JP2022513517A - 癌の処置又は予防において使用する為のキノリン誘導体 - Google Patents
癌の処置又は予防において使用する為のキノリン誘導体 Download PDFInfo
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
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Abstract
Description
有効量:処置される癌に対して効果をもたらす医薬化合物の量、及び/又は本明細書に記載された疾病及び状態、すなわち癌及び/又は異形成、より特には、前癌状態、初期段階の癌又は非転移性癌、の症状を予防する、軽減する、除去する、処置する又は制御することにおいて有効である本発明の化合物の量。語「有効量」は、「予防有効量」並びに「処置有効量」を包含する。語「予防有効量」は、癌及び/又は異形成、より特には前癌状態、初期段階の癌又は非転移性癌、の可能性を抑制する、予防する、減少させること、又は癌及び/又は異形成、より特には前癌状態、初期段階の癌又は非転移性癌、の遅発性発病を予防することにおいて有効である本発明の化合物の濃度を云う。同様に、語「処置有効量」は、癌及び/又は異形成、より特には前癌状態、初期段階の癌又は非転移性癌を処置する際に有効である化合物の濃度、例えば癌及び/又は異形成が発生した後に投与された場合の検査後に、腫瘍サイズにおける減少、腫瘍負荷(tumor burden)における減少、及び/又は前癌腫瘍、初期腫瘍若しくは非転移性腫瘍の腫瘍数における減少をもたらす化合物の濃度、を云う。
別々の投与、同時投与、又は薬の組み合わせの時間の経過とともに広がる投与は、組み合わせの基本的な構成要素が同時に、それぞれが別個の瞬間に、又は繰り返し若しくは異なる瞬間に、特にサイクル中、投与されることができることを意味する。該基本的な成分は、これを行う為に、それらが同時に投与される場合にのみ混合物として製剤化されることができ、そうでなければ他の投与スキームの為に別々に製剤化されることができる。
a.少なくとも1つのmiRNAの存在又は発現レベルを測定すること、ここで、該少なくとも1つのmiRNAが、上記キノリン誘導体を投与する前に該患者から予め得られた第1の生物学的サンプル中のmiRNA、及び上記キノリン誘導体を投与した後に該患者から予め得られた第2の生物学的サンプル中のmiRNAである、及び
b.上記存在又は発現レベルが、上記処置の前に得られた上記第1の生物学的サンプルと比較して、上記処置の後に得られた上記第2の生物学的サンプルにおいて調節されるかを決定すること
の工程を少なくとも含み、
ここで、上記miRNAの発現の調節された存在又はレベルが、上記キノリン誘導体の抗癌作用を示す、上記方法が本明細書において提供される。
ZはC又はNであり、
VはC又はNであり、
各Rは独立して、水素原子、ハロゲン原子、-CN、ヒドロキシル、(C1~C3)フルオロアルキル、(C1~C3)フルオロアルコキシ、(C3~C6)シクロアルキル、-NO2、-NR1R2、(C1~C4)アルコキシ、フェノキシ、-NR1-SO2-NR1R2、-NR1-SO2-R1、-NR1-C(=O)-R1、-NR1-C(=O)-NR1R2、-SO2-NR1R2、-SO3H、-O-SO2-OR3、-O-P(=O)-(OR3)(OR4)、-O-CH2-COOR3、(C1~C3)アルキルであり、ここで、該アルキルは任意的に、ヒドロキシル基、下記の式(IIa)の基
QはN又はOであり、但し、QがOである場合に、R”は存在しない、
R1及びR2の各々は独立して、水素原子又は(C1~C3)アルキルであり、
R3及びR4の各々は独立して、水素原子、Li+、Na+、K+、N+(Ra)4又はベンジルであり、
nは、1、2又は3であり、
n’は、1、2又は3であり、
各R’は独立して、水素原子、(C1~C3)アルキル、ヒドロキシル、ハロゲン原子、-NO2、-NR1R2、モルホリニル、モルホリノ、N-メチルピペラジニル、(C1~C3)フルオロアルキル、(C1~C4)アルコキシ、-O-P(=O)-(OR3)(OR4)、-CN、下記の式(IIa)の基
Aは、共有結合、酸素原子又はNHであり、
Bは、共有結合又はNHであり、
mは、1、2、3、4又は5であり、
pは、1、2又は3であり、
Ra及びRbの各々は独立して、水素原子、(C1~C5)アルキル若しくは(C3~C6)シクロアルキルであり、又は、
Ra及びRbは、それらが結合されている窒素原子と一緒になって飽和した5員又は6員の複素環を形成していてもよく、該複素環は任意的に、1以上のRaによって置換されていてもよく、但し、R’が(IIa)基又は(IIIa)基である場合、他のR’基が前記(IIa)基又は(IIIa)基と異なる場合にのみ、n’は2又は3でありうる、並びに、
R”は、水素原子、(C1~C4)アルキル、上記で定義された式(IIa)の基である。
ここで、
各Rは独立して、ハロゲン原子、(C1~C3)フルオロアルキル、(C1~C3)フルオロアルコキシ、-NR1R2、(C1~C4)アルコキシ、又は(C1~C3)アルキルであり、ここで、該アルキルは任意的に、ヒドロキシル基によって一又は二置換されていてもよい、
nは、1又は2であり、
n’は、1又は2であり、
R1及びR2の各々は独立して、水素原子又は(C1~C3)アルキルであり、
R’の各々は独立して、ハロゲン原子、(C1~C3)アルキル、ヒドロキシル、-NR1R2、モルホリニル、モルホリノ、N-メチルピペラジニル、(C1~C3)フルオロアルキル、(C1~C4)アルコキシ、又は本明細書において記載された式(IIa)若しくは式(IIIa)であり、
Aは、共有結合、酸素原子又はNHであり、
Bは、共有結合又はNHであり、
mは、1、2、3、4又は5であり、
pは、1、2又は3であり、
Ra及びRbの各々は独立して、水素原子、(C1~C5)アルキル若しくは(C3~C6)シクロアルキルであり、又は
Ra及びRbは、それらが結合されている窒素原子と一緒になって飽和した5員又は6員の複素環を形成していてもよく、ここで、該複素環は任意的に、N、O及びSから選択される追加のヘテロ原子を有していてもよく、該複素環は任意的に、1以上のRaによって置換されていてもよく、但し、R’が(IIa)基又は(IIIa)基である場合、他のR’基が該(IIa)基又は(IIIa)基と異なる場合にのみ、n’は2でありうる、及び
R”は、水素原子又は(C1~C4)アルキルである。
Rは独立して、ハロゲン原子又は、(C1~C3)フルオロアルキル基、(C1~C3)フルオロアルコキシ基、-NR1R2基、(C1~C4)アルコキシ基及び(C1~C3)アルキル基から選択される基を表し、ここで、該アルキルは任意的に、ヒドロキシル基によって、一又は二置換されていてもよい、
nは、1又は2であり、
n’は、1又は2であり、
R1及びR2は独立して、水素原子又は(C1~C3)アルキル基であり、
R’は独立して、ハロゲン原子又は、(C1~C3)アルキル基、ヒドロキシル基、-NR1R2基、モルホリニル基若しくはモルホリノ基、N-メチルピペラジニ基、(C1~C3)フルオロアルキル基及び(C1~C4)アルコキシ基から選択される基を表し、且つさらに、下記から選択されるであってもよく
Bは、共有結合又はNHであり、
mは、2、3又は4であり、
pは、1、2又は3であり、
Ra及びRbは独立して、水素原子、(C1~C5)アルキル基又は(C3~C6)シクロアルキル基を表し、又は
Ra及びRbはさらに、それらが結合されている窒素原子と一緒になって飽和した5員又は6員の複素環を形成していてもよく、ここで、該複素環は任意的に、N、O及びSから選択される追加のヘテロ原子を有していてもよく、該複素環は任意的に、1以上のRaによって置換されていてもよく、但し、R’が(IIa)基又は(IIIa)基である場合、他のR’基が該(IIa)基又は(IIIa)基と異なる場合にのみ、n’は2でありうる、
R’’は、水素原子又は(C1~C4)アルキル基である。
Rは、メチル基、メトキシ基、トリフルオロメチル基、ハロゲン原子、より特にはフッ素原子若しくは塩素原子、トリフルオロメトキシ基及びアミノ基から選択され、並びに
R’は、ハロゲン原子、より特にはフッ素原子若しくは塩素原子、又はメチル基を表し、並びに、
R’’’は、水素原子又は下記の基を表す。
各Rは独立して、水素原子、ハロゲン原子、-CN、ヒドロキシル、(C1~C3)フルオロアルキル、(C1~C3)フルオロアルコキシ、(C3~C6)シクロアルキル、-NO2、-NR1R2、(C1~C4)アルコキシ、フェノキシ、-NR1-SO2-NR1R2、-NR1-SO2-R1、-NR1-C(=O)-R1、-NR1-C(=O)-NR1R2、-SO2-NR1R2、-SO3H、-O-SO2-OR3、-O-P(=O)-(OR3)(OR4)、-O-CH2-COOR3、(C1~C3)アルキルであり、ここで、該アルキルは任意的に、ヒドロキシル基、-A-(CH2)m-B-NRaRb基(式IIa)又は-(O-CH2-CH2)p-O-Ra基(式IIIa)によって、一又は二置換されていてもよい、
R1及びR2の各々は独立して、水素原子又は(C1~C3)アルキルであり、
R3及びR4の各々は独立して、水素原子、Li+、Na+、K+、N+(Ra)4又はベンジルであり、
nは、1、2又は3であり、
各R’は独立して、水素原子、(C1~C3)アルキル、ヒドロキシル、ハロゲン原子、-NO2、-NR1R2、モルホリニル、モルホリノ、N-メチルピペラジニル、(C1~C3)フルオロアルキル、(C1~C4)アルコキシ、-O-P(=O)(OR3)(OR4)、-CN、-NH-SO2-N(CH3)2基、-A-(CH2)m-B-NRaRb基(式IIa)、又は-(O-CH2-CH2)p-O-Ra基(式IIIa)であり、
Aは、共有結合、酸素原子又はNHであり、
Bは、共有結合又はNHであり、
mは、1、2、3、4又は5であり、
pは、1、2又は3であり、
Ra及びRbの各々は独立して、水素原子、(C1~C5)アルキル若しくは(C3~C6)シクロアルキルであり、又は
