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1. 发明公开

EP2418210A1 Thiophene-carboxamides useful as inhibitors of protein kinases 审中-公开
标题翻译： Als蛋白激酶 - 抑制剂nutzbare噻吩 - 甲酰胺
公开(公告)号：EP2418210A1
公开(公告)日：2012-02-15
申请号：EP11188838.4
申请日：2007-04-12
申请人： Vertex Pharmaceuticals Incorporated
发明人： Brenchley, Guy , Charrier, Jean-Damien , Durrant, Steven , Knegtel, Ron , Ramaya, Sharn , Sadiq, Shazia
IPC分类号： C07D409/04 , A61K31/4178 , A61P35/00
CPC分类号： C07D409/04
摘要： The present invention relates to compounds of formula I useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various diseases, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
摘要翻译：本发明涉及可用作蛋白激酶抑制剂的式I化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。本发明还提供了制备本发明化合物的方法。

2. 发明公开

EP2264028A1 Pyrazole compounds useful as protein kinase inhibitors 审中-公开
标题翻译：吡唑并噻吩类蛋白激酶
公开(公告)号：EP2264028A1
公开(公告)日：2010-12-22
申请号：EP10184271.4
申请日：2001-12-19
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： Bebbington, David , Charrier, Jean-Damien , Golec, Julian , Miller, Andrew , Knegtel, Ronald
IPC分类号： C07D403/12 , C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： C07D403/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： This invention describes novel pyrazole compounds of formula (I), wherein R 1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R x , R y , R 2 , and R 2' are as described in the specification, and processes for preparing these compounds. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
摘要翻译：本发明描述了式（I）的新型吡唑化合物，其中R 1是T环D，其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环; R x，R y，R 2和R 2'如说明书中所述，以及制备这些化合物的方法。该化合物可用作蛋白激酶抑制剂，特别是作为Aurora-2和GSK-3的抑制剂，用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病。

3. 发明公开

EP1702920A1 Pyrazole compounds useful as protein kinase inhibitors 有权
标题翻译：吡唑并噻嗪类化合物蛋白酶
公开(公告)号：EP1702920A1
公开(公告)日：2006-09-20
申请号：EP06011799.1
申请日：2001-12-19
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： Bebbington, David , Charrier, Jean-Damien , Golec, Julian , Miller, Andrew , Knegtel, Ronald
IPC分类号： C07D403/12 , C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： C07D403/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： This invention describes novel pyrazole compounds of formula (IIIa), wherein R 1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R x , R y , R 2 , and R 2' are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
摘要翻译：本发明描述了式（IIIa）的新型吡唑化合物，其中R 1是T环D，其中环D是5-7元单环或选自芳基，杂芳基，杂环基或碳环基的8-10元双环; R x，R y，R 2和R 2'如说明书中所述。该化合物可用作蛋白激酶抑制剂，特别是作为Aurora-2和GSK-3的抑制剂，用于治疗诸如癌症，糖尿病和阿尔茨海默病的疾病。

4. 发明授权

EP2332940B1 Azaindoles useful as inhibitors of JAK and other protein kinases 失效
标题翻译：作为JAK和其他蛋白质的激酶抑制剂的氮杂吲哚适当
公开(公告)号：EP2332940B1
公开(公告)日：2012-10-31
申请号：EP10182365.6
申请日：2005-03-30
申请人： Vertex Pharmaceuticals Incorporated
发明人： Salituro, Francesco , Farmer, Luc , Bethiel, Randy , Harrington, Edmund , Green, Jeremy , Court, John , Come, Jon , Lauffer, David , Aronov, Alex , Binch, Hayley , Boyall, Dean , Charrier, Jean-Damien , Everitt, Simon , Fraysse, Damien , Mortimore, Michael , Pierard, Françoise , Robinson, Daniel , Pinder, Joanne , Wang, Tiansheng , Pierce, Albert , Wang, Jian
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D519/00 , C07F7/0809

