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1. 发明申请

WO2009011836A1 BETA CARBOLINE DERIVATIVES AS ANTIDIABETIC COMPOUNDS 审中-公开
标题翻译：作为抗菌化合物的碳氢化合物衍生物
公开(公告)号：WO2009011836A1
公开(公告)日：2009-01-22
申请号：PCT/US2008/008611
申请日：2008-07-15
申请人： MERCK & CO., INC. , DOBBELAAR, Peter, H. , DU, Wu , GUO, Liangqin , HAGMANN, William, K. , HE, Shuwen , JIAN, Tianying , LIU, Jian , NARGUND, Ravi, P. , PASTERNAK, Alexander , SHAH, Shrenik, K. , TRUONG, Quang, T. , YE, Zhixiong , DELLUREFICIO, James , BAKSHI, Raman
发明人： DOBBELAAR, Peter, H. , DU, Wu , GUO, Liangqin , HAGMANN, William, K. , HE, Shuwen , JIAN, Tianying , LIU, Jian , NARGUND, Ravi, P. , PASTERNAK, Alexander , SHAH, Shrenik, K. , TRUONG, Quang, T. , YE, Zhixiong , DELLUREFICIO, James , BAKSHI, Raman
IPC分类号： A61K31/535
CPC分类号： C07D471/04
摘要： Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.
摘要翻译：结构式I的β-咔啉衍生物是生长抑素亚型受体3（SSTR3）的选择性拮抗剂，可用于治疗2型糖尿病和通常与该疾病相关的病症，包括高血糖症，胰岛素抵抗，肥胖症，脂质障碍和高血压。这些化合物也可用于治疗抑郁症和焦虑症。

2. 发明申请

WO2011088025A1 OXADIAZOLE BETA CARBOLINE DERIVATIVES AS ANTIDIABETIC COMPOUNDS 审中-公开
标题翻译：作为抗菌化合物的奥沙唑苯甲酰胺衍生物
公开(公告)号：WO2011088025A1
公开(公告)日：2011-07-21
申请号：PCT/US2011/020796
申请日：2011-01-11
申请人： MERCK SHARP & DOHME CORP. , GUO, Liangqin , HAGMANN, William, K. , HE, Shuwen , LAI, Zhong , LIU, Jian , NARGUND, Ravi, P. , SHAH, Shrenik, K. , TRUONG, Quang, T.
发明人： GUO, Liangqin , HAGMANN, William, K. , HE, Shuwen , LAI, Zhong , LIU, Jian , NARGUND, Ravi, P. , SHAH, Shrenik, K. , TRUONG, Quang, T.
IPC分类号： A01N43/42
CPC分类号： C07D471/04
摘要： Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.
摘要翻译：结构式I的β-咔啉衍生物是生长抑素亚型受体3（SSTR3）的选择性拮抗剂，可用于治疗2型糖尿病和通常与该疾病相关的病症，包括高血糖症，胰岛素抵抗，肥胖症，脂质障碍和高血压。这些化合物也可用于治疗抑郁症和焦虑症。

3. 发明申请

WO2010083136A1 OXADIAZOLE BETA CARBOLINE DERIVATIVES AS ANTIDIABETIC COMPOUNDS 审中-公开
标题翻译：作为抗菌化合物的奥沙唑苯甲酰胺衍生物
公开(公告)号：WO2010083136A1
公开(公告)日：2010-07-22
申请号：PCT/US2010/020695
申请日：2010-01-12
申请人： MERCK SHARP & DOHME CORP. , DU, Wu , HAGMANN, William, K. , HE, Shuwen , LAI, Zhong , SHAH, Shrenik, K. , TRUONG, Quang, T.
发明人： DU, Wu , HAGMANN, William, K. , HE, Shuwen , LAI, Zhong , SHAH, Shrenik, K. , TRUONG, Quang, T.
IPC分类号： C07D471/04 , A61K31/407 , A61K31/437
CPC分类号： C07D471/04
摘要： Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety. Formula (I).
摘要翻译：结构式I的β-咔啉衍生物是生长抑素亚型受体3（SSTR3）的选择性拮抗剂，可用于治疗2型糖尿病和通常与该疾病相关的病症，包括高血糖症，胰岛素抵抗，肥胖症，脂质障碍和高血压。这些化合物也可用于治疗抑郁症和焦虑症。式（I）。