Ra及びRbは、それらが結合されている窒素原子と一緒になって飽和した5員又は6員の複素環を形成していてもよく、ここで、該複素環は任意的に、N、O及びSから選択される追加のヘテロ原子を有していてもよく、該複素環は任意的に、1以上のRaによって置換されていてもよい、並びに、
R”は、水素原子、(C1~C4)アルキル、又は-A-(CH2)m-B-NRaRb基(式IIa)である。
ここで、
Rは独立して、ハロゲン原子又は、(C1~C3)フルオロアルコキシ基、-NR1R2基、(C1~C4)アルコキシ基、-O-P(=O)(OR3)(OR4)基、(C1~C3)アルキル基、NO2基、-A-(CH2)m-B-NRaRb基(式IIa)、及び-(O-CH2-CH2)p-O-Ra基(式IIIa)から選択される基を表し、
nは、1又は2であり、
R’は、水素原子、ハロゲン原子又は、-NR1R2基、-O-P(=O)(OR3)(OR4)基、-NH-SO2-N(CH3)2基、及び-A-(CH2)m-B-NRaRb基(IIa)から選択される基を表し、
R’’は、水素原子、(C1~C4)アルキル基、又は-A-(CH2)m-B-NRaRb基(式IIa)であり、
R1及びR2は独立して、水素原子又は(C1~C3)アルキル基であり、
R3及びR4は独立して、水素原子、Li+、Na+、K+、N+(Ra)4又はベンジルであり、
Aは、共有結合、酸素原子又はNHであり、
Bは共有結合であり、
mは、2、3又は4であり、
pは、1、2又は3であり、
Ra及びRb独立して、水素原子又は(C1~C5)アルキル基を表し、又は、
Ra及びRbはさらに、それらが結合されている窒素原子と一緒になって飽和した5員又は6員の複素環を形成していてもよく、ここで、該複素環は任意的に、N、O及びSから選択される追加のヘテロ原子を有していてもよく、該複素環は任意的に、1以上のRaによって置換されていてもよい。
ここで、
Rは独立して、F、Cl、-NH2、-N(CH3)2、-OCH3、-O-(CH2)3-CH3、-OCF3、-CH3、-O-(CH2)2-OH、-O-(CH2)2-O-(CH2)2-OCH3、-NO2基、-O-P(=O)(OH)(OH)基、-O-(CH2)2-モルホリノ基、又は-O-(CH2)2-ピペリジノ基を表し、
nは、1又は2であり、
R’は、水素原子、Cl、-CH2-CH2-CH3、-O-(CH2)2-モルホリノ基、-O-(CH2)2-ピペリジノ基、-O-(CH2)3-ピペリジノ基、-N-CH2)3-モルホリノ基、-NH-SO2-N(CH3)2基、NH2、又は-O-P(=O)(OH)(OH)基を表し、
R’’は、水素原子、-CH3、-(CH2)3-ピペリジノ基、-(CH2)2-モルホリノ基、-(CH2)4-モルホリノ基、又は-(CH2)2-ピロリジノ基である。
ここで、
Rは(C1~C3)フルオロアルコキシ基であり、
nは1であり、並びに
R’及びR’’は、本明細書において定義された通りである。
ここで、
Rは(C1~C3)フルオロアルコキシ基であり、
nは1であり、
R’は水素原子を表し、並びに
R’’は水素原子である。
ここで、
R’はを表し、並びに
R、n及びR’’は、本明細書において定義された通りである。
ここで、上記化合物が、化合物96、98、108、109、111、115、122、125、128、129、130、132、133、135、138~141、143、及び145~164のうちから選択される。
ここで、上記化合物が、8-クロロ-N-(4-(トリフルオロメトキシ)フェニル)キノリン-2-アミン(化合物111)である。
- 「ハロゲン原子」は、塩素原子、フッ素原子、臭素原子又はヨウ素原子を意味し、特に塩素原子、フッ素原子又は臭素原子、を示すと理解される、
- 「(C1~C5)アルキル」はそれぞれ、本明細書において使用される場合に、C1~C5の直鎖、第2級又は第3級の飽和炭化水素を云う。例が、メチル、エチル、1-プロピル、2-プロピル、ブチル、ペンチルであるがこれらに限定されるものでない、
- 「(C3~C6)シクロアルキル」はそれぞれ、本明細書において使用される場合に、環状飽和炭化水素を云う。例が、シクロプロピル、シクロブチル、シクロペンチル、シクロヘキシルであるがこれらに限定されるものでない、
- 「(C1~C4)アルコキシ」はそれぞれ、本明細書において使用される場合に、O-(C1~C4)アルキル残基を云い、ここで、アルキルは上記に定義された通りである。例が、メトキシ、エトキシ、1-プロポキシ、2-プロポキシ、ブトキシであるがこれらに限定されるものでない、
- 「フルオロアルキル基」及び「フルオロアルコキシ基」はそれぞれ、上記に定義された通りのアルキル基及びアルコキシ基を云い、ここで、該基は少なくとも1つのフッ素原子によって置換されている。例が、ペルフルオロアルキル基、例えばトリフルオロメチル又はペルフルオロプロピル、である、
- 「飽和5員又は6員の複素環」はそれぞれ、本明細書において使用される場合に、少なくとも1つのヘテロ原子を含む飽和環を云う。例が、モルホリン、ピペラジン、チオモルホリン、ピペリジン、及びピロリジンであるがこれらに限定されるものでない。
小リンパ球性リンパ腫、非ホジキンリンパ腫、無痛性非ホジキンリンパ腫(iNHL:indolent non-Hodgkin's lymphoma)、難治性iNHL、外套細胞リンパ腫、濾胞性リンパ腫、リンパ形質細胞性リンパ腫、辺縁帯リンパ腫、免疫芽球性大細胞リンパ腫、リンパ芽球性リンパ腫、脾臓辺縁帯B細胞リンパ腫(+/-絨毛リンパ球)、リンパ節辺縁帯リンパ腫(+/-単球様B細胞)、粘膜に関連付けられたリンパ組織型の節外辺縁帯B細胞リンパ腫、皮膚T-細胞リンパ腫、結節外T細胞リンパ腫、未分化大細胞リンパ腫、血管免疫芽球性T細胞リンパ腫、菌状息肉症、B細胞リンパ腫、びまん性大細胞型B細胞リンパ腫、縦隔大細胞型B細胞リンパ腫、血管内大細胞型B細胞リンパ腫、原発性滲出液リンパ腫、小非切断細胞リンパ腫、バーキットリンパ腫、多発性骨髄腫、形質細胞腫、急性リンパ性白血病、T細胞急性リンパ性白血病、B細胞急性リンパ性白血病、B細胞前リンパ球性白血病、急性骨髄性白血病、慢性リンパ性白血病、若年性骨髄単球性白血病、微小残存病変、ヘアリーセル白血病、原発性骨髄線維症、続発性骨髄線維症、慢性骨髄性白血病、骨髄異形成症候群、骨髄増殖性疾患、又はワルデンストレーム高ガンマグロブリン血症。
ここで、該患者は臨床的に検出可能な転移を示さず、特に該患者は前癌状態、初期段階の癌、又は非転移性癌を有し、又は
ここで、該患者は臨床的に検出可能な転移を示し、及び式(Ib’)又は式(IVb’)の上記化合物は転移の侵入を直接的に標的としない。
ここで、該患者は臨床的に検出可能な転移を示し、及びABX464、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは下記式の上記化合物は転移の侵入を直接的に標的としない。
Tは、元の(原発性)腫瘍のサイズと、それが近くの組織に浸潤しているかどうかを示し、
Nは、関与している近くの(局所的な)リンパ節を表し、
Mは、遠隔転移(体のある部分から別の部分への癌の広がり)を表す。
本発明はさらに、癌又は異形成を予防及び/又は処置する為の方法であって、宿主に、上記で定義された化合物又はその医薬的に許容される塩の有効量を、10~1000mg、特に25~800mg、又はより特には30~600mg、例えば30~200mg、の投与量で、投与することの工程を含む上記方法に関する。
-アンドロゲン受容体阻害剤、例えばエンザルタミド(Xtandi(商標),Astellas/Medivation)、アビラテロン(Zytiga(商標),Centocor/Ortho)、ゴナドトロピン放出ホルモン(GnRH)受容体のアンタゴニスト、例えばデガレリクス(degaralix)(Firmagon(商標),Ferring Pharmaceuticals);
-抗アポトーシス薬、例えばベネトクラクス(Venclexta(商標),AbbVie/Genentech)、ブリナツモマブ(Blincyto(商標),Amgen)、ナビトクラックス(ABT-263,Abbott);
-抗増殖剤及び有糸分裂阻害剤、例えばビンカアルカロイド(それは、ビンブラスチン、ビンクリスチンを包含する);
-抗生物質、例えばダクチノマイシン、ダウノルビシン、ドキソルビシン、イダルビシン、アントラサイクリン、ミトキサントロン、ブレオマイシン、プリカマイシン(ミトラマイシン)、及びマイトマイシン;
-L-アスパラギナーゼ;
-抗血小板薬;
-抗増殖剤/有糸分裂阻害アルキル化剤、例えばナイトロジェンマスタード、シクロホスファミド及びその類似体(それは、メルファラン、クロラムブシル、ヘキサメチルメラミン、及びチオテパを包含する)、アルキルニトロソ尿素(それは、カルムスチンを包含する)及びその類似体、ストレプトゾシン、及びトリアゼン(それは、ダカルバジンを包含する);
-抗増殖剤/抗有糸分裂代謝拮抗剤、例えば葉酸類似体(それは、メトトレキサートを包含する)、アロマターゼ阻害剤;抗エストロゲン;トポイソメラーゼI阻害剤;トポイソメラーゼII阻害剤;微小管活性化合物;アルキル化剤化合物;ヒストンデアセチラーゼ阻害剤;細胞分化プロセスを誘発する化合物;シクロオキシゲナーゼ阻害剤;MMP阻害剤;mTOR阻害剤;抗悪性腫瘍性代謝拮抗剤;プラチナ化合物;タンパク質又は脂質キナーゼ活性を標的とする/減少させる化合物並びにさらに抗血管新生化合物;タンパク質又は脂質ホスファターゼの活性を標的とする、減少させる又は阻害する化合物;ゴナドレリンアゴニスト;抗アンドロゲン薬;メチオニンアミノペプチダーゼ阻害剤;マトリックスメタロプロテアーゼ阻害剤;ビスホスホネート;生体応答修飾物質;抗増殖抗体;ヘパラナーゼ阻害剤;Ras発癌性アイソフォームの阻害剤;テロメラーゼ阻害剤;プロテアソーム阻害剤;血液系腫瘍の処置に使用される化合物;Flt-3の活性を標的とする、減少させる又は阻害する化合物;Hsp90阻害剤、例えば17-AAG(17-アリルアミノゲルダナマイシン、NSC330507)、17-DMAG(17-ジメチルアミノエチルアミノ17-デメトキシゲルダナマイシン、NSC707545)、IPI-504、CNF1010、CNF2024、CNF1010(Conforma Therapeuticsから);テモゾロミド(Temodal(商標));キネシン紡錘体タンパク質阻害剤、例えばGlaxoSmithKlineからのSB715992若しくはSB743921、又は、CombinatoRxからのペンタミジン/クロールプロマジン;MEK阻害剤、例えばArray BioPharmaからのARRY142886、AstraZenecaからのAZd6244、PfizerからのPD181461,及びロイコボリン;
