Title:
Indoline 2-ON, or pyrrolo pyridine / pyrimidine 2-ON derivative
Document Type and Number:
Japanese Patent JP6130061
Kind Code:
B2
Abstract:
The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein Ar is a 6-membered heteroaryl group, containing one or two N-atoms, which are the groups, pyridinyl, pyrimidinyl, pyridazinyl, or a 5-membered heteroaryl group containing from 1 to 3 heteroatoms, selected from N, S or O, which groups are imidazolyl, 1,2,4-oxadiazolyl, 1,3,4-oxadazolyl, isoxazolyl, oxazolyl, 1,3,4-thiadiazolyl or pyrazolyl; 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; is 0, 1, 2 or 3; m is 0, 1 or 2; and the dotted line indicates a bond may or may not be present; or, 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.
Inventors:
Bruner, Daniela
Hilpelt, Hans
Korzewski, Sabine
Limberg, Anya
Marberg, Jessica
Erich Prinzen
Reamel, claus
Shankar, Bhavani Gee
Stol, Theodor
Hilpelt, Hans
Korzewski, Sabine
Limberg, Anya
Marberg, Jessica
Erich Prinzen
Reamel, claus
Shankar, Bhavani Gee
Stol, Theodor
Application Number:
JP2016520396A
Publication Date:
May 17, 2017
Filing Date:
June 16, 2014
Export Citation:
Assignee:
F. HOFFMANN-LA ROCHE AKTIENGESELLSCHAFT
International Classes:
C07D401/04; A61K31/19; A61K31/4155; A61K31/4178; A61K31/422; A61K31/4245; A61K31/433; A61K31/435; A61K31/437; A61K31/4439; A61K31/444; A61K31/496; A61K31/497; A61K31/501; A61K31/506; A61K31/519; A61K31/53; A61K31/5383; A61K31/55; A61K31/551; A61K31/5513; A61K33/00; A61K45/00; A61P1/14; A61P19/02; A61P21/00; A61P25/00; A61P25/04; A61P25/16; A61P25/18; A61P25/20; A61P25/22; A61P25/24; A61P25/28; A61P25/30; A61P25/32; A61P29/00; A61P43/00; C07D403/04; C07D405/14; C07D413/04; C07D413/14; C07D417/04; C07D471/04; C07D471/10; C07D487/04; C07D498/04
Foreign References:
| WO1991006545A1 |
Attorney, Agent or Firm:
Patent business corporation Tsukuni