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51. 发明授权

EP1668013B1 PYRAZOLOPYRROLE DERIVATIVES AS PROTEIN KINASE INHIBITORS 有权
标题翻译： PYRAZOLOPYRROLDERIVATE ALS蛋白激酶抑制剂
公开(公告)号：EP1668013B1
公开(公告)日：2012-02-22
申请号：EP04785111.8
申请日：2004-09-23
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： BINCH, Hayley , EVERITT, Simon , MAZZEI, Francesca , ROBINSON, Daniel
IPC分类号： C07D487/04 , A61K31/41 , A61P35/00
CPC分类号： C07D487/04 , A61K31/41 , A61K45/06 , A61K2300/00
摘要： The present invention provides compounds of formula (I): or a pharmaceutically acceptable derivative thereof, wherein A, B, Q, R1, and R2 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT or PDK1 kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds, and methods of utilizing those compositions in the treatment of various disorders.

52. 发明公开

EP2411011A1 NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION 审中-公开
标题翻译：具有选择性抑制作用的新型氨基吡啶衍生物
公开(公告)号：EP2411011A1
公开(公告)日：2012-02-01
申请号：EP10756584.8
申请日：2010-03-15
申请人： MSD K.K. , Vertex Pharmaceuticals Incorporated
发明人： BINCH, Hayley , HASHIMOTO, Masaya , MORTIMORE, Michael , OHKUBO, Mitsuru , SUNAMI, Tomoko
IPC分类号： A61K31/535 , C07D401/04
CPC分类号： A61K31/535 , C07D401/14 , C07D417/14
摘要： The present invention relates to a compound of Formula (I): wherein: R
1 is H, -NHCOOR
1a , C
5-6 cycloalkyl, or phenyl; where the cycloalkyl and phenyl each independently may be substituted with one to three of the same or different substituents selected from R
10 ; R
1a is C
1-3 alkyl which may be substituted with one to three of the same or different substituents selected from F and Cl; R
2 is H, -COOH, -CH
2 COOH, -COOR
2a , or -CH
2 COOR
2a ; R
2a is C
1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from halogen atoms; R
3 is H, C
1-6 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R
11 ; R
10 is F, Cl, CF
3 , or C
1-2 alkyl; R
11 is halogen atom, hydroxy, or cyano; W is selected from: W
2a is H, halogen atom, cyano, C
1-2 alkyl, or C
3-5 cycloalkyl, or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明涉及式（I）的化合物：其中：R 1是H，-NHCOOR 1a，C 5-6环烷基或苯基; 其中环烷基和苯基各自独立地可以被1至3个选自R 10的相同或不同的取代基取代; R 1a是可以被1-3个选自F和Cl的相同或不同取代基取代的C 1-3烷基; R 2是H，-COOH，-CH 2 COOH，-COOR 2a或-CH 2 COOR 2a; R 2a为C 1-2烷基，其中所述烷基可被1-3个选自卤素原子的相同或不同取代基取代; R 3是H，C 1-6烷基，其中烷基可以被1-3个选自R 11的相同或不同的取代基取代; R 10是F，Cl，CF 3或C 1-2烷基; R 11是卤原子，羟基或氰基; W选自：W 2a是H，卤素原子，氰基，C 1-2烷基或C 3-5环烷基，或其药学上可接受的盐或酯。

53. 发明公开

EP2358721A1 Modulators of cystic fibrosis transmembrane conductance regulator 有权
标题翻译：囊性纤维化跨膜电导调节的调节剂
公开(公告)号：EP2358721A1
公开(公告)日：2011-08-24
申请号：EP09753253.5
申请日：2009-10-23
申请人： Vertex Pharmaceuticals Incorporated
发明人： BINCH, Hayley , FANNING, Lev, T.D. , BOTFIELD, Martyn , GROOTENHUIS, Peter, D.J. , VAN GOOR, Fredrick , NUMA, Mehdi, Michel Djamel
IPC分类号： C07D487/08 , A61K31/4709 , A61P11/00 , A61P43/00
CPC分类号： C07D401/14 , C07D487/08 , Y02P20/55
摘要： The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator ("CFTR"), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR (Formula I) or pharmaceutically acceptable salts thereof, wherein: ring A is selected from: (a), (b), (c), (d), wherein: R
1 is -CH
3 -CF
3 or -CN; R
2 is hydrogen, -CH
3 , -CF
3 , -OH, or -CH
2 OH; R
3 is hydrogen, -CH
3 , -OCH
3 , or -CN; provided that both R
2 and R
3 are not simultaneously hydrogen; and one of X and Y is nitrogen and the other is carbon.

54. 发明授权

EP1937667B1 BENZIMIDAZOLES USEFUL AS INHIBITORS OF PROTEIN KINASES 有权
标题翻译：作为蛋白激酶抑制剂的苯并咪唑
公开(公告)号：EP1937667B1
公开(公告)日：2010-10-13
申请号：EP06787944.5
申请日：2006-07-21
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： BINCH, Hayley , MORTIMORE, Michael , ROBINSON, Daniel , STAMOS, Dean , EVERITT, Simon
IPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , A61K31/506 , A61K31/4439 , A61K31/55 , A61K31/551 , A61P35/00
CPC分类号： C07D403/04 , C07D401/04 , C07D401/14 , C07D403/14 , C07D487/08
摘要： The present invention relates to compounds useful as inhibitors of Aurora, FLT-3, or PDKl protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the invention.

