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1. 发明授权

US08883783B2 Solid forms comprising N-(5-tert-butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea, compositions thereof, and uses therewith 有权
标题翻译：包含N-（5-叔丁基 - 异恶唑-3-基）-N' - {4- [7-（2-吗啉-4-基 - 乙氧基）咪唑并[2,1-b] [1,3] 3]苯并噻唑-2-基]苯基}脲，其组合物及其用途
公开(公告)号：US08883783B2
公开(公告)日：2014-11-11
申请号：US12233906
申请日：2008-09-19
申请人： Shripad S. Bhagwat , Wei Lai , Stephan D. Parent , Melanie J. Roe , Alan Schwartz , Valeriya N. Smolenskaya
发明人： Shripad S. Bhagwat , Wei Lai , Stephan D. Parent , Melanie J. Roe , Alan Schwartz , Valeriya N. Smolenskaya
IPC分类号： A61K31/535 , C07D415/00 , C07D417/00 , C07D513/04
CPC分类号： A61K31/5377 , A61K31/185 , C07D513/04
摘要： Solid forms comprising N-(5-tert-butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed.
摘要翻译：包含N-（5-叔丁基 - 异恶唑-3-基）-N' - {4- [7-（2-吗啉-4-基 - 乙氧基）咪唑并[2,1-b] [1,3] 3]苯并噻唑-2-基]苯基}脲，包含固体形式的组合物，制备固体形式的方法及其用于治疗各种疾病和/或病症的方法。

2. 发明申请

US20090131426A1 SOLID FORMS COMPRISING N-(5-TERT-BUTYL-ISOXAZOL-3-YL)-N'-UREA, COMPOSITIONS THEREOF, AND USES THEREWITH 有权
标题翻译：包含N-（5-叔丁基 - 异唑-3-基）-N'-尿素的固体形式，其组合物及其用途
公开(公告)号：US20090131426A1
公开(公告)日：2009-05-21
申请号：US12233906
申请日：2008-09-19
申请人： Shripad S. Bhagwat , Wei Lai , Stephan D. Parent , Melanie J. Roe , Alan Schwartz , Valeriya N. Smolenskaya
发明人： Shripad S. Bhagwat , Wei Lai , Stephan D. Parent , Melanie J. Roe , Alan Schwartz , Valeriya N. Smolenskaya
IPC分类号： A61K31/5377 , C07D513/04 , A61P35/00
CPC分类号： A61K31/5377 , A61K31/185 , C07D513/04
摘要： Solid forms comprising N-(5-tert-butyl-isoxazol-3-yl)-N′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed.
摘要翻译：包含N-（5-叔丁基 - 异恶唑-3-基）-N' - {4- [7-（2-吗啉-4-基 - 乙氧基）咪唑并[2,1-b] [1,3] 3]苯并噻唑-2-基]苯基}脲，包含固体形式的组合物，制备固体形式的方法及其用于治疗各种疾病和/或病症的方法。

3. 发明授权

US08618289B2 RAF kinase modulator compounds and methods of use thereof 有权
标题翻译： RAF激酶调节剂化合物及其使用方法
公开(公告)号：US08618289B2
公开(公告)日：2013-12-31
申请号：US12933402
申请日：2009-03-17
申请人： Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
发明人： Sunny Abraham , Shripad S. Bhagwat , Brian T. Campbell , Qi Chao , Raffaella Faraoni , Mark W. Holladay , Andiliy G. Lai , Martin W. Rowbottom , Eduardo Setti , Kelly G. Sprankle
IPC分类号： C07D239/70 , A01N43/54
CPC分类号： C07D239/88 , A61K9/20 , A61K9/48 , A61K31/517 , A61K45/06 , C07D239/93 , C07D261/14 , C07D413/12
摘要： Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.
摘要翻译：提供根据式（I）的化合物，组合物和方法用于调节RAF激酶（包括BRAF激酶）的活性，并用于治疗，预防或改善由RAF激酶介导的疾病或病症的一种或多种症状。式（I）：或其药学上可接受的盐，溶剂合物，其水合物的包合物，其中X为O或S（O）t; Ra是O或S.

