 31 , -S (O) R 31 , -S (O) 2 R 31 , -CN, haloalkyl, haloalkoxy, -C (O) OR 31 , -C (O) NR 31 R 31 ' ,- OCH 2 CH 2 OR 31 , -NR 31 S (O) 2 NR 31 ' R 31 '' and -C (CH 3 ) 2 OR 31 ;
Wherein R 31, R 31 'and R 31' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
If an alkyl, alkenyl or alkynyl group as defined in R 3 ′ is substituted, it is substituted with one or more substituents selected from: -OR 32 , halogen, -CN, haloalkyl, haloalkoxy And -NR 32 R 32 ' ;
Wherein R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
Where alkyl, alkenyl or alkynyl in alkylaryl, alkylheteroaryl or alkylcycloalkyl as defined in R 5 is substituted, it is substituted by one or more of the following Group substitution: -OR 51 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 51 R 51 ' ;
Where cycloalkyl, aryl or heteroaryl, which is also in alkylaryl, alkylheteroaryl or alkylcycloalkyl, as defined in R 5 is substituted, it is selected from one or more selected from The following substituents are substituted: halogen, -R 51 , -OR 51 , -NO 2 , -NR 51 R 51 ' , -NR 51 C (O) R 51 ' , -NR 51 S (O) 2 R 51 ' , -S (O) 2 NR 51 R 51 ' , -NR 51 C (O) NR 51 ' R 51 '' , -SR 51 , -S (O) R 51 , -S (O) 2 R 51 , -CN , Haloalkyl, haloalkoxy, -C (O) OR 51 , -C (O) NR 51 R 51 ' , -OCH 2 CH 2 OR 51 , -NR 51 S (O) 2 NR 51 ' R 51 '' And -C (CH 3 ) 2 OR 51 ;
And / or substituted with one or more substituents selected from: substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted Or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheterocyclyl;
Wherein R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
among them
If an alkyl, alkenyl or alkynyl group as defined in R 5 ' is substituted, it is substituted with one or more substituents selected from -OR 52 , halogen, -CN, haloalkyl, haloalkoxy And -NR 52 R 52 ' ;
Wherein R 52 and R 52 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 ' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
Alkyl, alkenyl, or alkynyl that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group if substituted and the substitution is not otherwise defined, is selected from one or more selected from The following substituents are substituted: = O, -OR 13 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 13 R 13 ′ ;
Wherein R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
If an aryl, heterocyclyl, or cycloalkyl group that is also in an alkylaryl, alkylheterocyclyl, or alkylcycloalkyl group is substituted and the substitution is not otherwise defined, it is substituted by one or more Substituted by a substituent selected from: = O, halogen, -R 14 , -OR 14 , -NO 2 , -NR 14 R 14 ' , -NR 14 C (O) R 14 ' , -NR 14 S (O) 2 R 14 ' , -S (O) 2 NR 14 R 14 ' , -NR 14 C (O) NR 14 ' R 14 '' , -SR 14 , -S (O) R 14 , -S (O) 2 R 14 , -CN, haloalkyl, haloalkoxy, -C (O) OR 14 , -C (O) NR 14 R 14 ' , -OCH 2 CH 2 OR 14 , -NR 14 S (O) 2 NR 14 ' R 14 '' and -C (CH 3 ) 2 OR 14 ;
Wherein R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl, unsubstituted alkenyl group of C 2-6, unsubstituted C 2-6 alkynyl group of , Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic group;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

為了清楚起見，當在本發明說明書中所描述且參考通式(I)化合物之所有基團及定義存在於所提及之通用馬庫什式中時，彼等基團亦適用於通式(I')、(Ia )、(Ia ' )、(Ib )及(Ib ' )化合物(適用時)，且適用於所有合成中間物，此係因為通式(I')、(Ia )、(Ia ' )、(Ib )及(Ib ' )化合物包括於通式(I)之較大定義的範疇內。For the sake of clarity, when all groups and definitions described in the description of the present invention with reference to compounds of general formula (I) are present in the general Markush formula mentioned, their groups also apply to the general formula (I '), (I a ), (I a ' ), (I b ), and (I b ' ) compounds (where applicable) and are applicable to all synthetic intermediates because of the general formula (I'), (I a ), (I a ' ), (I b ), and (I b ' ) compounds are included in the broader definition of the general formula (I).

為了清楚起見，通用馬庫什式(I)

等效於

其中僅-CH2 -包括於方括號中，且n意謂-CH2 -重複之次數。適用時，相同情況將適用於通用馬庫什式(I)、(I')、(Ia )、(Ia ' )、(Ib )及(Ib ' )，且適用於所有合成中間物。For clarity, the general Markush formula (I)

Equivalent to

Wherein only -CH 2 -is included in square brackets, and n means the number of times that -CH 2 -is repeated. When applicable, the same would apply to the generic Markush formula (I), (I ') , (I a), (I a'), (I b) and (I b '), and is applicable to all synthetic intermediates Thing.

另外且為了清楚起見，應進一步理解，若n為0，則自然地，適用時，氧原子及/或苯基仍存在於通用馬庫什式(I)、(I')、(Ia )、(Ia ' )、(Ib )及(Ib ' )中，且適用於所有合成中間物。In addition and for the sake of clarity, it should be further understood that if n is 0, then naturally, when applicable, oxygen atoms and / or phenyl groups are still present in the general Markush formula (I), (I '), (I a ), (I a ' ), (I b ), and (I b ' ), and apply to all synthetic intermediates.

為了清楚起見，表述「R10 -R10 ' 中之環烷基」意謂當R10 及R10 ' 與其所連接之碳一起形成環烷基時所得的環烷基。此環烷基可隨後經取代或不經取代。此定義亦一般可適用，且亦可適用作由兩個不同官能團形成之任何其他環(如雜環基、芳基或環烷基)的定義，如例如「Ri -Ri ' 中之環」意謂當及Ri ' 與其所連接之原子一起形成環時所得的環。此環可隨後經取代或不經取代。For clarity, the expression "R 10 -R 10 'in the cycloalkyl" means that when R 10 and R 10' resulting in forming a cycloalkyl group together with the carbon they are attached a cycloalkyl group. This cycloalkyl may be subsequently substituted or unsubstituted. This definition is also generally applicable and can also be applied to the definition of any other ring (such as heterocyclyl, aryl or cycloalkyl) formed by two different functional groups, such as, for example, "R i -R i ' "Means a ring that is obtained when and R i ′ forms a ring with the atom to which it is connected. This ring may be subsequently substituted or unsubstituted.

在本發明之上下文中，烷基理解為意謂飽和、直鏈或分支鏈烴，其可未經取代或經一次或若干次取代。其涵蓋例如-CH3 及-CH2 -CH3 。在此等基團中，C1-2 烷基表示C1或C2烷基，C1-3 烷基表示C1、C2或C3烷基，C1-4 烷基表示C1、C2、C3或C4烷基，C1-5 烷基表示C1、C2、C3、C4或C5烷基，C1-6 烷基表示C1、C2、C3、C4、C5或C6烷基，C1-7 烷基表示C1、C2、C3、C4、C5、C6或C7烷基，C1-8 烷基表示C1、C2、C3、C4、C5、C6、C7或C8烷基，C1-10 烷基表示C1、C2、C3、C4、C5、C6、C7、C8、C9或C10烷基，且C1-18 烷基表示C1、C2、C3、C4、C5、C6、C7、C8、C9、C10、C11、C12、C13、C14、C15、C16、C17或C18烷基 烷基較佳為甲基、乙基、丙基、甲基乙基、丁基、1-甲基丙基、2-甲基丙基、1,1-二甲基乙基、戊基、1,1-二甲基丙基、1,2-二甲基丙基、2,2-二甲基丙基、己基、1-甲基戊基，若經取代，亦為CHF2 、CF3 或CH2 OH等。較佳地，在本發明之上下文中，烷基理解為C1-8 烷基，如甲基、乙基、丙基、丁基、戊基、己基、庚基或辛基；較佳為C1-6 烷基，如甲基、乙基、丙基、丁基、戊基或己基；更佳為C1-4 烷基，如甲基、乙基、丙基或丁基。In the context of the present invention, alkyl is understood to mean a saturated, linear or branched hydrocarbon, which may be unsubstituted or substituted one or more times. It covers, for example, -CH 3 and -CH 2 -CH 3 . Among these groups, C 1-2 alkyl represents C1 or C2 alkyl, C 1-3 alkyl represents C1, C2 or C3 alkyl, and C 1-4 alkyl represents C1, C2, C3 or C4 alkyl C 1-5 alkyl means C1, C2, C3, C4 or C5 alkyl, C 1-6 alkyl means C1, C2, C3, C4, C5 or C6 alkyl, C 1-7 alkyl means C1 , C2, C3, C4, C5, C6 or C7 alkyl, C 1-8 alkyl means C1, C2, C3, C4, C5, C6, C7 or C8 alkyl, C 1-10 alkyl means C1, C2 , C3, C4, C5, C6, C7, C8, C9 or C10 alkyl, and C 1-18 alkyl means C1, C2, C3, C4, C5, C6, C7, C8, C9, C10, C11, C12 , C13, C14, C15, C16, C17 or C18 alkylalkyl is preferably methyl, ethyl, propyl, methylethyl, butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, pentyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, 2,2-dimethylpropyl, hexyl, 1-methylpentane The group, if substituted, is also CHF 2 , CF 3 or CH 2 OH. Preferably, in the context of the present invention, alkyl is understood as C 1-8 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl or octyl; preferably C 1-6 alkyl such as methyl, ethyl, propyl, butyl, pentyl or hexyl; more preferably C 1-4 alkyl such as methyl, ethyl, propyl or butyl.

烯基理解為意謂不飽和、直鏈或分支鏈烴，其可未經取代或經一次或若干次取代。其涵蓋如例如-CH=CH-CH3 之基團。烯基較佳為乙烯基(vinyl/ethenyl)、烯丙基(2-丙烯基)。較佳地，在本發明之上下文中，烯基為C2-10 烯基或C2-8 烯基，如乙烯、丙烯、丁烯、戊烯、己烯、庚烯或辛烯；或為C2-6 烯基，如乙烯、丙烯、丁烯、戊烯或己烯；或為C2-4 烯基，如乙烯、丙烯或丁烯。Alkenyl is understood to mean unsaturated, linear or branched hydrocarbons, which may be unsubstituted or substituted one or more times. As it covers e.g. -CH = CH-CH 3 group of the group. Alkenyl is preferably vinyl (ethenyl) or allyl (2-propenyl). Preferably, in the context of the present invention, alkenyl is C 2-10 alkenyl or C 2-8 alkenyl, such as ethylene, propylene, butene, pentene, hexene, heptene or octene; or C 2-6 alkenyl, such as ethylene, propylene, butene, pentene or hexene; or C 2-4 alkenyl, such as ethylene, propylene or butene.

炔基理解為意謂不飽和、直鏈或分支鏈烴，其可未經取代或經一次或若干次取代。其涵蓋如例如-C≡C-CH3 (1-丙炔基)之基團。較佳地，在本發明之上下文中，炔基為C2-10 炔基或C2-8 炔基，如乙炔、丙炔、丁炔、戊炔、己炔、庚炔或辛炔；或為C2-6 炔基，如乙炔、丙炔、丁炔、戊炔或己炔；或為C2-4 炔基，如乙炔、丙炔或丁炔。An alkynyl is understood to mean an unsaturated, straight or branched chain hydrocarbon, which may be unsubstituted or substituted one or more times. As it covers e.g. -C≡C-CH 3 (1- propynyl) of the group. Preferably, in the context of the present invention, the alkynyl is a C 2-10 alkynyl or a C 2-8 alkynyl, such as acetylene, propyne, butyne, pentyne, hexyne, heptyne or octyne; or Is C 2-6 alkynyl, such as acetylene, propyne, butyne, pentyne, or hexyne; or C 2-4 alkynyl, such as acetylene, propyne, or butyne.

與烷基(亦在烷基芳基、烷基雜環基或烷基環烷基中)、烯基、炔基及O-烷基結合，除非另外定義，否則在本發明之上下文中，術語經取代理解為意謂碳原子上之至少一種氫基團由以下置換：鹵素(F、Cl、Br、I)、-NRk Rk ' 、-SRk 、-S(O)Rk 、-S(O)2 Rk 、-ORk 、-C(O)Rk 、-C(O)ORk 、-CN、-C(O)NRk Rk ' 、鹵烷基、鹵烷氧基，Rk 由R13 、R31 、R32 、R51 或R52 表示(Rk ' 由R13 ' 、R31 ' 、R32 ' 、R51 ' 或R52 ' 表示；Rk '' 由R13 '' 、R31 '' 、R32 '' 、R51 '' 或R52 '' 表示)；其中R1 至R52 '' 及Rz 如本說明書中所定義，且其中當不同基團R1 至R52 '' 及Rz 同時存在於式I中時，其可相同或不同。In combination with alkyl (also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl), alkenyl, alkynyl, and O-alkyl, unless otherwise defined, in the context of the present invention, the term Substitution is understood to mean that at least one hydrogen group on a carbon atom is replaced by: halogen (F, Cl, Br, I), -NR k R k ' , -SR k , -S (O) R k ,- S (O) 2 R k , -OR k , -C (O) R k , -C (O) OR k , -CN, -C (O) NR k R k ' , haloalkyl, haloalkoxy R k is represented by R 13 , R 31 , R 32 , R 51 or R 52 (R k ' is represented by R 13 ' , R 31 ' , R 32 ' , R 51 ' or R 52 ' ; R k '' is represented by R 13 '' , R 31 '' , R 32 '' , R 51 '' or R 52 '' ); wherein R 1 to R 52 '' and R z are as defined in the present specification, and wherein when different groups when the group R 1 to R 52 '' and R z are present in formula I, which may be the same or different.

最佳地，與烷基(亦在烷基芳基、烷基雜環基或烷基環烷基中)、烯基、炔基及O-烷基結合，在本發明之上下文中，經取代理解為任何烷基(亦在烷基芳基、烷基雜環基或烷基環烷基中)、烯基、炔基及O-烷基經以下中之一或多者取代：鹵素(F、Cl、Br、I)、-NRk Rk ' 、-ORk 、-CN、-SRk 、鹵烷基、鹵烷氧基，Rk 由R13 、R31 、R32 、R51 或R52 表示(Rk ' 由R13 ' 、R31 ' 、R32 ' 、R51 ' 或R52 ' 表示；Rk '' 由R13 '' 、R31 '' 、R32 '' 、R51 '' 或R52 '' 表示)；其中R1 至R52 '' 及Rz 如本說明書中所定義，且其中當不同基團R1 至R52 '' 及Rz 同時存在於式I中時，其可相同或不同。Optimally, in combination with alkyl (also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl), alkenyl, alkynyl and O-alkyl, in the context of the present invention, substituted It is understood that any alkyl (also in alkylaryl, alkylheterocyclyl, or alkylcycloalkyl), alkenyl, alkynyl, and O-alkyl groups are substituted with one or more of the following: halogen (F , Cl, Br, I), -NR k R k ' , -OR k , -CN, -SR k , haloalkyl, haloalkoxy, R k consists of R 13 , R 31 , R 32 , R 51 or R 52 means (R k ' is represented by R 13 ' , R 31 ' , R 32 ' , R 51 ' or R 52 ' ; R k '' is represented by R 13 '' , R 31 '' , R 32 '' , R 51 '' or R 52 '' ); wherein R 1 to R 52 '' and R z are as defined in the present specification, and when different groups R 1 to R 52 '' and R z are both present in formula I It can be the same or different.

同一個分子以及同一個碳原子上可能經相同或不同取代基置換超過一次。此包括例如同一C原子上之3個氫經置換，如在CF3 之情況下；或在同一分子之不同位置處經置換，如在例如-CH(OH)-CH=CH-CHCl2 之情況下。The same molecule and the same carbon atom may be substituted more than once with the same or different substituents. This includes, for example, the replacement of 3 hydrogens on the same C atom, as in the case of CF 3 ; or the replacement on different positions of the same molecule, as in the case of -CH (OH) -CH = CH-CHCl 2 under.

在本發明之上下文中，鹵烷基理解為意謂經鹵素(選自F、Cl、Br、I)取代一次或若干次之烷基。其涵蓋例如-CH2 Cl、-CH2 F、-CHCl2 、-CHF2 、-CCl3 、-CF3 及-CH2 -CHCI2 。較佳地，在本發明之上下文中，鹵烷基理解為經鹵素取代之C1-4 烷基，表示經鹵素取代之C1、C2、C3或C4烷基。經鹵素取代之烷基因此較佳為甲基、乙基、丙基及丁基。較佳實例包括-CH2 Cl、-CH2 F、-CHCl2 、-CHF2 及-CF3 。In the context of the present invention, haloalkyl is understood to mean an alkyl substituted one or more times with a halogen (selected from F, Cl, Br, I). It covers, for example, -CH 2 Cl, -CH 2 F, -CHCl 2 , -CHF 2 , -CCl 3 , -CF 3 and -CH 2 -CHCI 2 . Preferably, in the context of the present invention, a haloalkyl group is understood as a C 1-4 alkyl group substituted with a halogen, and represents a C1, C2, C3 or C4 alkyl group substituted with a halogen. Halogen-substituted alkyl groups are therefore preferably methyl, ethyl, propyl and butyl. Preferred examples include -CH 2 Cl, -CH 2 F, -CHCl 2 , -CHF 2 and -CF 3 .

在本發明之上下文中，鹵烷氧基理解為意謂經鹵素(選自F、Cl、Br、I)取代一次或若干次之-O-烷基。其涵蓋例如-OCH2 Cl、-OCH2 F、-OCHCl2 、-OCHF2 、-OCCl3 、-OCF3 及-OCH2 -CHCI2 。較佳地，在本發明之上下文中，鹵烷氧基理解為經鹵素取代之-OC1-4 烷基，表示經鹵素取代之C1、C2、C3或C4烷氧基。經鹵素取代之烷基因此較佳為O-甲基、O-乙基、O-丙基及O-丁基。較佳實例包括-OCH2 Cl、-OCH2 F、-OCHCl2 、-OCHF2 及-OCF3 。In the context of the present invention, haloalkoxy is understood to mean -O-alkyl substituted one or more times with a halogen (chosen from F, Cl, Br, I). It covers, for example, -OCH 2 Cl, -OCH 2 F, -OCHCl 2 , -OCHF 2 , -OCCl 3 , -OCF 3 and -OCH 2 -CHCI 2 . Preferably, in the context of the present invention, haloalkoxy is understood to be -OC 1-4 alkyl substituted with halogen, meaning C1, C2, C3 or C4 alkoxy substituted with halogen. Halogen-substituted alkyl groups are therefore preferably O-methyl, O-ethyl, O-propyl and O-butyl. Preferred examples include -OCH 2 Cl, -OCH 2 F, -OCHCl 2 , -OCHF 2 and -OCF 3 .

在本發明之上下文中，環烷基理解為意謂飽和及不飽和(但並非芳族)環烴(環中無雜原子)，其可未經取代或經一次或若干次取代。此外，C3-4 環烷基表示C3或C4環烷基，C3-5 環烷基表示C3、C4或C5環烷基，C3-6 環烷基表示C3、C4、C5或C6環烷基，C3-7 環烷基表示C3、C4、C5、C6或C7環烷基，C3-8 環烷基表示C3、C4、C5、C6、C7或C8環烷基，C4-5 環烷基表示C4或C5環烷基，C4-6 環烷基表示C4、C5或C6環烷基，C4-7 環烷基表示C4、C5、C6或C7環烷基，C5-6 環烷基表示C5或C6環烷基，且C5-7 環烷基表示C5、C6或C7環烷基。實例為環丙基、2-甲基環丙基、環丙基甲基、環丁基、環戊基、環戊基甲基、環己基、環庚基、環辛基以及金剛烷基。較佳地，在本發明之上下文中，環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；或為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；或為C3-6 環烷基，如環丙基、環丁基、環戊基或環己基，尤其環戊基或環己基。In the context of the present invention, cycloalkyl is understood to mean saturated and unsaturated (but not aromatic) cyclic hydrocarbons (without heteroatoms in the ring), which may be unsubstituted or substituted one or more times. In addition, C 3-4 cycloalkyl means C3 or C4 cycloalkyl, C 3-5 cycloalkyl means C3, C4 or C5 cycloalkyl, and C 3-6 cycloalkyl means C3, C4, C5 or C6 ring Alkyl, C 3-7 cycloalkyl means C3, C4, C5, C6 or C7 cycloalkyl, C 3-8 cycloalkyl means C3, C4, C5, C6, C7 or C8 cycloalkyl, C 4- 5 cycloalkyl means C4 or C5 cycloalkyl, C 4-6 cycloalkyl means C4, C5 or C6 cycloalkyl, C 4-7 cycloalkyl means C4, C5, C6 or C7 cycloalkyl, C 5 -6 cycloalkyl means C5 or C6 cycloalkyl, and C 5-7 cycloalkyl means C5, C6 or C7 cycloalkyl. Examples are cyclopropyl, 2-methylcyclopropyl, cyclopropylmethyl, cyclobutyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cycloheptyl, cyclooctyl and adamantyl. Preferably, in the context of the present invention, a cycloalkyl is a C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; or C 3-7 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; or C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, or Cyclohexyl, especially cyclopentyl or cyclohexyl.

芳基理解為意謂具有至少一個芳族環但即使在僅一個環中亦不具有雜原子的5員至18員(較佳地，6員至14員)單環或多環系統。實例為苯基、萘基、茀蒽基、茀基、萘滿基、二氫茚或茚滿基、9H-茀基或蒽基，其可未經取代或經一次或若干次取代。最佳地，在本發明之上下文中，芳基理解為苯基、萘基或蒽基，較佳為苯基。Aryl is understood to mean a 5- to 18-membered (preferably 6- to 14-membered) monocyclic or polycyclic ring system having at least one aromatic ring but no heteroatoms even in only one ring. Examples are phenyl, naphthyl, fluoranthenyl, fluorenyl, naphthyl, indan or indanyl, 9H-fluorenyl or anthracenyl, which may be unsubstituted or substituted one or more times. Optimally, in the context of the present invention, aryl is understood to be phenyl, naphthyl or anthracenyl, preferably phenyl.

雜環基團(在下文中亦稱為雜環基)理解為意謂尤其5員至18員單環或多環雜環系統，其中至少一個飽和或不飽和環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子。雜環基亦可經一次或若干次取代。Heterocyclic groups (hereinafter also referred to as heterocyclic groups) are understood to mean especially 5- to 18-membered monocyclic or polycyclic heterocyclic systems in which at least one saturated or unsaturated ring contains one or more in the ring A heteroatom selected from the group consisting of nitrogen, oxygen, and / or sulfur. Heterocyclyl can also be substituted one or more times.

雜環基為具有以下一或多個飽和或不飽和環之雜環系統，該等環中之至少一個環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子；較佳為具有以下一或兩個飽和或不飽和環之雜環系統，該等環中之至少一個環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子，更佳選自氧氮雜環庚烷、吡咯啶、咪唑、噁二唑、四唑、氮雜環丁烷、吡啶、嘧啶、哌啶、哌嗪、苯并呋喃、苯并咪唑、吲唑、苯并噻唑、苯并二唑、噻唑、苯并噻唑、四氫哌喃、嗎啉、吲哚啉、呋喃、三唑、異噁唑、吡唑、噻吩、苯并噻吩、吡咯、吡嗪、吡咯并[2,3b]吡啶、喹啉、喹諾酮、異喹啉、四氫噻吩并吡啶、酞嗪、苯并-1,2,5-噻二唑、吲哚、苯并三唑、苯并噁唑、側氧基吡咯啶、苯并二氧雜環戊烷、苯并二噁烷、咔唑、氧雜螺癸烷或噻唑。一般而言，此類雜環基可在環中含有介於3與32個之間的原子(較佳地，在環中含有4至20個原子，或最佳地，在環中含有5至18個原子)。因此，在具有一個飽和或不飽和環之雜環基的情況下，雜環基可在環中含有介於3與12個之間的原子(較佳地，在環中含有4至10個原子，或在環中含有5至8個原子，或在環中含有5至6個原子)。在具有兩個飽和或不飽和環之雜環基的情況下，此類雜環基亦可在兩個環中一起含有介於5與22個之間的原子(較佳地，在兩個環中一起含有6至16個原子，或在兩個環中一起含有7至12個原子，或在兩個環中一起含有8至10個原子)。在具有三個飽和或不飽和環之雜環基的情況下，此類雜環基亦可在3個環中一起含有介於7與32個之間的原子(較佳地，在三個環中一起含有10至22個原子，或在三個環中一起含有12至20個原子，或在三個環中一起含有10至18個原子)。Heterocyclyl is a heterocyclic system having one or more saturated or unsaturated rings, at least one of which contains one or more groups selected from the group consisting of nitrogen, oxygen, and / or sulfur in the ring. Heteroatom; preferably a heterocyclic ring system having one or two of the following saturated or unsaturated rings, at least one of which contains one or more selected from the group consisting of nitrogen, oxygen, and / or sulfur in the ring Heteroatoms of the group, more preferably selected from oxazepine, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzo Imidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropiperan, morpholine, indolinoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, Pyrrole, pyrazine, pyrrolo [2,3b] pyridine, quinoline, quinolone, isoquinoline, tetrahydrothienopyridine, phthalazine, benzo-1,2,5-thiadiazole, indole, benzo Triazole, benzoxazole, pendant oxopyridine, benzodioxolane, benzodioxane, carbazole, oxaspirodecane or thiazole. In general, such heterocyclyls may contain between 3 and 32 atoms in the ring (preferably, 4 to 20 atoms in the ring, or most preferably, 5 to 20 in the ring 18 atoms). Therefore, in the case of a heterocyclic group having a saturated or unsaturated ring, the heterocyclic group may contain 3 to 12 atoms in the ring (preferably, 4 to 10 atoms in the ring , Or contains 5 to 8 atoms in the ring, or 5 to 6 atoms in the ring). In the case of heterocyclic groups having two saturated or unsaturated rings, such heterocyclic groups may also contain between 5 and 22 atoms in both rings (preferably, in the two rings Contains 6 to 16 atoms together, or 7 to 12 atoms together in two rings, or 8 to 10 atoms together in two rings). In the case of a heterocyclic group having three saturated or unsaturated rings, such heterocyclic groups may also contain 7 to 32 atoms together in 3 rings (preferably, in three rings Contains 10 to 22 atoms together, or 12 to 20 atoms together in three rings, or 10 to 18 atoms together in three rings).

實例包括非芳族雜環基，諸如四氫哌喃、氧氮雜環庚烷、嗎啉、哌啶、吡咯啶以及雜芳基，諸如呋喃、苯并呋喃、噻吩、苯并噻吩、吡咯、吡啶、嘧啶、吡嗪、喹啉、異喹啉、酞嗪、噻唑、苯并噻唑、吲哚、苯并三唑、咔唑及喹唑啉。Examples include non-aromatic heterocyclic groups such as tetrahydropiperan, oxazepine, morpholine, piperidine, pyrrolidine, and heteroaryl groups such as furan, benzofuran, thiophene, benzothiophene, pyrrole, Pyridine, pyrimidine, pyrazine, quinoline, isoquinoline, phthalazine, thiazole, benzothiazole, indole, benzotriazole, carbazole and quinazoline.

如本文所理解，雜環基內部之子組包括雜芳基及非芳族雜環基。
- 雜芳基(等效於雜芳族基團或芳族雜環基，或亦等效於「含有至少一個含有至少一個雜原子之芳族環的雜環基」)為具有以下一或多個環之芳族5員至18員單環或多環雜環系統，該等環中之至少一個芳族環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子；較佳為具有以下一或兩個環之5員至18員單環或多環芳族雜環系統，該等環中之至少一個芳族環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子，更佳選自呋喃、苯并呋喃、噻吩、苯并噻吩、吡咯、吡啶、嘧啶、吡嗪、喹啉、異喹啉、酞嗪、苯并噻唑、吲哚、苯并三唑、咔唑、喹唑啉、噻唑、咪唑、吡唑、噁唑、噻吩及苯并咪唑；
- 非芳族雜環基為具有以下一或多個環之5員至18員單環或多環雜環系統，該等環中之至少一個環(則其中此(或此等)環不為芳族的)在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子；較佳為具有以下一或兩個環之5員至18員單環或多環雜環系統，該等環中之一個或兩個環(則其中此一或兩個環不為芳族的)在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子，更佳選自氧氮雜環庚烷、吡咯啶、哌啶、哌嗪、四氫哌喃、嗎啉、吲哚啉、側氧基吡咯啶、苯并二噁烷，尤其為苯并二噁烷、嗎啉、四氫哌喃、哌啶、側氧基吡咯啶及吡咯啶。As understood herein, subgroups within a heterocyclyl include heteroaryl and non-aromatic heterocyclyl.
-Heteroaryl (equivalent to a heteroaromatic group or an aromatic heterocyclic group, or equivalent to "a heterocyclic group containing at least one aromatic ring containing at least one heteroatom") is one or more of A 5- to 18-membered monocyclic or polycyclic heterocyclic ring system of each ring, at least one of the aromatic rings in the rings containing one or more groups selected from the group consisting of nitrogen, oxygen, and / or sulfur Heteroatoms; preferably 5- to 18-membered monocyclic or polycyclic aromatic heterocyclic ring systems having one or two of the following rings, at least one of the aromatic rings in the rings containing one or more of the rings Heteroatom selected from the group consisting of nitrogen, oxygen and / or sulfur, more preferably selected from furan, benzofuran, thiophene, benzothiophene, pyrrole, pyridine, pyrimidine, pyrazine, quinoline, isoquinoline, phthalazine , Benzothiazole, indole, benzotriazole, carbazole, quinazoline, thiazole, imidazole, pyrazole, oxazole, thiophene, and benzimidazole;
-Non-aromatic heterocyclyl is a 5- to 18-membered monocyclic or polycyclic heterocyclic ring system having one or more of the following rings, at least one of the rings (thus where the (or such) ring is not Aromatic) contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen, and / or sulfur in the ring; preferably 5 to 18 members of the following one or two rings are monocyclic or polycyclic Heterocyclic system, one or two of the rings (then one or two of which are not aromatic) contains one or more groups selected from the group consisting of nitrogen, oxygen and / or sulfur in the ring Heteroatoms are more preferably selected from oxazepine, pyrrolidine, piperidine, piperazine, tetrahydropiperan, morpholine, indolino, pendant oxopyridine, benzodioxane, especially Benzodioxane, morpholine, tetrahydropiran, piperidine, pendant oxypyrridine and pyrrolidine.

較佳地，在本發明之上下文中，雜環基定義為具有以下一或多個飽和或不飽和環之5員至18員單環或多環雜環系統，該等環中之至少一個環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子。較佳地，其為具有以下一或兩個飽和或不飽和環之5員至18員單環或多環雜環系統，該等環中之至少一個環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子。Preferably, in the context of the present invention, a heterocyclyl is defined as a 5- to 18-membered monocyclic or polycyclic heterocyclic system having one or more of the following saturated or unsaturated rings, at least one of the rings The ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen, and / or sulfur. Preferably, it is a 5- to 18-membered monocyclic or polycyclic heterocyclic ring system having one or two of the following saturated or unsaturated rings. At least one of the rings contains one or more options in the ring. A heteroatom in a group consisting of nitrogen, oxygen, and / or sulfur.

雜環基之較佳實例包括氧氮雜環庚烷、吡咯啶、咪唑、噁二唑、四唑、吡啶、嘧啶、哌啶、哌嗪、苯并呋喃、苯并咪唑、吲唑、苯并二唑、噻唑、苯并噻唑、四氫哌喃、嗎啉、吲哚啉、呋喃、三唑、異噁唑、吡唑、噻吩、苯并噻吩、吡咯、吡嗪、吡咯并[2,3b]吡啶、喹啉、異喹啉、四氫異喹啉、酞嗪、苯并-1,2,5-噻二唑、吲哚、苯并三唑、苯并噁唑、側氧基吡咯啶、嘧啶、苯并二氧雜環戊烷、苯并二噁烷、咔唑及喹唑啉，尤其為吡啶、吡嗪、吲唑、苯并二噁烷、噻唑、苯并噻唑、嗎啉、四氫哌喃、吡唑、咪唑、哌啶、噻吩、吲哚、苯并咪唑、吡咯并[2,3b]吡啶、苯并噁唑、側氧基吡咯啶、嘧啶、氧氮雜環庚烷及吡咯啶。Preferred examples of heterocyclyl include oxazepine, pyrrolidine, imidazole, oxadiazole, tetrazole, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzo Diazole, thiazole, benzothiazole, tetrahydropiperan, morpholine, indolin, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo [2,3b ] Pyridine, quinoline, isoquinoline, tetrahydroisoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, pendant oxopyrrolidine , Pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline, especially pyridine, pyrazine, indazole, benzodioxane, thiazole, benzothiazole, morpholine, Tetrahydropiran, pyrazole, imidazole, piperidine, thiophene, indole, benzimidazole, pyrrolo [2,3b] pyridine, benzoxazole, pendant oxygen pyrrolidine, pyrimidine, oxazepine And pyrrolidine.

在本發明之上下文中，側氧基吡咯啶理解為意謂吡咯啶-2-酮。In the context of the present invention, pendant pyrrolidine is understood to mean pyrrolidin-2-one.

與芳族雜環基(雜芳基)、非芳族雜環基、芳基及環烷基結合，當環系統同時屬於上文環定義中之兩者或超過兩者時，則環系統在至少一個芳族環含有雜原子的情況下首先定義為芳族雜環基(雜芳基)。若無芳環含有雜原子，則環系統在至少一個非芳族環含有雜原子的情況下定義為非芳族雜環基。若無非芳族環含有雜原子，則環系統在其含有至少一個芳基環的情況下定義為芳基。若不存在芳基，則環系統在存在至少一個非芳族環烴的情況下定義為環烷基。Combined with aromatic heterocyclyl (heteroaryl), non-aromatic heterocyclyl, aryl and cycloalkyl, when the ring system belongs to two or more of the above ring definitions, the ring system is When at least one aromatic ring contains a hetero atom, it is first defined as an aromatic heterocyclic group (heteroaryl). If no aromatic ring contains heteroatoms, the ring system is defined as a non-aromatic heterocyclic group if at least one non-aromatic ring contains a heteroatom. If no non-aromatic ring contains heteroatoms, the ring system is defined as an aryl group if it contains at least one aryl ring. If no aryl group is present, the ring system is defined as a cycloalkyl group in the presence of at least one non-aromatic cyclic hydrocarbon.

在本發明之上下文中，烷基芳基理解為意謂經由C1-6 烷基(參見上文)連接至另一原子之芳基(參見上文)，該C1-6 烷基可為分支鏈或直鏈且未經取代或經一次或若干次取代。較佳地，烷基芳基理解為意謂經由1至4個(-CH2 -)基團連接至另一原子之芳基(參見上文)。最佳地，烷基芳基為苄基(亦即-CH2 -苯基)。In the context of the present invention, an alkylaryl group is understood to mean an aryl group (see above) attached to another atom via a C1-6 alkyl group (see above), which C1-6 alkyl group may be Branched or linear and unsubstituted or substituted one or more times. Preferably, alkylaryl is understood to mean an aryl group attached to another atom via 1 to 4 (-CH 2- ) groups (see above). Optimally, the alkylaryl group is benzyl (i.e. -CH 2 - phenyl).

在本發明之上下文中，烷基雜環基理解為意謂經由C1-6 烷基(參見上文)連接至另一原子之雜環基，該C1-6 烷基可為分支鏈或直鏈且未經取代或經一次或若干次取代。較佳地，烷基雜環基理解為意謂經由1至4個(-CH2 -)基團連接至另一原子之雜環基(參見上文)。最佳地，烷基雜環基為-CH2 -吡啶。In the context of the present invention, an alkylheterocyclyl is understood to mean a heterocyclyl attached to another atom via a C1-6 alkyl (see above), which C1-6 alkyl may be branched or Linear and unsubstituted or substituted one or more times. Preferably, an alkylheterocyclyl is understood to mean a heterocyclyl group attached to another atom via 1 to 4 (-CH 2- ) groups (see above). Most preferably, the alkylheterocyclyl is -CH 2 -pyridine.

在本發明之上下文中，烷基環烷基理解為意謂經由C1-6 烷基(參見上文)連接至另一原子之環烷基，該C1-6 烷基可為分支鏈或直鏈且未經取代或經一次或若干次取代。較佳地，烷基環烷基理解為意謂經由1至4個(-CH2 -)基團連接至另一原子之環烷基(參見上文)。最佳地，烷基環烷基為-CH2 -環丙基。In the context of the present invention, alkylcycloalkyl is understood to mean a cycloalkyl group attached to another atom via a C 1-6 alkyl group (see above), which C 1-6 alkyl group may be branched or Linear and unsubstituted or substituted one or more times. Preferably, alkylcycloalkyl is understood to mean a cycloalkyl group connected to another atom via 1 to 4 (-CH 2- ) groups (see above). Most preferably, the alkylcycloalkyl is -CH 2 -cyclopropyl.

較佳地，芳基為單環芳基。更佳地，芳基為5員、6員或7員單環芳基。甚至更佳地，芳基為5員或6員單環芳基。Preferably, the aryl group is a monocyclic aryl group. More preferably, the aryl group is a 5-membered, 6-membered, or 7-membered monocyclic aryl group. Even more preferably, the aryl is a 5- or 6-membered monocyclic aryl.

較佳地，雜芳基為單環雜芳基。更佳地，雜芳基為5員、6員或7員單環雜芳基。甚至更佳地，雜芳基為5員或6員單環雜芳基。Preferably, the heteroaryl is a monocyclic heteroaryl. More preferably, the heteroaryl is a 5-membered, 6-membered, or 7-membered monocyclic heteroaryl. Even more preferably, the heteroaryl is a 5- or 6-membered monocyclic heteroaryl.

較佳地，非芳族雜環基為單環非芳族雜環基。更佳地，非芳族雜環基為4員、5員、6員或7員單環非芳族雜環基。甚至更佳地，非芳族雜環基為5員或6員單環非芳族雜環基。Preferably, the non-aromatic heterocyclic group is a monocyclic non-aromatic heterocyclic group. More preferably, the non-aromatic heterocyclic group is a 4-membered, 5-membered, 6-membered, or 7-membered monocyclic non-aromatic heterocyclic group. Even more preferably, the non-aromatic heterocyclic group is a 5- or 6-membered monocyclic non-aromatic heterocyclic group.

較佳地，環烷基為單環環烷基。更佳地，環烷基為3員、4員、5員、6員、7員或8員單環環烷基。甚至更佳地，環烷基為3員、4員、5員或6員單環環烷基。Preferably, the cycloalkyl is a monocyclic cycloalkyl. More preferably, the cycloalkyl group is a 3-, 4-, 5-, 6-, 7-, or 8-membered monocyclic cycloalkyl group. Even more preferably, the cycloalkyl is a 3-, 4-, 5- or 6-membered monocyclic cycloalkyl.

與芳基(包括烷基-芳基)、環烷基(包括烷基-環烷基)或雜環基(包括烷基-雜環基)結合，除非另外定義，否則經取代理解為芳基或烷基-芳基、環烷基或烷基-環烷基；雜環基或烷基-雜環基之環系統經以下中之一或多者取代：鹵素(F、Cl、Br、I)、-Rk 、-ORk 、-CN、-NO2 、-NRk Rk ' 、-C(O)ORk 、NRk C(O)Rk ' 、-C(O)NRk Rk ' 、-NRk S(O)2 Rk ' 、=O、-OCH2 CH2 OH、-NRk C(O)NRk ' Rk '' 、-S(O)2 NRk Rk ' 、-NRk S(O)2 NRk ' Rk '' 、鹵烷基、鹵烷氧基、-SRk 、-S(O)Rk 、-S(O)2 Rk 或C(CH3 )ORk 、或經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基、經取代或未經取代之烷基雜環基，其中Rk 、Rk ' 及Rk '' 獨立地為H或飽和或不飽和、直鏈或分支鏈、經取代或未經取代之C1-6 烷基；飽和或不飽和、直鏈或分支鏈、經取代或未經取代之C1-6 烷基；飽和或不飽和、直鏈或分支鏈、經取代或未經取代之-O-C1-6 烷基(烷氧基)；飽和或不飽和、直鏈或分支鏈、經取代或未經取代之-S-C1-6 烷基；飽和或不飽和、直鏈或分支鏈、經取代或未經取代之-C(O)-C1-6 烷基-基團；飽和或不飽和、直鏈或分支鏈、經取代或未經取代之-C(O)-O-C1-6 烷基-基團；經取代或未經取代之芳基或烷基-芳基；經取代或未經取代之環烷基或烷基-環烷基；經取代或未經取代之雜環基或烷基-雜環基，Rk 為R11 、R14 、R21 、R31 或R51 中之一者(Rk ' 為R11 ' 、R14 ' 、R21 ' 、R31 ' 或R51 ' 中之一者，Rk '' 為R11 '' 、R14 '' 、R21 '' 、R31 '' 或R51 '' 中之一者)； 其中R1 至R52 '' 及Rz 如本說明書中所定義，且其中當在式I中同時存在不同基團R1 至R52 '' 及Rz 時，其可相同或不同。In combination with aryl (including alkyl-aryl), cycloalkyl (including alkyl-cycloalkyl) or heterocyclyl (including alkyl-heterocyclyl), unless otherwise defined, substituted is understood to be aryl Or alkyl-aryl, cycloalkyl, or alkyl-cycloalkyl; heterocyclic or alkyl-heterocyclyl ring systems are substituted with one or more of the following: halogen (F, Cl, Br, I ), -R k , -OR k , -CN, -NO 2 , -NR k R k ' , -C (O) OR k , NR k C (O) R k ' , -C (O) NR k R k ' , -NR k S (O) 2 R k ' , = O, -OCH 2 CH 2 OH, -NR k C (O) NR k ' R k '' , -S (O) 2 NR k R k ' , -NR k S (O) 2 NR k ' R k '' , haloalkyl, haloalkoxy, -SR k , -S (O) R k , -S (O) 2 R k or C ( CH 3 ) OR k , or substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylheterocyclyl, where R k , R k ' and Rk ''are independently H or saturated or unsaturated, straight or branched, substituted or unsubstituted C 1-6 alkyl; saturated or unsaturated, straight or branched, substituted or non-substituted C 1-6 alkyl group; a saturated or unsaturated, straight or branched, Substituted or non-substituted -OC 1-6 alkyl (alkoxy); a saturated or unsaturated, linear or branched, substituted or non-substituted -SC 1-6 alkyl group; a saturated or unsaturated, Straight or branched, substituted or unsubstituted -C (O) -C 1-6 alkyl-groups; saturated or unsaturated, straight or branched, substituted or unsubstituted -C ( O) -OC 1-6 alkyl-group; substituted or unsubstituted aryl or alkyl-aryl; substituted or unsubstituted cycloalkyl or alkyl-cycloalkyl; substituted or the unsubstituted heterocyclic alkyl group or - a heterocyclic group, R k is R 11, R 14, R 21 , R 31 R 51 or one of those (R k 'to R 11', R 14 ', R 21 ', R 31' or R 51 'in one of those, R k' 'to R 11'', R 14' ', R 21'', R 31'' or R 51' 'in one of those); wherein R 1 to R 52 'and R z as defined in the specification, and wherein when present in formula I different radicals R 1 to R 52 simultaneously''and R z, which may be the same or different.

