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公开(公告)号:EP1089973B1
公开(公告)日:2005-11-09
申请号:EP99930402.5
申请日:1999-06-18
发明人: BISACCHI, Gregory , SLUSARCHYK, William, A. , TREUNER, Uwe , SUTTON, James, C. , ZAHLER, Robert , SEILER, Steven , KRONENTHAL, David, R. , RANDAZZO, Michael, E. , XU, Zhongmin , SHI, Zhongping , SCHWINDEN, Mark, D.
IPC分类号: C07D205/08 , C07D205/09 , C07D403/12 , C07D401/06 , C07D403/06 , A61K31/395
CPC分类号: C07D403/12 , C07D205/08
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2.CONFORMATIONALLY RESTRICTED AROMATIC INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND METHOD 失效
标题翻译: 微粒体甘油三酯转运和程序的构象芳香酶抑制剂公开(公告)号:EP0904262B1
公开(公告)日:2004-04-21
申请号:EP97903805.6
申请日:1997-01-13
发明人: BILLER, Scott, A. , DICKSON, John, K. , LAWRENCE, R., Michael , MAGNIN, David, R. , POSS, Michael, A. , ROBL, Jeffrey, A. , SLUSARCHYK, William, A. , SULSKY, Richard, B. , TINO, Joseph, A.
IPC分类号: C07C217/04 , C07D471/04 , C07D471/10 , C07D233/78 , C07D401/08 , C07D403/08 , A61K31/24 , A61K31/445 , A61K31/415 , A61K31/44 , A61K31/47
CPC分类号: C07F7/1856 , A61K31/191 , A61K31/366 , A61K31/404 , A61K31/4468 , C07C17/093 , C07C47/453 , C07C49/563 , C07C49/567 , C07C49/573 , C07C69/00 , C07C205/11 , C07C205/43 , C07C205/55 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/62 , C07C233/63 , C07C233/78 , C07C235/40 , C07C235/56 , C07C237/22 , C07C237/24 , C07C255/41 , C07C259/08 , C07C271/22 , C07C291/04 , C07C311/19 , C07C311/21 , C07C311/37 , C07C311/42 , C07C311/46 , C07C317/12 , C07C321/22 , C07C323/60 , C07C2601/02 , C07C2601/14 , C07C2603/00 , C07C2603/18 , C07C2603/32 , C07C2603/74 , C07D207/335 , C07D207/38 , C07D209/08 , C07D209/16 , C07D209/34 , C07D209/38 , C07D209/46 , C07D209/48 , C07D211/60 , C07D211/62 , C07D213/40 , C07D213/64 , C07D213/74 , C07D213/75 , C07D213/80 , C07D213/89 , C07D221/16 , C07D231/56 , C07D233/24 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D235/08 , C07D235/16 , C07D235/24 , C07D235/26 , C07D235/28 , C07D235/30 , C07D239/38 , C07D239/42 , C07D239/47 , C07D249/12 , C07D249/14 , C07D249/18 , C07D253/07 , C07D263/38 , C07D263/46 , C07D263/58 , C07D271/07 , C07D277/36 , C07D277/56 , C07D277/74 , C07D285/08 , C07D285/125 , C07D295/108 , C07D295/155 , C07D295/185 , C07D307/14 , C07D311/84 , C07D317/30 , C07D317/58 , C07D319/06 , C07D327/06 , C07D333/20 , C07D335/14 , C07D401/12 , C07D403/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07C25/22
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公开(公告)号:EP1089973A1
公开(公告)日:2001-04-11
申请号:EP99930402.5
申请日:1999-06-18
发明人: BISACCHI, Gregory , SLUSARCHYK, William, A. , TREUNER, Uwe , SUTTON, James, C. , ZAHLER, Robert , SEILER, Steven , KRONENTHAL, David, R. , RANDAZZO, Michael, E. , XU, Zhongmin , SHI, Zhongping , SCHWINDEN, Mark, D.
IPC分类号: C07D205/08 , C07D205/09
CPC分类号: C07D403/12 , C07D205/08
摘要: Compounds of formulae (I), (II), (III).