4. 发明授权

US07119114B1 Pyrazoloanthrone and derivatives thereof as JNK inhibitors and compositions and methods related thereto 失效
标题翻译：吡唑烷酮及其衍生物作为JNK抑制剂及其组合物和方法
公开(公告)号：US07119114B1
公开(公告)日：2006-10-10
申请号：US09642557
申请日：2000-08-18
申请人： Brydon L. Bennett , Shripad S. Bhagwat , Anthony M. Manning , Brion W. Murray , Eoin C. O'Leary , Yoshitaka Satoh
发明人： Brydon L. Bennett , Shripad S. Bhagwat , Anthony M. Manning , Brion W. Murray , Eoin C. O'Leary , Yoshitaka Satoh
IPC分类号： A61K31/416 , C07D231/54
CPC分类号： A61K31/416 , C07D231/54 , C07D401/12 , C07D409/12
摘要： Compounds having activity as selective inhibitors of JNK are disclosed The compounds of this invention are pyrazoloanthrone and derivatives thereof having the following structure: wherein R1 and R2 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
摘要翻译：公开了具有JNK选择性抑制剂活性的化合物。本发明化合物是具有以下结构的吡唑啉酮及其衍生物：其中R 1和R 2 2如本文所定义。这些化合物可用于治疗对JNK抑制作用有响应的广泛范围的病症。因此，还公开了治疗这些病症的方法，以及含有一种或多种上述化合物的化合物的药物组合物。

5. 发明授权

US6143749A Heterocyclic substituted cyclopentane compounds 失效
标题翻译：杂环取代环戊烷化合物
公开(公告)号：US6143749A
公开(公告)日：2000-11-07
申请号：US651882
申请日：1996-06-04
申请人： Shripad S. Bhagwat , Marlon Daniel Cowart
发明人： Shripad S. Bhagwat , Marlon Daniel Cowart
IPC分类号： C07D487/04 , A61K31/00 , A61K31/505 , A61K31/519 , A61K31/529 , A61P9/00 , A61P9/10 , A61P25/08 , A61P29/00 , A61P31/00 , A61P43/00 , C07D471/04 , C07D473/00 , C07F9/6561 , A61K31/40 , A61K31/415
CPC分类号： C07D473/00 , C07D471/04 , C07F9/6561 , Y02P20/55
摘要： The present invention provides new heterocyclic substituted cyclopentane compounds that are useful in inhibiting adenosine kinase. The present invention also provides pharmaceutical compositions containing such compounds and methods of using such compounds for inhibiting adenosine kinase.
摘要翻译：本发明提供了可用于抑制腺苷激酶的新的杂环取代的环戊烷化合物。本发明还提供含有这些化合物的药物组合物和使用这些化合物抑制腺苷激酶的方法。

6. 发明授权

US5670497A Cyclic hydrazine compounds 失效
标题翻译：环肼化合物
公开(公告)号：US5670497A
公开(公告)日：1997-09-23
申请号：US581508
申请日：1996-01-11
申请人： Guido Bold , Shripad S. Bhagwat , Alexander Fassler , Marc Lang
发明人： Guido Bold , Shripad S. Bhagwat , Alexander Fassler , Marc Lang
IPC分类号： A61K31/55 , A61K31/554 , A61P31/12 , A61P31/18 , C07D255/02 , C07D285/36 , C07F9/6584 , A01N43/00 , A61K31/33
CPC分类号： C07D285/36 , C07D255/02 , C07F9/65848
摘要： This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating vital infection.
摘要翻译： PCT No.PCT / EP94 / 02235 Sec。 371日期1996年1月11日 102（e）日期1996年1月11日PCT提交1994年7月7日PCT公布。第WO95 / 02582号公报日期1995年1月26日本发明涉及用作用于包含这些化合物的药物组合物的逆转录病毒蛋白酶抑制剂的取代的环状羰基及其衍生物，以及使用这些化合物治疗重要感染的方法。