最佳地，與芳基(包括烷基-芳基)、環烷基(包括烷基-環烷基)或雜環基(包括烷基-雜環基)結合，在本發明之上下文中，經取代理解為經取代之任何芳基、環烷基及雜環基(亦在烷基芳基、烷基環烷基或烷基雜環基)中經以下中之一或多者取代：鹵素(F、Cl、Br、I)、-Rk 、-ORk 、-CN、-NO2 、-NRk Rk ''' 、NRk C(O)Rk ' 、-NRk S(O)2 Rk ' 、-S(O)2 NRk Rk ' 、-NRk C(O)NRk ' Rk '' 、鹵烷基、鹵烷氧基、-SRk 、-S(O)Rk 或S(O)2 Rk 、或經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基、經取代或未經取代之烷基雜環基，Rk 為R11 、R14 、R21 、R31 或R51 中之一者(Rk ' 為R11 ' 、R14 ' 、R21 ' 、R31 ' 或R51 ' 中之一者； Rk '' 為R11 '' 、R14 '' 、R21 '' 、R31' ' 或R51 '' 中之一者)； 其中R1 至R52 '' 及Rz 如本說明書中所定義，且其中當在式I中同時存在不同基團R1 至R52 '' 及Rz 時，其可相同或不同。Optimally, in combination with aryl (including alkyl-aryl), cycloalkyl (including alkyl-cycloalkyl) or heterocyclyl (including alkyl-heterocyclyl), in the context of the present invention, Substituted is understood to be substituted for any aryl, cycloalkyl, and heterocyclyl (also in alkylaryl, alkylcycloalkyl, or alkylheterocyclyl) substituted with one or more of the following: halogen (F, Cl, Br, I), -R k , -OR k , -CN, -NO 2 , -NR k R k ''' , NR k C (O) R k ' , -NR k S (O ) 2 R k ' , -S (O) 2 NR k R k ' , -NR k C (O) NR k ' R k '' , haloalkyl, haloalkoxy, -SR k , -S (O ) R k or S (O) 2 R k , or substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, substituted or unsubstituted alkylheterocyclyl , R k is one of R 11 , R 14 , R 21 , R 31 or R 51 (R k ' is one of R 11 ′ , R 14 ′ , R 21 ′ , R 31 ′ or R 51 ′ ; R k '' is one of R 11 '' , R 14 '' , R 21 '' , R 31 ' ′, or R 51 '' ) ; wherein R 1 to R 52 '' and R z are as described in this specification defined, and wherein when in formula I different radicals R 1 to R 52 '' and R z exist, It may be the same or different.

與環烷基(包括烷基-環烷基)或雜環基(包括烷基雜環基) (即非芳族雜環基(包括非芳族烷基-雜環基))結合，除非另外定義，否則經取代亦理解為意謂環烷基或烷基-環烷基；非芳族雜環基或非芳族烷基-雜環基經取代(產生螺環結構)及/或經=O取代。In combination with cycloalkyl (including alkyl-cycloalkyl) or heterocyclyl (including alkylheterocyclyl) (i.e. non-aromatic heterocyclyl (including non-aromatic alkyl-heterocyclyl)), unless otherwise Definition, otherwise substituted is also understood to mean cycloalkyl or alkyl-cycloalkyl; non-aromatic heterocyclyl or non-aromatic alkyl-heterocyclyl via Substitution (producing a spiro ring structure) and / or substitution with = 0.

環系統為由至少一個具有連接原子之環組成的系統，但亦包括其中兩個或超過兩個具有連接原子之環接合的系統，其中「接合」意謂各別環共有一個原子(如螺環結構)、兩個或超過兩個原子，該或該等原子為兩個接合環之成員。A ring system is a system composed of at least one ring with connected atoms, but also includes a system in which two or more rings with connected atoms are joined, where "joined" means that each ring has one atom in common (such as a spiro ring) Structure), two or more atoms that are members of two bonded rings.

術語「離去基」意謂在異質鍵裂解中與電子對分離之分子片段。離去基可為陰離子或中性分子。常見陰離子性離去基為鹵離子，諸如Cl-、Br-及I-，及磺酸酯，諸如甲苯磺酸酯(TsO-)或甲磺酸酯。The term "leaving group" means a molecular fragment that is separated from an electron pair during the cleavage of a hetero bond. The leaving group can be an anionic or neutral molecule. Common anionic leaving groups are halide ions, such as Cl-, Br-, and I-, and sulfonates, such as tosylate (TsO-) or mesylate.

術語「鹽(salt)」應理解為意謂任何形式的根據本發明使用之活性化合物，其中其採用離子形式、或帶電荷且與相對離子(陽離子或陰離子)偶合、或處於溶液中。此亦應理解為活性化合物與其他分子及離子之複合物，尤其經由離子相互作用之複合物。The term "salt" is understood to mean any form of the active compound used according to the invention, wherein it is in ionic form, or is charged and coupled with a counter ion (cation or anion), or is in solution. This should also be understood as a complex of the active compound with other molecules and ions, especially a complex that interacts via ions.

在本發明之上下文中，術語「生理學上可接受之鹽」意謂在以恰當方式用於治療的情況下，尤其在用於或應用於人類及/或哺乳動物的情況下，生理學上耐受(大部分時間意謂無毒性，尤其並非由相對離子所導致)之任何鹽。In the context of the present invention, the term "physiologically acceptable salt" means that physiologically, when used in a proper manner for treatment, especially when used or applied to humans and / or mammals Any salt that is tolerant (most of the time means non-toxic, especially not caused by the opposite ion).

此等生理學上可接受之鹽可用陽離子或鹼形成，且在本發明之上下文中，理解為意謂根據本發明使用之至少一種化合物(通常為(脫質子化之)酸)作為陰離子與至少一種生理學上耐受(尤其在用於人類及/或哺乳動物的情況下)之(較佳無機)陽離子的鹽。鹼金屬及鹼土金屬之鹽以及與NH4 之彼等鹽尤其較佳，但尤其為(單)或(二)鈉、(單)或(二)鉀、鎂或鈣鹽。These physiologically acceptable salts can be formed with cations or bases, and in the context of the present invention are understood to mean that at least one compound (usually a (deprotonated) acid) used according to the present invention as an anion and at least A salt of a (preferably inorganic) cation that is physiologically tolerated, especially for use in humans and / or mammals. Salts of alkali metals and alkaline earth metals and their salts with NH 4 are particularly preferred, but especially are (mono) or (di) sodium, (mono) or (di) potassium, magnesium or calcium salts.

生理學上可接受之鹽亦可用陰離子或酸形成，且在本發明之上下文中，理解為意謂根據本發明使用之至少一種化合物作為陽離子與至少一種生理學上耐受(尤其在用於人類及/或哺乳動物的情況下)之陰離子的鹽。詳言之，在本發明之上下文中，此理解為用生理學上耐受之酸形成的鹽，換言之，特定活性化合物與生理學上耐受(尤其在用於人類及/或哺乳動物的情況下)之無機或有機酸的鹽。特定酸之生理學上耐受之鹽的實例為以下酸之鹽：鹽酸、氫溴酸、硫酸、甲磺酸、甲酸、乙酸、乙二酸、丁二酸、蘋果酸、酒石酸、杏仁酸、反丁烯二酸、乳酸或檸檬酸。Physiologically acceptable salts can also be formed with anions or acids, and in the context of the present invention are understood to mean that at least one compound used according to the present invention is cationic and at least one physiologically tolerable (especially for use in human And / or in the case of mammals). In particular, in the context of the present invention, this is understood to mean salts formed with physiologically tolerated acids, in other words, specific active compounds are physiologically tolerated (especially in the case of use in humans and / or mammals) (Below) salts of inorganic or organic acids. Examples of physiologically tolerated salts of specific acids are the salts of the following acids: hydrochloric acid, hydrobromic acid, sulfuric acid, methanesulfonic acid, formic acid, acetic acid, succinic acid, succinic acid, malic acid, tartaric acid, mandelic acid, Fumaric acid, lactic acid or citric acid.

本發明化合物可以結晶形式或以自由化合物(如自由鹼或酸)形式存在。The compounds of the invention may exist in crystalline form or as a free compound, such as a free base or acid.

本身為如上文所定義之本發明化合物(如根據通式I之化合物)之溶劑合物的任何化合物理解為亦由本發明之範疇所覆蓋。溶劑化方法一般為此項技術中已知的。適合之溶劑合物為醫藥學上可接受之溶劑合物。本發明之術語「溶劑合物」應理解為意謂任何形式之本發明活性化合物，其中此化合物已經由非共價結合另一分子(最可能為極性溶劑)而與其連接。尤其較佳實例包括水合物及醇合物，如甲醇合物或乙醇合物。Any compound which is itself a solvate of a compound of the invention as defined above (such as a compound according to Formula I) is understood to also be covered by the scope of the invention. Solvation methods are generally known in the art. Suitable solvates are pharmaceutically acceptable solvates. The term "solvate" according to the present invention is understood to mean any form of the active compound of the present invention, in which the compound has been attached thereto by non-covalent bonding to another molecule (most likely a polar solvent). Particularly preferred examples include hydrates and alcoholates, such as methanolate or ethanolate.

本身為如上文所定義之本發明化合物(如根據通式I之化合物)之前藥的任何化合物理解為亦由本發明之範疇所覆蓋。術語「前藥」以其最廣泛之含義進行使用，且涵蓋活體內轉化為本發明化合物之彼等衍生物。此類衍生物應易於由熟習此項技術者想到，且視存在於分子中之官能基而定，包括(但不限於)本發明化合物之以下衍生物：酯、胺基酸酯、磷酸酯、金屬鹽磺酸酯、胺基甲酸酯及醯胺。產生既定起效化合物之前藥的熟知方法之實例為熟習此項技術者已知的，且可見於例如Krogsgaard-Larsen等人 「Textbook of Drug design and Discovery」 Taylor & Francis (2002年4月)中。Any compound which is itself a prodrug of a compound of the invention as defined above (such as a compound according to Formula I) is understood to also be covered by the scope of the invention. The term "prodrug" is used in its broadest sense and encompasses in vivo conversion of these derivatives into compounds of the invention. Such derivatives should be easily conceivable by those skilled in the art and depend on the functional groups present in the molecule, including (but not limited to) the following derivatives of the compounds of the invention: esters, amino esters, phosphates, Metal salt sulfonates, carbamates and amidines. Examples of well-known methods for generating prodrugs of a given active compound are known to those skilled in the art and can be found in, for example, Krogsgaard-Larsen et al. "Textbook of Drug Design and Discovery" Taylor & Francis (April 2002).

本身為如上文所定義之本發明化合物(如根據通式I之化合物)之N-氧化物的任何化合物理解為亦由本發明之範疇所覆蓋。Any compound which is itself an N-oxide of a compound of the invention as defined above (such as a compound according to Formula I) is understood to also be covered by the scope of the invention.

除非另外陳述，否則本發明之化合物亦意欲包括不同之處僅在於存在一或多個經同位素增濃之原子的化合物。舉例而言，除氫由氘或氚置換、或碳由經13 C或14 C增濃之碳置換、或氮由經15 N增濃之氮置換以外具有本發明結構的化合物處於本發明之範疇內。此將尤其亦適用於上文所描述之條件，以使得在式中任何提及氫或任何「H」亦將覆蓋氘或氚。Unless stated otherwise, the compounds of the present invention are also intended to include compounds that differ only in the presence of one or more isotopically enriched atoms. For example, compounds having the structure of the present invention fall within the scope of the present invention, except that hydrogen is replaced by deuterium or tritium, or carbon is replaced by 13 C or 14 C-enriched carbon, or nitrogen is replaced by 15 N-enriched nitrogen. Inside. This will especially apply to the conditions described above, so that any reference to hydrogen or any "H" in the formula will also cover deuterium or tritium.

