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1. 发明授权

US08198283B2 Cysteine protease inhibitors 有权
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US08198283B2
公开(公告)日：2012-06-12
申请号：US12986830
申请日：2011-01-07
申请人： Magnus Nilsson , Lourdes Salvador Oden , Pia Kahnberg , Urszula Grabowska
发明人： Magnus Nilsson , Lourdes Salvador Oden , Pia Kahnberg , Urszula Grabowska
IPC分类号： A61K31/496 , A61K31/407 , C07D491/04
CPC分类号： C07D491/048
摘要： Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq′ is H or Rq and Rq′ define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl-moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R2是亮氨酸的侧链，异亮氨酸，环己基甘氨酸，O-甲基苏氨酸，4-氟亮氨酸或3-甲氧基缬氨酸; R3是H，甲基或F; Rq是三氟甲基，Rq'是H或Rq，Rq'定义酮基; Q是对 - （C 1 -C 6烷基磺酰基）苯基 - 或任选取代的4-（C 1 -C 6烷基）哌嗪-1-基 - 噻唑-4-基 - 部分可用于治疗以不适当表达或活化为特征的疾病组织蛋白酶K，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

2. 发明授权

US08853281B2 Cysteine protease inhibitors 有权
标题翻译：半胱氨酸蛋白酶抑制剂
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。

3. 发明授权

US08466158B2 Cysteine protease inhibitors 有权
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US08466158B2
公开(公告)日：2013-06-18
申请号：US13468787
申请日：2012-05-10
申请人： Magnus Nilsson , Lourdes Salvador Odén , Pia Kahnberg , Urszula Grabowska
发明人： Magnus Nilsson , Lourdes Salvador Odén , Pia Kahnberg , Urszula Grabowska
IPC分类号： A61K31/496
CPC分类号： C07D491/048
摘要： Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq′ is H or Rq and Rq′ define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl-moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R2是亮氨酸的侧链，异亮氨酸，环己基甘氨酸，O-甲基苏氨酸，4-氟亮氨酸或3-甲氧基缬氨酸; R3是H，甲基或F; Rq是三氟甲基，Rq'是H或Rq，Rq'定义酮基; Q是对 - （C 1 -C 6烷基磺酰基）苯基 - 或任选取代的4-（C 1 -C 6烷基）哌嗪-1-基 - 噻唑-4-基 - 部分可用于治疗以不适当表达或活化为特征的疾病组织蛋白酶K，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

4. 发明申请

US20120289519A1 PROTEASE INHIBITORS 有权
标题翻译： PROTEASE抑制剂
公开(公告)号：US20120289519A1
公开(公告)日：2012-11-15
申请号：US13541519
申请日：2012-07-03
申请人： Lourdes Salvador ODÉN , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
发明人： Lourdes Salvador ODÉN , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
IPC分类号： A61K31/496 , A61P19/02
CPC分类号： C07D277/40 , C07D491/048 , C07D495/04
摘要： Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or optionally substituted C3-C6 cycloalkyl; R3 is (optionally substituted) C1-C3 alkyl or C3-C6 cycloalkyl; R4 is methyl or fluoro; m is 0-2; E is optionally substituted thiazolyl; A1 and A2 together define an optionally substituted piperazine or piperidine ring have utility in the treatment of osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R 1和R 2独立地是H，F或CH 3; 或R 1形成乙炔基，R 2为H或任选取代的C 3 -C 6环烷基; R3是（任选取代的）C 1 -C 3烷基或C 3 -C 6环烷基; R4是甲基或氟; m为0-2; E是任选取代的噻唑基; A1和A2一起限定任选取代的哌嗪或哌啶环可用于治疗骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

5. 发明授权

US07893067B2 Cysteine protease inhibitors 有权
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US07893067B2
公开(公告)日：2011-02-22
申请号：US12145987
申请日：2008-06-25
申请人： Magnus Nilsson , Lourdes Oden , Pia Kahnberg , Urszula Grabowska
发明人： Magnus Nilsson , Lourdes Oden , Pia Kahnberg , Urszula Grabowska
IPC分类号： A61K31/407 , C07D491/04
CPC分类号： C07D491/048
摘要： Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq′ is H or Rq and Rq′ define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl- moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R2是亮氨酸的侧链，异亮氨酸，环己基甘氨酸，O-甲基苏氨酸，4-氟亮氨酸或3-甲氧基缬氨酸; R3是H，甲基或F; Rq是三氟甲基，Rq'是H或Rq，Rq'定义酮基; Q是对（C 1 -C 6烷基磺酰基）苯基 - 或任选取代的4-（C 1 -C 6烷基）哌嗪-1-基 - 噻唑-4-基 - 部分可用于治疗以不适当表达或活化为特征的疾病组织蛋白酶K，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

