크너스트 헨너,코브렛 안드레아스,네테코벤 마티아스,라트니 하샌,리메르 클라우스,비피안 발터
申请号:
KR1020127018657
公开号:
KR1014900040000B1
申请日:
2010.12.14
申请国别(地区):
KR
年份:
2015
代理人:
摘要:
The present invention relates to a compound or a pharmaceutically active salt of formula (I) relates: Formula I Wherein, And R 1 is hydrogen, halogen, cyano, lower alkyl or lower alkyl substituted by halogen, n is 1, 2 or 3, provided that, when n is 2 or 3, R 1 may be different R 2 is C 2-7 - alkyl or C 3-6 - cycloalkyl R 3 is a group high X is CH or N R 5 is hydrogen, -C (O) - lower alkyl, -C (O) O- lower alkyl, S (O) 2 - lower alkyl, -C ( O) CH 2 O- lower alkyl, -C (O) -CH 2 -CN, -C (O) - cycloalkyl, cycloalkyl-alkyl, -CH 2 - cycloalkyl, -C (O) - heterocycloalkyl, heterocycloalkyl, -C (O) - heteroaryl, heteroaryl, -C (O) - aryl or aryl, wherein the cycloalkyl, group is optionally lower alkyl, -CH 2 -O- lower alkyl, lower alkoxy, CF 3 , halogen or cyano-substituted, and heterocycloalkyl, heteroaryl or aryl group is an optionally halogen, lower alkyl, = O, lower alkoxy, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, -C (O) -CH 2 -N (di-lower alkyl), C (O) NH- lower alkyl, C (O) NH 2 , -OC (O) - lower alkyl, C (O) - lower alkyl, S (O) 2 - substituted with lower alkyl or cyano R 4 s is aryl, optionally halogen, hydroxy, lower alkyl, lower alkyl substituted by halogen, S (O) 2 - lower alkyl, cyano or It is substituted by lower alkoxy. The compounds of the present invention are depression, pain, psychosis, Parkinsons disease, schizophrenia, and was found to be a highly potential NK3 receptor antagonist in the treatment of anxiety and attention deficit hyperactivity disorder (ADHD).본 발명은 하기 화학식 I의 화합물 또는 이의 약학적으로 활성인 염에 관한 것이다:화학식 I상기 식에서,R1은 수소, 할로겐, 시아노, 저급 알킬 또는 할로겐으로 치환된 저급 알킬이고, n은 1, 2 또는 3이되, n이 2 또는 3인 경우, R1은 상이할 수 있고R2는 C2-7-알킬 또는 C3-6-사이클로알킬이고R3은 기 고X는 CH 또는 N이고R5는 수소, -C(O)-저급 알킬, -C(O)O-저급 알킬, S(O)2-저급 알킬, -C(O)CH2O-저급 알킬, -C(O)-CH2-CN, -C(O)-사이클로알킬, 사이클로알킬, -CH2-사이클로알킬, -C(O)-헤테로사이클로알킬, 헤테로사이클로알킬, -C(O)-헤테로아릴, 헤테로아릴, -C(O)-아릴 또는 아릴이고, 이때 사이클로알킬 기는 임의적으로 저급 알킬, -CH2-O-저급 알킬, 저급 알콕시, CF3, 할로겐 또는 시아노로