式(I)化合物以及其鹽或該等化合物之溶劑合物較佳呈醫藥學上可接受或基本上純之形式。醫藥學上可接受之形式尤其意謂在不包括正常醫藥添加劑(諸如稀釋劑及載劑)且不包括在正常劑量水準下視為有毒之物質的情況下具有醫藥學上可接受之純度水準。藥物之純度水準較佳高於50%、更佳高於70%、最佳高於90%。在一個較佳實施例中，其為高於95%之式(I)化合物或其鹽。此亦適用於其溶劑合物或前藥。The compounds of formula (I) and their salts or solvates of these compounds are preferably in a pharmaceutically acceptable or substantially pure form. A pharmaceutically acceptable form means, in particular, that it has a pharmaceutically acceptable level of purity without including normal pharmaceutical additives such as diluents and carriers and excluding substances deemed toxic at normal dosage levels. The purity level of the drug is preferably higher than 50%, more preferably higher than 70%, and most preferably higher than 90%. In a preferred embodiment, it is greater than 95% of a compound of formula (I) or a salt thereof. This also applies to their solvates or prodrugs.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
-X-R1 係選自-R1 、-[C(Ra Rb )]p -R1 、-[CH2 ]p C(O)[CH2 ]q -R1 、-[CH2 ]p C(O)N(Rz )[CH2 ]q -R1 、-[CH2 ]p N(Rz )C(O)[CH2 ]q -R1 及-[CH2 ]p N(Rz )[CH2 ]q -R1 ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
-XR 1 is selected from -R 1 ,-[C (R a R b )] p -R 1 ,-[CH 2 ] p C (O) [CH 2 ] q -R 1 ,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -R 1 ,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -R 1 and-[CH 2 ] p N ( R z ) [CH 2 ] q -R 1 ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein, alternatively, R a and R b together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl group;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
X係選自一鍵、-[CH2 ]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
X is selected from one bond,-[CH 2 ] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
Rz 係選自氫及經取代或未經取代之C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R z is selected from hydrogen and substituted or unsubstituted C 1-6 alkyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
p為0、1、2、3、4或5；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
p is 0, 1, 2, 3, 4 or 5;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
q為0、1、2、3、4或5；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
q is 0, 1, 2, 3, 4 or 5;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
n為0或1；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
n is 0 or 1;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
Y1 為-C(R10 R10 ' )-；
其中R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 及R10 ' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
Y 1 is -C (R 10 R 10 ' )-;
Wherein R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
Alternatively, R 10 and R 10 ′ may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
Y1 為-C(R10 R10 ' )-；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
Y 1 is -C (R 10 R 10 ' )-;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 及R10 ' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
Alternatively, R 10 and R 10 ′ may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R10 及R10 ' 與其所連接之碳原子形成經取代或未經取代之環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 10 and R 10 ′ form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
Y2 為-C(R10 '' R10 ''' )-；
其中R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 '' 及R10 ''' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
Y 2 is -C (R 10 '' R 10 ''')-;
Wherein R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted the substituted C 2-6 alkynyl group;
Alternatively, R 10 '' and R 10 '''may form a substituted or unsubstituted cycloalkyl group with the carbon atom they are attached;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
Y2 為-C(R10 '' R10 ''' )-；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
Y 2 is -C (R 10 '' R 10 ''')-;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，R10 '' 及R10 ''' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
Alternatively, R 10 '' and R 10 '''may form a substituted or unsubstituted cycloalkyl group with the carbon atom they are attached;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R10 '' 及R10 ''' 與其所連接之碳原子形成經取代或未經取代之環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 10 '' and R 10 ''' and the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl group;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R2 係選自經取代或未經取代之芳基及經取代或未經取代之芳族雜環基，
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted aromatic heterocyclic group,
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R3 為經取代或未經取代之C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 3 is substituted or unsubstituted C 1-6 alkyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 5 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl , Substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheteroaryl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 5 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl 2, substituted or unsubstituted alkylaryl groups and substituted or unsubstituted alkylheteroaryl groups;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R10 及R10 ' 獨立地選自氫及經取代或未經取代之C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 10 and R 10 ′ are independently selected from hydrogen and substituted or unsubstituted C 1-6 alkyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R10 及R10 ' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 10 and R 10 ′ may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R10 '' 及R10 ''' 獨立地選自氫及經取代或未經取代之C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 10 '' and R 10 '''are independently selected from hydrogen and a substituted or unsubstituted alkyl group of C 1-6;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R10 '' 及R10 ''' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 10 '' and R 10 ''' may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 21, R 21 'and R 21' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R21 、R21 ' 及R21 '' 獨立地選自氫及經取代或未經取代之C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 21, R 21 'and R 21' 'are independently selected from hydrogen and a substituted or unsubstituted alkyl group of C 1-6;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R31 、R31 ' 及R31 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 31, R 31 'and R 31' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R31 、R31 ' 及R31 '' 獨立地選自氫及經取代或未經取代之C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 31, R 31 'and R 31' 'are independently selected from hydrogen and a substituted or unsubstituted alkyl group of C 1-6;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R32 及R32 ' 獨立地選自氫及經取代或未經取代之C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 32 and R 32 'are independently selected from hydrogen and substituted or unsubstituted C 1-6 alkyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R41 、R41 ' 及R41 '' 獨立地選自氫及經取代或未經取代之C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 41, R 41 'and R 41' 'are independently selected from hydrogen and a substituted or unsubstituted alkyl group of C 1-6;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R51 、R51 ' 及R51 '' 獨立地選自氫及經取代或未經取代之C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 51, R 51 'and R 51' 'are independently selected from hydrogen and a substituted or unsubstituted alkyl group of C 1-6;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 52 and R 52 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R52 及R52 ' 獨立地選自氫及經取代或未經取代之C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 52 and R 52 'are independently selected from hydrogen and substituted or unsubstituted C 1-6 alkyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R13 及R13 ' 獨立地選自氫及未經取代之C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 13 and R 13 ′ are independently selected from hydrogen and unsubstituted C 1-6 alkyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl, unsubstituted alkenyl group of C 2-6, unsubstituted C 2-6 alkynyl group of, Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic groups;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl group, the unsubstituted aryl, unsubstituted cycloalkyl, and the unsubstituted heterocyclic group of ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
其中R2 中之芳基或雜環基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
Wherein, if an aryl or heterocyclic group in R 2 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
其中，
R3 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR31 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR31 R31 ' ；
其中R3 中之環烷基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R31 、-OR31 、-NO2 、-NR31 R31 ' 、-NR31 C(O)R31 ' 、-NR31 S(O)2 R31 ' 、-S(O)2 NR31 R31 ' 、-NR31 C(O)NR31 ' R31 '' 、-SR31 、-S(O)R31 、-S(O)2 R31 、-CN、鹵烷基、鹵烷氧基、-C(O)OR31 、-C(O)NR31 R31 ' 、-OCH2 CH2 OR31 、-NR31 S(O)2 NR31 ' R31 ' 及-C(CH3 )2 OR31 ；
其中R31 、R31 ' 及R31 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
among them,
If an alkyl, alkenyl or alkynyl group as defined in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: -OR 31 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 31 R 31 ' ;
Wherein, if the cycloalkyl group in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 31 , -OR 31 , -NO 2 , -NR 31 R 31 ' , -NR 31 C (O) R 31 ' , -NR 31 S (O) 2 R 31 ' , -S (O) 2 NR 31 R 31 ' , -NR 31 C (O) NR 31 ' R 31 '' , -SR 31 , -S (O) R 31 , -S (O) 2 R 31 , -CN, haloalkyl, haloalkoxy, -C (O) OR 31 , -C (O) NR 31 R 31 ' ,- OCH 2 CH 2 OR 31 , -NR 31 S (O) 2 NR 31 ' R 31 ' and -C (CH 3 ) 2 OR 31 ;
Wherein R 31 , R 31 ′, and R 31 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
R3' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR32 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR32 R32 ' ；
其中R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物形式，或其對應之鹽，或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
If an alkyl, alkenyl or alkynyl group as defined in R 3 ′ is substituted, it is substituted with one or more substituents selected from: -OR 32 , halogen, -CN, haloalkyl, haloalkoxy And -NR 32 R 32 ' ;
Wherein R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
It optionally takes the form of one stereoisomer (preferably, an enantiomer or diastereomer), a racemate, or at least two stereoisomers (preferably, an Enantiomers and / or diastereomers) in the form of a mixture at any mixing ratio, or its corresponding salt, or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
其中
亦於R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR51 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR51 R51 ' ；
其中亦於R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜芳基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R51 、-OR51 、-NO2 、-NR51 R51 ' 、-NR51 C(O)R51 ' 、-NR51 S(O)2 R51 ' 、-S(O)2 NR51 R51 ' 、-NR51 C(O)NR51 ' R51 '' 、-SR51 、-S(O)R51 、-S(O)2 R51 、-CN、鹵烷基、鹵烷氧基、-C(O)OR51 、-C(O)NR51 R51 ' 、-OCH2 CH2 OR51 、-NR51 S(O)2 NR51 ' R51 ' 及-C(CH3 )2 OR51 ；
及/或經一或多個選自以下之取代基取代：經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜環基；
其中R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
Wherein alkyl, alkenyl or alkynyl in alkylaryl, alkylheteroaryl or alkylcycloalkyl as also defined in R 5 is substituted with one or more substitutions selected from Group substitution: -OR 51 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 51 R 51 ' ;
Wherein cycloalkyl, aryl, or heteroaryl in alkylaryl, alkylheteroaryl, or alkylcycloalkyl also defined in R 5 is substituted with one or more selected from Substituent substituents: halogen, -R 51 , -OR 51 , -NO 2 , -NR 51 R 51 ' , -NR 51 C (O) R 51 ' , -NR 51 S (O) 2 R 51 ' ,- S (O) 2 NR 51 R 51 ' , -NR 51 C (O) NR 51 ' R 51 '' , -SR 51 , -S (O) R 51 , -S (O) 2 R 51 , -CN, Haloalkyl, haloalkoxy, -C (O) OR 51 , -C (O) NR 51 R 51 ' , -OCH 2 CH 2 OR 51 , -NR 51 S (O) 2 NR 51 ' R 51 ' And -C (CH 3 ) 2 OR 51 ;
And / or substituted with one or more substituents selected from: substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted Or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheterocyclyl;
Wherein R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
R5 ' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR52 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR52 R52 ' ；
其中R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
among them
If an alkyl, alkenyl or alkynyl group as defined in R 5 ' is substituted, it is substituted with one or more substituents selected from -OR 52 , halogen, -CN, haloalkyl, haloalkoxy And -NR 52 R 52 ' ;
Wherein R 52 and R 52 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基。
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein R 21 , R 21 ′, and R 21 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted Substituted C 2-6 alkynyl.
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
亦處於烷基芳基、烷基雜環基或烷基環烷基中之烷基、烯基或炔基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、-OR13 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR13 R13 ' ；
其中R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein the alkyl, alkenyl or alkynyl group also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl When substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from: = O, -OR 13 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 13 R 13 ' ;
Wherein R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
亦處於烷基芳基、烷基雜環基或烷基環烷基中之芳基、雜環基或環烷基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R14 、-OR14 、-NO2 、-NR14 R14 ' 、-NR14 C(O)R14 ' 、-NR14 S(O)2 R14 ' 、-S(O)2 NR14 R14 ' 、-NR14 C(O)NR14 ' R14 '' 、-SR14 、-S(O)R14 、-S(O)2 R14 、-CN、鹵烷基、鹵烷氧基、-C(O)OR14 、-C(O)NR14 R14 ' 、-OCH2 CH2 OR14 、-NR14 S(O)2 NR14 ' R14 '' 及-C(CH3 )2 OR14 ；
其中R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein the aryl, heterocyclyl or cycloalkane is also in an alkylaryl, alkylheterocyclyl or alkylcycloalkyl group. If a group is substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from: = O, halogen, -R 14 , -OR 14 , -NO 2 , -NR 14 R 14 ' , -NR 14 C (O) R 14 ' , -NR 14 S (O) 2 R 14 ' , -S (O) 2 NR 14 R 14 ' , -NR 14 C (O) NR 14 ' R 14 '' , -SR 14 , -S (O) R 14 , -S (O) 2 R 14 , -CN, haloalkyl, haloalkoxy, -C (O) OR 14 , -C (O) NR 14 R 14 ' , -OCH 2 CH 2 OR 14 , -NR 14 S (O) 2 NR 14 ' R 14 '', and -C (CH 3 ) 2 OR 14 ;
Wherein R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl, unsubstituted alkenyl group of C 2-6, unsubstituted C 2-6 alkynyl group of , Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic group;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R2 中之芳基或雜環基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
If an aryl or heterocyclic group in R 2 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' ,- NR 21 C (O) R 21 ' , -NR 21 S (O) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' ,- SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '', and -C (CH 3 ) 2 OR 21 ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R3 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR31 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR31 R31 ' ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
If an alkyl, alkenyl or alkynyl group as defined in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: -OR 31 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 31 R 31 ' ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R3 中之環烷基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R31 、-OR31 、-NO2 、-NR31 R31 ' 、-NR31 C(O)R31 ' 、-NR31 S(O)2 R31 ' 、-S(O)2 NR31 R31 ' 、-NR31 C(O)NR31 ' R31 ' v 、-SR31 、-S(O)R31 、-S(O)2 R31 、-CN、鹵烷基、鹵烷氧基、-C(O)OR31 、-C(O)NR31 R31 ' 、-OCH2 CH2 OR31 、-NR31 S(O)2 NR31 ' R31 '' 及-C(CH3 )2 OR31 ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
If a cycloalkyl group in R 3 is substituted, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 31 , -OR 31 , -NO 2 , -NR 31 R 31 ' , -NR 31 C (O) R 31 ' , -NR 31 S (O) 2 R 31 ' , -S (O) 2 NR 31 R 31 ' , -NR 31 C (O) NR 31 ' R 31 ' v , -SR 31 , -S (O) R 31 , -S (O) 2 R 31 , -CN, haloalkyl, haloalkoxy, -C (O) OR 31 , -C (O) NR 31 R 31 ' , -OCH 2 CH 2 OR 31 , -NR 31 S (O) 2 NR 31 ' R 31 '' and -C (CH 3 ) 2 OR 31 ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R3' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR32 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR32 R32 ' ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
If an alkyl, alkenyl or alkynyl group as defined in R 3 ′ is substituted, it is substituted with one or more substituents selected from: -OR 32 , halogen, -CN, haloalkyl, haloalkoxy And -NR 32 R 32 ' ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
亦處於R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR51 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR51 R51 ' ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of the general formula (I) of the present invention is the following compound, wherein the alkyl group is also an alkylaryl group, an alkylheteroaryl group or an alkylcycloalkyl group as defined in R 5 , If an alkenyl or alkynyl group is substituted, it is substituted with one or more substituents selected from -OR 51 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 51 R 51 ' ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
亦處於如R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜芳基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R51 、-OR51 、-NO2 、-NR51 R51 ' 、-NR51 C(O)R51 ' 、-NR51 S(O)2 R51 ' 、-S(O)2 NR51 R51 ' 、-NR51 C(O)NR51 ' R51 '' 、-SR51 、-S(O)R51 、-S(O)2 R51 、-CN、鹵烷基、鹵烷氧基、-C(O)OR51 、-C(O)NR51 R51 ' 、-OCH2 CH2 OR51 、-NR51 S(O)2 NR51 ' R51 '' 及-C(CH3 )2 OR51 ；及/或經一或多個選自以下之取代基取代：經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound wherein the cycloalkane is also in an alkylaryl, alkylheteroaryl or alkylcycloalkyl group as defined in R 5 If substituted, aryl, or heteroaryl is substituted with one or more substituents selected from the group consisting of: halogen, -R 51 , -OR 51 , -NO 2 , -NR 51 R 51 ' , -NR 51 C (O) R 51 ' , -NR 51 S (O) 2 R 51 ' , -S (O) 2 NR 51 R 51 ' , -NR 51 C (O) NR 51 ' R 51 '' , -SR 51 , -S (O) R 51 , -S (O) 2 R 51 , -CN, haloalkyl, haloalkoxy, -C (O) OR 51 , -C (O) NR 51 R 51 ' ,- OCH 2 CH 2 OR 51 , -NR 51 S (O) 2 NR 51 ' R 51 '' and -C (CH 3 ) 2 OR 51 ; and / or substituted with one or more substituents selected from: Substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted Alkylaryl and substituted or unsubstituted alkylheterocyclyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
亦處於如R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜芳基若經取代，則經一或多個選自以下之取代基取代：鹵素、-R51 、-OR51 、-NO2 、-NR51 R51 ' 、-NR51 C(O)R51 ' 、-NR51 S(O)2 R51 ' 、-S(O)2 NR51 R51 ' 、-NR51 C(O)NR51 ' R51 '' 、-SR51 、-S(O)R51 、-S(O)2 R51 、-CN、鹵烷基、鹵烷氧基、-C(O)OR51 、-C(O)NR51 R51 ' 、-OCH2 CH2 OR51 、-NR51 S(O)2 NR51 ' R51 '' 及-C(CH3 )2 OR51 ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound wherein the cycloalkane is also in an alkylaryl, alkylheteroaryl or alkylcycloalkyl group as defined in R 5 If substituted, aryl, or heteroaryl, it is substituted with one or more substituents selected from the group consisting of: halogen, -R 51 , -OR 51 , -NO 2 , -NR 51 R 51 ' , -NR 51 C (O) R 51 ' , -NR 51 S (O) 2 R 51 ' , -S (O) 2 NR 51 R 51 ' , -NR 51 C (O) NR 51 ' R 51 '' , -SR 51 , -S (O) R 51 , -S (O) 2 R 51 , -CN, haloalkyl, haloalkoxy, -C (O) OR 51 , -C (O) NR 51 R 51 ' ,- OCH 2 CH 2 OR 51 , -NR 51 S (O) 2 NR 51 ' R 51 '' and -C (CH 3 ) 2 OR 51 ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
亦處於如R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜芳基若經取代，則經一或多個選自以下之取代基取代：經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜環基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound wherein the cycloalkane is also in an alkylaryl, alkylheteroaryl or alkylcycloalkyl group as defined in R 5 If substituted, aryl or heteroaryl is substituted with one or more substituents selected from: substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or Unsubstituted heterocyclyl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheterocyclyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
亦處於如R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜芳基若經取代，則經一或多個-NR51 R51 ' 取代；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound wherein the cycloalkane is also in an alkylaryl, alkylheteroaryl or alkylcycloalkyl group as defined in R 5 If substituted, aryl, or heteroaryl is substituted with one or more -NR 51 R 51 ' ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
亦處於如R5 中所定義之烷基芳基、烷基雜芳基或烷基環烷基中的環烷基、芳基或雜芳基若經取代，則經一或多個選自以下之取代基取代：經取代或未經取代之芳基及經取代或未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is a compound wherein the cycloalkane is also in an alkylaryl, alkylheteroaryl or alkylcycloalkyl group as defined in R 5 If substituted, aryl, or heteroaryl is substituted with one or more substituents selected from: substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
R5 ' 中所定義之烷基、烯基或炔基若經取代，則經一或多個選自以下之取代基取代：-OR52 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR52 R52 ' ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein
If an alkyl, alkenyl or alkynyl group as defined in R 5 ' is substituted, it is substituted with one or more substituents selected from -OR 52 , halogen, -CN, haloalkyl, haloalkoxy And -NR 52 R 52 ' ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個實施例中，本發明之通式(I)化合物為以下化合物，其中
亦處於烷基芳基、烷基雜環基或烷基環烷基中之烷基、烯基或炔基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、-OR13 、鹵素、-CN、鹵烷基、鹵烷氧基及-NR13 R13 ' ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment, the compound of general formula (I) of the present invention is the following compound, wherein the alkyl, alkenyl or alkynyl group also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl When substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from: = O, -OR 13 , halogen, -CN, haloalkyl, haloalkoxy, and -NR 13 R 13 ' ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明之通式(I)化合物的另一個較佳實施例中為以下化合物，其中
亦處於烷基芳基、烷基雜環基或烷基環烷基中之芳基、雜環基或環烷基若經取代且該取代未以其他方式進行定義，則其經一或多個選自以下之取代基取代：=O、鹵素、-R14 、-OR14 、-NO2 、-NR14 R14 ' 、-NR14 C(O)R14 ' 、-NR14 S(O)2 R14 ' 、-S(O)2 NR14 R14 ' 、-NR14 C(O)NR14 ' R14 '' 、-SR14 、-S(O)R14 、-S(O)2 R14 、-CN、鹵烷基、鹵烷氧基、-C(O)OR14 、-C(O)NR14 R14 ' 、-OCH2 CH2 OR14 、-NR14 S(O)2 NR14 ' R14 '' 及-C(CH3 )2 OR14 ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the compound of general formula (I) of the present invention is the following compound, wherein the aryl group, heterocyclic group, or alkylaryl group, alkylheterocyclyl group or alkylcycloalkyl group is also If a cycloalkyl is substituted and the substitution is not otherwise defined, it is substituted with one or more substituents selected from: = O, halogen, -R 14 , -OR 14 , -NO 2 , -NR 14 R 14 ' , -NR 14 C (O) R 14 ' , -NR 14 S (O) 2 R 14 ' , -S (O) 2 NR 14 R 14 ' , -NR 14 C (O) NR 14 ' R 14 '' , -SR 14 , -S (O) R 14 , -S (O) 2 R 14 , -CN, haloalkyl, haloalkoxy, -C (O) OR 14 , -C (O ) NR 14 R 14 ' , -OCH 2 CH 2 OR 14 , -NR 14 S (O) 2 NR 14 ' R 14 '', and -C (CH 3 ) 2 OR 14 ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明之通式(I)化合物的另一個較佳實施例中為以下化合物，其中
X為一鍵、-[C(Ra Rb )]p -、-[C(Ra Rb )]p C(O)[C(Rc Rd )]q -、-[C(Ra Rb )]p C(O)N(Rz )[C(Rc Rd )]q -、-[C(Ra Rb )]p N(Rz )C(O)[C(Rc Rd )]q -或-[C(Ra Rb )]p N(Rz )[C(Rc Rd )]q -；
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基及C(O)-C1-6 烷基；
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基；
Rc 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
Rd 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the compound of general formula (I) of the present invention is the following compound, wherein
X is a bond,-[C (R a R b )] p -,-[C (R a R b )] p C (O) [C (R c R d )] q -,-[C (R a R b )] p C (O) N (R z ) [C (R c R d )] q -,-[C (R a R b )] p N (R z ) C (O) [C ( R c R d )] q - or- [C (R a R b )] p N (R z ) [C (R c R d )] q- ;
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, and C (O) -C 1-6 alkyl;
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
Alternatively, R a and R b with the carbon atom they are attached may form a substituted or non-substituted cycloalkyl group;
R c is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
R d is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明之通式(I)化合物的另一個較佳實施例中為以下化合物，其中
X為一鍵、-[C(Ra Rb )]p -、-[C(Ra Rb )]p C(O)[C(Rc Rd )]q -、-[C(Ra Rb )]p C(O)N(Rz )[C(Rc Rd )]q -、-[C(Ra Rb )]p N(Rz )C(O)[C(Rc Rd )]q -或-[C(Ra Rb )]p N(Rz )[C(Rc Rd )]q -；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the compound of general formula (I) of the present invention is the following compound, wherein
X is a bond,-[C (R a R b )] p -,-[C (R a R b )] p C (O) [C (R c R d )] q -,-[C (R a R b )] p C (O) N (R z ) [C (R c R d )] q -,-[C (R a R b )] p N (R z ) C (O) [C ( R c R d )] q - or- [C (R a R b )] p N (R z ) [C (R c R d )] q- ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明之通式(I)化合物的另一個較佳實施例中為以下化合物，其中
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基及C(O)-C1-6 烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the compound of general formula (I) of the present invention is the following compound, wherein
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, and C (O) -C 1-6 alkyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明之通式(I)化合物的另一個較佳實施例中為以下化合物，其中
Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the compound of general formula (I) of the present invention is the following compound, wherein
R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明之通式(I)化合物的另一個較佳實施例中為以下化合物，其中
Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the compound of general formula (I) of the present invention is the following compound, wherein
R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明之通式(I)化合物的另一個較佳實施例中為以下化合物，其中
Ra 及Rb 與其所連接之碳原子一起形成經取代或未經取代之環烷基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the compound of general formula (I) of the present invention is the following compound, wherein
R a and R b together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl group;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明之通式(I)化合物的另一個較佳實施例中為以下化合物，其中
Rc 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the compound of general formula (I) of the present invention is the following compound, wherein
R c is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明之通式(I)化合物的另一個較佳實施例中為以下化合物，其中
Rd 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the compound of general formula (I) of the present invention is the following compound, wherein
R d is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
X係選自一鍵、-[CH2 ]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
及/或
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；較佳地，Rz 係選自氫及經取代或未經取代之C1-6 烷基；更佳地，Rz 係選自氫及經取代或未經取代之甲基；
及/或
p為0、1、2、3、4或5；較佳地，p為0、1或2；
及/或
q為0、1、2、3、4或5；較佳地，q為0、1或2；
及/或
Y1 為-C(R10 R10 ' )-；較佳地，Y1 為-CH2 -；
及/或
Y2 為-C(R10 R10 ' )-；較佳地，Y2 為-CH2 -；
及/或
n為0或1；
及/或
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
及/或
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
及/或
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；較佳地，R3 為經取代或未經取代之C1-6 烷基；更佳地，R3 為經取代或未經取代之甲基或經取代或未經取代之乙基；
及/或
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R3 ' 為氫；
及/或
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
及/或
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；較佳地，R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
及/或
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R5 ' 係選自氫及經取代或未經取代之C1-6 烷基，
及/或
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；較佳地，R6 及R6 ' 為氫，
及/或
R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R10 及R10 ’ 獨立地選自氫；
及/或
R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R10 ' 及R10 ''' 獨立地選自氫；
及/或
R10 '' 及R10 ''' 與其所連接之碳原子形成經取代或未經取代之環烷基；
及/或
R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
及/或
R31 、R31 ' 及R31 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
及/或
R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
及/或
R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R41 、R41 ' 及R41 '' 均為氫；
及/或
R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R51 、R51 ' 及R51 '' 為經取代或未經取代之C1-6 烷基；
及/或
R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
及/或
R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
及/或
R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
X is selected from one bond,-[CH 2 ] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
And / or
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl; preferably, R z is selected from hydrogen and substituted or Unsubstituted C 1-6 alkyl; more preferably, R z is selected from hydrogen and substituted or unsubstituted methyl;
And / or
p is 0, 1, 2, 3, 4 or 5; preferably, p is 0, 1 or 2;
And / or
q is 0, 1, 2, 3, 4 or 5; preferably, q is 0, 1 or 2;
And / or
Y 1 is -C (R 10 R 10 ' )-; preferably, Y 1 is -CH 2- ;
And / or
Y 2 is -C (R 10 R 10 ' )-; preferably, Y 2 is -CH 2- ;
And / or
n is 0 or 1;
And / or
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
And / or
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
And / or
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; preferably, R 3 is substituted or unsubstituted C 1-6 alkyl; more preferably, R 3 is Substituted or unsubstituted methyl or substituted or unsubstituted ethyl;
And / or
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; Preferably, R 3 ′ is hydrogen;
And / or
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
And / or
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl; preferably, R 5 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted cycloalkyl , Substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheteroaryl;
And / or
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; Preferably, R 5 ′ is selected from hydrogen and substituted or unsubstituted C 1-6 alkyl,
And / or
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 'R 21' 'and -C (CH 3) 2 OR 21 ; preferably, R 6 and R 6' is hydrogen,
And / or
R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl; preferably, R 10 and R 10 'are independently selected from hydrogen;
And / or
R 10 '' and R 10 '''are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; preferably, R 10 ′ and R 10 ′ ″ are independently selected from hydrogen;
And / or
R 10 '' and R 10 ''' and the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl group;
And / or
R 21, R 21 'and R 21' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
And / or
R 31, R 31 'and R 31' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
And / or
R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
And / or
R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- the substituted C 2-6 alkynyl group; preferably, R 41, R 41 'and R 41' 'are hydrogen;
And / or
R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- the substituted C 2-6 alkynyl group; preferably the, R 51, R 51 'and R 51' 'is a substituted or non-substituted C 1-6 alkyl;
And / or
R 52 and R 52 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
And / or
R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
And / or
R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl, unsubstituted alkenyl group of C 2-6, unsubstituted C 2-6 alkynyl group of, Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic groups;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
X係選自一鍵、-[CH2 ]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
且
若X係選自一鍵、-[CH2 ]p -、-[CH2 ]p C(O)[CH2 ]q -及-[CH2 ]p N(Rz )C(O)[CH2 ]q -，則q為0、1、2、3、4或5；較佳地，q為0、1或2；且
若X係選自-[CH2 ]p C(O)N(Rz )[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -，則q為1、2、3、4或5；較佳地，q為1或2；
及/或
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；較佳地，Rz 係選自氫及經取代或未經取代之C1-6 烷基；更佳地，Rz 係選自氫及經取代或未經取代之甲基；
及/或
p為0、1、2、3、4或5；較佳地，p為0、1或2；
及/或
Y1 為-C(R10 R10 ' )-；較佳地，Y1 為-CH2 -；
及/或
Y2 為-C(R10 R10 ' )-；較佳地，Y2 為-CH2 -；
及/或
n為0或1；
及/或
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
及/或
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
及/或
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；較佳地，R3 為經取代或未經取代之C1-6 烷基；更佳地，R3 為經取代或未經取代之甲基或經取代或未經取代之乙基；
及/或
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R3 ' 為氫；
及/或
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
及/或
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；較佳地，R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
及/或
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R5 ' 係選自氫及經取代或未經取代之C1-6 烷基，
及/或
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 ' v 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；較佳地，R6 及R6 ' 為氫，
及/或
R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R10 及R10 ' 獨立地選自氫；
及/或
R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R10 '' 及R10 ''' 獨立地選自氫；
及/或
R10 '' 及R10 ''' 與其所連接之碳原子形成經取代或未經取代之環烷基；
及/或
R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
及/或
R31 、R31 ' 及R31 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
及/或
R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
及/或
R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R41 、R41 ' 及R41 '' 均為氫；
及/或
R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R51 、R51 ' 及R51 '' 為經取代或未經取代之C1-6 烷基；
及/或
R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
及/或
R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
及/或
R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
X is selected from one bond,-[CH 2 ] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
And if X is selected from one bond,-[CH 2 ] p -,-[CH 2 ] p C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) C (O) [ CH 2 ] q- , then q is 0, 1, 2, 3, 4 or 5; preferably, q is 0, 1 or 2; and if X is selected from-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- , then q is 1, 2, 3, 4 or 5; preferably, q is 1 or 2;
And / or
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl; preferably, R z is selected from hydrogen and substituted or Unsubstituted C 1-6 alkyl; more preferably, R z is selected from hydrogen and substituted or unsubstituted methyl;
And / or
p is 0, 1, 2, 3, 4 or 5; preferably, p is 0, 1 or 2;
And / or
Y 1 is -C (R 10 R 10 ' )-; preferably, Y 1 is -CH 2- ;
And / or
Y 2 is -C (R 10 R 10 ' )-; preferably, Y 2 is -CH 2- ;
And / or
n is 0 or 1;
And / or
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
And / or
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
And / or
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; preferably, R 3 is substituted or unsubstituted C 1-6 alkyl; more preferably, R 3 is Substituted or unsubstituted methyl or substituted or unsubstituted ethyl;
And / or
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; Preferably, R 3 ′ is hydrogen;
And / or
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
And / or
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl; preferably, R 5 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted cycloalkyl , Substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheteroaryl;
And / or
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; Preferably, R 5 ′ is selected from hydrogen and substituted or unsubstituted C 1-6 alkyl,
And / or
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 ' v , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 'R 21' 'and -C (CH 3) 2 OR 21 ; preferably, R 6 and R 6' is hydrogen,
And / or
R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl; preferably, R 10 and R 10 'are independently selected from hydrogen;
And / or
R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted the C 2-6 alkynyl group; preferably, R 10 '' and R 10 '''are independently selected from hydrogen;
And / or
R 10 '' and R 10 ''' and the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl group;
And / or
R 21, R 21 'and R 21' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
And / or
R 31, R 31 'and R 31' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
And / or
R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
And / or
R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- the substituted C 2-6 alkynyl group; preferably, R 41, R 41 'and R 41' 'are hydrogen;
And / or
R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- the substituted C 2-6 alkynyl group; preferably the, R 51, R 51 'and R 51' 'is a substituted or non-substituted C 1-6 alkyl;
And / or
R 52 and R 52 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
And / or
R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
And / or
R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl, unsubstituted alkenyl group of C 2-6, unsubstituted C 2-6 alkynyl group of, Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic groups;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明之通式(I)化合物的另一個較佳實施例中為以下化合物，其中
X係選自一鍵、-[CH2 ]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；
及/或
p為0、1、2、3、4或5；
及/或
q為0、1、2、3、4或5；
及/或
n為0或1；
及/或
Y1 為-C(R10 R10 ' )-；
及/或
Y2 為-C(R10 ' ' R10 ''' )-；
及/或
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；
其中
烷基為C1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該C1-6 烷基為甲基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C3-6 環烷基，如環丙基、環丁基、環戊基或環己基；
及/或
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；
及/或
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基，
其中
芳基係選自苯基、萘基或蒽；較佳為萘基及苯基；較佳地，該芳基為苯基；
及/或
雜環基為具有以下一或多個飽和或不飽和環之雜環系統，該等環中之至少一個環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子；較佳為具有以下一或兩個飽和或不飽和環之雜環系統，該等環中之至少一個環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子，更佳選自氧氮雜環庚烷、吡咯啶、咪唑、噁二唑、四唑、氮雜環丁烷、吡啶、嘧啶、哌啶、哌嗪、苯并呋喃、苯并咪唑、吲唑、苯并噻唑、苯并二唑、噻唑、苯并噻唑、四氫哌喃、嗎啉、吲哚啉、呋喃、三唑、異噁唑、吡唑、噻吩、苯并噻吩、吡咯、吡嗪、吡咯并[2,3b]吡啶、喹啉、喹諾酮、異喹啉、四氫噻吩并吡啶、酞嗪、苯并-1,2,5-噻二唑、吲哚、苯并三唑、苯并噁唑、側氧基吡咯啶、苯并二氧雜環戊烷、苯并二噁烷、咔唑、氧雜螺癸烷或噻唑；較佳地，該雜環基為噻吩；
及/或
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；
其中
烷基為C1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該C1-6 烷基為甲基或乙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C3-6 環烷基，如環丙基、環丁基、環戊基或環己基；
及/或
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中
烷基為C1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；
其中
烷基為C1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該烷基為甲基或乙基；
及/或
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該C1-6 烷基為甲基、乙基、異丙基或異丁基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C3-6 環烷基，如環丙基、環丁基、環戊基或環己基；較佳地，該環烷基為環己基或環丙基；
及/或
芳基係選自苯基、萘基、二氫茚或蒽；較佳為萘基、二氫茚及苯基；較佳地，該芳基為苯基或二氫茚；
及/或雜芳基為具有以下一或多個環之芳族5員至18員單環或多環雜環系統，該等環中之至少一個芳族環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子；較佳為具有以下一或兩個環之5員至18員單環或多環芳族雜環系統，該等環中之至少一個芳族環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子，更佳選自呋喃、苯并呋喃、噻吩、苯并噻吩、吡咯、吡啶、嘧啶、吡嗪、喹啉、異喹啉、酞嗪、苯并噻唑、吲哚、苯并三唑、咔唑、喹唑啉、噻唑、咪唑、吡唑、噁唑、噻吩及苯并咪唑；較佳地，該雜芳基為吡啶、噻吩、喹啉或異喹啉；
及/或
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該C1-6 烷基為甲基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；
其中
烷基為C1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
R10 及R10 ' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
其中
環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C3-6 環烷基，如環丙基、環丁基、環戊基或環己基；
及/或
R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
R10 '' 及R10 ''' 可與其所連接之碳原子形成經取代或未經取代之環烷基；
其中
環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C3-6 環烷基，如環丙基、環丁基、環戊基或環己基；
及/或
R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基，更佳地，該C1-6 烷基為甲基、乙基或丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
R31 、R31 ' 及R31 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基，
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該C1-6 烷基為甲基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其中
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基，
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
其中
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；
其中
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C3-6 環烷基，如環丙基、環丁基、環戊基或環己基；
及/或
芳基係選自苯基、萘基或蒽；較佳為萘基及苯基；
及/或
雜環基為具有以下一或多個飽和或不飽和環之雜環系統，該等環中之至少一個環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子；較佳為具有以下一或兩個飽和或不飽和環之雜環系統，該等環中之至少一個環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子，更佳選自氧氮雜環庚烷、吡咯啶、咪唑、噁二唑、四唑、氮雜環丁烷、吡啶、嘧啶、哌啶、哌嗪、苯并呋喃、苯并咪唑、吲唑、苯并噻唑、苯并二唑、噻唑、苯并噻唑、四氫哌喃、嗎啉、吲哚啉、呋喃、三唑、異噁唑、吡唑、噻吩、苯并噻吩、吡咯、吡嗪、吡咯并[2,3b]吡啶、喹啉、喹諾酮、異喹啉、四氫噻吩并吡啶、酞嗪、苯并-1,2,5-噻二唑、吲哚、苯并三唑、苯并噁唑、側氧基吡咯啶、苯并二氧雜環戊烷、苯并二噁烷、咔唑、氧雜螺癸烷或噻唑；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the compound of general formula (I) of the present invention is the following compound, wherein
X is selected from one bond,-[CH 2 ] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ;
And / or
p is 0, 1, 2, 3, 4 or 5;
And / or
q is 0, 1, 2, 3, 4 or 5;
And / or
n is 0 or 1;
And / or
Y 1 is -C (R 10 R 10 ' )-;
And / or
Y 2 is -C (R 10 ' ' R 10 ''')-;
And / or
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl;
Wherein alkyl is C 1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C 1-6 alkyl is methyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or cycloalkyl is C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C 3-7 cycloalkyl, Such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably derived from C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;
And / or
R 1 is selected from -NR 5 R 5 'and -NR 5' C (O) R 5;
And / or
R 2 is selected from a substituted or unsubstituted aryl group and a substituted or unsubstituted heterocyclic group,
Wherein the aryl group is selected from phenyl, naphthyl or anthracene; preferably naphthyl and phenyl; preferably, the aryl is phenyl;
And / or heterocyclyl is a heterocyclic ring system having one or more saturated or unsaturated rings, at least one of which contains one or more selected from the group consisting of nitrogen, oxygen, and / or sulfur in the ring A group of heteroatoms; preferably a heterocyclic ring system having one or two saturated or unsaturated rings, at least one of which contains one or more selected from the group consisting of nitrogen, oxygen, and / or Heteroatoms of the group consisting of sulfur, more preferably selected from oxazepine, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran , Benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropiperan, morpholine, indolin, furan, triazole, isoxazole, pyrazole, thiophene, benzene Benzothiophene, pyrrole, pyrazine, pyrrolo [2,3b] pyridine, quinoline, quinolone, isoquinoline, tetrahydrothienopyridine, phthalazine, benzo-1,2,5-thiadiazole, indole Benzotriazole, benzoxazole, pendant oxopyridine, benzodioxolane, benzodioxane, carbazole, oxaspirodecane or thiazole; preferably, the heterocyclic ring Is thiophene;
And / or
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
Wherein alkyl is C 1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C 1-6 alkyl is Methyl or ethyl
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or cycloalkyl is C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C 3-7 cycloalkyl, Such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably derived from C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;
And / or
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
among them
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein alkyl is C 1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl;
Wherein the alkyl group is a C 1-6 alkyl group, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably, the alkyl group is methyl Or ethyl
And / or
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C 1-6 alkyl is Methyl, ethyl, isopropyl or isobutyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or cycloalkyl is C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C 3-7 cycloalkyl, Such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably derived from C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably , The cycloalkyl is cyclohexyl or cyclopropyl;
And / or aryl is selected from phenyl, naphthyl, dihydroindene or anthracene; preferably naphthyl, dihydroindene and phenyl; preferably, the aryl is phenyl or dihydroindene;
And / or heteroaryl is an aromatic 5- to 18-membered monocyclic or polycyclic heterocyclic ring system having one or more of the following rings, and at least one of the aromatic rings in the rings contains one or more Heteroatoms selected from the group consisting of nitrogen, oxygen and / or sulfur; preferably 5- to 18-membered monocyclic or polycyclic aromatic heterocyclic systems having one or two of the following rings, at least one of these rings The aromatic ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and / or sulfur in the ring, more preferably selected from furan, benzofuran, thiophene, benzothiophene, pyrrole, pyridine, pyrimidine, Pyrazine, quinoline, isoquinoline, phthalazine, benzothiazole, indole, benzotriazole, carbazole, quinazoline, thiazole, imidazole, pyrazole, oxazole, thiophene, and benzimidazole; preferably Preferably, the heteroaryl group is pyridine, thiophene, quinoline or isoquinoline;
And / or
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
among them
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C 1-6 alkyl is methyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ;
Wherein alkyl is C 1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
among them
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or
R 10 and R 10 ′ may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
Wherein cycloalkyl is C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably C 3-7 cycloalkyl, such as cyclo Propyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably derived from C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;
And / or
R 10 '' and R 10 ′ '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
among them
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or
R 10 '' and R 10 ''' may form a substituted or unsubstituted cycloalkyl group with the carbon atom to which they are attached;
Wherein cycloalkyl is C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably C 3-7 cycloalkyl, such as cyclo Propyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably derived from C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;
And / or
R 21, R 21 'and R 21' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
among them
The C 1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl. More preferably, the C 1-6 alkyl group is Methyl, ethyl or propyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or
R 31, R 31 'and R 31' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
among them
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or
R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
among them
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or
R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
among them
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl,
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or
R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
among them
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C 1-6 alkyl is methyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or
R 52 and R 52 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
among them
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl,
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or
R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
among them
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or
R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl, unsubstituted alkenyl group of C 2-6, unsubstituted C 2-6 alkynyl group of, Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic groups;
among them
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or cycloalkyl is C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C 3-7 cycloalkyl, Such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably derived from C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;
And / or aryl is selected from phenyl, naphthyl or anthracene; preferably naphthyl and phenyl;
And / or heterocyclyl is a heterocyclic ring system having one or more saturated or unsaturated rings, at least one of which contains one or more selected from the group consisting of nitrogen, oxygen, and / or sulfur in the ring A group of heteroatoms; preferably a heterocyclic ring system having one or two saturated or unsaturated rings, at least one of which contains one or more selected from the group consisting of nitrogen, oxygen, and / or Heteroatoms of the group consisting of sulfur, more preferably selected from oxazepine, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran , Benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropiperan, morpholine, indolin, furan, triazole, isoxazole, pyrazole, thiophene, benzene Benzothiophene, pyrrole, pyrazine, pyrrolo [2,3b] pyridine, quinoline, quinolone, isoquinoline, tetrahydrothienopyridine, phthalazine, benzo-1,2,5-thiadiazole, indole Benzotriazole, benzoxazole, pendant oxopyridine, benzodioxane, benzodioxane, carbazole, oxaspirodecane or thiazole;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的Rz 中，
烷基為C1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該C1-6 烷基為甲基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C3-6 環烷基，如環丙基、環丁基、環戊基或環己基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R z as defined in any one of the embodiments of the present invention,
Alkyl is C 1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C 1-6 alkyl is methyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or cycloalkyl is C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C 3-7 cycloalkyl, Such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably derived from C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R2 中，
芳基係選自苯基、萘基或蒽；較佳為萘基及苯基；較佳地，該芳基為苯基；
及/或
雜環基為具有以下一或多個飽和或不飽和環之雜環系統，該等環中之至少一個環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子；較佳為具有以下一或兩個飽和或不飽和環之雜環系統，該等環中之至少一個環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子，更佳選自氧氮雜環庚烷、吡咯啶、咪唑、噁二唑、四唑、氮雜環丁烷、吡啶、嘧啶、哌啶、哌嗪、苯并呋喃、苯并咪唑、吲唑、苯并噻唑、苯并二唑、噻唑、苯并噻唑、四氫哌喃、嗎啉、吲哚啉、呋喃、三唑、異噁唑、吡唑、噻吩、苯并噻吩、吡咯、吡嗪、吡咯并[2,3b]吡啶、喹啉、喹諾酮、異喹啉、四氫噻吩并吡啶、酞嗪、苯并-1,2,5-噻二唑、吲哚、苯并三唑、苯并噁唑、側氧基吡咯啶、苯并二氧雜環戊烷、苯并二噁烷、咔唑、氧雜螺癸烷或噻唑；較佳地，該雜環基為噻吩；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R 2 as defined in any one of the embodiments of the present invention,
The aryl group is selected from phenyl, naphthyl or anthracene; preferably naphthyl and phenyl; preferably, the aryl is phenyl;
And / or heterocyclyl is a heterocyclic ring system having one or more saturated or unsaturated rings, at least one of which contains one or more selected from the group consisting of nitrogen, oxygen, and / or sulfur in the ring A group of heteroatoms; preferably a heterocyclic ring system having one or two saturated or unsaturated rings, at least one of which contains one or more selected from the group consisting of nitrogen, oxygen, and / or Heteroatoms of the group consisting of sulfur, more preferably selected from oxazepine, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran , Benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropiperan, morpholine, indolin, furan, triazole, isoxazole, pyrazole, thiophene, benzene Benzothiophene, pyrrole, pyrazine, pyrrolo [2,3b] pyridine, quinoline, quinolone, isoquinoline, tetrahydrothienopyridine, phthalazine, benzo-1,2,5-thiadiazole, indole Benzotriazole, benzoxazole, pendant oxopyridine, benzodioxolane, benzodioxane, carbazole, oxaspirodecane or thiazole; preferably, the heterocyclic ring Is thiophene;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R3 中，
烷基為C1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該C1-6 烷基為甲基或乙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C3-6 環烷基，如環丙基、環丁基、環戊基或環己基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to formula (I), the compound is the following compound, wherein in R 3 as defined in any one of the embodiments of the present invention
Alkyl is C 1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C 1-6 alkyl is Methyl or ethyl
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or cycloalkyl is C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C 3-7 cycloalkyl, Such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably derived from C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R3 ' 中，
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R 3 ′ as defined in any one of the embodiments of the present invention,
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R4 及R4 ' 中，
烷基為C1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R 4 and R 4 ′ as defined in any one of the embodiments of the present invention,
Alkyl is C 1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R5 中，
烷基為C1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該烷基為甲基或乙基；
及/或
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該C1-6 烷基為甲基、乙基、異丙基或異丁基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C3-6 環烷基，如環丙基、環丁基、環戊基或環己基；較佳地，該環烷基為環己基或環丙基；
及/或
芳基係選自苯基、萘基、二氫茚或蒽；較佳為萘基、二氫茚及苯基；較佳地，該芳基為苯基或二氫茚；
及/或
雜芳基為具有以下一或多個環之芳族5員至18員單環或多環雜環系統，該等環中之至少一個芳族環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子；較佳為具有以下一或兩個環之5員至18員單環或多環芳族雜環系統，該等環中之至少一個芳族環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子，更佳選自呋喃、苯并呋喃、噻吩、苯并噻吩、吡咯、吡啶、嘧啶、吡嗪、喹啉、異喹啉、酞嗪、苯并噻唑、吲哚、苯并三唑、咔唑、喹唑啉、噻唑、咪唑、吡唑、噁唑、噻吩及苯并咪唑；較佳地，該雜芳基為吡啶、噻吩、喹啉或異喹啉；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R 5 as defined in any one of the embodiments of the present invention,
Alkyl is C 1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably, the alkyl is methyl or Ethyl
And / or
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C 1-6 alkyl is Methyl, ethyl, isopropyl or isobutyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or cycloalkyl is C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C 3-7 cycloalkyl, Such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably derived from C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably , The cycloalkyl is cyclohexyl or cyclopropyl;
And / or aryl is selected from phenyl, naphthyl, dihydroindene or anthracene; preferably naphthyl, dihydroindene and phenyl; preferably, the aryl is phenyl or dihydroindene;
And / or heteroaryl is an aromatic 5- to 18-membered monocyclic or polycyclic heterocyclic ring system having one or more of the following rings, and at least one of the aromatic rings in the rings contains one or more Heteroatoms selected from the group consisting of nitrogen, oxygen and / or sulfur; preferably 5- to 18-membered monocyclic or polycyclic aromatic heterocyclic systems having one or two of the following rings, at least one of these rings The aromatic ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and / or sulfur in the ring, more preferably selected from furan, benzofuran, thiophene, benzothiophene, pyrrole, pyridine, pyrimidine, Pyrazine, quinoline, isoquinoline, phthalazine, benzothiazole, indole, benzotriazole, carbazole, quinazoline, thiazole, imidazole, pyrazole, oxazole, thiophene, and benzimidazole; preferably Preferably, the heteroaryl group is pyridine, thiophene, quinoline or isoquinoline;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R5 ' 中，
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，該C1-6 烷基為甲基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R 5 ′ as defined in any one of the embodiments of the present invention,
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, the C 1-6 alkyl is methyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R6 及R6 ' 中，
烷基為C1-6 烷基，如甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to formula (I), the compound is the following compound, wherein in R 6 and R 6 ′ as defined in any one of the embodiments of the present invention,
Alkyl is C 1-6 alkyl, such as methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R10 及R10 ' 中，
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R 10 and R 10 ′ as defined in any one of the embodiments of the present invention,
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R10 及R10 ' 中，
環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C3-6 環烷基，如環丙基、環丁基、環戊基或環己基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R 10 and R 10 ′ as defined in any one of the embodiments of the present invention,
Cycloalkyl is C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably C 3-7 cycloalkyl, such as cyclopropyl Base, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably derived from C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R10 ' ' 及R10 ''' 中，
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R 10 ′ ′ and R 10 ′ ″ as defined in any one of the embodiments of the present invention,
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R10 '' 及R10 ''' 中，
環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C3-6 環烷基，如環丙基、環丁基、環戊基或環己基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R 10 '' and R 10 ′ '' as defined in any one of the embodiments of the present invention
Cycloalkyl is C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably C 3-7 cycloalkyl, such as cyclopropyl Base, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably derived from C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R21 、R21 ' 及R21 '' 中，
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基，更佳地，該C1-6 烷基為甲基、乙基或丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another general formula (I) of the preferred embodiment of the present invention, the compound is a compound wherein R in the embodiment as defined in any of one embodiment of the present invention 21, R 21 'and R 21' ', the
The C 1-6 alkyl group is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl. More preferably, the C 1-6 alkyl group is Methyl, ethyl or propyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R31 、R31 ' 及R31 '' 中，
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another general formula (I) of the preferred embodiment of the present invention, the compound is a compound wherein R in this embodiment as defined in any of one embodiment of the present invention 31, R 31 'and R 31' ',
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R32 及R32 ' 中，
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R 32 and R 32 ′ as defined in any one of the embodiments of the present invention,
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R41 、R41 ' 及R41 '' 中，
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基，
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another general formula (I) of the preferred embodiment of the present invention, the compound is a compound wherein R in the embodiment as defined in any of one embodiment of the present invention 41, R 41 'and R 41' ', the
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl,
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R51 、R51 ' 及R51 '' 中，
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；較佳地，C1-6 烷基為甲基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another general formula (I) of the preferred embodiment of the present invention, the compound is a compound wherein R 51 in the embodiment as defined in any of one embodiment of the present invention, R 51 'and R 51' ', the
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl; preferably, C 1-6 alkyl is methyl base;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R52 及R52 ' 中，
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基，
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R 52 and R 52 ′ as defined in any one of the embodiments of the present invention,
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl,
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R13 及R13 ' 中，
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein in R 13 and R 13 ′ as defined in any one of the embodiments of the present invention,
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中在如本發明之任一實施例中所定義的R14 、R14 ' 及R14 '' 中，
C1-6 烷基較佳選自甲基、乙基、丙基、丁基、戊基、己基、異丙基或2-甲基丙基；
及/或
C2-6 烯基較佳選自乙烯、丙烯、丁烯、戊烯、己烯、異丙烯及異丁烯；
及/或
C2-6 炔基較佳選自乙炔、丙炔、丁炔、戊炔、己炔、異丙炔及異丁炔；
及/或
環烷基為C3-8 環烷基，如環丙基、環丁基、環戊基、環己基、環庚基或環辛基；較佳為C3-7 環烷基，如環丙基、環丁基、環戊基、環己基或環庚基；更佳來自C3-6 環烷基，如環丙基、環丁基、環戊基或環己基；
及/或
芳基係選自苯基、萘基或蒽；較佳為萘基及苯基；
及/或
雜環基為具有以下一或多個飽和或不飽和環之雜環系統，該等環中之至少一個環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子；較佳為具有以下一或兩個飽和或不飽和環之雜環系統，該等環中之至少一個環在該環中含有一或多個選自由氮、氧及/或硫組成之群的雜原子，更佳選自氧氮雜環庚烷、吡咯啶、咪唑、噁二唑、四唑、氮雜環丁烷、吡啶、嘧啶、哌啶、哌嗪、苯并呋喃、苯并咪唑、吲唑、苯并噻唑、苯并二唑、噻唑、苯并噻唑、四氫哌喃、嗎啉、吲哚啉、呋喃、三唑、異噁唑、吡唑、噻吩、苯并噻吩、吡咯、吡嗪、吡咯并[2,3b]吡啶、喹啉、喹諾酮、異喹啉、四氫噻吩并吡啶、酞嗪、苯并-1,2,5-噻二唑、吲哚、苯并三唑、苯并噁唑、側氧基吡咯啶、苯并二氧雜環戊烷、苯并二噁烷、咔唑、氧雜螺癸烷或噻唑；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another general formula (I) of the preferred embodiment of the present invention, the compound is a compound wherein R in the embodiment as defined in any of one embodiment of the present invention 14, R 14 'and R 14' ', the
C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl or 2-methylpropyl;
And / or
C 2-6 alkenyl is preferably selected from ethylene, propylene, butene, pentene, hexene, isopropylene and isobutylene;
And / or
C 2-6 alkynyl is preferably selected from acetylene, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
And / or cycloalkyl is C 3-8 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl; preferably C 3-7 cycloalkyl, Such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl; more preferably derived from C 3-6 cycloalkyl, such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;
And / or aryl is selected from phenyl, naphthyl or anthracene; preferably naphthyl and phenyl;
And / or heterocyclyl is a heterocyclic ring system having one or more saturated or unsaturated rings, at least one of which contains one or more selected from the group consisting of nitrogen, oxygen, and / or sulfur in the ring A group of heteroatoms; preferably a heterocyclic ring system having one or two saturated or unsaturated rings, at least one of which contains one or more selected from the group consisting of nitrogen, oxygen, and / or Heteroatoms of the group consisting of sulfur, more preferably selected from oxazepine, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran , Benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropiperan, morpholine, indolin, furan, triazole, isoxazole, pyrazole, thiophene, benzene Benzothiophene, pyrrole, pyrazine, pyrrolo [2,3b] pyridine, quinoline, quinolone, isoquinoline, tetrahydrothienopyridine, phthalazine, benzo-1,2,5-thiadiazole, indole Benzotriazole, benzoxazole, pendant oxopyridine, benzodioxane, benzodioxane, carbazole, oxaspirodecane or thiazole;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
p為0、1、2、3、4或5；較佳地，p為0、1或2；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
p is 0, 1, 2, 3, 4 or 5; preferably, p is 0, 1 or 2;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
q為0、1、2、3、4或5；較佳地，q為0、1或2；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
q is 0, 1, 2, 3, 4 or 5; preferably, q is 0, 1 or 2;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
n為0或1；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
n is 0 or 1;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
係選自
;
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
Selected from
;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
為-[C(Ra Rb )]p -R1 ；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
Is-[C (R a R b )] p -R 1 ;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
X係選自一鍵、-[CH2 ]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -；較佳地，X係選自一鍵、-CH2-、-CH2CH2-、-C(O)-、-C(O)NH-、-C(O)NHCH2-、-C(O)NHCH2CH2-、-NHC(O)-、-NHC(O)CH2-、-NHC(O)CH2CH2-、-N(CH3)C(O)CH2CH2-、-CH2NH-、-NHCH2-、-NHCH2CH2-、-N(CH3)CH2CH2-及-CH2NHCH2-；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
X is selected from one bond,-[CH 2 ] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N (R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ; preferably, X series One bond, -CH2-, -CH2CH2-, -C (O)-, -C (O) NH-, -C (O) NHCH2-, -C (O) NHCH2CH2-, -NHC (O)- , -NHC (O) CH2-, -NHC (O) CH2CH2-, -N (CH3) C (O) CH2CH2-, -CH2NH-, -NHCH2-, -NHCH2CH2-, -N (CH3) CH2CH2-, and- CH2NHCH2-;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
Y1 為-C(R10 R10 ' )-；較佳地，Y1 為-CH2-；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
Y 1 is -C (R 10 R 10 ' )-; preferably, Y 1 is -CH2-;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
Y2 為-C(R10 '' R10 ''' )-；較佳地，Y2 為-CH2-；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
Y 2 is -C (R 10 '' R 10 ''')-; preferably, Y 2 is -CH2-;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基；較佳地，Rz 係選自氫及經取代或未經取代之C1-6 烷基；更佳地，Rz 係選自氫及經取代或未經取代之甲基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, Substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl, and -C (O) -C 1-6 alkyl; preferably, R z is selected from hydrogen and substituted or Unsubstituted C 1-6 alkyl; more preferably, R z is selected from hydrogen and substituted or unsubstituted methyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；較佳地，R1 為經取代或未經取代的選自以下之基團：-N(CH3)(CH2CH3)-、-N(CH3)(環丙基)-、-NH-環己基、-NH-吡啶基、-NH-苯基、-NH-CH2-吡啶基、-NH-CH2-苯基、-NH-CH2-CH(N[CH3]2)-苯基、-NH-CH2CH2-苯基、-NH-CH2CH3、-NH-CH3、-NH-CH2-喹啉基、-NH-CH2-異喹啉基、-NH-CH2-噻吩基、-NH-CH2CH2-噻吩基、-NH-CH2-二氫茚基、-N(CH3)2、-N(CH3)(異丁基)、-N(CH3)(CH2-苯基)、-N(CH3)(CH2CH2-苯基)、-N(CH3)(CH2-噻吩基)、-NHC(O)-吡啶基、-NHC(O)-異丙基、-NHC(O)-苯基、-NHC(O)-CH2-噻吩基及-NHC(O)-CH2-苯基。
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 1 is selected from -NR 5 R 5 ′ and -NR 5 ′ C (O) R 5 ; preferably, R 1 is a substituted or unsubstituted group selected from -N (CH3) ( CH2CH3)-, -N (CH3) (cyclopropyl)-, -NH-cyclohexyl, -NH-pyridyl, -NH-phenyl, -NH-CH2-pyridyl, -NH-CH2-phenyl, -NH-CH2-CH (N [CH3] 2) -phenyl, -NH-CH2CH2-phenyl, -NH-CH2CH3, -NH-CH3, -NH-CH2-quinolinyl, -NH-CH2-iso Quinolinyl, -NH-CH2-thienyl, -NH-CH2CH2-thienyl, -NH-CH2-dihydroindenyl, -N (CH3) 2, -N (CH3) (isobutyl), -N (CH3) (CH2-phenyl), -N (CH3) (CH2CH2-phenyl), -N (CH3) (CH2-thienyl), -NHC (O) -pyridyl, -NHC (O) -iso Propyl, -NHC (O) -phenyl, -NHC (O) -CH2-thienyl, and -NHC (O) -CH2-phenyl.
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ；較佳地，R1 為經取代或未經取代的選自以下之基團：-NH-環己基、-NH-吡啶基、-NH-苯基、-NH-CH2-吡啶基、-NH-CH2-苯基、-NH-CH2-CH(N[CH3]2)-苯基、-NH-CH2CH2-苯基、-NH-CH2CH3、-NH-CH3、-NH-CH2-喹啉基、-NH-CH2-異喹啉基、-NH-CH2-噻吩基、-NH-CH2CH2-噻吩基、-NH-CH2-二氫茚基、-N(CH3)2、-N(CH3)(異丁基)、-N(CH3)(CH2-苯基)、-N(CH3)(CH2CH2-苯基)、-N(CH3)(CH2-噻吩基)、-NHC(O)-吡啶基、-NHC(O)-異丙基、-NHC(O)-苯基、-NHC(O)-CH2-噻吩基及-NHC(O)-CH2-苯基。
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 1 is selected from -NR 5 R 5 ' and -NR 5 ' C (O) R 5 ; preferably, R 1 is a substituted or unsubstituted group selected from -NH-cyclohexyl, -NH-pyridyl, -NH-phenyl, -NH-CH2-pyridyl, -NH-CH2-phenyl, -NH-CH2-CH (N [CH3] 2) -phenyl, -NH-CH2CH2- Phenyl, -NH-CH2CH3, -NH-CH3, -NH-CH2-quinolinyl, -NH-CH2-isoquinolinyl, -NH-CH2-thienyl, -NH-CH2CH2-thienyl, -NH -CH2-dihydroindenyl, -N (CH3) 2, -N (CH3) (isobutyl), -N (CH3) (CH2-phenyl), -N (CH3) (CH2CH2-phenyl), -N (CH3) (CH2-thienyl), -NHC (O) -pyridyl, -NHC (O) -isopropyl, -NHC (O) -phenyl, -NHC (O) -CH2-thienyl And -NHC (O) -CH2-phenyl.
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基；較佳地，R2 係選自經取代或未經取代之芳基及經取代或未經取代之芳族雜環基；更佳地，R2 係選自經取代或未經取代之苯基及經取代或未經取代之噻吩；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 2 is selected from substituted or unsubstituted aryl groups and substituted or unsubstituted heterocyclic groups; preferably, R 2 is selected from substituted or unsubstituted aryl groups and substituted or unsubstituted Substituted aromatic heterocyclic groups; more preferably, R 2 is selected from substituted or unsubstituted phenyl and substituted or unsubstituted thiophene;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基；較佳地，R3 係選自經取代或未經取代之甲基及經取代或未經取代之乙基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; preferably, R 3 is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R3 ' 為氫；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 3 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; Preferably, R 3 ′ is hydrogen;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C(O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ；
其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
較佳地，R4 及R4 ' 均為氫；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 4 and R 4 'are independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' , -S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' and -C (CH 3 ) 2 OR 41 ;
Wherein R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted alkenyl group of C 2-6 and substituted or unsubstituted Substituted C 2-6 alkynyl;
Preferably, R 4 and R 4 ′ are both hydrogen;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；較佳地，R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；更佳地，R5 為經取代或未經取代的選自以下之基團：吡啶基、苯基、-CH2-吡啶基、苄基、-CH2CH(N[CH3]2)-苯基、苯乙基、乙基、甲基、異丙基、異丁基、-CH2-喹啉基、-CH2-異喹啉基、-CH2-噻吩基、-CH2CH2-噻吩基、-CH2-二氫茚基、環丙基及環己基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl; preferably, R 5 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted cycloalkyl , Substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheteroaryl; better R 5 is a substituted or unsubstituted group selected from the group consisting of pyridyl, phenyl, -CH2-pyridyl, benzyl, -CH2CH (N [CH3] 2) -phenyl, phenethyl, Ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2-dihydroindenyl, ring Propyl and cyclohexyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；較佳地，R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基；更佳地，R5 為經取代或未經取代的選自以下之基團：吡啶基、苯基、-CH2-吡啶基、苄基、-CH2CH(N[CH3]2)-苯基、苯乙基、乙基、甲基、異丙基、異丁基、-CH2-喹啉基、-CH2-異喹啉基、-CH2-噻吩基、-CH2-二氫茚基及環己基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 5 is selected from the group consisting of substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or Unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkane Aryl and substituted or unsubstituted alkylheteroaryl; preferably, R 5 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted cycloalkyl , Substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheteroaryl; more preferably R 5 is a substituted or unsubstituted group selected from the group consisting of pyridyl, phenyl, -CH2-pyridyl, benzyl, -CH2CH (N [CH3] 2) -phenyl, phenethyl, Ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2-dihydroindenyl, and cyclohexyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R5 ' 係選自氫及經取代或未經取代之C1-6 烷基，更佳地，R5 ' 係選自氫及經取代或未經取代之甲基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 5 ′ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; Preferably, R 5 ′ is selected from hydrogen and a substituted or unsubstituted C 1-6 alkyl group, more preferably, R 5 ′ is selected from hydrogen and a substituted or unsubstituted methyl group;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ；較佳地，R6 及R6 ' 均為氫；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 6 and R 6 'are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ' , -NR 21 C (O) R 21 ' , -NR 21 S (O ) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S (O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S (O) 2 NR 21 ' R 21 '' and -C (CH 3 ) 2 OR 21 ; preferably, R 6 and R 6 ′ are both hydrogen;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R10 及R10 ' 均為氫；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 10 and R 10 ′ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl; preferably, R 10 and R 10 ′ are both hydrogen;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R10 '' 及R10 ''' 均為氫；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 10 '' and R 10 '''are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; preferably, R 10 '' and R 10 ′ '' are both hydrogen;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 21, R 21 'and R 21' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R31 、R31 ' 及R31 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 31, R 31 'and R 31' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R32 及R32 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 32 and R 32 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R41 為氫；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 41, R 41 'and R 41' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl; preferably, R 41 is hydrogen;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R51 、R51 ' 及R51 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；較佳地，R51 及R51 ' 獨立地選自氫及經取代或未經取代之甲基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 51, R 51 'and R 51' 'are independently selected from hydrogen, substituted or unsubstituted alkyl group of C 1-6, substituted or unsubstituted C 2-6 alkenyl group and the substituted or non- Substituted C 2-6 alkynyl; preferably, R 51 and R 51 ′ are independently selected from hydrogen and substituted or unsubstituted methyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R52 及R52 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 52 and R 52 'are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R13 及R13 ' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基及未經取代之C2-6 炔基；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 13 and R 13 ′ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
R14 、R14 ' 及R14 '' 獨立地選自氫、未經取代之C1-6 烷基、未經取代之C2-6 烯基、未經取代之C2-6 炔基、未經取代之芳基、未經取代之環烷基及未經取代之雜環基；較佳地，R14 為氫；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
R 14, R 14 'and R 14' 'are independently selected from hydrogen, non-substituted C 1-6 alkyl, unsubstituted alkenyl group of C 2-6, unsubstituted C 2-6 alkynyl group of, Unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclic group; preferably, R 14 is hydrogen;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明根據通式(I)之另一個較佳實施例中，化合物為以下化合物，其中
p為0、1或2；
及
q為0、1或2
及
n為0或1；
及
X係選自一鍵、-CH2-、-CH2CH2-、-C(O)-、-C(O)NH-、-C(O)NHCH2-、-C(O)NHCH2CH2-、-NHC(O)-、-NHC(O)CH2-、-NHC(O)CH2CH2-、-N(CH3)C(O)CH2CH2-、-CH2NH-、-NHCH2-、-NHCH2CH2-、-N(CH3)CH2CH2-及-CH2NHCH2-；
及
Y1 為-CH2-；
及
Y2 為-CH2-；
及
Rz 係選自氫及經取代或未經取代之C1-6 烷基；更佳地，Rz 係選自氫及經取代或未經取代之甲基；
及
R1 為經取代或未經取代的選自以下之基團：-N(CH3)(CH2CH3)-、-N(CH3)(環丙基)-、-NH-環己基、-NH-吡啶基、-NH-苯基、-NH-CH3-吡啶基、-NH-CH2-苯基、-NH-CH2-CH(N[CH3]2)-苯基、-NH-CH2CH2-苯基、-NH-CH2CH3、-NH-CH3、-NH-CH2-喹啉基、-NH-CH2-異喹啉基、-NH-CH2-噻吩基、-NH-CH2CH2-噻吩基、-NH-CH2-二氫茚基、-N(CH3)2、-N(CH3)(異丁基)、-N(CH3)(CH2-苯基)、-N(CH3)(CH2CH2-苯基)、-N(CH3)(CH2-噻吩基)、-NHC(O)-吡啶基、-NHC(O)-異丙基、-NHC(O)-苯基、-NHC(O)-CH2-噻吩基及-NHC(O)-CH2-苯基；
及
R2 係選自經取代或未經取代之苯基及經取代或未經取代之噻吩；
及
R3 係選自經取代或未經取代之甲基及經取代或未經取代之乙基；
及
R3 ' 為氫；
及
R4 及R4 ' 均為氫；
及
R5 為經取代或未經取代的選自以下之基團：吡啶基、苯基、-CH2-吡啶基、苄基、-CH2CH(N[CH3]2)-苯基、苯乙基、乙基、甲基、異丙基、異丁基、-CH2-喹啉基、-CH2-異喹啉基、-CH2-噻吩基、-CH2CH2-噻吩基、-CH2-二氫茚基、環丙基及環己基；
及
R5 ' 係選自氫及經取代或未經取代之甲基；
及
R6 及R6 ' 均為氫；
及
R10 及R10 ' 均為氫；
及
R10 '' 及R10 ''' 均為氫；
及
R41 為氫；
及
R51 及R51 ' 獨立地選自氫及經取代或未經取代之甲基；
及
R14 為氫；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment of the present invention according to general formula (I), the compound is the following compound, wherein
p is 0, 1, or 2;
and
q is 0, 1, or 2
and
n is 0 or 1;
and
X is selected from one bond, -CH2-, -CH2CH2-, -C (O)-, -C (O) NH-, -C (O) NHCH2-, -C (O) NHCH2CH2-, -NHC (O )-, -NHC (O) CH2-, -NHC (O) CH2CH2-, -N (CH3) C (O) CH2CH2-, -CH2NH-, -NHCH2-, -NHCH2CH2-, -N (CH3) CH2CH2- And -CH2NHCH2-;
and
Y 1 is -CH2-;
and
Y 2 is -CH2-;
and
R z is selected from hydrogen and substituted or unsubstituted C 1-6 alkyl; more preferably, R z is selected from hydrogen and substituted or unsubstituted methyl;
and
R 1 is a substituted or unsubstituted group selected from -N (CH3) (CH2CH3)-, -N (CH3) (cyclopropyl)-, -NH-cyclohexyl, -NH-pyridyl , -NH-phenyl, -NH-CH3-pyridyl, -NH-CH2-phenyl, -NH-CH2-CH (N [CH3] 2) -phenyl, -NH-CH2CH2-phenyl, -NH -CH2CH3, -NH-CH3, -NH-CH2-quinolinyl, -NH-CH2-isoquinolinyl, -NH-CH2-thienyl, -NH-CH2CH2-thienyl, -NH-CH2-dihydro Indenyl, -N (CH3) 2, -N (CH3) (isobutyl), -N (CH3) (CH2-phenyl), -N (CH3) (CH2CH2-phenyl), -N (CH3) (CH2-thienyl), -NHC (O) -pyridyl, -NHC (O) -isopropyl, -NHC (O) -phenyl, -NHC (O) -CH2-thienyl and -NHC (O ) -CH2-phenyl;
and
R 2 is selected from substituted or unsubstituted phenyl and substituted or unsubstituted thiophene;
and
R 3 is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl;
and
R 3 ' is hydrogen;
and
R 4 and R 4 ' are both hydrogen;
and
R 5 is a substituted or unsubstituted group selected from pyridyl, phenyl, -CH2-pyridyl, benzyl, -CH2CH (N [CH3] 2) -phenyl, phenethyl, ethyl Methyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2-dihydroindenyl, cyclopropyl And cyclohexyl;
and
R 5 ' is selected from hydrogen and substituted or unsubstituted methyl;
and
R 6 and R 6 ' are both hydrogen;
and
R 10 and R 10 ' are both hydrogen;
and
R 10 '' and R 10 ''' are both hydrogen;
and
R 41 is hydrogen;
and
R 51 and R 51 'are independently selected from hydrogen and substituted or unsubstituted methyl;
and
R 14 is hydrogen;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在一個較佳實施例中
p為0、1或2；In a preferred embodiment
p is 0, 1, or 2;

在一個較佳實施例中
q為0、1或2In a preferred embodiment
q is 0, 1, or 2

在一個較佳實施例中
n為0或1；In a preferred embodiment
n is 0 or 1;

在一個較佳實施例中
X係選自一鍵、-CH2-、-CH2CH2-、-C(O)-、-C(O)NH-、-C(O)NHCH2-、-C(O)NHCH2CH2-、-NHC(O)-、-NHC(O)CH2-、-NHC(O)CH2CH2-、-N(CH3)C(O)CH2CH2-、-CH2NH-、-NHCH2-、-NHCH2CH2-、-N(CH3)CH2CH2-及-CH2NHCH2-；In a preferred embodiment
X is selected from one bond, -CH2-, -CH2CH2-, -C (O)-, -C (O) NH-, -C (O) NHCH2-, -C (O) NHCH2CH2-, -NHC (O )-, -NHC (O) CH2-, -NHC (O) CH2CH2-, -N (CH3) C (O) CH2CH2-, -CH2NH-, -NHCH2-, -NHCH2CH2-, -N (CH3) CH2CH2- And -CH2NHCH2-;

在一個較佳實施例中
X係選自一鍵、-CH2-、-CH2CH2-、-C(O)-、-C(O)NHCH2-、-C(O)NHCH2CH2-、-NHC(O)-、-NHC(O)CH2-、-NHC(O)CH2CH2-、-N(CH3)C(O)CH2CH2-、-NHCH2-、-NHCH2CH2-、-N(CH3)CH2CH2-及-CH2NHCH2-。In a preferred embodiment
X is selected from one bond, -CH2-, -CH2CH2-, -C (O)-, -C (O) NHCH2-, -C (O) NHCH2CH2-, -NHC (O)-, -NHC (O) CH2-, -NHC (O) CH2CH2-, -N (CH3) C (O) CH2CH2-, -NHCH2-, -NHCH2CH2-, -N (CH3) CH2CH2-, and -CH2NHCH2-.

