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1. 发明公开

EP1496838A2 SUBSTITUTED AMIDES 有权
标题翻译：取代的酰胺
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。

2. 发明公开

EP2321288A1 OXAZOLE DERIVATIVES USEFUL AS INHIBITORS OF FAAH 有权转让
标题翻译： AS FAAH SUITABLE恶唑抑制剂
公开(公告)号：EP2321288A1
公开(公告)日：2011-05-18
申请号：EP09790960.0
申请日：2009-07-30
申请人： Merck & Co., Inc.
发明人： CHOBANIAN, Harry , LIN, Linus, S. , LIU, Ping , CHIODA, Marc, D. , DEVITA, Robert, J. , NARGUND, Ravi, P. , GUO, Yan
IPC分类号： C07D263/46 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/14 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/4427 , A61K31/444 , A61K31/4709 , A61K31/497 , A61K31/506 , A61P25/00 , A61P19/00
CPC分类号： C07D413/14 , C07D263/46 , C07D271/06 , C07D271/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/14
摘要： The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.

3. 发明公开

EP1807388A2 ACYCLIC HYDRAZIDES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：无环肼类化合物作为CANNABINOID受体调节剂
公开(公告)号：EP1807388A2
公开(公告)日：2007-07-18
申请号：EP05800281.7
申请日：2005-10-03
申请人： Merck & Co., Inc.
发明人： LIN, Linus, S. , LIU, Ping
IPC分类号： C07C243/24 , C07C255/00 , C07D213/02 , A61K31/16 , A61K31/44 , A61K31/275
CPC分类号： C07C255/66 , C07C243/28 , C07C243/32 , C07C243/36 , C07C2601/08 , C07D213/64
摘要： The acyclic hydrazides 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 (including smoking cessation), 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：本发明的无环酰肼是大麻素-1（CB1）受体的拮抗剂和/或反激动剂，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药物滥用障碍（包括戒烟），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。

4. 发明公开

EP1725542A1 VLA-4 ANTAGONISTS 审中-公开
标题翻译： VLA-4拮抗剂
公开(公告)号：EP1725542A1
公开(公告)日：2006-11-29
申请号：EP05729422.5
申请日：2005-03-07
申请人： Merck & Co., Inc.
发明人： HAGMANN, William, K. , LIN, Linus, S. , LIU, Ping , MUMFORD, Richard, A. , REGER, Thomas, S. , SMITH, Nicholas, D. , STOCK, Nicholas, S. , ZUNIC, Jasmine
IPC分类号： C07D401/12 , C07D401/14 , A61K31/44
CPC分类号： C07K5/06026 , C07D401/12 , C07D401/14
摘要： Compounds of Formula I are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn’s disease, multiple sclerosis, asthma, and rheumatoid arthritis.

5. 发明公开

EP1641493A1 RADIOLABELED CANNABINOID-1 RECEPTOR MODULATORS 审中-公开
标题翻译：放射性注明大麻素1受体调节剂
公开(公告)号：EP1641493A1
公开(公告)日：2006-04-05
申请号：EP04777002.9
申请日：2004-06-25
申请人： Merck & Co., Inc.
发明人： BURNS, Donald, H. , CHEN, Alex, M. , GIBSON, Raymond, E. , GOULET, Mark, T. , HAGMANN, William, K. , HAMILL, Terence, G. , JEWELL, James, P. , LIN, Linus, S. , LIU, Ping , PERESYPKIN, Andrey, V.
IPC分类号： A61K51/00 , C07D213/00 , C07D211/70
CPC分类号： C07D213/64 , A61K51/0406 , A61K51/0455 , A61K51/0459 , C07D239/34
摘要： The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.

6. 发明公开

EP2102201A2 SUBSTITUTED DIAZEPINE SULFONAMIDES AS BOMBESIN RECEPTOR SUBTYPE-3 MODULATORS 有权
标题翻译：取代的二氮杂磺胺ALS铃蟾肽受体亚型3调节剂
公开(公告)号：EP2102201A2
公开(公告)日：2009-09-23
申请号：EP07862652.0
申请日：2007-12-07
申请人： Merck & Co., Inc.
发明人： BAKER, Robert K. , CHANG, Linda L. , CHIODA, Marc , CHOBANIAN, Harry R. , GAO, Ying-Duo , GUO, Yan , LIN, Linus S. , LIU, Ping , NARGUND, Ravi P. , RUPPRECHT, Kathleen M. , MIAO, Shouwu
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D471/14
摘要： Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.

7. 发明公开

EP1874299A2 VLA-4 ANTAGONISTS 审中-公开
标题翻译： VLA-4拮抗剂
公开(公告)号：EP1874299A2
公开(公告)日：2008-01-09
申请号：EP06750646.9
申请日：2006-04-17
申请人： Merck & Co., Inc.
发明人： LIU, Ping , JONES, Carrie , REGER, Thomas, S.
IPC分类号： A61K31/40 , A61K31/44 , A61K31/445 , C07D207/09 , C07D209/02 , C07D401/12
CPC分类号： C07K5/06139 , A61K38/00
摘要： Substituted N-[N-(sulphonylphenyl)sulfonyl-prolyl]-phenylalanine derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds.

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