发明名称 Derivatives of substituted 3-phenyl-1-(phenylthienyl)propan-1-ones and of 3-phenyl-1-(phenylfuranyl)propan-1-ones, preparation and use
摘要 <p>Substituted 3-phenyl-1-(phenylthienyl)propan-1-one and 3-phenyl-1-(phenylfuranyl)propan-1-one derivatives (I) and their stereoisomers (diastereoisomers, enantiomers), racemic mixtures, geometrical isomers, tautomers, salts, hydrates, solvates, solid forms or their mixtures are new. Substituted 3-phenyl-1-(phenylthienyl)propan-1-one and 3-phenyl-1-(phenylfuranyl)propan-1-one derivatives of formula (I) and their stereoisomers (diastereoisomers, enantiomers), racemic mixtures, geometrical isomers, tautomers, salts, hydrates, solvates, solid forms or their mixtures are new. X 1halo, R 1, -SR 1 or -OR 1; X 2S or O; X 3halo, R 3, -SR 3 or -OR 3; X 4halo, R 4, -SR 4 or -OR 4; X 5R 5, -SR 5 or -OR 5; X 6halo, R 6, -SR 6 or -OR 6; X 7halo, R 7, -SR 7 or -OR 7; X 8R 8; R 1, R 3, R 4, R 6-R 8H or alkyl; R 5alkyl substituted by -COOR 1 2, -CONR 1 2R 1 3, -SO 3H or -SO 2NR 1 2R 1 3, where substitutents are substituted by optionally substituted by (hetero)cycloalkyl or (hetero)aryl; A : CO, C=N-O-H, C=N-O-R 1 1, -CR 9R 1 0 or R 1 1; R 9, R 1 0H, alkyl or -OR 1 1; R 1 1H, aryl, heterocycloalkyl, heteroaryl or alkyl (optionally substituted by (hetero)cycloalkyl or (hetero)aryl); B 12C alkyl (unsubstituted, saturated), 2C alkene (unsubstituted) or 2C alkyne; and R 1 2, R 1 3H or alkyl (unsubstituted). An independent claim is included for a pharmaceutical composition comprising (I), in a support, optionally in combination with therapeutic and/or cosmetic active ingredients and a compound. [Image] - ACTIVITY : - Analgesic; Antianginal; Antidiabetic; Antilipemic; Cardiovascular-Gen; Anorectic; Hypotensive; Antiinflammatory; Cerebroprotective; Vasotropic; Immunosuppressive; Cytostatic; Neuroprotective. - MECHANISM OF ACTION : Peroxisome proliferator-activated receptor agonist.</p>
申请公布号 IL199488(A) 申请公布日期 2013.10.31
申请号 IL20090199488 申请日期 2009.06.22
申请人 GENFIT 发明人
分类号 A61K;A61P;C07D 主分类号 A61K
代理机构 代理人
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