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1. 发明授权

US08158620B2 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：US08158620B2
公开(公告)日：2012-04-17
申请号：US12355154
申请日：2009-01-16
申请人： Yuichi Suzuki , Takafumi Motoki , Toshihiko Kaneko , Mamoru Takaishi , Tasuku Ishida , Kunitoshi Takeda , Yoichi Kita , Noboru Yamamoto , Afzal Khan , Paschalis Dimopoulos
发明人： Yuichi Suzuki , Takafumi Motoki , Toshihiko Kaneko , Mamoru Takaishi , Tasuku Ishida , Kunitoshi Takeda , Yoichi Kita , Noboru Yamamoto , Afzal Khan , Paschalis Dimopoulos
IPC分类号： C07D513/02 , C07D279/08 , A61K31/542
CPC分类号： A61K31/542 , C07D279/08 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
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。

2. 发明申请

US20120094984A1 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：US20120094984A1
公开(公告)日：2012-04-19
申请号：US13333238
申请日：2011-12-21
申请人： Yuichi Suzuki , Takafumi Motoki , Toshihiko Kaneko , Mamoru Takaishi , Tasuku Ishida , Kunitoshi Takeda , Yoichi Kita , Noboru Yamamoto , Afzal Khan , Paschalis Dimopoulos
发明人： Yuichi Suzuki , Takafumi Motoki , Toshihiko Kaneko , Mamoru Takaishi , Tasuku Ishida , Kunitoshi Takeda , Yoichi Kita , Noboru Yamamoto , Afzal Khan , Paschalis Dimopoulos
IPC分类号： A61K31/5415 , A61P25/28 , C07D279/08 , C07D471/04 , C07D417/12 , C07D513/04
CPC分类号： A61K31/542 , C07D279/08 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
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。

3. 发明申请

US20100317850A1 CONDENSED AMINODIHYDROTHIAZINE DERIVATIVE 审中-公开
标题翻译：浓缩氨基二氢吡啶衍生物
公开(公告)号：US20100317850A1
公开(公告)日：2010-12-16
申请号：US12863364
申请日：2009-01-16
申请人： Yuichi Suzuki , Takafumi Motoki , Toshihiko Kaneko , Mamoru Takaishi , Tasuku Ishida , Kunitoshi Takeda , Yoichi Kita , Noboru Yamamoto , Afzal Khan , Paschalis Dimopoulos
发明人： Yuichi Suzuki , Takafumi Motoki , Toshihiko Kaneko , Mamoru Takaishi , Tasuku Ishida , Kunitoshi Takeda , Yoichi Kita , Noboru Yamamoto , Afzal Khan , Paschalis Dimopoulos
IPC分类号： C07D513/04 , C07D417/12
CPC分类号： A61K31/542 , C07D279/08 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
摘要： Disclosed is a compound represented by General formula (I), a pharmaceutically acceptable salt thereof, or a solvate of the compound or the pharmaceutically acceptable salt, which has an inhibitory activity of the production of Aβ or a BACE1-inhibiting activity, and is therefore useful as a prophylactic or therapeutic agent for Aβ-induced neurodegenerative diseases typified by Alzheimer-type dementia. Wherein the ring A represents a C6-14 aryl group or the like; L represents —NReCO— [wherein Re represents a hydrogen atom or the like] or the like; the ring B represents a C6-14 aryl group or the like; X represents a C1-3 alkylene group or the like; Y represents a single bond or the like; Z represents a C1-3 alkylene group or the like; R1 and R2 independently represent a hydrogen atom or the like; and R3, R4, R5 and R6 independently represent a hydrogen atom, a halogen atom or the like.
摘要翻译：公开了通式（I）表示的化合物或其药学上可接受的盐，或该化合物或其药学上可接受的盐的溶剂化物，其具有抑制A＆Bgr生产的活性; 或BACE1抑制活性，因此可用作用于以阿尔茨海默氏型痴呆为代表的引起神经退行性疾病的预防或治疗剂。其中环A表示C6-14芳基等; L表示-NReCO- [其中Re表示氢原子等]等; 环B表示C 6-14芳基等; X表示C1-3亚烷基等; Y表示单键等; Z表示C1-3亚烷基等; R1和R2独立地表示氢原子等; R 3，R 4，R 5和R 6独立地表示氢原子，卤素原子等。

