EP 1656134 A1 20060517 - INDOLINE-SULFANILIC ACID AMIDES USED AS PPAR DELTA MODULATORS
Title (en)
INDOLINE-SULFANILIC ACID AMIDES USED AS PPAR DELTA MODULATORS
Title (de)
INDOLIN-SULFANILSÄUREAMIDE ALS PPAR-DELTA MODULATOREN
Title (fr)
AMIDES D'ACIDE INDOLINO-SULFANILIQUE UTILISES COMME MODULATEURS DE PPAR-DELTA
Publication
Application
Priority
- EP 2004008076 W 20040720
- DE 10335450 A 20030802
Abstract (en)
[origin: DE10335450A1] N-(4-(Indoline-1-sulfonyl)-phenyl)-amino acid derivatives (I) are new. New N-(4-(indoline-1-sulfonyl)-phenyl)-amino acid derivatives of formula (I) and their salts, solvates and solvated salts are new. [Image] R1>phenyl or Het (both optionally substituted by 1-3 halo, CN, NO2, alkyl (optionally substituted by OH), alkoxy, CF3, OCF3, alkylsulfonyl, alkanoyl, alkoxycarbonyl, COOH, NH2, 1-6C acylamino or mono- or di-alkylamino); Het : 5- or 6-membered heteroaryl containing 1 or 2 N, O and/or S heteroatom(s); R2>-R4>, R7>, R8>H or A, or CR2>R3>3-7 membered, spiro-linked cycloalkyl; A : 1-4C alkyl; R5>H, A, OA or halo; R6>alkyl, 3-8C cycloalkyl, alkanoyl, alkylsulfonyl or alkoxycarbonyl, and R9>H or group hydrolyzable to H; 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. In a cellular transactivation assay for identifying PPAR-delta activators, using a GAL4-PPAR-delta chimera co-transfected with a reporter construct and stably expressed in Chinese hamster ovary cells, results showed that N-(4-((3,3-dimethyl-5-(4-(trifluoromethyl)-phenyl)-2,3-dihydro-1H-indol-1-yl)-sulfonyl)-phenyl)-N-methylglycine (Ia) exhibited an EC50 value of 8.5 nM.
IPC 1-7
IPC 8 full level
A61P 3/06 (2006.01); A61P 9/10 (2006.01); C07D 209/08 (2006.01); C07D 209/96 (2006.01)
CPC (source: EP US)
A61P 3/06 (2017.12 - EP); A61P 9/00 (2017.12 - EP); A61P 9/10 (2017.12 - EP); A61P 43/00 (2017.12 - EP); C07D 209/08 (2013.01 - EP US); C07D 209/96 (2013.01 - EP US)
Citation (search report)
See references of WO 2005016335A1
Designated contracting state (EPC)
DE ES FR GB IT
DOCDB simple family (publication)
DE 10335450 A1 20050217; CA 2534194 A1 20050224; EP 1656134 A1 20060517; JP 2007501196 A 20070125; US 2007185183 A1 20070809; WO 2005016335 A1 20050224
DOCDB simple family (application)
DE 10335450 A 20030802; CA 2534194 A 20040720; EP 04741154 A 20040720; EP 2004008076 W 20040720; JP 2006522268 A 20040720; US 56705804 A 20040720