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公开(公告)号：EP1490058B1
公开(公告)日：2007-10-10
申请号：EP03706045.6
申请日：2003-02-07
IPC分类号： C07D491/10 , C07D493/10 , C07D495/10 , A01N43/90 , C07F9/6561 , C07D309/10 , C07D309/14 , C07D309/08
CPC分类号： C07D235/12 , C07D235/02
摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: and pharmaceutically acceptable salts thereof, wherein: (a) W is selected from the group consisting of O, C, N and S; (b) Z is an aliphatic linker wherein one carbon atom of the aliphatic linker may be replaced with O, NH or S, and wherein such aliphatic linker is optionally substituted with Z'; (c) A is selected from the group consisting of carboxyl, carboxamide, sulfonamide, acylsulfonamide, tetrazole, and (CH2)n COOR19, and wherein said sulfonamide, acylsulfonamide, and tetrazole is each optionally substituted with from one to three substituents each independently selected from A'.
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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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公开(公告)号：EP1073447A1
公开(公告)日：2001-02-07
申请号：EP99909654.8
申请日：1999-02-26
IPC分类号： A61K38/00
摘要： The present invention is directed to N1-acylated derivatives of desleucylA82846B. These derivatives are useful as antibacterials.
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公开(公告)号：EP1869049A1
公开(公告)日：2007-12-26
申请号：EP06738924.7
申请日：2006-03-20
发明人： BARBOSA, Heather, Janelle , COLLINS, Elizabeth, Aaron , HAMDOUCHI, Chafiq , HEMBRE, Erik, James , HIPSKIND, Philip, Arthur , JOHNSTON, Richard, Duane , LU, Jianliang , RUPP, Michael, John , TAKAKUWA, Takako , THOMPSON, Richard, Craig
IPC分类号： C07D487/04 , A61K31/5025 , A61P25/20
CPC分类号： C07D487/04
摘要： The present invention relates to novel substituted imidazo[1,2-b]pyridazine compounds of Formula (I): pharmaceutical compositions thereof, and the use such compounds as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric disorders and neurological diseases.
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公开(公告)号：EP1490058A1
公开(公告)日：2004-12-29
申请号：EP03706045.6
申请日：2003-02-07
IPC分类号： A61K31/4184 , C07D235/16 , C07D235/02
CPC分类号： C07D235/12 , C07D235/02
摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: and pharmaceutically acceptable salts thereof, wherein: (a) W is selected from the group consisting of O, C, N and S; (b) Z is an aliphatic linker wherein one carbon atom of the aliphatic linker may be replaced with O, NH or S, and wherein such aliphatic linker is optionally substituted with Z'; (c) A is selected from the group consisting of carboxyl, carboxamide, sulfonamide, acylsulfonamide, tetrazole, and (CH2)n COOR19, and wherein said sulfonamide, acylsulfonamide, and tetrazole is each optionally substituted with from one to three substituents each independently selected from A'.
摘要翻译： 本发明涉及由以下结构式表示的化合物及其药学上可接受的盐：其中：（a）W选自O，C，N和S; （b）Z为脂族连接基，其中脂族连接基的一个碳原子可以被O，NH或S替代，并且其中这种脂族连接基任选被Z'取代; （c）A选自羧基，羧酰胺，磺酰胺，酰基磺酰胺，四唑和（CH 2）n COOR 19，并且其中所述磺酰胺，酰基磺酰胺和四唑各自任选被1至3个各自独立地选自 来自A'。
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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：EP1073447B1
公开(公告)日：2007-05-09
申请号：EP99909654.8
申请日：1999-02-26
摘要： The present invention is directed to N1-acylated derivatives of desleucylA82846B. These derivatives are useful as antibacterials.
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公开(公告)号：EP1453811A2
公开(公告)日：2004-09-08
申请号：EP02804416.2
申请日：2002-11-26
发明人： GIBSON, Tracey, Ann , JOHNSTON, Richard, Duane , MANTLO, Nathan, Bryan , THOMPSON, Richard, Craig , WANG, Xiaodong , WINNEROSKI, Leonard, Larry, Junior , XU, Yanping
IPC分类号： C07D233/32 , A61K31/4166 , A61P43/00 , C07D233/76 , C07D233/70 , C07D401/06 , C07D403/12 , C07D405/06 , C07D405/12
CPC分类号： C07D401/06 , C07D233/32 , C07D233/70 , C07D233/76 , C07D403/12 , C07D405/06 , C07D405/12
摘要： The present ilnvention is directed to compounds represented by the following structural Formula (I), (c) W is O or S; (d) X is an optionally substituted Cl-C5 alkylene linker wherein one carbon atom of the linker may optionally be replaced. with O, NH, S, and optionally two carbons together may form a double bond; (e) Y is selected from the group consisting of C, O, S, NH and a single bond; and (f) E is selected from the group consisting of C(R3) (R4)A, A, and a substituted or unsubstituted group selected from the group consisting of (CH2)n COOR19.
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公开(公告)号：EP1869049B1
公开(公告)日：2009-03-04
申请号：EP06738924.7
申请日：2006-03-20
发明人： BARBOSA, Heather, Janelle , COLLINS, Elizabeth, Aaron , HAMDOUCHI, Chafiq , HEMBRE, Erik, James , HIPSKIND, Philip, Arthur , JOHNSTON, Richard, Duane , LU, Jianliang , RUPP, Michael, John , TAKAKUWA, Takako , THOMPSON, Richard, Craig
IPC分类号： C07D487/04 , A61K31/5025 , A61P25/20
CPC分类号： C07D487/04
摘要： The present invention relates to novel substituted imidazo[1,2-b]pyridazine compounds of Formula (I): pharmaceutical compositions thereof, and the use such compounds as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric disorders and neurological diseases.
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公开(公告)号：EP1254164B1
公开(公告)日：2005-11-02
申请号：EP01910588.1
申请日：2001-02-12
摘要： The present invention provides a process for selectively acylating an A82846A, A82846B, A82846C or PA-42867-A glycopeptide at the N1, N2 or N3 positions and the monoacylated compounds prepared therefrom.
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