公开(公告)号：EP0681571A1

公开(公告)日：1995-11-15

申请号：EP94907866.0

申请日：1994-01-25

申请人： MERCK & CO. INC.

发明人： HALE, Jeffrey, J. ,  MACCOSS, Malcolm ,  MILLS, Sander, G. ,  QI, Hongbo ,  SHAH, Shrenik, K.

IPC分类号： A61K31 ,  A61P1 ,  A61P11 ,  A61P25 ,  A61P29 ,  A61P43 ,  C07D221 ,  C07D491 ,  C07D495

CPC分类号： C07D221/20 ,  C07D491/10

摘要： Disclosed are spiro-substituted azacycles of formula (I), are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, emesis and asthma. In particular compounds of formula (I) are shown to be neurokinin antagonists.

公开(公告)号：EP1322596B1

公开(公告)日：2007-08-15

申请号：EP01973294.0

申请日：2001-09-21

申请人： Merck & Co., Inc.

发明人： FINKE, Paul, E. ,  MEURER, Laura, C. ,  MILLS, Sander, G. ,  MACCOSS, Malcolm ,  QI, Hongbo

IPC分类号： C07C229/22 ,  C07C229/46 ,  C07C229/48 ,  C07D207/16 ,  C07D211/34 ,  C07D241/04 ,  A61K31/397 ,  A61K31/40 ,  A61K31/41 ,  A61K31/445 ,  A61K31/495 ,  A61K31/195 ,  A61P25/26 ,  C07D205/04 ,  C07D401/04 ,  C07C217/52 ,  C07C62/34 ,  C07C43/196

CPC分类号： C07D257/04 ,  C07C43/196 ,  C07C51/09 ,  C07C62/34 ,  C07C217/52 ,  C07C229/22 ,  C07C229/46 ,  C07C229/48 ,  C07C2601/08 ,  C07C2601/14 ,  C07D205/04 ,  C07D207/16 ,  C07D211/60 ,  C07D211/62 ,  C07D265/30 ,  C07D401/04

摘要： The present invention is directed to certain novel compounds represented by structural formula (I), or a pharmaceutically acceptable salt thereof, wherein R?3, R5, R6, R7, R8, R11, R12, R13¿, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.

摘要翻译： 本发明涉及某些由结构式I表示的新化合物或其药学上可接受的盐，其中R3，R5，R6，R7，R8，R11，R12，R13，Q，W，X，Y和Z定义 于此。 本发明还涉及包含这些新化合物作为活性成分的药物制剂，以及新型化合物及其制剂在治疗某些疾病中的用途。 本发明的化合物是速激肽受体拮抗剂，可用于治疗精神障碍，包括抑郁和焦虑。

公开(公告)号：EP0681571B1

公开(公告)日：1998-07-29

申请号：EP94907866.1

申请日：1994-01-25

申请人： Merck & Co., Inc.

发明人： HALE, Jeffrey, J. ,  MACCOSS, Malcolm ,  MILLS, Sander, G. ,  QI, Hongbo ,  SHAH, Shrenik, K.

IPC分类号： C07D221/20 ,  C07D491/10 ,  C07D495/20 ,  A61K31/445

CPC分类号： C07D221/20 ,  C07D491/10

公开(公告)号：EP1682494A1

公开(公告)日：2006-07-26

申请号：EP04796666.8

申请日：2004-10-27

申请人： Merck & Co., Inc.

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，并且可用于治疗，预防和抑制由CB1受体介导的疾病。 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的炎性后遗症，脑血管障碍 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，包括酒精和尼古丁成瘾，治疗肥胖症或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

公开(公告)号：EP0702681A1

公开(公告)日：1996-03-27

申请号：EP95901979.0

申请日：1994-05-17

申请人： MERCK & CO. INC.

发明人： MacCOSS, Malcolm ,  MILLS, Sander, G. ,  SHAH, Shrenik, K. ,  CHIANG, Yuan-Ching, P. ,  DUNN, Patrick T. ,  KOYAMA, Hiroo ,  FINKE, Paul E. ,  QI, Hongbo ,  ROBICHAUD, Albert, J.

IPC分类号： C07D487 ,  A61K31 ,  A61P1 ,  A61P9 ,  A61P21 ,  A61P25 ,  A61P27 ,  C07D471 ,  C07D491 ,  C07D495 ,  C07D513

CPC分类号： C07D471/10 ,  C07D491/10 ,  C07D495/10

摘要： Disclosed are spiro-substituted azacycles of formula (I), tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma. In particular compounds of formula (I) are shown to be neurokinin antagonists.

公开(公告)号：EP1496838A2

公开(公告)日：2005-01-19

申请号：EP03714051.4

申请日：2003-03-07

申请人： Merck & Co., Inc.

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： A61K7/00

CPC分类号： C07D213/64 ,  C07C233/13 ,  C07C235/06 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C255/55 ,  C07C255/60 ,  C07C271/14 ,  C07C271/22 ,  C07C275/30 ,  C07C311/03 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D209/34 ,  C07D209/94 ,  C07D211/34 ,  C07D213/65 ,  C07D213/68 ,  C07D215/06 ,  C07D231/12 ,  C07D233/56 ,  C07D233/70 ,  C07D237/28 ,  C07D237/32 ,  C07D239/34 ,  C07D249/04 ,  C07D249/08 ,  C07D249/12 ,  C07D263/58 ,  C07D267/14 ,  C07D277/30 ,  C07D277/36 ,  C07D295/13 ,  C07D295/15 ,  C07D513/04

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，并且可用于治疗，预防和抑制由CB1受体介导的疾病。 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的炎性后遗症，脑血管障碍 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物质滥用障碍，肥胖或饮食失调的治疗，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

公开(公告)号：EP1322596A1

公开(公告)日：2003-07-02

申请号：EP01973294.0

申请日：2001-09-21

申请人： Merck & Co., Inc.

发明人： FINKE, Paul, E. ,  MEURER, Laura, C. ,  MILLS, Sander, G. ,  MACCOSS, Malcolm ,  QI, Hongbo

IPC分类号： C07C229/22 ,  C07C229/46 ,  C07C229/48 ,  C07D207/16 ,  C07D211/34 ,  C07D241/04 ,  A61K31/397 ,  A61K31/40 ,  A61K31/41 ,  A61K31/445 ,  A61K31/495 ,  A61K31/195 ,  A61P25/26 ,  C07D205/04 ,  C07D401/04 ,  C07C217/52 ,  C07C62/34 ,  C07C43/196

CPC分类号： C07D257/04 ,  C07C43/196 ,  C07C51/09 ,  C07C62/34 ,  C07C217/52 ,  C07C229/22 ,  C07C229/46 ,  C07C229/48 ,  C07C2601/08 ,  C07C2601/14 ,  C07D205/04 ,  C07D207/16 ,  C07D211/60 ,  C07D211/62 ,  C07D265/30 ,  C07D401/04

摘要： The present invention is directed to certain novel compounds represented by structural formula (I), or a pharmaceutically acceptable salt thereof, wherein R?3, R5, R6, R7, R8, R11, R12, R13¿, Q, W, X, Y and Z are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of psychiatric disorders including depression and anxiety.