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公开(公告)号：EP2331547B1
公开(公告)日：2014-07-30
申请号：EP09782051.8
申请日：2009-08-20
发明人： BESONG, Gilbert , BRAIN, Christopher Thomas , BROOKS, Clinton A. , CONGREVE, Miles Stuart , DAGOSTIN, Claudio , HE, Guo , HOU, Ying , HOWARD, Steven , LI, Yue , LU, Yipin , MORTENSON, Paul , SMITH, Troy , SUNG, Moo , WOODHEAD, Steven , WRONA, Wojciech , LAGU, Bharat
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , A61K31/519 , C07D487/08
摘要： The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.
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2.发明授权PYRAZOLE DERIVATIVES AND USE THEREOF AS INHIBITORS OF CYCLIN DEPENDENT KINASES 有权PYRAZOLEDERIVATE及其作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：EP2231636B1
公开(公告)日：2011-09-14
申请号：EP08857078.3
申请日：2008-12-08
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D407/14 , A61K31/4439 , A61K31/506 , A61P35/00
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D453/02
摘要： The present application describes organic compounds of formula (I) that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrazole compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.
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3.发明公开PYRAZOLE DERIVATIVES AND USE THEREOF AS INHIBITORS OF CYCLIN DEPENDENT KINASES 有权PYRAZOLEDERIVATE及其作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：EP2231636A1
公开(公告)日：2010-09-29
申请号：EP08857078.3
申请日：2008-12-08
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D407/14 , A61K31/4439 , A61K31/506 , A61P35/00
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D453/02
摘要： The present application describes organic compounds of formula (I) that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrazole compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.
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公开(公告)号：EP2331547A1
公开(公告)日：2011-06-15
申请号：EP09782051.8
申请日：2009-08-20
发明人： BESONG, Gilbert , BRAIN, Christopher Thomas , BROOKS, Clinton A. , CONGREVE, Miles Stuart , DAGOSTIN, Claudio , HE, Guo , HOU, Ying , HOWARD, Steven , LI, Yue , LU, Yipin , MORTENSON, Paul , SMITH, Troy , SUNG, Moo , WOODHEAD, Steven , WRONA, Wojciech
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , A61K31/519 , C07D487/08
摘要： The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.
摘要翻译： 所公开的化合物涉及蛋白激酶相关病症的治疗和治疗。 还需要用于治疗或预防或改善癌症，移植排斥和自身免疫疾病的一种或多种症状的化合物。 此外，需要使用本文提供的化合物来调节蛋白激酶例如CDK1，CDK2，CDK4，CDK5，CDK6，CDK7，CDK8和CDK9的活性的方法。
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公开(公告)号：EP2029145B1
公开(公告)日：2017-01-25
申请号：EP07811927.8
申请日：2007-05-24
IPC分类号： A61K31/519 , A61K31/52 , A61K31/522 , A61P1/00 , A61P3/10 , A61P9/00 , A61P11/06 , A61P15/00 , A61P17/06 , A61P17/00 , A61P19/02 , A61P25/28 , A61P35/00 , A61P35/02 , A61P37/06 , C07D487/04
CPC分类号： A61K31/519 , A61K31/52 , A61K31/522 , C07D487/04
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6.发明授权IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES 有权咪唑衍生物及其作为细胞周期蛋白依赖性激酶的调节剂
公开(公告)号：EP2424843B1
公开(公告)日：2014-03-26
申请号：EP10719772.5
申请日：2010-04-30
发明人： HOWARD, Steven , MORTENSON, Paul Neil , HISCOCK, Steven Douglas , WOOLFORD, Alison Jo-Anne , WOODHEAD, Andrew James , CHESSARI, Gianni , O'REILLY, Marc , CONGREVE, Miles Stuart , DAGOSTIN, Claudio , CHO, Young Shin , YANG, Fan , CHEN, Christine Hiu-Tung , BRAIN, Christopher Thomas , LAGU, Bharat , WANG, Yaping , KIM, Sunkyu , GRIALDES, John , LUZZIO, Michael Joseph , PEREZ, Lawrence Blas , LU, Yipin