-抗遊走剤;
-血管新生阻害剤、例えばTNP-470;
-アロマターゼ阻害剤、例えばレトロゾール及びアナストロゾール(anastrozole)、エキセメスタン;
-アンジオテンシン;
-アンチセンスオリゴヌクレオチド、例えばmiR-124に向けられたアンチセンス核酸;
-抗凝血剤、例えばヘパリン、合成ヘパリン塩、及びトロンビンの他の阻害剤;
-アルギニン阻害剤、例えばAEB1102(ペグ化された組換えアルギナーゼ,Aeglea Biotherapeutics)及びCB-1158(Calithera Biosciences);
-骨吸収阻害剤、例えばデノスマブ(Xgeva(商標),Amgen)、ビスホスホネート、例えばゾレドロン酸(Zometa(商標),Novartis);
-CCケモカイン受容体4(CCR4:CC chemokine receptor 4)阻害剤、例えばモガムリズマブ(Poteligeo(商標),Kyowa Hakko Kirin,日本);
-CDK阻害剤、例えばCDK4/CDK6阻害剤、例えばパルボシクリブ(Ibrance(商標),Pfizer);リボシクリブ(Kisqali(商標),Novartis);アベマシクリブ(Ly2835219,Eli Lilly);及び、トリラシクリブ(trilaciclib)(G1T28,G1 Therapeutics);
-細胞周期阻害剤及び分化誘導剤、例えばトレチノイン;
-コルチコステロイド、例えばコルチゾン、デキサメタゾン、ヒドロコルチゾン、メチルプレドニゾロン、プレドニゾン、及びプレドニゾロン;
-DNA損傷剤、例えばアクチノマイシン、アムサクリン、ブスルファン、カルボプラチン、クロラムブシル、シスプラチン、シクロホスファミド(CYTOXAN(商標))、ダクチノマイシン、ダウノルビシン、ドキソルビシン、エピルビシン、イホスファミド、メルファラン、メクロレタミン、マイトマイシン、ミトキサントロン、ニトロソウレア、プロカルバジン、タキソール、タキソテール、テニポシド、エトポシド、及びトリエチレンチオホスホルアミド;
-血栓溶解剤、例えば組織プラスミノーゲンアクチベーター、ストレプトキナーゼ、ウロキナーゼ、アスピリン、ジピリダモール、チクロピジン、及びクロピドグレル;
-葉酸アンタゴニスト;
-FLT3受容体阻害剤、例えばエンザルタミド、アビラテロン、アパルタミド、エルロチニブ、クリゾチニブ、ニラパリブ、オラパリブ、オシメルチニブ、レゴラフェニブ、スニチニブ、レスタウルチニブ、ミドスタウリン、ギルテリチニブ、セマキシニブ、リニファニブ、ホスタマチニブ、ペキシダルチニブ、ソラフェニブ、カボザンチニブ、ポナチニブ、イロラセルチブ、パクリチニブ(pacritinib)、ファミチニブ、ペキシダルチニブ、キザルチニブ;
-グルタミナーゼ阻害剤、例えばCD-839(Calithera Biosciences);
-成長因子シグナル伝達キナーゼ阻害剤;
-成長因子阻害剤、例えば血管内皮成長因子阻害剤及び線維芽細胞成長因子阻害剤、例えばオララタマブ(Lartruvo(商標),Eli Lilly)、セツキシマブ(Erbitux(商標),Eli Lilly);ネシツムマブ(Portrazza(商標),Eli Lilly)、パニツムマブ(Vectibix(商標),Amgen);及びオシメルチニブ(活性化されたEGFRを標的とする,Tagrisso(商標),AstraZeneca);
-ヘッジホッグ経路阻害剤、例えばソニデギブ(Odomzo商標),Sun Pharmaceuticals);及びビスモデギブ(Erivedge(商標),Genentech);
-ヒストンデアセチラーゼ(HDAC:Histone deacetylase)阻害剤、例えばボリノスタット(Zolinza(商標),Merck);ロミデプシン(Istodax(商標),Celgene);パノビノスタット(Farydak(商標),Novartis);ベリノスタット(Beleodaq(商標),Spectrum Pharmaceuticals);エンチノスタット(SNDX-275、Syndax Pharmaceuticals)(NCT00866333);及びチダミド(Epidaza(商標),HBI-8000、Chipscreen Biosciences,中国);
-ホルモン及びその類似体、例えばエストロゲン、タモキシフェン、ゴセレリン、ビカルタミド、及びニルタミド);
-イソクエン酸デヒドロゲナーゼ(IDH:Isocitrate dehydrogenase)阻害剤、例えばAG120(Celgene;NCT02677922);AG221(Celgene,CT02677922;NCT02577406);BAY1436032(Bayer,NCT02746081);IDH305(Novartis,NCT02987010)
-イソフラボン、例えばゲニステイン;
-免疫抑制剤、例えばタクロリムス、シロリムス、アザチオプリン、及びミコフェノレート;
-p53サプレッサータンパク質の阻害剤、例えばALRN-6924(Aileron);
-成長因子ベータを変換する阻害剤(TGF-ベータ又はTGFβ)、例えばNIS793(Novartis)、フレソリムマブ(GC1008;Sanofi-Genzyme)、M7824(Merck KgaA-以前は、MSB0011459X);
-iNKT細胞アゴニスト、例えばABX196 5 Abivax)
-mTOR阻害剤、例えばエベロリムス(Afinitor(商標),Novartis);テムシロリムス(Torisel(商標),Pfizer);及びシロリムス(Rapamune(商標),Pfizer);
-微小管阻害薬、例えばタキサン類(それは、パクリタキセル、ドセタキセルを包含する)、ビンブラスチン、ノコダゾール、エポチロン、ビノレルビン)(NAVELBINE(商標))、及びエピポドフィロトキシン類(エトポシド、テニポシド);
-一酸化窒素ドナー;
-ヌクレオシド阻害剤、例えばトラベクテジン(グアニジンアルキル化剤,Yondelis(商標),Janssen Oncology)、メクロレタミン(アルキル化剤,Valchlor(商標),Aktelion Pharmaceuticals);ビンクリスチン(Oncovin(商標),Eli Lilly;Vincasar(商標),Teva Pharmaceuticals;Marqibo(商標),Talon Therapeutics);テモゾロミド(アルキル化剤5-(3-メチルトリアゼン-1-イル)-イミダゾール-4-カルボキサミド(MTIC)に対するプロドラッグ,Temodar(商標),Merck);シタラビン注射剤(ara-C,代謝拮抗性シチジン類似体,Pfizer);ロムスチン(アルキル化剤,CeeNU(商標),Bristol-Myers Squibb;Gleostine(商標),NextSource Biotechnology);アザシチジン(ピリミジンヌクレオシドシチジンの類似体,Vidaza(商標),Celgene);オマセタキシン・メペサクシネート(セファロタキシンエステル)(タンパク質合成阻害剤,Synribo(商標);Teva Pharmaceuticals);アスパラギナーゼErwinia chrysanthemi(アスパラギンの枯渇の為の酵素,Elspar(商標),Lundbeck;Erwinaze(商標),EUSA Pharma);エリブリンメシル酸塩(微小管阻害剤,チューブリンベースの有糸分裂阻害剤,Halaven(商標),Eisai);カバジタキセル(微小管阻害剤,チューブリンベースの有糸分裂阻害剤,Jevtana(商標),Sanofi-Aventis);カパセトリン(チミジル酸シンターゼ阻害剤,Xeloda(商標),Genentech);ベンダムスチン(二官能性メクロレタミン誘導体、鎖間DNA架橋結合を形成すると考えられている,Treanda(商標),Cephalon/Teva);イクサベピロン(エポチロンBの半合成類似体,微小管阻害剤,チューブリンベースの有糸分裂阻害剤,Ixempra(商標),Bristol-Myers Squibb);ネララビン(デオキシグアノシン類似体のプロドラッグ,ヌクレオシド代謝阻害剤,Arranon(商標),Novartis);クロラファビン(リボヌクレオチドレダクターゼ阻害剤のプロドラッグ、デオキシシチジンの競合的阻害剤,Clolar(商標),Sanofi-Aventis);及びトリフルリジン及びチピラシル(チミジンベースのヌクレオシド類似体及びチミジンホスホリラーゼ阻害剤,Lonsurf(商標),Taiho Oncology);
-PI3K阻害剤、例えばイデラリシブ(Zydelig(商標),Gilead)、アルペリシブ(BYL719,Novartis)、タセリシブ(GDC-0032,Genentech/Roche);ピクチリシブ(GDC-0941,Genentech/Roche);コパンリシブ(BAY806946,Bayer);ヅヴェリシブ(以前は、IPI-145,Infinity Pharmaceuticals);PQR309(Piqur Therapeutics,スイス);及びTGR1202(以前は、RP5230,TG Therapeutics);
-プラチナ配位錯体(例えば、シスプラチン、オキサリプラチン(oxiloplatin)、カルボプラチン、ネダプラチン、ピコプラチン、プロカルバジン、ミトタン、サトラプラチン、及びアミノグルテチミド;
-ポリADBリボースポリメラーゼ(PARP:Poly ADB ribose polymerase)阻害剤、例えば下記から選択されるもの:オラパリブ(Lynparza(商標),AstraZeneca);ルカパリブ(Rubraca(商標),Clovis Oncology);ニラパリブ(Zejula(商標),Tesaro);タラゾパリブ(MDV3800/BMN 673/LT00673,Medivation/Pfizer/Biomarin);ベリパリブ(ABT-888,AbbVie);及びBGB-290(BeiGene Inc.);
