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![Substituted 7,8,9,10-tetrahydro-5H-dipyrido[1,2-a:3′,2′-e]pyrazin-6(6aH)-ones](/abs-image/US/2012/02/28/US08124606B2/abs.jpg.150x150.jpg)
21.发明授权Substituted 7,8,9,10-tetrahydro-5H-dipyrido[1,2-a:3′,2′-e]pyrazin-6(6aH)-ones 有权取代的7,8,9,10-四氢-5H-二吡啶并[1,2-a：3'，2'-e]吡嗪-6（6aH） - 酮公开(公告)号：US08124606B2
公开(公告)日：2012-02-28
申请号：US13041200
申请日：2011-03-04
IPC分类号： A61K31/495
CPC分类号： C07D513/14 , A61K31/4985 , A61K31/506 , A61K31/53 , A61K31/5383 , A61K31/542 , A61K31/5517 , A61K31/635 , A61K45/06 , C07D471/04 , C07D471/14 , C07D498/14
摘要： Disclosed are compounds of the following formula: in which R1, R2, R5, R6, R7, R11, X, and m are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
摘要翻译： 公开了下式的化合物：其中R 1，R 2，R 5，R 6，R 7，R 11，X和m在说明书中定义。 还公开了含有可用于制备化合物的化合物，方法和中间体的药物组合物，试剂盒和制品，以及使用该化合物治疗与PARP活性相关的疾病，病症和病症的方法。
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公开(公告)号：US20090312288A1
公开(公告)日：2009-12-17
申请号：US12425249
申请日：2009-04-16
申请人： Jason W. Brown , Qing Dong , Anthony R. Gangloff , Bheema R. Paraselli , Nicholas Scorah , Jeffrey A. Stafford , Sanjib Das , Jonathon S. Salsbury
发明人： Jason W. Brown , Qing Dong , Anthony R. Gangloff , Bheema R. Paraselli , Nicholas Scorah , Jeffrey A. Stafford , Sanjib Das , Jonathon S. Salsbury
IPC分类号： A61K31/437 , C07D471/04 , C07D413/14 , C07D417/14 , A61K31/5377 , A61K31/541 , A61K31/675 , A61P25/28 , A61P35/00 , A61P19/02
CPC分类号： C07D471/04 , C07F9/6561
摘要： Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
摘要翻译： 提供化合物用于与包含选自以下的化合物的激酶一起使用：其中变量如本文所定义。 还提供了包含这些化合物的药物组合物，试剂盒和制品; 用于制备化合物的方法和中间体; 以及使用所述化合物的方法。
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公开(公告)号：US07550598B2
公开(公告)日：2009-06-23
申请号：US11208437
申请日：2005-08-18
申请人： Sheldon X. Cao , Anthony R. Gangloff , Bheema R. Paraselli , Jeffrey A. Stafford , Hasanthi P. Wijesekera
发明人： Sheldon X. Cao , Anthony R. Gangloff , Bheema R. Paraselli , Jeffrey A. Stafford , Hasanthi P. Wijesekera
IPC分类号： C07D215/38 , A61K38/40
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： Compounds, pharmaceutical compositions, kits and methods are provided for use with kinases that comprise a compound of the formula: wherein R1, R2, R3, Q, U, V, W, X, and Y are as defined herein.
