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公开(公告)号：EP0805802B1
公开(公告)日：2000-08-16
申请号：EP96900634.5
申请日：1996-01-22
发明人： PORTER, Barry , SMITH, Christopher , WALSH, Roger, John, Aitchison , MAJID, Tahir, Nadeem , McCARTHY, Clive , HARRIS, Neil, Victor , ASTLES, Peter, Charles , McLAY, Iain, McFarlane , MORLEY, Andrew, David , HALLEY, Frank , BRIDGE, Andrew, William , VAN SICKLE, Andrew, Paul
IPC分类号： C07D213/30 , A61K31/19 , A61K31/41 , A61K31/44 , C07D333/16 , C07D317/54 , C07C59/70
CPC分类号： C07D213/30 , C07C255/54 , C07D213/61 , C07D237/08 , C07D263/56 , C07D275/02 , C07D277/24 , C07D307/12 , C07D317/54 , C07D333/16 , C07D405/12 , C07D411/12
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2.发明公开SUBSTITUTED AZABICYLIC COMPOUNDS AND THEIR USE AS INHIBITORS OF THE PRODUCTION OF TNF AND CYCLIC AMP PHOSPHODIESTERASE 失效取代的氮杂双环化合物及其作为肿瘤坏死因子和cAMP磷酸二酯酶抑制剂的
公开(公告)号：EP0934307A1
公开(公告)日：1999-08-11
申请号：EP97926148.0
申请日：1997-06-19
发明人： COX, Paul, Joseph , BOWER, Shelley , ALDOUS, David, John , ASTLES, Peter, Charles , McGARRY, Daniel, Gerard, Rhone-Poulenc Rorer Inc. , HULME, Christopher, Rhone-Poulenc Rorer Inc. , REGAN, John, Robinson, Rhone-Poulenc Rorer Inc. , HUANG, Fu-Chih, Rhone-Poulenc Rorer Inc. , DJURIC, Stevan, Wakefield, Rhone-Poulenc Rorer Inc , MORIARTY, Kevin, Joseph, Rhone-Poulenc Rorer Inc. , MATHEW, Rose, M., Rhone-Poulenc Rorer Inc. , POLI, Gregory, Bernard, Rhone-Poulenc Rorer Inc.
IPC分类号： C07D235 , A61K31 , A61P9 , A61P11 , A61P17 , A61P25 , A61P29 , A61P35 , A61P37 , A61P43 , C07D209 , C07D401 , C07D403 , C07D405 , C07D409 , C07D413 , C07D417
CPC分类号： C07D235/24 , C07D209/12 , C07D209/42 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： This invention is directed to physiologically active compounds of formula (I) wherein (i) represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring (ii) is an azaheterocycle, and the ring (iii) represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; wherein R?1-R3, A1, Z1¿, m and n are as defined herein. Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.
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公开(公告)号：EP0805802A1
公开(公告)日：1997-11-12
申请号：EP96900634.0
申请日：1996-01-22
发明人： PORTER, Barry , SMITH, Christopher , WALSH, Roger, John, Aitchison , MAJID, Tahir, Nadeem , McCARTHY, Clive , HARRIS, Neil, Victor , ASTLES, Peter, Charles , McLAY, Iain, McFarlane , MORLEY, Andrew, David , HALLEY, Frank , BRIDGE, Andrew, William , VAN SICKLE, Andrew, Paul
IPC分类号： A61K31 , A61P9 , A61P25 , A61P43 , C07C255 , C07D213 , C07D237 , C07D263 , C07D275 , C07D277 , C07D307 , C07D317 , C07D333 , C07D405 , C07D411
CPC分类号： C07D213/30 , C07C255/54 , C07D213/61 , C07D237/08 , C07D263/56 , C07D275/02 , C07D277/24 , C07D307/12 , C07D317/54 , C07D333/16 , C07D405/12 , C07D411/12
摘要： Compounds of formula (I) are described, wherein: R1 is CN, CH¿2?CN, CH=CHCN, CHO, or CH=CHCO2H; R?2¿ is aryl lower alkoxy, heteroaryl lower alkoxy, aryl lower alkylthio or heteroaryl lower alkylthio in which each of the aryl and heteroaryl moieties is optionally substituted; R3 is halogen; R4 is optionally substituted aryl or optionally substituted heteroaryl; R5 is carboxy or an acid isostere; X is oxygen or sulphur; and n is zero or 1; and their N-oxides and prodrugs, and pharmaceutically acceptable salts thereof. The compounds have endothelin antagonist activity and are useful as pharmaceuticals.
摘要翻译： 描述了式（I）化合物，其中：R 1是CN，CH 2 CN，CH = CHCN，CHO或CH = CHCO 2 H; R2是芳基低级烷氧基，杂芳基低级烷氧基，芳基低级烷硫基或杂芳基低级烷硫基，其中每个芳基和杂芳基部分任选被取代; R3是卤素; R4是任选取代的芳基或任选取代的杂芳基; R5是羧基或酸等电点; X是氧或硫; 并且n是零或1; 及其N-氧化物和前药及其药学上可接受的盐。 该化合物具有内皮素拮抗剂活性并可用作药物。
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