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公开(公告)号:US07381734B2
公开(公告)日:2008-06-03
申请号:US11186870
申请日:2005-07-22
申请人: Sarah Elizabeth Lively , Bohdan Waszkowycz , Martin James Harrison , Christopher Neil Farthing , Keith Michael Johnson
发明人: Sarah Elizabeth Lively , Bohdan Waszkowycz , Martin James Harrison , Christopher Neil Farthing , Keith Michael Johnson
IPC分类号: A61K31/445 , A61K31/381 , A61K31/428 , C07D211/08 , C07D211/20 , C07D333/56 , C07D277/30 , C07D277/82 , C07D333/68 , C07D401/12 , C07D417/12 , C07C233/00
CPC分类号: C07D417/12 , A61K31/165 , A61K31/277 , A61K31/381 , A61K31/426 , C07C237/22 , C07C255/58 , C07C271/22 , C07C271/66 , C07C2601/08 , C07D209/08 , C07D209/12 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/55 , C07D215/38 , C07D233/24 , C07D277/30 , C07D277/40 , C07D277/46 , C07D277/54 , C07D277/82 , C07D295/135 , C07D295/185 , C07D307/54 , C07D307/81 , C07D317/46 , C07D317/60 , C07D333/38 , C07D333/60 , C07D333/66 , C07D333/68 , C07D401/06 , C07D401/12 , C07D403/06 , C07D409/06 , C07D417/06
摘要: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
摘要翻译: 其中R 5,R 6a,各X,L,Cy和Lp的式(I)化合物如说明书中所定义,是可用作抗炎剂的类胰蛋白酶抑制剂。
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公开(公告)号:US07074934B2
公开(公告)日:2006-07-11
申请号:US10296245
申请日:2001-06-12
申请人: Sarah Elizabeth Lively , Bohdan Waszkowycz , Martin James Harrison , Christopher Neil Farthing , Keith Michael Johnson
发明人: Sarah Elizabeth Lively , Bohdan Waszkowycz , Martin James Harrison , Christopher Neil Farthing , Keith Michael Johnson
IPC分类号: C07D211/08 , C07D211/20 , C07D333/56 , C07C233/00 , A61K31/445
CPC分类号: C07D417/12 , A61K31/165 , A61K31/277 , A61K31/381 , A61K31/426 , C07C237/22 , C07C255/58 , C07C271/22 , C07C271/66 , C07C2601/08 , C07D209/08 , C07D209/12 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/55 , C07D215/38 , C07D233/24 , C07D277/30 , C07D277/40 , C07D277/46 , C07D277/54 , C07D277/82 , C07D295/135 , C07D295/185 , C07D307/54 , C07D307/81 , C07D317/46 , C07D317/60 , C07D333/38 , C07D333/60 , C07D333/66 , C07D333/68 , C07D401/06 , C07D401/12 , C07D403/06 , C07D409/06 , C07D417/06
摘要: Compounds of formula (I) where R2, each X, L, Y, Cy, Lp, D and n are as defined in the specification, are serine protease inhibitors useful as antithrombotic agents.
