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51.发明申请3-SUBSTITUTED-5- AND 6-AMINOALKYL INDOLE-2-CARBOXYLIC ACID AMIDES AND RELATED ANALOGS AS INHIBITORS OF CASEIN KINASE I 有权3-取代的5-和6-氨基烷基吲哚-2-羧酸和作为CASEIN KINASE I的抑制剂的相关模拟物公开(公告)号：US20090082340A1
公开(公告)日：2009-03-26
申请号：US12269216
申请日：2008-11-12
IPC分类号： A61K31/404 , A61K31/454 , A61K31/5377 , A61K31/506 , A61K31/551 , A61K31/496 , A61K31/438 , A61P25/00
CPC分类号： C07D491/10 , C07D209/42 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14
摘要： The present invention discloses and claims methods for the treatment of a patient suffering from a disease or disorder ameliorated by inhibition of casein kinase Iε activity comprising the administration of a compounds of formula (I) and formula (II) as inhibitors of human casein kinase Iε, and methods of using said compounds of formula (I) and formula (II) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. The R-group substituents are defined herein and pharmaceutical compositions comprising compounds of formula (I) or formula (II) useful in the claimed methods of treatment are also disclosed.
摘要翻译： 本发明公开并说明了治疗患有通过抑制酪蛋白激酶Iepsilon活性而改善的疾病或病症的患者的方法，其包括施用式（I）和式（II）化合物作为人酪蛋白激酶Iepsilon的抑制剂 以及使用所述式（I）和式（II）化合物治疗中枢神经系统疾病和病症（包括情绪障碍和睡眠障碍）的方法。 R基取代基在本文中定义，并且也公开了包含用于所要求保护的治疗方法的式（I）或式（II）化合物的药物组合物。
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52.发明申请Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment 审中-公开烟酸受体激动剂，包含这些化合物的组合物和治疗方法公开(公告)号：US20120178750A1
公开(公告)日：2012-07-12
申请号：US13423618
申请日：2012-03-19
申请人： Subharekha Raghavan , Steven L. Colletti , Fa-Xiang Ding , Hong Shen , James R. Tata , Ashley Rouse Lins , Abigail Lee Smenton , Weichun Chen , Darby Rye Schmidt , George Scott Tria
发明人： Subharekha Raghavan , Steven L. Colletti , Fa-Xiang Ding , Hong Shen , James R. Tata , Ashley Rouse Lins , Abigail Lee Smenton , Weichun Chen , Darby Rye Schmidt , George Scott Tria
IPC分类号： A61K31/4439 , A61K31/423 , A61K31/429 , A61K31/41 , A61K31/426 , A61K31/427 , A61K31/403 , A61K31/4375 , A61K31/437 , A61K31/538 , A61K31/4196 , A61P9/10 , A61P3/06 , A61P3/10 , A61P3/00 , A61K31/196
CPC分类号： C07D261/20 , C07C233/52 , C07C233/55 , C07C235/36 , C07C237/20 , C07C2601/10 , C07C2601/16 , C07D231/12 , C07D249/06 , C07D249/08 , C07D257/04 , C07D271/06 , C07D277/30 , C07D307/79 , C07D309/14 , C07D309/28 , C07D401/04 , C07D413/04 , C07D417/04 , C07D513/04
摘要： The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括可用于治疗动脉粥样硬化，血脂异常等的式I化合物及其药学上可接受的盐和水合物。 还包括药物组合物和使用方法。
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53.发明授权3-substituted-5- and 6-aminoalkyl indole-2-carboxylic acid amides and related analogs as inhibitors of casein kinase I 有权3-取代-5-和6-氨基烷基吲哚-2-羧酸酰胺和相关类似物作为酪蛋白激酶I的抑制剂公开(公告)号：US07923466B2
公开(公告)日：2011-04-12
申请号：US12269216
申请日：2008-11-12
IPC分类号： A61K31/404
CPC分类号： C07D491/10 , C07D209/42 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14
摘要： Methods for the treatment of a patient suffering from a disease or disorder ameliorated by inhibition of casein kinase Iε activity comprising the administration of a compounds of formula (I) and formula (II) as inhibitors of human casein kinase Iε, and methods of using the compounds of formula (I) and formula (II) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. The R-group substituents are defined herein and pharmaceutical compositions comprising compounds of formula (I) or formula (II) useful in the claimed methods of treatment are also disclosed.
