EP 1654227 A1 20060510 - BICYCLIC INDOLINE SULFONAMIDE DERIVATIVES
Title (en)
BICYCLIC INDOLINE SULFONAMIDE DERIVATIVES
Title (de)
BICYCLISCHE INDOLINSULFONAMID-DERIVATE
Title (fr)
DERIVES BICYCLIQUES D'INDOLINE-SULFONAMIDES
Publication
Application
Priority
- EP 2004008075 W 20040720
- DE 10335449 A 20030802
Abstract (en)
[origin: DE10335449A1] 2-(((5-(Phenyl or heteroaryl)-2,3-dihydro-1H-indol-1-yl)-sulfonyl)-1,2,3,4-tetrahydronaphthyl or indanyl)-alkanoic acid derivatives (I) are new. Bicyclic indoline-sulfonamide derivatives of formula (I) and their salts, solvates and solvated salts are new. [Image] R1>phenyl or Het (both optionally substituted by 1-3 of halo, CN, NO2, alkyl (optionally substituted by OH), alkoxy, CF3, OCF3, alkylsulfonyl, alkanoyl, alkoxycarbonyl, COOH, NH2, 1-6C acylamino or mono- or dialkylamino); Het : 5- or 6-membered heteroaryl containing 1 or 2 of N, O and/or S as heteroatom(s); R2> - R6>H or 1-4C alkyl; or CR2>R3>3-7 membered, spiro-linked cycloalkyl ring; R7>H or group hydrolyzable to H; n : 1 or 2; alkyl moieties have 1-6C unless specified otherwise. An independent claim is included for the preparation of (I). ACTIVITY : Cerebroprotective; antiarteriosclerotic; cardiant; antilipemic; vasotropic; anorectic; antidiabetic; hypotensive; hepatotropic; antiinflammatory; cytostatic. MECHANISM OF ACTION : Peroxisome proliferator activated receptor-delta (PPAR-delta ) activator. N-(4-((3,3-Dimethyl-5-(4-(trifluoromethyl)-phenyl)-2,3-dihydro-1H-indol-1-yl)-sulfonyl)-phenyl)-N-methylglycine (Ia) had EC50 in the range 10-100 nM in a cellular transactivation assay for identifying PPAR-delta ) activators, utilizing a GAL4-PPAR-delta chimera co-transfected with a reporter construct and stably expressed in CHO cells.
IPC 1-7
IPC 8 full level
A61P 3/04 (2006.01); C07D 209/08 (2006.01)
CPC (source: EP US)
A61P 3/04 (2017.12 - EP); A61P 9/00 (2017.12 - EP); A61P 9/10 (2017.12 - EP); C07D 209/08 (2013.01 - EP US)
Citation (search report)
See references of WO 2005016881A1
Designated contracting state (EPC)
DE ES GB GR IT
DOCDB simple family (publication)
DE 10335449 A1 20050217; CA 2534171 A1 20050224; EP 1654227 A1 20060510; JP 2007501195 A 20070125; US 2007117860 A1 20070524; WO 2005016881 A1 20050224
DOCDB simple family (application)
DE 10335449 A 20030802; CA 2534171 A 20040720; EP 04763344 A 20040720; EP 2004008075 W 20040720; JP 2006522267 A 20040720; US 56634004 A 20040720