摘要翻译: 其中R 2,X,L,Y,Cy,Lp,D和n如说明书中所定义的式(I)化合物是用作抗血栓形成剂的丝氨酸蛋白酶抑制剂。
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公开(公告)号:US06916957B2
公开(公告)日:2005-07-12
申请号:US10148174
申请日:2000-12-13
申请人: Sarah Elizabeth Lively , Bohdan Waszkowycz , Martin James Harrison , Christopher Neil Farthing , Keith Michael Johnson
发明人: Sarah Elizabeth Lively , Bohdan Waszkowycz , Martin James Harrison , Christopher Neil Farthing , Keith Michael Johnson
IPC分类号: C07C237/36 , C07C237/42 , C07C255/60 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/53 , C07D213/56 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/82 , C07D215/38 , C07D217/04 , C07D217/06 , C07D231/56 , C07D233/54 , C07D235/06 , C07D241/24 , C07D273/00 , C07D277/28 , C07D277/30 , C07D277/40 , C07D277/46 , C07D277/52 , C07D277/64 , C07D277/68 , C07D277/82 , C07D295/135 , C07D295/185 , C07D307/54 , C07D307/79 , C07D317/68 , C07D333/36 , C07D333/38 , C07D333/60 , C07D333/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/06 , C07D417/12 , C07D487/04 , C07C233/64 , A61K31/16
CPC分类号: C07D217/04 , C07B2200/07 , C07C237/36 , C07C237/42 , C07C255/60 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/53 , C07D213/56 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/82 , C07D215/38 , C07D217/06 , C07D231/56 , C07D233/64 , C07D235/06 , C07D241/24 , C07D273/00 , C07D277/28 , C07D277/30 , C07D277/40 , C07D277/46 , C07D277/52 , C07D277/64 , C07D277/68 , C07D277/82 , C07D295/135 , C07D295/185 , C07D307/54 , C07D307/79 , C07D317/68 , C07D333/36 , C07D333/38 , C07D333/60 , C07D333/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/06 , C07D417/12 , C07D487/04
摘要: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
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公开(公告)号:US07157585B2
公开(公告)日:2007-01-02
申请号:US11126309
申请日:2005-05-11
申请人: Sarah Elizabeth Lively , Bohdan Waszkowycz , Martin James Harrison , Christopher Neil Farthing , Keith Michael Johnson
发明人: Sarah Elizabeth Lively , Bohdan Waszkowycz , Martin James Harrison , Christopher Neil Farthing , Keith Michael Johnson
IPC分类号: C07D277/62 , A61K31/425 , C07C233/64 , A61K31/16
CPC分类号: C07D217/04 , C07B2200/07 , C07C237/36 , C07C237/42 , C07C255/60 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/53 , C07D213/56 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/82 , C07D215/38 , C07D217/06 , C07D231/56 , C07D233/64 , C07D235/06 , C07D241/24 , C07D273/00 , C07D277/28 , C07D277/30 , C07D277/40 , C07D277/46 , C07D277/52 , C07D277/64 , C07D277/68 , C07D277/82 , C07D295/135 , C07D295/185 , C07D307/54 , C07D307/79 , C07D317/68 , C07D333/36 , C07D333/38 , C07D333/60 , C07D333/68 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/06 , C07D417/12 , C07D487/04
摘要: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
摘要翻译: 其中R 5,R 6a,各X,L,Cy和Lp的式(I)化合物如说明书中所定义,是可用作抗炎剂的类胰蛋白酶抑制剂。
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公开(公告)号:US07067516B2
公开(公告)日:2006-06-27
申请号:US10432365
申请日:2001-12-12
申请人: Sarah Elizabeth Lively , Martin James Harrison , Neil Jason Naylor , Christopher Neil Farthing , Bohdan Waszkowycz
发明人: Sarah Elizabeth Lively , Martin James Harrison , Neil Jason Naylor , Christopher Neil Farthing , Bohdan Waszkowycz
IPC分类号: A61K31/381 , A61K31/428 , C07D277/30 , C07D277/82 , C07D333/68 , C07D401/12 , C07D417/12
