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1.发明公开BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE 审中-公开台达P110选择性双环嘧啶，其PI3K抑制化合物及使用方法
公开(公告)号：EP2435438A1
公开(公告)日：2012-04-04
申请号：EP10720979.3
申请日：2010-05-26
发明人： CASTANEDO, Georgette , CHAN, Bryan , GOLDSTEIN, David Michael , KONDRU, Rama K. , LUCAS, Matthew C. , PALMER, Wylie Solang , PRICE, Stephen , SAFINA, Brian , SAVY, Pascal Pierre Alexandre , SEWARD, Eileen Mary , SUTHERLIN, Daniel P. , SWEENEY, Zachary Kevin
IPC分类号： C07D487/04 , C07D491/04 , C07D513/04 , A61K31/519 , A61P35/00 , A61P9/00 , A61P29/00 , A61P25/00
CPC分类号： C07D513/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Formula (I) ((Ia) and (Ib)) compounds wherein (i) X
1 is N and X
2 is S, (ii) X
1 is CR
7 and X
2 is S, (iii) X
1 is N and X
2 is NR
2 , or (iv) X
1 is CR
7 and X
2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula (I) for
in vitro, in situ , and
in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.-
公开(公告)号：EP2427458A1
公开(公告)日：2012-03-14
申请号：EP10719306.2
申请日：2010-04-28
发明人： LUCAS, Matthew C. , THOMAS, Andrew
IPC分类号： C07D413/12
CPC分类号： C07D413/12
摘要： The present invention is concerned with isoxazole-pyridazine derivatives of Formula (I), having affinity and selectivity for GABA A α5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
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公开(公告)号：EP2691399B1
公开(公告)日：2016-07-13
申请号：EP12710724.1
申请日：2012-03-26
发明人： HERMANN, Johannes Cornelius , LOWRIE, JR., Lee Edwin , LUCAS, Matthew C. , LUK, Kin-Chun Thomas , PADILLA, Fernando , WANNER, Jutta , XIE, Wenwei , ZHANG, Xiaohu
IPC分类号： C07D513/04 , A61K31/519 , A61P19/02
CPC分类号： C07D513/04 , A61K45/06
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公开(公告)号：EP2864300A1
公开(公告)日：2015-04-29
申请号：EP13729330.4
申请日：2013-06-17
发明人： GABRIEL, Stephen Deems , HAMILTON, Matthew Michael , LUCAS, Matthew C. , QIAN, Yimin , SIDDURI, Achyutharao
IPC分类号： C07D249/06 , A61K31/4192 , A61P29/00 , A61P37/00
CPC分类号： C07D249/04 , C07D249/06
摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, pulmonary fibrosis...
摘要翻译： 本文提供了式（I）化合物：及其药学上可接受的盐，其中取代基如说明书中公开的那些。 这些化合物和含有它们的药物组合物可用于治疗炎性疾病和病症，例如肺纤维化......
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公开(公告)号：EP2763990A1
公开(公告)日：2014-08-13
申请号：EP12761923.7
申请日：2012-08-27
发明人： CHEN, Shaoqing , DE VICENTE FIDALGO, Javier , HAMILTON, Matthew Michael , HERMANN, Johannes Cornelius , KENNEDY-SMITH, Joshua , LI, Hongju , LOVEY, Allen John , LUCAS, Matthew C. , LUK, Kin-Chun Thomas , LYNCH, Stephen M. , O'YANG, Counde , PADILLA, Fernando , SCHOENFELD, Ryan Craig , SIDDURI, Achyutharao , SOTH, Michael , WANG, Ce , WOVKULICH, Peter Michael , ZHANG, Xiaohu
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/5025 , A61P29/00
CPC分类号： C07D487/04
摘要： The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译： 本发明涉及式I的新型吡咯并吡嗪衍生物的用途，其中变量如本文所述定义，其抑制JAK和SYK并可用于治疗自身免疫和炎性疾病。
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公开(公告)号：EP2427457B1
公开(公告)日：2013-07-17
申请号：EP10715849.5
申请日：2010-04-28
IPC分类号： C07D413/12 , C07D413/14 , A61K31/4439 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14
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7.发明公开PYRIDO[3,2-D]PYRIMIDINE PI3K DELTA INHIBITOR COMPOUNDS AND METHODS OF USE 审中-公开吡啶并[3,2-d]嘧啶的PI3Kδ抑制剂的化合物及其使用方法
公开(公告)号：EP2539337A1
公开(公告)日：2013-01-02
申请号：EP11704604.5
申请日：2011-02-18
发明人： CASTANEDO, Georgette , CHAN, Bryan , LUCAS, Matthew C. , SAFINA, Brian , SUTHERLIN, Daniel P. , SWEENEY, Zachary Kevin
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04 , C07D491/107
摘要： Formula (I) compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula (I) for
in vitro, in situ, and
in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.-
公开(公告)号：EP2427458B1
公开(公告)日：2014-05-07
申请号：EP10719306.2
申请日：2010-04-28
发明人： LUCAS, Matthew C. , THOMAS, Andrew
IPC分类号： C07D413/12 , A61K31/501 , A61P25/00 , A61P25/18 , A61P25/28 , A61P25/30
CPC分类号： C07D413/12
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公开(公告)号：EP2427457A1
公开(公告)日：2012-03-14
申请号：EP10715849.5
申请日：2010-04-28
IPC分类号： C07D413/12 , C07D413/14 , A61K31/4439 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14
摘要： The present invention is concerned with novel isoxazole derivatives of formula (I) wherein X, R
1 , R
2 , R
3 and R
4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A α5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula (I), pharmaceutical compositions containing them and their use as medicaments.摘要翻译： 本发明涉及式（I）的新异唑衍生物及其药学上可接受的盐和酯，其中X，R 1，R 2，R 3和R 4如本文所述。 本发明的活性化合物对GABA Aα5受体具有亲和性和选择性。 此外，本发明涉及式（I）的活性化合物，含有它们的药物组合物以及它们作为药物的用途的制备。
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公开(公告)号：EP2888262A1
公开(公告)日：2015-07-01
申请号：EP13750700.0
申请日：2013-08-19
发明人： HERMANN, Johannes Cornelius , KENNEDY-SMITH, Joshua , LUCAS, Matthew C. , PADILLA, Fernando , SCHOENFELD, Ryan Craig , WOVKULICH, Peter Michael
IPC分类号： C07D487/04 , A61K31/4985 , A61P37/00 , A61P37/06 , A61P35/00 , A61P25/28 , A61P3/10 , C07D519/00
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/506 , A61K45/06 , C07D471/04 , C07D519/00
摘要： The present invention relates to the use of novel pyrrolo[2,3-b]]pyrazines wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
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