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1.发明授权THIOPHENES AND THEIR USE AS PHOSPHATIDYLINOSITOL 3-KINASE (PI3K) INHIBITORS 有权噻吩衍生物及它们作为磷脂酰肌醇3-激酶（PI3K）抑制剂的用途
公开(公告)号：EP2250160B1
公开(公告)日：2015-11-11
申请号：EP09703864.0
申请日：2009-01-26
IPC分类号： C07D333/38 , C07D333/40 , C07D409/04 , C07D409/12 , C07D417/12 , A61K31/381 , A61K31/4436 , A61K31/4155 , A61K31/433 , A61K31/4535 , A61K31/397 , A61K31/4025 , A61P35/00
CPC分类号： C07D409/04 , C07D333/38 , C07D333/40 , C07D409/12 , C07D417/12
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2.发明授权5,7-DIHYDRO-6H-PYRIMIDO[5,4-D][1]BENZAZEPIN-6-THIONES AS PLK INHIBITORS 有权5,7-二氢-6H-吡啶并[5,4-D] [1]苯并嗪-6-THIONE ALS PLK INHIBITOREN
公开(公告)号：EP2373657B1
公开(公告)日：2016-09-14
申请号：EP09795577.7
申请日：2009-12-04
发明人： BHARATHAN, Indu, T. , DUFFEY, Matthew, O. , ELDER, Amy, M. , GUO, Jianping , LI, Gang , REYNOLDS, Dominic , SOUCY, Francois , VOS, Tricia, J.
IPC分类号： A61N5/10 , C07D213/75 , C07D215/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D471/04 , C07D487/04 , A61K31/55
CPC分类号： C07D213/75 , A61K31/55 , A61N5/10 , C07D215/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D471/04 , C07D487/04
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3.发明公开HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF SUMO ACTIVATING ENZYME 有权HETEROARYLVERBINDUNGEN ALS HEMMER DES SUMO-AKTIVIERENDEN ENZYMS
公开(公告)号：EP3016934A2
公开(公告)日：2016-05-11
申请号：EP14819587.8
申请日：2014-07-01
发明人： DUFFEY, Matthew, O. , ENGLAND, Dylan, B. , HU, Zhigen , ITO, Mitsuhiro , LANGSTON, Steven, P. , MCINTYRE, Charles , MIZUTANI, Hirotake , XU, He
IPC分类号： C07D239/48
CPC分类号： C07D403/06 , A61K31/505 , A61K31/506 , C07D239/28 , C07D401/06 , C07D401/14 , C07D403/14 , C07D405/14
摘要： Disclosed are compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein Y, R
a , R
a' , R
c , R
f , X
2 , R
d , R
d' , R
e , R
e' , m, and G have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry, useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular and neurodegenerative diseases or disorders.摘要翻译： 公开了式（I）的化合物; 或其药学上可接受的盐; 其中Y，Ra，Ra'，Rc，Rf，X2，Rd，Rd'，Re，Re'2，m和G具有本文所述的值，并且在星号位置处描绘的立体化学构型表示绝对立体化学，可用作Sumo的抑制剂 活化酶（SAE）。 还提供了包含本公开的化合物和使用该组合物治疗增殖性，炎性，心血管和神经变性疾病或病症的方法的药物组合物。
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公开(公告)号：EP2793894A1
公开(公告)日：2014-10-29
申请号：EP12859082.5
申请日：2012-12-20
发明人： CHAU, Ryan, W. , CULLIS, Courtney, A. , DUFFEY, Matthew, O. , GIPSON, Krista, E. , HU, Yongbo , LI, Gang , SINTCHAK, Michael, D. , VOS, Tricia, J.
