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51. 发明申请

US20130012493A1 NOVEL SPIRO IMIDAZOLONE DERIVATIVES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE 审中-公开
标题翻译：作为GLUCAGON受体拮抗剂，组合物及其使用方法的新型SPIRO咪达唑仑衍生物
公开(公告)号：US20130012493A1
公开(公告)日：2013-01-10
申请号：US13636276
申请日：2011-03-22
申请人： He Zhao , Ping Chen , Peishan Lin , Peng Dai , Jason Louis Davis , Duane E. DeMong , Michael W. Miller , Xing Dai , Michael K. Wong , Brian J. Lavey , Wensheng Yu , Guowei Zhou , Andrew W. Stamford , Joseph A. Kozlowski , William J. Greenlee
发明人： He Zhao , Ping Chen , Peishan Lin , Peng Dai , Jason Louis Davis , Duane E. DeMong , Michael W. Miller , Xing Dai , Michael K. Wong , Brian J. Lavey , Wensheng Yu , Guowei Zhou , Andrew W. Stamford , Joseph A. Kozlowski , William J. Greenlee
IPC分类号： A61K31/454 , A61P3/10 , C07D403/12 , A61K31/4178 , A61K31/5386 , A61K31/55 , A61K31/496 , C07D413/14 , A61K31/5377 , C07D498/08 , C07D401/14 , C07D403/14
CPC分类号： C07D403/12 , C07D401/04 , C07D401/14 , C07D403/14 , C07D413/04 , C07D413/14 , C07D491/08 , C07D498/08
摘要： The present invention relates to compounds of the general formula (I): wherein ring A, ring B, G, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
摘要翻译：本发明涉及通式（I）的化合物：其中环A，环B，G，R 3，Z，L 1和L 2彼此独立地并且如本文所定义，包含该化合物的组合物，和涉及使用该化合物作为胰高血糖素受体拮抗剂并用于治疗或预防2型糖尿病及与之有关的病症的方法。

52. 发明申请

US20130012434A1 NOVEL SPIRO IMIDAZOLONES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE 审中-公开
标题翻译：作为GLUCAGON受体拮抗剂，组合物及其使用方法的新型SPIRO咪唑烷
公开(公告)号：US20130012434A1
公开(公告)日：2013-01-10
申请号：US13636244
申请日：2011-03-22
申请人： Michael K. Wong , Brian J. Lavey , Wensheng Yu , Joseph A. Kozlowski , Duanc E. DeMong , Xing Dai , Andrew W. Stamford , Michael W. Miller , Guowei Zhou , De-Yi Yang , William J. Greenlee
发明人： Michael K. Wong , Brian J. Lavey , Wensheng Yu , Joseph A. Kozlowski , Duanc E. DeMong , Xing Dai , Andrew W. Stamford , Michael W. Miller , Guowei Zhou , De-Yi Yang , William J. Greenlee
IPC分类号： A61K31/4184 , C07D235/02 , C07D471/10 , A61K31/438 , C07F7/10 , A61K31/695 , C07D491/107 , C07D487/10 , A61K31/4188 , C07D403/14 , A61K31/497 , A61K31/506 , C07D487/04 , A61K31/4985 , A61K38/28 , A61P3/10 , A61K38/17 , A61K38/26 , A61K31/7034 , A61K31/7048 , A61P3/04 , A61P3/06 , A61P9/10 , C07D403/12
CPC分类号： C07D403/12 , C07D233/70 , C07D401/10 , C07D405/10 , C07F7/0812
摘要： The present invention relates to compounds of the general formula: wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
摘要翻译：本发明涉及以下通式的化合物：其中环A，环B，R 1，R 3，Z，L 1和L 2彼此独立地并且如本文所定义，包含该化合物的组合物，以及使用该化合物作为胰高血糖素受体拮抗剂，并用于治疗或预防2型糖尿病及与此有关的病症。

53. 发明申请

US20120108505A1 THIOPHENES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE 有权
标题翻译：作为GLUCAGON受体拮抗剂的THIOPHENES，组合物及其使用方法
公开(公告)号：US20120108505A1
公开(公告)日：2012-05-03
申请号：US13377707
申请日：2010-06-10
申请人： Eric J. Gilbert , Michael W. Miller , Andrew W. Stamford , William J. Greenlee
发明人： Eric J. Gilbert , Michael W. Miller , Andrew W. Stamford , William J. Greenlee
IPC分类号： A61K31/4155 , A61K38/28 , A61K38/17 , A61K31/70 , A61K31/7034 , A61K31/7048 , A61P3/10 , A61P3/08 , A61P5/48 , A61P3/04 , A61P3/06 , A61P7/00 , A61P9/10 , A61P1/18 , A61P25/28 , A61P27/02 , A61P13/12 , A61P25/02 , A61P3/00 , C07D409/06
CPC分类号： C07D409/06 , A61K31/4155 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds of the general formula (I): wherein R1, R2, R3, R5, s, and Z are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
摘要翻译：本发明涉及通式（I）的化合物：其中R 1，R 2，R 3，R 5，S和Z彼此独立地选自并且如本文所定义，包括该化合物的组合物，以及使用化合物作为胰高血糖素受体拮抗剂并用于治疗或预防2型糖尿病及其相关病症。

