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1. 发明公开

EP1990343A2 Azaindoles 有权
标题翻译：氮杂吲哚
公开(公告)号：EP1990343A2
公开(公告)日：2008-11-12
申请号：EP08162392.8
申请日：2000-12-27
申请人： Aventis Pharma Limited
发明人： Cox, Paul Joseph , Majid, Tahir Nadeem , Lai, Justine Yeun Quai , Morley, Andrew David , Amendola, Shelley , Deprets, Stephanie , Edlin, Chris
IPC分类号： C07D471/04 , C07D487/04 , C07D519/00 , A61K31/437 , A61K31/4985 , A61P11/06 , A61P17/06 , A61P29/00
CPC分类号： A61K31/4985 , A61K31/437 , C07D471/04 , C07D487/04
摘要： The invention is directed to compositions containing physiologically active compounds of general formula (I):-

wherein R 1 is aryl or heteroaryl; R 2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -Z 1 R 8 , -C(=O)-NY 3 Y 4 , -CO 2 R 8 , -NY 3 Y 4 , -N(R 6 )-C(=O)-R 7 , -N(R 6 )-C(=O)-NY 3 Y 4 , -N(R 6 )-C(=O)-OR 7 , -N(R 6 )-SO 2 -R 7 , -N(R 6 )-SO 2 -NY 3 Y 4 and one or more halogen atoms; R 3 represents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, -C(=O)-OR 5 or -C(=O)-NY 3 Y; and X 1 represents CH, C-halo, C-CN, C-R 7 , C-NY 3 Y 4 , C-OH, C-Z 2 R 7 , C-C(=O)-OR 5 , C-C(=O)-NY 3 Y 4 , C-N(R 8 )-C(=O)-R 7 , C-SO 2 -NY 3 Y 4 , C-N(R 8 )-SO 2 -R 7 , C-alkenyl, C-alkynyl or C-NO 2 ; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I).
Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.
摘要翻译：本发明涉及含有通式（I）的生理活性化合物的组合物：其中R 1是芳基或杂芳基; R 2表示氢，酰基，氰基，卤素，低级烯基或任选被选自氰基，杂芳基，杂环烷基，-Z 1 R 8，-C（= O）-NY 3 Y 4，-CO 2 R 8，-NY 3 Y 4，-N（R 6）-C（= O）-R 7，-N（R 6）-C（= O）-NY 3 Y 4，-N（R 6） C（= O）-OR 7，-N（R 6）-SO 2 -R 7，-N（R 6）-SO 2 -NY 3 Y 4和一个或多个卤素原子; R 3表示氢，芳基，氰基，卤素，杂芳基，低级烷基，-C（= O）-OR 5或-C（= O）-NY 3 Y; 并且X 1表示CH，C-卤代，C-CN，CR 7，C-NY 3 Y 4，C-OH，CZ 2 R 7，CC（= O）-OR 5，CC（= O）-NY 3 Y 4，CN（R 8）-C（= O）-R 7，C-SO 2 -NY 3 Y 4，CN（R 8）-SO 2 -R 7，C-链烯基， NO 2; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物，以及式（I）范围内的新化合物。这些化合物和组合物具有有价值的药物特性，特别是抑制蛋白激酶的能力。

