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아릴-아이속사졸-4-일-옥사다이아졸 유도체
专利权人:
发明人:
부에텔만 베른드,한 보,크누스트 헨너,코블렛 앤드리스,토마스 앤드류
申请号:
KR1020087017952
公开号:
KR1011212400000B1
申请日:
2006.12.13
申请国别(地区):
KR
年份:
2012
代理人:
摘要:
The present invention relates to one of formula (I) isoxazol-4-oxadiazole derivatives, or relates to a pharmaceutically acceptable acid addition salts.Formula (I)WhereinR 1 is hydrogen, halogen, aryl, heterocyclyl, heteroaryl, cyano, lower alkyl, - (CH 2)n - cycloalkyl, - (CH 2) n -N (R) 2, - (CH 2) n -O- lower alkyl or - (CH 2)n -OH andn is 0, 1 or 2R is hydrogen or lower alkylR 2 is halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen, lower alkyl substituted by halogen, C (O) O- lower alkyl, lower alkylsulfonyl, -NR a R b , -C (O) -NR a R b, -C (O) - heterocyclyl, benzyloxy, and hydroxy, halogen or lower alkyl substituted by heterocycle reel optionally substituted with one or more substituents selected from the group consisting of optionally the C 3-7 cycloalkyl, aryl, heteroaryl or heterocyclyl, or is lower alkyl optionally substituted with heteroarylR a and R b are independently lower alkyl optionally substituted with hydrogen, lower alkylsulfonyl, -C (O) H, - (CH 2) n -N (R) 2, - (CH 2) n -O- lower alkyl, - (CH 2)n -S- lower alkyl, - (CH 2)n -S (O) 2 - lower alkyl, heterocyclic aryl-sulfonyl, lower alkyl or - (CH 2)n - or heterocyclyl , or - (CH 2)n-C3-7 cycloalkyl, - (CH 2)n - heteroaryl, - (CH 2)n-OH or - (CO)-R (wherein, R is lower alkyl , cycloalkyl, or heteroaryl is), andR 3 is aryl or heteroaryl optionally substituted with lower alkyl substituted by halogen or halogen.Compounds of this class has been found that can be useful for the treatment of cognitive disorders, such as high affinity and exhibits a selectivity, as cognitive enhancer or Alzheimers disease and α5 receptor binding sites for GABA.본 발명은 하기 화학식 I의 아이속사졸-4-일-옥사다이아졸 유도체 또는 그의 약학적으로 허용가능한 산 부가 염에 관한 것이다:화학식 I상기 식에서,R1은 수소, 할로겐, 아릴, 헤테로사이클릴, 헤테로아릴, 시아노, 저급 알킬, -(CH2)n-사이클로알킬, -(CH2)n-N(R)2, -(CH2)n-O-저급 알킬 또는 -(CH2)n-OH이고n은 0, 1 또는 2이고R은 수소 또는 저급 알킬이고R2는 할로겐, 시아노, 나이트로, 저급 알킬, 저급 알콕시, 할로겐으로 치환된 저급 알콕시, 할로겐으로 치환된 저급 알킬, C(O)O-저급 알킬, 저급 알킬술포닐, -NRaRb, -C(O)-NRaRb
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