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PYRROLIDINE DERIVATIVES AS NK - 3 RECEPTOR ANTAGONISTS
专利权人:
发明人:
申请号:
EP10790561.4
公开号:
EP2513084A1
申请日:
2010.12.14
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
The present application relates to compounds of formula (I) wherein R1 is hydrogen, halogen, cyano, lower alkyl or lower alkyl substituted by halogen n is 1, 2 or 3, if n is 2 or 3, R1 can be different R2 is C2-7-alkyl or C3-6-cycloalkyl R3 is the group (II) wherein X is CH or N R5 is hydrogen, -C(O)-lower alkyl, -C(O)O-lower alkyl, S(O)2-lower alkyl, -C(O)CH2O-lower alkyl, -C(O)-CH2-CN, or is - or -C(O)-cycloalkyl, cycloalkyl, or -CH2-cycloalkyl, wherein the cycloalkyl groups are optionally substituted by lower alkyl, -CH2-O-Iower alkyl, lower alkoxy, CF3, halogen or cyano, or is -C(O)-heterocycloalkyl or heterocycloalkyl, or is -C(O)-heteroaryl or is heteroaryl or is -C(O)-aryl or aryl, which heterocycloalkyl, heteroaryl or aryl groups are optionally substituted by halogen, lower alkyl, =O, lower alkoxy, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, -C(O)-CH2-N(di-lower alkyl), C(O)NH-lower alkyl, C(O)NH2, -O-C(O)- lower alkyl, C(O)-lower alkyl, S(O)2-lower alkyl or cyano R4 is aryl, which is optionally substituted by halogen, hydroxy, lower alkyl, lower alkyl substituted by halogen, S(O)2-lower alkyl, cyano or by lower alkoxy or to a pharmaceutically active salt thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinsons disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Cette invention concerne des composés de formule (I) ou un sel pharmaceutiquement actif de ceux-ci. Dans ladite formule, R1 est un atome dhydrogène, un atome dhalogène, un groupe cyano, alkyle inférieur ou alkyle inférieur substitué par un atome dhalogène n est 1, 2 ou 3, et si n est 2 ou 3, R1 peut être différent R2 est un groupe alkyle C2-7 ou cycloalkyle C3-6 R3 est le groupe (II) où X est CH ou N R5 est un atome dhydrogène, un groupe -C(O)-alkyle inférieur, -C(O)O-alkyle inférieur, S(O)2-alkyle inférieur, -C(O)CH2O-alkyle inférieur,
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