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公开(公告)号：EP1335908B1
公开(公告)日：2008-02-13
申请号：EP01989704.0
申请日：2001-11-09
发明人： MANTLO, Nathan, Bryan , COLLADO CANO, Ivan , DOMINIANNI, Samuel, James , ETGEN, Garret, Jay, Junior , GARCIA-PAREDES, Cristina , JOHNSTON, Richard, Duane , LETOURNEAU, Michael, Edward , MARTINELLI, Michael, John , MAYHUGH, Daniel, Ray , SAEED, Ashraf , THOMPSON, Richard, Craig , WANG, Xiadong , COFFEY, David, Scott , SCHMID, Christopher, Randall , VICENZI, Jeffrey, Thomas , XU, Yanping
IPC分类号： C07D249/12 , A61K31/4196 , C07D401/06 , C07D413/06 , C07D409/06 , C07D409/12 , C07D417/12 , C07D405/06 , A61K31/4439 , A61K31/427 , C07C257/22 , C07C281/04 , C07C281/06
CPC分类号： C07C281/06 , C07C257/22 , C07C281/04 , C07D249/12 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12
摘要： he present invention is directed to compounds represented by the following structural formula (I'), and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.
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公开(公告)号：EP0979076A1
公开(公告)日：2000-02-16
申请号：EP98919936.9
申请日：1998-04-28
IPC分类号： A61K31/38 , A61K31/40 , A61K31/445 , A61K31/55 , A61K31/535 , C07D333/58 , C07D409/10 , C07D409/12 , C07D413/10 , C07D413/12
CPC分类号： C07D333/64 , C07D333/56 , C07D333/68
摘要： The instant invention provides processes for preparing compounds of formulae (IV, V, and IX), having structures provided. These compounds are useful intermediates in the further preparation of benzo[b]thiophenes.
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公开(公告)号：EP1335908A2
公开(公告)日：2003-08-20
申请号：EP01989704.0
申请日：2001-11-09
发明人： MANTLO, Nathan, Bryan , COLLADO CANO, Ivan , DOMINIANNI, Samuel, James , ETGEN, Garret, Jay, Junior , GARCIA-PAREDES, Cristina , JOHNSTON, Richard, Duane , LETOURNEAU, Michael, Edward , MARTINELLI, Michael, John , MAYHUGH, Daniel, Ray , SAEED, Ashraf , THOMPSON, Richard, Craig , WANG, Xiadong , COFFEY, David, Scott , SCHMID, Christopher, Randall , VICENZI, Jeffrey, Thomas , XU, Yanping
IPC分类号： C07D249/12 , A61K31/4196 , C07D401/06 , C07D413/06 , C07D409/06 , C07D409/12 , C07D417/12 , C07D405/06 , A61K31/4439 , A61K31/427 , C07C257/22 , C07C281/04 , C07C281/06
CPC分类号： C07C281/06 , C07C257/22 , C07C281/04 , C07D249/12 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12
摘要： he present invention is directed to compounds represented by the following structural formula (I'), and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.
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