-
1.发明授权POLYMORPHIC, AMORPHOUS AND HYDRATED FORMS OF 5-CHLORO-3-(4-METHANESULFONYLPHENYL)-6'-METHYL- 2,3']BIPYRIDINYL 有权多晶型物，无定形和5-氯-3-（甲磺酰基 - 苯基）-6'-甲基 - 2,3“]联吡啶水合形式
公开(公告)号：EP1248618B1
公开(公告)日：2006-03-22
申请号：EP00980817.1
申请日：2000-11-27
发明人： CLAS, Sophie, Dorothee , O'SHEA, Paul , DALTON, Chad , CROCKER, Louis, S. , MCCAULEY, James, A. , TILLYER, Richard, D. , DAVIES, Ian
IPC分类号： A61K31/44 , C07D213/22 , A61K31/444
CPC分类号： A61K31/444 , C07D213/61
摘要： Polymorphic, amorphous and hydrated forms of the title compound having the following structure: are disclosed. The compound is a potent and selective cyclooxygenase -2 (COX-2) inhibitor.
-
2.发明公开POLYMORPHIC, AMORPHOUS AND HYDRATED FORMS OF 5-CHLORO-3-(4-METHANESULFONYLPHENYL)-6'-METHYL- 2,3']BIPYRIDINYL 有权多晶型物，无定形和5-氯-3-（甲磺酰基 - 苯基）-6'-甲基 - 2,3“]联吡啶水合形式
公开(公告)号：EP1248618A1
公开(公告)日：2002-10-16
申请号：EP00980817.1
申请日：2000-11-27
发明人： CLAS, Sophie, Dorothee , O'SHEA, Paul , DALTON, Chad , CROCKER, Louis, S. , MCCAULEY, James, A. , TILLYER, Richard, D. , DAVIES, Ian
IPC分类号： A61K31/44 , C07D213/22
CPC分类号： A61K31/444 , C07D213/61
摘要： Polymorphic, amorphous and hydrated forms of the title compound having the following structure: are disclosed. The compound is a potent and selective cyclooxygenase -2 (COX-2) inhibitor.
-
公开(公告)号：EP0923556B1
公开(公告)日：2003-10-08
申请号：EP97936396.7
申请日：1997-08-05
申请人： MERCK & CO., INC.
IPC分类号： C07D213/02 , C07D401/04 , C07D401/06 , A61K31/335 , A61K31/415 , A61K31/42 , A61K31/44
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.
-
4.发明公开
公开(公告)号：EP1161236A1
公开(公告)日：2001-12-12
申请号：EP00907111.9
申请日：2000-02-02
申请人： Merck & Co., Inc.
发明人： TILLYER, Richard, D. , REIDER, Paul, J. , GRABOWSKI, Edward, J., J. , XU, Feng , VEGA, Jose, M.
CPC分类号： A61K9/2833
摘要： The instant invention provides methods and pharmaceutical compositions for inhibiting HMG-CoA reductase, as well as for treating and/or reducing the risk for diseases and conditions affected by inhibition of HMG-CoA reductase, comprising orally administering a therapeutically effective amount of a compound selected from a dihydroxy open acid statin and a pharmaceutically acceptable salt or ester thereof in a delayed-release pharmaceutical dosage form to a patient in need of such treatment wherein substantial release of the compound from the dosage form is delayed until after passage of the dosage form through the stomach.
-
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。
-
6.发明授权EFFICIENT SYNTHESIS OF A 1,4-DIHYDRO-2H-3,1-BENZOXAZIN-2-ONE 失效WIRKSAMES VERFAHREN ZUR HERSTELLUNG VON 1,4-DIHYDRO-2H-3，1-BENZOXAZIN-2-ON
公开(公告)号：EP0968197B1
公开(公告)日：2005-04-27
申请号：EP98906255.9
申请日：1998-02-09
申请人： MERCK & CO., INC.
IPC分类号： C07D265/18 , C07C271/28
CPC分类号： C07D265/18 , C07C271/28 , C07C2601/02
摘要： An efficient method for the preparation of a compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one, also known as DMP-266, a reverse transcriptase inhibitor is achieved using a cyclization reaction of the amino alcohol intermediate with an alkyl or aryl chloroformate and a base.
摘要翻译： 制备（ - ） - 6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1-苯并恶嗪-2-酮的化合物的有效方法，也称为DMP-266 ，使用氨基醇中间体与氯甲酸烷基酯或芳基酯和碱的环化反应来实现逆转录酶抑制剂。
-
7.发明授权EFFICIENT ENANTIOSELECTIVE ADDITION REACTION USING AN ORGANOZINC REAGENT 失效对映选择性ADDITIONS反应中，用有机锌试剂
公开(公告)号：EP0981520B1
公开(公告)日：2004-07-07
申请号：EP98922084.3
申请日：1998-05-12
申请人： MERCK & CO., INC.
IPC分类号： C07D265/18
CPC分类号： C07D265/18 , C07B2200/07 , C07C213/08 , C07C215/68 , C07C215/70
摘要： An efficient method for the preparation of key intermediate, in the synthesis of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addition reaction to the 4-chloro-2-trifluoromethylketoaniline with an organozinc complex to give the desired alcohol. This instant method has broad applicability in the chiral addition to any prochiral ketone.
-
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.
-
公开(公告)号：EP0851850B1
公开(公告)日：2001-12-12
申请号：EP96930823.8
申请日：1996-09-11
申请人： MERCK & CO., INC.
IPC分类号： C07C45/00 , C07C45/45 , C07C259/06
CPC分类号： C07C319/20 , C07C45/004 , C07C45/45 , C07C259/06 , C07D317/54 , C07D333/22 , C07C323/22
-
10.发明公开EFFICIENT ENANTIOSELECTIVE ADDITION REACTION USING AN ORGANOZINC REAGENT 失效对映选择性ADDITIONS反应中，用有机锌试剂
公开(公告)号：EP0981520A1
公开(公告)日：2000-03-01
申请号：EP98922084.3
申请日：1998-05-12
申请人： MERCK & CO., INC.
IPC分类号： C07D265/18
CPC分类号： C07D265/18 , C07B2200/07 , C07C213/08 , C07C215/68 , C07C215/70
摘要： An efficient method for the preparation of key intermediate, in the synthesis of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addition reaction to the 4-chloro-2-trifluoromethylketoaniline with an organozinc complex to give the desired alcohol. This instant method has broad applicability in the chiral addition to any prochiral ketone.
-
-
-
-
-
-
-
-
-
搜索结果
23 条记录 (耗时 0.015 秒)