在一個較佳實施例中
Y1 為-CH2-；In a preferred embodiment
Y 1 is -CH2-;

在一個較佳實施例中
Y2 為-CH2-；In a preferred embodiment
Y 2 is -CH2-;

在一個較佳實施例中
Rz 係選自氫及經取代或未經取代之甲基；In a preferred embodiment
R z is selected from hydrogen and substituted or unsubstituted methyl;

在一個較佳實施例中
R1 為經取代或未經取代的選自以下之基團：-NH-環己基、-NH-吡啶基、-NH-苯基、-NH-CH3-吡啶基、-NH-CH2-苯基、-NH-CH2-CH(N[CH3]2)-苯基、-NH-CH2CH2-苯基、-NH-CH2CH3、-NH-CH3、-NH-CH2-喹啉基、-NH-CH2-異喹啉基、-NH-CH2-噻吩基、-NH-CH2CH2-噻吩基、-NH-CH2-二氫茚基、-N(CH3)2、-N(CH3)(異丁基)、-N(CH3)(CH2-苯基)、-N(CH3)(CH2CH2-苯基)、-N(CH3)(CH2-噻吩基)、-NHC(O)-吡啶基、-NHC(O)-異丙基、-NHC(O)-苯基、-NHC(O)-CH2-噻吩基及-NHC(O)-CH2-苯基。In a preferred embodiment
R 1 is a substituted or unsubstituted group selected from -NH-cyclohexyl, -NH-pyridyl, -NH-phenyl, -NH-CH3-pyridyl, -NH-CH2-phenyl , -NH-CH2-CH (N [CH3] 2) -phenyl, -NH-CH2CH2-phenyl, -NH-CH2CH3, -NH-CH3, -NH-CH2-quinolinyl, -NH-CH2- Isoquinolinyl, -NH-CH2-thienyl, -NH-CH2CH2-thienyl, -NH-CH2-dihydroindenyl, -N (CH3) 2, -N (CH3) (isobutyl),- N (CH3) (CH2-phenyl), -N (CH3) (CH2CH2-phenyl), -N (CH3) (CH2-thienyl), -NHC (O) -pyridyl, -NHC (O)- Isopropyl, -NHC (O) -phenyl, -NHC (O) -CH2-thienyl, and -NHC (O) -CH2-phenyl.

在另一個較佳實施例中
R1 為經取代或未經取代的選自以下之基團：-N(CH3)(CH2CH3)、-N(CH3)(CH2CH2OCH3)、-N(CH3)(CH2CH2-CN)、-N(CH3)(環丙基)、-NH-環己基、-NH-吡啶基、-NH-苯基、-NH-CH3-吡啶基、-NH-CH2-苯基、-NH-CH2-CH(N[CH3]2)-苯基、-NH-CH2CH2-苯基、-NH-CH2CH3、-NH-CH3、-NH-CH2-喹啉基、-NH-CH2-異喹啉基、-NH-CH2-噻吩基、-NH-CH2CH2-噻吩基、-NH-CH2-二氫茚基、-N(CH3)2、-N(CH3)(異丁基)、-N(CH3)(CH2-苯基)、-N(CH3)(CH2CH2-苯基)、-N(CH3)(CH2-噻吩基)、-NHC(O)-吡啶基、-NHC(O)-異丙基、-NHC(O)-苯基、-NHC(O)-CH2-噻吩基及-NHC(O)-CH2-苯基。In another preferred embodiment
R 1 is a substituted or unsubstituted group selected from -N (CH3) (CH2CH3), -N (CH3) (CH2CH2OCH3), -N (CH3) (CH2CH2-CN), -N (CH3 ) (Cyclopropyl), -NH-cyclohexyl, -NH-pyridyl, -NH-phenyl, -NH-CH3-pyridyl, -NH-CH2-phenyl, -NH-CH2-CH (N [ CH3] 2) -phenyl, -NH-CH2CH2-phenyl, -NH-CH2CH3, -NH-CH3, -NH-CH2-quinolinyl, -NH-CH2-isoquinolinyl, -NH-CH2- Thienyl, -NH-CH2CH2-thienyl, -NH-CH2-dihydroindenyl, -N (CH3) 2, -N (CH3) (isobutyl), -N (CH3) (CH2-phenyl) , -N (CH3) (CH2CH2-phenyl), -N (CH3) (CH2-thienyl), -NHC (O) -pyridyl, -NHC (O) -isopropyl, -NHC (O)- Phenyl, -NHC (O) -CH2-thienyl, and -NHC (O) -CH2-phenyl.

在一個較佳實施例中
R2 係選自經取代或未經取代之苯基及經取代或未經取代之噻吩；In a preferred embodiment
R 2 is selected from substituted or unsubstituted phenyl and substituted or unsubstituted thiophene;

在一個較佳實施例中
R3 係選自經取代或未經取代之甲基及經取代或未經取代之乙基；In a preferred embodiment
R 3 is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl;

在一個較佳實施例中
R3 ' 為氫；In a preferred embodiment
R 3 ' is hydrogen;

在一個較佳實施例中
R4 及R4 ' 均為氫；In a preferred embodiment
R 4 and R 4 ' are both hydrogen;

在一個較佳實施例中
R5 為經取代或未經取代的選自以下之基團：吡啶基、苯基、-CH2-吡啶基、苄基、-CH2CH(N[CH3]2)-苯基、苯乙基、乙基、甲基、異丙基、異丁基、-CH2-喹啉基、-CH2-異喹啉基、-CH2-噻吩基、-CH2-二氫茚基、及環己基。In a preferred embodiment
R 5 is a substituted or unsubstituted group selected from pyridyl, phenyl, -CH2-pyridyl, benzyl, -CH2CH (N [CH3] 2) -phenyl, phenethyl, ethyl Group, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2-dihydroindenyl, and cyclohexyl.

在另一個較佳實施例中
R5 為經取代或未經取代的選自以下之基團：吡啶基、苯基、-CH2-吡啶基、CH2CH3、CH2CH2OCH3、CH2CH2-CN、苄基、-CH2CH(N[CH3]2)-苯基、苯乙基、乙基、甲基、異丙基、異丁基、-CH2-喹啉基、-CH2-異喹啉基、-CH2-噻吩基、-CH2CH2-噻吩基、-CH2-二氫茚基、環丙基及環己基。In another preferred embodiment
R 5 is a substituted or unsubstituted group selected from: pyridyl, phenyl, -CH2-pyridyl, CH2CH3, CH2CH2OCH3, CH2CH2-CN, benzyl, -CH2CH (N [CH3] 2)- Phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2 -Dihydroindenyl, cyclopropyl and cyclohexyl.

在一個較佳實施例中
R5 ' 係選自氫及經取代或未經取代之甲基；In a preferred embodiment
R 5 ' is selected from hydrogen and substituted or unsubstituted methyl;

在一個較佳實施例中
R6 及R6 ' 均為氫；In a preferred embodiment
R 6 and R 6 ' are both hydrogen;

在一個較佳實施例中
R10 及R10 ' 均為氫；In a preferred embodiment
R 10 and R 10 ' are both hydrogen;

在一個較佳實施例中
R10 '' 及R10 ''' 均為氫；In a preferred embodiment
R 10 '' and R 10 ''' are both hydrogen;

在一個較佳實施例中
R14 為氫；In a preferred embodiment
R 14 is hydrogen;

在一個較佳實施例中
R41 為氫；In a preferred embodiment
R 41 is hydrogen;

在一個較佳實施例中
R51 及R51 ' 均為經取代或未經取代之甲基；In a preferred embodiment
R 51 and R 51 ' are substituted or unsubstituted methyl groups;

在一個較佳實施例中
R51 為經取代或未經取代之甲基；In a preferred embodiment
R 51 is a substituted or unsubstituted methyl group;

在一個較佳實施例中
R51 為氫；In a preferred embodiment
R 51 is hydrogen;

在一個較佳實施例中
R3 係選自經取代或未經取代之甲基及經取代或未經取代之乙基，而R3 ' 為氫；In a preferred embodiment
R 3 is selected from a substituted or unsubstituted methyl group and a substituted or unsubstituted ethyl group, and R 3 ′ is hydrogen;

在一個較佳實施例中
R5 為經取代或未經取代的選自以下之基團：吡啶基、苯基、-CH2-吡啶基、苄基、-CH2CH(N[CH3]2)-苯基、苯乙基、乙基、甲基、異丙基、異丁基、-CH2-喹啉基、-CH2-異喹啉基、-CH2-噻吩基、-CH2-二氫茚基、及環己基，而R5 ' 係選自氫及經取代或未經取代之甲基。In a preferred embodiment
R 5 is a substituted or unsubstituted group selected from pyridyl, phenyl, -CH2-pyridyl, benzyl, -CH2CH (N [CH3] 2) -phenyl, phenethyl, ethyl Methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2-dihydroindenyl, and cyclohexyl, and R 5 ' It is selected from hydrogen and substituted or unsubstituted methyl.

在另一個較佳實施例中
R5 為經取代或未經取代的選自以下之基團：吡啶基、苯基、-CH2-吡啶基、CH2CH3、CH2CH2OCH3、CH2CH2-CN、苄基、-CH2CH(N[CH3]2)-苯基、苯乙基、乙基、甲基、異丙基、異丁基、-CH2-喹啉基、-CH2-異喹啉基、-CH2-噻吩基、-CH2CH2-噻吩基、-CH2-二氫茚基、環丙基及環己基，而R5 ' 係選自氫及經取代或未經取代之甲基。In another preferred embodiment
R 5 is a substituted or unsubstituted group selected from: pyridyl, phenyl, -CH2-pyridyl, CH2CH3, CH2CH2OCH3, CH2CH2-CN, benzyl, -CH2CH (N [CH3] 2)- Phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2 - indanyl, cyclopropyl and cyclohexyl, and R 5 'is selected from hydrogen and a substituted or non-substituted methyl group.

在一個較佳實施例中
R5 為經取代或未經取代的選自以下之基團：吡啶基、苯基、-CH2-吡啶基、苄基、-CH2CH(N[CH3]2)-苯基、苯乙基、乙基、甲基、異丙基、異丁基、-CH2-喹啉基、-CH2-異喹啉基、-CH2-噻吩基、-CH2CH2-噻吩基、-CH2-二氫茚基及環己基，而R5 ' 為氫。In a preferred embodiment
R 5 is a substituted or unsubstituted group selected from pyridyl, phenyl, -CH2-pyridyl, benzyl, -CH2CH (N [CH3] 2) -phenyl, phenethyl, ethyl Methyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2-dihydroindenyl, and cyclohexyl And R 5 ' is hydrogen.

在一個較佳實施例中
R5 為經取代或未經取代的選自以下之基團：吡啶基、苯基、-CH2-吡啶基、苄基、-CH2CH(N[CH3]2)-苯基、苯乙基、乙基、甲基、異丙基、異丁基、-CH2-喹啉基、-CH2-異喹啉基、-CH2-噻吩基、-CH2CH2-噻吩基、-CH2-二氫茚基及環己基，而R5 ' 為經取代或未經取代之甲基。In a preferred embodiment
R 5 is a substituted or unsubstituted group selected from pyridyl, phenyl, -CH2-pyridyl, benzyl, -CH2CH (N [CH3] 2) -phenyl, phenethyl, ethyl Methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2-dihydroindenyl, and cyclohexyl And R 5 ' is a substituted or unsubstituted methyl group.

在一個較佳實施例中
R5 為經取代或未經取代的選自以下之基團：甲基、異丁基、苄基、苯乙基及噻吩基，而R5 ' 為經取代或未經取代之甲基。In a preferred embodiment
R 5 is a substituted or unsubstituted group selected from methyl, isobutyl, benzyl, phenethyl, and thienyl, and R 5 ′ is a substituted or unsubstituted methyl.

在另一個較佳實施例中
R5 為經取代或未經取代的選自以下之基團：甲基、乙基、異丁基、CH2CH2OCH3、CH2CH2-CN、環丙基、苄基、苯乙基及 -CH2-噻吩基，而R5 ' 為經取代或未經取代之甲基In another preferred embodiment
R 5 is a substituted or unsubstituted group selected from methyl, ethyl, isobutyl, CH2CH2OCH3, CH2CH2-CN, cyclopropyl, benzyl, phenethyl, and -CH2-thienyl, R 5 ' is a substituted or unsubstituted methyl group

在一個較佳實施例中
R5 為經取代或未經取代的選自以下之基團：吡啶基、苯基、-CH2-吡啶基、苄基、-CH2CH(N[CH3]2)-苯基、苯乙基、乙基、甲基、異丙基、-CH2-喹啉基、-CH2-異喹啉基、-CH2-噻吩基、-CH2CH2-噻吩基、-CH2-二氫茚基及環己基，而R5 ' 為氫；In a preferred embodiment
R 5 is a substituted or unsubstituted group selected from pyridyl, phenyl, -CH2-pyridyl, benzyl, -CH2CH (N [CH3] 2) -phenyl, phenethyl, ethyl Methyl, isopropyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2-dihydroindenyl, and cyclohexyl, and R 5 ' Is hydrogen;

在本發明之通式(I)化合物的一個實施例中，
鹵素為氟、氯、碘或溴；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In one embodiment of the compound of formula (I) of the present invention,
Halogen is fluorine, chlorine, iodine or bromine;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明之通式(I)化合物的一個實施例中，
鹵烷基為-CF3；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In one embodiment of the compound of formula (I) of the present invention,
Haloalkyl is -CF3;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在本發明之通式(I)化合物的另一個實施例中，
鹵烷氧基為-OCF3；
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another embodiment of the compound of formula (I) of the present invention,
Haloalkoxy is -OCF3;
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個較佳實施例中，通式(I)化合物係選自
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment, the compound of general formula (I) is selected from
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個較佳實施例中，化合物為
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment, the compound is
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個較佳實施例中，化合物為
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment, the compound is
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個較佳實施例中，化合物為
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment, the compound is
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

在另一個較佳實施例中，通式(I)化合物係選自
其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，為外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物的形式，或為其對應之鹽或其對應之溶劑合物。In another preferred embodiment, the compound of general formula (I) is selected from
It optionally takes the form of a stereoisomer (preferably, an enantiomer or a diastereomer), a racemate, or at least two stereoisomers (preferably, Enantiomers and / or diastereomers) in the form of a mixture in any mixing ratio, or as its corresponding salt or its corresponding solvate.

由於本發明旨在提供充當電壓閘控鈣通道之α2 δ子單元(尤其α2 δ-1子單元)之雙重配位體的化合物或一系列化學相關化合物，故極佳實施例為其中選擇充當電壓閘控鈣通道之α2 δ子單元(尤其α2 δ-1子單元)之配位體的化合物及尤其以Ki 表示之結合對應於以下標度的化合物：
Ki(α2δ1)較佳＜ 10000 nM，更佳＜ 5000 nM，甚至更佳＜ 500 nM。Since the present invention aims to provide a compound or a series of chemically related compounds that serve as dual ligands of the α 2 δ subunit (especially α 2 δ-1 subunit) of a voltage-gated calcium channel, an excellent embodiment is selected among them Compounds that act as ligands for the α 2 δ subunit (especially the α 2 δ-1 subunit) of the voltage-gated calcium channel, and the compounds represented by K i in particular correspond to the following scales:
Ki (α2δ1) is preferably <10000 nM, more preferably <5000 nM, even more preferably <500 nM.

在下文中，使用片語「本發明化合物」。此應理解為如上文根據通式(I)、(I')、(Ia )、(Ia ' )、(Ib )、(Ib ' )及(IZ)所描述的本發明之任何化合物。In the following, the phrase "compounds of the invention" is used. This is understood to be any according to the above general formula (I), (I ') , (I a), (I a'), (I b), (I b ') , and the present invention (IZ) as described Compound.

由上文所描述之式(I)表示的本發明化合物可包括對映異構體，視對掌性中心之存在而定，或異構體(例如Z、E)，視多重鍵之存在而定。單個異構體、對映異構體或非對映異構體及其混合物屬於本發明之範疇。The compounds of the present invention represented by the formula (I) described above may include enantiomers, depending on the existence of a palmar center, or isomers (e.g., Z, E), depending on the presence of multiple bonds set. Individual isomers, enantiomers or diastereomers and mixtures thereof fall within the scope of the invention.

為清楚起見，表述「式(I)之化合物，其中例如R1 、R2 、R3 、R3 ' 、R4 、R4 ' 、X、Y1 、Y2 及n如下文詳細說明中所定義」將(正如技術方案中所見之表述「例如技術方案1至8中任一項所定義之式(I)化合物」)係指「式(I)之化合物」，其中應用各別取代基R1 等之定義(亦來自所引用之技術方案)。另外，此亦意謂，儘管如此(尤其關於技術方案)，本說明書中所定義(或在所引用之技術方案中任一項(例如技術方案1)中所用)的一或多個排除式請求(disclaimers)可適用於定義各別化合物。因此，見於例如技術方案1中之排除式請求亦用於定義「如對應之相關技術方案(例如技術方案1至8)中任一項所定義之式(I)」化合物。For the sake of clarity, the expression "compounds of formula (I), where for example R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , X, Y 1 , Y 2 and n are described in the detailed description below. "Defined" will (as the expression "such as the compound of formula (I) defined in any one of schemes 1 to 8" as seen in the technical scheme) means "the compound of formula (I)" in which the respective substituents are applied The definition of R 1 etc. (also from the cited technical solution). In addition, this also means that, despite this (especially regarding the technical solution), one or more excluded requests defined in this specification (or used in any of the cited technical solutions (such as technical solution 1)) (disclaimers) can be applied to define individual compounds. Therefore, the exclusion request found in, for example, technical solution 1 is also used to define a compound of formula (I) as defined in any one of the corresponding related technical solutions (for example, technical solutions 1 to 8).

一般而言，該等方法描述於下文實驗部分中。起始物質為市售的或可藉由習知方法製備。In general, these methods are described in the experimental section below. The starting materials are commercially available or can be prepared by conventional methods.

本發明之一個較佳態樣亦為一種用於產生式(I)之化合物的方法，其遵循流程1、流程2、流程3、流程4、流程5、流程6或流程7進行。A preferred aspect of the present invention is also a method for producing a compound of formula (I), which is performed according to Scheme 1, Scheme 2, Scheme 3, Scheme 4, Scheme 5, Scheme 6 or Scheme 7.

已開發出兩種不同通用方法用於獲得本發明化合物，如下文方法A及B中所描述，且進一步詳述於流程1至7中。Two different general methods have been developed for obtaining the compounds of the invention, as described below in Methods A and B, and are further detailed in Schemes 1-7.

本發明之一個較佳實施例為一種用於產生式(I)之化合物的方法，其中，若未另外定義，則R1 、R2 、R3 、R3 ' 、R4 、R4 ' 、X、Y1 、Y2 及n具有本說明書中所定義之意義。A preferred embodiment of the present invention is a method for producing a compound of formula (I), wherein, if not otherwise defined, R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , X, Y 1 , Y 2 and n have the meanings defined in this specification.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，

其中-X為一鍵，且R1 表示-NR5 R5 ' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，該方法包含使式(IIa)化合物

其中Q表示氯、溴、碘或三氟甲磺酸酯，A表示-NR3 R3' ，且R2 、R3 、R3' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-2之胺反應，

其中R5 及R5 ' 具有如本說明書中所定義之意義。In a particular embodiment, there is a method for producing a compound of formula (I),

Where -X is a bond, and R 1 represents -NR 5 R 5 ′ , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n Having the meaning as defined in this specification, the method comprising making a compound of formula (IIa)

Wherein Q represents chlorine, bromine, iodine or triflate, A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3' , R 4 , R 4 ' and n have Meaning of definition, reaction with amine of formula III-2,

R 5 and R 5 ′ have the meanings as defined in the present specification.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，

其中-X為一鍵，且R1 表示-NR5 ' C(O)R5 ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，該方法包含使式(IIa)化合物

其中Q表示氯、溴、碘或三氟甲磺酸酯，A表示-NR3 R3' ，且R2 、R3 、R3' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-3之胺反應，

其中R5 及R5 ' 具有如本說明書中所定義之意義。In a particular embodiment, there is a method for producing a compound of formula (I),

Where -X is a bond, and R 1 represents -NR 5 ' C (O) R 5 , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ' , R 4 , R 4 ' and n have the meanings as defined in the present specification, and the method comprises making a compound of formula (IIa)

Wherein Q represents chlorine, bromine, iodine or triflate, A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3' , R 4 , R 4 ' and n have Meaning of definition, reaction with amine of formula III-3,

R 5 and R 5 ′ have the meanings as defined in the present specification.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，

其中-X-R1 表示-[CH2 ]p -NR5 R5' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 及n及p具有如本說明書中所定義之意義，該方法包含使式(IIb)化合物

其中r為1、2、3或4，A表示-NR3 R3' ，且R2 、R3 、R3' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-2之胺反應，

其中R5 及R5 ' 具有如本說明書中所定義之意義。In a particular embodiment, there is a method for producing a compound of formula (I),

Where -XR 1 represents-[CH 2 ] p -NR 5 R 5 ' , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ' , R 4 , R 4 ' and n And p have the meanings as defined in the present specification, and the method comprises making a compound of formula (IIb)

Where r is 1, 2, 3 or 4, and A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3' , R 4 , R 4 ' and n have the meanings as defined in the present specification, and The amine reaction of formula III-2,

R 5 and R 5 ′ have the meanings as defined in the present specification.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，

其中-X-R1 表示-[CH2 ]p -NR5 R5' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 及n及p具有如本說明書中所定義之意義，該方法包含使式(IIa)化合物

其中Q表示氯、溴、碘或三氟甲磺酸酯，A表示-NR3 R3' ，且R2 、R3 、R3' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-4之有機金屬試劑反應，

其中R5 及R5 ' 及p具有如本說明書中所定義之意義，且M表示適合之有機金屬基團，較佳為硼或鋅試劑。In a particular embodiment, there is a method for producing a compound of formula (I),

Where -XR 1 represents-[CH 2 ] p -NR 5 R 5 ' , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ' , R 4 , R 4 ' and n And p have the meanings as defined in the present specification, and the method comprises making a compound of formula (IIa)

Wherein Q represents chlorine, bromine, iodine or triflate, A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3' , R 4 , R 4 ' and n have Meaning of definition, reaction with organometallic reagent of formula III-4,

Wherein R 5 and R 5 ′ and p have the meanings as defined in the present specification, and M represents a suitable organometallic group, preferably a boron or zinc reagent.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，

其中-X為一鍵，且R1 表示-NR5 R5 ' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 及n具有如本說明書中所定義之意義，該方法包含使式(IIc)化合物

其中A表示-NR3 R3' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-5之醛在還原性胺化條件下反應，
或
與式III-6之烷基化劑在常規烷基化條件下反應，

其中R5 具有如本說明書中所定義之意義，且LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基。In a particular embodiment, there is a method for producing a compound of formula (I),

Where -X is a bond, and R 1 represents -NR 5 R 5 ′ , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 5, R 5 'and n have the meanings as defined in the present specification, the method comprising compound (IIc) of the formula

Wherein A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ and n have the meanings as defined in the present specification. Reaction under chemical conditions,
Or react with an alkylating agent of formula III-6 under conventional alkylating conditions,

Wherein R 5 has the meaning as defined in the present specification, and LG represents a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate .

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，

其中-X為一鍵，且R1 表示-NR5 ' C(O)R5 ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 及n具有如本說明書中所定義之意義，該方法包含使式(Ie)化合物

其中A表示-NR3 R3' ，且R2 、R3 、R3 ' 、R4 、R4 ' 、R5 及n具有如本說明書中所定義之意義，與式III-6'之烷基化劑反應，

其中R5 ' 具有如本說明書中所定義之意義但與氫不同，且LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基。In a particular embodiment, there is a method for producing a compound of formula (I),

Where -X is a bond, and R 1 represents -NR 5 ' C (O) R 5 , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ' , R 4 , R 4 ', R 5, R 5 ' and n have the meanings as defined in the present specification, the method comprising compound (Ie) of formula

Wherein A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 5 and n have the meanings as defined in the present specification, and the alkane of formula III-6 ′ Basing agent reaction,

Wherein R 5 ′ has the meaning as defined in the present specification but is different from hydrogen, and LG represents such as chlorine, bromine, iodine, methanesulfonate, tosylate, nitrobenzenesulfonate, or triflate Ester leaving group.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，

其中-X為-[CH2 ]p-，且R1 表示-C(O)NR5 R5 ' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 及n及p具有如本說明書中所定義之意義，該方法包含使式(IId)化合物

其中A表示-NR3 R3' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n及p具有如本說明書中所定義之意義，與式III-2之胺在醯胺化條件下反應，

其中R5 ' 及R5 ' 具有如本說明書中所定義之意義。In a particular embodiment, there is a method for producing a compound of formula (I),

Where -X is-[CH 2 ] p-, and R 1 represents -C (O) NR 5 R 5 ' , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ' , R 4 , R 4 ′ , R 5 , R 5 ′, and n and p have the meanings as defined in the present specification, and the method includes making a compound of formula (IId)

Wherein A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n and p have the meanings as defined in the present specification, and are the same as those of the amine of formula III-2. Reaction under amination conditions,

R 5 ′ and R 5 ′ have the meanings as defined in the present specification.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，

其中n為0，Y1 及Y2 均表示-CH2 -，且其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 及X具有如本說明書中所定義之意義，該方法包含使式(VIa)化合物

其中G為OH，且R4 、R4 ' 具有如本說明書中所定義之意義，與式VII化合物反應，

其中Z表示OH (在此情況下，光延型條件(Mitsunobu type condiction)適用)或諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基(在此情況下，烷基化條件適用)，A表示-NR3 R3' ，且R2 、R3 及R3 ' 具有如本說明書中所定義之意義。In a particular embodiment, there is a method for producing a compound of formula (I),

Where n is 0, Y 1 and Y 2 each represent -CH 2- , and R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and X have the meanings as defined in the present specification, The method comprises applying a compound of formula (VIa)

Wherein G is OH, and R 4 and R 4 ′ have the meanings as defined in the present specification, and react with a compound of formula VII,

Where Z represents OH (in this case, Mitsunobu type condiction applies) or such as chlorine, bromine, iodine, methanesulfonate, tosylate, nitrobenzenesulfonate, or triflate an ester of a leaving group (in this case, the alkylation conditions apply), A represents -NR 3 R 3 ', and R 2, R 3 and R 3' have the meanings as defined in the present specification.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，

其中n為1，Y1 及Y2 均表示-CH2 -，且其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 及X具有如本說明書中所定義之意義，該方法包含使式(VIb)化合物

與式VII化合物反應，

其中Z表示OH，且G表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；或者Z表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，且G表示OH，且其中R4 、R4 ' 具有如本說明書中所定義之意義，A表示-NR3 R3' ，且R2 、R3 及R3 ' 具有如本說明書中所定義之意義。In a particular embodiment, there is a method for producing a compound of formula (I),

Where n is 1, Y 1 and Y 2 each represent -CH 2- , and R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and X have the meanings as defined in the present specification, The method comprises applying a compound of formula (VIb)

Reacting with a compound of formula VII,

Where Z represents OH and G represents a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate; or Z represents such as chlorine, bromine , Iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate, and G represents OH, and R 4 and R 4 ′ have In the meaning of the definition, A represents -NR 3 R 3 ' , and R 2 , R 3 and R 3 ′ have the meanings as defined in the present specification.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，

其中-X為一鍵，且R1 表示-NR5 R5 ' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，該方法包含使式(IIa)化合物

其中Q表示氯、溴、碘或三氟甲磺酸酯，A表示-NR3 R3' ，且R2 、R3 、R3' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-2之胺反應，

其中R5 及R5 ' 具有如本說明書中所定義之意義；
或
其中-X為一鍵，且R1 表示-NR5 ' C(O)R5 ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，該方法包含使式(IIa)化合物

其中Q表示氯、溴、碘或三氟甲磺酸酯，A表示-NR3 R3' ，且R2 、R3 、R3' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-3之胺反應，

其中R5 及R5 ' 具有如本說明書中所定義之意義；
或
其中-X-R1 表示-[CH2 ]p -NR5 R5' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 及n及p具有如本說明書中所定義之意義，該方法包含使式(IIb)化合物

其中r為1、2、3或4，A表示-NR3 R3' ，且R2 、R3 、R3' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-2之胺反應，

其中R5 及R5 ' 具有如本說明書中所定義之意義；
或
其中-X-R1 表示-[CH2 ]p -NR5 R5' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 及n及p具有如本說明書中所定義之意義，該方法包含使式(IIa)化合物

其中Q表示氯、溴、碘或三氟甲磺酸酯，A表示-NR3 R3' ，且R2 、R3 、R3' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-4之有機金屬試劑反應，

其中R5 及R5 ' 及p具有如本說明書中所定義之意義，且M表示適合之有機金屬基團，較佳為硼或鋅試劑；
或
其中-X為一鍵，且R1 表示-NR5 R5 ' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 及n具有如本說明書中所定義之意義，該方法包含使式(IIc)化合物

其中A表示-NR3 R3' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-5之醛在還原性胺化下反應，
或
與式III-6之烷基化劑在常規烷基化條件下反應，

其中R5 具有如本說明書中所定義之意義，且LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或
其中-X為一鍵，且R1 表示-NR5 ' C(O)R5 ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 及n具有如本說明書中所定義之意義，該方法包含使式(Ie)化合物

其中A表示-NR3 R3' ，且R2 、R3 、R3 ' 、R4 、R4 ' 、R5 及n具有如本說明書中所定義之意義，與式III-6'之烷基化劑反應，

其中R5 ' 具有如本說明書中所定義之意義但與氫不同，且LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或
其中-X為-[CH2 ]p-，且R1 表示-C(O)NR5 R5 ' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 及n及p具有如本說明書中所定義之意義，該方法包含使式(IId)化合物

其中A表示-NR3 R3' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n及p具有如本說明書中所定義之意義，與式III-2之胺在醯胺化條件下反應，

其中R5 ' 及R5 ' 具有如本說明書中所定義之意義；
或
其中n為0，Y1 及Y2 均表示-CH2 -，且其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 及X具有如本說明書中所定義之意義，該方法包含使式(VIa)化合物

其中G為OH，且R4 、R4 ' 具有如本說明書中所定義之意義，與式VII化合物反應，

其中Z表示OH或諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，A表示-NR3 R3' ，且R2 、R3 及R3 ' 具有如本說明書中所定義之意義；
或
其中n為1，Y1 及Y2 均表示-CH2 -，且其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 及X具有如本說明書中所定義之意義，該方法包含使式(VIa)化合物

與式VII化合物反應，

其中Z表示OH，且G表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；或者Z表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，且G表示OH或諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，且其中R4 、R4 ' 具有如本說明書中所定義之意義，A表示-NR3 R3' ，且R2 、R3 及R3 ' 具有如本說明書中所定義之意義。In a particular embodiment, there is a method for producing a compound of formula (I),

Where -X is a bond, and R 1 represents -NR 5 R 5 ′ , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n Having the meaning as defined in this specification, the method comprising making a compound of formula (IIa)

Wherein Q represents chlorine, bromine, iodine or triflate, A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3' , R 4 , R 4 ' and n have Meaning of definition, reaction with amine of formula III-2,

Wherein R 5 and R 5 ′ have the meanings as defined in the present specification;
Or wherein -X is a bond, and R 1 represents -NR 5 ' C (O) R 5 , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ' , R 4 , R 4 ′ and n have the meanings as defined in the present specification, and the method comprises making a compound of formula (IIa)

Wherein Q represents chlorine, bromine, iodine or triflate, A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3' , R 4 , R 4 ' and n have Meaning of definition, reaction with amine of formula III-3,

Wherein R 5 and R 5 ′ have the meanings as defined in the present specification;
Or where -XR 1 represents-[CH 2 ] p -NR 5 R 5 ' , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ' , R 4 , R 4 ' and n and p have the meanings as defined in the present specification, and the method comprises making a compound of formula (IIb)

Where r is 1, 2, 3 or 4, and A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3' , R 4 , R 4 ' and n have the meanings as defined in the present specification, and The amine reaction of formula III-2,

Wherein R 5 and R 5 ′ have the meanings as defined in the present specification;
Or where -XR 1 represents-[CH 2 ] p -NR 5 R 5 ' , Y 1 and Y 2 both represent -CH 2- , and R 2 , R 3 , R 3 ' , R 4 , R 4 ' and n and p have the meanings as defined in the present specification, and the method comprises making a compound of formula (IIa)

Wherein Q represents chlorine, bromine, iodine or triflate, A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3' , R 4 , R 4 ' and n have Meaning of definition, reaction with organometallic reagent of formula III-4,

Wherein R 5 and R 5 ′ and p have the meanings as defined in the present specification, and M represents a suitable organometallic group, preferably a boron or zinc reagent;
Or wherein -X is a bond, and R 1 represents -NR 5 R 5 ′ , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 5 , R 5 ′ and n have the meanings as defined in the present specification, and the method comprises making a compound of formula (IIc)

Wherein A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ and n have the meanings as defined in the present specification. Chemical reaction,
Or react with an alkylating agent of formula III-6 under conventional alkylating conditions,

Wherein R 5 has the meaning as defined in the present specification, and LG represents a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate ;
Or wherein -X is a bond, and R 1 represents -NR 5 ' C (O) R 5 , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ' , R 4 , R 4 ′ , R 5 , R 5 ′ and n have the meanings as defined in the present specification, and the method comprises making a compound of formula (Ie)

Wherein A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 5 and n have the meanings as defined in the present specification, and the alkane of formula III-6 ′ Basing agent reaction,

Wherein R 5 ′ has the meaning as defined in the present specification but is different from hydrogen, and LG represents such as chlorine, bromine, iodine, methanesulfonate, tosylate, nitrobenzenesulfonate, or triflate Leaving group of ester;
Or where -X is-[CH 2 ] p-, and R 1 represents -C (O) NR 5 R 5 ' , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ', R 4, R 4' , R 5, R 5 ' and n and p have the meanings as defined in the present specification, the method comprising compound (IId) formula

Wherein A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n and p have the meanings as defined in the present specification, and are the same as those of the amine of formula III-2. Reaction under amination conditions,

Wherein R 5 ′ and R 5 ′ have the meanings as defined in the present specification;
Or where n is 0, Y 1 and Y 2 both represent -CH 2- , and R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and X have the meanings as defined in the present specification The method comprises applying a compound of formula (VIa)

Wherein G is OH, and R 4 and R 4 ′ have the meanings as defined in the present specification, and react with a compound of formula VII,

Where Z represents OH or a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate, and A represents -NR 3 R 3 ' , and R 2 , R 3 and R 3 ′ have the meanings as defined in the present specification;
Or where n is 1, Y 1 and Y 2 both represent -CH 2- , and R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and X have the meanings as defined in the present specification The method comprises applying a compound of formula (VIa)

Reacting with a compound of formula VII,

Where Z represents OH and G represents a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate; or Z represents such as chlorine, bromine , Iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate, and G represents OH or such as chlorine, bromine, iodine, mesylate, tosylate Leaving group of an acid ester, nitrobenzene sulfonate or triflate, and wherein R 4 and R 4 ′ have the meanings as defined in the present specification, A represents -NR 3 R 3 ′ , and R 2. R 3 and R 3 ′ have the meanings as defined in the present specification.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，其藉由在有機溶劑(較佳為MeOH)中使羰基衍生物與適合之還原性試劑(較佳為硼氫化鈉)進行還原反應以得到羥基化合物來進行。In a specific embodiment, there is a method for producing a compound of formula (I) by carbonyl derivative and a suitable reducing agent (preferably borohydride) in an organic solvent (preferably MeOH) Sodium) is subjected to a reduction reaction to obtain a hydroxy compound.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，其藉由在適當溶劑(諸如1,4-二噁烷、DCM、乙酸乙酯或有機溶劑及水之混合物)中，藉由任何適合之方法(諸如用酸處理，較佳用HCl或三氟乙酸處理)對含有胺保護基(諸如胺基甲酸酯，較佳為第三丁氧基羰基)之式I化合物進行保護基脫除反應來進行。In a particular embodiment, there is a method for producing a compound of formula (I) by using a suitable solvent (such as 1,4-dioxane, DCM, ethyl acetate, or a mixture of an organic solvent and water) In the formula I containing an amine protecting group (such as a carbamate, preferably a third butoxycarbonyl group) by any suitable method (such as treatment with an acid, preferably with HCl or trifluoroacetic acid) The compound is subjected to a protective group removal reaction.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，其藉由在有機溶劑(較佳為DCE)中，在有機鹼(較佳為DIPEA或TEA)存在下使含有胺基之式I化合物與醛進行還原性胺化反應來進行，較佳地用還原性試劑(較佳為三乙醯氧基硼氫化鈉)來進行。或者，反應可在酸(較佳為乙酸)存在下進行。In a specific embodiment, there is a method for producing a compound of formula (I), which is carried out in an organic solvent (preferably DCE) in the presence of an organic base (preferably DIPEA or TEA) The amine-based compound of formula I is subjected to a reductive amination reaction with an aldehyde, preferably using a reducing reagent (preferably sodium triethoxylate borohydride). Alternatively, the reaction can be performed in the presence of an acid, preferably acetic acid.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，其藉由在有機溶劑(較佳為乙腈)中，在適合之溫度(諸如介於0℃-120℃範圍內)下，在鹼(較佳為DIPEA或K2 CO3 )存在下使含有胺基之式I化合物與烷基化試劑反應來進行。In a specific embodiment, there is a method for producing a compound of formula (I) by using an organic solvent (preferably acetonitrile) at a suitable temperature (such as between 0 ° C and 120 ° C). ) In the presence of a base, preferably DIPEA or K 2 CO 3 , by reacting a compound of formula I containing an amine group with an alkylating agent.