IPC分类号： A61K31/535
CPC分类号： C07D401/14 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06 , C07D207/416 , C07D401/04 , C07D403/04 , C07D417/14 , C07D471/04 , C07D471/14 , A61K2300/00
摘要： This invention provides compounds of formula IA: and also provides compounds of formula IIA, IIIA, IVA, or VA: wherein HY, R
1 , R
2 , R
3 , R
14 , G
1 , G
2 , G
3 and G
4 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.-
5.发明公开THIOPHENES AND THEIR USE AS PHOSPHATIDYLINOSITOL 3-KINASE (PI3K) INHIBITORS 有权噻吩衍生物及它们作为磷脂酰肌醇3-激酶（PI3K）抑制剂的用途
公开(公告)号：EP2250160A1
公开(公告)日：2010-11-17
申请号：EP09703864.0
申请日：2009-01-26
IPC分类号： C07D333/38 , C07D333/40 , C07D409/04 , C07D409/12 , C07D417/12 , A61K31/381 , A61K31/4436 , A61K31/4155 , A61K31/433 , A61K31/4535 , A61K31/397 , A61K31/4025 , A61P35/00
CPC分类号： C07D409/04 , C07D333/38 , C07D333/40 , C07D409/12 , C07D417/12
摘要： This invention provides thiophene compounds of formula (I) : wherein R1, R2, R3, R4, n, p, and m are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
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公开(公告)号：EP2793880A1
公开(公告)日：2014-10-29
申请号：EP12860844.5
申请日：2012-12-20
发明人： CHAU, Ryan, W. , CULLIS, Courtney, A. , DUFFEY, Matthew, O. , GIPSON, Krista, E. , HU, Yongbo , LI, Gang , SINTCHAK, Michael, D. , VOS, Tricia, J.
IPC分类号： A61K31/40 , A61K31/415
CPC分类号： C07D401/14 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06 , C07D207/416 , C07D401/04 , C07D403/04 , C07D417/14 , C07D471/04 , C07D471/14 , A61K2300/00
摘要： This invention provides compounds of formula IB and also provides compounds of formulas ID, IIB, VB, and IIC. wherein HY, R
1 , R
2 , G
5 , G
6 , G
7 , G
8 , and G
9 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.-
公开(公告)号：EP2793879A1
公开(公告)日：2014-10-29
申请号：EP12859324.1
申请日：2012-12-20
发明人： CHAU, Ryan, W. , CULLIS, Courtney, A. , DUFFEY, Matthew, O. , GIPSON, Krista, E. , HU, Yongbo , LI, Gang , SINTCHAK, Michael, D. , STROUD, Steven, G. , VOS, Tricia, J.
IPC分类号： A61K31/40 , A61K31/415
CPC分类号： C07D401/14 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06 , C07D207/416 , C07D401/04 , C07D403/04 , C07D417/14 , C07D471/04 , C07D471/14 , A61K2300/00
摘要： This invention provides compounds of formula IB: (lB) wherein HY, R
1 , R
2, R
3, R
15 , G
5 , G
6 , G
7 , G
8 , and G
9 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.摘要翻译： 本发明提供了式IB化合物：其中HY，R 1，R 2，R 3，R 15，G 5，G 6，G 7，G 8和G 9如说明书中所述。 该化合物是VPS34和/或PI3K的抑制剂，因此可用于治疗增殖性，炎症或心血管疾病。
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8.发明公开5, 7-DIHYDRO- 6H-PYRIMIDO Ý 5, 4-D¨Ý 1¨BENZAZEPIN-6-THIONES AS PLK INHIBITORS 有权5,7-二氢-6H-嘧啶并[5,4-D] [1]苯并氮杂_-6-硫酮AS PLK抑制剂
公开(公告)号：EP2373657A1
公开(公告)日：2011-10-12
申请号：EP09795577.7
申请日：2009-12-04
发明人： BHARATHAN, Indu, T. , DUFFEY, Matthew, O. , ELDER, Amy, M. , GUO, Jianping , LI, Gang , REYNOLDS, Dominic , SOUCY, Francois , VOS, Tricia, J.
IPC分类号： C07D487/04 , A61K31/55 , A61P35/00
CPC分类号： C07D213/75 , A61K31/55 , A61N5/10 , C07D215/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D471/04 , C07D487/04
摘要： This invention provides compounds of formula I: wherein R
1 , R
2 , R
3 , R
4 , R
5 , and R
6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
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