-
公开(公告)号:US08853281B2
公开(公告)日:2014-10-07
申请号:US13139962
申请日:2009-12-18
申请人: Susana Ayesa , Anna Karin Belfrage , Bjorn Classon , Urszula Grabowska , Ellen Hewitt , Vladimir Ivanov , Daniel Jönsson , Pia Kahnberg , Peter Lind , Magnus Nilsson , Lourdes Odén , Mikael Pelcman , Horst Wähling
发明人: Susana Ayesa , Anna Karin Belfrage , Bjorn Classon , Urszula Grabowska , Ellen Hewitt , Vladimir Ivanov , Daniel Jönsson , Pia Kahnberg , Peter Lind , Magnus Nilsson , Lourdes Odén , Mikael Pelcman , Horst Wähling
IPC分类号: A01N33/02 , A61K31/13 , A01N37/00 , A61K31/21 , A01N33/00 , A61K31/16 , A01N37/18 , A61K31/165 , A01N35/00 , A61K31/12 , A01N33/18 , A01N33/24 , A61K31/04 , A01N29/00 , A61K31/02 , A01N29/02 , C07D231/00 , C07D413/00 , C07D295/22 , C07D307/02 , C07C303/00 , C07C307/00 , C07C309/00 , C07C311/00 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00 , C07C261/00 , C07C269/00 , C07C271/00 , C07D405/12 , C07D403/12 , C07C271/24 , C07D417/12 , C07C311/21 , C07D241/24 , C07D401/12 , C07D277/36 , C07D307/85 , C07D307/68 , C07D277/56 , C07D295/215 , C07C237/24 , C07D231/40 , C07D207/34 , C07D213/71 , C07D231/14 , C07D239/80 , C07D213/40
CPC分类号: C07C311/21 , C07C237/24 , C07C271/24 , C07C2601/02 , C07C2601/04 , C07C2601/06 , C07C2601/08 , C07D207/34 , C07D213/40 , C07D213/71 , C07D231/14 , C07D231/40 , C07D239/80 , C07D241/24 , C07D277/36 , C07D277/56 , C07D295/215 , C07D307/68 , C07D307/85 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12
摘要: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, 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-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.
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是H,卤素,C1-C4烷基,C1-C4卤代烷基,C1-C4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; R3是支链C 5 -C 10烷基链,C 2 -C 4卤代烷基或C 3 -C 7环烷基甲基,R 4是Het,碳环基,如说明书中所定义的任选取代,以及其药学上可接受的盐,水合物和N-氧化物; 是组织蛋白酶S的抑制剂,并且可用于治疗牛皮癣,自身免疫性疾病和其它疾病如哮喘,动脉硬化,COPD和慢性疼痛。
-
公开(公告)号:US20110312964A1
公开(公告)日:2011-12-22
申请号:US13139962
申请日:2009-12-18
申请人: Susana Ayesa , Anna Karin Belfrage , Björn Classon , Urszula Grabowska , Ellen Hewitt , Vladimir Ivanov , Daniel Jönsson , Pia Kahnberg , Peter Lind , Magnus Nilsson , Lourdes Odén , Mikael Pelcman , Horst Wähling
发明人: Susana Ayesa , Anna Karin Belfrage , Björn Classon , Urszula Grabowska , Ellen Hewitt , Vladimir Ivanov , Daniel Jönsson , Pia Kahnberg , Peter Lind , Magnus Nilsson , Lourdes Odén , Mikael Pelcman , Horst Wähling
IPC分类号: A61K31/5377 , C07D265/30 , C07D413/12 , C07D307/68 , C07D405/12 , C07C237/52 , C07C311/46 , C07C271/24 , A61K31/415 , A61K31/5375 , A61K31/341 , A61K31/18 , A61K31/166 , A61K31/4965 , A61P25/00 , A61P19/02 , A61P11/06 , A61P9/10 , A61P29/00 , A61P11/00 , A61P17/06 , C07D231/40
CPC分类号: C07C311/21 , C07C237/24 , C07C271/24 , C07C2601/02 , C07C2601/04 , C07C2601/06 , C07C2601/08 , C07D207/34 , C07D213/40 , C07D213/71 , C07D231/14 , C07D231/40 , C07D239/80 , C07D241/24 , C07D277/36 , C07D277/56 , C07D295/215 , C07D307/68 , C07D307/85 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12
摘要: Compounds of the formula I whereinR1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; orR1a and R1b together define a saturated cyclic amine with 3-6 ring atoms;R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; orR2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl;R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl,R4 is Het, Carbocyclyl,optionally substituted as defined in the specification and pharmaceutically acceptable salts,hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain
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是H,卤素,C1-C4烷基,C1-C4卤代烷基,C1-C4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; R3是支链C 5 -C 10烷基链,C 2 -C 4卤代烷基或C 3 -C 7环烷基甲基,R 4是Het,碳环基,如本说明书中所定义的任选取代,及其药学上可接受的盐,水合物和N-氧化物; 是组织蛋白酶S的抑制剂,并且可用于治疗牛皮癣,自身免疫性疾病和其它疾病如哮喘,动脉硬化,COPD和慢性疼痛
-
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。
-
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。
-
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。
-
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。
-
公开(公告)号:US20050112660A1
公开(公告)日:2005-05-26
申请号:US10975979
申请日:2004-10-28
申请人: Gabriel Vogeli , Peter Lind , Luis Parodi , Linda Wood , Ronald Hiebsch
发明人: Gabriel Vogeli , Peter Lind , Luis Parodi , Linda Wood , Ronald Hiebsch
CPC分类号: C07H21/04 , A61K39/00 , C07K14/723
摘要: The present invention provides a gene encoding a G protein-coupled receptor termed nGPCR-x; constructs and recombinant host cells incorporating the genes; the nGPCR-x polypeptides encoded by the gene; antibodies to the nGPCR-x polypeptides; and methods of making and using all of the foregoing.