-プロテアソーム阻害剤、例えばエベロリムス(Afinitor(商標),Novartis);テムシロリムス(Torisel(商標),Pfizer);及びシロリムス(Rapamune(商標),Pfizer)、ボルテゾミブ(Bortezomib) (Velcade(商標),Takeda);カーフィルゾミブ(carfilzomib)(Kyprolis(商標),Amgen);及びイキサゾミブ(ixazomib)(Ninlaro(商標),Takeda);
-ピリミジン類似体及びプリン類似体、例えばフロクスウリジン、カペシタビン、及びシタラビン;
-受容体遮断剤、抗分泌剤、例えばブレフェルジン(breveldin);
-選択的エストロゲン受容体モジュレーター(SERM:Selective estrogen receptor modulator)、例えばラロキシフェン(Evista(商標),Eli Lilly);
-治療用抗体、例えば、下記から選択されるもの:抗TNF抗体、抗VEGF抗体、抗EGFR抗体、抗PD-1抗体、抗HER2抗体、抗CD20抗体、抗IL17抗体、and抗CTLA4抗体、抗PDL1、抗CD25、抗α4インテグリン、抗IL6R、抗C5、抗IL1、抗TPO、抗IL12/23、抗EPCAM/CD3、抗CD30、抗CD80/86、抗anthrax、抗CCR4、抗CD6、抗CD19、抗α4β7、抗IL6、抗VEGFR-2、抗SLAMF7、抗GD2、抗IL17A、抗PCSK9、抗IL5、抗CD22、抗IL4、抗PDGFRα、抗IL17RA、及び抗TcdB、並びに、例えば、下記から選択されるもの:アバゴヴォマブ(Abagovomab)、アバタセプト(Abatacept)、アブシキシマブ(Abciximab)、アビツズマブ(Abituzumab)、アブリルマブ(Abrilumab)、アクトクスマブ(Actoxumab)、アダリムマブ(Adalimumab)、アデカツマブ(Adecatumab)、アデュカヌマブ(Aducanumab)、アフリベルセプト(Aflibercept)、アフツジマブ(Afutuzymab)、アラシズマブ(Alacizumab)、アレファセプト(Alefacept)、アレムツズマブ(Alemtuzumab)、アリロクマブ(Alirocumab)、アルツモマブ(Altumomab)、アマチクスマブ(Amatixumab)、アナツモマブ(Anatumomab)、アネツマブ(Anetumab)、アニフロムマブ(Anifromumab)、アンルキンズマブ(Anrukinzumab)、アポリズマブ(Apolizumab)、アルシツモマブ(Arcitumomab)、アスクリンヴァクマブ(Ascrinvacumab)、アセリズマブ(Aselizumab)、アテゾリズマブ(Atezolizumab)、アチヌマブ(Atinumab)、アルチズマブ(Altizumab)、アトロリムマブ(Atorolimumab)、バピネウズマブ(Bapineuzumab)、バシリキシマブ(Basiliximab)、バヴィツキシマブ(Bavituximab)、ベクツモマブ(Bectumomab)、ベゲロマブ(Begelomab)、ベラタセプト(Belatacept)、ベリムマブ(Belimumab)、ベンラリズマブ(Benralizumab)、ベルチリムマブ(Bertilimumab)、ベシレソマブ(Besilesomab)、ベバシズマブ(Bevacizumab)、ベズロトクスマブ(Bezlotoxumab)、ビシロマブ(Biciromab)、ビマグルマブ(Bimagrumab)、ビメキズマブ(Bimekizumab)、ビヴァツズマブ(Bivatuzumab)、ブリナツモマブ(Blinatumomab)、ブロソズマブ(Blosozumab)、ボコシズマブ(Bococizumab)、ブレンツキシマブ(Brentuximab)、ブリアキヌマブ(Briakimumab)、ブロダルマブ(Brodalumab)、ブロルシズマブ(Brolucizumab)、ブロンチシズマブ(Bronticizumab)、カナキヌマブ(Canakinumab)、カンツズマブ(Cantuzumab)、カプラシズマブ(Caplacizumab)、カプロマブ(Capromab)、カルルマブ(Carlumab)、カツマキソマブ(Catumaxomab)、セデリズマブ(Cedelizumab)、セルトリズマブ(Certolizumab)、セツキシマブ(Cetixumab)、シタツズマブ(Citatuzumab)、シクスツムマブ(Cixutumumab)、クラザキズマブ(Clazakizumab)、クレノリキシマブ(Clenoliximab)、クリヴァツズマブ(Clivatuzumab)、コドリツズマブ(Codrituzumab)、コルツキシマブ(Coltuximab)、コナツムマブ(Conatumumab)、コンシズマブ(Concizumab)、クレネズマブ(Crenezumab)、ダセツズマブ(Dacetuzumab)、ダクリズマブ(Daclizumab)、ダロツズマブ(Dalotuzumab)、ダピロリズマブ(Dapirolizumab)、ダラツムマブ(Daratumumab)、デクトレクマブ(Dectrekumab)、デムシズマブ(Demcizumab)、デニンツズマブ(Denintuzumab)、デノスマブ(Denosumab)、デルロチクスマブ(Derlotixumab)、デツモマブ(Detumomab)、ジヌツキシマブ(Dinutuximab)、ディリダヴマブ(Diridavumab)、ドリノマブ(Dorlinomab)、ドロジツマブ(Drozitumab)、デュピルマブ(Dupilumab)、デュルヴァルマブ(Durvalumab)、デュシギツマブ(Dusigitumab)、エクロメキシマブ(Ecromeximab)、エクリズマブ(Eculizumab)、エドバコマブ(Edobacomab)、エドレコロマブ(Edrecolomab)、エファリズマブ(Efalizumab)、エフングマブ(Efungumab)、エルデルマブ(Eldelumab)、エルゲムツマブ(Elgemtumab)、エロツズマブ(Elotuzumab)、エルシリモバブ(Elsilimomab)、エマクツズマブ(Emactuzumab)、エミベツズマブ(Emibetuzumab)、エナヴァバツズマブ(Enavatuzumab)、エンフォルツマブ(Enfortumab)、エンリモマブ(Enlimomab)、エノブリツズマブ(Enoblituzumab)、エノキズマブ(Enokizumab)、エノチクマブ(Enoticumab)、エンシツキシマブ(Ensituximab)、エピツモマブ(Epitumomab)、エプラツズマブ(Epratuzomab)、エルリズマブ(Erlizumab)、エルツマキソマブ(Ertumaxomab)、エタネルセプト(Etanercept)、エタラシズマブ(Etaracizumab)、エトロリズマブ(Etrolizumab)、エヴィナクマブ(Evinacumab)、エヴォロクマブ(Evolocumab)、エキスビヴィルマブ(Exbivirumab)、ファノレソマブ(Fanolesomab)、ファラリモマブ(Faralimomab)、ファ-レツズマブ(Farletuzomab)、ファシヌマブ(Fasimumab)、フェルヴィズマブ(Felvizumab)、フェズキムマブ(Fezkimumab)、フィクラツズマブ(Ficlatuzumab)、フィギツムマブ(Figitumumab)、フィリヴマブ(Firivumab)、フランヴォツマブ(Flanvotumab)、フレチクマブ(Fletikumab)、フォントリズマブ(Fontolizumab)、フォラルマブ(Foralumab)、フォラヴィルマブ(Foravirumab)、フレソリムマブ(Fresolimumab)、フルラヌマブ(Fulramumab)、フツキシマブ(Futuximab)、ガリキシマブ(Galiximab)、ガニツマブ(Ganitumab)、ガンテネルマブ(Gantenerumab)、ガヴィリモマブ(Gavilimomab)、ゲムツズマブ(Gemtuzumab)、ゲヴォキズマブ(Gevokizumab)、ギレンツキシマブ(Girentuximab)、グレンバツムマブ(Glembatumumab)、ゴリムマブ(Golimumab)、ゴミリキシマブ(Gomiliximab)、グセルクマブ(Guselkumab)、イバリズマブ(Ibalizumab)、イブリツモマブ(Ibritumomab)、イクルクマブ(Icrucumab)、イダルシズマブ(Idarucizumab)、イゴヴォマブ(Igovomab)、イマルマブ(Imalumab)、イミシロマブ(Imciromab)、イムガツズマブ(Imgatuzumab)、インクラクマブ(Inclacumab)、インダツキシマブ(Indatuximab)、インデュサツマブ(Indusatumab)、インフリキシマブ(Infliximab)、インテツムマブ(Intetumumab)、イノリモマブ(Inolimomab)、イノツズマブ(Inotuzumab)、イピリムマブ(Ipilimumab)、イラツムマブ(Iratumumab)、イサツキシマブ(Isatuximab)、イトリズマブ(Itolizumab)、イキセキズマブ(Ixekizumab)、ケリキシマブ(Keliximab)、ラベツズマブ(Labetuzumab)、ランブロリズマブ(Lambrolizumab)、ランパリズマブ(Lampalizumab)、レブリキズマブ(Lebrikizumab)、レマレソマブ(Lemalesomab)、レンジルマブ(Lenzilumab)、レルデリムマブ(Lerdelimumab)、レクサツムマブ(Lexatumumab)、リビヴィルマブ(Libivirumab)、リファスツズマブ(Lifastuzumab)、リゲリズマブ(Ligelizumab)、リロトマブ(Lilotomab)、リンツズマブ(Lintuzumab)、リリルマブ(Lirilumab)、ロデルシズマブ(Lodelcizumab)、ロキヴェトマブ(Lokivetmab)、ロルヴォツズマブ(Lorvotuzumab)、ルカツムマブ(Lucatumumab)、ルリズマブ(Lulizumab)、ルミリキシマブ(Lumiliximab)、ルムレツズマブ(Lumretuzumab)、マパツムマブ(Mapatumumab)、マルジェツキシマブ(Margetuximab)、マスリモマブ(Maslimomab)、マヴリリムマブ(Mavrilimumab)、マツズマブ(Matuzumab)、メポリズマブ(Mepolizumab)、メテリムマブ(Metelimumab)、ミラツズマブ(Milatuzumab)、ミンレツモマブ(Minetumomab)、ミルヴェツキシマブ(Mirvetuximab)、ミツモマブ(Mitumomab)、モガムリズマブ(Mogamulizumab)、モロリムマブ(Morolimumab)、モタヴィズマブ(Motavizumab)、モキセツモマブ(Moxetumomab)、ムロモナブ-CD3(Muromonab-CD3)、ナコロマブ(Nacolomab)、ナミルマブ(Namilumab)、ナプツモマブ(Naptumomab)、ナルナツマブ(Narnatumab)、ナタリズマブ(Natalizumab)、ネバクマブ(Nebacumab)、ネシツムマブ(Necitumumab)、ネモリズマブ(Nemolizumab)、ネレリモマブ(Nerelimomab)、ネスヴァクマブ(Nesvacumab)、ニモツズマブ(Nimotuzumab)、ニヴォルマブ(Nivolumab)、ノフェツモマブ(Nofetumomab)、オビルトキサキシマブ(Obiltoxaximab)、オビヌツズマブ(Obinutuzumab)、オカラツズマブ(Ocaratuzumab)、オクレリズマブ(Ocrelizumab)、オデュリモマブ(Odulimomab)、オファツムマブ(Ofatumumab)、オララタマブ(Olaratumab)、オロキズマブ(Olokizumab)、オマリズマブ(Omalizumab)、オナルツズマブ(Onartuzumab)、オンツキシズマブ(Ontuxizumab)、オピシヌマブ(Opicinumab)、オポルツズマブ(Oportuzumab)、オレゴヴォマブ(Oregovomab)、オルチクマブ(Orticumab)、オテリキシズマブ(Otelixizumab)、オルテルツズマブ(Oltertuzumab)、オキセルマブ(Oxelumab)、オザネズマブ(Ozanezumab)、オゾラリズマブ(Ozoralizumab)、パジバキシマブ(Pagibaximab)、パリヴィズマブ(Palivizumab)、パニツムマブ(Panitumumab)、パンコマブ(Pankomab)、パノバクマブ(Panobacumab)、パルサツズマブ(Parsatuzumab)、パスコリズマブ(Pascolizumab)、パソツキシズマブ(Pasotuxizumab)、パテクリズマブ(Pateclizumab)、パトリツマブ(Patritumab)、ペムブロリズマブ(Pembrolizumab)、ペムツモマブ(Pemtumomab)、ペラキズマブ(Perakizumab)、ペルツズマブ(Pertuzumab)、ペキセリズマブ(Pexelizumab)、ピディリズマブ(Pidilizumab)、ピナツズマブ(Pinatuzumab)、ピンツモマブ(Pintumomab)、ポラツズマブ(Polatuzumab)、ポネズマブ(Ponezumab)、プリリキシマブ(Priliximab)、プリツムマブ(Pritumumab)、キリズマブ(Quilizumab)、ラコツモマブ(Racotumomab)、ラドレツマブ(Radretumab)、ラフィヴィルマブ(Rafivirumab)、ラルパンシズマブ(Ralpancizumab)、ラムシルマブ(Ramucirumab)、ラニビズマブ(Ranibizumab)、ラキシバクマブ(Raxibacumab)、レファネズマブ(Refanezumab)、レガヴィルマブ(Regavirumab)、レスリズマブ(Reslizumab)、リロナセプト(Rilonacept)、リロツムマブ(Rilotumumab)、リヌクマブ(Rinucumab)、リツキシマブ(Rituximab)、ロバツムマブ(Robatumumab)、ロレデュマブ(Roledumab)、ロモソズマブ(Romosozumab)、ロンタリズマブ(Rontalizumab)、ロヴェリズマブ(Rovelizumab)、ルプリズマブ(Ruplizumab)、サシツズマブ(Sacituzumab)、サマリズマブ(Samalizumab)、サリルマブ(Sarilumab)、サツモマブ(Satumomab)、セクキムマブ(Secukimumab)、セリバンツマブ(Seribantumab)、セトキサキシマブ(Setoxaximab)、セヴィルマブ(Sevirumab)、シブロツズマブ(Sibrotuzumab)、シファリムマブ(Sifalimumab)、シルツキシマブ(Siltuximab)、シプリズマブ(Siplizumab)、シルクマブ(Sirukumab)、ソフィツズマブ(Sofituzumab)、ソラネズマブ(Solanezumab)、ソリトマブ(Solitomab)、ソネプシズマブ(Sonepcizumab)、ソンツズマブ(Sontuzumab)、スタムルマブ(Stamulumab)、スレソマブ(Sulesomab)、スビヴィズマブ(Suvizumab)、タバルマブ(Tabalumab)、タカツズマブ(Tacatuzumab)、タドシズマブ(Tadocizumab)、タリズマブ(Talizumab)、タネズマブ(Tanezumab)、タプリツモマブ(Taplitumomab)、タレクスツマブ(Tarextumab)、テフィバズマブ(Tefibazumab)、テリモマブ・アリトクス(Telimomab aritox)、テナツモマブ(Tenatumomab)、テネリキシマブ(Teneliximab)、テプリズマブ(Teplizumab)、テシドルマブ(Tesidolumab)、TGN 1412、ティクリムマブ(Ticlimumab)、ティルドラキズマブ(Tildrakizumab)、ティガツズマブ(Tigatuzumab)、TNX-650、トシリズマブ(Tocilizumab)、トラリズマブ(Toralizumab)、トサトクスマブ(Tosatoxumab)、トシツモマブ(Tositumomab)、トヴェツマブ(Tovetumab)、トラロキヌマブ(Tralokimumab)、トラスツズマブ(Trastuzumab)、TRBS07、トレガリズマブ(Tregalizumab)、トレメリムマブ(Tremelimumab)、トレヴォグルマブ(Trevogrumab)、ツコツズマブ(Tucotuzumab)、ツヴィルマブ(Tuvirumab)、ウブリツキシマブ(Ublituximab)、ウロクプルマブ(Ulocuplumab)、ウレルマブ(Urelumab)、ウルトキサズマブ(Urtoxazumab)、ウステキヌマブ(Ustekimumab)、ヴァンドルツズマブ(Vandortuzumab)、ヴァンチクツマブ(Vantictumab)、ヴァヌシズマブ(Vanucizumab)、ヴァパリキシマブ(Vapaliximab)、ヴァルリルマブ(Varlimumab)、ヴァテリズマブ(Vatelizumab)、ヴェドリズマブ(Vedolizumab)、ヴェルツズマブ(Veltuzumab)、ヴェパリモマブ(Vepalimomab)、ヴェセンクマブ(Vesencumab)、ヴィシリズマブ(Visilizumab)、ヴォロシキシマブ(Volocixumab)、ヴォルセツズマブ(Vorsetuzumab)、ヴォツムマブ(Votumumab)、ザルツムマブ(Zalutumimab)、ザノリムマブ(Zanolimumab)、ザ
ツキシマブ(Zatuximab)、ジラリムマブ(Ziralimumab)、Ziv-アフリベルセプト(Ziv-Aflibercept)、及びゾリモマブ(Zolimomab);
-トポイソメラーゼ阻害剤、例えばドキソルビシン、ダウノルビシン、ダクチノマイシン、エニポシド、エピルビシン、エトポシド、イダルビシン、イリノテカン、ミトキサントロン、トポテカン、及びイリノテカン;
-毒素類、例えばコレラ毒素、リシン(ricin)、シュードモナス(Pseudomonas)外毒素、百日咳菌(Bordetella pertussis)アデニル酸シクラーゼ毒素、ジフテリア毒素、及びカスパーゼ活性化因子;
-キナーゼ又はVEGF阻害剤、例えばレゴラフェニブ(Stivarga(商標),Bayer);バンデタニブ(Caprelsa(商標),AstraZeneca);アキシチニブ(Inlyta(商標),Pfizer);及びレンバチニブ(Lenvima(商標),Eisai);Raf阻害剤、例えばソラフェニブ(Nexavar(商標),Bayer AG and Onyx);ダブラフェニブ(Tafinlar(商標),Novartis);及びベムラフェニブ(Zelboraf(商標),Genentech/Roche);MEK阻害剤、例えばコビメタニブ(Cotellic(商標),Exelexis/Genentech/Roche);トラメチニブ(Mekinist(商標),Novartis);Bcr-Ablチロシンキナーゼ阻害剤、例えばイマチニブ(Gleevec(商標),Novartis);ニロチニブ(Tasigna(商標),Novartis);ダサチニブ(Sprycel(商標)Bristol-Myers Squibb);ボスチニブ(Bosulif(商標),Pfizer);及びポナチニブ(Inclusig(商標),Ariad Pharmaceuticals);Her2及びEGFR阻害剤、例えばゲフィチニブ(Iressa(商標),AstraZeneca);エルロチニブ(Tarceeva(商標),Genentech/Roche/Astellas);ラパチニブ(Tykerb(商標),Novartis);アファチニブ(Gilotrif(商標),Boehringer Ingelheim);オシメルチニブ(活性化されたEGFRを標的とする、Tagrisso(商標),AstraZeneca);及びブリグチニブ(Alunbrig(商標),Ariad