55. 发明授权

EP1485380B1 AZOLYLAMINOAZINES AS INHIBITORS OF PROTEIN KINASES 有权
标题翻译：作为蛋白激酶抑制剂的偶氮基氨基酰胺
公开(公告)号：EP1485380B1
公开(公告)日：2010-05-19
申请号：EP03714208.0
申请日：2003-03-14
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： BEBBINGTON, David , BINCH, Hayley , CHARRIER, Jean-Damien , EVERITT, Simon , GOLEC, Julian M. C. , KAY, David , KNEGTEL, Ronald , MILLER, Andrew , PIERARD, Francoise
IPC分类号： C07D417/12 , C07D471/04 , C07D487/04 , C07D413/12 , C07D413/14 , C07D417/14 , A61K31/505 , A61P37/00 , A61P31/12 , A61P35/00 , A61P9/00 , A61P7/00 , A61P19/00 , A61P3/00 , C07D411/12
CPC分类号： C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的化合物。本发明还提供了包含所述化合物的药学上可接受的组合物以及使用该组合物治疗各种疾病，病症或障碍的方法。

56. 发明授权

EP1485100B1 AZINYLAMINOAZOLES AS INHIBITORS OF PROTEIN KINASES 有权
标题翻译： AZOLYLAMINOAZINE ALS PROTEINKINASEHEMMER
公开(公告)号：EP1485100B1
公开(公告)日：2010-05-05
申请号：EP03716597.4
申请日：2003-03-14
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： BEBBINGTON, David , BINCH, Hayley , CHARRIER, Jean-Damien , EVERITT, Simon , GOLEC, Julian, M., C. , KAY, David , KNEGTEL, Ronald , MILLER, Andrew , PIERARD, Francoise
IPC分类号： A61K31/505 , A61P37/00 , A61P31/12 , A61P35/00 , A61P9/00 , A61P7/00 , A61P19/00 , A61P3/00 , C07D403/12 , C07D487/04 , C07D417/14 , C07D409/14 , C07D471/04 , C07D401/14
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

57. 发明公开

EP2027106A2 CGRP RECEPTOR ANTAGONISTS 审中-公开
标题翻译： CGRP受体拮抗剂
公开(公告)号：EP2027106A2
公开(公告)日：2009-02-25
申请号：EP07796082.1
申请日：2007-06-13
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： GUTIERREZ, Corey , TERMIN, Andreas , HADIDA-RUAH, Sara , JOSHI, Pramod , BERGERON, Daniele , YOO, Sanghee , BINCH, Hayley , COME, Jon , NANTHAKUMAR, Suganthi , CAO, Jingrong
IPC分类号： C07D401/00
CPC分类号： C07D417/14 , C07D277/14 , C07D417/06 , C07D471/04 , C07D471/10 , C07D498/10 , C07D513/10
摘要： The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions. The present invention relates to CGRP receptor antagonists of formula 1, wherein: X is S, SO, or SO2; pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
摘要翻译：本发明涉及CGRP受体拮抗剂，其药物组合物及其用于治疗CGRP受体介导的疾病和病症的方法。本发明涉及式1的CGRP受体拮抗剂，其中：X是S，SO或SO 2; 其药物组合物及其用于治疗CGRP受体介导的疾病和病症的方法。

58. 发明公开

EP1979367A2 QUINOLIN-4-ONE DERIVATIVES AS MODULATORS OF ABC TRANSPORTERS 审中-公开
标题翻译：喹啉-4-酮衍生物AS ABC转运蛋白的调节剂
公开(公告)号：EP1979367A2
公开(公告)日：2008-10-15
申请号：EP06848958.2
申请日：2006-12-21
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： GROOTENHUIS, Peter D.J. , HADIDA RUAH, Sara , ZHOU, Jinglan , HAZLEWOOD, Anna , ARUMUGAM, Vijayalaksmi , GUTIERREZ, Corey , BINCH, Hayley
IPC分类号： C07F9/60 , C07D215/56 , A61P31/00 , A61P29/00 , A61K31/47 , A61K31/661
CPC分类号： G01N33/502 , A61K31/47 , A61K31/675 , A61K45/06 , C07D215/56 , C07F9/60 , C12Q1/34 , G01N33/6872 , G01N2333/914 , G01N2500/10 , G01N2500/20
摘要： The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

59. 发明公开

EP1951715A2 AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS 有权
标题翻译：作为激酶抑制剂的氨基嘧啶适合...
公开(公告)号：EP1951715A2
公开(公告)日：2008-08-06
申请号：EP06827465.3
申请日：2006-11-03
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： BINCH, Hayley , MORTIMORE, Michael , FRAYSSE, Damien , RUTHERFORD, Alistair
IPC分类号： C07D403/14 , A61K31/4155 , C07D239/02
CPC分类号： C07D403/12 , C07D239/38 , C07D401/14 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds useful as inhibitors of Aurora protein kinases . The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders . The invention also provides processes for preparing compounds of the invention.

60. 发明公开

EP1937667A2 BENZIMIDAZOLES USEFUL AS INHIBITORS OF PROTEIN KINASES 有权
标题翻译：作为蛋白激酶抑制剂的苯并咪唑
公开(公告)号：EP1937667A2
公开(公告)日：2008-07-02
申请号：EP06787944.5
申请日：2006-07-21
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： BINCH, Hayley , MORTIMORE, Michael , ROBINSON, Daniel , STAMOS, Dean , EVERITT, Simon
IPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , A61K31/506 , A61K31/4439 , A61K31/55 , A61K31/551 , A61P35/00
CPC分类号： C07D403/04 , C07D401/04 , C07D401/14 , C07D403/14 , C07D487/08
摘要： The present invention relates to compounds useful as inhibitors of Aurora, FLT-3, or PDKl protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the invention.

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