摘要翻译： 提供化合物，药物组合物，试剂盒和方法用于包含下式化合物的激酶：其中R 1，R 2，R 3，Q，U，V，W，X和Y如本文所定义。
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![Substituted derivatives of pyrido[3,2-e][1,4]thiazino[4,3-a]pyrazine and pyrido[3,2-e][1,4]oxazino[4,3-a]pyrazine](/abs-image/US/2013/05/28/US08450323B2/abs.jpg.150x150.jpg)
24.发明授权Substituted derivatives of pyrido[3,2-e][1,4]thiazino[4,3-a]pyrazine and pyrido[3,2-e][1,4]oxazino[4,3-a]pyrazine 有权吡啶并[3,2-e] [1,4]噻嗪并[4,3-a]吡嗪和吡啶并[3,2-e] [1,4]恶嗪并[4,3-a]吡嗪的取代衍生物公开(公告)号：US08450323B2
公开(公告)日：2013-05-28
申请号：US13352902
申请日：2012-01-18
IPC分类号： A61K31/495
CPC分类号： C07D513/14 , A61K31/4985 , A61K31/506 , A61K31/53 , A61K31/5383 , A61K31/542 , A61K31/5517 , A61K31/635 , A61K45/06 , C07D471/04 , C07D471/14 , C07D498/14
摘要： Disclosed are compounds of the following formula: in which R1, R2, R6, R7, R12, X, and q are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
摘要翻译： 公开了下式的化合物：其中R1，R2，R6，R7，R12，X和q在本说明书中定义。 还公开了含有可用于制备化合物的化合物，方法和中间体的药物组合物，试剂盒和制品，以及使用该化合物治疗与PARP活性相关的疾病，病症和病症的方法。
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公开(公告)号：US20120122835A1
公开(公告)日：2012-05-17
申请号：US13352902
申请日：2012-01-18
IPC分类号： A61K31/4985 , C07D403/14 , A61K31/53 , C07D471/04 , C07D513/14 , A61K31/542 , C07D498/14 , A61K31/5383 , A61K31/397 , C07D487/14 , A61K31/551 , A61P35/00 , A61P9/00 , A61P3/00 , A61P29/00 , A61P9/10 , A61P25/28 , C07D471/14
CPC分类号： C07D513/14 , A61K31/4985 , A61K31/506 , A61K31/53 , A61K31/5383 , A61K31/542 , A61K31/5517 , A61K31/635 , A61K45/06 , C07D471/04 , C07D471/14 , C07D498/14
摘要： Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
摘要翻译： 公开了下式的化合物：其中R1，R2，R3，R4，R5，R6，R7，X和t在本说明书中定义。 还公开了含有可用于制备化合物的化合物，方法和中间体的药物组合物，试剂盒和制品，以及使用该化合物治疗与PARP活性相关的疾病，病症和病症的方法。
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公开(公告)号：US20110158989A1
公开(公告)日：2011-06-30
申请号：US13041200
申请日：2011-03-04
IPC分类号： A61K39/395 , C07D487/14 , C07D279/10 , C07D471/14 , A61K31/551 , A61K31/4985 , A61K31/542 , A61P35/00
CPC分类号： C07D513/14 , A61K31/4985 , A61K31/506 , A61K31/53 , A61K31/5383 , A61K31/542 , A61K31/5517 , A61K31/635 , A61K45/06 , C07D471/04 , C07D471/14 , C07D498/14
摘要： Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
摘要翻译： 公开了下式的化合物：其中R1，R2，R3，R4，R5，R6，R7，X和t在本说明书中定义。 还公开了含有可用于制备化合物的化合物，方法和中间体的药物组合物，试剂盒和制品，以及使用该化合物治疗与PARP活性相关的疾病，病症和病症的方法。
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公开(公告)号：US07279489B2
公开(公告)日：2007-10-09
申请号：US10434341
申请日：2003-05-07
申请人： Shripad S. Bhagwat , Leah Marie Gayo-Fung , Bernd M. Stein , Qi Chao , Anthony R. Gangloff , Jeffrey A. McKie , Kenneth D. Rice
发明人： Shripad S. Bhagwat , Leah Marie Gayo-Fung , Bernd M. Stein , Qi Chao , Anthony R. Gangloff , Jeffrey A. McKie , Kenneth D. Rice
