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。

公开(公告)号：US20110152253A1

公开(公告)日：2011-06-23

申请号：US13055830

申请日：2009-07-24

申请人： Takafumi Motoki ,  Toshihiko Kaneko ,  Noboru Yamamoto ,  Afzal Khan

发明人： Takafumi Motoki ,  Toshihiko Kaneko ,  Noboru Yamamoto ,  Afzal Khan

IPC分类号： A61K31/547 ,  C07D513/10 ,  A61P25/28

CPC分类号： C07D513/10

摘要： A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof, 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。

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。