4. 发明授权

US08946210B2 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：US08946210B2
公开(公告)日：2015-02-03
申请号：US13333238
申请日：2011-12-21
申请人： Yuichi Suzuki , Takafumi Motoki , Toshihiko Kaneko , Mamoru Takaishi , Tasuku Ishida , Yoichi Kita , Kunitoshi Takeda , Noboru Yamamoto , Afzal Khan , Paschalis Dimopoulos
发明人： Yuichi Suzuki , Takafumi Motoki , Toshihiko Kaneko , Mamoru Takaishi , Tasuku Ishida , Yoichi Kita , Kunitoshi Takeda , Noboru Yamamoto , Afzal Khan , Paschalis Dimopoulos
IPC分类号： C07D239/14 , A61K31/5415
CPC分类号： A61K31/542 , C07D279/08 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
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。

5. 发明申请

US20100093999A1 NOVEL FUSED AMINODIHYDROTHIAZINE DERIVATIVE 有权
标题翻译：新型融合氨基吡啶衍生物
公开(公告)号：US20100093999A1
公开(公告)日：2010-04-15
申请号：US12568151
申请日：2009-09-28
申请人： Takafumi Motoki , Kunitoshi Takeda , Yoichi Kita , Mamoru Takaishi , Yuichi Suzuki , Tasuku Ishida
发明人： Takafumi Motoki , Kunitoshi Takeda , Yoichi Kita , Mamoru Takaishi , Yuichi Suzuki , Tasuku Ishida
IPC分类号： C07D498/04
CPC分类号： C07D513/04
摘要： A compound represented by the general formula: wherein Ring A is a C6-14 aryl group or the like, L is —NRLCO— or the like (wherein RL 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 C1-3 alkylene group or the like, Z is an oxygen atom 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, or a pharmaceutically acceptable salt thereof, or a solvate thereof, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a 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：其中环A是C 6-14芳基等，L是-NRLCO-等（其中RL是氢原子等），环B是C 6-14芳基基团等，X是C 1-3亚烷基等，Y是C 1-3亚烷基等，Z是氧原子等，R 1和R 2各自独立地是氢原子等，R 3，R 4，R 5和R 6独立地为氢原子，卤素原子等或其药学上可接受的盐或其溶剂合物，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治疗剂; 并以阿尔茨海默氏型痴呆为代表。

6. 发明授权

US08198269B2 Fused aminodihydrothiazine derivative 有权
标题翻译：融合氨基二氢噻嗪衍生物
公开(公告)号：US08198269B2
公开(公告)日：2012-06-12
申请号：US12568151
申请日：2009-09-28
申请人： Takafumi Motoki , Kunitoshi Takeda , Yoichi Kita , Mamoru Takaishi , Yuichi Suzuki , Tasuku Ishida
发明人： Takafumi Motoki , Kunitoshi Takeda , Yoichi Kita , Mamoru Takaishi , Yuichi Suzuki , Tasuku Ishida
IPC分类号： C07D513/04 , C07D239/14 , A61K31/542
CPC分类号： C07D513/04
摘要： A compound represented by the general formula: wherein Ring A is a C6-14 aryl group or the like, L is —NRLCO— or the like (wherein RL 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 C1-3 alkylene group or the like, Z is an oxygen atom 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, or a pharmaceutically acceptable salt thereof, or a solvate thereof, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a 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：其中环A是C 6-14芳基等，L是-NRLCO-等（其中RL是氢原子等），环B是C 6-14芳基基团等，X是C 1-3亚烷基等，Y是C 1-3亚烷基等，Z是氧原子等，R 1和R 2各自独立地是氢原子等，R 3，R 4，R 5和R 6独立地为氢原子，卤素原子等或其药学上可接受的盐或其溶剂合物，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治疗剂; 并以阿尔茨海默氏型痴呆为代表。