Pharmaceuticals);c-Met及びVEGFR2阻害剤、例えばカボザニチニブ(Cometriq(商標),Exelexis);及び多種キナーゼ阻害剤、例えばスニチニブ(Sutent(商標),Pfizer);パゾパニブ(Votrient(商標),Novartis);ALK阻害剤、例えばクリゾチニブ(Xalkori(商標),Pfizer);セリチニブ(Zykadia(商標),Novartis);及びアレクチニブ(Alecenza(商標),Genentech/Roche);ブルトンの(Bruton’s)チロシンキナーゼ阻害剤、例えばイブルチニブ(Imbruvica(商標),Pharmacyclics/Janssen);及びFlt3受容体阻害剤、例えばミドスタウリン(Rydapt(商標),Novartis)、チボザニブ(Aveo Pharmaecuticals);バタラニブ(Bayer/Novartis);ルシタニブ(Clovis Oncology);dovitinib(TKI258、Novartis);チアウアニブ(Chiauanib)(Chipscreen Biosciences);CEP-11981(Cephalon);リニファニブ(Abbott Laboratories);ネラチニブ(HKI-272,Puma Biotechnology);ラドチニブ(Supect(商標),IY5511,Il-Yang Pharmaceuticals,大韓民国);ルキソリチニブ(Jakafi(商標),Incyte Corporation);PTC299(PTC Therapeutics);CP-547,632(Pfizer);フォレチニブ(Exelexis,GlaxoSmithKline);キザルチニブ(Daiichi Sankyo)及びモテサニブ(Amgen/Takeda);
ZはC又はNであり;
VはC又はNであり;
各Rは独立して、水素原子、ハロゲン原子、-CN、ヒドロキシル、(C1~C3)フルオロアルキル、(C1~C3)フルオロアルコキシ、(C3~C6)シクロアルキル、-NO2、-NR1R2、(C1~C4)アルコキシ、フェノキシ、-NR1-SO2-NR1R2、-NR1-SO2-R1、-NR1-C(=O)-R1、-NR1-C(=O)-NR1R2、-SO2-NR1R2、-SO3H、-O-SO2-OR3、-O-P(=O)-(OR3)(OR4)、-O-CH2-COOR3、(C1~C3)アルキルであり、ここで、該アルキルは任意的に、ヒドロキシル基、下記の式(IIa)の基
QはN又はOであり、但し、QがOである場合に、R”は存在しない、
R1及びR2の各々は独立して、水素原子又は(C1~C3)アルキルであり、
R3及びR4の各々は独立して、水素原子、Li+、Na+、K+、N+(Ra)4又はベンジルであり、
nは、1、2又は3であり、
n’は、1、2又は3であり、
各R’は独立して、水素原子、(C1~C3)アルキル、ヒドロキシル、ハロゲン原子、-NO2、-NR1R2、モルホリニル、モルホリノ、N-メチルピペラジニル、(C1~C3)フルオロアルキル、(C1~C4)アルコキシ、-O-P(=O)-(OR3)(OR4)、-CN、下記の式(IIa)の基
Aは、共有結合、酸素原子又はNHであり、
Bは、共有結合又はNHであり、
mは、1、2、3、4又は5であり、
pは、1、2又は3であり、
Ra及びRbの各々は独立して、水素原子、(C1~C5)アルキル若しくは(C3~C6)シクロアルキルであり、又は
Ra及びRbは、それらが結合されている窒素原子と一緒になって飽和した5員又は6員の複素環を形成していてもよく、ここで、該複素環は任意的に、1以上のRaによって置換されていてもよく、但し、R’が(IIa)基又は(IIIa)基である場合、他のR’基が該(IIa)基又は(IIIa)基と異なる場合にのみ、n’は2又は3でありうる、並びに、
R”は、水素原子、(C1~C4)アルキル又は、上記で定義された式(IIa)の基である。
ZはC又はNであり、
VはC又はNであり、
各Rは独立して、水素原子、ハロゲン原子、-CN、ヒドロキシル、(C1~C3)フルオロアルキル、(C1~C3)フルオロアルコキシ、(C3~C6)シクロアルキル、-NO2、-NR1R2、(C1~C4)アルコキシ、フェノキシ、-NR1-SO2-NR1R2、-NR1-SO2-R1、-NR1-C(=O)-R1、-NR1-C(=O)-NR1R2、-SO2-NR1R2、-SO3H、-O-SO2-OR3、-O-P(=O)-(OR3)(OR4)、-O-CH2-COOR3、(C1~C3)アルキルであり、ここで、該アルキルは任意的に、ヒドロキシル基、又は下記の式(IIa)の基
QはN又はOであり、但し、QがOである場合に、R”は存在しない、
R1及びR2の各々は独立して、水素原子又は(C1~C3)アルキルであり、
R3及びR4の各々は独立して、水素原子、Li+、Na+、K+、N+(Ra)4又はベンジルであり、
nは、1、2又は3であり、
n’は、1、2又は3であり、
各R’は独立して、水素原子、(C1~C3)アルキル、ヒドロキシル、ハロゲン原子、-NO2、-NR1R2、モルホリニル、モルホリノ、N-メチルピペラジニル、(C1~C3)フルオロアルキル、(C1~C4)アルコキシ、-O-P(=O)-(OR3)(OR4)、-CN、下記の式(IIa)の基
Aは、共有結合、酸素原子又はNHであり、
Bは、共有結合又はNHであり、
mは、1、2、3、4又は5であり、
pは、1、2又は3であり、
Ra及びRbの各々は独立して、水素原子、(C1~C5)アルキル若しくは(C3~C6)シクロアルキルであり、又は
Ra及びRbは、それらが結合されている窒素原子と一緒になって飽和した5員又は6員の複素環を形成していてもよく、ここで、該複素環は任意的に、1以上のRaによって置換されていてもよく、但し、R’が(IIa)基又は(IIIa)基である場合、他のR’基が前記(IIa)基又は(IIIa)基と異なる場合にのみ、n’は2又は3でありうる、並びに、
R”は、水素原子、(C1~C4)アルキル又は、上記で定義された式(IIa)の基である。
・DMEM/F12 (高グルコース)(Gibco,Cat# 11320033)
・FBS (Cat# FND500,ExCell Bio)
・CellTiter-Glo(商標) 発光細胞生存率アッセイ(Luminescent Cell Viability Assay) (Cat# G7571,Promega,-20℃で保存)。
・96ウェルプレート(Cat#3610,Corning)
・DMEM/F12培地 (低グルコース): DMEM(低グルコース)(Gibco,Cat# 11885076)とF-12K(Gibco,Cat# 21127022)との1:1混合物
20mgの化合物111(ABX464とも名付けられている)が使用された(MW=338.7g/モル,純度=100%)。この化合物は室温(18~25℃)で保存され、及び溶媒はDMSOであった。
化合物26は、本発明において定義されている式(Ia)に属する化合物であり、国際公開第2010/143168号パンフレット(化合物37と名付けられている)に記載されている。
20mgの化合物26が使用された(MW=323.71g/モル,純度=100%)。この化合物は室温(18~25℃)で保存され、及び溶媒はDMSOであった。
BMRP004;CO2インキュベーター,SANYO Electric Co.,Ltd(02100400059)。
逆顕微鏡,Chongguang XDS-1B,Chongqing Guangdian Corp.(TAMIC0200)
Envision multilabel machine (TAREA0011)。
Vi-Cell XR,Beckman Coulter (TACEL0030)。
1.96ウェルプレートの各ウェルは、細胞を有する90μLの細胞懸濁物を含む。播種されるべき細胞の数は、細胞密度最適化アッセイ(Cell Density Optimization Assay)に基づいて決定される。
2.細胞を有する全ての96ウェルプレートが、5% CO2を含む37℃で一晩、インキュベーター内に置かれた。
3.ABX464を希釈し、そして10μL/ウェルのABX464を下記に示された濃度で添加する(下記のプレートマップを参照)。最終用量は、100μL/ウェルである。
4.古い培地を、示された同じ濃度でABX464を有する予め調製された新鮮な培地によって交換する。最終濃度は、100μL/ウェルである。
5.細胞が顕微鏡下で観察され、ビヒクル対照で処理した細胞が良好な状態であることを確認する。
6.50μLのCellTiter-Glo(商標)試薬を各ウェルに加える。
7.細胞溶解を促進する為に、オービタルシェーカーで2分間内容物を混合する。
8.発光シグナルを安定化させる為に、プレートを室温で10分間インキュベートする。
9.EnVisionマルチラベルリーダーマルチラベルリーダーを使用して発光を記録する。
データ分析が、GraphPad Prism 7.0を使用して行われる。
IC50を計算する為に、用量反応曲線が、シグモイド用量応答を伴う非線形回帰モデルを使用して生成される。生存率(surviving rate)の式が下記に示され、及びIC50はGraphPad Prism 7.0によって自動的に生成されるだろう。
Claims (21)
- 癌及び/又は異形成を処置及び/又は予防する使用の為の、下記の式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つ
各Rは独立して、水素原子、ハロゲン原子、-CN、ヒドロキシル、(C1~C3)フルオロアルキル、(C1~C3)フルオロアルコキシ、(C3~C6)シクロアルキル、-NO2、-NR1R2、(C1~C4)アルコキシ、フェノキシ、-NR1-SO2-NR1R2、-NR1-SO2-R1、-NR1-C(=O)-R1、-NR1-C(=O)-NR1R2、-SO2-NR1R2、-SO3H、-O-SO2-OR3、-O-P(=O)(OR3)(OR4)、-O-CH2-COOR3、(C1~C3)アルキルであり、ここで、該アルキルは任意的に、ヒドロキシル基、-A-(CH2)m-B-NRaRb基(式IIa)又は-(O-CH2-CH2)p-O-Ra基(式IIIa)によって、一又は二置換されていてもよい、