IPC分类号： A61P35/00 , A61K31/47 , C07D217/00
CPC分类号： C07D223/16 , C07D209/44 , C07D217/04 , C07D217/16 , C07D217/18 , C07D217/20 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/04 , C07D405/12 , C07D413/10 , C07D417/12
摘要： Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective for ER-β over ER-α. Methods are disclosed for modulating ER-β in cell and/or tissues expressing the same, including cells and/or tissue that preferentially ER-β. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
摘要翻译： 公开了调节雌激素受体（ER）的化合物以及含有它们的药物组合物。 在一个具体实施方案中，化合物对ER-β对ER-α是选择性的。 公开了用于在表达其中的细胞和/或组织中调节ER-β的方法，包括优先ER-β的细胞和/或组织。 还公开了治疗雌激素相关病症的方法，包括诸如乳腺癌，睾丸癌，骨质疏松症，子宫内膜异位症，心血管疾病，高胆固醇血症，前列腺肥大，前列腺癌，肥胖症，潮热，皮肤效应，情绪波动，记忆丧失 ，尿失禁，脱发，白内障，自然激素失衡和与暴露于环境化学物质相关的不良生殖影响。
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公开(公告)号：US20150031652A1
公开(公告)日：2015-01-29
申请号：US14450101
申请日：2014-08-01
IPC分类号： C07D513/14 , A61K31/4985 , A61K31/506 , A61K31/53 , A61K31/635 , A61K31/542 , C07D498/14 , A61K31/5383 , A61K31/5517 , C07D471/14 , C07D471/04
CPC分类号： C07D513/14 , A61K31/4985 , A61K31/506 , A61K31/53 , A61K31/5383 , A61K31/542 , A61K31/5517 , A61K31/635 , A61K45/06 , C07D471/04 , C07D471/14 , C07D498/14
摘要： Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
摘要翻译： 公开了下式的化合物：其中R1，R2，R3，R4，R5，R6，R7，X和t在本说明书中定义。 还公开了含有可用于制备化合物的化合物，方法和中间体的药物组合物，试剂盒和制品，以及使用该化合物治疗与PARP活性相关的疾病，病症和病症的方法。
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公开(公告)号：US20120129868A1
公开(公告)日：2012-05-24
申请号：US13387342
申请日：2010-07-29
IPC分类号： A61K31/519 , A61P35/00 , A61P25/28 , A61P3/00 , A61P29/00 , A61P9/10 , C07D471/14 , A61P9/00
CPC分类号： C07D471/14
摘要： Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.
摘要翻译： 提供下式的化合物用于PARP：其中变量如本文所定义。 还提供了包含这种化合物的药物组合物，试剂盒和制品，用于制备化合物的方法和中间体，以及使用该化合物的方法。
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![Substituted 6a,7,8,9-tetrahydropyrido[3,2-e]pyrrolo[1,2-a]pyrazin-6(5H)-ones](/abs-image/US/2011/04/19/US07928105B2/abs.jpg.150x150.jpg)
30.发明授权Substituted 6a,7,8,9-tetrahydropyrido[3,2-e]pyrrolo[1,2-a]pyrazin-6(5H)-ones 有权取代的6a，7,8,9-四氢吡啶并[3,2-e]吡咯并[1,2-a]吡嗪-6（5H） - 酮公开(公告)号：US07928105B2
公开(公告)日：2011-04-19
申请号：US12691668
申请日：2010-01-21
IPC分类号： A61K31/495
CPC分类号： C07D513/14 , A61K31/4985 , A61K31/506 , A61K31/53 , A61K31/5383 , A61K31/542 , A61K31/5517 , A61K31/635 , A61K45/06 , C07D471/04 , C07D471/14 , C07D498/14
摘要： Disclosed are compounds of the following formula: in which R1, R2, R5, R6, R7, R31, u, and X are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
摘要翻译： 公开了下式的化合物：其中R1，R2，R5，R6，R7，R31，u和X在本说明书中定义。 还公开了含有可用于制备化合物的化合物，方法和中间体的药物组合物，试剂盒和制品，以及使用该化合物治疗与PARP活性相关的疾病，病症和病症的方法。
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