7. 发明授权

US07279489B2 Compounds and methods for modulation of estrogen receptors 失效
标题翻译：用于调节雌激素受体的化合物和方法
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。

8. 发明授权

US07129242B2 Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto 失效
标题翻译：苯丙嘧啶衍生物作为JNK途径抑制剂及其组合物和方法
公开(公告)号：US07129242B2
公开(公告)日：2006-10-31
申请号：US10004645
申请日：2001-12-04
申请人： Yoshitaka Satoh , Shripad S. Bhagwat
发明人： Yoshitaka Satoh , Shripad S. Bhagwat
IPC分类号： A61K31/50 , A61K31/497
CPC分类号： C07D239/42 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D487/08 , C07D491/10 , A61K2300/00
摘要： Compounds having activity as inhibitors of the JNK pathway are disclosed. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 through R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to inhibition of the JNK pathway. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
摘要翻译：公开了具有JNK途径抑制剂活性的化合物。本发明的化合物是具有以下结构的苯胺基嘧啶衍生物：其中R 1至R 6如本文所定义。这些化合物可用于治疗对抑制JNK通路有反应的广泛的条件。因此，还公开了治疗这些病症的方法，以及含有一种或多种上述化合物的化合物的药物组合物。

9. 发明授权

US06897231B2 Indazole derivatives as JNK inhibitors and compositions and methods related thereto 失效
标题翻译：作为JNK抑制剂的吲唑衍生物及其相关的组合物和方法
公开(公告)号：US06897231B2
公开(公告)日：2005-05-24
申请号：US09910950
申请日：2001-07-23
申请人： Shripad S. Bhagwat , Yoshitaka Satoh , Steven T. Sakata , Chris A. Buhr , Ronald Albers , John Sapienza , Veronique Plantevin , Qi Chao , Kiran Sahasrabudhe , Rachel Ferri
发明人： Shripad S. Bhagwat , Yoshitaka Satoh , Steven T. Sakata , Chris A. Buhr , Ronald Albers , John Sapienza , Veronique Plantevin , Qi Chao , Kiran Sahasrabudhe , Rachel Ferri
IPC分类号： A61K31/41 , A61K31/416 , A61K31/4178 , A61K31/4184 , A61K31/4196 , A61K31/42 , A61K31/4245 , A61K31/427 , A61K31/4409 , A61K31/4439 , A61K31/4453 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P17/02 , A61P17/08 , A61P19/02 , A61P19/06 , A61P19/08 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/08 , A61P27/16 , A61P29/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/02 , A61P37/06 , C07D231/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/12
CPC分类号： C07D403/12 , C07D231/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/12
摘要： Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure: wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
摘要翻译：公开了具有活性作为JNK的选择性抑制剂的化合物。本发明的化合物是具有以下结构的吲唑衍生物：其中R 1，R 2和A如本文所定义。这些化合物可用于治疗对JNK抑制作用有响应的广泛范围的病症。因此，还公开了治疗这些病症的方法，以及含有一种或多种上述化合物的化合物的药物组合物。

10. 发明授权

US06686351B2 Compounds and methods for modulation of estrogen receptors 失效
标题翻译：用于调节雌激素受体的化合物和方法
公开(公告)号：US06686351B2
公开(公告)日：2004-02-03
申请号：US10085999
申请日：2002-02-27
申请人： Shripad S. Bhagwat , Leah M. Gayo-Fung , Qi Chao
发明人： Shripad S. Bhagwat , Leah M. Gayo-Fung , Qi Chao
IPC分类号： C07D21718
CPC分类号： C07D223/16 , C07D209/44 , C07D217/04 , C07D217/16 , C07D217/18 , C07D217/20 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04
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 modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, 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, natural 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。在一个具体的实施方案中，化合物是针对ER-α的ER-β的选择性调节剂。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，包括优先表达ER-β的细胞和/或组织。更一般地，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，天然荷尔蒙失衡，以及与暴露于环境化学品相关的不良生殖影响。

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