6. 发明申请

US20110039862A1 Protease Inhibitors 有权
标题翻译：蛋白酶抑制剂
公开(公告)号：US20110039862A1
公开(公告)日：2011-02-17
申请号：US12739489
申请日：2009-09-24
申请人： Lourdes Salvadore Odén , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
发明人： Lourdes Salvadore Odén , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
IPC分类号： A61K31/496 , C07D491/048 , A61P19/10 , A61P1/02 , A61P35/00 , A61P29/00 , A61P19/02 , A61P19/08 , A61P7/00
CPC分类号： C07D277/40 , C07D491/048 , C07D495/04
摘要： Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R 1和R 2独立地是H，F或CH 3; 或R1形成乙炔基，R2是H或C3-C6环烷基，其任选地被一个或两个独立地选自甲基，CF 3，OMe或卤素的取代基取代; R 3是C 1 -C 3烷基或C 3 -C 6环烷基，当R 3是C 3 -C 6环烷基时，它们任选被一个或两个甲基和/或氟，三氟甲基或甲氧基取代，也可以被氟取代; R4是甲基或氟; m为0,1或2; E是任选被甲基或氟取代的键或噻唑基; A1是CH或N，A2是CR6R7或NR6，条件是A1和A2中的至少一个包括N; R6是H，C1-C4烷基，C1-C4卤代烷基，C1-C3烷基-O-C1-C3烷基，或当A2是C时，R6也可以是C1-C4烷氧基或F; R7是H，C1-C4烷基或F或其药学上可接受的盐，N-氧化物或其水合物，可用于治疗组织蛋白酶K不适当表达或活化的疾病，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨骼转移。

7. 发明申请

US20120220602A1 CYSTEINE PROTEASE INHIBITORS 有权
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：US20120220602A1
公开(公告)日：2012-08-30
申请号：US13468787
申请日：2012-05-10
申请人： Magnus Nilsson , Lourdes Oden , Pia Kahnberg , Urszula Grabowska
发明人： Magnus Nilsson , Lourdes Oden , Pia Kahnberg , Urszula Grabowska
IPC分类号： A61K31/496 , A61K31/407 , A61P1/02 , A61P29/00 , A61P35/00 , A61P3/00 , A61P19/02 , C07D491/048 , A61P19/08
CPC分类号： C07D491/048
摘要： Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq′ is H or Rq and Rq′ define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl- moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R2是亮氨酸的侧链，异亮氨酸，环己基甘氨酸，O-甲基苏氨酸，4-氟亮氨酸或3-甲氧基缬氨酸; R3是H，甲基或F; Rq是三氟甲基，Rq'是H或Rq，Rq'定义酮基; Q是对（C 1 -C 6烷基磺酰基）苯基 - 或任选取代的4-（C 1 -C 6烷基）哌嗪-1-基 - 噻唑-4-基 - 部分可用于治疗以不适当表达或活化为特征的疾病组织蛋白酶K，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

8. 发明申请

US20110312964A1 CYSTEINE PROTEASE INHIBITORS 有权
标题翻译： CYSTEINE PROTEASE抑制剂
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

9. 发明申请

US20110105524A1 CYSTEINE PROTEASE INHIBITORS 有权
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：US20110105524A1
公开(公告)日：2011-05-05
申请号：US12986830
申请日：2011-01-07
申请人： Magnus NILSSON , Lourdes Oden , Pia Kahnberg , Urszula Grabowska
发明人： Magnus NILSSON , Lourdes Oden , Pia Kahnberg , Urszula Grabowska
IPC分类号： A61K31/497 , C07D413/14 , A61P1/02 , A61P35/00 , A61P25/00
CPC分类号： C07D491/048
摘要： Compounds of the formula II: wherein R2 is the side chain of leucine, isoleucine, cyclohexylglycine, O-methyl threonine, 4-fluoroleucine or 3-methoxyvaline; R3 is H, methyl or F; Rq is trifluoromethyl and Rq′ is H or Rq and Rq′ define keto; Q is a p-(C1-C6alkylsulphonyl)phenyl- or an optionally substituted 4-(C1-C6alkyl)piperazin-1-yl-thiazol-4-yl-moiety have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R2是亮氨酸的侧链，异亮氨酸，环己基甘氨酸，O-甲基苏氨酸，4-氟亮氨酸或3-甲氧基缬氨酸; R3是H，甲基或F; Rq是三氟甲基，Rq'是H或Rq，Rq'定义酮基; Q是对 - （C 1 -C 6烷基磺酰基）苯基 - 或任选取代的4-（C 1 -C 6烷基）哌嗪-1-基 - 噻唑-4-基 - 部分可用于治疗以不适当表达或活化为特征的疾病组织蛋白酶K，例如骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

10. 发明授权

US08426421B2 Protease inhibitors 有权
标题翻译：蛋白酶抑制剂
公开(公告)号：US08426421B2
公开(公告)日：2013-04-23
申请号：US13541519
申请日：2012-07-03
申请人： Lourdes Salvador Odén , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
发明人： Lourdes Salvador Odén , Magnus Nilsson , Pia Kahnberg , Bertil Samuelsson , Urszula Grabowska
IPC分类号： A61K31/496
CPC分类号： C07D277/40 , C07D491/048 , C07D495/04
摘要： Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or optionally substituted C3-C6 cycloalkyl; R3 is (optionally substituted) C1-C3 alkyl or C3-C6 cycloalkyl; R4 is methyl or fluoro; m is 0-2; E is optionally substituted thiazolyl; A1 and A2 together define an optionally substituted piperazine or piperidine ring have utility in the treatment of osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
摘要翻译：式II化合物：其中R 1和R 2独立地为H，F或CH 3; 或R 1形成乙炔基，R 2为H或任选取代的C 3 -C 6环烷基; R 3是（任选取代的）C 1 -C 3烷基或C 3 -C 6环烷基; R4是甲基或氟; m为0-2; E是任选取代的噻唑基; A1和A2一起限定任选取代的哌嗪或哌啶环可用于治疗骨质疏松症，骨关节炎，类风湿性关节炎或骨转移。

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