7. 发明申请

US20110207723A1 NOVEL FUSED AMINODIHYDROTHIAZINE DERIVATIVE 审中-公开
标题翻译：新型融合氨基吡啶衍生物
公开(公告)号：US20110207723A1
公开(公告)日：2011-08-25
申请号：US13121062
申请日：2009-09-28
申请人： Takafumi Motoki , Kunitoshi Takeda , Yoichi Kita , Mamoru Takaishi , Yuichi Suzuki , Tasuku Ishida
发明人： Takafumi Motoki , Kunitoshi Takeda , Yoichi Kita , Mamoru Takaishi , Yuichi Suzuki , Tasuku Ishida
IPC分类号： A61K31/542 , C07D513/04 , C12N9/99 , A61P25/28
CPC分类号： C07D513/04
摘要： A compound represented by the general formula (I): a pharmaceutically acceptable salt thereof, or a solvate of the compound or salt has an Aβ production inhibitory activity or BACE 1 inhibitory activity, and is thus useful as an agent for treating neurodegenerative diseases caused by Aβ as typified by Alzheimer's disease. In the formula, ring A represents a C6-14 aryl group or the like; L represents —NR1CO— (wherein RL represents a hydrogen atom or the like) or the like; ring B represents a C6-14 aryl group or the like; X represents a C1-3 alkylene group or the like; Y represents a C1-3 alkylene group or the like; Z represents an oxygen atom or the like; R1 and R2 each independently represents a hydrogen atom or the like; and R3, R4, R5 and R6 each independently represents a hydrogen atom, a halogen atom or the like.
摘要翻译：由通式（I）表示的化合物：其药学上可接受的盐或该化合物或其盐的溶剂合物具有A＆bgr; 生产抑制活性或BACE1抑制活性，因此可用作治疗由A＆Bgr引起的神经变性疾病的药剂; 以阿尔茨海默病为代表。在该式中，环A表示C 6-14芳基等; L表示-NR1CO-（其中RL表示氢原子等）等; 环B表示C 6-14芳基等; X表示C1-3亚烷基等; Y表示C1-3亚烷基等; Z表示氧原子等; R1和R2各自独立地表示氢原子等; R 3，R 4，R 5和R 6各自独立地表示氢原子，卤素原子等。

8. 发明授权

US08431603B2 3-phenylpyrazolo[5,1-b]thiazole compounds 有权
标题翻译： 3-苯基吡唑并[5,1-b]噻唑化合物
公开(公告)号：US08431603B2
公开(公告)日：2013-04-30
申请号：US12421182
申请日：2009-04-09
申请人： Hisashi Shibata , Kodo Shikata , Akira Inomata , Kogyoku Shin , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda
发明人： Hisashi Shibata , Kodo Shikata , Akira Inomata , Kogyoku Shin , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda
IPC分类号： A61K31/4439 , C07D513/02
CPC分类号： C07D513/04
摘要： A compound represented by the following formula (I), or salt thereof exhibits excellent CRF receptor antagonism, and sufficient pharmacological activity, safety and pharmacokinetic properties as a drug. wherein R1 represents the formula -A11-A12; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 1,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl having methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine.
摘要翻译：由下式（I）表示的化合物或其盐表现出优异的CRF受体拮抗作用，作为药物具有充分的药理活性，安全性和药代动力学性质。其中R1表示式-A11-A12; R2表示四氢呋喃基甲基，四氢吡喃基甲基或四氢吡喃基; A11表示单键，亚甲基或1,2-亚乙基; A12表示C1-6烷基，C3-6环烷基或具有甲基的C3-6环烷基; R3表示甲氧基，氰基，环丁氧基甲基，甲氧基甲基或乙氧基甲基; R4表示甲氧基或氯。

