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公开(公告)号：US20120202828A1
公开(公告)日：2012-08-09
申请号：US13386199
申请日：2010-07-21
IPC分类号： A61K31/519 , A61P25/28 , C07D491/048
CPC分类号： C07D491/048
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, R2 and Rx 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，R 2和R 3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：US09139594B2
公开(公告)日：2015-09-22
申请号：US13386199
申请日：2010-07-21
IPC分类号： A61K31/519 , A61P25/28 , C07D491/048
CPC分类号： C07D491/048
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, R2 and Rx 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，R 2和R 3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：US20110166136A1
公开(公告)日：2011-07-07
申请号：US13002374
申请日：2009-07-03
申请人： Nawaz Mohammed Khan , Svenja Burckhardt , Julie Elaine Cansfield , Ngoc-Tri Vo , Richard Edward Armer , Raymond John Boffey
发明人： Nawaz Mohammed Khan , Svenja Burckhardt , Julie Elaine Cansfield , Ngoc-Tri Vo , Richard Edward Armer , Raymond John Boffey
IPC分类号： A61K31/5377 , C07D403/06 , A61K31/496 , C07D413/06 , C07D209/42 , A61K31/404 , A61P29/00 , A61P9/00 , A61P25/22 , A61P13/00 , A61P25/06 , A61P1/00 , A61P3/00
CPC分类号： C07D491/056 , A61K31/404 , C07D209/18 , C07D209/24 , C07D401/06
摘要： Compounds of formula (1), salts and pro-drugs wherein: R1, R2, R3 and R4 are hydrogen, alkyl, hydroxyalkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, nitro, amino, monalkylamino, dialkylamino, acylamino, alkoxycarbonylamino, alkylsulphonyl, arylsulphonyl, alkylsulphonylamino, arylsulphonylamino, aminosulphonyl or cyano, or any two of R1 to R4 that are adjacent on the ring may together represent the moiety —O—(CH2)n—O— wherein n is 1 to 3; R5 is hydrogen or alkyl; R6 is hydrogen or alkyl; and X is selected from the group consisting of: (a) groups of formula OR7 wherein R7 is hydrogen or alkyl which is optionally substituted with a substituent selected from alkylsulfonylalkyl, saturated or partially unsaturated heterocyclic, alkoxy, carboxyl, nitro, amino, monalkylamino, dialkylamino, halogen, and alkoxycarbonyl, provided that when R7 is hydrogen or ethyl, then R1, R2, R3 and R4 cannot be selected from hydrogen, halogen and alkyl; and (b) groups of formula NR8R9 wherein R8 and R9 together with the nitrogen atom to which they are attached form a saturated or partially unsaturated heterocyclic group which optionally contains at least one more heteroatom selected from nitrogen, oxygen and sulphur atoms, said saturated or partially unsaturated heterocyclic group optionally further being substituted by one or more substituents selected from alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, nitro, amino, monalkylamino, dialkylamino and hydroxyl, provided that: (i) when R8+R9+N=piperazine, and ≧1 of R1 to R4 are hydrogen, hydroxyl, nitro, amino, alkylamino, dialkylamino, alkoxycarbonylamino, halogen, alkoxy or alkyl, the nitrogen atom at the 4-position of the piperazine is not alkyl substituted, (ii) when each of R1, R2, R3, R4, R5 and R6 is hydrogen, X is not unsubstituted piperazinyl or unsubstituted morpholino, (iii) when each of R1, R2, R4, R5 and R6 is hydrogen and R3 hydrogen, bromine or hydroxyl, X is not methoxy, (iv) when each of R2 and R3 is methoxy or they together represent —O—CH2—O— and each of R1, R4, R5 and R6 is hydrogen, X is not unsubstituted piperidine, are Cavx channel blockers and are of use in the treatment of various conditions including pain.
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