R1及びR2の各々は独立して、水素原子又は(C1~C3)アルキルであり、
R3及びR4の各々は独立して、水素原子、Li+、Na+、K+、N+(Ra)4又はベンジルであり、
nは、1、2又は3であり、
各R’は独立して、水素原子、(C1~C3)アルキル、ヒドロキシル、ハロゲン原子、-NO2、-NR1R2、モルホリニル、モルホリノ、N-メチルピペラジニル、(C1~C3)フルオロアルキル、(C1~C4)アルコキシ、-O-P(=O)(OR3)(OR4)、-CN、-NH-SO2-N(CH3)2基、-A-(CH2)m-B-NRaRb基(式IIa)又は-(O-CH2-CH2)p-O-Ra基(式IIIa)であり、
Aは、共有結合、酸素原子又はNHであり、
Bは、共有結合又はNHであり、
mは、1、2、3、4又は5であり、
pは、1、2又は3であり、
Ra及びRbの各々は独立して、水素原子、(C1~C5)アルキル若しくは(C3~C6)シクロアルキルであり、又は
Ra及びRbは、それらが結合されている窒素原子と一緒になって飽和した5員又は6員の複素環を形成していてもよく、ここで、前記複素環は任意的に、N、O及びSから選択される更なるヘテロ原子を有していてもよく、前記複素環は任意的に、1以上のRaによって置換されていてもよい、及び
R”は、水素原子、(C1~C4)アルキル又は-A-(CH2)m-B-NRaRb基(式IIa)である。 - Rは独立して、ハロゲン原子又は、(C1~C3)フルオロアルコキシ基、-NR1R2基、(C1~C4)アルコキシ基、-O-P(=O)(OR3)(OR4)基、(C1~C3)アルキル基、NO2基、-A-(CH2)m-B-NRaRb基(式IIa)及び-(O-CH2-CH2)p-O-Ra基(式IIIa)のうちから選択される基を表し、
nは、1又は2であり、
R’は、水素原子、ハロゲン原子又は、-NR1R2基、-O-P(=O)(OR3)(OR4)基、-NH-SO2-N(CH3)2基及び-A-(CH2)m-B-NRaRb基(IIa)のうちから選択される基を表し、
R’’は、水素原子、(C1~C4)アルキル基又は-A-(CH2)m-B-NRaRb基(式IIa)であり、
R1及びR2は独立して、水素原子又は(C1~C3)アルキル基であり、
R3及びR4は独立して、水素原子、Li+、Na+、K+、N+(Ra)4又はベンジルであり、
Aは、共有結合、酸素原子又はNHであり、
Bは共有結合であり、
mは、2、3又は4であり、
pは、1、2又は3であり、
Ra及びRbは独立して、水素原子又は(C1~C5)アルキル基を表し、
Ra及びRbはさらに、それらが結合されている窒素原子と一緒になって飽和した5員又は6員の複素環を形成していてもよく、ここで、前記複素環は任意的に、N、O及びSから選択される更なるヘテロ原子を有していてもよく、前記複素環は任意的に、1以上のRaによって置換されていてもよい、
請求項1に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つ。 - Rは独立して、F、Cl、-NH2、-N(CH3)2、-OCH3、-O-(CH2)3-CH3、-OCF3、-CH3、-O-(CH2)2-OH、-O-(CH2)2-O-(CH2)2-OCH3、-NO2基、-O-P(=O)(OH)(OH)基、-O-(CH2)2-モルホリノ基又は-O-(CH2)2-ピペリジノ基を表し、
nは、1又は2であり、
R’は、水素原子、Cl、-CH2-CH2-CH3、-O-(CH2)2-モルホリノ基、-O-(CH2)2-ピペリジノ基、-O-(CH2)3-ピペリジノ基、-N-(CH2)3-モルホリノ基、-NH-SO2-N(CH3)2基、NH2又は-O-P(=O)(OH)(OH)基を表し、
R’’は、水素原子、-CH3、-(CH2)3-ピペリジノ基、-(CH2)2-モルホリノ基、-(CH2)4-モルホリノ基又は-(CH2)2-ピロリジノ基である、
請求項1又は2に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つ。 - 前記化合物が8-クロロ-N-(4-(トリフルオロメトキシ)フェニル)キノリン-2-アミンである、請求項1~4のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つ。
- 前記癌が、頭頸部癌、頭頸部扁平上皮癌、頚部扁平上皮癌、大人又は子供における急性リンパ性白血病(ALL)、大人又は子供における急性骨髄性白血病(AML)、急性リンパ性白血病、副腎癌、肛門癌、星細胞腫、星状細胞腫(悪性度I、I、III又はIV)、B-又はNK/T-細胞リンパ腫、基底細胞及び扁平上皮癌、胆管癌、膀胱癌、骨癌、脳癌、大人における脳及び脊髄腫瘍、子供における脳及び脊髄腫瘍、未分化星状細胞腫、乳癌、消化器癌、女性における乳癌、若い女性における乳癌、男性における乳癌、再発乳癌、遺伝性乳癌、HER2陽性の乳癌、リンパ節転移に関連付けられた乳癌、ER-アルファー陽性の乳癌、思春期における癌、子供における癌、若年成人における癌、原発不明の癌、キャッスルマン病、子宮頸癌、子宮頸部上皮内腫瘍、胆管細胞癌、慢性リンパ性白血病(CLL)、慢性骨髄性白血病(CML)、慢性骨髄単球性白血病(CMML)、結腸直腸癌、結腸直腸腺腫、有棘細胞癌、子宮内膜癌、卵巣上皮癌、転移に関連付けられた卵巣上皮癌、食道癌(esophageal cancer)、食道の扁平上皮癌(Esophagus Squamous cell)、ユーイング肉腫、ユーイング腫瘍、リンパ性白血病(ALL)、眼癌、例えば眼内黒色腫及びリンパ腫、胆嚢癌、胃癌(gastric cancer)、消化管カルチノイド腫瘍、消化管間質腫瘍(GIST)、妊娠性絨毛性疾病、神経膠芽腫、多形神経膠芽腫(GBM)、ヘアリーセル白血病、神経膠腫、高悪性度神経膠腫、肝細胞癌、肝内胆管癌、浸潤性乳腺管癌、ホジキンリンパ腫、カポジ肉腫、腎臓癌(kidney cancer)、喉頭部及び下咽頭の癌、平滑筋肉腫、白血病、子供における白血病、肝臓癌、肺癌、カルチノイド腫瘍、リンパ腫、皮膚のリンパ腫、悪性中皮腫、外套細胞リンパ腫、髄芽腫、黒色腫皮膚癌、悪性黒色腫、髄膜腫、メルケル細胞皮膚癌、多発性骨髄腫、顎骨壊死を伴う多発性骨髄腫、骨髄異形成症候群、鼻腔及び副鼻腔の癌、上咽頭癌、再発性又は転移性上咽頭癌、神経芽細胞腫、神経膠腫、非ホジキンリンパ腫、子供における非ホジキンリンパ腫、非小細胞肺癌、ゲフィチニブ抵抗性非小細胞肺癌、口腔癌、口腔及び中咽頭の癌、骨肉腫、肺転移骨肉腫、卵巣癌(Ovarian Cancer)、膵臓癌、甲状腺癌、甲状腺乳頭癌、小児脊髄上衣腫、陰茎癌、下垂体腫瘍、下垂体腺腫、前神経腫瘍、前立腺癌、網膜芽細胞腫、横紋筋肉腫、唾液腺癌、皮膚癌、小細胞肺癌、小腸癌、軟部肉腫、舌の扁平上皮癌、胃癌(stomach cancer)、精巣癌、胸腺癌、甲状腺癌、子宮肉腫、腟癌、外陰癌、腎臓癌(renal cancer)、網膜芽細胞腫、ワルデンストレーム高ガンマグロブリン血症、及びウィルムス腫瘍から選択される、請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩。
- 前記癌又はその転移が、頭頸部扁平上皮癌、頚部扁平上皮癌、大人又は子供における急性リンパ性白血病(ALL)、大人又は子供における急性骨髄性白血病(AML)、急性リンパ性白血病、副腎癌、肛門癌、星細胞腫、星状細胞腫(悪性度I、I、III又はIV)、B-又はNK/T-細胞リンパ腫、基底細胞及び扁平上皮癌、胆管癌、骨癌、脳癌、大人における脳及び脊髄腫瘍、子供における脳及び脊髄腫瘍、未分化星状細胞腫、消化器癌、女性における乳癌、若い女性における乳癌、男性における乳癌、再発乳癌、遺伝性乳癌、HER2陽性の乳癌、リンパ節転移に関連付けられた乳癌、ER-アルファー陽性の乳癌、思春期における癌、子供における癌、若年成人における癌、原発不明の癌、キャッスルマン病、子宮頸部上皮内腫瘍、胆管細胞癌、慢性リンパ性白血病(CLL)、慢性骨髄性白血病(CML)、慢性骨髄単球性白血病(CMML)、結腸直腸腺腫、有棘細胞癌、子宮内膜癌、卵巣上皮癌、転移に関連付けられた卵巣上皮癌、食道の扁平上皮癌(Esophagus Squamous cell)、ユーイング肉腫、ユーイング腫瘍、リンパ性白血病(ALL)、眼癌、例えば眼内黒色腫及びリンパ腫、胃癌(gastric cancer)、消化管カルチノイド腫瘍、消化管間質腫瘍(GIST)、 妊娠性絨毛性疾病、神経膠芽腫、多形神経膠芽腫(GBM)、ヘアリーセル白血病、神経膠腫、高悪性度神経膠腫、肝細胞癌、肝内胆管癌、浸潤性乳腺管癌、ホジキンリンパ腫、カポジ肉腫、喉頭部及び下咽頭の癌、平滑筋肉腫、白血病、子供における白血病、カルチノイド腫瘍、リンパ腫、皮膚のリンパ腫、悪性中皮腫、外套細胞リンパ腫、髄芽腫、悪性黒色腫、髄膜腫、メルケル細胞皮膚癌、多発性骨髄腫、顎骨壊死を伴う多発性骨髄腫、骨髄異形成症候群、鼻腔及び副鼻腔の癌、上咽頭癌、再発性又は転移性上咽頭癌、神経芽細胞腫、神経膠腫、非ホジキンリンパ腫、子供における非ホジキンリンパ腫、ゲフィチニブ抵抗性非小細胞肺癌、口腔癌、口腔及び中咽頭の癌、骨肉腫、肺転移骨肉腫、甲状腺癌、甲状腺乳頭癌、小児脊髄上衣腫、陰茎癌、下垂体腫瘍、下垂体腺腫、前神経腫瘍、網膜芽細胞腫、横紋筋肉腫、唾液腺癌、皮膚癌、小細胞肺癌、小腸癌、軟部肉腫、舌の扁平上皮癌、精巣癌、胸腺癌、子宮肉腫、腟癌、外陰癌、腎臓癌(renal cancer)、網膜芽細胞腫、ワルデンストレーム高ガンマグロブリン血症、及びウィルムス腫瘍から選択される、請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩。