9. 发明授权

US08530504B2 Pyrazolothiazole compound 失效
标题翻译：吡唑并噻唑化合物
公开(公告)号：US08530504B2
公开(公告)日：2013-09-10
申请号：US12900026
申请日：2010-10-07
申请人： Kogyoku Shin , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda , Kodo Shikata , Akira Inomata
发明人： Kogyoku Shin , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda , Kodo Shikata , Akira Inomata
IPC分类号： A61K31/429 , A61P25/24
CPC分类号： C07D513/04
摘要： A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism wherein X is a nitrogen atom or CH; R1 is -A11-A12; A11 is a single bond or a C1-6 alkylene group; A12 is a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group, etc.; R2 is -A21-A22; A21 is a single bond or a C1-6 alkylene group; A22 is a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a non-aromatic heterocyclic group, or a heteroaryl group, etc.; R3 is a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C3-6 cycloalkoxy C1-6 alkyl group, di-C1-6 alkyl amino group, a halogen atom, a cyano group, a formyl group, or a carboxyl group, etc; R4 is a hydrogen atom or a C1-6 alkoxy group; R5 is a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R6 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylthio group, or a C1-6 alkyl sulfinyl group etc.; and R7 is a C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6 alkylthio group.
摘要翻译：由式（I）表示的化合物或其药理学上可接受的盐表现出优异的CRF受体拮抗作用，其中X为氮原子或CH; R1为-A11-A12; A11是单键或C1-6亚烷基; A12是氢原子，C1-6烷基或C3-6环烷基等; R2为-A21-A22; A21是单键或C1-6亚烷基; A22为氢原子，C1-6烷基，C3-6环烷基，非芳族杂环基或杂芳基等; R3是C1-6烷基，C3-6环烷基，C1-6烷氧基，C3-6环烷氧基C1-6烷基，二C1-6烷基氨基，卤素原子，氰基，甲酰基或羧基等; R4是氢原子或C1-6烷氧基; R5是卤素原子，C1-6烷基或C1-6烷氧基; R6是氢原子，C1-6烷基，C1-6烷氧基，C1-6烷硫基或C1-6烷基亚磺酰基等; 且R 7为C 1-6烷基，C 1-6烷氧基或C 1-6烷硫基。

10. 发明申请

US20110086898A1 PYRAZOLOOXAZOLE COMPOUND 审中-公开
标题翻译：吡唑并噻唑化合物
公开(公告)号：US20110086898A1
公开(公告)日：2011-04-14
申请号：US12900046
申请日：2010-10-07
申请人： Kogyoku SHIN , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda , Kodo Shikata , Akira Inomata
发明人： Kogyoku SHIN , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda , Kodo Shikata , Akira Inomata
IPC分类号： A61K31/4162 , C07D487/04 , A61P25/00 , A61P1/00
CPC分类号： C07D498/04
摘要： A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism. wherein R1 and R2 are the same or different and are a hydrogen atom, a C1-6 alkyl group, a cyclic group selected from a C3-6 cycloalkyl group, a tetrahydropyranyl group, a dihydropyranyl group, a tetrahydrofuryl group, a dioxanyl group, a tetrahydrothienyl group, a dithianyl group and a hexahydrothiepinyl group, a C1-6 alkyl group substituted with a cyclic group selected from a C3-6 cycloalkyl group, a tetrahydropyranyl group, a dihydropyranyl group, a tetrahydrofuryl group, a dioxanyl group, a tetrahydrothienyl group, a dithianyl group and a hexahydrothiepinyl group, etc; R3, R4 and R5 are the same or different and are a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C1-6 alkoxy-C1-6 alkyl group, a C3-6 cycloalkoxy-C1-6 alkyl group or a halogen atom; R6 is a hydrogen atom or a C1-6 alkyl group; and R7 is a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkylthio group.
摘要翻译：由式（I）表示的化合物或其药理学上可接受的盐表现出优异的CRF受体拮抗作用。其中R1和R2相同或不同，为氢原子，C1-6烷基，选自C 3-6环烷基，四氢吡喃基，二氢吡喃基，四氢呋喃基，二氧杂环己烷基，四噻吩基，二噻烷基和六氢硫杂基，被选自C 3-6环烷基，四氢吡喃基，二氢吡喃基，四氢呋喃基，二烷基，四氢噻吩基中的环状基取代的C 1-6烷基二硫代基，六氢噻吩基等; R 3，R 4和R 5相同或不同，为氢原子，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基，C 1-6烷氧基-C 1-6烷基， C 3-6环烷氧基-C 1-6烷基或卤素原子; R6是氢原子或C1-6烷基; 并且R 7是C 1-6烷基，C 1-6烷氧基或C 1-6烷硫基。

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