54. 发明申请

US20110166165A1 BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS 有权
标题翻译：双相异构体衍生物及其作为GPR119调节剂的用途
公开(公告)号：US20110166165A1
公开(公告)日：2011-07-07
申请号：US13003681
申请日：2009-07-15
申请人： Santhosh Francis Neelamkavil , Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Bernard R. Neustadt , Andrew W. Stamford
发明人： Santhosh Francis Neelamkavil , Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Bernard R. Neustadt , Andrew W. Stamford
IPC分类号： A61K31/519 , C07D487/04 , A61P3/04 , A61P3/10 , A61P3/00
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.
摘要翻译：本发明涉及式（I）的双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖，糖尿病，代谢紊乱，心血管疾病或与在患者中G蛋白偶联受体（GPCR）如GPR119的活性。

55. 发明授权

US08236805B2 Substituted piperazines as CB1 antagonists 失效
标题翻译：取代的哌嗪作为CB1拮抗剂
公开(公告)号：US08236805B2
公开(公告)日：2012-08-07
申请号：US12564678
申请日：2009-09-22
申请人： Eric J. Gilbert , Michael W. Miller , Jack D. Scott , Andrew W. Stamford , William J. Greenlee , Jay Weinstein
发明人： Eric J. Gilbert , Michael W. Miller , Jack D. Scott , Andrew W. Stamford , William J. Greenlee , Jay Weinstein
IPC分类号： A61K31/497 , C07D403/00
CPC分类号： C07D241/04 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/08 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/10
摘要： Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或酯可用于治疗由CB1受体介导的疾病或病症，例如代谢综合征和肥胖症，神经炎症性疾病，认知障碍和精神病，成瘾（例如吸烟停止），胃肠道疾病和心血管疾病。

56. 发明授权

US08470773B2 Thiophenes as glucagon receptor antagonists, compositions, and methods for their use 有权
标题翻译：噻吩类作为胰高血糖素受体拮抗剂，组合物及其使用方法
公开(公告)号：US08470773B2
公开(公告)日：2013-06-25
申请号：US13377707
申请日：2010-06-10
申请人： Eric J. Gilbert , Michael W. Miller , Andrew W. Stamford , William J. Greenlee
发明人： Eric J. Gilbert , Michael W. Miller , Andrew W. Stamford , William J. Greenlee
IPC分类号： C07D409/06 , A61K31/4155 , A61P3/10
CPC分类号： C07D409/06 , A61K31/4155 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds of the general formula: wherein R1, R2, R3, R5, s, and Z are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
摘要翻译：本发明涉及以下通式的化合物：其中R 1，R 2，R 3，R 5，S和Z彼此独立地并且如本文所定义，包含该化合物的组合物，以及使用该化合物作为胰高血糖素的方法受体拮抗剂和用于治疗或预防2型糖尿病及其相关病症。

57. 发明申请

US20120178789A1 NOVEL PYRROLIDINES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE 有权
标题翻译：作为GLUCAGON受体拮抗剂的新型吡咯烷酮，组合物及其使用方法
公开(公告)号：US20120178789A1
公开(公告)日：2012-07-12
申请号：US13496236
申请日：2010-09-16
申请人： Eric J. Gilbert , Michael W. Miller , Duane Eugene DeMong , Andrew W. Stamford , William J. Greenlee
发明人： Eric J. Gilbert , Michael W. Miller , Duane Eugene DeMong , Andrew W. Stamford , William J. Greenlee
IPC分类号： A61K31/40 , C07D207/48 , C07D207/09 , A61P25/28 , A61P3/04 , A61P3/10 , A61P3/06 , A61P9/10 , C07D207/16 , A61P9/12
CPC分类号： A61K31/40 , C07D207/08 , C07D207/09 , C07D207/48 , C07D207/50
摘要： The present invention relates to compounds of the general formula: (I) wherein ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
摘要翻译：本发明涉及以下通式的化合物：其中环B，R 1，R 2，R 3，Z和L 1彼此独立地并且如本文所定义，包含该化合物的组合物，以及使用的方法该化合物作为胰高血糖素受体拮抗剂并用于治疗或预防2型糖尿病及与之相关的病症。

