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1. 发明申请

US20170166538A1 PROTEASE INHIBITORS 审中-公开
公开(公告)号：US20170166538A1
公开(公告)日：2017-06-15
申请号：US15247804
申请日：2016-08-25
申请人： MEDIVIR AB
发明人： Lourdes Salvador ODEN , Magnus NILSSON , PIA KAHNBERG , Bertil SAMUELSSON , Urszula GRABOWSKA
IPC分类号： C07D277/40
CPC分类号： C07D277/40 , C07D491/048 , C07D495/04
摘要： Compounds of the formula wherein R1 and R2 are independently H, F or CH3 ; or R1 forms an ethynyl bond and R2 is H or C3-C8 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-C8 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 subsituted 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 NR8, provided at least one of A1 and A2 comprises N; R6 is H, C-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4 alkoxy 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:

2. 发明申请

US20140221654A1 PROTEASE INHIBITORS 有权
标题翻译： PROTEASE抑制剂
公开(公告)号：US20140221654A1
公开(公告)日：2014-08-07
申请号：US14249332
申请日：2014-04-09
申请人： MEDIVIR AB
发明人： Lourdes Salvador ODEN , Magnus NILSSON , Pia KAHNBERG , Bertil SAMUELSSON , Urszula GRABOWSKA
IPC分类号： C07D491/048
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-C4 alkoxy 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独立地为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。

3. 发明申请

US20130231349A1 PROTEASE INHIBITORS 有权
标题翻译： PROTEASE抑制剂
公开(公告)号：US20130231349A1
公开(公告)日：2013-09-05
申请号：US13831267
申请日：2013-03-14
申请人： MEDIVIR AB
发明人： Lourdes Salvador ODEN , Magnus NILSSON , Pia KAHNBERG , Bertil SAMUELSSON , Urszula GRABOWSKA
IPC分类号： C07D495/04
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独立地为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，可用于治疗特征为组织蛋白酶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。

4. 发明申请

US20210017140A1 PROTEASE INHIBITORS 有权
公开(公告)号：US20210017140A1
公开(公告)日：2021-01-21
申请号：US16940067
申请日：2020-07-27
申请人： MEDIVIR AB
发明人： Lourdes Salvador ODEN , Magnus NILSSON , Pia KAHNBERG , Bertil SAMUELSSON , Urszula GRABOWSKA
IPC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-C4 alkoxy 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.

5. 发明申请

US20170334867A1 PROTEASE INHIBITORS 审中-公开
公开(公告)号：US20170334867A1
公开(公告)日：2017-11-23
申请号：US15667292
申请日：2017-08-02
申请人： MEDIVIR AB
发明人： Lourdes Salvador ODEN , Magnus NILSSON , Pia KAHNBERG , Bertil SAMUELSSON , Urszula GRABOWSKA
IPC分类号： C07D277/40
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; Al is CH or N, A2 is CR6R7 or NR6, provided at least one of Aland 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-C4 alkoxy 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.

6. 发明申请

US20220332690A1 PROTEASE INHIBITORS 有权
公开(公告)号：US20220332690A1
公开(公告)日：2022-10-20
申请号：US17728943
申请日：2022-04-25
申请人： MEDIVIR AB
发明人： Lourdes Salvador ODEN , Magnus NILSSON , Pia KAHNBERG , Bertil SAMUELSSON , Urszula GRABOWSKA
IPC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 subsituted 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-C4 alkoxy 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.

7. 发明申请

US20180327371A1 PROTEASE INHIBITORS 审中-公开
公开(公告)号：US20180327371A1
公开(公告)日：2018-11-15
申请号：US15941947
申请日：2018-03-30
申请人： MEDIVIR AB
发明人： Lourdes Salvador ODEN , Magnus NILSSON , Pia KAHNBERG , Bertil SAMUELSSON , Urszula GRABOWSKA
IPC分类号： C07D277/40 , C07D495/04 , C07D491/048
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-C4 alkoxy 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.

8. 发明申请

US20200010434A1 PROTEASE INHIBITORS 审中-公开
公开(公告)号：US20200010434A1
公开(公告)日：2020-01-09
申请号：US16449850
申请日：2019-06-24
申请人： MEDIVIR AB
发明人： Lourdes Salvador ODEN , Magnus NILSSON , Pia KAHNBERG , Bertil SAMUELSSON , Urszula GRABOWSKA
IPC分类号： C07D277/40 , C07D495/04 , C07D491/048
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 subsituted 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.

9. 发明申请

US20160194334A1 FORM 2 CRYSTALLINE POLYMORPH OF A SALT OF N-[1-6-(ETHYNYL-3-OXO-HEXAHYDRO-FURO[3,2-B]PYRROLE-4-CARBONYL)-3-METHYL-BUTYL]-4-[5-FLUORO-2-(4-METHYL-PIPERAZINYL)THIAZOL-4-YL]-BENZAMIDE USEFUL AS CYSTEINE PROTEASE INHIBITOR 有权
标题翻译： N- [1-6-（乙基-3-氧代 - 十六氢 - 呋喃并[3,2-b]吡咯-4-羰基）-3-甲基 - 丁基] -4- [5 - 氟代-2-（4-甲基 - 哌嗪基）噻唑-4-基] - 苯甲酰胺有效用作CYSTEINE PROTEASE抑制剂
公开(公告)号：US20160194334A1
公开(公告)日：2016-07-07
申请号：US14911992
申请日：2014-08-13
申请人： MEDIVIR AB
发明人： Urszula GRABOWSKA , Lourdes Salvador ODEN , Victor M. DIAZ PEREZ , Andrew CARR
IPC分类号： C07D491/048 , A61K31/496 , A61K45/06 , A61K9/00
CPC分类号： C07D491/048 , A61K9/0019 , A61K9/0053 , A61K31/496 , A61K45/06 , C07B2200/13
摘要： There is provided Form 2 crystalline polymorph consisting of N-[1-6-(ethynyl-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[5-fluoro-2-(4-methyl-piperazin-1-yl)thiazol-4-yl]-benzamide monohydrochloride and N-[1-6-(ethynyl-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[5-fluoro-2-(4-methyl-piperazin-1-yl)thiazol-4-yl]benzamide hydrate monohydrochloride, its use as a medicament and methods for its preparation.
摘要翻译：提供由N- [1-6-（乙炔基-3-氧代 - 六氢 - 呋喃并[3,2-b]吡咯-4-羰基）-3-甲基 - 丁基] -4- [ 5-氟-2-（4-甲基 - 哌嗪-1-基）噻唑-4-基] - 苯甲酰胺一盐酸盐和N- [1-6-（乙炔基-3-氧代 - 六氢 - 呋喃并[3,2-b ]吡咯-4-羰基）-3-甲基 - 丁基] -4- [5-氟-2-（4-甲基 - 哌嗪-1-基）噻唑-4-基]苯甲酰胺水合物一盐酸盐，其用作药物及其制备方法。

10. 发明申请

US20160068539A1 PROTEASE INHIBITORS 有权
标题翻译： PROTEASE抑制剂
公开(公告)号：US20160068539A1
公开(公告)日：2016-03-10
申请号：US14940817
申请日：2015-11-13
申请人： MEDIVIR AB
发明人： Lourdes Salvador ODEN , Magnus NILSSON , Pia KAHNBERG , Bertil SAMUELSSON , Urszula GRABOWSKA
IPC分类号： C07D491/048
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-C4 alkoxy 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独立地为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。

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