5. 发明公开

EP2308846A3 Caspase inhibitors and uses thereof 审中-公开
标题翻译：蛋白酶抑制剂及其用途
公开(公告)号：EP2308846A3
公开(公告)日：2011-08-10
申请号：EP10196409.6
申请日：2000-12-08
申请人： Vertex Pharmaceuticals Incorporated
发明人： Golec, Julian , Charifson, Paul , Charrier, Jean-Damien , Binch, Hayley
IPC分类号： C07D213/64 , A61K31/4412 , C07D215/22 , A61K31/4704 , C07D217/24 , A61K31/517 , C07D239/36 , A61K31/513 , C07D239/90 , C07D209/46 , A61K31/4035 , C07D209/48 , C07D471/04 , C07D495/04
CPC分类号： C07D209/48 , C07D209/46 , C07D213/64 , C07D215/227 , C07D217/24 , C07D239/36 , C07D239/80 , C07D239/88 , C07D239/90 , C07D471/04 , C07D495/04
摘要： This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula (IE):

where R 1 is hydrogen, CN, CHN 2 , R, -CH 2 Y;
R is an aliphatic group, a substituted aliphatic group, an aryl group, a substituted aryl group, an aralkyl group, a substituted aralkyl group, a non-aromatic heterocyclic group or a substituted non-aromatic heterocyclic group;
Y is an electronegative leaving group or -OR, -SR, -OC=O (R), or -OPO(R 8 ) (R 9 );
R 8 and R 9 are independently selected from R or OR;
R 2 is CO 2 H, CH 2 CO 2 H, or esters or isosteres thereof;
R 3 is hydrogen or a C 1-6 straight chained or branched alkyl;
X 2 is selected from a valence bond, oxygen, sulfur, nitrogen or carbon;
R 4 and R 5 are each independently selected from hydrogen, halo, R, OR, SR, aryl, substituted aryl, OH, NO 2 , CN, NH 2 , NHR, N(R) 2 , NHCOR, NHCONHR, NHCON(R) 2 , NRCOR, NHCO 2 R, CO 2 R, CO 2 H, COR, CONHR, CON(R) 2 , S(O) 2 R, SONH 2 , S(O)R, SO 2 NHR, or NHS(O) 2 R; and
the fused ring is an aromatic or non-aromatic heterocyclic ring.

6. 发明公开

EP2277876A1 Substituted pyrimidines for the treatment of cancer 审中-公开
标题翻译：在癌症治疗中有用取代嘧啶
公开(公告)号：EP2277876A1
公开(公告)日：2011-01-26
申请号：EP10182211.2
申请日：2003-06-19
申请人： Vertex Pharmaceuticals Incorporated
发明人： Charrier, Jean-Damien , Mazzei, Francesca , Kay, David , Miller, Andrew
IPC分类号： C07D403/12 , C07D403/14 , A61K31/506 , A61P35/00
CPC分类号： C07D403/14 , C07D239/34 , C07D401/14 , C07D403/12 , C07D453/02
摘要： The present invention provides tri substituted pyrimidines useful for treating or lessening cancer.
摘要翻译：本发明提供了用于治疗或减轻癌症的三substituiertem嘧啶。

7. 发明公开

EP2412707A3 3-[2-(3-Amino-2-oxo-2H-pyridin-1-yl)-acetylamino]-4-oxo-pentanoic acid derivatives and their use as caspase inhibitors 审中-公开
标题翻译： 3- [2-（3-氨基-2-氧代-2H-吡啶-1-基）乙酰氨基] -4-氧代Pentansäurederivative和它们作为半胱氨酸蛋白酶抑制剂的用途
公开(公告)号：EP2412707A3
公开(公告)日：2012-06-13
申请号：EP11183025.3
申请日：2004-05-27
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： Brenchley, Guy , Charrier, Jean-Damien , Durrant, Steven , Knegtel, Ronald , Mortimore, Michael , Studley, John R.
IPC分类号： C07D213/74 , A61K31/4412 , A61P29/00 , A61P35/00 , A61P37/00 , C07D213/75 , C07D213/76 , C07D213/81 , C07D213/82 , C07D405/12 , C07D417/12
CPC分类号： C07D213/75 , C07D213/82 , C07D405/12 , C07D417/12
摘要： The present invention provides a compound of formula I:

wherein R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.

8. 发明授权

EP1702920B1 Pyrazole compounds useful as protein kinase inhibitors 有权
标题翻译：吡唑并噻吩类蛋白激酶
公开(公告)号：EP1702920B1
公开(公告)日：2011-10-12
申请号：EP06011799.1
申请日：2001-12-19
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： Bebbington, David , Charrier, Jean-Damien , Golec, Julian , Miller, Andrew , Knegtel, Ronald
IPC分类号： C07D403/12 , C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： C07D403/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D407/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/16 , C07D487/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04