4. 发明申请

WO2005044785A1 ARALKYL AMINES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译： ARALKYL AMINES作为CANNABINOID受体调节剂
公开(公告)号：WO2005044785A1
公开(公告)日：2005-05-19
申请号：PCT/US2004/035846
申请日：2004-10-27
申请人： MERCK & CO., INC. , SHAH, Shrenik, K. , TRUONG, Quang, T. , QI, Hongbo , HAGMANN, William, K.
发明人： SHAH, Shrenik, K. , TRUONG, Quang, T. , QI, Hongbo , HAGMANN, William, K.
IPC分类号： C07C255/59
CPC分类号： C07D213/74 , C07C255/58 , C07C317/28 , C07C317/48 , C07C323/63 , C07C2601/04 , C07C2601/14 , C07D207/32 , C07D207/325 , C07D213/38 , C07D213/57 , C07D213/61 , C07D213/64 , C07D231/12 , C07D231/38 , C07D239/26 , C07D249/06 , C07D249/08 , C07D249/14
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson’s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, including alcohol and nicotine addiction, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。该化合物还可用于治疗药物滥用障碍，包括酒精和尼古丁成瘾，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

5. 发明申请

WO2003007887A2 SUBSTITUTED IMIDAZOLES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：取代的咪唑作为大麻素受体调节剂
公开(公告)号：WO2003007887A2
公开(公告)日：2003-01-30
申请号：PCT/US2002/023230
申请日：2002-07-16
申请人： MERCK & CO., INC. , FINKE, Paul, E. , MILLS, Sander, G. , PLUMMER, Christopher, W. , SHAH, Shrenik, K. , TRUONG, Quang, T.
发明人： FINKE, Paul, E. , MILLS, Sander, G. , PLUMMER, Christopher, W. , SHAH, Shrenik, K. , TRUONG, Quang, T.
IPC分类号： A61K
CPC分类号： C07D405/12 , C07D233/90
摘要： The use of compounds of the present invention as antagonists and/or inverse agonists of the Cannabinoid-1 (CB1)receptor particularly in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB1) receptor. The invention is concerned with the use of these novel compounds to selectively antagonize the Cannabinoid-1 (CB1) receptor. As such, compounds of the present invention are useful as psychotropic drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith. Novel compounds of structural formula (I) are also claimed.
摘要翻译：本发明化合物作为大麻素-1（CB1）受体的拮抗剂和/或反向激动剂的用途，特别是在治疗，预防和抑制由大麻素-1（CB1）介导的疾病）受体。本发明涉及这些新型化合物选择性拮抗大麻素-1（CB1）受体的用途。因此，本发明化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化症和格林 - 巴利综合征的神经炎症和病毒性脑炎，脑炎的炎性后遗症的精神药物血管意外，头部创伤，焦虑症，压力，癫痫，帕金森病和精神分裂症。这些化合物还可用于治疗物质滥用障碍，特别是阿片类药物，酒精和尼古丁。该化合物还可用于治疗与过量食物摄入和与之相关的并发症相关的肥胖症或进食障碍。结构式（I）的新化合物也被要求保护。

6. 发明申请

WO2003086288A2 BICYCLIC AMIDES 审中-公开
标题翻译：双酚A
公开(公告)号：WO2003086288A2
公开(公告)日：2003-10-23
申请号：PCT/US2003/010740
申请日：2003-04-08
申请人： MERCK & CO., INC. , CASTONGUAY, Laurie, A. , HAGMANN, William, K. , LIN, Linus, S. , SHAH, Shrenik, K.
发明人： CASTONGUAY, Laurie, A. , HAGMANN, William, K. , LIN, Linus, S. , SHAH, Shrenik, K.
IPC分类号： A61K
CPC分类号： C07D405/12 , C07C233/59 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D307/84 , C07D311/58 , C07D319/20
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管事故和头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

