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公开(公告)号：EP1558605A2
公开(公告)日：2005-08-03
申请号：EP03776347.1
申请日：2003-10-14
发明人： VOLANTE, Ralph, P. , TSCHAEN, David, M. , WEISSMAN, Steven, A. , HEILEMAN, Matthew , MASE, Toshiaki , IIDA, Takehiko , MAEDA, Kenji , WADA, Toshihiro , SATO, Hiroki , ASAKAWA, Kenichi
IPC分类号： C07D405/12 , C07D405/14 , C07D307/94 , C07D491/107
CPC分类号： C07D493/10
摘要： This invention relates to a process for making spirolactone compounds analogous to formula I.
摘要翻译： 本发明涉及制备类似于式I的螺内酯化合物的方法。
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公开(公告)号：EP1070062B1
公开(公告)日：2002-03-06
申请号：EP99916377.7
申请日：1999-04-05
IPC分类号： C07D405/04 , C07D221/04
CPC分类号： C07D221/04 , C07D405/04
摘要： The present invention relates to an oxidation using sodium chlorite in the presence of a catalytic amount of TEMPO and sodium hypochlorite which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula (I) having a carboxylic acid.
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公开(公告)号：EP0923557A1
公开(公告)日：1999-06-23
申请号：EP97937187.0
申请日：1997-08-08
发明人： DEVINE, Paul, N. , DOLLING, Ulf, H. , FREY, Lisa, F. , TILLYER, Richard, D. , TSCHAEN, David, M. , KATO, Yoshiaki
CPC分类号： C07D405/04
摘要： This invention relates to a key intermediate in the synthesis of an endothelin antagonist, the synthesis of this key intermediate and the synthesis of an endothelin antagonist using this intermediate in a stereoselective deoxygenation reaction.
摘要翻译： 本发明涉及内皮素拮抗剂合成中的关键中间体，该关键中间体的合成以及使用该中间体在立体选择性脱氧反应中合成内皮素拮抗剂。
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公开(公告)号：EP1070062A1
公开(公告)日：2001-01-24
申请号：EP99916377.7
申请日：1999-04-05
IPC分类号： C07D405/04 , C07D221/04
CPC分类号： C07D221/04 , C07D405/04
摘要： The present invention relates to an oxidation using sodium chlorite in the presence of a catalytic amount of TEMPO and sodium hypochlorite which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula (I) having a carboxylic acid.
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5.发明公开THERAPEUTIC POLYMORPHS OF A GABA-A ALPHA-5 INVERSE AGONIST AND PAMOATE FORMULATIONS OF THE SAME 审中-公开的GABA-A ALPHA-5受体和双羟萘酸制剂的反相激动剂治疗性多晶型
公开(公告)号：EP1129094A2
公开(公告)日：2001-09-05
申请号：EP99961637.8
申请日：1999-11-10
申请人： Merck & Co., Inc.
发明人： KAUFMAN, Michael, J. , MCCAULEY, James, A. , RUSH, Daniel, J. , TSCHAEN, David, M. , VARSOLONA, Richard, J. , HO, Guo-Jie
IPC分类号： C07D487/04 , A61K31/5025 , A61P25/28
CPC分类号： C07D487/04
摘要： There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.
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公开(公告)号：EP1070061A1
公开(公告)日：2001-01-24
申请号：EP99915282.0
申请日：1999-04-05
申请人： MERCK & CO., INC.
发明人： SONG, Zhiguo , TSCHAEN, David, M. , ZHAO, Mangzu
IPC分类号： C07D405/04
CPC分类号： C07D405/04
摘要： The present invention relates to a periodic acid oxidation which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula (I) having a carboxylic acid.
摘要翻译： 本发明涉及将具有伯醇的倒数第二个中间体转化为具有羧酸的式（I）的目标内皮素拮抗剂化合物的高碘酸氧化。
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公开(公告)号：EP0851850A1
公开(公告)日：1998-07-08
申请号：EP96930823.0
申请日：1996-09-11
申请人： MERCK & CO., INC.
CPC分类号： C07C319/20 , C07C45/004 , C07C45/45 , C07C259/06 , C07D317/54 , C07D333/22 , C07C323/22
摘要： A simple, high yielding synthesis of α-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-M-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.
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公开(公告)号：EP0912537B1
公开(公告)日：2004-05-12
申请号：EP97932424.1
申请日：1997-06-27
申请人： MERCK & CO., INC.
发明人： DESMOND, Richard , DOLLING, Ulf, H. , FREY, Lisa, F. , TILLYER, Richard, D. , TSCHAEN, David, M.
IPC分类号： C07D307/38
CPC分类号： C07D307/38
摘要： The invention encompasses a process for making compounds of Formula (I) useful in the treatment of inflammation and other cyclooxygenase-2 mediated diseases.
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公开(公告)号：EP1070041A1
公开(公告)日：2001-01-24
申请号：EP99915281.2
申请日：1999-04-05
IPC分类号： C07C63/36 , C07C69/74 , C07C69/76 , C07C233/58 , C07D221/02
CPC分类号： C07D405/04 , C07C231/18 , C07D213/55 , C07D405/06 , C07D413/04 , C07C233/57
摘要： This invention relates to a cyclization process useful in the preparation of a key intermediate in the preparation of an endothelin antagonist of formula (I).
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公开(公告)号：EP0923556A1
公开(公告)日：1999-06-23
申请号：EP97936396.0
申请日：1997-08-05
申请人： MERCK & CO., INC.
CPC分类号： C07D401/04 , C07D263/06 , C07D405/06 , C07D413/04 , C07F7/1892
摘要： This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.
摘要翻译： 本发明涉及合成内皮素拮抗剂的关键中间体和使用不对称共轭加成反应合成该关键中间体。
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