在一個特定實施例中，存在一種用於產生式(I)之化合物的方法，其藉由在有機溶劑(較佳為2-甲氧基乙醇)中，在適合之溫度(諸如介於20℃-140℃範圍內)下使含有胺基之式I化合物與乙烯基衍生物反應來進行。In a particular embodiment, there is a method for producing a compound of formula (I) by using an organic solvent (preferably 2-methoxyethanol) at a suitable temperature (such as between 20 ° C) The reaction is carried out by reacting a compound of formula I containing an amine group with a vinyl derivative at a temperature of -140 ° C.

本發明之一個特定實施例涉及一種式(II)化合物之用途，

其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，且Y表示適合之官能基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (II),

Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, forma A leaving group of a sulfonate, tosylate, nitrobenzenesulfonate or triflate, and Y represents a suitable functional group, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(IIa)化合物之用途，

其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，Q表示氯、溴、碘或三氟甲磺酸酯，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (IIa),

Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n have the meanings as defined in the present specification, and Q represents chlorine, bromine, iodine, or trifluoro Mesylate, LG means a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate or triflate, which is used to prepare formula (I) Compound.

本發明之一個特定實施例涉及一種式(IIb)化合物之用途，

其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n及r具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (IIb),

Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n and r have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine , A leaving group of mesylate, tosylate, nitrobenzenesulfonate or trifluoromethanesulfonate, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(IIc)化合物之用途，

其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (IIc),

Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, forma Leaving group of a sulfonate, tosylate, nitrobenzenesulfonate, or triflate, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(IId)化合物之用途，

其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n及p具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (IId),

Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n and p have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine , A leaving group of mesylate, tosylate, nitrobenzenesulfonate or trifluoromethanesulfonate, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(III)化合物之用途，

其中R1 具有如本說明書中所定義之意義，且W表示適合之官能基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (III),

Wherein R 1 has the meaning as defined in the present specification, and W represents a suitable functional group, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(III-2)化合物之用途，

其中R5 及R5 '具有如本說明書中所定義之意義，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (III-2),

Wherein R 5 and R 5 ′ have the meanings as defined in the present specification and are used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(III-3)化合物之用途，

其中R5 及R5 '具有如本說明書中所定義之意義，其用於製備式(I)化合物。A specific embodiment of the present invention relates to the use of a compound of formula (III-3),

Wherein R 5 and R 5 ′ have the meanings as defined in the present specification and are used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(III-4)化合物之用途，

其中p、R5 及R5 '具有如本說明書中所定義之意義，且M表示適合之有機金屬基團，較佳為硼或鋅試劑，其用於製備式(I)化合物。A specific embodiment of the present invention relates to the use of a compound of formula (III-4),

Wherein p, R 5 and R 5 ′ have the meanings as defined in the present specification, and M represents a suitable organometallic group, preferably a boron or zinc reagent, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(III-5)化合物之用途，

其中R5 具有如本說明書中所定義之意義，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (III-5),

Wherein R 5 has the meaning as defined in the present specification and is used for preparing a compound of formula (I).

本發明之一個特定實施例涉及一種式(III-6)化合物之用途，

其中R5 具有如本說明書中所定義之意義，且LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the present invention relates to the use of a compound of formula (III-6),

Wherein R 5 has the meaning as defined in the present specification, and LG represents a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate , Which is used to prepare compounds of formula (I).

本發明之一個特定實施例涉及一種式(III-6')化合物之用途，

其中R5 ' 具有如本說明書中所定義之意義，且LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the present invention relates to the use of a compound of formula (III-6 '),

Where R 5 ′ has the meaning as defined in the present specification, and LG represents the departure of such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate Group for the preparation of compounds of formula (I).

本發明之一個特定實施例涉及一種式(IVb)化合物之用途，

IVb，其中A=LG
其中A為LG，R2 、R4 、R4 ' 、R5 、R5 '及n具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (IVb),

IVb, where A = LG
Where A is LG, and R 2 , R 4 , R 4 ′ , R 5 , R 5 ′, and n have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, toluenesulfonic acid A leaving group of an ester, nitrobenzenesulfonate or triflate, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(IVc)化合物之用途，

其中A為LG，R2 、R4 、R4 ' 、R5 、R5 '及n具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (IVc),

Where A is LG, and R 2 , R 4 , R 4 ′ , R 5 , R 5 ′, and n have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, toluenesulfonic acid A leaving group of an ester, nitrobenzenesulfonate or triflate, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(IVd)化合物之用途，

IVd，其中A=LG
其中A為LG，R2 、R4 、R4 ' 、R5 、R5 '及n及p具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (IVd),

IVd, where A = LG
Where A is LG, R 2 , R 4 , R 4 ′ , R 5 , R 5 ′, and n and p have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, toluene Leaving group of a sulfonate, nitrobenzenesulfonate or triflate, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(IVe)化合物之用途，

IVe，其中A=LG
其中A為LG，R2 、R4 、R4 ' 、R5 及n具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (IVe),

IVe, where A = LG
Where A is LG, and R 2 , R 4 , R 4 ′ , R 5 and n have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, tosylate, nitro Leaving group of besylate or triflate, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(IVf)化合物之用途，

IVf，其中A=LG
其中A為LG，R2 、R4 、R4 ' 、R5 、R5 '及n及p具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (IVf),

IVf, where A = LG
Where A is LG, R 2 , R 4 , R 4 ′ , R 5 , R 5 ′, and n and p have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, toluene Leaving group of a sulfonate, nitrobenzenesulfonate or triflate, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(IVg)化合物之用途，

IVg，其中A=LG
其中A為LG，R1 、R2 、R4 及R4 ' 具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (IVg),

IVg, where A = LG
Where A is LG, and R 1 , R 2 , R 4 and R 4 ′ have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate A leaving group of an acid ester or triflate, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(IVh)化合物之用途，

IVh，其中A=LG
其中A為LG，R1 、R2 、R4 及R4 ' 具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (IVh),

IVh, where A = LG
Where A is LG, and R 1 , R 2 , R 4 and R 4 ′ have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate A leaving group of an acid ester or triflate, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(V)化合物之用途，

其中R3 及R3 ' 具有如本說明書中所定義之意義，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (V),

Wherein R 3 and R 3 ′ have the meanings as defined in the present specification and are used to prepare a compound of formula (I).

在一個特定實施例中，存在一種式(VI)化合物之用途，

其中G表示OH、鹵素或離去基，R1 、R4 及R4 ' 及n具有如本說明書中所定義之意義，其用於製備式(I)化合物。In a specific embodiment, there is a use of a compound of formula (VI),

Wherein G represents OH, halogen or a leaving group, R 1 , R 4 and R 4 ′ and n have the meanings as defined in the present specification, and are used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(VIa)化合物之用途，

其中G表示OH、鹵素或離去基，R1 、R4 及R4 ' 具有如本說明書中所定義之意義，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (VIa),

Wherein G represents OH, halogen or a leaving group, and R 1 , R 4 and R 4 ′ have the meanings as defined in the present specification, and are used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(VIb)化合物之用途，

其中G表示OH、鹵素或離去基，R1 、R4 及R4 ' 具有如本說明書中所定義之意義，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (VIb),

Wherein G represents OH, halogen or a leaving group, and R 1 , R 4 and R 4 ′ have the meanings as defined in the present specification, and are used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(VII)化合物之用途，

其中Z表示OH或離去基，A為LG或NR3 R3 ' ，R2 、R3 及R3 ' 具有如本說明書中所定義之意義，且LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (VII),

Where Z represents OH or a leaving group, A is LG or NR 3 R 3 ′ , R 2 , R 3 and R 3 ′ have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, methanesulfonate A leaving group of an acid ester, tosylate, nitrobenzenesulfonate, or triflate, which is used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(VIII)化合物之用途，

Y表示適合之官能基，G表示OH、鹵素或離去基，R4 及R4 ' 及n具有如本說明書中所定義之意義，其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (VIII),

Y represents a suitable functional group, G represents OH, halogen, or a leaving group, and R 4 and R 4 ′ and n have the meanings as defined in the present specification, and are used to prepare a compound of formula (I).

本發明之一個特定實施例涉及一種式(II)化合物之用途，

其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基，且Y表示適合之官能基；
或一種式(IIa)化合物之用途，

其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，Q表示氯、溴、碘或三氟甲磺酸酯，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(IIb)化合物之用途，

其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n及r具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(IIc)化合物之用途，

其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(IId)化合物之用途，

其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n及p具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(III)化合物之用途，

其中R1 具有如本說明書中所定義之意義，且W表示適合之官能基；
或一種式(III-2)化合物之用途，

其中R5 及R5 '具有如本說明書中所定義之意義；
或一種式(III-3)化合物之用途，

其中R5 及R5 '具有如本說明書中所定義之意義；
或一種式(III-4)化合物之用途，

其中p、R5 及R5 '具有如本說明書中所定義之意義，且M表示適合之有機金屬基團，較佳為硼或鋅試劑；
或一種式(III-5)化合物之用途，

其中R5 具有如本說明書中所定義之意義；
或一種式(III-6)化合物之用途，

其中R5 具有如本說明書中所定義之意義，且LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(III-6')化合物之用途，

其中R5 ' 具有如本說明書中所定義之意義，且LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(IVb)化合物之用途，

IVb，其中A=LG
其中A為LG，R2 、R4 、R4 ' 、R5 、R5 '及n具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(IVc)化合物之用途，

其中A為LG，R2 、R4 、R4 ' 、R5 、R5 '及n具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(IVd)化合物之用途，

IVd，其中A=LG
其中A為LG，R2 、R4 、R4 ' 、R5 、R5 '及n及p具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(IVe)化合物之用途，

IVe，其中A=LG
其中A為LG，R2 、R4 、R4 ' 、R5 及n具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(IVf)化合物之用途，

IVf，其中A=LG
其中A為LG，R2 、R4 、R4 ' 、R5 、R5 '及n及p具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(IVg)化合物之用途，

IVg，其中A=LG
其中A為LG，R1 、R2 、R4 及R4 ' 具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(IVh)化合物之用途，

IVh，其中A=LG
其中A為LG，R1 、R2 、R4 及R4 ' 具有如本說明書中所定義之意義，LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(V)化合物之用途，

其中R3 及R3 ' 具有如本說明書中所定義之意義；
或一種式(VI)化合物之用途，

其中G表示OH、鹵素或離去基，R1 、R4 及R4 ' 及n具有如本說明書中所定義之意義；
或一種式(VIa)化合物之用途，

其中G表示OH、鹵素或離去基，R1 、R4 及R4 ' 具有如本說明書中所定義之意義；
或一種式(VIb)化合物之用途，

其中G表示OH、鹵素或離去基，R1 、R4 及R4 ' 具有如本說明書中所定義之意義；
或一種式(VII)化合物之用途，

其中Z表示OH或離去基，A為LG或NR3 R3 ' ，R2 、R3 及R3 ' 具有如本說明書中所定義之意義，且LG表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基；
或一種式(VIII)化合物之用途，

Y表示適合之官能基，G表示OH、鹵素或離去基，R4 及R4 ' 及n具有如本說明書中所定義之意義，
其用於製備式(I)化合物。A specific embodiment of the invention relates to the use of a compound of formula (II),

Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, forma Leaving group of sulfonate, tosylate, nitrobenzenesulfonate or triflate, and Y represents a suitable functional group;
Or the use of a compound of formula (IIa),

Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n have the meanings as defined in the present specification, and Q represents chlorine, bromine, iodine, or trifluoro Mesylate, LG means a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate or triflate;
Or the use of a compound of formula (IIb),

Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n and r have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine The leaving group of mesylate, tosylate, nitrobenzenesulfonate or triflate;
Or the use of a compound of formula (IIc),

Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, forma Leaving group of sulfonate, tosylate, nitrobenzenesulfonate or triflate;
Or the use of a compound of formula (IId),

Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n and p have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine The leaving group of mesylate, tosylate, nitrobenzenesulfonate or triflate;
Or the use of a compound of formula (III),

Wherein R 1 has the meaning as defined in the present specification, and W represents a suitable functional group;
Or the use of a compound of formula (III-2),

Wherein R 5 and R 5 ′ have the meanings as defined in the present specification;
Or the use of a compound of formula (III-3),

Wherein R 5 and R 5 ′ have the meanings as defined in the present specification;
Or the use of a compound of formula (III-4),

Wherein p, R 5 and R 5 ′ have the meanings as defined in the present specification, and M represents a suitable organometallic group, preferably a boron or zinc reagent;
Or the use of a compound of formula (III-5),

Wherein R 5 has the meaning as defined in the present specification;
Or the use of a compound of formula (III-6),

Wherein R 5 has the meaning as defined in the present specification, and LG represents a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate ;
Or the use of a compound of formula (III-6 '),

Where R 5 ′ has the meaning as defined in the present specification, and LG represents the departure of such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate base;
Or the use of a compound of formula (IVb),

IVb, where A = LG
Where A is LG, and R 2 , R 4 , R 4 ′ , R 5 , R 5 ′, and n have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, toluenesulfonic acid Leaving group of ester, nitrobenzenesulfonate or triflate;
Or the use of a compound of formula (IVc),

Where A is LG, and R 2 , R 4 , R 4 ′ , R 5 , R 5 ′, and n have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, toluenesulfonic acid Leaving group of ester, nitrobenzenesulfonate or triflate;
Or the use of a compound of formula (IVd),

IVd, where A = LG
Where A is LG, R 2 , R 4 , R 4 ′ , R 5 , R 5 ′, and n and p have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, toluene Leaving group of sulfonate, nitrobenzenesulfonate or triflate;
Or the use of a compound of formula (IVe),

IVe, where A = LG
Where A is LG, and R 2 , R 4 , R 4 ′ , R 5 and n have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, tosylate, nitro Leaving group of besylate or triflate;
Or the use of a compound of formula (IVf),

IVf, where A = LG
Where A is LG, R 2 , R 4 , R 4 ′ , R 5 , R 5 ′, and n and p have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, toluene Leaving group of sulfonate, nitrobenzenesulfonate or triflate;
Or the use of a compound of formula (IVg),

IVg, where A = LG
Where A is LG, and R 1 , R 2 , R 4 and R 4 ′ have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfon Leaving group of an acid ester or triflate;
Or the use of a compound of formula (IVh),

IVh, where A = LG
Where A is LG, and R 1 , R 2 , R 4 and R 4 ′ have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate Leaving group of an acid ester or triflate;
Or the use of a compound of formula (V),

Wherein R 3 and R 3 ′ have the meanings as defined in the present specification;
Or the use of a compound of formula (VI),

Where G represents OH, halogen or leaving group, and R 1 , R 4 and R 4 ′ and n have the meanings as defined in the present specification;
Or the use of a compound of formula (VIa),

Where G represents OH, halogen, or leaving group, and R 1 , R 4 and R 4 ′ have the meanings as defined in the present specification;
Or the use of a compound of formula (VIb),

Where G represents OH, halogen, or leaving group, and R 1 , R 4 and R 4 ′ have the meanings as defined in the present specification;
Or the use of a compound of formula (VII),

Where Z represents OH or a leaving group, A is LG or NR 3 R 3 ′ , R 2 , R 3 and R 3 ′ have the meanings as defined in the present specification, and LG represents such as chlorine, bromine, iodine, methanesulfon Leaving groups of acid esters, tosylate, nitrobenzenesulfonate or triflate;
Or the use of a compound of formula (VIII),

Y represents a suitable functional group, G represents OH, halogen or a leaving group, R 4 and R 4 ′ and n have the meanings as defined in the present specification,
It is used to prepare compounds of formula (I).

必要時，所獲得之反應產物可藉由諸如結晶及層析之習知方法來進行純化。在上文所描述的用於製備本發明化合物之方法產生立體異構體混合物的情況下，此等異構體可藉由諸如製備型層析之習知技術來進行分離。若存在對掌性中心，則化合物可以外消旋形式來加以製備，或個別對映異構體可藉由對映選擇性合成或藉由解析來加以製備。If necessary, the obtained reaction product can be purified by conventional methods such as crystallization and chromatography. Where the methods described above for preparing the compounds of the present invention produce a mixture of stereoisomers, these isomers can be separated by conventional techniques such as preparative chromatography. If there is an anomeric center, the compound can be prepared in racemic form, or individual enantiomers can be prepared by enantioselective synthesis or by resolution.

本發明化合物的一種較佳醫藥學上可接受之形式為結晶形式，包括醫藥組合物中之此類形式。在本發明化合物之鹽以及溶劑合物的情況下，額外離子及溶劑部分必須亦無毒性。本發明化合物可存在不同多晶型形式，意欲本發明涵蓋全部此類形式。A preferred pharmaceutically acceptable form of a compound of the invention is a crystalline form, including such forms in pharmaceutical compositions. In the case of the salts and solvates of the compounds of the invention, the additional ionic and solvent moieties must also be non-toxic. The compounds of the invention may exist in different polymorphic forms, and it is intended that the invention encompass all such forms.

本發明之另一態樣涉及一種醫藥組合物，其包含如上文根據通式I所描述之本發明化合物或其醫藥學上可接受之鹽或立體異構體，及醫藥學上可接受之載劑、佐劑或媒劑。本發明因此提供包含本發明化合物或其醫藥學上可接受之鹽或立體異構體與醫藥學上可接受之載劑、佐劑或媒劑一起的醫藥組合物，其用於向患者投與。Another aspect of the present invention relates to a pharmaceutical composition comprising a compound of the present invention or a pharmaceutically acceptable salt or stereoisomer thereof as described above according to Formula I, and a pharmaceutically acceptable compound Agent, adjuvant or vehicle. The invention therefore provides a pharmaceutical composition comprising a compound of the invention or a pharmaceutically acceptable salt or stereoisomer thereof together with a pharmaceutically acceptable carrier, adjuvant or vehicle for administration to a patient .

醫藥組合物之實例包括用於經口、局部或非經腸投藥之任何固體(錠劑、丸劑、膠囊、顆粒等)或液體(溶液、懸浮液或乳液)組合物。Examples of pharmaceutical compositions include any solid (tablet, pill, capsule, granule, etc.) or liquid (solution, suspension or emulsion) composition for oral, topical or parenteral administration.

在一個較佳實施例中，醫藥組合物呈口服形式，亦即固體或液體。用於經口投藥之適合劑型可為錠劑、囊劑、糖漿或溶液，且可含有此項技術中已知之習知賦形劑，諸如結合劑，例如糖漿、阿拉伯膠、明膠、山梨糖醇、黃蓍或聚乙烯吡咯啶酮；填充劑，例如乳糖、糖、玉米澱粉、磷酸鈣、山梨糖醇或甘胺酸；製錠潤滑劑，例如硬脂酸鎂；崩解劑，例如澱粉、聚乙烯吡咯啶酮、乙醇酸澱粉鈉或微晶纖維素；或醫藥學上可接受之濕潤劑，諸如月桂基硫酸鈉。In a preferred embodiment, the pharmaceutical composition is in an oral form, that is, a solid or liquid. Suitable dosage forms for oral administration may be lozenges, sachets, syrups or solutions, and may contain conventional excipients known in the art, such as binding agents such as syrup, acacia, gelatin, sorbitol, yellow Tincture or polyvinylpyrrolidone; fillers such as lactose, sugar, corn starch, calcium phosphate, sorbitol or glycine; tablet lubricants such as magnesium stearate; disintegrating agents such as starch, polyethylene Pyrrolidone, sodium starch glycolate, or microcrystalline cellulose; or a pharmaceutically acceptable wetting agent, such as sodium lauryl sulfate.

固體口服組合物可藉由摻合、填充或製錠之習知方法來加以製備。重複摻合操作可用於使活性劑分佈在採用大量填充劑之整個彼等組合物中。此類操作為此項技術中習知的。錠劑可例如藉由濕式或乾式造粒來加以製備，且視情況根據正規醫藥實踐中熟知之方法來進行包覆，尤其用腸溶包衣進行包覆。Solid oral compositions can be prepared by conventional methods of blending, filling or tabletting. Repeated blending operations can be used to distribute the active agents throughout their compositions using large amounts of fillers. Such operations are known in the art. Lozenges can be prepared, for example, by wet or dry granulation and, if appropriate, coated according to methods well known in normal pharmaceutical practice, especially with enteric coatings.

醫藥組合物亦可經調適以用於非經腸投藥，諸如呈適當單位劑型之無菌溶液、懸浮液或凍乾產品。可使用恰當之賦形劑，諸如增積劑、緩衝劑或界面活性劑。Pharmaceutical compositions may also be adapted for parenteral administration, such as sterile solutions, suspensions or lyophilized products in appropriate unit dosage forms. Appropriate excipients can be used, such as builders, buffers or surfactants.

所提及之調配物將使用標準方法來加以製備，諸如西班牙及美國藥典及類似參考文獻正文中所描述或提及之彼等標準方法。The formulations mentioned will be prepared using standard methods, such as those described or referred to in the body of the Spanish and US Pharmacopoeia and similar references.

本發明之化合物或組合物的投藥可藉由任何適合之方法來進行，諸如靜脈內輸注、口服製劑及腹膜內及靜脈內投藥。經口投藥因為對患者之便利性及待治療疾病之慢性特徵而為較佳的。Administration of a compound or composition of the present invention can be performed by any suitable method, such as intravenous infusion, oral preparations, and intraperitoneal and intravenous administration. Oral administration is preferred because of the convenience to the patient and the chronic characteristics of the disease to be treated.

一般而言，本發明化合物之有效投與量將視所選化合物之相對功效、所治療病症之嚴重程度及患病者之體重而定。然而，活性化合物將通常一天投與一或多次，例如每天1、2、3或4次，而典型總日劑量在每天0.1至1000 mg/kg範圍內。In general, the effective dosage of a compound of the present invention will depend on the relative efficacy of the selected compound, the severity of the condition being treated, and the weight of the patient. However, the active compound will usually be administered one or more times a day, for example 1, 2, 3 or 4 times a day, while a typical total daily dose will be in the range of 0.1 to 1000 mg / kg per day.

本發明之化合物及組合物可與其他藥物一起使用以提供組合療法。其他藥物可形成同一組合物之一部分，或以同時或不同時間投與之另一單獨組合物的形式進行提供。The compounds and compositions of the invention can be used with other drugs to provide combination therapies. Other drugs may form part of the same composition or be provided in the form of another separate composition administered simultaneously or at different times.

本發明之另一態樣涉及本發明化合物或其醫藥學上可接受之鹽或異構體在藥劑製造中的用途。Another aspect of the invention relates to the use of a compound of the invention or a pharmaceutically acceptable salt or isomer thereof in the manufacture of a medicament.

本發明之另一態樣涉及如上文根據通式I所描述之本發明化合物或其醫藥學上可接受之鹽或異構體，其用作用於治療疼痛之藥劑。較佳地，疼痛為中度至重度疼痛、內臟疼痛、慢性疼痛、癌症疼痛、偏頭痛、發炎性疼痛、急性疼痛或神經病性疼痛、觸摸痛或痛覺過敏。此可包括機械性觸摸痛或熱痛覺過敏。Another aspect of the invention relates to a compound of the invention, or a pharmaceutically acceptable salt or isomer thereof, as described above according to Formula I, for use as a medicament for the treatment of pain. Preferably, the pain is moderate to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute or neuropathic pain, touch pain or hyperalgesia. This may include mechanical touch or thermal hyperalgesia.

本發明之另一態樣涉及本發明化合物在製造用於治療或預防疼痛之藥劑中的用途。Another aspect of the invention relates to the use of a compound of the invention in the manufacture of a medicament for the treatment or prevention of pain.

在一個較佳實施例中，疼痛係選自中度至重度疼痛、內臟疼痛、慢性疼痛、癌症疼痛、偏頭痛、發炎性疼痛、急性疼痛或神經病性疼痛、觸摸痛或痛覺過敏，亦較佳包括機械性觸摸痛或熱痛覺過敏。In a preferred embodiment, the pain is selected from moderate to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute pain or neuropathic pain, touch pain or hyperalgesia, and more preferably Including mechanical touch or thermal hyperalgesia.

本發明之另一態樣涉及一種治療或預防疼痛之方法，該方法包含向需要此類治療之患者投與治療有效量的如上文所定義之化合物或其藥物組合物。在可治療之疼痛症候群當中為中度至重度疼痛、內臟疼痛、慢性疼痛、癌症疼痛、偏頭痛、發炎性疼痛、急性疼痛或神經病性疼痛、觸摸痛或痛覺過敏，然而，此亦可包括機械性觸摸痛或熱痛覺過敏。Another aspect of the invention relates to a method of treating or preventing pain, the method comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound or a pharmaceutical composition thereof as defined above. Among the treatable pain syndromes are moderate to severe pain, visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute or neuropathic pain, touch pain or hyperalgesia, however, this can also include mechanical Sexual touch or thermal hyperalgesia.

本發明在下文藉助於實例加以說明。此等說明僅僅藉由實例給出，而不限制本發明之一般精神。The invention is explained below by means of examples. These descriptions are given by way of example only, and do not limit the general spirit of the invention.

通用實驗部分 ( 合成及分析之方法及設備
合成描述
已開發出兩種不同通用方法用於獲得本發明化合物，如下文方法A及B中所描述且進一步詳述於流程1至7中。 General experimental part ( synthesis and analysis methods and equipment
Synthetic descriptions <br/> Two different general methods have been developed for obtaining the compounds of the present invention, as described below in Methods A and B and further detailed in Schemes 1 to 7.

方法 A
描述用於自式II化合物開始製備通式(I)化合物之一步法，如以下流程中所示：

HNR3 R3 ' V
方法A
其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 、X及n具有如技術方案1中所定義之意義，LG表示離去基，且Y及W表示適合之官能基，以執行下文在流程1至4中詳述之此類轉換。 Method A
A one-step process for preparing compounds of general formula (I) starting from compounds of formula II is described, as shown in the following scheme:

HNR 3 R 3 ' V
Method A
Wherein R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , X and n have the meanings as defined in the technical scheme 1, LG represents a leaving group, and Y and W represent suitable functional groups To perform such conversions detailed below in Processes 1 to 4.

另外，存在於式(I)化合物中之胺基NR3 R3 ' 可稍後在合成中併入，該合成藉由如上文流程中所示，使式IV化合物(其中LG表示離去基(諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯))與式V之胺反應來進行，得到式I化合物。烷基化反應在適合之溶劑(諸如乙醇、二甲基甲醯胺、二甲亞碸或乙腈，較佳為乙醇)中；使用過量之胺V，或視情況在鹼(諸如K2 CO3 、N,N -二異丙基乙胺或三乙胺)存在下；在包含於室溫與回流溫度之間的適合之溫度下(較佳在加熱的情況下)進行，或者，該反應可在微波反應器中進行。另外，可使用活化劑，諸如碘化鈉或碘化鉀。此類轉換亦可自式II-LG化合物開始執行以製備式II化合物。In addition, the amine group NR 3 R 3 ′ present in the compound of the formula (I) can be incorporated later in the synthesis by making the compound of the formula IV (wherein LG represents a leaving group ( Such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate or trifluoromethanesulfonate)) with an amine of formula V to obtain a compound of formula I. The alkylation reaction is in a suitable solvent (such as ethanol, dimethylformamide, dimethylmethylene or acetonitrile, preferably ethanol); an excess of amine V is used, or optionally a base (such as K 2 CO 3 , N, N -diisopropylethylamine or triethylamine); at a suitable temperature (preferably under heating) comprised between room temperature and reflux temperature, or the reaction may be Performed in a microwave reactor. In addition, activators such as sodium iodide or potassium iodide can be used. Such conversions can also be performed starting from compounds of Formula II-LG to prepare compounds of Formula II.

流程 1
根據方法A的用於自式IIa或IIa-LG化合物開始製備式(I)化合物(其中X表示一鍵)之通用合成途徑呈現於流程1中，得到式Ia、Ib及Ic化合物：

其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 及n具有如技術方案1中所定義之意義，Q表示氯、溴、碘或三氟甲磺酸酯，LG表示離去基(諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯)。 Flow 1
The general synthetic route for the preparation of a compound of formula (I) (where X represents a bond) according to method A, starting from a compound of formula IIa or IIa-LG, is presented in Scheme 1, to obtain compounds of formula Ia, Ib and Ic:

Wherein R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 5 , R 5 ′, and n have the meanings as defined in the technical scheme 1, and Q represents chlorine, bromine, iodine, or trifluoromethanesulfonic acid. Ester, LG means a leaving group (such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate).

隨後，自式IIa化合物製備式Ib化合物係藉由在標準布赫瓦爾德-哈特維希條件(Buchwald-Hartwig condition)下，使用Pd催化劑(諸如參(二苯亞甲基丙酮)二鈀(0)或乙酸鈀)及適合之配位體(較佳為膦配位體，諸如BINAP或XPhos)，使用適合之鹼(諸如第三丁醇鈉或碳酸銫)，在適合之溶劑(諸如甲苯或1,4-二噁烷)中，在適合之溫度下(較佳在加熱的情況下)用式III-2之胺處理式IIa化合物來進行。或者，反應可在烏爾曼芳基化條件(Ullmann arylation condition)下，使用Cu催化劑(諸如碘化銅)及適合之配位體(較佳為胺基配位體，諸如N 1 ,N 2 -二甲基乙烷-1,2-二胺)，在適合之鹼(諸如磷酸鉀)存在下，在適合之溶劑(諸如1,4-二噁烷或二甲基甲醯胺)中，在適合之溫度下(較佳在加熱的情況下)進行。Subsequently, a compound of formula Ib is prepared from a compound of formula IIa by using a Pd catalyst (such as ginsyl (diphenylmethyleneacetone) dipalladium ( 0) or palladium acetate) and a suitable ligand (preferably a phosphine ligand such as BINAP or XPhos), using a suitable base (such as sodium tert-butoxide or cesium carbonate) in a suitable solvent (such as toluene Or 1,4-dioxane) by treating the compound of formula IIa with an amine of formula III-2 at a suitable temperature (preferably under heating). Alternatively, the reaction can be performed under Ullmann arylation conditions using a Cu catalyst (such as copper iodide) and a suitable ligand (preferably an amine ligand, such as N 1 , N 2 -Dimethylethane-1,2-diamine), in the presence of a suitable base such as potassium phosphate, in a suitable solvent such as 1,4-dioxane or dimethylformamide, It is carried out at a suitable temperature, preferably under heating.

最後，自式IIa化合物製備式Ic化合物係藉由在與上文對式Ib化合物之製備所描述相同的烏爾曼芳基化條件下，用式III-3之醯胺處理式IIa化合物來進行。Finally, the preparation of the compound of formula Ic from the compound of formula IIa is carried out by treating the compound of formula IIa with amidine of formula III-3 under the same Ullman arylation conditions as described above for the preparation of compound of formula Ib. .

或者，存在於式Ib、Ic或IIa化合物中之胺基NR3 R3 ' 可稍後在合成中併入，該合成藉由遵循上文在方法A中所描述之條件，使式IVb、IVc或IIa-LG之前驅化合物分別與式V之胺反應來進行。Alternatively, the amine group NR 3 R 3 ′ present in the compound of formula Ib, Ic or IIa may be incorporated later in the synthesis, which makes the formula IVb, IVc by following the conditions described in Method A above Or the IIa-LG precursor compound is reacted with an amine of formula V, respectively.

流程 2
根據方法A的用於自式IIb或IIb-LG化合物開始製備式(I)化合物(其中-X-R1 表示-[CH2 ]p -NR5 R5' )之通用合成途徑呈現於流程2中，得到式Id化合物：

其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 、n及p具有如技術方案1中所定義之意義，LG表示離去基(諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯)，Q表示氯、溴、碘或三氟甲磺酸酯，M表示適合之有機金屬基團(較佳為硼或鋅試劑)，且r表示0至4。 Process 2
The general synthetic route for preparing compounds of formula (I) starting from compounds of formula IIb or IIb-LG (where -XR 1 represents-[CH 2 ] p -NR 5 R 5 ' ) according to method A is presented in Scheme 2, The compound of formula Id is obtained:

Wherein R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 5 , R 5 ′ , n and p have the meanings as defined in the technical scheme 1, LG represents a leaving group (such as chlorine, bromine, Iodine, methanesulfonate, tosylate, nitrobenzenesulfonate or triflate), Q for chlorine, bromine, iodine or triflate, M for suitable organometallic groups (Preferably a boron or zinc reagent), and r represents 0 to 4.

自式IIb之醛化合物製備式Id化合物可藉由在標準還原性胺化條件下用式III-2之胺處理式IIb化合物來進行。反應在還原性試劑(諸如三乙醯氧基硼氫化鈉、硼氫化鈉或氰基硼氫化鈉)存在下，在適合之溶劑(較佳為四氫呋喃、二氯乙烷或甲醇)中，視情況在酸(較佳為乙酸)存在下進行。Preparation of a compound of formula Id from an aldehyde compound of formula IIb can be performed by treating a compound of formula IIb with an amine of formula III-2 under standard reductive amination conditions. The reaction is in the presence of a reducing agent (such as sodium triacetoxyborohydride, sodium borohydride or sodium cyanoborohydride) in a suitable solvent (preferably tetrahydrofuran, dichloroethane or methanol), as appropriate This is done in the presence of an acid, preferably acetic acid.

或者，式Id化合物可藉由在偶合條件下使式IIa化合物與式III-4之有機金屬試劑(較佳為硼或鋅試劑)反應來加以製備。偶合反應在文獻中所描述之習知偶合程序下，使用適合之催化劑(較佳為Pd催化劑)及適合之配位體(較佳為膦配位體，諸如肆(三苯基膦)鈀(0))來進行。Alternatively, a compound of formula Id can be prepared by reacting a compound of formula IIa with an organometallic reagent (preferably a boron or zinc reagent) of formula III-4 under coupling conditions. Coupling reaction Under the conventional coupling procedures described in the literature, a suitable catalyst (preferably a Pd catalyst) and a suitable ligand (preferably a phosphine ligand, such as tris (triphenylphosphine) palladium ( 0)).

另外，存在於式Id、IIa或IIb化合物中之胺基NR3 R3 ' 可稍後在合成中併入，該合成藉由遵循上文在方法A中所描述之條件，使式IVd、IIa-LG或IIb-LG之前驅化合物分別與式V之胺反應來進行。In addition, the amine group NR 3 R 3 ′ present in the compound of the formula Id, IIa or IIb may be incorporated later in the synthesis, which makes the formula IVd, IIa by following the conditions described in Method A above. -LG or IIb-LG precursors are reacted with the amine of formula V, respectively.

流程 3
根據方法A的用於自式IIc或IIc-LG之胺基化合物開始製備式Ib及Ic化合物之替代性合成途徑呈現於流程3中：

其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 及n具有如技術方案1中所定義之意義，LG表示離去基(諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯)，且Z表示OH或鹵素(較佳為溴或氯)。 Process 3
An alternative synthetic route for preparing compounds of formulae Ib and Ic starting from an amine compound of formula IIc or IIc-LG according to Method A is presented in Scheme 3:

Wherein R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 5 , R 5 ′, and n have the meanings as defined in the technical scheme 1, and LG represents a leaving group (such as chlorine, bromine, iodine, Mesylate, tosylate, nitrobenzenesulfonate or triflate), and Z represents OH or halogen (preferably bromine or chlorine).

自式IIc之胺基化合物製備式Ib化合物可藉由在上文於流程2中所描述之還原性胺化條件下用式III-5之醛處理式IIc化合物或者藉由在諸如方法A中所描述之習知烷基化條件下用式III-6之烷基化劑處理式IIc化合物來進行。Compounds of formula Ib can be prepared from amine compounds of formula IIc by treating compounds of formula IIc with an aldehyde of formula III-5 under reductive amination conditions described above in Scheme 2 or by using methods such as those described in method A Conventional described alkylation conditions are used to treat a compound of formula IIc with an alkylating agent of formula III-6.

或者，其中R5 ' 為H之式Ic化合物(式Ie化合物)可藉由在式II化合物與式III-7之醯化劑之間進行醯胺化反應來加以製備。當Z為OH時，式III-7化合物為羧酸，且反應使用適合之偶合試劑(諸如N -(3-二甲基胺基丙基)-N ′-乙基碳化二亞胺(EDC)、二環己基碳化二亞胺(DCC)、N -[(二甲基胺基)-1H -1,2,3-三唑并-[4,5-b ]吡啶-1-基亞甲基]-N -甲基甲銨六氟磷酸鹽N -氧化物(HATU)或N ,N ,N ′,N ′-四甲基-O -(1H- 苯并三唑-1-基)六氟磷酸鹽(HBTU))，視情況在1-羥基苯并三唑存在下，視情況在有機鹼(諸如N -甲基嗎啉或N,N -二異丙基乙胺)存在下，在適合之溶劑(諸如二氯甲烷或二甲基甲醯胺)中，且在適合之溫度下(較佳在室溫下)進行。當Z為鹵素時，式III-7化合物為醯基鹵化物，且反應在適合之溶劑(諸如二氯甲烷、四氫呋喃、乙酸乙酯或乙酸乙酯-水混合物)中；在有機鹼(諸如三乙胺或N,N -二異丙基乙胺)一種無機鹼(諸如K2 CO3 )存在下；且在適合之溫度(較佳包含於0℃與室溫之間)下進行。另外，可使用活化劑，諸如4-二甲基胺基吡啶。Alternatively, a compound of formula Ic (compound of formula Ie) in which R 5 ′ is H can be prepared by performing an amination reaction between a compound of formula II and a halogenating agent of formula III-7. When Z is OH, III-7 as a carboxylic acid compound of the formula, and the reaction using a suitable coupling reagent (such as N - (3- dimethylaminopropyl) - N '- ethylcarbodiimide (EDC) , Dicyclohexylcarbodiimide (DCC), N -[(dimethylamino) -1 H -1,2,3-triazolo- [4,5- b ] pyridin-1-ylmethylene Group] -N -methylmethylammonium hexafluorophosphate N -oxide (HATU) or N , N , N ′, N′ -tetramethyl- O- ( 1H -benzotriazol-1-yl) Hexafluorophosphate (HBTU)), optionally in the presence of 1-hydroxybenzotriazole, and optionally an organic base such as N -methylmorpholine or N, N -diisopropylethylamine, This is carried out in a suitable solvent, such as dichloromethane or dimethylformamide, and at a suitable temperature, preferably at room temperature. When Z is a halogen, the compound of formula III-7 is a fluorenyl halide and is reacted in a suitable solvent such as dichloromethane, tetrahydrofuran, ethyl acetate or an ethyl acetate-water mixture; Ethylamine or N, N -diisopropylethylamine) in the presence of an inorganic base (such as K 2 CO 3 ); and at a suitable temperature, preferably between 0 ° C and room temperature. In addition, an activator such as 4-dimethylaminopyridine can be used.

最後，或者，式Ic化合物可藉由使式Ie化合物與式III-6'之烷基化劑反應來加以製備。此烷基化反應在非質子溶劑(較佳為二甲基甲醯胺)中，在無機鹼(諸如NaH)存在下，在適合之溫度下(較佳在室溫下)進行。Finally, or alternatively, a compound of formula Ic can be prepared by reacting a compound of formula Ie with an alkylating agent of formula III-6 '. This alkylation reaction is performed in an aprotic solvent (preferably dimethylformamide) in the presence of an inorganic base (such as NaH) at a suitable temperature (preferably at room temperature).