2. 发明授权

EP1990343B1 Azaindoles 有权
标题翻译：氮杂吲哚
公开(公告)号：EP1990343B1
公开(公告)日：2012-04-04
申请号：EP08162392.8
申请日：2000-12-27
申请人： Aventis Pharma Limited
发明人： Cox, Paul Joseph , Majid, Tahir Nadeem , Lai, Justine Yeun Quai , Morley, Andrew David , Amendola, Shelley , Deprets, Stephanie , Edlin, Chris
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61K31/4985 , A61P11/06 , A61P17/06 , A61P29/00 , C07D221/00 , C07D209/00 , C07D471/00
CPC分类号： A61K31/4985 , A61K31/437 , C07D471/04 , C07D487/04
摘要： The invention is directed to compositions containing physiologically active compounds of general formula (I):- wherein R 1 is aryl or heteroaryl; R 2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -Z 1 R 8 , -C(=O)-NY 3 Y 4 , -CO 2 R 8 , -NY 3 Y 4 , -N(R 6 )-C(=O)-R 7 , -N(R 6 )-C(=O)-NY 3 Y 4 , -N(R 6 )-C(=O)-OR 7 , -N(R 6 )-SO 2 -R 7 , -N(R 6 )-SO 2 -NY 3 Y 4 and one or more halogen atoms; R 3 represents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, -C(=O)-OR 5 or -C(=O)-NY 3 Y; and X 1 represents CH, C-halo, C-CN, C-R 7 , C-NY 3 Y 4 , C-OH, C-Z 2 R 7 , C-C(=O)-OR 5 , C-C(=O)-NY 3 Y 4 , C-N(R 8 )-C(=O)-R 7 , C-SO 2 -NY 3 Y 4 , C-N(R 8 )-SO 2 -R 7 , C-alkenyl, C-alkynyl or C-NO 2 ; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.

3. 发明公开

EP2233486A1 Azaindoles 审中-公开
标题翻译：氮杂吲哚
公开(公告)号：EP2233486A1
公开(公告)日：2010-09-29
申请号：EP09171579.7
申请日：2002-06-20
申请人： Aventis Pharma Limited
发明人： Cox, Paul Joseph , Majid, Tahir Nadeem , Morley, Andrew David , Amendola, Shelley , Deprets, Stephanie , Edlin, Chris , Gardner, Charles J , Kominos, Dorothea , Pedgrift, Brian Leslie , Halley, Frank , Lai, Justine Yeun Quai , Gillespy, Timothy Alan , Edwards, Michael , Clerc, Francois Frederic , Nemecek, Conception , Houille, Olivier , Damour, Dominique , Bouchard, Herve , Bezard, Daniel
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/4985 , A61P29/00 , A61P11/00 , A61P9/00 , A61P35/00
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04
摘要： The invention is directed to compounds of general formula (I):-

and pharmaceutically acceptable salts and solvates of such compounds. Such compounds have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译：本发明涉及通式（I）的化合物： - 和这些化合物的药学上可接受的盐和溶剂合物。这些化合物具有有价值的药物性质，特别是抑制激酶的能力。

4. 发明公开

EP1990343A3 Azaindoles 有权
标题翻译：氮杂吲哚
公开(公告)号：EP1990343A3
公开(公告)日：2008-12-10
申请号：EP08162392.8
申请日：2000-12-27
申请人： Aventis Pharma Limited
发明人： Cox, Paul Joseph , Majid, Tahir Nadeem , Lai, Justine Yeun Quai , Morley, Andrew David , Amendola, Shelley , Deprets, Stephanie , Edlin, Chris
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61K31/4985 , A61P11/06 , A61P17/06 , A61P29/00 , C07D221/00 , C07D209/00 , C07D471/00
CPC分类号： A61K31/4985 , A61K31/437 , C07D471/04 , C07D487/04
摘要： The invention is directed to compositions containing physiologically active compounds of general formula (I):-

wherein R 1 is aryl or heteroaryl; R 2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -Z 1 R 8 , -C(=O)-NY 3 Y 4 , -CO 2 R 8 , -NY 3 Y 4 , -N(R 6 )-C(=O)-R 7 , -N(R 6 )-C(=O)-NY 3 Y 4 , -N(R 6 )-C(=O)-OR 7 , -N(R 6 )-SO 2 -R 7 , -N(R 6 )-SO 2 -NY 3 Y 4 and one or more halogen atoms; R 3 represents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, -C(=O)-OR 5 or -C(=O)-NY 3 Y; and X 1 represents CH, C-halo, C-CN, C-R 7 , C-NY 3 Y 4 , C-OH, C-Z 2 R 7 , C-C(=O)-OR 5 , C-C(=O)-NY 3 Y 4 , C-N(R 8 )-C(=O)-R 7 , C-SO 2 -NY 3 Y 4 , C-N(R 8 )-SO 2 -R 7 , C-alkenyl, C-alkynyl or C-NO 2 ; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I).
Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.

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