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公开(公告)号：US20120283305A1
公开(公告)日：2012-11-08
申请号：US13514760
申请日：2010-12-10
申请人： Susana Ayesa , Peter Carlqvist , Karolina Ersmark , Urszula Grabowska , Ellen Hewitt , Daniel Jönsson , Pia Kahnberg , Björn Klasson , Peter Lind , Lourdes Odén , Kevin Parkes , Daniel Wiktelius
发明人： Susana Ayesa , Peter Carlqvist , Karolina Ersmark , Urszula Grabowska , Ellen Hewitt , Daniel Jönsson , Pia Kahnberg , Björn Klasson , Peter Lind , Lourdes Odén , Kevin Parkes , Daniel Wiktelius
IPC分类号： A61K31/415 , C07C237/22 , A61K31/16 , A61P17/06 , A61P37/00 , A61P7/00 , A61P29/00 , A61P19/02 , A61P25/00 , A61P21/04 , A61P11/02 , A61P11/06 , A61P9/10 , A61P11/00 , C07D231/40
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。
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公开(公告)号：US20120309673A1
公开(公告)日：2012-12-06
申请号：US13514758
申请日：2010-12-10
申请人： Susana Ayesa , Karolina Ersmark , Urszula Grabowska , Ellen Hewitt , Daniel Jönsson , Pia Kahnberg , Björn Klasson , Peter Lind , Stina Lundgren , Lourdes Odén , Kevin Parkes , Daniel Wiktelius
发明人： Susana Ayesa , Karolina Ersmark , Urszula Grabowska , Ellen Hewitt , Daniel Jönsson , Pia Kahnberg , Björn Klasson , Peter Lind , Stina Lundgren , Lourdes Odén , Kevin Parkes , Daniel Wiktelius
IPC分类号： A61K38/05 , A61P19/02 , A61P25/00 , C07D241/04 , A61P9/00 , C07D233/48 , C07C271/20 , C07D261/14 , C07D231/40 , A61P11/06
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 Formula II 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 or oxetany-3-yl. for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
摘要翻译： 式II的化合物，其中R 1a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卤代烷基或氧杂环丁烷-3-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。
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公开(公告)号：US08815809B2
公开(公告)日：2014-08-26
申请号：US13514758
申请日：2010-12-10
申请人： Susana Ayesa , Karolina Ersmark , Urszula Grabowska , Ellen Hewitt , Daniel Jönsson , Pia Kahnberg , Björn Klasson , Peter Lind , Stina Lundgren , Lourdes Odèn , Kevin Parkes , Daniel Wiktelius
发明人： Susana Ayesa , Karolina Ersmark , Urszula Grabowska , Ellen Hewitt , Daniel Jönsson , Pia Kahnberg , Björn Klasson , Peter Lind , Stina Lundgren , Lourdes Odèn , Kevin Parkes , Daniel Wiktelius
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 Formula II 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 or oxetany-3-yl. for use in the prophylaxis or treatment of a disorder characterized by inappropriate expression or activation of cathepsin S.
摘要翻译： 式II的化合物，其中R 1a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卤代烷基或氧杂环丁烷-3-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。
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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。
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