摘要翻译: 式(I),(II),(III)的化合物。
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4.LACTAM COMPOUNDS AND THEIR USE AS INHIBITORS OF SERINE PROTEASES AND METHOD 审中-公开
标题翻译: LAKTAMVERBINDUNGN及其作为抑制剂丝氨酸蛋白酶和相关程序公开(公告)号:EP1309609A2
公开(公告)日:2003-05-14
申请号:EP01959048.8
申请日:2001-07-20
发明人: BISACCHI, Gregory, S. , SEILER, Steven, M. , LAWRENCE, R., Michael , SUTTON, James, C., Jr. , SLUSARCHYK, William, A. , ZHAO, Guohua
CPC分类号: C07D223/10 , A61K31/55 , A61K38/00 , A61K45/06 , C07K5/06139 , C07K5/06191 , A61K2300/00
摘要: Lactam inhibitors are provided which have the structure (I), x is (a) or (b) wherein Y is O or S and R4 is (i), (ii) or R8 at least one of R?1 and R2¿ is hydrogen, and R?1, R2, R3, R5, R6, R7, and R8¿, are as defined herein. These compounds are inhibitors of tryptase and thus are useful in treating asthma. Methods for treating asthma and related diseases are also provided.
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5.CONFORMATIONALLY RESTRICTED AROMATIC INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND METHOD 失效
标题翻译: 微粒体甘油三酯转运和程序的构象芳香酶抑制剂公开(公告)号:EP0904262A1
公开(公告)日:1999-03-31
申请号:EP97903805.0
申请日:1997-01-13
发明人: BILLER, Scott, A. , DICKSON, John, K. , LAWRENCE, R., Michael , MAGNIN, David, R. , POSS, Michael, A. , ROBL, Jeffrey, A. , SLUSARCHYK, William, A. , SULSKY, Richard, B. , TINO, Joseph, A.
IPC分类号: A61K31 , C07C17 , C07C33 , C07C47 , C07C49 , C07C69 , C07C205 , C07C233 , C07C235 , C07C237 , C07C255 , C07C259 , C07C271 , C07C291 , C07C311 , C07C317 , C07C321 , C07C323 , C07D207 , C07D209 , C07D211 , C07D213 , C07D221 , C07D231 , C07D233 , C07D235 , C07D239 , C07D249 , C07D253 , C07D263 , C07D271 , C07D277 , C07D285 , C07D295 , C07D307 , C07D311 , C07D317 , C07D319 , C07D327 , C07D333 , C07D335 , C07D401 , C07D403 , C07D405 , C07D407 , C07D409 , C07D417 , C07D471 , C07D473 , C07D487 , C07F7 , C07F9
CPC分类号: C07F7/1856 , A61K31/191 , A61K31/366 , A61K31/404 , A61K31/4468 , C07C17/093 , C07C47/453 , C07C49/563 , C07C49/567 , C07C49/573 , C07C69/00 , C07C205/11 , C07C205/43 , C07C205/55 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/62 , C07C233/63 , C07C233/78 , C07C235/40 , C07C235/56 , C07C237/22 , C07C237/24 , C07C255/41 , C07C259/08 , C07C271/22 , C07C291/04 , C07C311/19 , C07C311/21 , C07C311/37 , C07C311/42 , C07C311/46 , C07C317/12 , C07C321/22 , C07C323/60 , C07C2601/02 , C07C2601/14 , C07C2603/00 , C07C2603/18 , C07C2603/32 , C07C2603/74 , C07D207/335 , C07D207/38 , C07D209/08 , C07D209/16 , C07D209/34 , C07D209/38 , C07D209/46 , C07D209/48 , C07D211/60 , C07D211/62 , C07D213/40 , C07D213/64 , C07D213/74 , C07D213/75 , C07D213/80 , C07D213/89 , C07D221/16 , C07D231/56 , C07D233/24 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/06 , C07D235/08 , C07D235/16 , C07D235/24 , C07D235/26 , C07D235/28 , C07D235/30 , C07D239/38 , C07D239/42 , C07D239/47 , C07D249/12 , C07D249/14 , C07D249/18 , C07D253/07 , C07D263/38 , C07D263/46 , C07D263/58 , C07D271/07 , C07D277/36 , C07D277/56 , C07D277/74 , C07D285/08 , C07D285/125 , C07D295/108 , C07D295/155 , C07D295/185 , C07D307/14 , C07D311/84 , C07D317/30 , C07D317/58 , C07D319/06 , C07D327/06 , C07D333/20 , C07D335/14 , C07D401/12 , C07D403/04 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07C25/22
摘要: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure (I) or (IA) or (IB) including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0,1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) -O-; or (3) (i); B is: (ii) or (iii) or (iv) or (v) (wherein (a = 2, 3 or 4)) or (vi) or (vii) or (viii); and wherein L?2, L1, R1, R2, R3, R3', R3a, R3b, R4, R4', R5¿, X, (ix), (x) and (xi) are as defined herein.
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