摘要翻译： 用于治疗患有通过抑制酪蛋白激酶I改变的疾病或病症的患者的方法; 包括施用式（I）和式（II）化合物作为人酪蛋白激酶I的抑制剂的活性;以及使用式（I）和式（II）化合物治疗中枢神经系统疾病和病症的方法 包括情绪障碍和睡眠障碍。 R基取代基在本文中定义，并且也公开了包含用于所要求保护的治疗方法的式（I）或式（II）化合物的药物组合物。
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54.发明申请Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment 审中-公开烟酸受体激动剂，包含这些化合物的组合物和治疗方法公开(公告)号：US20070299101A1
公开(公告)日：2007-12-27
申请号：US11666966
申请日：2005-10-31
申请人： Steven Colletti , Richard Beresis , Weichun Chen , James Tata , Hong Shen , Daria Marley , Qiaolin Deng , Jessica Frie , Fa-Xiang Ding
发明人： Steven Colletti , Richard Beresis , Weichun Chen , James Tata , Hong Shen , Daria Marley , Qiaolin Deng , Jessica Frie , Fa-Xiang Ding
IPC分类号： A61K31/47 , A61K31/195 , A61K31/403 , A61K31/41 , A61P3/10 , C07C233/64 , C07D215/02 , C07D257/04 , C07D487/00 , C07D513/00 , C07D471/02 , C07D217/00 , C07D209/56 , A61P9/00 , A61K31/425 , A61K31/428 , A61K31/437
CPC分类号： C07C233/55 , C07C235/38 , C07C237/20 , C07C237/22 , C07C255/57 , C07C259/10 , C07C271/30 , C07C271/58 , C07C275/42 , C07C311/08 , C07C311/13 , C07D213/80 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/227 , C07D215/38 , C07D217/02 , C07D217/24 , C07D231/54 , C07D231/56 , C07D235/30 , C07D257/04 , C07D261/20 , C07D277/82 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to niacin receptor agonists of formula: (I); as well as pharmaceutically acceptable salts and solvates. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译： 本发明涉及式（I）的烟酸受体激动剂： 以及药学上可接受的盐和溶剂合物。 该化合物可用于治疗血脂异常，特别是降低血清LDL，VLDL和甘油三酸酯，并提高HDL水平。 还包括药物组合物和治疗方法。
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55.发明申请SOLUBLE EPOXIDE HYDROLASE INHIBITORS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT 有权可溶性环氧化物水解酶抑制剂，含有这些化合物的组合物和处理方法公开(公告)号：US20100197691A1
公开(公告)日：2010-08-05
申请号：US12668494
申请日：2008-07-11
申请人： Steven L. Colletti , Hong Shen , Fa-Xiang Ding
发明人： Steven L. Colletti , Hong Shen , Fa-Xiang Ding
IPC分类号： A61K31/498 , A61K31/47 , A61K31/4545 , A61K31/454 , A61K31/445 , C07D401/12 , C07D211/40 , A61P3/10
CPC分类号： C07D211/22 , C07D211/16 , C07D211/34 , C07D401/06 , C07D401/12 , C07D413/06 , C07D413/12 , C07D417/12
摘要： Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 公开了可用于治疗高血压，糖尿病，炎症，动脉粥样硬化，疼痛等的式（I）化合物及其药学上可接受的盐和水合物。 还包括药物组合物和使用方法。
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56.发明申请Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment 有权烟酸受体激动剂，包含这些化合物的组合物和治疗方法公开(公告)号：US20100144778A1
公开(公告)日：2010-06-10
申请号：US11922629
申请日：2006-06-26
申请人： Subharekha Raghavan , Steven L. Colletti , Fa-Xiang Ding , Hong Shen , James R. Tata , Ashley Rouse Lins , Abigail Lee Smenton , Weichun Chen , Darby Rye Schmidt , George Scott Tria
发明人： Subharekha Raghavan , Steven L. Colletti , Fa-Xiang Ding , Hong Shen , James R. Tata , Ashley Rouse Lins , Abigail Lee Smenton , Weichun Chen , Darby Rye Schmidt , George Scott Tria
IPC分类号： A61K31/437 , C07C233/02 , C07C229/38 , C07D413/04 , C07D513/04 , C07D471/14 , A61K31/165 , A61K31/192 , A61K31/4439 , A61K31/4245 , A61P9/10
CPC分类号： C07D261/20 , C07C233/52 , C07C233/55 , C07C235/36 , C07C237/20 , C07C2601/10 , C07C2601/16 , C07D231/12 , C07D249/06 , C07D249/08 , C07D257/04 , C07D271/06 , C07D277/30 , C07D307/79 , C07D309/14 , C07D309/28 , C07D401/04 , C07D413/04 , C07D417/04 , C07D513/04
摘要： The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括可用于治疗动脉粥样硬化，血脂异常等的式（I）化合物及其药学上可接受的盐和水合物。 还包括药物组合物和使用方法。
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57.发明申请Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment 审中-公开烟酸受体激动剂，包含这些化合物的组合物和治疗方法公开(公告)号：US20070281969A1
公开(公告)日：2007-12-06
申请号：US11791183
申请日：2005-11-18
申请人： Steven Colletti , James Tata , Hong Shen , Fa-Xiang Ding , Jessica Frie , Jason Imbriglio , Weichun Chen