另外，存在於式Ib、Ic、Ie或IIc化合物中之胺基NR3 R3 ' 可稍後在合成中併入，該合成藉由遵循上文在方法A中所描述之條件，使式IVb、IVc、IVe或IIc-LG之前驅化合物分別與式V之胺反應來進行。In addition, the amine group NR 3 R 3 ′ present in the compound of formula Ib, Ic, Ie or IIc may be incorporated later in the synthesis, which makes formula IVb by following the conditions described in method A above. , IVc, IVe, or IIc-LG precursor compounds are reacted with the amine of formula V, respectively.

流程 4
根據方法A的用於自式IId或IId-LG化合物開始製備式(I)化合物(其中-X-R1 表示-[CH2 ]p -C(O)NR5 R5' )之通用合成途徑呈現於流程4中，得到式If化合物：

其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 、n及p具有如技術方案1中所定義之意義，且LG表示離去基(諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯)。 Flow 4
The general synthetic route for preparing compounds of formula (I) starting from compounds of formula IId or IId-LG (where -XR 1 represents-[CH 2 ] p -C (O) NR 5 R 5 ' ) according to method A is presented in In Scheme 4, a compound of formula If is obtained:

Wherein R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 5 , R 5 ′ , n and p have the meanings as defined in the technical scheme 1, and LG represents a leaving group (such as chlorine, bromine , Iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate).

自式IId之酸化合物及式III-2之胺製備式If化合物可在上文於流程3中所描述之醯胺化條件下進行。Preparation of a compound of formula If from an acid compound of formula IId and an amine of formula III-2 can be carried out under the amidation conditions described above in Scheme 3.

方法 B
描述用於自式VI化合物開始製備通式(I)化合物之替代性一步法，如以下流程中所示：

方法B
其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 、X及n具有如技術方案1中所定義之意義，Z表示OH或離去基，且視n之意義而定，G表示OH、鹵素或離去基。具體反應條件詳述於下文流程5及6中。 Method B
Describes an alternative one-step process for preparing compounds of formula (I) starting from compounds of formula VI, as shown in the following scheme:

Method B
Wherein R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , X and n have the meanings as defined in the technical solution 1, Z represents OH or a leaving group, and depends on the meaning of n G represents OH, halogen or leaving group. Specific reaction conditions are detailed in Schemes 5 and 6 below.

如先前已提及，或者，存在於式I化合物中之胺基NR3 R3 ' 可稍後在合成中併入，該合成藉由遵循上文在方法A中所描述之條件，使式IV之前驅化合物與式V之胺反應來進行。As already mentioned previously, or the amine group NR 3 R 3 ′ present in the compound of formula I may be incorporated later in a synthesis which makes formula IV by following the conditions described in method A above The precursor compound is reacted with an amine of formula V to proceed.

流程 5
根據方法B的用於製備式(I)化合物(其中n為0)之通用合成途徑呈現於流程5中，得到式Ig化合物：

其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 及X具有如技術方案1中所定義之意義，n為0，Z表示OH或a 離去基，且G表示OH或鹵素。 Flow 5
The general synthetic route for the preparation of a compound of formula (I) (where n is 0) according to method B is presented in scheme 5 to obtain a compound of formula Ig:

Wherein R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and X have the meanings as defined in the technical scheme 1, n is 0, Z represents OH or a leaving group, and G represents OH Or halogen.

視G及Z之意義而定，不同反應條件將適用：
a) 當G為OH且Z表示諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯之離去基時，烷基化反應在適合之溶劑(諸如二甲基甲醯胺、二甲基乙醯胺、二甲亞碸、乙腈、二氯甲烷或1,4-二噁烷)中；在鹼(諸如K2 CO3 、Cs2 CO3 、氫化鈉或第三丁醇鉀)存在下；在包含於室溫與回流溫度之間的適合之溫度下進行，或者，該反應可在微波反應器中進行。另外，可使用活化劑，諸如碘化鈉。
b) 當G為OH且Z表示OH時，反應在習知光延條件(Mitsunobu condition)下，藉由在偶氮化合物(諸如1,1'-(氮雜二羰基)二哌啶(ADDP)、偶氮二甲酸二異丙酯(DIAD)或偶氮二甲酸二乙酯(DEAD))及膦(諸如三丁基膦或三苯基膦)存在下用式VII之醇處理式VIa之苯酚來進行。光延反應在適合之溶劑(諸如甲苯或四氫呋喃)中；在包含於室溫與回流溫度之間的適合之溫度下進行。
c) 當G為鹵素且Z表示OH時，反應在習知芳族親核取代條件下，藉由在強鹼(諸如氫化鈉或第三丁醇鉀)存在下用式VIa化合物(其中G表示鹵素，較佳為氟)處理式VII之醇來進行。反應在適合之溶劑(諸如極性非質子溶劑，較佳為二甲基甲醯胺、二甲基乙醯胺或二甲亞碸)中；在包含於室溫與回流溫度之間的適合之溫度下(較佳在加熱的情況下)進行，或者，該反應可在微波反應器中進行。或者，當G為溴或碘時，式VII化合物可在交叉偶合條件下，使用Pd或Cu催化劑及適合之配位體來進行引入。Depending on the meaning of G and Z, different reaction conditions will apply:
a) When G is OH and Z represents a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate, the alkylation reaction is at Suitable solvents (such as dimethylformamide, dimethylacetamide, dimethylmethane, acetonitrile, dichloromethane, or 1,4-dioxane); in bases (such as K 2 CO 3 , Cs 2 CO 3 , sodium hydride or potassium tert-butoxide); performed at a suitable temperature comprised between room temperature and reflux temperature, or the reaction may be performed in a microwave reactor. In addition, activators such as sodium iodide can be used.
b) When G is OH and Z represents OH, the reaction is performed under the conventional Mitsunobu condition by using an azo compound such as 1,1 '-(azadicarbonyl) dipiperidine (ADDP), Phenol of formula VIa is treated with an alcohol of formula VII in the presence of diisopropyl azodicarboxylate (DIAD) or diethyl azodicarboxylate (DEAD) and a phosphine (such as tributylphosphine or triphenylphosphine). get on. The light extension reaction is carried out in a suitable solvent such as toluene or tetrahydrofuran; it is carried out at a suitable temperature comprised between room temperature and reflux temperature.
c) When G is halogen and Z represents OH, the reaction is performed under conventional aromatic nucleophilic substitution conditions by using a compound of formula VIa in the presence of a strong base such as sodium hydride or potassium tert It is preferably carried out by treating the alcohol of formula VII with fluorine. Reaction in a suitable solvent (such as a polar aprotic solvent, preferably dimethylformamide, dimethylacetamide or dimethylformamide); at a suitable temperature comprised between room temperature and reflux temperature The reaction may be carried out (preferably under heating), or the reaction may be performed in a microwave reactor. Alternatively, when G is bromine or iodine, the compound of formula VII can be introduced under cross-coupling conditions using a Pd or Cu catalyst and a suitable ligand.

流程 6
根據方法B的用於製備式(I)化合物(其中n為1)之通用合成途徑呈現於流程6中，得到式Ih化合物：

其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 及X具有如技術方案1中所定義之意義，n為1，且Z表示OH且G表示離去基，或者Z表示離去基且G表示OH。 Flow 6
The general synthetic route for the preparation of a compound of formula (I) (where n is 1) according to method B is presented in Scheme 6 to obtain a compound of formula Ih:

Wherein R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and X have the meanings as defined in the technical scheme 1, n is 1, and Z represents OH and G represents a leaving group, or Z Represents a leaving group and G represents OH.

反應在諸如上文流程5中所描述之彼等條件的標準烷基化反應條件下進行。The reaction is carried out under standard alkylation reaction conditions such as those described in Scheme 5 above.

流程 7
自共同式VIII前驅物製備關鍵式II及VI化合物概述於下文流程7中：

其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 、X及n具有如技術方案1中所定義之意義，且G、W、Y及Z具有如上文在流程1至6中所定義之意義。 Process 7
The preparation of key compounds of formula II and VI from a common formula VIII precursor is outlined in Scheme 7 below:

Wherein R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , X and n have the meanings as defined in the technical scheme 1, and G, W, Y, and Z have the same meanings as in the above schemes 1 to Meaning as defined in 6.

自式VIII化合物及式III化合物製備式VI化合物可在上文於通用方法A中所描述且進一步詳述於流程1至4中的反應條件下進行。The preparation of a compound of formula VI from a compound of formula VIII and a compound of formula III can be carried out under the reaction conditions described above in General Method A and further detailed in Schemes 1 to 4.

自式VIII化合物及式VII化合物製備式II或II-LG化合物可在上文於通用方法B中所描述且進一步詳述於流程5及6中的反應條件下進行。The preparation of a compound of formula II or II-LG from a compound of formula VIII and a compound of formula VII can be carried out under the reaction conditions described above in General Method B and further detailed in Schemes 5 and 6.

在上文所揭示之方法及流程中所用的式III、III-2、III-3、III-4、III-5、III-6、III-6'、III-7、V、VII及VIII化合物為市售的，或可遵循文獻中所描述之常用程序來加以合成。Compounds of formula III, III-2, III-3, III-4, III-5, III-6, III-6 ', III-7, V, VII and VIII used in the methods and schemes disclosed above It is commercially available, or it can be synthesized by following common procedures described in the literature.

此外，本發明之某些化合物亦可自其他式(I)化合物開始，藉由官能基之適當轉化反應，在一個或若干個步驟中，使用有機化學方法中之熟知反應在標準實驗條件下獲得。In addition, some compounds of the present invention can also be obtained from other compounds of formula (I) by appropriate conversion reactions of functional groups in one or several steps using well-known reactions in organic chemistry methods under standard experimental conditions. .

在上文所描述之一些方法中，可能有必要用適合之保護基來保護所存在之反應性或不穩定基團，諸如Boc (第三丁氧基羰基)、Teoc (2-(三甲基矽烷基)乙氧基羰基)或苄基用於保護胺基，及常用矽烷基保護基團用於保護羥基。用於引入及移除此等保護基之程序為此項技術中熟知的，且可發現其充分描述於文獻中。In some of the methods described above, it may be necessary to protect the presence of reactive or labile groups with suitable protecting groups, such as Boc (third butoxycarbonyl), Teoc (2- (trimethyl Silyl) ethoxycarbonyl) or benzyl is used to protect amine groups, and common silyl protecting groups are used to protect hydroxyl groups. The procedures for introducing and removing such protecting groups are well known in the art and can be found to be fully described in the literature.

另外，式(I)化合物可以對映純之形式獲得，其藉由用對掌性製備型HPLC或用非對映異構鹽或共晶之結晶來對外消旋式(I)化合物進行解析來進行。或者，解析步驟可在先前階段，使用任何適合之中間物來進行。In addition, compounds of formula (I) can be obtained in enantiomerically pure form by resolving the racemic compounds of formula (I) by using preparative HPLC or diastereomeric salts or eutectic crystals. get on. Alternatively, the resolution step can be performed at a previous stage using any suitable intermediate.

實例
在實例中使用以下縮寫：
ACN：乙腈
AcOH：乙酸
ADDP：1,1'-(氮雜二羰基)二哌啶
aq：水溶液
BINAP：2,2'-雙(二苯基膦基)-1,1'-聯萘
Boc：第三丁氧基羰基
CH：環己烷
DCE：二氯乙烷
DCM：二氯甲烷
脫保護：保護基脫除
DIAD：偶氮二甲酸二異丙酯
DIBALH：氫化二異丁基鋁
DIPEA：N,N -二異丙基乙胺
DMF：N,N -二甲基甲醯胺
DMSO：二甲亞碸
EtOAc：乙酸乙酯
EtOH：乙醇
EX：實例
h：小時
HATU：O -(7-氮雜苯并三唑-1-基)-N ,N ,N' ,N' -四甲基六氟磷酸鹽
HPLC：高效液相層析
INT：中間物
MeOH：甲醇
MS：質譜
Min：分鐘
Pd2 (dba)3 ：參(二苯亞甲基丙酮)二鈀(0)
Quant：定量
Ret.：滯留
r.t.：室溫
Sat：飽和
Sol.：溶液
Teoc：2-(三甲基矽烷基)乙氧基羰基
TFA：三氟乙酸
THF：四氫呋喃
TMSI：三甲基矽烷基碘化物(或又名碘基三甲基矽烷)
Wt：重量 Examples <br/> Use the following abbreviations in the examples:
ACN: Acetonitrile
AcOH: acetic acid
ADDP: 1,1 '-(azadicarbonyl) dipiperidine
aq: aqueous solution
BINAP: 2,2'-bis (diphenylphosphino) -1,1'-binaphthalene
Boc: third butoxycarbonyl
CH: Cyclohexane
DCE: Dichloroethane
DCM: methylene chloride deprotection: protecting group removal
DIAD: Diisopropyl azodicarboxylate
DIBALH: Diisobutyl aluminum hydride
DIPEA: N, N -diisopropylethylamine
DMF: N, N -dimethylformamide
DMSO: Dimethoate
EtOAc: ethyl acetate
EtOH: ethanol
EX: Examples
h: hour
HATU: O- (7-azabenzotriazol-1-yl) -N , N , N ' , N' -tetramethyl Hexafluorophosphate
HPLC: High Performance Liquid Chromatography
INT: Intermediate
MeOH: methanol
MS: mass spectrometry
Min: minutes
Pd 2 (dba) 3 : Ginseng (diphenylmethyleneacetone) dipalladium (0)
Quant: quantitative
Ret .: stranded
rt: room temperature
Sat: Saturated
Sol .: Solution
Teoc: 2- (trimethylsilyl) ethoxycarbonyl
TFA: trifluoroacetic acid
THF: tetrahydrofuran
TMSI: Trimethylsilyl iodide (also known as iodotrimethylsilane)
Wt: weight

以下方法用於測定HPLC-MS譜：
方法 A
管柱：Gemini-NX 30 × 4.6 mm，3 μm
溫度：40℃
流量：2.0 mL/min
梯度：NH4 HCO3 pH 8 : ACN (95:5)---0.5 min---(95:5)---6.5 min---(0:100)---1 min---(0:100)
樣品以大約1 mg/mL溶解於NH4 HCO3 pH 8/ ACN中
方法 B
管柱：Kinetex EVO 50 × 4.6 mm，2.6 μm
溫度：40℃
流量：2.0 mL/min
梯度：NH4 HCO3 pH 8 : ACN (95:5)---0.5 min---(95:5)---6.5 min---(0:100)---1 min---(0:100)
樣品以大約1 mg/mL溶解於NH4 HCO3 pH 8/ CAN中
方法 C
管柱：Kinetex EVO 50 × 4.6 mm，2.6 μm
溫度：40℃
流量：1.5 mL/min
梯度：NH4 HCO3 pH 8 : ACN (95:5)---0.5 min---(95:5)---6.5 min---(0:100)---2 min---(0:100)
樣品以大約1 mg/mL溶解於NH4 HCO3 pH 8/ CAN中
方法 D
管柱：Kromasil C18 250 × 4.6 mm，5 μm
溫度：40℃
流量：1 mL/min
梯度：H2 O-0.1% HCOOH / ACN (100:0)---30 min---(0:100)
樣品以大約4 mg/mL溶解於ACN/H2 O 1:1中
方法 E
管柱：Luna C18 250 × 4.6 mm，5 μm
溫度：40℃
流量：1 mL/min
梯度：H2 O-0.1% HCOOH /ACN (100:0)---30 min---(0:100)---10 min---(0:100)
樣品以大約1 mg/mL溶解於ACN中
方法 F
管柱：Gemini C18 30 × 4.6 mm，3 μm
溫度：40℃
流量：1.5 mL/min
梯度H2 O-0.1% HCOOH / ACN (95:5)---0.5 min---(95:5) ---8.5 min-----(0:100)---1 min---(0:100)
樣品以大約1 mg/mL溶解於ACN中The following methods were used to determine the HPLC-MS spectrum:
Method A
Column: Gemini-NX 30 × 4.6 mm, 3 μm
Temperature: 40 ° C
Flow: 2.0 mL / min
Gradient: NH 4 HCO 3 pH 8: ACN (95: 5) --- 0.5 min --- (95: 5) --- 6.5 min --- (0: 100) --- 1 min --- ( 0: 100)
The sample was dissolved in NH 4 HCO 3 pH 8 / ACN at approximately 1 mg / mL
Method B
Column: Kinetex EVO 50 × 4.6 mm, 2.6 μm
Temperature: 40 ° C
Flow: 2.0 mL / min
Gradient: NH 4 HCO 3 pH 8: ACN (95: 5) --- 0.5 min --- (95: 5) --- 6.5 min --- (0: 100) --- 1 min --- ( 0: 100)
The sample is dissolved in NH 4 HCO 3 pH 8 / CAN at approximately 1 mg / mL
Method C
Column: Kinetex EVO 50 × 4.6 mm, 2.6 μm
Temperature: 40 ° C
Flow: 1.5 mL / min
Gradient: NH 4 HCO 3 pH 8: ACN (95: 5) --- 0.5 min --- (95: 5) --- 6.5 min --- (0: 100) --- 2 min --- ( 0: 100)
The sample is dissolved in NH 4 HCO 3 pH 8 / CAN at approximately 1 mg / mL
Method D
Column: Kromasil C18 250 × 4.6 mm, 5 μm
Temperature: 40 ° C
Flow: 1 mL / min
Gradient: H 2 O-0.1% HCOOH / ACN (100: 0) --- 30 min --- (0: 100)
The sample was dissolved in ACN / H 2 O 1: 1 at approximately 4 mg / mL
Method E
Column: Luna C18 250 × 4.6 mm, 5 μm
Temperature: 40 ° C
Flow: 1 mL / min
Gradient: H 2 O-0.1% HCOOH / ACN (100: 0) --- 30 min --- (0: 100) --- 10 min --- (0: 100)
The sample is dissolved in ACN at approximately 1 mg / mL
Method F
Column: Gemini C18 30 × 4.6 mm, 3 μm
Temperature: 40 ° C
Flow: 1.5 mL / min
Gradient H 2 O-0.1% HCOOH / ACN (95: 5) --- 0.5 min --- (95: 5) --- 8.5 min ----- (0: 100) --- 1 min-- -(0: 100)
The sample is dissolved in ACN at approximately 1 mg / mL

中間物之合成
中間物1：(R )-(3-(2-溴苯氧基)-3-(噻吩-2-基)丙基)(乙基)胺基甲酸2-(三甲基矽烷基)乙酯
 Synthesis of intermediates <br/> Intermediate 1: ( R )-(3- (2-bromophenoxy) -3- (thien-2-yl) propyl) (ethyl) aminocarboxylic acid 2- ( Trimethylsilyl) ethyl ester

步驟1. (R )-3-(乙基胺基)-1-(噻吩-2-基)丙-1-醇：在密封燒瓶中將(R )-3-氯-1-(噻吩-2-基)丙-1-醇(7 g，39.6 mmol)及乙基胺 (於水中之70 wt%溶液，31 mL，396 mmol)於EtOH (175 mL) 中之溶液在90℃下加熱隔夜。蒸發溶劑，將殘餘物溶解於DCM中，且用1 N NaOH對其進行洗滌，經MgSO4 乾燥，過濾，且濃縮至乾燥。將粗產物(7.74 g)在甲基環己烷-甲苯之混合物(3:1 v/v，22 mL)中製成漿液，且在60℃下加熱1小時。隨後，使其冷卻，且將其在室溫下攪拌1小時。濾出固體，用甲基環己烷洗滌，且在真空下乾燥，獲得標題化合物(2.68 g，產率36%)。Step 1. ( R ) -3- (ethylamino) -1- (thien-2-yl) propan-1-ol: ( R ) -3-chloro-1- (thiophene-2) in a sealed flask -Yl) propan-1-ol (7 g, 39.6 mmol) and a solution of ethylamine (70 wt% solution in water, 31 mL, 396 mmol) in EtOH (175 mL) were heated at 90 ° C. overnight. The solvent was evaporated, the residue was dissolved in DCM, and washed with 1 N NaOH subjected washed, dried over MgSO 4, filtered, and concentrated to dryness. The crude product (7.74 g) was slurried in a methylcyclohexane-toluene mixture (3: 1 v / v, 22 mL) and heated at 60 ° C for 1 hour. Subsequently, it was allowed to cool, and it was stirred at room temperature for 1 hour. The solid was filtered off, washed with methylcyclohexane, and dried under vacuum to obtain the title compound (2.68 g, yield 36%).

步驟2. (R )-3-(2-溴苯氧基)-N -乙基-3-(噻吩-2-基)丙-1-胺：在N2 氛圍下，向步驟1中所獲得之產物(0.98 g，5.3 mmol)及1-溴-2-氟苯(2.29 mL，21.1 mmol)於DMSO (1.6 mL)中之溶液中添加第三丁醇鉀(0.6 g，5.3 mmol)，且將反應混合物在60℃下加熱8小時。隨後將其冷卻至室溫，且添加水。用EtOAc萃取水相兩次。經MgSO4 乾燥經合併之有機相，過濾，且蒸發至乾燥。藉由急驟層析，矽膠，梯度DCM至MeOH:DCM (1:4)來純化粗產物，得到標題化合物(1.14 g，產率63%)。Step 2. ( R ) -3- (2-Bromophenoxy) -N -ethyl-3- (thien-2-yl) propan-1-amine: Under N 2 atmosphere, proceed to step 1 To a solution of the product (0.98 g, 5.3 mmol) and 1-bromo-2-fluorobenzene (2.29 mL, 21.1 mmol) in DMSO (1.6 mL) was added potassium tert-butoxide (0.6 g, 5.3 mmol), and The reaction mixture was heated at 60 ° C for 8 hours. It was then cooled to room temperature and water was added. The aqueous phase was extracted twice with EtOAc. The organic phase was dried over MgSO 4 merger, filtered, and evaporated to dryness. The crude product was purified by flash chromatography, silica gel, gradient DCM to MeOH: DCM (1: 4) to give the title compound (1.14 g, yield 63%).

步驟3. 標題化合物：在N2 氛圍下，向步驟2中所獲得之產物(1.14 g，3.3 mmol)於DCM (1.5 mL)中之溶液中添加DIPEA (0.58 mL，3.3 mml)及(2-(三甲基矽烷基)乙基)碳酸4-硝基苯酯(0.95 g，3.3 mmol)於DCM (1.5 mL)中之溶液。在於室溫下攪拌隔夜之後，添加NaHCO3 飽和溶液，且用DCM對其進行萃取兩次。用2 N NaOH溶液洗滌經合併之有機相，經MgSO4 乾燥，過濾，且濃縮至乾燥。藉由急驟層析，矽膠，梯度CH至EtOAc來純化殘餘物，得到標題化合物(1.46 g，產率90%)。Step 3. The title compound: To a solution of the product obtained in Step 2 (1.14 g, 3.3 mmol) in DCM (1.5 mL) under N 2 atmosphere was added DIPEA (0.58 mL, 3.3 mml) and (2- (Trimethylsilyl) ethyl) 4-nitrophenyl carbonate (0.95 g, 3.3 mmol) in DCM (1.5 mL). After that stirring overnight at room temperature, saturated NaHCO 3 solution, and extracted twice with DCM. , Washed with 2 N NaOH solution was dried by the combined organic phases over MgSO 4, filtered, and concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (1.46 g, yield 90%).

此方法用於使用適合之起始物質來製備中間物2-4：
This method is used to prepare intermediates 2-4 using suitable starting materials:

中間物5：2-(3-氯-1-(噻吩-2-基)丙氧基)苯甲醛
Intermediate 5: 2- (3-chloro-1- (thien-2-yl) propoxy) benzaldehyde

步驟1. 2-(3-氯-1-(噻吩-2-基)丙氧基)苯甲腈：向在0℃下冷卻的3-氯-1-(噻吩-2-基)丙-1-醇(10 g，52 mmol)、三苯基膦(15 g，57.2 mmol)及2-羥基苯甲腈(6.8 g，57.2 mmol)於無水THF (252 mL)中之溶液中逐滴添加DIAD (11.5 mL，58.3 mmol)。在於室溫下攪拌隔夜之後，在真空下濃縮溶劑，且藉由急驟層析，矽膠，梯度CH至EtOAc來純化殘餘物，得到標題化合物(13.9 g，產率96%)。Step 1. 2- (3-Chloro-1- (thien-2-yl) propoxy) benzonitrile: To 3-chloro-1- (thien-2-yl) propan-1 cooled at 0 ° C -DIAD was added dropwise to a solution of an alcohol (10 g, 52 mmol), triphenylphosphine (15 g, 57.2 mmol) and 2-hydroxybenzonitrile (6.8 g, 57.2 mmol) in anhydrous THF (252 mL). (11.5 mL, 58.3 mmol). After stirring overnight at room temperature, the solvent was concentrated under vacuum and the residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (13.9 g, yield 96%).

步驟2. 標題化合物：向在0℃下冷卻的步驟1中所獲得之產物(4 g，14.4 mol)於甲苯(40 mL)中之溶液中逐滴添加DIBALH (於甲苯中之25 wt%溶液，13.5 mL，20.2 mmol)，將反應物在0℃-5℃下攪拌4小時。隨後，緩慢添加10% HCl水溶液以使反應淬滅，且將混合物在室溫下攪拌10分鐘。用EtOAc對其進行萃取，且用水及鹽水洗滌經合併之有機相，經Na2 SO4 乾燥，且濃縮至乾燥。藉由急驟層析，矽膠，梯度CH至EtOAc來純化殘餘物，得到標題化合物(4 g，產率38%)。Step 2. Title compound: To a solution of the product obtained in Step 1 (4 g, 14.4 mol) in toluene (40 mL) cooled at 0 ° C was added DIBALH (25 wt% solution in toluene) dropwise. , 13.5 mL, 20.2 mmol), and the reaction was stirred at 0 ° C-5 ° C for 4 hours. Subsequently, a 10% aqueous HCl solution was slowly added to quench the reaction, and the mixture was stirred at room temperature for 10 minutes. Be extracted with EtOAc, and washed with water and brine of the combined organic phases were dried over Na 2 SO 4, and concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (4 g, yield 38%).

此方法用於使用適合之起始物質來製備中間物6：
(1) 在步驟2中使用DIBALH於DCM中之1 M溶液This method is used to prepare intermediate 6 using suitable starting materials:
(1) Use a 1 M solution of DIBALH in DCM in step 2

中間物7. 2-(3-氯-1-(噻吩-2-基)丙氧基)苯甲酸鋰
Intermediate 7. lithium 2- (3-chloro-1- (thien-2-yl) propoxy) benzoate

步驟1. 2-(3-氯-1-(噻吩-2-基)丙氧基)苯甲酸甲酯：向3-氯-1-(噻吩-2-基)丙-1-醇(2 g，11.3 mmol)、三丁基膦(3.4 mL，13.6 mmol)及2-羥基苯甲酸甲酯 (1.45 mL，11.3 mmol)於無水THF (20 mL)中之溶液中添加ADDP (3.4 g，13.6 mmol)。將混合物在室溫下攪拌隔夜。經由矽藻土墊過濾懸浮液，用THF洗滌，且在真空中濃縮濾液。藉由急驟層析，矽膠，梯度CH至EtOAc來純化粗產物，得到標題化合物(1.27 g，產率36%)。Step 1. Methyl 2- (3-chloro-1- (thien-2-yl) propoxy) benzoate: 3-chloro-1- (thien-2-yl) propan-1-ol (2 g , 11.3 mmol), tributylphosphine (3.4 mL, 13.6 mmol) and methyl 2-hydroxybenzoate (1.45 mL, 11.3 mmol) in anhydrous THF (20 mL) was added ADDP (3.4 g, 13.6 mmol) ). The mixture was stirred at room temperature overnight. The suspension was filtered through a celite pad, washed with THF, and the filtrate was concentrated in vacuo. The crude product was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (1.27 g, 36% yield).

步驟2. 標題化合物：將步驟1中所獲得之化合物(1.05 g，3.4 mmol)於THF (17 mL)中之溶液及1 M LiOH溶液(17 mL，17 mmol)在50℃下加熱隔夜。蒸發溶劑，添加甲苯，且將其再次濃縮至乾燥以移除殘餘水。粗產物不經進一步純化即用於下一步驟中(1.76 g，定量)。Step 2. The title compound: A solution of the compound obtained in step 1 (1.05 g, 3.4 mmol) in THF (17 mL) and a 1 M LiOH solution (17 mL, 17 mmol) were heated at 50 ° C overnight. The solvent was evaporated, toluene was added, and it was concentrated to dryness again to remove residual water. The crude product was used in the next step without further purification (1.76 g, quantitative).

中間物8. (3-(2-溴苯氧基)-3-(噻吩-2-基)丙基)(甲基)胺基甲酸第三丁酯
Intermediate 8. (3- (2-Bromophenoxy) -3- (thien-2-yl) propyl) (methyl) aminoformic acid third butyl ester

步驟1. 2-(1-(2-溴苯氧基)-3-氯丙基)噻吩：遵循中間物7之步驟1中所描述的實驗程序，但使用2-溴苯酚替代2-羥基苯甲酸甲酯，獲得標題化合物且其不經進一步純化即使用(3.85 g，產率定量)。Step 1. 2- (1- (2-Bromophenoxy) -3-chloropropyl) thiophene: Follow the experimental procedure described in step 1 of intermediate 7, but use 2-bromophenol instead of 2-hydroxybenzene Methyl formate, the title compound was obtained and used without further purification (3.85 g, quantitative yield).

步驟2. 3-(2-溴苯氧基)-N -甲基-3-(噻吩-2-基)丙-1-胺：在密封管中，將步驟1中所獲得之產物(3.75 g，11.32 mmol)及甲胺(於EtOH中之33 wt%溶液，30 mL，226 mmol)的混合物在100℃下加熱隔夜。隨後，將其濃縮至乾燥，且粗物質不經進一步純化即用於下一步驟中(3.72 g，產率定量)。Step 2. 3- (2-Bromophenoxy) -N -methyl-3- (thien-2-yl) propan-1-amine: In a sealed tube, combine the product obtained in step 1 (3.75 g , 11.32 mmol) and methylamine (33 wt% solution in EtOH, 30 mL, 226 mmol) were heated at 100 ° C. overnight. It was then concentrated to dryness and the crude material was used in the next step without further purification (3.72 g, quantitative yield).

步驟3. 標題化合物：向步驟2中所獲得之產物(3.7 g，11.32 mmol)於第三丁醇(10 mL)中之溶液中添加2 M NaOH溶液(10 mL)及二碳酸二第三丁酯(2.5 g，11.3 mmol)，且將反應混合物在室溫下攪拌隔夜。添加鹽水及DCM，且分離各相，且用DCM萃取水層。用鹽水洗滌經合併之有機相，經MgSO4 ，過濾，且濃縮至乾燥。藉由急驟層析，矽膠，梯度CH至EtOAc來純化殘餘物，得到標題化合物(1.34 g，對於3個步驟，產率28%)。Step 3. The title compound: To a solution of the product obtained in Step 2 (3.7 g, 11.32 mmol) in tert-butanol (10 mL) was added 2 M NaOH solution (10 mL) and di-tert-butyl dicarbonate. Ester (2.5 g, 11.3 mmol), and the reaction mixture was stirred at room temperature overnight. Brine and DCM were added and the phases were separated and the aqueous layer was extracted with DCM. Washed with brine the combined organic phases, dried over MgSO 4, filtered, and concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (1.34 g, 28% yield over 3 steps).

中間物9. 2-(3-(甲基((2-(三甲基矽烷基)乙氧基)羰基)胺基)-1-(噻吩-2-基)丙氧基)苯甲酸鋰
Intermediate 9. lithium 2- (3- (methyl ((2- (trimethylsilyl) ethoxy) carbonyl) amino) -1- (thien-2-yl) propoxy) lithium benzoate

步驟1. 2-(3-(苄基(甲基)胺基)-1-(噻吩-2-基)丙氧基)苯甲酸甲酯：遵循中間物7之步驟1中所描述的實驗程序，自3-(苄基(甲基)胺基)-1-(噻吩-2-基)丙-1-醇及2-羥基苯甲酸甲酯開始，獲得標題化合物(195 mg，產率43%)。Step 1. Methyl 2- (3- (benzyl (methyl) amino) -1- (thien-2-yl) propoxy) benzoate: follow the experimental procedure described in step 1 of intermediate 7 Starting from 3- (benzyl (methyl) amino) -1- (thien-2-yl) propan-1-ol and methyl 2-hydroxybenzoate, the title compound (195 mg, 43% yield ).

步驟2. 2-(3-(甲基((2-(三甲基矽烷基)乙氧基)羰基)胺基)-1-(噻吩-2-基)丙氧基)苯甲酸甲酯：在0℃下向2-(三甲基矽烷基)乙醇(0.21 mL，1.5 mmol)及K2 CO3 (0.42 g，3 mmol)於甲苯(2 mL)中之溶液中逐滴添加三光氣(146 mg，0.49 mmol)於甲苯(1 mL)中之溶液。將混合物在室溫下攪拌1小時，且隨後冷卻至0℃。向此混合物中，在0℃下添加步驟1中所獲得之化合物(195 mg，0.49 mmol)於甲苯(2 mL)中之溶液，且將所得混合物在室溫下攪拌隔夜。將反應混合物傾入NaHCO3 飽和溶液中，且用EtOAc對其進行萃取兩次。經MgSO4 乾燥經合併之有機萃取物，過濾，且濃縮至乾燥。藉由急驟層析，矽膠，梯度CH至EtOAc來純化粗產物，得到標題化合物(190 mg，產率85%)。Step 2. Methyl 2- (3- (methyl ((2- (trimethylsilyl) ethoxy) carbonyl) amino) -1- (thien-2-yl) propoxy) benzoate: To a solution of 2- (trimethylsilyl) ethanol (0.21 mL, 1.5 mmol) and K 2 CO 3 (0.42 g, 3 mmol) in toluene (2 mL) at 0 ° C was added triphosgene ( 146 mg, 0.49 mmol) in toluene (1 mL). The mixture was stirred at room temperature for 1 hour, and then cooled to 0 ° C. To this mixture, a solution of the compound obtained in Step 1 (195 mg, 0.49 mmol) in toluene (2 mL) was added at 0 ° C, and the resulting mixture was stirred at room temperature overnight. The reaction mixture was poured into a saturated solution of NaHCO 3, and the mixture was extracted twice with EtOAc thereof. Dried over MgSO 4 the organic extracts were combined, filtered, and concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (190 mg, yield 85%).

步驟3. 標題化合物：遵循中間物7之步驟2中所描述的實驗程序，自步驟2中所獲得之產物開始，獲得呈粗產物形式之標題化合物，其藉由經由C18-柱溶離來進行純化，得到標題化合物(49 mg，產率26%)。Step 3. The title compound: Following the experimental procedure described in step 2 of intermediate 7, starting from the product obtained in step 2, the title compound was obtained as a crude product, which was purified by dissociation through a C18-column To give the title compound (49 mg, yield 26%).

中間物10. (3-(2-溴苯氧基)-3-苯基丙基)(甲基)胺基甲酸第三丁酯：
Intermediate 10. (3- (2-Bromophenoxy) -3-phenylpropyl) (methyl) aminocarboxylic acid third butyl ester:

在密封管中，將(3-氯-3-苯基丙基)(甲基)胺基甲酸第三丁酯(4 g，14.1 mmol)、K2 CO3 (5.84 g，42.3 mmol)、KI (234 mg，1.41 mmol)及2-溴苯酚(2.4 g，14.1 mmol)於ACN (92 mL)中之混合物在60℃下加熱隔夜。向反應混合物中添加水，且用EtOAc對其進行萃取。經MgSO4 乾燥經合併之有機萃取物，過濾，且濃縮至乾燥。藉由急驟層析，矽膠，梯度CH至EtOAc來純化粗產物，得到標題化合物(2.36 g，產率40%)。In a sealed tube, (3-chloro-3-phenylpropyl) (meth) aminocarboxylic acid tert-butyl ester (4 g, 14.1 mmol), K 2 CO 3 (5.84 g, 42.3 mmol), KI A mixture of (234 mg, 1.41 mmol) and 2-bromophenol (2.4 g, 14.1 mmol) in ACN (92 mL) was heated at 60 ° C overnight. Water was added to the reaction mixture, and it was extracted with EtOAc. Dried over MgSO 4 the organic extracts were combined, filtered, and concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (2.36 g, 40% yield).

此方法用於使用適合之起始物質來製備中間物11：
This method is used to prepare intermediate 11 using suitable starting materials:

中間物12. 2-(3-((第三丁氧基羰基)(甲基)胺基)-1-苯基丙氧基)苯甲酸
Intermediate 12. 2- (3-((third butoxycarbonyl) (methyl) amino) -1-phenylpropoxy) benzoic acid

步驟1. 2-(3-((第三丁氧基羰基)(甲基)胺基)-1-苯基丙氧基)苯甲酸甲酯：遵循中間物10中所描述之實驗程序，但使用2-羥基苯甲酸甲酯替代2-溴苯酚，獲得標題化合物(1.48 g，產率63%)。Step 1. Methyl 2- (3-((third butoxycarbonyl) (methyl) amino) -1-phenylpropoxy) benzoate: follow the experimental procedure described in Intermediate 10, but Using methyl 2-hydroxybenzoate in place of 2-bromophenol gave the title compound (1.48 g, 63% yield).

步驟2. 標題化合物：向步驟1中所獲得之化合物(1.48 g，3.7 mmol)於THF:水之混合物(1:1，15 mL)中的溶液中添加單水合氫氧化鋰(1.2 g，30 mmol)，且將反應混合物在50℃下加熱隔夜。濃縮溶劑，用6 M HCl將pH值調節至3，且用EtOAc對其進行萃取。經MgSO4 乾燥經合併之有機萃取物，過濾，且濃縮至乾燥，得到標題化合物(1.1 g，產率78%)。Step 2. Title compound: To a solution of the compound obtained in Step 1 (1.48 g, 3.7 mmol) in a THF: water mixture (1: 1, 15 mL) was added lithium hydroxide monohydrate (1.2 g, 30 mmol) and the reaction mixture was heated at 50 ° C. overnight. The solvent was concentrated, the pH was adjusted to 3 with 6 M HCl, and it was extracted with EtOAc. Dried over MgSO 4 the organic extracts were combined, filtered, and concentrated to dryness to give the title compound (1.1 g, 78% yield).

中間物13. (3-((2-溴苄基)氧基)-3-苯基丙基)(甲基)胺基甲酸第三丁酯
Intermediate 13. (3-((2-bromobenzyl) oxy) -3-phenylpropyl) (meth) carbamic acid third butyl ester

在N2 氛圍下，向在0℃下冷卻的(3-羥基-3-苯基丙基)(甲基)胺基甲酸第三丁酯 (2 g，7.5 mmol)及碘化四丁銨(2.8 g，7.5 mmol)於DMF (10 mL)中之溶液中逐份添加NaH (於礦物油中之60%分散液，603 mg，15 mmol)。將反應物在0℃下攪拌30分鐘，且隨後添加1-溴-2-(溴甲基)苯(1.8 g，7.5 mmol)於DMF (4 mL)中之溶液。將反應混合物在室溫下攪拌隔夜。添加水及EtOAc，分離各相，且用EtOAc萃取水相。用水及鹽水洗滌經合併之有機萃取物，經MgSO4 乾燥，過濾，且濃縮至乾燥。藉由急驟層析，矽膠，梯度CH至EtOAc來純化粗產物，得到標題化合物(2.34 g，產率71%)。Under a N 2 atmosphere, to (3-hydroxy-3-phenylpropyl) (meth) carbamic acid third butyl ester (2 g, 7.5 mmol) and tetrabutylammonium iodide ( To a solution of 2.8 g, 7.5 mmol) in DMF (10 mL) was added NaH (60% dispersion in mineral oil, 603 mg, 15 mmol) in portions. The reaction was stirred at 0 ° C for 30 minutes, and then a solution of 1-bromo-2- (bromomethyl) benzene (1.8 g, 7.5 mmol) in DMF (4 mL) was added. The reaction mixture was stirred at room temperature overnight. Water and EtOAc were added, the phases were separated, and the aqueous phase was extracted with EtOAc. , Washed with water and brine and dried by the combined organic extracts were dried over MgSO 4, filtered, and concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (2.34 g, yield 71%).

中間物14. (3-(2-胺基苯氧基)-3-苯基丙基)(甲基)胺基甲酸第三丁酯
Intermediate 14. (3- (2-Aminophenoxy) -3-phenylpropyl) (meth) carbamic acid third butyl ester

步驟1. 甲基(3-(2-硝基苯氧基)-3-苯基丙基)胺基甲酸第三丁酯：遵循中間物5之步驟1中所描述的實驗程序，自(3-羥基-3-苯基丙基)(甲基)胺基甲酸第三丁酯及2-硝基苯酚開始，獲得標題化合物(1.55 g，產率63%)。Step 1. Methyl (3- (2-nitrophenoxy) -3-phenylpropyl) aminocarboxylic acid third butyl ester: Follow the experimental procedure described in step 1 of intermediate 5 from (3 -Hydroxy-3-phenylpropyl) (meth) carbamic acid tert-butyl ester and 2-nitrophenol to obtain the title compound (1.55 g, 63% yield).

