公开(公告)号：EP1326846A1

公开(公告)日：2003-07-16

申请号：EP01977866.1

申请日：2001-10-01

申请人： Merck & Co., Inc.

发明人： MCWILLIAMS, James Christopher ,  BUCK, Elizabeth ,  ENG, Kan, K. ,  MALIGRES, Peter, E. ,  SAGER, Jess, W. ,  WATERS, Marjorie See ,  HUMPHREY, Guy, R.

IPC分类号： C07D239/02 ,  C07D401/00 ,  C07D471/02 ,  C07D487/02

CPC分类号： C07D471/04

摘要： A novel process is provided for the preparation of chiral intermediates useful in the asymmetric syntheses of αvβ3 integrin receptor antagonists. Also provided are the enantiomerically enriched intermediates that are obtained from the process.

公开(公告)号：EP0748319B1

公开(公告)日：2001-12-12

申请号：EP95911105.5

申请日：1995-02-27

申请人： Merck & Co., Inc.

发明人： ASKIN, David ,  ENG, Kan, K. ,  MALIGRES, Peter, E. ,  REIDER, Paul, J. ,  ROSSEN, Kai ,  VOLANTE, Ralph, P. ,  UPADHYAY, Veena

IPC分类号： C07D413/06 ,  C07D263/52 ,  C07D413/04

CPC分类号： C07D263/52 ,  C07D413/06

摘要： A process for synthesizing the epoxide of formula (I) consists of, at a minimum, formation of a halohydrin form the allyl acetonide reactant, followed by base-induced cyclization, the epoxide product (I) being useful as an intermediate for the synthesis of inhibitors of renin or HIV protease or other proteases.

公开(公告)号：EP0748319A1

公开(公告)日：1996-12-18

申请号：EP95911105.0

申请日：1995-02-27

申请人： Merck & Co., Inc.

发明人： ASKIN, David ,  ENG, Kan, K. ,  MALIGRES, Peter, E. ,  REIDER, Paul, J. ,  ROSSEN, Kai ,  VOLANTE, Ralph, P. ,  UPADHYAY, Veena

IPC分类号： C07D213 ,  A61K31 ,  A61P31 ,  A61P37 ,  C07D263 ,  C07D413

CPC分类号： C07D263/52 ,  C07D413/06

摘要： A process for synthesizing the epoxide of formula (I) consists of, at a minimum, formation of a halohydrin form the allyl acetonide reactant, followed by base-induced cyclization, the epoxide product (I) being useful as an intermediate for the synthesis of inhibitors of renin or HIV protease or other proteases.

公开(公告)号：EP1427726A1

公开(公告)日：2004-06-16

申请号：EP02763531.7

申请日：2002-08-13

申请人： Merck & Co., Inc.

发明人： MALIGRES, Peter, E. ,  ASKIN, David

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  Y02P20/55

摘要： The preparation of 5-sulfonamido-8-hydroxy-1,6-naphthyridine-7-carboxamides is disclosed. A 5-halo-8-hydroxy-1,6-napthyridine-7-carboxylic acid or acid ester in which the hydroxy is derivatized with a protecting group is reacted with a sulfonamide (e.g., an alkanesulfonamide, N-alkyl alkanesulfonamide, or alkanesultam) in the presence of a copper promoter and a chelating agent, followed by deprotection of the hydroxy group, and then coupling with an amine to obtain the 5-sulfonamido-8-hydroxy-1,6-naphthyridine-7-carboxamide. Alternatively, the hydroxy-protected 5-halo-8-hydroxy-1,6-napthyridine-7-carboxylic acid (or ester) is first coupled with an amine, the resulting carboxamide reacted with a sulfonamide followed by deprotection of the hydroxy group to obtain the 5-sulfonamido-8-hydroxy-1,6-naphthyridine-7-carboxamide. The 5-sulfonamido-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and are useful for treating HIV infection, preventing HIV infection, delaying the onset of AIDS, and treating AIDS.

公开(公告)号：EP0823904A1

公开(公告)日：1998-02-18

申请号：EP96911786.0

申请日：1996-04-15

申请人： MERCK & CO., INC.

发明人： ASKIN, David ,  MALIGRES, Peter, E. ,  REIDER, Paul, J. ,  ROSSEN, Kai ,  SAGER, Jess ,  UPADHYAY, Veena ,  VOLANTE, Ralph, P. ,  WELLS, Kenneth, M.

IPC分类号： C07D471

CPC分类号： C07D471/10 ,  Y02P20/55

摘要： The present invention is directed to a novel process for the preparation of a spiroindoline sulfonamides of formula (I), wherein L is hydrogen or an amino protecting group. These compounds are useful in the preparation of certain spiro compounds which have the ability to stimulate the release of natural or endogeneous growth hormone. The spiro compounds may be used to treat conditions which require the stimulation of growth hormone production or secretion such as in humans with a deficiency of natural growth hormone or in animals used for food or wool production where the stimulation of growth hormone will result in a larger, more productive animal.