发明人： Steven Colletti , James Tata , Hong Shen , Fa-Xiang Ding , Jessica Frie , Jason Imbriglio , Weichun Chen
IPC分类号： A61K31/192 , A61K31/47 , A61P3/00 , A61P9/10 , C07C229/40 , C07D215/12
CPC分类号： C07D217/02 , C07C233/55 , C07C235/38 , C07C317/44 , C07D209/08 , C07D209/88 , C07D209/94 , C07D213/56 , C07D213/61 , C07D213/64 , C07D213/65 , C07D213/80 , C07D215/12 , C07D231/12 , C07D231/56 , C07D239/26 , C07D261/08 , C07D271/113 , C07D277/30 , C07D307/54 , C07D307/79 , C07D317/60 , C07D333/24 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/14
摘要： The present invention encompasses compounds of Formula (I); as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating dyslipidemias. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括式（I）的化合物; 以及其药学上可接受的盐和水合物，其可用于治疗血脂异常。 还包括药物组合物和使用方法。
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公开(公告)号：US09284301B2
公开(公告)日：2016-03-15
申请号：US13636760
申请日：2011-03-22
申请人： Darby Schmidt , Subharekha Raghavan , John Stelmach , Jian Guo , Jonathan Groeper , Linda Brockunier , Keith Rosauer , Hong Shen , Rui Liang , Fa-Xiang Ding
发明人： Darby Schmidt , Subharekha Raghavan , John Stelmach , Jian Guo , Jonathan Groeper , Linda Brockunier , Keith Rosauer , Hong Shen , Rui Liang , Fa-Xiang Ding
IPC分类号： C07D403/14 , C07D401/14 , C07D403/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
CPC分类号： C07D403/14 , C07D401/14 , C07D403/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.
摘要翻译： 本发明涉及具有式（I）结构的化合物及其药学上可接受的盐，它们是可溶性鸟苷酸环化酶活化剂。 这些化合物能够调节人体的环鸟苷酸（“cGMP”）的产生，并且通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病。 该化合物可用于治疗或预防心血管疾病，内皮功能障碍，舒张功能障碍，动脉粥样硬化，高血压，肺动脉高压，心绞痛，血栓形成，再狭窄，心肌梗死，中风，心功能不全，肺性高血压，勃起功能障碍，支气管哮喘，慢性 肾功能不全，糖尿病或肝硬化。
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公开(公告)号：US20130012511A1
公开(公告)日：2013-01-10
申请号：US13636760
申请日：2011-03-22
申请人： Darby Schmidt , Subharekha Raghavan , John Stelmach , Jian Guo , Jonathan Groeper , Linda Brockunier , Keith Rosauer , Hong Shen , Rui Liang , Fa-Xiang Ding
发明人： Darby Schmidt , Subharekha Raghavan , John Stelmach , Jian Guo , Jonathan Groeper , Linda Brockunier , Keith Rosauer , Hong Shen , Rui Liang , Fa-Xiang Ding
IPC分类号： C07D403/14 , A61K31/506 , C07D471/04 , C07D401/14 , C07D413/14 , A61K31/5377 , C07D417/14 , C07D403/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P9/04 , A61P7/02 , A61P11/00 , A61P15/00 , A61P11/06 , A61P13/12 , A61P3/10 , A61P1/16 , A61P9/08 , A61P7/10 , A61P3/00 , A61P3/06 , C07D487/04
CPC分类号： C07D403/14 , C07D401/14 , C07D403/04 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.
摘要翻译： 本发明涉及具有式（I）结构的化合物及其药学上可接受的盐，它们是可溶性鸟苷酸环化酶活化剂。 这些化合物能够调节身体产生的环鸟苷酸（cGMP），通常适用于治疗和预防与受干扰的cGMP平衡有关的疾病。 该化合物可用于治疗或预防心血管疾病，内皮功能障碍，舒张功能障碍，动脉粥样硬化，高血压，肺动脉高压，心绞痛，血栓形成，再狭窄，心肌梗死，中风，心功能不全，肺性高血压，勃起功能障碍，支气管哮喘，慢性 肾功能不全，糖尿病或肝硬化。
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60.发明申请Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment 审中-公开烟酸受体激动剂，包含这些化合物的组合物和治疗方法公开(公告)号：US20090170891A1
公开(公告)日：2009-07-02
申请号：US12226050
申请日：2007-04-06
申请人： Steven L. Colletti , James R. Tata , Weichun Chen , Richard T. Beresis , Fa-Xiang Ding , Darby Rye Schmidt , Hong Shen , Subharekha Raghavan
发明人： Steven L. Colletti , James R. Tata , Weichun Chen , Richard T. Beresis , Fa-Xiang Ding , Darby Rye Schmidt , Hong Shen , Subharekha Raghavan
IPC分类号： A61K31/4375 , C07D333/36 , A61K31/381 , C07D413/04 , A61K31/444 , C07D333/38 , A61P3/10
CPC分类号： C07D333/38 , C07D277/56 , C07D333/40 , C07D413/14
摘要： The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.
摘要翻译： 本发明包括可用于治疗动脉粥样硬化，血脂异常等的式I化合物及其药学上可接受的盐和水合物。 还包括药物组合物和使用方法。
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