- 前記癌又はその転移が、頭頸部癌、頭頸部扁平上皮癌、頚部扁平上皮癌、悪性黒色腫、胃癌(stomach cancer)、乳癌、女性における乳癌、若い女性における乳癌、基底細胞及び扁平上皮癌、肝臓癌、脳癌、未分化星状細胞腫、肺癌、非小細胞肺癌、ゲフィチニブ抵抗性非小細胞肺癌、口腔癌、眼癌、胃癌(gastric cancer)、消化器癌、星細胞腫、星状細胞腫(悪性度I、I、III又はIV)、結腸直腸癌、結腸直腸腺腫、有棘細胞癌、膀胱癌、骨癌、再発乳癌、遺伝性乳癌、HER2陽性の乳癌、リンパ節転移に関連付けられた乳癌、ER-アルファー陽性の乳癌、腎臓癌(renal cancer)、子宮頸部上皮内腫瘍、胆管細胞癌、平滑筋肉腫、慢性リンパ性白血病(CLL)、慢性骨髄性白血病(CML)、慢性骨髄単球性白血病(CMML)、大人又は子供における急性骨髄性白血病(AML)、急性リンパ性白血病,B-又はNK/T-細胞リンパ腫、子宮頸癌、神経膠芽腫、多形神経膠芽腫(GBM)、ヘアリーセル白血病、神経膠腫、高悪性度神経膠腫、肝細胞癌、肝内胆管癌、浸潤性乳腺管癌、腎臓癌(kidney cancer)、子宮内膜癌、卵巣癌(ovarian cancer)、卵巣上皮癌、転移に関連付けられた卵巣上皮癌、食道癌(esophageal cancer)、食道扁平上皮癌、ユーイング肉腫、リンパ性白血病(ALL)、マントル細胞リンパ腫、髄芽腫、リンパ腫、骨髄異形成症候群、髄膜腫、多発性骨髄腫(MM)、顎骨壊死を伴う多発性骨髄腫、上咽頭癌、再発性又は転移性上咽頭癌、神経芽細胞腫、神経膠腫、甲状腺乳頭癌、小児脊髄上衣腫、骨肉腫、肺転移骨肉腫、膵臓癌、甲状腺癌、肉腫、下垂体腫瘍、下垂体腺腫、前神経腫瘍、舌の扁平上皮癌、中皮腫、網膜芽細胞腫、及び前立腺癌から選択される、請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩。
- 前記癌が、頭頸部癌、頭頸部扁平上皮癌、頚部扁平上皮癌、悪性黒色腫、星細胞腫、神経膠腫、胃癌(stomach cancer)、乳癌、胆管細胞癌、再発性又は転移性上咽頭癌、基底細胞及び扁平上皮癌、肝臓癌、脳癌、未分化星状細胞腫、肺癌、非小細胞肺癌、ゲフィチニブ抵抗性非小細胞肺癌、口腔癌、神経膠芽腫、骨肉腫、肺転移骨肉腫、膵癌、眼癌、消化器癌、結腸直腸癌、結腸直腸腺腫、有棘細胞癌、子宮内膜癌、卵巣上皮癌、食道癌(esophageal cancer)、ユーイング肉腫、胃癌(gastric cancer)、肝細胞癌、HER2陽性の乳癌、膀胱癌、骨癌、前立腺癌、網膜芽細胞腫、及び腎臓癌(renal cancer)から選択される、請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩。
- 前記癌が、未分化星状細胞腫、星細胞腫、膀胱癌、乳癌、胆管細胞癌、結腸直腸癌、結腸直腸腺腫、有棘細胞癌、子宮内膜癌、卵巣上皮癌、食道癌(esophageal cancer)、ユーイング肉腫、胃癌(gastric cancer)、ゲフィチニブ抵抗性非小細胞肺癌、神経膠芽腫、神経膠腫、肝細胞癌、HER2陽性の乳癌、頭頸部扁平上皮癌、悪性黒色腫、上咽頭癌(再発性又は転移性)、頚部扁平上皮癌、非小細胞肺癌、口腔癌、骨肉腫、骨肉腫(肺転移)、前立腺癌、及び網膜芽細胞腫から選択される、請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩。
- 前記癌が、肛門癌、胆管癌、消化器癌、胆管細胞癌、結腸直腸癌、結腸直腸腺腫、食道癌(esophageal cancer)、食道の扁平上皮癌(Esophagus Squamous cell)、胃癌(gastric cancer)、消化管カルチノイド腫瘍、消化管間質腫瘍(GIST)、肝細胞癌、肝内胆管癌、肝臓癌、肺癌、カルチノイド腫瘍、非小細胞肺癌、ゲフィチニブ抵抗性非小細胞肺癌、肺転移骨肉腫、胃癌(stomach cancer)、膵臓癌、小細胞肺癌、及び小腸癌から選択される、請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩。
- 前記癌が、胃癌(stomach cancer)、胃癌(gastric cancer)、消化器癌、結腸直腸癌、膵臓癌、肺癌及び肝臓癌から選択される、請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは請求項6又は7に記載の使用の為の式(IVb’)の化合物又はその医薬的に許容される塩。
- 患者における請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは患者における請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩
ここで、前記患者は、臨床的に検出可能な転移を示さない、特に、前記患者は、前癌状態、初期段階の癌、若しくは非転移性の癌を有し、又は
前記患者は、臨床的に検出可能な転移を示し、及び前記式(Ib’)の化合物又は式(IVb’)の化合物が転移の侵入を直接的に標的としない。 - 患者における請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは患者における請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩
ここで、前記患者の血液及び/又は組織のサンプル中のmiR-124の存在及び/又は発現レベルが、前記使用の前及び/又は間に測定される。 - 請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩
ここで、血液及び/又は組織のサンプル中のmiR-124の存在及び/又は発現レベルが測定されて、投与量をガイドする又は処置に対する応答を監視する。 - 請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩
ここで、miR-124レベルと、サイトカイン若しくは他のバイオマーカーのレベル或いは請求項1~5のいずれか1項に定義された式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つ請求項6~7のいずれか1項に定義された式(IVb’)の化合物又はその医薬的に許容される塩のレベルとを結び付けるアルゴリズムが使用されて、癌の重症度を監視する及び/又は処置の有効性を監視する。 - 患者における請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは患者における請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩
ここで、請求項1~5のいずれか1項に記載の式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは請求項6~7のいずれか1項に記載の式(IVb’)の化合物又はその医薬的に許容される塩の、前記患者の血液、血漿、組織、唾液及び/又は血清のサンプル中のレベルが前記使用の間に測定される。 - 別の抗腫瘍剤と組み合わせて使用される、
患者における請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは患者における請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩。 - 化学療法、免疫療法、放射線療法、手術、超音波、モノクローナル抗体及び癌ワクチンから選択される他の療法と組み合わせて使用される、
患者における請求項1~5のいずれか1項に記載の使用の為の、式(Ib’)の化合物、又はその代謝物若しくはその医薬的に許容される塩のいずれか1つの、或いは患者における請求項6~7のいずれか1項に記載の使用の為の、式(IVb’)の化合物又はその医薬的に許容される塩。
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EP18306783.4A EP3669874A1 (en) | 2018-12-20 | 2018-12-20 | Quinoline derivatives for use in the treatment or prevention of cancer |
EP18306783.4 | 2018-12-20 | ||
PCT/EP2019/086470 WO2020127839A1 (en) | 2018-12-20 | 2019-12-19 | Quinoline derivatives for use in the treatment or prevention of cancer |
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EP (2) | EP3669874A1 (ja) |
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WO2024109936A1 (zh) * | 2022-11-25 | 2024-05-30 | 江苏恒瑞医药股份有限公司 | 一种喹啉胺类化合物晶型及其制备方法 |
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EP2757161A1 (en) * | 2013-01-17 | 2014-07-23 | Splicos | miRNA-124 as a biomarker of viral infection |
CN103787992B (zh) * | 2014-01-21 | 2016-04-20 | 华东理工大学 | N,n-双取代苯并氮杂环-2-胺类化合物及其用途 |
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PT3429998T (pt) * | 2016-03-18 | 2021-11-04 | Prosynergia S A R L | Processo para preparação de derivados de quinolin-2-il-fenilamina e seus sais |
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MX2021007178A (es) | 2021-07-07 |
CA3122912A1 (en) | 2020-06-25 |
EP3897639A1 (en) | 2021-10-27 |
KR20210136969A (ko) | 2021-11-17 |
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