摘要翻译: 本发明提供编码称为nGPCR-x的G蛋白偶联受体的基因; 构建体和掺入该基因的重组宿主细胞; 由该基因编码的nGPCR-x多肽; 针对nGPCR-x多肽的抗体; 以及制作和使用上述所有方法。
-
公开(公告)号:US20180056122A1
公开(公告)日:2018-03-01
申请号:US15597027
申请日:2017-05-16
申请人: Peter Lind
发明人: Peter Lind
IPC分类号: A63B23/035 , A63B21/00 , A63B21/008 , A63B21/02 , A63B22/00 , A63B21/012
CPC分类号: A63B23/03575 , A63B21/00069 , A63B21/005 , A63B21/0083 , A63B21/0087 , A63B21/012 , A63B21/02 , A63B21/023 , A63B21/154 , A63B21/4015 , A63B21/4029 , A63B21/4034 , A63B21/4035 , A63B21/4037 , A63B21/4043 , A63B21/4047 , A63B21/4049 , A63B22/0012 , A63B23/03541 , A63B23/0405 , A63B23/1209 , A63B2210/50 , A63B2225/09 , A63B2225/093 , A63B2225/10 , A63B2230/06 , A63B2230/207 , A63B2230/30 , A63B2230/50
摘要: A rehabilitative and/or exercise machine that has a frame with attachments to multiple independent bidirectional resistance devices (pneumatic, hydraulic, spring actuated, pulley system, cam, or any other resistance devices) used by the arms and/or legs to provide resistance against movement of the user's appendages in two substantially opposed directions. The resistance devices may have a mechanism such as one or more valves, brakes, springs, or the like that control bi-directional resistance. The action of the arms and/or legs in bi-directional resistance offers near full body exercise of the agonist/antagonist muscles using flexion and extension action of the larger muscle groups in a gait pattern, simultaneously. Hand engaging members attach to the arm resistance devices and foot engaging members attach to the leg resistance devices. The unit may include an attached inclined backboard, mat, bench, or cushion to fully or partially support the user, such as for the user to sit or lay on. The unit may have separate adjustment mechanisms for adjusting the height and/or length of the various portions of the unit to adjust the range of motion of the appendages. The unit may have devices to monitor pulse, oxygen flow and other vital signs.
-
公开(公告)号:US11369841B2
公开(公告)日:2022-06-28
申请号:US16390867
申请日:2019-04-22
申请人: Peter Lind , Kenneth Courian , Andrew Sorg
发明人: Peter Lind , Kenneth Courian , Andrew Sorg
IPC分类号: A63B23/035 , A63B21/005 , A63B21/00 , A63B21/008
摘要: An exercise apparatus having a frame with attachments to multiple independent bidirectional resistance devices used by arms and/or legs of a user to provide resistance against movement of the user's appendages in two substantially opposed directions. The resistance devices may have a mechanism to control bi-directional resistance. The movement of the user's appendages in bi-directional resistance offers near full body exercise of agonist/antagonist muscles using flexion and extension action of larger muscle groups in a gait pattern, simultaneously. Hand engaging members attach to arm resistance devices and foot engaging members attach to leg resistance devices. The exercise apparatus may include an attached inclined backboard, mat, bench, or cushion to fully or partially support the user. The exercise apparatus may have separate height and/or length adjustment mechanisms for adjusting a range of motion of the user's appendages.
-
公开(公告)号:US20200330821A1
公开(公告)日:2020-10-22
申请号:US16390867
申请日:2019-04-22
申请人: Peter Lind , Kenneth Courian , Andrew Sorg
发明人: Peter Lind , Kenneth Courian , Andrew Sorg
IPC分类号: A63B23/035 , A63B21/005 , A63B21/00 , A63B21/008
摘要: A rehabilitative and/or exercise machine that has a frame with attachments to multiple independent bidirectional resistance devices (pneumatic, hydraulic, spring actuated, pulley system, cam, or any other resistance devices) used by the arms and/or legs to provide resistance against movement of the user's appendages in two substantially opposed directions. The resistance devices may have a mechanism such as one or more valves, brakes, springs, or the like that control bi-directional resistance. The action of the arms and/or legs in bi-directional resistance offers near full body exercise of the agonist/antagonist muscles using flexion and extension action of the larger muscle groups in a gait pattern, simultaneously. Hand engaging members attach to the arm resistance devices and foot engaging members attach to the leg resistance devices. The unit may include an attached inclined backboard, mat, bench, or cushion to fully or partially support the user, such as for the user to sit or lay on. The unit may have separate adjustment mechanisms for adjusting the height and/or length of the various portions of the unit to adjust the range of motion of the appendages. The unit may have devices to monitor pulse, oxygen flow and other vital signs.
-
-
-
-
-
-
-
-
-