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1. 发明申请

US20040229915A1 Cysteine protease inhibitors 审中-公开
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US20040229915A1
公开(公告)日：2004-11-18
申请号：US10853408
申请日：2004-05-24
申请人： MEDIVIR AB
发明人： Martin Quibell , Steven Taylor , Urszula Grabowska , Magnus Nilsson , Veronique Morrison
IPC分类号： A61K031/452 , A61K031/4025 , A61K031/366 , C07D45/02
CPC分类号： C07D405/12 , C07D307/22 , C07D307/32 , C07D307/68 , C07D307/85 , C07D309/14 , C07D309/30 , C07D405/14 , C07D409/12 , C07D409/14
摘要： of the formula (IV): 1 where: R1nullRnullC(O), RnullSO2, Rnullnulla bicyclic, saturated or unsaturated, 8-12 membered ring system containing 0-4 hetero atoms selected from S, O and N, which is optionally substituted with up to four substituents independently selected from groups a), b) and c) below; or Rnullnulla monocyclic, saturated or unsaturated, 5-7 membered ring containing 0-3 hetero atoms selected from S, O and N, which monocyclic ring bears at least one substituent selected from group a) and/or c) and which may optionally bear one or two further substituents selected from group b); R4nullH, C1-7-alkyl, ArnullC1-7-alkyl, Ar, C3-7-cycloalkyl; C2-7alkenyl,; R3nullC1-7-alkyl, C2-C7 alkenyl, C2-C7 alkenyl, C3-7-cycloalkyl, ArnullC1-7-alkyl, Ar; R5nullC1-7-alkyl, halogen,ArnullC1-7-alkyl, C0-3-alkyl-CONR3R4 or a bulky amine R6 is H, C1-7-alkyl, ArnullC1-7-alkyl, C1-3-alkyl-SO2-Rix, C1-3-alkyl-C(O)nullNHRix or CH2XAr q is 0 or 1 have utility as inhibitors of cysteine proteases such as cathepsin K and falcipain.
摘要翻译：式（Ⅳ）：其中：R1 = R'C（O），R'SO2，R'=含有0-4个杂原子的双环饱和或不饱和的8-12元环系，其选自S，O和 N，其任选被至多四个独立地选自以下的基团a），b）和c）中的取代基取代; 或R'=含有0-3个选自S，O和N的杂原子的单环，饱和或不饱和的5-7元环，该单环具有至少一个选自a）和/或c）的取代基，并且其中可以任选地带有一个或两个其它选自组b）的取代基; R 4 = H，C 1-7 - 烷基，Ar-C 1-7 - 烷基，Ar，C 3-7 - 环烷基; C2-7烯基 R 3 = C 1-7 - 烷基，C 2 -C 7烯基，C 2 -C 7烯基，C 3-7 - 环烷基，Ar-C 1-7 - 烷基，Ar; R5 = C1-7烷基，卤素，Ar-C1-7 - 烷基，C0-3 - 烷基-CONR3R4或大体积的胺R6是H，C1-7 - 烷基，Ar-C1-7 - 烷基，C1-3 - 烷基-SO 2 -R 5，C 1-3 - 烷基-C（O）-NHR x或CH 2 XAr q为0或1可用作半胱氨酸蛋白酶如组织蛋白酶K和恶性蛋白酶的抑制剂。

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