58. 发明申请

US20100029607A1 Substituted Piperazines as CB1 Antagonists 失效
标题翻译：取代的Piperazines作为CB1拮抗剂
公开(公告)号：US20100029607A1
公开(公告)日：2010-02-04
申请号：US12564678
申请日：2009-09-22
申请人： Eric J. Gilbert , Michael W. Miller , Jack D. Scott , Andrew W. Stamford , William J. Greenlee , Jay Weinstein
发明人： Eric J. Gilbert , Michael W. Miller , Jack D. Scott , Andrew W. Stamford , William J. Greenlee , Jay Weinstein
IPC分类号： A61K31/496 , C07D295/06 , C07D401/04 , C07D405/06 , C07D409/14 , A61K31/4965 , A61P3/00 , A61P25/00 , A61K31/397
CPC分类号： C07D241/04 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/08 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/10
摘要： Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或酯可用于治疗由CB1受体介导的疾病或病症，例如代谢综合征和肥胖症，神经炎症性疾病，认知障碍和精神病，成瘾（例如吸烟停止），胃肠道疾病和心血管疾病。

59. 发明授权

US07157472B2 Neuropeptide Y Y5 receptor antagonists 失效
标题翻译：神经肽Y Y5受体拮抗剂
公开(公告)号：US07157472B2
公开(公告)日：2007-01-02
申请号：US10609638
申请日：2003-06-30
申请人： Andrew W. Stamford , Yusheng Wu
发明人： Andrew W. Stamford , Yusheng Wu
IPC分类号： A61K31/454 , C07D401/12
CPC分类号： C07D401/12
摘要： The present invention discloses compounds which, are receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
摘要翻译：本发明公开了作为NPY Y5的受体拮抗剂的化合物以及这些化合物的制备方法。在另一个实施方案中，本发明公开了包含这种NPY Y5受体拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

60. 发明授权

US06329395B1 Neuropeptide Y5 receptor antagonists 失效
标题翻译：神经肽Y5受体拮抗剂
公开(公告)号：US06329395B1
公开(公告)日：2001-12-11
申请号：US09326575
申请日：1999-06-07
申请人： Sundeep Dugar , Bernard R. Neustadt , Andrew W. Stamford , Yusheng Wu
发明人： Sundeep Dugar , Bernard R. Neustadt , Andrew W. Stamford , Yusheng Wu
IPC分类号： A61K31445
CPC分类号： C07D213/40 , C07C233/15 , C07C233/25 , C07C233/29 , C07C275/28 , C07C275/32 , C07C275/34 , C07C275/38 , C07C311/05 , C07C323/41 , C07C323/44 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D211/58 , C07D213/38 , C07D213/74 , C07D295/135 , C07D295/15 , C07D295/215 , C07D317/72
摘要： Compounds of the formula I or a pharmaceutically acceptable salt thereof, wherein a and b are 0-2, provided that the sum is 0-3; X is —O—, —S—, —SO—, —SO2—, —CH(OR8)—, —C(O)—, —C(R23)2—, optionally substituted alkenyl, alkynyl or; R1 is optionally substituted aryl, heteroaryl, substituted amino, alkyl-OC(O)R8, aryloxyalkyl, wherein m is 1-4, or wherein d and e are 0-2; R2, R3, R4 and R5 are H, alkyl, optionally substituted cycloalkyl, halogen, —OR8, —N(R8)2, —CO2R8 or CF3; R6 and R7 are H, alkyl, alkenyl, hydroxyalkyl, aminoalkyl, alkoxy-alkyl, cycloalkyl or cycloalkylalkyl, or R6 and R7, form a 3-7-membered carbocyclic ring, or a 4-7-membered heterocyclic ring; R8 is H, alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R9 is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R11 is H, alkyl or cycloalkyl; and R23 is R8 or halogen; are claimed, as well as additional novel compounds; also claimed are pharmaceutical compositions and methods of using said novel compounds in the treatment of eating disorders and diabetes.
摘要翻译：式I的化合物或其药学上可接受的盐，其中a和b为0-2，条件是总和为0-3; X是-O - ， - S - ， - SO - ， - SO 2 - ， - CH（OR 8 ） - ， - C（O） - ， - C（R 23）2 - ，任选取代的烯基，炔基或R 1是任选取代的芳基，杂芳基，取代的氨基，烷基-C（O）R 8，芳氧基烷基，其中m是1 -4或其中d和e为0-2; R 2，R 3，R 4和R 5为H，烷基，任选取代的环烷基，卤素，-OR 8，-N（R 8）2，-CO 2 R 8或CF 3; R 6和R 7为 H，烷基，烯基，羟基烷基，氨基烷基，烷氧基 - 烷基，环烷基或环烷基烷基，或R6和R7形成3-7元碳环或4-7元杂环; R8是H，烷基，环烷基，任选取代的芳基或杂芳基; R 9为烷基，环烷基，任选取代的芳基或杂芳基; R 11为H，烷基或环烷基; R 23为R 8或卤素; 以及其他新型化合物; 还要求的是使用所述新型化合物治疗进食障碍和糖尿病的药物组合物和方法。

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