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INDOLIN-2-ONE DERIVATIVES
专利权人:
Hoffmann-La Roche Inc.
发明人:
Delphine Gaufreteau,Hans Hilpert,Roland Humm,Sabine Kolczewski,Thorsten Muser,Jean-Marc Plancher,Theodor Stoll
申请号:
US15971426
公开号:
US20180251455A1
申请日:
2018.05.04
申请国别(地区):
US
年份:
2018
代理人:
摘要:
The present invention is concerned with indolin-2-one derivatives of general formulawhereinA is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected fromR1 is S(O)2lower alkyl, S(O)2NR4R5, S(O)2cycloalkyl, S-lower alkyl or S(O)2-azetidin-1-yl; R4 and R5 are independently from each other hydrogen, lower alkyl or (CH2)2OCH3; or the group A-R1 may form together with two neighboring carbon atoms from the groupA an additional fused ring, selected fromR2 is hydrogen or cycloalkyl;R3 is methyl or halogen;n is 1 or 2;X is N, N+O− or CH;--- the dotted line may be nothing or —CH2—;as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.The compounds may be used in the treatment of CNS diseases related to 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, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co-morbid epilepsy.
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