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1. 发明授权

US07067516B2 Serine protease inhibitors 失效
标题翻译：丝氨酸蛋白酶抑制剂
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。

2. 发明授权

US07381734B2 Serine protease inhibitors 失效
标题翻译：丝氨酸蛋白酶抑制剂
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。

3. 发明授权

US07074934B2 Serine protease inhibitors 失效
标题翻译：丝氨酸蛋白酶抑制剂
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。

5. 发明授权

US07157585B2 Serine protease inhibitors 失效
标题翻译：丝氨酸蛋白酶抑制剂
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。

6. 发明申请

US20120190672A1 FUSED AMINODIHYDROTHIAZINE DERIVATIVES 有权
标题翻译：熔融氨基二氢卟吩衍生物
公开(公告)号：US20120190672A1
公开(公告)日：2012-07-26
申请号：US13354716
申请日：2012-01-20
申请人： Adrian Hall , Christopher Neil Farthing , Jose Luis Castro Pineiro
发明人： Adrian Hall , Christopher Neil Farthing , Jose Luis Castro Pineiro
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。

7. 发明授权

US09079914B2 Fused aminodihydro-oxazine derivatives 有权
标题翻译：熔融氨基二氢恶嗪衍生物
公开(公告)号：US09079914B2
公开(公告)日：2015-07-14
申请号：US13386092
申请日：2010-07-21
申请人： John Mark Ellard , Christopher Neil Farthing , Adrian Hall
发明人： John Mark Ellard , Christopher Neil Farthing , Adrian Hall
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。

8. 发明授权

US07951802B2 Use of 7-azaindoles in the inhibition of c-Jun N-terminal kinase 有权
标题翻译：使用7-氮杂吲哚抑制c-Jun N-末端激酶
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。

9. 发明申请

US20120202804A1 FUSED AMINODIHYDRO-OXAZINE DERIVATIVES 有权
标题翻译：熔融氨基二氧杂环丁烷衍生物
公开(公告)号：US20120202804A1
公开(公告)日：2012-08-09
申请号：US13386092
申请日：2010-07-21
申请人： John Mark Ellard , Christopher Neil Farthing , Adrian Hall
发明人： John Mark Ellard , Christopher Neil Farthing , Adrian Hall
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。

10. 发明授权

US08338407B2 Fused aminodihydrothiazine derivatives 有权
标题翻译：融合氨基二氢噻嗪衍生物
公开(公告)号：US08338407B2
公开(公告)日：2012-12-25
申请号：US13354716
申请日：2012-01-20
申请人： Adrian Hall , Christopher Neil Farthing
发明人： Adrian Hall , Christopher Neil Farthing
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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