步驟2.標題化合物：向步驟1中所獲得之化合物(1.55 g, 4 mmol)於EtOH:水之混合物(4:1，33 mL)中的溶液中添加鐵(2.2 g，40 mmol)及氯化銨(107 mg，2 mmol)。將混合物在回流溫度下加熱4小時。使其冷卻，且經由矽藻土墊過濾懸浮液，用EtOH洗滌，且濃縮至乾燥，得到標題化合物，其不經進一步純化即使用(1.24 g，產率87%)。Step 2. The title compound: To a solution of the compound (1.55 g, 4 mmol) obtained in Step 1 in a mixture of EtOH: water (4: 1, 33 mL) was added iron (2.2 g, 40 mmol) and chlorine Ammonium (107 mg, 2 mmol). The mixture was heated at reflux temperature for 4 hours. It was allowed to cool, and the suspension was filtered through a celite pad, washed with EtOH, and concentrated to dryness to give the title compound, which was used without further purification (1.24 g, yield 87%).

中間物 15. (R )-(3-(2- 溴苯氧基 )-3-( 噻吩 -3- 基 ) 丙基 )( 甲基 ) 胺基甲酸 2-( 三甲基矽烷基 ) 乙酯
Intermediate 15. ( R )-(3- (2- bromophenoxy ) -3- ( thien- 3 -yl ) propyl ) ( methyl ) aminocarboxylic acid 2- ( trimethylsilyl ) ethyl ester

遵循對於製備中間物1所描述之實驗程序，使用(R )-3-氯-1-(噻吩-3-基)丙-1-醇及甲胺作為起始物質，獲得標題化合物。Following the experimental procedure described for the preparation of intermediate 1, using ( R ) -3-chloro-1- (thien-3-yl) propan-1-ol and methylamine as starting materials, the title compound was obtained.

中間物 16: (R )- 乙基 (3-(2-(2- 側氧基乙基 ) 苯氧基 )-3-( 噻吩 -2- 基 ) 丙基 ) 胺基甲酸 2-( 三甲基矽烷基 ) 乙酯
Intermediate 16: (R) - ethyl (3- (2- (2-oxoethyl) phenoxy) -3- (thiophen-2-yl) propyl) carbamic acid 2- (trimethylsilyl Silyl ) ethyl

步驟 1. (R )-(3-(2- 烯丙基苯氧基 )-3-( 噻吩 -2- 基 ) 丙基 )( 乙基 ) 胺基甲酸 2-( 三甲基矽烷基 ) 乙酯： 在密封管中，裝入Pd(PPh3 )4 (137 mg，0.145 mmol)、2-烯丙基-4,4,5,5-四甲基-1,3,2-二氧㖦硼戊環(0.73 g，4.3 mmol)及碳酸鉀(0.3 g，2.17 mmol)，且用氬氣使該管惰性化。隨後，添加中間物1 (0.7 g，1.45 mmol)於1,4-二噁烷(18 mL)中之溶液，且在氬氣氛圍下將反應物在110℃下加熱4小時。經由矽藻土墊過濾反應混合物，用EtOAc對該墊進行洗滌。用鹽水洗滌濾液，經MgSO4 乾燥，過濾，且濃縮至乾燥。藉由急驟層析，矽膠，梯度CH至EtOAc來純化殘餘物，得到標題化合物(478 mg，產率74%)。 Step 1. ( R )-(3- (2- allylphenoxy ) -3- ( thien -2- yl ) propyl ) ( ethyl ) aminocarboxylic acid 2- ( trimethylsilyl ) ethyl Esters: Fill a sealed tube with Pd (PPh 3 ) 4 (137 mg, 0.145 mmol), 2-allyl-4,4,5,5-tetramethyl-1,3,2-dioxin Borapentane (0.73 g, 4.3 mmol) and potassium carbonate (0.3 g, 2.17 mmol), and the tube was inertized with argon. Subsequently, a solution of Intermediate 1 (0.7 g, 1.45 mmol) in 1,4-dioxane (18 mL) was added, and the reaction was heated at 110 ° C. for 4 hours under an argon atmosphere. The reaction mixture was filtered through a pad of celite and the pad was washed with EtOAc. , The filtrate was washed with brine, dried over MgSO 4, filtered, and concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (478 mg, yield 74%).

步驟 2. 標題化合物： 向步驟1中所獲得之產物(478 mg，1.07 mmol)於THF-水之混合物(2:1，22.5 mL)中的溶液中添加OsO4 之溶液(4 wt%水溶液，0.75 mL，0.118 mmol)。將其在室溫下攪拌10分鐘，且隨後添加NaIO4 (573 mg，2.68 mmol)，且將反應混合物在室溫下攪拌15分鐘。蒸發溶劑，且用EtOAc萃取水相。經MgSO4 乾燥經合併之有機萃取物，過濾，且濃縮至乾燥，得到標題化合物(448 mg，產率93%)。 Step 2. The title compound: To a solution of the product obtained in Step 1 (478 mg, 1.07 mmol) in a THF-water mixture (2: 1, 22.5 mL) was added a solution of OsO 4 (4 wt% aqueous solution, 0.75 mL, 0.118 mmol). It was stirred at room temperature for 10 minutes, and then NaIO 4 (573 mg, 2.68 mmol) was added, and the reaction mixture was stirred at room temperature for 15 minutes. The solvent was evaporated and the aqueous phase was extracted with EtOAc. The combined organic extracts were dried over MgSO 4 , filtered, and concentrated to dryness to give the title compound (448 mg, yield 93%).

此方法用於使用適合之起始物質來製備中間物17-19：
This method is used to prepare intermediates 17-19 using suitable starting materials:

實例之合成
通用保護基脫除方法
方法1. 用TMSI進行Boc保護基脫除。向N -Boc保護之化合物(1 mmol)於無水ACN (45 mL)中之溶液中逐滴添加TMSI (2 mmol)。在於室溫下攪拌15分鐘之後，添加NaHCO3 飽和溶液及DCM，且將混合物再攪拌10分鐘。分離各相，經MgSO4 乾燥有機相，且濃縮至乾燥，得到粗化合物，藉由急驟層析，矽膠，梯度DCM至MeOH:DCM (1:4)來對其進行純化。 Synthesis of Examples <br/> General Protective Group Removal Method Method 1. Boc protective group removal using TMSI. To a solution of the N- Boc protected compound (1 mmol) in anhydrous ACN (45 mL) was added TMSI (2 mmol) dropwise. After 15 minutes stirring at room temperature that the addition of a saturated solution of NaHCO 3 and DCM, and the mixture was stirred for a further 10 minutes. The phases were separated, the organic phase was dried over MgSO 4 and concentrated to dryness to give the crude compound, which was purified by flash chromatography, silica gel, gradient DCM to MeOH: DCM (1: 4).

方法2. 用TFA進行Boc保護基脫除。在室溫下攪拌N -Boc保護之化合物(1 mmol)於DCM (15 mL)及TFA (10 mmol)之混合物中的溶液，直至達成完全轉化為止。蒸發揮發物，且將殘餘物再溶解於DCM中，且用1 M NaOH溶液及鹽水洗滌，經MgSO4 乾燥，且濃縮。藉由急驟層析，矽膠，梯度DCM至MeOH:DCM (1:4)來純化粗化合物。Method 2. Removal of Boc protecting group by TFA. A solution of the N- Boc protected compound (1 mmol) in a mixture of DCM (15 mL) and TFA (10 mmol) was stirred at room temperature until complete conversion was achieved. The volatiles were evaporated, and the residue was dissolved in DCM, and washed with 1 M NaOH solution and brine, dried over MgSO 4, and concentrated. The crude compound was purified by flash chromatography, silica gel, gradient DCM to MeOH: DCM (1: 4).

方法3. 用HCl進行Boc保護基脫除。在N2 氛圍下，向N -Boc保護之化合物(1 mmol)於二噁烷(10 mL)中之溶液中添加HCl (於二噁烷中之4 N溶液，10 mmol)。將反應物在室溫下攪拌隔夜。蒸發溶劑，且藉由經由酸性離子交換樹脂柱(SCX)溶離來純化殘餘物，得到所需化合物，藉由急驟層析，矽膠，梯度DCM至MeOH:DCM (1:4)來對其進行進一步純化。Method 3. Removal of Boc protecting group with HCl. To a solution of the N- Boc protected compound (1 mmol) in dioxane (10 mL) under N 2 atmosphere was added HCl (4 N solution in dioxane, 10 mmol). The reaction was stirred at room temperature overnight. The solvent was evaporated and the residue was purified by dissolution through an acidic ion exchange resin column (SCX) to obtain the desired compound, which was further purified by flash chromatography, silica gel, gradient DCM to MeOH: DCM (1: 4) purification.

方法4 用ZnBr2 進行Boc保護基脫除。在N2 氛圍下，將N -Boc保護之化合物(1 mmol)於DCM (5 mL)中之溶液添加至ZnBr2 (5.7 mmol)於DCM (50 mL)中之攪拌懸浮液中。在將混合物於室溫下攪拌隔夜之後，添加水，且將其攪拌5分鐘。分離各層，且用DCM萃取水相。經MgSO4 乾燥經合併之有機萃取物，且濃縮。藉由急驟層析，矽膠，梯度DCM至MeOH:DCM (1:4)來純化粗化合物。Method 4 Removal of the Boc protecting group with ZnBr 2 . A solution of N- Boc protected compound (1 mmol) in DCM (5 mL) was added to a stirred suspension of ZnBr 2 (5.7 mmol) in DCM (50 mL) under N 2 atmosphere. After the mixture was stirred at room temperature overnight, water was added, and it was stirred for 5 minutes. The layers were separated and the aqueous phase was extracted with DCM. Dried over MgSO 4 the organic extracts were combined, and concentrated. The crude compound was purified by flash chromatography, silica gel, gradient DCM to MeOH: DCM (1: 4).

方法5. 用CsF進行Teoc保護基脫除。將N -Teoc保護之化合物(1 mmol)及氟化銫(5 mmol)於DMF (26 mL)中之溶液在90℃下加熱1小時。將溶劑濃縮至乾燥，且藉由急驟層析，矽膠，梯度DCM至MeOH:DCM (1:4)來純化粗產物。Method 5. Teoc protecting group removal using CsF. A solution of the N- Teoc protected compound (1 mmol) and cesium fluoride (5 mmol) in DMF (26 mL) was heated at 90 ° C for 1 hour. The solvent was concentrated to dryness and the crude product was purified by flash chromatography, silica gel, gradient DCM to MeOH: DCM (1: 4).

實例1：2-(3-(甲胺基)-1-苯基丙氧基)-N -(噻吩-2-基甲基)苯胺
Example 1: 2- (3- (methylamino) -1-phenyl-propoxy) - N - (thiophen-2-ylmethyl) aniline

步驟1. 甲基(3-苯基-3-(2-((噻吩-2-基甲基)胺基)苯氧基)丙基)胺基甲酸第三丁酯：在密封管中，在氬氣氛圍下，將中間物10 (100 mg，0.238 mmol)、噻吩-2-基甲胺(50 mg，0.442 mmol)、Pd2 (dba)3 (22 mg，0.024 mmol)、BINAP (29 mg，0.048 mmol)及第三丁醇鈉(67 mg，0.714 mmol)於無水甲苯(4 mL)中之混合物在120℃下加熱隔夜。經由矽藻土墊過濾反應混合物，用EtOAc洗滌，且將濾液濃縮至乾燥。藉由急驟層析，矽膠，梯度CH至EtOAc來純化殘餘物，得到標題化合物(90 mg，產率83%)。Step 1. Methyl (3-phenyl-3- (2-((thiophen-2-ylmethyl) amino) phenoxy) propyl) aminocarboxylic acid third butyl ester: In a sealed tube, in Under argon atmosphere, intermediate 10 (100 mg, 0.238 mmol), thien-2-ylmethylamine (50 mg, 0.442 mmol), Pd 2 (dba) 3 (22 mg, 0.024 mmol), BINAP (29 mg , 0.048 mmol) and sodium tert-butoxide (67 mg, 0.714 mmol) in anhydrous toluene (4 mL) were heated at 120 ° C. overnight. The reaction mixture was filtered through a celite pad, washed with EtOAc, and the filtrate was concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (90 mg, yield 83%).

步驟2. 標題化合物：自步驟1中所獲得之化合物(90 mg，0.2 mmol)開始且遵循通用保護基脫除方法2，獲得標題化合物(48 mg，產率68%)。Step 2. The title compound: Starting from the compound (90 mg, 0.2 mmol) obtained in Step 1 and following the general protecting group removal method 2, the title compound (48 mg, yield 68%) was obtained.

HPLC滯留時間(方法B): 4.44 min; MS: 353.1 (M+H)。HPLC residence time (Method B): 4.44 min; MS: 353.1 (M + H).

此方法用於使用適合之起始物質來製備實例2-7：
This method was used to prepare Examples 2-7 using suitable starting materials:

實例8：N -甲基-3-苯基-3-(2-(4,5,6,7-四氫噻吩并[3,2-c ]吡啶-2-基)苯氧基)丙-1-胺
Example 8: N -methyl-3-phenyl-3- (2- (4,5,6,7-tetrahydrothieno [3,2- c ] pyridin-2-yl) phenoxy) propane- 1-amine

步驟1. 2-(4,4,5,5-四甲基-1,3,2-二氧㖦硼戊環-2-基)-6,7-二氫噻吩并[3,2-c ]吡啶-5(4H )-甲酸第三丁酯：在N2 氛圍下，向在-78℃下冷卻的2-溴-6,7-二氫噻吩并[3,2-c ]吡啶-5(4H )-甲酸第三丁酯(0.3 g，0.943 mmol) 於無水THF (7 mL)中之溶液中逐滴添加丁基鋰(於己烷中之1.6 M溶液，0.71 mL，1.31 mmol)，且將混合物在-78℃下攪拌30分鐘。隨後，逐滴添加2-異丙氧基-4,4,5,5-四甲基-1,3,2-二氧㖦硼戊環(0.29 mL，1.41 mmol)於無水THF (2 mL)中之溶液。將反應混合物在-78℃下攪拌20分鐘，隨後使其逐漸升溫至室溫。添加NH4 Cl飽和溶液，且用EtOAc萃取混合物。用鹽水洗滌經合併之有機萃取物，經MgSO4 乾燥，且濃縮至乾燥。藉由急驟層析，矽膠，梯度CH至EtOAc來純化粗產物，得到標題化合物(78 mg，產率22%)。Step 1. 2- (4,4,5,5-tetramethyl-1,3,2-dioxoboropentyl-2-yl) -6,7-dihydrothieno [3,2- c ] Pyridine-5 ( 4H ) -tert-butyl formate: 2 -Bromo-6,7-dihydrothieno [3,2- c ] pyridine- To a solution of 5 (4 H ) -tert-butyl formate (0.3 g, 0.943 mmol) in anhydrous THF (7 mL) was added dropwise butyllithium (1.6 M solution in hexane, 0.71 mL, 1.31 mmol). ), And the mixture was stirred at -78 ° C for 30 minutes. Subsequently, 2-isopropoxy-4,4,5,5-tetramethyl-1,3,2-dioxoboropentane (0.29 mL, 1.41 mmol) was added dropwise to anhydrous THF (2 mL). In solution. The reaction mixture was stirred at -78 ° C for 20 minutes, and then allowed to gradually warm to room temperature. A saturated solution of NH 4 Cl was added, and the mixture was extracted with EtOAc. , Washed with brine and dried the combined organic extracts were dried over MgSO 4, and concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (78 mg, 22% yield).

步驟2. 2-(2-(3-((第三丁氧基羰基)(甲基)胺基)-1-苯基丙氧基)苯基)-6,7-二氫噻吩并[3,2-c ]吡啶-5(4H )-甲酸第三丁酯：在密封管中，在氬氣氛圍下，將中間物10 (86 mg，0.205 mmol)、步驟1中所獲得之化合物(75 mg，0.205 mmol)、肆(三苯基膦)鈀(0) (24 mg，0.021 mmol)及K2 CO3 (57 mg，0.411 mmol)於二噁烷:水 (15:1，2.7 mL)之混合物中的混合物在100℃下加熱隔夜。經由矽藻土墊過濾反應混合物，用EtOAc洗滌，且將濾液濃縮至乾燥。藉由急驟層析，矽膠，梯度CH至EtOAc來純化粗產物，得到標題化合物(44 mg，產率37%)。Step 2. 2- (2- (3-((Third butoxycarbonyl) (methyl) amino) -1-phenylpropoxy) phenyl) -6,7-dihydrothieno [3 , 2- c ] pyridine-5 ( 4H ) -formic acid third butyl ester: In a sealed tube, under an argon atmosphere, the intermediate 10 (86 mg, 0.205 mmol), the compound obtained in step 1 ( 75 mg, 0.205 mmol), (triphenylphosphine) palladium (0) (24 mg, 0.021 mmol), and K 2 CO 3 (57 mg, 0.411 mmol) in dioxane: water (15: 1, 2.7 mL The mixture in) was heated at 100 ° C overnight. The reaction mixture was filtered through a celite pad, washed with EtOAc, and the filtrate was concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (44 mg, yield 37%).

步驟3. 標題化合物：自步驟2中所獲得之化合物(44 mg，0.076 mmol)開始且遵循通用保護基脫除方法2，獲得標題化合物(12 mg，產率42%)。Step 3. The title compound: Starting from the compound (44 mg, 0.076 mmol) obtained in step 2 and following the general protecting group removal method 2, the title compound (12 mg, yield 42%) was obtained.

HPLC滯留時間(方法B): 3.53 min; MS: 379.1 (M+H)。HPLC retention time (Method B): 3.53 min; MS: 379.1 (M + H).

實例9.N -(2-(3-(甲胺基)-1-(噻吩-2-基)丙氧基)苯基)-2-苯基乙醯胺
Example 9. N- (2- (3- (methylamino) -1- (thien-2-yl) propoxy) phenyl) -2-phenylacetamidamine

步驟1. 甲基(3-(2-(2-苯基乙醯胺基)苯氧基)-3-(噻吩-2-基)丙基)胺基甲酸2-(三甲基矽烷基)乙酯：在密封管中，在氬氣氛圍下，將中間物4 (150 mg，0.319 mmol)、2-苯基乙醯胺(56 mg，0.414 mmol)、N 1 ,N 2 -二甲基乙烷-1,2-二胺(10 μL，0.096 mmol)、碘化銅(I) (18 mg，0.096 mmol)及磷酸鉀(135 mg，0.638 mmol)於1,4-二噁烷(4.5 mL)中之混合物在120℃下加熱隔夜。添加額外N 1 ,N 2 -二甲基乙烷-1,2-二胺(10 μL，0.096 mmol)及碘化銅(I) (18 mg，0.096 mmol)，且將反應混合物在120℃下再加熱隔夜。經由矽藻土墊對其進行過濾，用DCM洗滌，且將濾液濃縮至乾燥。藉由急驟層析，矽膠，梯度CH至EtOAc來純化殘餘物，得到標題化合物(130 mg，產率78%)。Step 1. Methyl (3- (2- (2-phenylacetamido) phenoxy) -3- (thien-2-yl) propyl) aminocarboxylic acid 2- (trimethylsilyl) Ethyl ester: In a sealed tube, under the argon atmosphere, the intermediate 4 (150 mg, 0.319 mmol), 2-phenylacetamide (56 mg, 0.414 mmol), N 1 , N 2 -dimethyl Ethane-1,2-diamine (10 μL, 0.096 mmol), copper (I) iodide (18 mg, 0.096 mmol) and potassium phosphate (135 mg, 0.638 mmol) in 1,4-dioxane (4.5 The mixture was heated at 120 ° C. overnight. Additional N 1 , N 2 -dimethylethane-1,2-diamine (10 μL, 0.096 mmol) and copper (I) iodide (18 mg, 0.096 mmol) were added and the reaction mixture was at 120 ° C Reheat overnight. It was filtered through a pad of celite, washed with DCM, and the filtrate was concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (130 mg, yield 78%).

步驟2. 標題化合物：自步驟1中所獲得之化合物(130 mg，0.248 mmol)開始且遵循通用保護基脫除方法5，獲得標題化合物(83 mg，產率88%)。Step 2. The title compound: Starting from the compound (130 mg, 0.248 mmol) obtained in step 1 and following the general protecting group removal method 5, the title compound (83 mg, yield 88%) was obtained.

HPLC滯留時間(方法B): 3.84 min; MS: 381.1 (M+H)。HPLC retention time (Method B): 3.84 min; MS: 381.1 (M + H).

此方法用於使用適合之起始物質來製備實例10-13：
This method was used to prepare Examples 10-13 using suitable starting materials:

實例14：N -甲基-3-(2-(2-(甲基(苯乙基)胺基)乙基)苯氧基)-3-(噻吩-2-基)丙-1-胺
Example 14: N -methyl-3- (2- (2- (methyl (phenethyl) amino) ethyl) phenoxy) -3- (thien-2-yl) propan-1-amine

步驟1.N -(2-(3-氯-1-(噻吩-2-基)丙氧基)苯乙基)-N -甲基-2-苯基乙胺：在N2 氛圍下，將中間物6 (250 mg，0.85 mmol)、N -甲基-2-苯基乙胺(0.12 mL，0.85 mmol)及AcOH (4.8 μL，0.085 mmol)於DCE (3.54 mL) 中之溶液攪拌2小時。隨後，添加三乙醯氧基硼氫化鈉(270 mg，1.27 mmol)，且將反應混合物在室溫下攪拌隔夜。添加NaHCO3 飽和溶液，且用DCM萃取混合物。用鹽水洗滌經合併之有機萃取物，經MgSO4 乾燥，且濃縮至乾燥。藉由急驟層析，矽膠，梯度DCM至MeOH:DCM (1:4)來純化粗產物，得到標題化合物(248 mg，產率70%)。Step 1. N- (2- (3-Chloro-1- (thien-2-yl) propoxy) phenethyl) -N -methyl-2-phenylethylamine: Under an N 2 atmosphere, A solution of intermediate 6 (250 mg, 0.85 mmol), N -methyl-2-phenylethylamine (0.12 mL, 0.85 mmol) and AcOH (4.8 μL, 0.085 mmol) in DCE (3.54 mL) was stirred for 2 hours . Subsequently, sodium triethoxylate borohydride (270 mg, 1.27 mmol) was added, and the reaction mixture was stirred at room temperature overnight. Saturated NaHCO 3 solution was added, and the mixture was extracted with DCM. , Washed with brine and dried the combined organic extracts were dried over MgSO 4, and concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient DCM to MeOH: DCM (1: 4) to give the title compound (248 mg, yield 70%).

步驟2. 標題化合物：在密封管中，將步驟1中所獲得之化合物(103 mg，0.25 mmol)及甲胺(於EtOH中之33 wt%溶液，1.6 mL，12.44 mmol)的溶液在50℃下加熱20小時。將溶劑蒸發至乾燥，將殘餘物溶解於DCM中，且用1 N NaOH對其進行洗滌，經MgSO4 乾燥，且濃縮至乾燥。藉由急驟層析，矽膠，梯度DCM至MeOH:DCM (1:4)來純化粗產物，得到標題化合物(63 mg，產率62%)。Step 2. The title compound: In a sealed tube, a solution of the compound obtained in step 1 (103 mg, 0.25 mmol) and methylamine (33 wt% solution in EtOH, 1.6 mL, 12.44 mmol) at 50 ° C. Heat for 20 hours. The solvent was evaporated to dryness, the residue was dissolved in DCM, and washed with 1 N NaOH subjected, dried over MgSO 4, and concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient DCM to MeOH: DCM (1: 4) to give the title compound (63 mg, yield 62%).

HPLC滯留時間(方法C): 5.39 min; MS: 408.9 (M+H)。HPLC residence time (Method C): 5.39 min; MS: 408.9 (M + H).

此方法用於使用適合之起始物質來製備實例15-26：

This method was used to prepare Examples 15-26 using suitable starting materials:

實例27：N -甲基-3-苯基-3-(2-(((2-(4-(吡啶-2-基)四氫-2H -哌喃-4-基)乙基)胺基)甲基)苯氧基)丙-1-胺
Example 27: N -methyl-3-phenyl-3- (2-(((2- (4- (pyridin-2-yl) tetrahydro- 2H -piperan-4-yl) ethyl) amine Yl) methyl) phenoxy) propan-1-amine

步驟1. 甲基(3-苯基-3-(2-(((2-(4-(吡啶-2-基)四氫-2H -哌喃-4-基)乙基)胺基)甲基)苯氧基)丙基)胺基甲酸第三丁酯：遵循實例14之步驟1中所描述的實驗程序，自中間物11 (100 mg，0.27 mmol)及2-(4-(吡啶-2-基)四氫-2H -哌喃-4-基)乙胺(55 mg，0.27 mmol)開始，獲得標題化合物(83 mg，產率54%)。Step 1. Methyl (3-phenyl-3- (2-(((2- (4- (pyridin-2-yl) tetrahydro- 2H -piperan-4-yl) ethyl) amino) Methyl) phenoxy) propyl) aminocarboxylic acid third butyl ester: Follow the experimental procedure described in Example 1, step 1 from intermediate 11 (100 mg, 0.27 mmol) and 2- (4- (pyridine) Starting with 2-yl) tetrahydro- 2H -piperan-4-yl) ethylamine (55 mg, 0.27 mmol), the title compound (83 mg, yield 54%) was obtained.

步驟2. 標題化合物：自步驟1中所獲得之化合物(83 mg，0.15 mmol)開始且遵循通用保護基脫除方法2，獲得標題化合物(20 mg，產率30%)。Step 2. The title compound: Starting from the compound (83 mg, 0.15 mmol) obtained in step 1 and following the general protecting group removal method 2, the title compound (20 mg, yield 30%) was obtained.

HPLC滯留時間(方法B): 3.60 min; MS: 460.3 (M+H)。HPLC retention time (Method B): 3.60 min; MS: 460.3 (M + H).

此方法用於使用適合之起始物質來製備實例28-32：
This method was used to prepare Examples 28-32 using suitable starting materials:

實例33：N -(2-(3-(甲胺基)-1-苯基丙氧基)苄基)吡啶-4-胺
Example 33: N- (2- (3- (methylamino) -1-phenylpropoxy) benzyl) pyridine-4-amine

步驟1. 甲基(3-苯基-3-(2-((吡啶-4-基胺基)甲基)苯氧基)丙基)胺基甲酸第三丁酯：將中間物11 (100 mg，0.25 mmol)及吡啶-4-胺(23 mg，0.25 mmol)於甲苯(0.8 mL)中之溶液在120℃下加熱48小時。濃縮溶劑，將殘餘物溶解於MeOH (0.8 mL)中，且添加NaBH4 (14 mg，0.374 mmol)。將混合物在室溫下攪拌4小時，且蒸發溶劑。用水及DCM稀釋粗產物，分離各相，且用DCM萃取水層。經MgSO4 乾燥經合併之有機萃取物，過濾，且濃縮至乾燥。藉由急驟層析，矽膠，梯度DCM至MeOH:DCM (1:4)來純化粗產物，得到標題化合物(31 mg，產率28%)。Step 1. Methyl (3-phenyl-3- (2-((pyridin-4-ylamino) methyl) phenoxy) propyl) carbamic acid third butyl ester: intermediate 11 (100 mg, 0.25 mmol) and a solution of pyridine-4-amine (23 mg, 0.25 mmol) in toluene (0.8 mL) was heated at 120 ° C for 48 hours. The solvent was concentrated, the residue was dissolved in MeOH (0.8 mL), and NaBH 4 (14 mg, 0.374 mmol) was added. The mixture was stirred at room temperature for 4 hours, and the solvent was evaporated. The crude product was diluted with water and DCM, the phases were separated, and the aqueous layer was extracted with DCM. Dried over MgSO 4 the organic extracts were combined, filtered, and concentrated to dryness. The crude product was purified by flash chromatography, silica gel, gradient DCM to MeOH: DCM (1: 4) to give the title compound (31 mg, yield 28%).

步驟2. 標題化合物：自步驟1中所獲得之化合物(30 mg，0.07 mmol)開始且遵循通用保護基脫除方法2，獲得標題化合物(19 mg，產率83%)。Step 2. The title compound: Starting from the compound (30 mg, 0.07 mmol) obtained in step 1 and following the general protecting group removal method 2, the title compound (19 mg, yield 83%) was obtained.

HPLC滯留時間(方法D): 10.34 min; MS: 348.2 (M+H)。HPLC residence time (Method D): 10.34 min; MS: 348.2 (M + H).

此方法用於使用適合之起始物質來製備實例34：
This method was used to prepare Example 34 using a suitable starting material:

實例35：2-(3-(甲胺基)-1-(噻吩-2-基)丙氧基)-N -苯乙基苯甲醯胺
Example 35: 2- (3- (methylamino) -1- (thien-2-yl) propoxy) -N -phenethylbenzamide

步驟1. 2-(3-氯-1-(噻吩-2-基)丙氧基)-N -苯乙基苯甲醯胺：向中間物7 (235 mg，57 wt%、0.44 mmol)及2-苯基乙胺(56 μL，0.44 mmol)於無水DMF (7 mL)中之溶液中添加DIPEA (345 μL，2.0 mmol)及HATU (201 mg，0.53 mmol)。將反應混合物在室溫下攪拌隔夜。添加NaHCO3 飽和溶液，且用EtOAc萃取混合物。用水及鹽水洗滌經合併之有機萃取物，經MgSO4 乾燥，且濃縮至乾燥。粗產物不經進一步純化即使用(188 mg，產率定量)。Step 1. 2- (3-Chloro-1- (thien-2-yl) propoxy) -N -phenethylbenzamide: to intermediate 7 (235 mg, 57 wt%, 0.44 mmol) and To a solution of 2-phenylethylamine (56 μL, 0.44 mmol) in anhydrous DMF (7 mL) was added DIPEA (345 μL, 2.0 mmol) and HATU (201 mg, 0.53 mmol). The reaction mixture was stirred at room temperature overnight. A saturated solution of NaHCO 3 was added, and the mixture was extracted with EtOAc. , Washed with water and brine and dried by the combined organic extracts were dried over MgSO 4, and concentrated to dryness. The crude product was used without further purification (188 mg, quantitative yield).

步驟2. 標題化合物：遵循實例14之步驟2中所描述的實驗程序，自步驟1中所獲得之產物(188 mg，0.44 mmol)開始，獲得標題化合物(15 mg，產率8%)。Step 2. The title compound: Following the experimental procedure described in step 2 of Example 14, starting with the product (188 mg, 0.44 mmol) obtained in step 1, the title compound (15 mg, yield 8%) was obtained.

HPLC滯留時間(方法C): 4.5 min; MS: 395.0 (M+H)。HPLC retention time (method C): 4.5 min; MS: 395.0 (M + H).

實例36：N -苄基-2-(3-(甲胺基)-1-(噻吩-2-基)丙氧基)苯甲醯胺
Example 36: N -Benzyl-2- (3- (methylamino) -1- (thien-2-yl) propoxy) benzamide

步驟1. (3-(2-(苄基胺甲醯基)苯氧基)-3-(噻吩-2-基)丙基)(甲基)胺基甲酸2-(三甲基矽烷基)乙酯：遵循實例35之步驟1中所描述的程序，自中間物9 (49 mg，0.11 mmol)及苄胺(12 μL，0.11 mmol)開始，獲得標題化合物(28 mg，產率48%)。Step 1. (3- (2- (benzylaminomethylamidino) phenoxy) -3- (thien-2-yl) propyl) (methyl) aminocarboxylic acid 2- (trimethylsilyl) Ethyl ester: Following the procedure described in step 1 of Example 35, starting with intermediate 9 (49 mg, 0.11 mmol) and benzylamine (12 μL, 0.11 mmol), the title compound (28 mg, yield 48%) was obtained .

步驟2. 標題化合物：遵循通用保護基脫除方法5，自步驟1中所獲得之化合物(28 mg，0.053 mmol)開始，獲得標題化合物(5.7 mg，產率28%)。Step 2. The title compound: Following the general protecting group removal method 5, starting from the compound (28 mg, 0.053 mmol) obtained in step 1, the title compound (5.7 mg, yield 28%) was obtained.

HPLC滯留時間(方法B): 3.74 min; MS: 381.1 (M+H)。HPLC residence time (Method B): 3.74 min; MS: 381.1 (M + H).

此方法用於使用適合之起始物質來製備實例37-50：
This method was used to prepare Examples 37-50 using suitable starting materials:

實例51：N -(2-(3-(甲胺基)-1-苯基丙氧基)苯基)-2-(噻吩-2-基)乙醯胺
Example 51: N- (2- (3- (methylamino) -1-phenylpropoxy) phenyl) -2- (thien-2-yl) acetamidamine

步驟1. 甲基(3-苯基-3-(2-(2-(噻吩-2-基)乙醯胺基)苯氧基)丙基)胺基甲酸第三丁酯：遵循實例35之步驟1中所描述的實驗程序，自中間物14 (100 mg，0.28 mmol)及2-(噻吩-2-基)乙酸(40 mg，0.28 mmol)開始，獲得標題化合物(84 mg，產率56%)。Step 1. Methyl (3-phenyl-3- (2- (2- (thien-2-yl) acetamido) phenoxy) propyl) aminocarboxylic acid third butyl ester: follow the procedure of Example 35 The experimental procedure described in step 1 starts with intermediate 14 (100 mg, 0.28 mmol) and 2- (thien-2-yl) acetic acid (40 mg, 0.28 mmol) to obtain the title compound (84 mg, yield 56 %).

步驟2. 標題化合物：遵循通用保護基脫除方法2，自步驟1中所獲得之化合物(84 mg，0.158 mmol)開始，獲得標題化合物(20 mg，產率33%)。Step 2. The title compound: Following the general protecting group removal method 2, starting from the compound (84 mg, 0.158 mmol) obtained in step 1, the title compound (20 mg, yield 33%) was obtained.

HPLC滯留時間(方法B): 3.86 min; MS: 381.1 (M+H)。HPLC retention time (Method B): 3.86 min; MS: 381.1 (M + H).

實例52：3-(苄基(甲基)胺基)-N -(2-(3-(甲胺基)-1-苯基丙氧基)苯基)丙醯胺
Example 52: 3- (benzyl (methyl) amino) - N - (2- (3- ( methylamino) -1-phenyl-propoxy) phenyl) propan Amides

步驟1. (3-(2-(3-氯丙醯胺基)苯氧基)-3-苯基丙基)(甲基)胺基甲酸第三丁酯：在N2 氛圍下，向中間物14 (200 mg，0.56 mmol)於ACN (5 mL)中之溶液中逐滴添加DIPEA (0.244 mL，1.4 mmol)及3-氯丙醯氯(64 μL，0.67 mmol)。將混合物在室溫下攪拌1小時，且濃縮至乾燥。藉由急驟層析，矽膠，梯度CH至EtOAc來純化殘餘物，得到標題化合物(167 mg，產率67%)。Step 1. (3- (2- (3-Chloropropylamido) phenoxy) -3-phenylpropyl) (methyl) aminoformic acid third butyl ester: under N 2 atmosphere, toward the middle To a solution of Compound 14 (200 mg, 0.56 mmol) in ACN (5 mL) was added DIPEA (0.244 mL, 1.4 mmol) and 3-chloropropanyl chloride (64 μL, 0.67 mmol) dropwise. The mixture was stirred at room temperature for 1 hour and concentrated to dryness. The residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (167 mg, yield 67%).

步驟2. (3-(2-(3-(苄基(甲基)胺基)丙醯胺基)苯氧基)-3-苯基丙基)(甲基)胺基甲酸第三丁酯：在密封管中，將步驟1中所獲得之產物(167 mg，0.37 mmol)及N -甲基-1-苯基甲胺(42 μL，0.33 mmol)於EtOH (1.6 mL)中之溶液在60℃下加熱隔夜。蒸發溶劑，將殘餘物溶解於EtOAc中。用1 N NaOH溶液洗滌混合物，且經MgSO4 乾燥有機相，且濃縮至乾燥。由此獲得之粗產物不經進一步純化即使用(194 mg，超重，假設產率定量)。Step 2. (3- (2- (3- (benzyl (methyl) amino) propanamido) phenoxy) -3-phenylpropyl) (meth) amino third butyl ester : In a sealed tube, the solution of the product obtained in step 1 (167 mg, 0.37 mmol) and N -methyl-1-phenylmethylamine (42 μL, 0.33 mmol) in EtOH (1.6 mL) was dissolved in Heat overnight at 60 ° C. The solvent was evaporated and the residue was dissolved in EtOAc. The mixture was washed with a 1 N NaOH solution, and the organic phase was dried over MgSO 4 and concentrated to dryness. The crude product thus obtained was used without further purification (194 mg, overweight, assuming quantitative yield).

步驟3. 標題化合物：遵循通用保護基脫除方法2，自步驟2中所獲得之化合物(70 mg，0.131 mmol)開始，獲得標題化合物(46 mg，產率82%)。Step 3. The title compound: Following the general protecting group removal method 2, starting from the compound (70 mg, 0.131 mmol) obtained in step 2, the title compound (46 mg, yield 82%) was obtained.

HPLC滯留時間(方法B): 4.58 min; MS: 432.2 (M+H)。HPLC residence time (Method B): 4.58 min; MS: 432.2 (M + H).

此方法用於使用適合之起始物質來製備實例53-55：
This method was used to prepare Examples 53-55 using suitable starting materials:

實例56. 3-(苄基(甲基)胺基)-N -甲基-N -(2-(3-(甲胺基)-1-苯基丙氧基)苯基)丙醯胺
Example 56. 3- (Benzyl (methyl) amino) -N -methyl- N- (2- (3- (methylamino) -1-phenylpropoxy) phenyl) propanilamine

步驟1. (3-(2-(3-(苄基(甲基)胺基)-N -甲基丙醯胺基)苯氧基)-3-苯基丙基)(甲基)胺基甲酸第三丁酯：在N2 氛圍下，向在0℃下冷卻的實例52之步驟2中所獲得之產物(70 mg, 0.131 mmol)於無水DMF (2 mL)中之溶液中添加NaH (於礦物油中之60%分散液，10 mg，0.26 mmol)。將反應混合物在室溫下攪拌30分鐘，隨後添加碘甲烷(8 μL，0.131 mmol)，且將其在室溫下攪拌隔夜。在0℃下添加額外NaH (於礦物油中之60%分散液，5 mg，0.13 mmol)，且將混合物在室溫下攪拌30分鐘。添加額外碘甲烷(4 μL，0.7 mmol)，且將反應物在室溫下攪拌隔夜。添加水及EtOAc，分離各相，且用EtOAc萃取水層。經MgSO4 乾燥經合併之有機萃取物，且濃縮。藉由急驟層析，矽膠，梯度CH至EtOAc來純化粗物質，得到標題化合物(45 mg，產率63%)。Step 1. (3- (2- (3- (benzyl (methyl) amino) -N -methylpropylamido) phenoxy) -3-phenylpropyl) (methyl) amino Third butyl formate: To a solution of the product obtained in Step 2 of Example 52 (70 mg, 0.131 mmol) in anhydrous DMF (2 mL) under N 2 atmosphere was added NaH ( 60% dispersion in mineral oil, 10 mg, 0.26 mmol). The reaction mixture was stirred at room temperature for 30 minutes, then methyl iodide (8 μL, 0.131 mmol) was added, and it was stirred at room temperature overnight. Additional NaH (60% dispersion in mineral oil, 5 mg, 0.13 mmol) was added at 0 ° C, and the mixture was stirred at room temperature for 30 minutes. Additional methyl iodide (4 μL, 0.7 mmol) was added and the reaction was stirred at room temperature overnight. Water and EtOAc were added, the phases were separated, and the aqueous layer was extracted with EtOAc. Dried over MgSO 4 the organic extracts were combined, and concentrated. The crude material was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (45 mg, yield 63%).

步驟2. 標題化合物：遵循通用保護基脫除方法2，自步驟1中所獲得之化合物(45 mg，0.082 mmol)開始，獲得標題化合物(11 mg，產率30%)。Step 2. The title compound: Following the general protecting group removal method 2, starting from the compound (45 mg, 0.082 mmol) obtained in step 1, the title compound (11 mg, yield 30%) was obtained.

HPLC滯留時間(方法B): 4.47 min; MS: 446.3 (M+H)。HPLC residence time (Method B): 4.47 min; MS: 446.3 (M + H).

實例57. 4-(二甲基胺基)-N -(2-(3-(甲胺基)-1-苯基丙氧基)苯基)菸鹼醯胺
Example 57. 4- (dimethylamino) - N - (2- (3- ( methylamino) -1-phenyl-propoxy) phenyl) niacinamide

步驟1. (3-(2-(4-氯菸鹼醯胺基)苯氧基)-3-苯基丙基)(甲基)胺基甲酸第三丁酯：遵循實例35之步驟1中所描述的實驗程序，自中間物14 (150 mg，0.42 mmol)及4-氯菸鹼酸(66 mg，0.42 mmol)，開始獲得標題化合物(175 mg，產率84%)。Step 1. (3- (2- (4-chloronicotinylamino) phenoxy) -3-phenylpropyl) (meth) amino third butyl ester: Follow step 1 of Example 35 The described experimental procedure started with the intermediate 14 (150 mg, 0.42 mmol) and 4-chloronicotinic acid (66 mg, 0.42 mmol) to obtain the title compound (175 mg, yield 84%).

