New indole derivatives are peroxisome proliferator activated receptor activators useful to treat e.g. hypertriglyceridimia, hyperlipidemia, hypercholesterolemia and diabetes

摘要

Indole derivatives (I), are new. Indole derivatives of formula (I) and their salts are new. R a, R bH, halo, 1-6C alkyl, CF 3, CN, COR 2, OR 2 or phenyl (optionally substituted by 1-4C alkyl or CF 3); R 21-4C alkyl, CF 3 or phenyl (optionally substituted by 1-4C alkyl or CF 3); R 2H or 1-4C alkyl; R : H or 1-3C alkyl; n : 1-3; X : a bond or O, and Ar 1phenyl, naphthyl, quinolinyl, isoquinolinyl, pyridinyl, pyrazolyl, imidazolyl, isoxazolyl, thiazolyl, benzothiazolyl, 2,1,3-benzothiadiazolyl, 3,4-dihydro-1,4-benzoxazinyl, 5,6,7,8-tetrahydronaphthlaneyl, 1,2,3,4-tetrahydroquinolinyl, 1,2,3,4-tetrahydroisoquinolinyl, 1,2,3,4-tetrahydro-2-oxoquinolinyl, 3,4-dihydro-2H-benzopyranyl, indolyl, 2,3-dihydroindolyl, 2,3-dihydrobenzofuranyl, 1,3-benzodioxolyl, 1,4-benzodioxanyl or benzoxazolyl (all optionally substituted by halo, 1-6C alkyl, CF 3, CN, CO-R 2, OR 2, NH-COR 2, morpholinyl, amino or 4-morpholinosulfonyl). Independent claims are included for the preparation of (I). [Image] ACTIVITY : Antilipemic; Antidiabetic; Cardiovascular-Gen.; Antiinflammatory; Neuroprotective; Nootropic; Antiparkinsonian; Anorectic; Antiarteriosclerotic; Cardiant; Hypotensive; Antiarthritic; Antirheumatic. MECHANISM OF ACTION : Peroxisome proliferator activated receptor (PPAR) activator. In a test used to determine activation of PPAR-alpha and/or PPAR-gamma , results showed that (I) exhibited an EC 50 value of 50 nM.