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1. 发明申请

US20120202832A1 KINASE INHIBITORS, PRODRUG FORMS THEREOF AND THEIR USE IN THERAPY 有权
标题翻译：激素抑制剂，其制剂及其在治疗中的使用
公开(公告)号：US20120202832A1
公开(公告)日：2012-08-09
申请号：US13390398
申请日：2010-09-02
申请人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Guo-Liang Lu , Ho Huat Lee , Amir Ashoorzadeh , Robert Forbes Anderson , William Robert Wilson , William Alexander Denny , Huai-Ling (Annie) Hsu , Andrej Maroz , Stephen Michael Frazer Jamieson , Alexandra Marie Mowday , Kendall Marie Carlin
发明人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Guo-Liang Lu , Ho Huat Lee , Amir Ashoorzadeh , Robert Forbes Anderson , William Robert Wilson , William Alexander Denny , Huai-Ling (Annie) Hsu , Andrej Maroz , Stephen Michael Frazer Jamieson , Alexandra Marie Mowday , Kendall Marie Carlin
IPC分类号： A61K31/519 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04 , A61K31/519
摘要： The invention provides kinase inhibitors of Formula I: wherein either: (1) R1 is H, and (a) R2 is (3-chlorobenzyl)oxy- and R3 is chloro; (b) R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; (c) R2 is 2-pyridinylmethoxy and R3 is chloro; (d) R2 and R3 are both chloro; (e) R2 is chloro and R1 is bromo; (f) R2 and R3 are both bromo; (g) R2 is fluoro and R3 is ethynyl; (h) R2 is chloro and R3 is ethynyl; (i) R2 is bromo and R3 is ethynyl; (j) other than when R1 is in the 3-position in combination with R3, in the 4-position, R2 is bromo and R3 is fluoro; (k) R2 is 2-pyridinylmethoxy and R3 is fluoro; or (l) R2 is 2-pyridinylmethoxy and R1 is bromo; or (2) at least one of R1, R2 and R3 is selected from benzyloxy, 3-chlorobenzyloxy and 2-pyridinylmethoxy and when at least one of R1, R2 and R3 is not benzyloxy, 3-chlorobenzyloxy or 2-pyridinylmethoxy, each of the others is independently selected from H, halogen, and C2-C4 alkynyl, with the proviso that when one of R1, R2 and R3 is benzyloxy or 2-pyridinylmethoxy, the other two of R1, R2 and R3 are not H; or (3) two of R1, R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; and the other is selected from H, halogen and C2-C4 alkynyl. Also provided are reductive prodrugs, comprising a kinase inhibitor as defined above and a reductive trigger linked directly or indirectly to a nitrogen of the kinase inhibitor. Further provided are pharmaceutical compositions, comprising the kinase inhibitors or the prodrugs, and the use of such compositions in therapy, in particular for treating cancer.
摘要翻译：本发明提供了式I的激酶抑制剂：其中：（1）R 1是H，和（a）R 2是（3-氯苄基）氧基，R 3是氯; （b）R2和R3与它们所连接的碳原子一起形成1-（3-氟苄基）-1H-吡唑; （c）R2是2-吡啶基甲氧基，R3是氯; （d）R2和R3均为氯; （e）R 2是氯，R 1是溴; （f）R2和R3都是溴; （g）R2是氟，R3是乙炔基; （h）R2是氯，R3是乙炔基; （i）R2是溴，R3是乙炔基; （j）除了当R 1与R 3结合在一起的3位时，在4-位上，R 2是溴并且R 3是氟; （k）R2是2-吡啶基甲氧基，R3是氟; 或（1）R 2是2-吡啶基甲氧基，R 1是溴; 或（2）R 1，R 2和R 3中的至少一个选自苄氧基，3-氯苄氧基和2-吡啶基甲氧基，当R 1，R 2和R 3中的至少一个不是苄氧基，3-氯苄氧基或2-吡啶基甲氧基时，其余的独立地选自H，卤素和C 2 -C 4炔基，条件是当R 1，R 2和R 3中的一个是苄氧基或2-吡啶基甲氧基时，R 1，R 2和R 3中的另外两个不是H; 或（3）R 1，R 2和R 3中的两个与它们所连接的碳原子一起形成1-（3-氟苄基）-1H-吡唑; 另一个选自H，卤素和C 2 -C 4炔基。还提供了还原前药，其包含如上定义的激酶抑制剂和直接或间接连接于激酶抑制剂的氮的还原性触发剂。还提供了包含激酶抑制剂或前药的药物组合物，以及这些组合物在治疗中的用途，特别是用于治疗癌症。