9. 发明公开

EP2308844A3 Caspase inhibitors and uses thereof 审中-公开
标题翻译： Caspase抑制剂及其用途
公开(公告)号：EP2308844A3
公开(公告)日：2011-08-10
申请号：EP10196401.3
申请日：2000-12-08
申请人： Vertex Pharmaceuticals Incorporated
发明人： Golec, Julian , Charfison, Paul , Charrier, Jean-Damien , Binch, Hayley
IPC分类号： C07D213/64 , A61K31/4412 , C07D215/22 , A61K31/4704 , C07D217/24 , A61K31/517 , C07D239/36 , A61K31/513 , C07D239/90 , C07D209/46 , A61K31/4035 , C07D209/48 , C07D471/04 , C07D495/04
CPC分类号： C07D209/48 , C07D209/46 , C07D213/64 , C07D215/227 , C07D217/24 , C07D239/36 , C07D239/80 , C07D239/88 , C07D239/90 , C07D471/04 , C07D495/04
摘要： This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula (IA):

where R 1 is hydrogen, CN, CHN 2 , R, -CH 2 Y;
R is an aliphatic group, a substituted aliphathic group, an aryl group, a substituted aryl group, an aralkyl group, a substituted aralkyl group, a non-aromatic heterocyclic group or a substituted non-aromatic heterocyclic group;
Y is an electronegative leaving group, -OR, -SR, -OC=O(R), or -OPO (R 8 ) (R 9 );
R 8 and R 9 are each independently selected from R or OR;
R 1 is CO 2 H, CH 2 CO 2 H, or esters, amides or isosteres thereof;
R 3 is hydrogen or a C 1-6 straight chained or branched alkyl;
each of R 4 -R 6 is independently selected from hydrogen, halo, R, OR, SR, aryl, substituted aryl, OH, NO 2 , CN, NH 2 , NHR, N(R) 2 , NHCOR, NHCONHR, NHCON(R) 2 , NRCOR, NHCO 2 R, CO 2 R, CO 2 H, COR, CONHR, CON(R) 2 , S(O) 2 R, SONH 2 , S(O)R, SO 2 NHR or NHS(O) 2 R, and
R 7 is selected from hydrogen, halo, R, OR, SR, aryl, substituted aryl, OH, CN, CO 2 R, CO 2 H, COR, CONHR, CON(R) 2 , S(O) 2 R, SONH 2 , S(O)R, or SO 2 NHR.
摘要翻译：本发明提供了可用作半胱天冬酶抑制剂的新化合物及其药学上可接受的衍生物。这些化合物具有通式（IA）：其中R 1为氢，CN，CHN 2，R，-CH 2 Y; R为脂族基团，取代的脂族基团，芳基，取代的芳基，芳烷基，取代的芳烷基，非芳族杂环基或取代的非芳族杂环基; Y是电负离子基团，-OR，-SR，-OC = O（R）或-OPO（R 8）（R 9）; R8和R9各自独立地选自R或OR; R1是CO2H，CH2CO2H或其酯，酰胺或电子等排体; R3是氢或C1-6直链或支链烷基; 每个R 4 -R 6独立地选自氢，卤素，R，OR，SR，芳基，取代的芳基，OH，NO 2，CN，NH 2，NHR，N（R）2，NHCOR，NHCONHR，NHCON 2， NRCOR，NHCO 2 R，CO 2 R，CO 2 H，COR，CONHR，CON（R）2，S（O）2 R，SONH 2，S（O）R，SO 2 NHR或NHS（O）2 R，R 7选自氢，，OR，SR，芳基，取代的芳基，OH，CN，CO2R，CO2H，COR，CONHR，CON（R）2，S（O）2R，SONH2，S（O）R或SO2NHR。

10. 发明公开

EP2311837A1 Azaindoles useful as inhibitors of jak and other protein kinases 有权
标题翻译： Als Inhibitoren von jak und anderen Proteinkinasen geeignete Azaindole
公开(公告)号：EP2311837A1
公开(公告)日：2011-04-20
申请号：EP10182255.9
申请日：2005-03-30
申请人： Vertex Pharmaceuticals Incorporated
发明人： Salituro, Francesco , Farmer, Luc , Bethiel, Randy , Harrington, Edmund , Green, Jeremy , Court, John , Come, Jon , Lauffer, David , Aronov, Alex , Binch, Hayley , Boyall, Dean , Charrier, Jean-Damien , Everitt, Simon , Fraysse, Damien , Mortimore, Michael , Pierard, Francoise , Robinson, Daniel , Pinder, Joanne , Wang, Tiansheng , Pierce, Albert
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/695 , A61K45/06 , C07D519/00 , C07F7/0809
摘要： The present invention relates to compounds of formula (I), which are inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
摘要翻译：本发明涉及作为蛋白激酶抑制剂的式（I）化合物。本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。

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