公开(公告)号：EP0973755A1

公开(公告)日：2000-01-26

申请号：EP98914408.4

申请日：1998-04-02

申请人： Du Pont Pharmaceuticals Company ,  Merck & Co., Inc.

发明人： PIERCE, Michael, E. ,  CHEN, Cheng, Y. ,  CHOUDHURY, Anusuya ,  RADESCA, Lilian, A. ,  TAN, Lushi ,  ZHAO, Dalian

IPC分类号： C07D265/18 ,  C07C215/68 ,  C07C211/52

CPC分类号： C07D265/18 ,  C07C213/00 ,  C07C213/02 ,  C07C221/00 ,  C07C2601/02 ,  C07C215/68 ,  C07C217/58 ,  C07C225/22

摘要： The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In an embodiment, the present invention provides a process for the preparation of an amino alcohol compound of formula (V-i) comprising adding a toluene solution of 2,3-dichloro-5,6-dicyano-1,4-benzoquinone to a toluene solution of a compound of formula (III-i), via a compound of formula (IV-i).

摘要翻译： 本发明提供了用于不对称合成式（Ⅵ-ⅰ）的（S）-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-酮的新方法 ），其可用作人类免疫缺陷病毒（HIV）逆转录酶抑制剂。

公开(公告)号：EP0973737A1

公开(公告)日：2000-01-26

申请号：EP98903459.0

申请日：1998-01-06

申请人： MERCK & CO., INC.

发明人： CHEN, Cheng, Yi ,  XU, Feng ,  TILLYER, Richard, D. ,  ZHAO, Dalian

IPC分类号： C07D205/04 ,  C07D209/44 ,  C07D211/14 ,  C07D221/04 ,  C07D295/088 ,  C07D295/092 ,  C07D295/096

CPC分类号： C07D221/14 ,  C07B2200/07 ,  C07C2602/08 ,  C07D205/04 ,  C07D209/44 ,  C07D295/092 ,  C07D295/096

摘要： An efficient method for the quantitative preparation and isolation of a compound of formula (I) or its enantiomer, a chiral mediator used in enantioselective synthesis.

摘要翻译： 用于定量制备和分离式（I）化合物或其对映异构体的有效方法，其用于对映选择性合成中使用的手性介体。

公开(公告)号：EP1858844A1

公开(公告)日：2007-11-28

申请号：EP06737635.0

申请日：2006-03-10

申请人： Merck & Co., Inc.

发明人： ZHAO, Dalian ,  MARCOUX, Jean-Francois ,  BOARDMAN, David ,  LEYES, Aquiles, E.

IPC分类号： C07D209/10 ,  A01N43/38

CPC分类号： C07D209/12

摘要： Novel crystalline forms of two indole compounds connected to phenoxyalkylcarboxylic acid groups are selective PPAR gamma partial agonists that are useful in the treatment of type 2 diabetes, hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. The novel crystal forms include a crystalline free acid dihydrate and crystalline free acid anhydrate of one compound and several crystalline forms of the free acid and the sodium salt of the second compound. The invention also relates to pharmaceutical compositions comprising these novel crystal forms, processes to prepare the crystal forms and their pharmaceutical compositions, and uses of the crystal forms in the treatment of type 2 diabetes and other PPAR gamma modulated diseases.

公开(公告)号：EP1124798A1

公开(公告)日：2001-08-22

申请号：EP99955168.2

申请日：1999-10-25

申请人： Merck & Co., Inc.

发明人： TILLYER, Richard, D. ,  LARSEN, Robert, D. ,  DAVIES, Ian, W. ,  ZHAO, Dalian ,  KING, Anthony, On-Ping ,  CHEN, Cheng, Y. ,  GRABOWSKI, Edward, J., J. ,  WANG, Xin ,  O'SHEA, Paul

IPC分类号： C07C319/14 ,  C07C321/28

CPC分类号： C07C319/20 ,  C07C323/22

摘要： This invention encompasses a novel process for synthesizing compounds represented by formula (A). These compounds are intermediates useful in the preparation of certain agents that are selective COX-2 inhibitors.