2. 发明授权

US09101632B2 Kinase inhibitors, prodrug forms thereof and their use in therapy 有权
标题翻译：激酶抑制剂，其前药形式及其在治疗中的用途
公开(公告)号：US09101632B2
公开(公告)日：2015-08-11
申请号：US13390398
申请日：2010-09-02
申请人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Guo-Liang Lu , Ho Huat Lee , Amir Ashoorzadeh , Robert Forbes Anderson , William Robert Wilson , William Alexander Denny , Huai-Ling Annie Hsu , Andrej Maroz , Stephen Michael Frazer Jamieson , Alexandra Marie Mowday , Kendall Marie Carlin
发明人： Jeffrey Bruce Smaill , Adam Vorn Patterson , Guo-Liang Lu , Ho Huat Lee , Amir Ashoorzadeh , Robert Forbes Anderson , William Robert Wilson , William Alexander Denny , Huai-Ling Annie Hsu , Andrej Maroz , Stephen Michael Frazer Jamieson , Alexandra Marie Mowday , Kendall Marie Carlin
IPC分类号： A61K31/519 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04 , A61K31/519
摘要： The invention provides kinase inhibitors of Formula I: wherein either: (1) R1 is H, and (a) R2 is (3-chlorobenzyl)oxy-and R3 is chloro; (b) R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; (c) R2 is 2-pyridinylmethoxy and R3 is chloro; (d) R2 and R3 are both chloro; (e) R2 is chloro and R1 is bromo; (f) R2 and R3 are both bromo; (g) R2 is fluoro and R3 is ethynyl; (h) R2 is chloro and R3 is ethynyl; (i) R2 is bromo and R3 is ethynyl; (j) other than when R1 is in the 3-position in combination with R3, in the 4-position, R2 is bromo and R3 is fluoro; (k) R2 is 2-pyridinylmethoxy and R3 is fluoro; or (l) R2 is 2-pyridinylmethoxy and R1 is bromo; or (2) at least one of R1, R2 and R3 is selected from benzyloxy, 3-chlorobenzyloxy and 2-pyridinylmethoxy and when at least one of R1, R2 and R3 is not benzyloxy, 3-chlorobenzyloxy or 2-pyridinylmethoxy, each of the others is independently selected from H, halogen, and C2-C4 alkynyl, with the proviso that when one of R1, R2 and R3 is benzyloxy or 2-pyridinylmethoxy, the other two of R1, R2 and R3 are not H; or (3) two of R1, R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; and the other is selected from H, halogen and C2-C4 alkynyl. Also provided are reductive prodrugs, comprising a kinase inhibitor as defined above and a reductive trigger linked directly or indirectly to a nitrogen of the kinase inhibitor. Further provided are pharmaceutical compositions, comprising the kinase inhibitors or the prodrugs, and the use of such compositions in therapy, in particular for treating cancer.
摘要翻译：本发明提供了式I的激酶抑制剂：其中：（1）R 1是H，和（a）R 2是（3-氯苄基）氧基，R 3是氯; （b）R2和R3与它们所连接的碳原子一起形成1-（3-氟苄基）-1H-吡唑; （c）R2是2-吡啶基甲氧基，R3是氯; （d）R2和R3均为氯; （e）R 2是氯，R 1是溴; （f）R2和R3都是溴; （g）R2是氟，R3是乙炔基; （h）R2是氯，R3是乙炔基; （i）R2是溴，R3是乙炔基; （j）除了当R 1与R 3结合在一起的3位时，在4-位上，R 2是溴并且R 3是氟; （k）R2是2-吡啶基甲氧基，R3是氟; 或（1）R 2是2-吡啶基甲氧基，R 1是溴; 或（2）R 1，R 2和R 3中的至少一个选自苄氧基，3-氯苄氧基和2-吡啶基甲氧基，当R 1，R 2和R 3中的至少一个不是苄氧基，3-氯苄氧基或2-吡啶基甲氧基时，其余的独立地选自H，卤素和C 2 -C 4炔基，条件是当R 1，R 2和R 3中的一个是苄氧基或2-吡啶基甲氧基时，R 1，R 2和R 3中的另外两个不是H; 或（3）R 1，R 2和R 3中的两个与它们所连接的碳原子一起形成1-（3-氟苄基）-1H-吡唑; 另一个选自H，卤素和C 2 -C 4炔基。还提供了还原前药，其包含如上定义的激酶抑制剂和直接或间接连接于激酶抑制剂的氮的还原性触发剂。还提供了包含激酶抑制剂或前药的药物组合物，以及这些组合物在治疗中的用途，特别是用于治疗癌症。

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