-
公开(公告)号：US08859505B2
公开(公告)日：2014-10-14
申请号：US13704441
申请日：2011-06-16
申请人： Susana Ayesa , Urszula Grabowska , Ellen Hewitt , Daniel Jonsson , Bjorn Klasson , Pia Kahnberg , Stina Lundgren , Jan Tejbrant , Daniel Wiktelius
发明人： Susana Ayesa , Urszula Grabowska , Ellen Hewitt , Daniel Jonsson , Bjorn Klasson , Pia Kahnberg , Stina Lundgren , Jan Tejbrant , Daniel Wiktelius
IPC分类号： C07K14/81 , C07D233/60 , C07K5/065 , C07C271/22 , C07D277/56 , A61K38/55 , C07D305/08 , C07K5/062 , C07C275/18 , C07K5/078 , C07C237/22 , C07D213/81
CPC分类号： C07D233/61 , A61K38/55 , C07C231/12 , C07C235/80 , C07C237/22 , C07C271/22 , C07C275/18 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/81 , C07D233/60 , C07D277/56 , C07D305/08 , C07K5/06034 , C07K5/0606 , C07K5/06078 , C07K5/06139
摘要： Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
摘要翻译： 其中R 2a和R 2b独立地是H，卤素，C 1 -C 4烷基，C 1 -C 4卤代烷基或C 1 -C 4烷氧基或R 2a和R 2b与它们所连接的碳原子一起形成C 3 -C 6环烷基的式I化合物; R3是任选地被1-3个独立地选自卤素，C 1 -C 4卤代烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷氧基的取代基取代的C 5 -C 10烷基; 或R3是具有至少2个氯或3个氟取代基的C 2 -C 4烷基链; 或R3是C3-C7环烷基甲基，任选地被1-3个独立地选自C 1 -C 4烷基，卤素，C 1 -C 4卤代烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷氧基的取代基取代; R 4是C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷氧基，C 1 -C 6烷基氨基，C 1 -C 6二烷基氨基或 R 4是Het或碳环基，其任一个任选被1-3个取代基取代，R 4是Het，碳环基，C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷氧基或C 1 -C 6卤代烷氧基; n为1,2或3; 用于预防或治疗以组织蛋白酶S的不适当表达或活化为特征的病症。
-
公开(公告)号：US20130172232A1
公开(公告)日：2013-07-04
申请号：US13704441
申请日：2011-06-16
申请人： Susana Ayesa , Urszula Grabowska , Ellen Hewitt , Daniel Jonsson , Bjorn Klasson , Pia Kahnberg , Stina Lundgren , Jan Tejbrant , Daniel Wiktelius
发明人： Susana Ayesa , Urszula Grabowska , Ellen Hewitt , Daniel Jonsson , Bjorn Klasson , Pia Kahnberg , Stina Lundgren , Jan Tejbrant , Daniel Wiktelius
CPC分类号： C07D233/61 , A61K38/55 , C07C231/12 , C07C235/80 , C07C237/22 , C07C271/22 , C07C275/18 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/81 , C07D233/60 , C07D277/56 , C07D305/08 , C07K5/06034 , C07K5/0606 , C07K5/06078 , C07K5/06139
摘要： Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
-
公开(公告)号：US08859605B2
公开(公告)日：2014-10-14
申请号：US13514760
申请日：2010-12-10
申请人： Susana Ayesa , Peter Carlqvist , Karolina Ersmark , Urszula Grabowska , Ellen Hewitt , Daniel Jonsson , Pia Kahnberg , Bjorn Klasson , Peter Lind , Lourdes Oden , Kevin Parkes , Daniel Wiktelius
发明人： Susana Ayesa , Peter Carlqvist , Karolina Ersmark , Urszula Grabowska , Ellen Hewitt , Daniel Jonsson , Pia Kahnberg , Bjorn Klasson , Peter Lind , Lourdes Oden , Kevin Parkes , Daniel Wiktelius
IPC分类号： C07C271/22 , C07D405/12 , C07D231/40 , C07D277/46
CPC分类号： C07K5/06078 , A61K38/05 , C07C271/22 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D231/40 , C07D277/46 , C07D405/12 , C07K5/06034 , C07K5/0606 , C07K5/06139
摘要： Compounds of the formula I wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylamino or C1-C6dialkylamino; for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
摘要翻译： 式Ⅰ化合物，其中R1a是H; 并且R 1b是C 1 -C 6烷基，碳环或Het; 或R 1a和R 1b一起限定具有3-6个环原子的饱和环胺; R2a和R2b独立地为H，卤素，C1-C4烷基，C1-C4卤代烷基或C1-C4烷氧基，或R2a和R2b与它们所连接的碳原子一起形成C 3 -C 6环烷基; R3是支链C 5 -C 10烷基链，C 2 -C 4卤代烷基或-CH 2 C 3 -C 7环烷基; R 4是C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷基氨基或C 1 -C 6二烷基氨基; 用于预防或治疗以组织蛋白酶S不适当表达或活化为特征的病症。
-
-
搜索结果
3 条记录 (耗时 0.035 秒)