7. 发明申请

WO2005027837A2 SUBSTITUTED SULFONAMIDES 审中-公开
标题翻译：取代的磺酰胺
公开(公告)号：WO2005027837A2
公开(公告)日：2005-03-31
申请号：PCT/US2004/030122
申请日：2004-09-14
申请人： MERCK & CO., INC. , ARMSTRONG, Helen, M. , CHANG, Linda, L. , GUTHIKONDA, Ravindra, N. , HAGMANN, William, K. , LIN, Linus, S. , SHAH, Shrenik, K.
发明人： ARMSTRONG, Helen, M. , CHANG, Linda, L. , GUTHIKONDA, Ravindra, N. , HAGMANN, William, K. , LIN, Linus, S. , SHAH, Shrenik, K.
IPC分类号： A61K
CPC分类号： C07C311/06 , A61K31/18 , A61K31/277 , A61K31/44 , C07C311/03 , C07C311/13 , C07C311/16 , C07C311/17 , C07C311/19 , C07C311/29 , C07D209/08
摘要： The substituted sulfonamides of the invention are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson’s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：本发明的取代磺酰胺是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

8. 发明申请

WO2003077847A3 SUBSTITUTED AMIDES 审中-公开
公开(公告)号：WO2003077847A3
公开(公告)日：2003-09-25
申请号：PCT/US2003/007320
申请日：2003-03-07
申请人： MERCK & CO., INC. , HAGMANN, William, K. , LIN, Linus, S. , SHAH, Shrenik, K. , GUTHIKONDA, Ravindra, N. , QI, Hongbo , CHANG, Linda, L. , LIU, Ping , ARMSTRONG, Helen, M. , JEWELL, James, P. , LANZA, Thomas, J., Jr.
发明人： HAGMANN, William, K. , LIN, Linus, S. , SHAH, Shrenik, K. , GUTHIKONDA, Ravindra, N. , QI, Hongbo , CHANG, Linda, L. , LIU, Ping , ARMSTRONG, Helen, M. , JEWELL, James, P. , LANZA, Thomas, J., Jr.
IPC分类号： C07C233/05
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

9. 发明申请

WO2004048317A1 SUBSTITUTED AMIDES ACTIVE AT THE CANNABINOID-1 RECEPTOR 审中-公开
标题翻译：在CANNABINOID-1受体中活性的取代的氨基酸
公开(公告)号：WO2004048317A1
公开(公告)日：2004-06-10
申请号：PCT/US2003/007039
申请日：2003-03-07
申请人： MERCK & CO., INC. , HAGMANN, William, K. , LIN, Linus, S. , SHAH, Shrenik, K. , GUTHIKONDA, Ravindra, N. , QI, Hongbo , CHANG, Linda, L. , LIU, Ping , ARMSTRONG, Helen, M. , JEWELL, James, P. , LANZA, Thomas, J., Jr.
发明人： HAGMANN, William, K. , LIN, Linus, S. , SHAH, Shrenik, K. , GUTHIKONDA, Ravindra, N. , QI, Hongbo , CHANG, Linda, L. , LIU, Ping , ARMSTRONG, Helen, M. , JEWELL, James, P. , LANZA, Thomas, J., Jr.
IPC分类号： C07C235/20
CPC分类号： C07D213/64 , A61K31/165 , A61K31/435 , A61K31/505 , C07C235/20 , C07C237/06 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D213/40 , C07D213/89 , C07D239/34 , C07D401/12 , C07D409/12 , C07D471/04 , C40B40/04 , C40B50/08
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译：结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管事故和头部创伤，焦虑障碍，压力，癫痫，帕金森病，运动障碍和精神分裂症。这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

10. 发明申请

WO2003086288A3 BICYCLIC AMIDES 审中-公开
公开(公告)号：WO2003086288A3
公开(公告)日：2003-10-23
申请号：PCT/US2003/010740
申请日：2003-04-08
申请人： MERCK & CO., INC. , CASTONGUAY, Laurie, A. , HAGMANN, William, K. , LIN, Linus, S. , SHAH, Shrenik, K.
发明人： CASTONGUAY, Laurie, A. , HAGMANN, William, K. , LIN, Linus, S. , SHAH, Shrenik, K.
IPC分类号： A61K31/335
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

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