步驟2. (3-(2-(4-(二甲基胺基)菸鹼醯胺基)苯氧基)-3-苯基丙基)(甲基)胺基甲酸第三丁酯：在密封管中，將步驟1中所獲得之產物(175 mg，0.35 mmol)及二甲基胺(於THF中之2 M溶液，1.7 mL，3.4 mmol)的混合物在70℃下加熱隔夜。用水稀釋反應混合物，且用EtOAc對其進行萃取。用鹽水洗滌經合併之有機萃取物，經MgSO4 乾燥，且濃縮。由此獲得之粗產物不經進一步純化即使用(135 mg，產率75%)。Step 2. (3- (2- (4- (dimethylamino) nicotinylamino) phenoxy) -3-phenylpropyl) (methyl) aminocarboxylic acid third butyl ester: In a sealed tube, a mixture of the product obtained in step 1 (175 mg, 0.35 mmol) and dimethylamine (2 M solution in THF, 1.7 mL, 3.4 mmol) was heated at 70 ° C. overnight. The reaction mixture was diluted with water and extracted with EtOAc. , Washed with brine and dried the combined organic extracts were dried over MgSO 4, and concentrated. The crude product thus obtained was used without further purification (135 mg, yield 75%).

步驟3. 標題化合物：遵循通用保護基脫除方法1，自步驟2中所獲得之化合物(45 mg，0.082 mmol)開始，獲得標題化合物(22 mg，產率55%)。Step 3. The title compound: Following the general protecting group removal method 1, starting from the compound (45 mg, 0.082 mmol) obtained in step 2, the title compound (22 mg, yield 55%) was obtained.

HPLC滯留時間(方法A): 3.59 min; MS: 405.2 (M+H)。HPLC retention time (Method A): 3.59 min; MS: 405.2 (M + H).

實例58.N -(2-(3-(甲胺基)-1-苯基丙氧基)苯基)苯甲醯胺
Example 58. N - (2- (3- (methylamino) -1-phenyl-propoxy) phenyl) benzoyl amine

步驟1. (3-(2-苯甲醯胺基苯氧基)-3-苯基丙基)(甲基)胺基甲酸第三丁酯：在N2 氛圍下，向中間物14 (200 mg，0.56 mmol)於THF (8 mL)中之溶液中逐滴添加DIPEA (0.147 mL，0.84 mmol)及苯甲醯氯(92 μL，0.78 mmol)，且將混合物在室溫下攪拌隔夜。將其濃縮至乾燥，且藉由急驟層析，矽膠，梯度CH至EtOAc來純化殘餘物，得到標題化合物(203 mg，產率80%)。Step 1. (3- (2-Benzamidoaminophenoxy) -3-phenylpropyl) (meth) carbamic acid third butyl ester: Under an N 2 atmosphere, to the intermediate 14 (200 To a solution of mg, 0.56 mmol) in THF (8 mL) was added DIPEA (0.147 mL, 0.84 mmol) and benzamidine chloride (92 μL, 0.78 mmol) dropwise, and the mixture was stirred at room temperature overnight. It was concentrated to dryness and the residue was purified by flash chromatography, silica gel, gradient CH to EtOAc to give the title compound (203 mg, yield 80%).

步驟2. 標題化合物：遵循通用保護基脫除方法2，自步驟1中所獲得之化合物(100 mg，0.22 mmol)開始，獲得標題化合物(35 mg，產率45%)。Step 2. The title compound: Following the general protecting group removal method 2, starting from the compound (100 mg, 0.22 mmol) obtained in step 1, the title compound (35 mg, yield 45%) was obtained.

HPLC滯留時間(方法A): 3.87 min; MS: 361.1 (M+H)。HPLC retention time (Method A): 3.87 min; MS: 361.1 (M + H).

此方法用於使用適合之起始物質來製備實例59-62：
This method was used to prepare Examples 59-62 using suitable starting materials:

實例63.N -苄基-2-(3-(甲胺基)-1-苯基丙氧基)苯胺
Example 63. N -Benzyl-2- (3- (methylamino) -1-phenylpropoxy) aniline

步驟1. (3-(2-(苄胺基)苯氧基)-3-苯基丙基)(甲基)胺基甲酸第三丁酯：遵循實例14之步驟1中所描述的實驗程序，自中間物14 (160 mg，045 mmol)及苯甲醛(48 μL，0.53 mmol)開始，獲得標題化合物(83 mg，產率41%)。Step 1. (3- (2- (benzylamino) phenoxy) -3-phenylpropyl) (meth) carbamic acid third butyl ester: Follow the experimental procedure described in step 1 of Example 14 Starting from intermediate 14 (160 mg, 045 mmol) and benzaldehyde (48 μL, 0.53 mmol), the title compound (83 mg, yield 41%) was obtained.

步驟2. 標題化合物：遵循通用保護基脫除方法2，自步驟1中所獲得之化合物(83 mg，0.18 mmol)開始，獲得標題化合物(53 mg，產率82%)。Step 2. The title compound: Following the general protecting group removal method 2, starting from the compound (83 mg, 0.18 mmol) obtained in step 1, the title compound (53 mg, yield 82%) was obtained.

HPLC滯留時間(方法A): 4.84 min; MS: 347.1 (M+H)。HPLC retention time (Method A): 4.84 min; MS: 347.1 (M + H).

此方法用於使用適合之起始物質來製備實例64-65：
This method was used to prepare Examples 64-65 using suitable starting materials:

遵循實例1之步驟1中所描述的方法，使用適合之起始物質，後接通用保護基脫除方法5，獲得實例66-68：

Following the method described in step 1 of Example 1, using a suitable starting material, and then using the protective group removal method 5 to obtain Examples 66-68:

遵循實例14之步驟1中所描述的方法，使用適合之起始物質，後接通用保護基脫除方法5，獲得實例69-76：
Following the method described in step 1 of Example 14, using a suitable starting material, and then using the protective group removal method 5 to obtain Examples 69-76:

結合於電壓閘控鈣通道之 α2 δ-1 子單元的實例之表
生物活性
藥理學研究
人類 Cav 2.2 鈣通道之 α2 δ-1 子單元的分析
將富含α2 δ-1之人類膜(2.5 µg)與15 nM放射性標記之[3H]-加巴噴丁一起在含有Hepes-KOH 10 mM之分析緩衝液，pH 7.4中進行培育。藉由添加10 µM普瑞巴林來量測NSB (非特異性結合)。在五個不同濃度下量測測試化合物之結合。在於27℃下培育60分鐘之後，在真空歧管台中藉由經由預浸在0.5%聚乙亞胺中之Multiscreen GF/C (Millipore)過濾來終止結合反應，後接用含有50 mM Tris-HCl之冰冷過濾緩衝液，pH 7.4洗滌3次。將過濾板在60℃下乾燥1小時，且向各孔中添加30 µl閃爍混合液，隨後進行放射性讀取。讀取在Trilux 1450 Microbeta放射性計數器(Perkin Elmer)中執行。 Table of examples of α 2 δ-1 subunits incorporated in voltage-gated calcium channels
Biological activity
Pharmacological research
Analysis of the α 2 δ-1 subunit of the human Ca v 2.2 calcium channel <br/> A human membrane (2.5 µg) enriched with α 2 δ-1 was added with 15 nM radiolabeled [3H] -gabapentin in Hepes -KOH 10 mM analysis buffer, pH 7.4 for incubation. NSB (non-specific binding) was measured by adding 10 µM pregabalin. Binding of test compounds was measured at five different concentrations. After incubation at 27 ° C for 60 minutes, the binding reaction was stopped in a vacuum manifold by filtering through Multiscreen GF / C (Millipore) pre-soaked in 0.5% polyethyleneimine, followed by 50 mM Tris-HCl Wash the solution three times with ice-cold filter buffer, pH 7.4. The filter plate was dried at 60 ° C for 1 hour, and 30 µl of the scintillation mixture was added to each well, followed by radioactive reading. Readings were performed in a Trilux 1450 Microbeta radioactivity counter (Perkin Elmer).

結果：
由於本發明旨在提供充當電壓閘控鈣通道之α2 δ子單元之配位體的化合物或一系列化學相關化合物，故極佳實施例為其中選擇充當電壓閘控鈣通道之α2 δ子單元之配位體的化合物及尤其以Ki 表示之結合對應於以下標度的化合物：
Ki (α2 δ-1)較佳＜ 10000 nM，更佳＜ 5000 nM，或甚至更佳＜ 500 nM。 result:
Since the present invention aims to provide a compound or a series of chemically related compounds that act as ligands for the α 2 δ subunits of a voltage-gated calcium channel, an excellent embodiment is one in which the α 2 δ molecules that are selected to function as voltage-gated calcium channels Compounds of the unit's ligands and in particular the binding represented by K i correspond to compounds of the following scale:
K i (α 2 δ-1) is preferably <10000 nM, more preferably <5000 nM, or even more preferably <500 nM.

已採用以下標度用於表示以Ki 表示的與電壓閘控鈣通道之α2 δ-1子單元的結合：
+ Ki (α2 δ-1) ＞= 5000 nM
++ 500 nM ＜= Ki (α2 δ-1) ＜5000 nM
+++ Ki (α2 δ-1) ＜500 nMThe following scales have been used to represent the binding to the α 2 δ-1 subunit of the voltage-gated calcium channel, denoted by K i :
+ K i (α 2 δ-1) ＞ = 5000 nM
++ 500 nM ＜ = K i (α 2 δ-1) ＜ 5000 nM
+++ K i (α 2 δ-1) ＜ 500 nM

在本申請案中所製備之所有化合物均展現結合於電壓閘控鈣通道之α2 δ-1子單元，詳言之，展示以下結合結果：
All the compounds prepared in this application exhibit the α 2 δ-1 subunit bound to the voltage-gated calcium channel. In detail, the following binding results are shown:

Claims (16)

一種通式(I)化合物， 其中 X係選自一鍵、-[C(Ra Rb )]p -、-[CH2 ]p C(O)[CH2 ]q -、-[CH2 ]p C(O)N(Rz )[CH2 ]q -、-[CH2 ]p N(Rz )C(O)[CH2 ]q -及-[CH2 ]p N(Rz )[CH2 ]q -； Ra 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基； Rb 係選自氫、鹵素、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基； 或者，Ra 及Rb 與其所連接之碳原子一起可形成經取代或未經取代之環烷基； Rz 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之烷基環烷基及-C(O)-C1-6 烷基； p為0、1、2、3、4或5； q為0、1、2、3、4或5； Y1 為-C(R10 R10 ' )-； 其中R10 及R10 ' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基； 或者，R10 及R10 ' 可與其所連接之碳原子形成經取代或未經取代之環烷基； Y2 為-C(R10 '' R10 ''' )-； 其中R10 '' 及R10 ''' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基； 或者，R10 '' 及R10 ''' 可與其所連接之碳原子形成經取代或未經取代之環烷基； n為0或1； R1 係選自-NR5 R5 ' 及-NR5 ' C(O)R5 ； R2 係選自經取代或未經取代之芳基及經取代或未經取代之雜環基， R3 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基、經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基及經取代或未經取代之烷基環烷基； R3 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基； R4 及R4 ' 獨立地選自鹵素、-R41 、-OR41 、-NO2 、-NR41 R41 ' 、-NR41 C (O)R41 ' 、-NR41 S(O)2 R41 ' 、-S(O)2 NR41 R41 ' 、-NR41 C(O)NR41 ' R41 '' 、-SR41 、-S(O)R41 、-S(O)2 R41 、-CN、鹵烷基、鹵烷氧基、-C(O)OR41 、-C(O)NR41 R41 ' 、-OCH2 CH2 OR41 、-NR41 S(O)2 NR41 ' R41 '' 及-C(CH3 )2 OR41 ； 其中R41 、R41 ' 及R41 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基； R5 係選自經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基、經取代或未經取代之環烷基、經取代或未經取代之芳基、經取代或未經取代之雜芳基、經取代或未經取代之烷基環烷基、經取代或未經取代之烷基芳基及經取代或未經取代之烷基雜芳基； R5 ' 係選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基； 其視情況呈一種立體異構體(較佳地，對映異構體或非對映異構體)之形式，外消旋體，或呈至少兩種立體異構體(較佳地，對映異構體及/或非對映異構體)以任何混合比率之混合物形式，或其對應之鹽，或其對應之溶劑合物； 進一步排除以下化合物：。A compound of general formula (I), Where X is selected from one bond,-[C (R a R b )] p -,-[CH 2 ] p C (O) [CH 2 ] q -,-[CH 2 ] p C (O) N ( R z ) [CH 2 ] q -,-[CH 2 ] p N (R z ) C (O) [CH 2 ] q -and-[CH 2 ] p N (R z ) [CH 2 ] q- ; R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl ; R b is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkyne Or R a and R b together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, Substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkane And -C (O) -C 1-6 alkyl; p is 0, 1 , 2, 3, 4 or 5; q is 0, 1, 2, 3, 4 or 5; Y 1 is -C (R 10 R 10 ' )-; wherein R 10 and R 10 ' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, Substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; or, R 10 and R 10 ′ may form a substituted or unsubstituted carbon atom to which they are attached. Cycloalkyl; Y 2 is -C (R 10 '' R 10 ''')-; wherein R 10 '' and R 10 ′''are independently selected from hydrogen, substituted or unsubstituted C 1-6 Alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; or, R 10 '' and R 10 '' may be attached to the carbon atom to which they are attached Forms a substituted or unsubstituted cycloalkyl; n is 0 or 1; R 1 is selected from -NR 5 R 5 ' and -NR 5 ' C (O) R 5 ; R 2 is selected from substituted or unsubstituted A substituted aryl group and a substituted or unsubstituted heterocyclic group, R 3 is selected from a substituted or unsubstituted C 1-6 alkyl group, a substituted or unsubstituted C 2-6 alkenyl group, Substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl, and substituted or unsubstituted alkylcycloalkyl; R 3 ′ is selected from hydrogen, substituted or unsubstituted Substituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; R 4 and R 4 ' Independently selected from halogen, -R 41 , -OR 41 , -NO 2 , -NR 41 R 41 ' , -NR 41 C (O) R 41 ' , -NR 41 S (O) 2 R 41 ' ,- S (O) 2 NR 41 R 41 ' , -NR 41 C (O) NR 41 ' R 41 '' , -SR 41 , -S (O) R 41 , -S (O) 2 R 41 , -CN, Haloalkyl, haloalkoxy, -C (O) OR 41 , -C (O) NR 41 R 41 ' , -OCH 2 CH 2 OR 41 , -NR 41 S (O) 2 NR 41 ' R 41 '' And -C (CH 3 ) 2 OR 41 ; wherein R 41 , R 41 ' and R 41 '' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; R 5 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2 -6 alkenyl and substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl , Substituted or unsubstituted alkylcycloalkyl, substituted or unsubstituted alkylaryl, and substituted or unsubstituted alkylheteroaryl; R 5 ' is selected from hydrogen, substituted or Unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2 -6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; optionally in the form of a stereoisomer (preferably, an enantiomer or a diastereomer), Racemates, or a mixture of at least two stereoisomers (preferably, enantiomers and / or diastereomers) in any mixing ratio, or their corresponding salts, or their corresponding Solvates; further exclude the following compounds: . 如請求項1之化合物，其中R2 為選自苯基及噻吩基之經取代或未經取代的基團。A compound as claimed in claim 1, wherein R 2 is a substituted or unsubstituted group selected from phenyl and thienyl. 如請求項1或2中任一項之化合物，其中該式(I)化合物為式(I')、(Ia )、(Ia ' )、(Ib )或(Ib ' )化合物， 、、、， 其中R6 及R6 ' 獨立地選自氫、鹵素、-R21 、-OR21 、-NO2 、-NR21 R21 ' 、-NR21 C(O)R21 ' 、-NR21 S(O)2 R21 ' 、-S(O)2 NR21 R21 ' 、-NR21 C(O)NR21 ' R21 '' 、-SR21 、-S(O)R21 、-S(O)2 R21 、-CN、鹵烷基、鹵烷氧基、-C(O)OR21 、-C(O)NR21 R21 ' 、-OCH2 CH2 OR21 、-NR21 S(O)2 NR21 ' R21 '' 及-C(CH3 )2 OR21 ； 其中R21 、R21 ' 及R21 '' 獨立地選自氫、經取代或未經取代之C1-6 烷基、經取代或未經取代之C2-6 烯基及經取代或未經取代之C2-6 炔基。A compound according to any one of items 1 or 2 requests compound, wherein the compound of formula (I) is of formula (I '), (I a ), (I a'), (I b) or (I b '), , , , , Wherein R 6 and R 6 ′ are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R 21 ′ , -NR 21 C (O) R 21 ′ , -NR 21 S (O) 2 R 21 ' , -S (O) 2 NR 21 R 21 ' , -NR 21 C (O) NR 21 ' R 21 '' , -SR 21 , -S (O) R 21 , -S ( O) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C (O) OR 21 , -C (O) NR 21 R 21 ' , -OCH 2 CH 2 OR 21 , -NR 21 S ( O) 2 NR 21 'R 21 '' and -C (CH 3) 2 oR 21 ; wherein R 21, R 21' and R 21 '' are independently selected from hydrogen, C of a substituted or unsubstituted 1-6 Alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl. 如請求項1至3中任一項之化合物，其中R1 為經取代或未經取代的選自以下之基團：-N(CH3)(CH2CH3)、-N(CH3)(CH2CH2OCH3)、-N(CH3)(C H2CH2-CN)、-N(CH3)(環丙基)、-NH-環己基、-NH-吡啶基、-NH-苯基、-NH-CH3-吡啶基、-NH-CH2-苯基、-NH-CH2-CH(N[CH3]2)-苯基、-NH-CH2CH2-苯基、-NH-CH2CH3、-NH-CH3、-NH-CH2-喹啉基、-NH-CH2-異喹啉基、-NH-CH2-噻吩基、-NH-CH2CH2-噻吩基、-NH-CH2-二氫茚基、-N(CH3)2、-N(CH3)(異丁基)、-N(CH3)(CH2-苯基)、-N(CH3)(CH2CH2-苯基)、-N(CH3)(CH2-噻吩基)、-NHC(O)-吡啶基、-NHC(O)-異丙基、-NHC(O)-苯基、-NHC(O)-CH2-噻吩基及-NHC(O)-CH2-苯基。The compound according to any one of claims 1 to 3, wherein R 1 is a substituted or unsubstituted group selected from -N (CH3) (CH2CH3), -N (CH3) (CH2CH2OCH3),- N (CH3) (CH2CH2-CN), -N (CH3) (cyclopropyl), -NH-cyclohexyl, -NH-pyridyl, -NH-phenyl, -NH-CH3-pyridyl, -NH -CH2-phenyl, -NH-CH2-CH (N [CH3] 2) -phenyl, -NH-CH2CH2-phenyl, -NH-CH2CH3, -NH-CH3, -NH-CH2-quinolinyl, -NH-CH2-isoquinolinyl, -NH-CH2-thienyl, -NH-CH2CH2-thienyl, -NH-CH2-dihydroindenyl, -N (CH3) 2, -N (CH3) (iso (Butyl), -N (CH3) (CH2-phenyl), -N (CH3) (CH2CH2-phenyl), -N (CH3) (CH2-thienyl), -NHC (O) -pyridyl,- NHC (O) -isopropyl, -NHC (O) -phenyl, -NHC (O) -CH2-thienyl, and -NHC (O) -CH2-phenyl. 如請求項1至3中任一項之化合物，其中R5 為經取代或未經取代的選自以下之基團：吡啶基、苯基、-CH2-吡啶基、CH2CH3、CH2CH2OCH3、CH2CH2-CN、苄基、-CH2CH(N[CH3]2)-苯基、苯乙基、乙基、甲基、異丙基、異丁基、-CH2-喹啉基、-CH2-異喹啉基、-CH2-噻吩基、-CH2CH2-噻吩基、-CH2-二氫茚基、環丙基及環己基。The compound of any one of claims 1 to 3, wherein R 5 is a substituted or unsubstituted group selected from the group consisting of pyridyl, phenyl, -CH2-pyridyl, CH2CH3, CH2CH2OCH3, CH2CH2-CN , Benzyl, -CH2CH (N [CH3] 2) -phenyl, phenethyl, ethyl, methyl, isopropyl, isobutyl, -CH2-quinolinyl, -CH2-isoquinolinyl, -CH2-thienyl, -CH2CH2-thienyl, -CH2-dihydroindenyl, cyclopropyl, and cyclohexyl. 如請求項1至5中任一項之化合物，其中X為選自以下的一鍵或經取代或未經取代之基團：鍵、-CH2-、-CH2CH2-、-C(O)-、-C(O)NH-、-C(O)NHCH2-、-C(O)NHCH2CH2-、-NHC(O)-、-NHC(O)CH2-、-NHC(O)CH2CH2-、-N(CH3)C(O)CH2CH2-、-CH2NH-、-NHCH2-、-NHCH2CH2-、-N(CH3)CH2CH2-及-CH2NHCH2-。The compound of any one of claims 1 to 5, wherein X is a single bond or a substituted or unsubstituted group selected from the group consisting of: bond, -CH2-, -CH2CH2-, -C (O)-, -C (O) NH-, -C (O) NHCH2-, -C (O) NHCH2CH2-, -NHC (O)-, -NHC (O) CH2-, -NHC (O) CH2CH2-, -N ( CH3) C (O) CH2CH2-, -CH2NH-, -NHCH2-, -NHCH2CH2-, -N (CH3) CH2CH2- and -CH2NHCH2-. 如請求項1至6中任一項之化合物，其中 p為0、1、2、3、4或5；較佳地，0、1或2。A compound according to any one of claims 1 to 6, wherein p is 0, 1, 2, 3, 4 or 5; preferably, 0, 1 or 2. 如請求項1至7中任一項之化合物，其中 q為0、1、2、3、4或5；較佳地，0、1或2。A compound as claimed in any one of claims 1 to 7, wherein q is 0, 1, 2, 3, 4 or 5; preferably, 0, 1 or 2. 如請求項1至8中任一項之化合物，其中該化合物係選自 The compound of any one of claims 1 to 8, wherein the compound is selected from 如請求項1至8中任一項之化合物，其中該化合物係選自 The compound of any one of claims 1 to 8, wherein the compound is selected from 一種選自以下之化合物， A compound selected from 一種用於製備如請求項1至10中任一項之式(I)化合物的方法， a) 其中-X為一鍵，且R1 表示-NR5 R5 ' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，該方法包含使式(IIa)化合物 其中Q表示氯、溴、碘或三氟甲磺酸酯，A表示-NR3 R3' ，且R2 、R3 、R3' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-2之胺反應， 其中R5 及R5 ' 具有如本說明書中所定義之意義； 或 b) 其中-X為一鍵，且R1 表示-NR5 ' C(O)R5 ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，該方法包含使式(IIa)化合物 其中Q表示氯、溴、碘或三氟甲磺酸酯，A表示-NR3 R3' ，且R2 、R3 、R3' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-3之胺反應， 其中R5 及R5 ' 具有如本說明書中所定義之意義； 或 c) 其中-X-R1 表示-[CH2 ]p -NR5 R5' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 及n及p具有如本說明書中所定義之意義，該方法包含使式(IIb)化合物 其中r為1、2、3或4，A表示-NR3 R3' ，且R2 、R3 、R3' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-2之胺反應， 其中R5 及R5 ' 具有如本說明書中所定義之意義； 或 d) 其中-X-R1 表示-[CH2 ]p -NR5 R5' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 及n及p具有如本說明書中所定義之意義，該方法包含使式(IIa)化合物 其中Q表示氯、溴、碘或三氟甲磺酸酯，A表示-NR3 R3' ，且R2 、R3 、R3' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-4之有機金屬試劑反應， 其中R5 及R5 ' 及p具有如本說明書中所定義之意義，且M表示適合之有機金屬基團，較佳為硼或鋅試劑； 或 e) 其中-X為一鍵，且R1 表示-NR5 R5 ' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 及n具有如本說明書中所定義之意義，該方法包含使式(IIc)化合物 其中A表示-NR3 R3' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，與式III-5之醛在還原胺化下反應，或 與式III-6之烷基化劑在常規烷基化條件下反應， 其中R5 具有如本說明書中所定義之意義，且LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或 f) 其中-X為一鍵，且R1 表示-NR5 ' C(O)R5 ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 及n具有如本說明書中所定義之意義，該方法包含使式(Ie)化合物 其中A表示-NR3 R3' ，且R2 、R3 、R3 ' 、R4 、R4 ' 、R5 及n具有如本說明書中所定義之意義，與式III-6'之烷基化劑反應， 其中R5 ' 具有如本說明書中所定義之意義但與氫不同，且LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或 g) 其中-X為-[CH2 ]p-，且R1 表示-C(O)NR5 R5 ' ，Y1 及Y2 均表示-CH2 -，且其中R2 、R3 、R3 ' 、R4 、R4 ' 、R5 、R5 ' 及n及p具有如本說明書中所定義之意義，該方法包含使式(IId)化合物 其中A表示-NR3 R3' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n及p具有如本說明書中所定義之意義，與式III-2之胺在醯胺化條件下反應， 其中R5 ' 及R5 ' 具有如本說明書中所定義之意義； 或 h) 其中n為0，Y1 及Y2 均表示-CH2 -，且其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 及X具有如本說明書中所定義之意義，該方法包含使式(VIa)化合物 其中G為OH，且R4 、R4 ' 具有如本說明書中所定義之意義，與式VII化合物反應， 其中Z表示OH或離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯，A表示-NR3 R3' ，且R2 、R3 及R3 ' 具有如本說明書中所定義之意義； 或 J) 其中n為1，Y1 及Y2 均表示-CH2 -，且其中R1 、R2 、R3 、R3 ' 、R4 、R4 ' 及X具有如本說明書中所定義之意義，該方法包含使式(VIa)化合物 與式VII化合物反應， 其中Z表示OH，且G表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯；或者Z表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯，且G表示OH或離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯，且其中R4 、R4 ' 具有如本說明書中所定義之意義，A表示-NR3 R3' ，且R2 、R3 及R3 ' 具有如本說明書中所定義之意義。A method for preparing a compound of formula (I) as in any one of claims 1 to 10, a) where -X is a bond, and R 1 represents -NR 5 R 5 ' , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ' , R 4 , R 4 ' And n have the meanings as defined in the present specification, and the method comprises making a compound of formula (IIa) Wherein Q represents chlorine, bromine, iodine or triflate, A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3' , R 4 , R 4 ' and n have Meaning of definition, reaction with amine of formula III-2, Wherein R 5 and R 5 ' have the meanings as defined in the present specification; or b) wherein -X is a bond, and R 1 represents -NR 5 ' C (O) R 5 , and Y 1 and Y 2 both represent- CH 2- , and wherein R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ and n have the meanings as defined in the present specification, the method comprises making a compound of formula (IIa) Wherein Q represents chlorine, bromine, iodine or triflate, A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3' , R 4 , R 4 ' and n have Meaning of definition, reaction with amine of formula III-3, Wherein R 5 and R 5 ' have the meanings as defined in the present specification; or c) wherein -XR 1 represents-[CH 2 ] p -NR 5 R 5' , Y 1 and Y 2 both represent -CH 2- , And wherein R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n and p have the meanings as defined in the present specification, the method includes making a compound of formula (IIb) Where r is 1, 2, 3 or 4, and A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3' , R 4 , R 4 ' and n have the meanings as defined in the present specification, and The amine reaction of formula III-2, Wherein R 5 and R 5 ' have the meanings as defined in the present specification; or d) wherein -XR 1 represents-[CH 2 ] p -NR 5 R 5' , Y 1 and Y 2 both represent -CH 2- , And wherein R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n and p have the meanings as defined in the present specification, the method includes making a compound of formula (IIa) Wherein Q represents chlorine, bromine, iodine or triflate, A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3' , R 4 , R 4 ' and n have Meaning of definition, reaction with organometallic reagent of formula III-4, Wherein R 5 and R 5 ′ and p have the meanings as defined in the present specification, and M represents a suitable organometallic group, preferably a boron or zinc reagent; or e) wherein -X is a bond, and R 1 Represents -NR 5 R 5 ′ , Y 1 and Y 2 both represent -CH 2- , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 5 , R 5 ′ and n have Having the meaning defined in the specification, the method comprising making a compound of formula (IIc) Wherein A represents -NR 3 R 3 ' and R 2 , R 3 , R 3 ' , R 4 , R 4 ' and n have the meanings as defined in the present specification, and are reductively aminated with an aldehyde of the formula III-5 Down reaction, Or react with an alkylating agent of formula III-6 under conventional alkylating conditions, Wherein R 5 has the meaning as defined in the present specification, and LG represents a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate Or f) where -X is a bond, and R 1 represents -NR 5 ' C (O) R 5 , Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ' , R 4 , R 4 ′ , R 5 , R 5 ′ and n have the meanings as defined in the present specification, and the method comprises making a compound of formula (Ie) Wherein A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 5 and n have the meanings as defined in the present specification, and the alkane of formula III-6 ′ Basing agent reaction, Wherein R 5 ′ has the meaning as defined in the present specification but is different from hydrogen, and LG represents a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate or Fluoromethanesulfonate; or g) wherein -X is-[CH 2 ] p-, and R 1 represents -C (O) NR 5 R 5 ' , and Y 1 and Y 2 both represent -CH 2- , and wherein R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ , R 5 , R 5 ′, and n and p have the meanings as defined in the present specification, and the method comprises making a compound of formula (IId) Wherein A represents -NR 3 R 3 ' , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n and p have the meanings as defined in the present specification, and are the same as those of the amine of formula III-2. Reaction under amination conditions, Where R 5 ′ and R 5 ′ have the meanings as defined in the present specification; or h) where n is 0, Y 1 and Y 2 both represent -CH 2- , and wherein R 1 , R 2 , R 3 , R 3 ', R 4, R 4 ' and X have the meanings as defined in the present specification, the method comprising compound (VIa) compound of formula Wherein G is OH, and R 4 and R 4 ′ have the meanings as defined in the present specification, and react with a compound of formula VII, Where Z represents OH or a leaving group, such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate, and A represents -NR 3 R 3 ' , and R 2 , R 3 and R 3 ′ have the meanings as defined in this specification; or J) wherein n is 1, Y 1 and Y 2 each represent -CH 2- , and wherein R 1 , R 2 , R 3 , R 3 ′ , R 4 , R 4 ′ and X have the meanings as defined in the present specification, and the method comprises making a compound of formula (VIa) Reacting with a compound of formula VII, Where Z represents OH and G represents a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate or triflate; or Z represents a leaving group, Such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate, and G represents OH or leaving group, such as chlorine, bromine, iodine, methanesulfonic acid Ester, tosylate, nitrobenzenesulfonate, or triflate, and wherein R 4 and R 4 ' have the meanings as defined in the present specification, A represents -NR 3 R 3' , and R 2. R 3 and R 3 ′ have the meanings as defined in the present specification. 一種式(II)化合物之用途， 其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯，且Y表示適合之官能基； 或一種式(IIa)化合物之用途， 其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，Q表示氯、溴、碘或三氟甲磺酸酯，LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(IIb)化合物之用途， 其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n及r具有如本說明書中所定義之意義，LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(IIc)化合物之用途， 其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n具有如本說明書中所定義之意義，LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(IId)化合物之用途， 其中A為LG或NR3 R3 ' ，且R2 、R3 、R3 ' 、R4 、R4 ' 及n及p具有如本說明書中所定義之意義，LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(III)化合物之用途， 其中R1 具有如本說明書中所定義之意義，且W表示適合之官能基； 或一種式(III-2)化合物之用途， 其中R5 及R5 '具有如本說明書中所定義之意義； 或一種式(III-3)化合物之用途， 其中R5 及R5 '具有如本說明書中所定義之意義； 或一種式(III-4)化合物之用途， 其中p、R5 及R5 '具有如本說明書中所定義之意義，且M表示適合之有機金屬基團，較佳為硼或鋅試劑； 或一種式(III-5)化合物之用途， 其中R5 具有如本說明書中所定義之意義； 或一種式(III-6)化合物之用途， 其中R5 具有如本說明書中所定義之意義，且LG表示離去基，氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(III-6')化合物之用途， 其中R5 ' 具有如本說明書中所定義之意義，且LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(IVb)化合物之用途， IVb，其中A=LG 其中A為LG，R2 、R4 、R4 ' 、R5 、R5 '及n具有如本說明書中所定義之意義，LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(IVc)化合物之用途， 其中A為LG，R2 、R4 、R4 ' 、R5 、R5 '及n具有如本說明書中所定義之意義，LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(IVd)化合物之用途， IVd，其中A=LG 其中A為LG，R2 、R4 、R4 ' 、R5 、R5 '及n及p具有如本說明書中所定義之意義，LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(IVe)化合物之用途， IVe，其中A=LG 其中A為LG，R2 、R4 、R4 ' 、R5 及n具有如本說明書中所定義之意義，LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(IVf)化合物之用途， IVf，其中A=LG 其中A為LG，R2 、R4 、R4 ' 、R5 、R5 '及n及p具有如本說明書中所定義之意義，LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(IVg)化合物之用途， IVg，其中A=LG 其中A為LG，R1 、R2 、R4 及R4 ' 具有如本說明書中所定義之意義，LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(IVh)化合物之用途， IVh，其中A=LG 其中A為LG，R1 、R2 、R4 及R4 ' 具有如本說明書中所定義之意義，LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(V)化合物之用途， 其中R3 及R3 ' 具有如本說明書中所定義之意義； 或一種式(VI)化合物之用途， 其中G表示OH、鹵素或離去基，R1 、R4 及R4 ' 及n具有如本說明書中所定義之意義； 或一種式(VIa)化合物之用途， 其中G表示OH、鹵素或離去基，R1 、R4 及R4 ' 具有如本說明書中所定義之意義； 或一種式(VIb)化合物之用途， 其中G表示OH、鹵素或離去基，R1 、R4 及R4 ' 具有如本說明書中所定義之意義； 或一種式(VII)化合物之用途， 其中Z表示OH或離去基，A為LG或NR3 R3 ' ，R2 、R3 及R3 ' 具有如本說明書中所定義之意義，且LG表示離去基，諸如氯、溴、碘、甲磺酸酯、甲苯磺酸酯、硝基苯磺酸酯或三氟甲磺酸酯； 或一種式(VIII)化合物之用途， Y表示適合之官能基，G表示OH、鹵素或離去基，R4 及R4 ' 及n具有如本說明書中所定義之意義， 其用於製備如請求項1至10中任一項之式(I)化合物。Use of a compound of formula (II), Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n have the meanings as defined in the present specification, and LG represents a leaving group such as chlorine, bromine , Iodine, mesylate, tosylate, nitrobenzenesulfonate or triflate, and Y represents a suitable functional group; or the use of a compound of formula (IIa), Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n have the meanings as defined in the present specification, and Q represents chlorine, bromine, iodine, or trifluoro Mesylate, LG represents a leaving group such as chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate or triflate; or a compound of formula (IIb) use, Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n and r have the meanings as defined in the present specification, LG represents a leaving group such as chloro , Bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate or triflate; or the use of a compound of formula (IIc), Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n have the meanings as defined in the present specification, and LG represents a leaving group such as chlorine, bromine , Iodine, mesylate, tosylate, nitrobenzenesulfonate or triflate; or the use of a compound of formula (IId), Where A is LG or NR 3 R 3 ′ , and R 2 , R 3 , R 3 ′ , R 4 , R 4 ′, and n and p have the meanings as defined in the present specification, LG represents a leaving group such as chloro , Bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate or triflate; or the use of a compound of formula (III), Wherein R 1 has the meaning as defined in the present specification, and W represents a suitable functional group; or the use of a compound of formula (III-2), Wherein R 5 and R 5 ′ have the meanings as defined in the present specification; or the use of a compound of formula (III-3), Wherein R 5 and R 5 ′ have the meanings as defined in the present specification; or the use of a compound of formula (III-4), Wherein p, R 5 and R 5 ′ have the meanings as defined in the present specification, and M represents a suitable organometallic group, preferably a boron or zinc reagent; or the use of a compound of formula (III-5), Wherein R 5 has the meaning as defined in the present specification; or the use of a compound of formula (III-6), Wherein R 5 has the meaning as defined in the present specification, and LG represents a leaving group, chlorine, bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate, or triflate; Or the use of a compound of formula (III-6 '), Wherein R 5 ′ has the meaning as defined in the present specification, and LG represents a leaving group such as chlorine, bromine, iodine, methanesulfonate, tosylate, nitrobenzenesulfonate, or triflate An ester; or the use of a compound of formula (IVb), IVb, where A = LG, where A is LG, R 2 , R 4 , R 4 ′ , R 5 , R 5 ′, and n have the meanings as defined in this specification, and LG represents a leaving group such as chlorine, bromine, Iodine, mesylate, tosylate, nitrobenzenesulfonate or triflate; or the use of a compound of formula (IVc), Where A is LG, and R 2 , R 4 , R 4 ′ , R 5 , R 5 ′, and n have the meanings as defined in the present specification, and LG represents a leaving group such as chlorine, bromine, iodine, and mesylate , Tosylate, nitrobenzenesulfonate or triflate; or the use of a compound of formula (IVd), IVd, where A = LG, where A is LG, R 2 , R 4 , R 4 ′ , R 5 , R 5 ′, and n and p have the meanings as defined in the present specification, LG represents a leaving group such as chlorine, Bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate or triflate; or the use of a compound of formula (IVe), IVe, where A = LG, where A is LG, R 2 , R 4 , R 4 ′ , R 5 and n have the meanings as defined in this specification, and LG represents a leaving group such as chlorine, bromine, iodine, methanesulfonate Acid ester, tosylate, nitrobenzenesulfonate or triflate; or the use of a compound of formula (IVf), IVf, where A = LG, where A is LG, R 2 , R 4 , R 4 ′ , R 5 , R 5 ′, and n and p have the meanings as defined in the present specification, LG represents a leaving group such as chlorine, Bromine, iodine, mesylate, tosylate, nitrobenzenesulfonate or triflate; or the use of a compound of formula (IVg), IVg, wherein A is A = LG where LG, R 1, R 2, R 4 and R 4 'have the meanings as defined in the present specification, LG represents a leaving group such as chloro, bromo, iodo, mesylate , Tosylate, nitrobenzenesulfonate or triflate; or the use of a compound of formula (IVh), IVh, where A = LG, where A is LG, R 1 , R 2 , R 4 and R 4 ′ have the meanings as defined in the present specification, and LG represents a leaving group such as chlorine, bromine, iodine, mesylate , Tosylate, nitrobenzenesulfonate or triflate; or the use of a compound of formula (V), Wherein R 3 and R 3 ′ have the meanings as defined in the present specification; or the use of a compound of formula (VI), Wherein G represents OH, halogen or a leaving group, and R 1 , R 4 and R 4 ′ and n have the meanings as defined in the present specification; or the use of a compound of formula (VIa), Wherein G represents OH, halogen or a leaving group, and R 1 , R 4 and R 4 ′ have the meanings as defined in the present specification; or the use of a compound of formula (VIb), Wherein G represents OH, halogen or a leaving group, and R 1 , R 4 and R 4 ′ have the meanings as defined in the present specification; or the use of a compound of formula (VII), Wherein Z represents OH or a leaving group, A is LG or NR 3 R 3 ′ , R 2 , R 3 and R 3 ′ have the meanings as defined in the present specification, and LG represents a leaving group such as chlorine, bromine, Iodine, mesylate, tosylate, nitrobenzenesulfonate or triflate; or the use of a compound of formula (VIII), Y represents a suitable functional group, G represents OH, halogen, or a leaving group, and R 4 and R 4 ′ and n have the meanings as defined in the present specification, and are used to prepare any one of claims 1 to 10 Compound of formula (I). 一種醫藥組合物，其包含如請求項1至10中任一項之式(I)化合物，或其包含如請求項11之化合物，或其醫藥學上可接受之鹽，及醫藥學上可接受之載劑、佐劑或媒劑。A pharmaceutical composition comprising a compound of formula (I) as claimed in any one of claims 1 to 10, or a compound as claimed in claim 11, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable Carrier, adjuvant or vehicle. 一種如請求項1至10中任一項之式(I)化合物或如請求項11之化合物，其用作藥劑。A compound of formula (I) as claimed in any one of claims 1 to 10 or a compound as claimed in claim 11 for use as a medicament. 一種如請求項1至10中任一項之式(I)化合物或如請求項11之化合物，其用作藥劑；較佳地用作用於治療疼痛之藥劑，該疼痛尤其為中度至重度疼痛、內臟疼痛、慢性疼痛、癌症疼痛、偏頭痛、發炎性疼痛、急性疼痛或神經病性疼痛、觸摸痛(allodynia)或痛覺過敏。A compound of formula (I) according to any one of claims 1 to 10 or a compound according to claim 11 for use as a medicament; preferably as a medicament for the treatment of pain, the pain being especially moderate to severe , Visceral pain, chronic pain, cancer pain, migraine, inflammatory pain, acute or neuropathic pain, allodynia, or hyperalgesia.
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