IPC分类号： C07D233/22 , C07D235/12 , C07D401/06 , C07D401/10 , C07D401/14 , C07D409/10 , C07D409/14 , C07D413/14 , C07D417/10 , A61K31/4164 , A61K31/4178 , A61P35/00
CPC分类号： C07D471/04 , C07D233/22 , C07D233/24 , C07D235/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D487/04 , C07D519/00
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7.发明公开IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES 有权咪唑衍生物及其作为细胞周期蛋白依赖性激酶的调节剂
公开(公告)号：EP2424843A1
公开(公告)日：2012-03-07
申请号：EP10719772.5
申请日：2010-04-30
发明人： HOWARD, Steven , MORTENSON, Paul Neil , HISCOCK, Steven Douglas , WOOLFORD, Alison Jo-Anne , WOODHEAD, Andrew James , CHESSARI, Gianni , O'REILLY, Marc , CONGREVE, Miles Stuart , DAGOSTIN, Claudio , CHO, Young Shin , YANG, Fan , CHEN, Christine Hiu-Tung , BRAIN, Christopher Thomas , LAGU, Bharat , WANG, Yaping , KIM, Sunkyu , GRIALDES, John , LUZZIO, Michael Joseph , PEREZ, Lawrence Blas , LU, Yipin
IPC分类号： C07D233/22 , C07D235/12 , C07D401/06 , C07D401/10 , C07D401/14 , C07D409/10 , C07D409/14 , C07D413/14 , C07D417/10 , A61K31/4164 , A61K31/4178 , A61P35/00
CPC分类号： C07D471/04 , C07D233/22 , C07D233/24 , C07D235/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D487/04 , C07D519/00
摘要： The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N
+ -O
- or CR
3 ; Y is N, N
+ -O
- or CR
3a ; R
1 and R
2 are independently selected from hydrogen and various substituents as defined in the claims; or R
1 and R
2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R
3 is selected from hydrogen and various substituents; and R
3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of
inter alia proliferative diseases such as cancers.-
公开(公告)号：EP2558092B1
公开(公告)日：2018-06-27
申请号：EP11715370.0
申请日：2011-04-12
申请人： Novartis AG
发明人： BORLAND, Maria , BRAIN, Christopher Thomas , DOSHI, Shivang , KIM, Sunkyu , MA, Jianguo , MURTIE, Josh , ZHANG, Hong
IPC分类号： A61K31/436 , A61K31/519 , A61K45/06 , A61P35/00
CPC分类号： A61K31/519 , A61K31/436 , A61K45/06 , A61K2300/00
摘要： A combination of a CDK4/6 inhibitor and an mTOR inhibitor for the treatment of cancer.
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9.发明公开COMBINATION COMPRISING A CYCLIN DEPENDENT KINASE 4 OR CYCLIN DEPENDENT KINASE (CDK4/6) INHIBITOR AND AN MTOR INHIBITOR FOR TREATING CANCER 有权WITH COMBINATION抑制剂细胞周期蛋白依赖性激酶4或周期蛋白依赖性激酶6（CDK4 / 6）和肿瘤依维莫司治疗
公开(公告)号：EP2558092A1
公开(公告)日：2013-02-20
申请号：EP11715370.0
申请日：2011-04-12
申请人： Novartis AG
发明人： BORLAND, Maria , BRAIN, Christopher Thomas , DOSHI, Shivang , KIM, Sunkyu , MA, Jianguo , MURTIE, Josh , ZHANG, Hong
IPC分类号： A61K31/436 , A61K31/519 , A61K45/06 , A61P35/00
CPC分类号： A61K31/519 , A61K31/436 , A61K45/06 , A61K2300/00
摘要： A combination of a CDK4/6 inhibitor and an mTOR inhibitor for the treatment of cancer.
摘要翻译： 在制备用于治疗癌症的CDK4 / 8抑制剂和mTOR抑制剂的组合。
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公开(公告)号：EP2536727A1
公开(公告)日：2012-12-26
申请号：EP11704225.9
申请日：2011-02-17
申请人： Novartis AG
IPC分类号： C07D487/04 , C07B59/00 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , C07B59/002
摘要： The invention is directed to novel deuterated pyrrolopyrimidine compounds of formula (I) wherein R
1 and R
2 are defined below and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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