CPC分类号: C07D273/00 , A61K31/381 , A61K31/428 , C07B2200/07 , C07C237/42 , C07C2601/14 , C07C2602/08 , C07D209/08 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/56 , C07D213/61 , C07D213/73 , C07D233/64 , C07D277/30 , C07D277/40 , C07D277/46 , C07D277/52 , C07D277/68 , C07D277/82 , C07D307/54 , C07D307/79 , C07D333/36 , C07D333/60 , C07D333/66 , C07D333/68 , C07D333/78 , C07D401/12 , C07D409/04 , C07D409/12 , C07D417/12 , C07D417/14 , C07D495/04
摘要: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
摘要翻译: 其中R 5,R 6a,各X,L,Cy和Lp的式(I)化合物如说明书中所定义,是可用作抗炎剂的类胰蛋白酶抑制剂。
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公开(公告)号:US20120190672A1
公开(公告)日:2012-07-26
申请号:US13354716
申请日:2012-01-20
IPC分类号: A61K31/542 , A61P25/28 , A61P3/10 , C07D513/04
CPC分类号: C07D513/04
摘要: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C≡N; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
摘要翻译: 本发明涉及式(I)的稠合氨基二氢噻嗪衍生物:其中X是氢或氟; A是CH或N; Y是甲基,乙基,一氟甲基,二氟甲基,三氟甲基,二氟乙基,甲氧基,乙氧基,甲氧基甲基或-C≡N; 及其药学上可接受的盐; 该化合物具有A&bgr; 产生抑制作用或BACE1抑制作用,可用作由A&Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。
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公开(公告)号:US09079914B2
公开(公告)日:2015-07-14
申请号:US13386092
申请日:2010-07-21
IPC分类号: C07D498/04 , A61K31/5365
CPC分类号: C07D498/04
摘要: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
摘要翻译: 由通式表示的化合物或其药学上可接受的盐或其溶剂化物,其中环A是C 6-14芳基等,L是-NReCO-等(其中Re是氢原子或 环)B是C 6-14芳基等,X是C 1-3亚烷基等,Y是单键等,Z是C 1-3亚烷基等,R 1 和R 2各自独立地为氢原子等,R 3,R 4,R 5和R 6独立地为氢原子,卤素原子等,具有A&bgr; 产生抑制作用或BACE1抑制作用,可用作由A&Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。
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8.
公开(公告)号:US07951802B2
公开(公告)日:2011-05-31
申请号:US12536354
申请日:2009-08-05
申请人: Piotr Pawel Graczyk , Paschalis Dimopoulos , Christopher Neil Farthing , Gurpreet Singh Bhatia , Afzal Khan
发明人: Piotr Pawel Graczyk , Paschalis Dimopoulos , Christopher Neil Farthing , Gurpreet Singh Bhatia , Afzal Khan
IPC分类号: A61K31/535 , A61K31/497 , A61K31/44 , C07D413/14 , C07D401/14 , C07D471/04
CPC分类号: C07D471/04
摘要: The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them.
摘要翻译: 本发明提供式(I)的化合物; 或其药学上可接受的盐在抑制c-Jun N-末端激酶(JNK)活性,特别是在治疗神经变性疾病,炎性疾病和/或自身免疫疾病中。 本发明还提供了制备式(I)化合物或其药学上可接受的盐和含有它们的组合物的方法。
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公开(公告)号:US20120202804A1
公开(公告)日:2012-08-09
申请号:US13386092
申请日:2010-07-21
IPC分类号: A61K31/5365 , A61P25/28 , C07D498/04
CPC分类号: C07D498/04
摘要: A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
摘要翻译: 由通式(I)表示的化合物或其药学上可接受的盐或其溶剂合物,其中环A为C 6-14芳基等,L为-NReCO-等(其中Re为氢原子 等),环B为C 6-14芳基等,X为C 1-3亚烷基等,Y为单键等,Z为C1-3亚烷基等 R 1和R 2各自独立地为氢原子等,R 3,R 4,R 5和R 6独立地为氢原子,卤素原子等,具有A&bgr; 产生抑制作用或BACE1抑制作用,可用作由A&Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。
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公开(公告)号:US08338407B2
公开(公告)日:2012-12-25
申请号:US13354716
申请日:2012-01-20
IPC分类号: C07D513/04 , A61K31/542
CPC分类号: C07D513/04
摘要: The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C≡N; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
摘要翻译: 本发明涉及式(I)的稠合氨基二氢噻嗪衍生物:其中X是氢或氟; A是CH或N; Y是甲基,乙基,一氟甲基,二氟甲基,三氟甲基,二氟乙基,甲氧基,乙氧基,甲氧基甲基或-C≡N; 及其药学上可接受的盐; 该化合物具有A&bgr; 产生抑制作用或BACE1抑制作用,可用作由A&Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。
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