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DERIVES INDOLIN-2-ONE OU PYRROLO-PYRIDIN/PYRIMIDIN-2-ONE
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
BRUNNER, DANIELA,HILPERT, HANS,KOLCZEWSKI, SABINE,LIMBERG, ANJA,MALBERG, JESSICA,PRINSSEN, ERIC,RIEMER, CLAUS,SHANKAR, BAVANI G.,STOLL, THEODOR
申请号:
CA2915536
公开号:
CA2915536A1
申请日:
2014.06.16
申请国别(地区):
CA
年份:
2014
代理人:
摘要:
The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein Ar is a heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O; R1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF3, (CH2)o-lower alkoxy, cycloalkyl optionally substituted by CF3, or heterocycloalkyl optionally substituted by lower alkyl; R2 is hydrogen, lower alkyl, (CH2)o-cycloalkyl, (CH2)o-O-cycloalkyl, (CH2)o-lower alkoxy, CH2)o-lower alkoxy substituted by halogen, (CH2)o-heterocycloalkyl optionally substituted by lower alkyl, (CH2)o-S(O)2-cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two lower alkoxy, (CH2)o-S(O)2-lower alkyl, lower alkyl substituted by halogen or CH2CH(OH)CF3; R3 is halogen or lower alkyl; X is CH or N; X1 is CH or N; n is 1 or 2; o is 0, 1, 2 or 3; m is 0, 1 or 2; and the dotted line is a bond or not; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof The compounds may be used for the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.
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