New substituted 1,3-diphenylpropane derivatives are peroxisome proliferator-activated receptor agonist useful treat e.g. diabetic, dyslipidemia, cardiovascular disease, obesity, hypertension, inflammatory diseases and cerebral ischaemia

摘要

Substituted 1,3-diphenylpropane derivatives (I) and their stereoisomers (diastereoisomers, enantiomers), racemic mixtures, geometrical isomers, tautomers, salts, hydrates, solvates, solid forms or their mixtures are new. Substituted 1,3-diphenylpropane derivatives of formula (I) and their stereoisomers (diastereoisomers, enantiomers), racemic mixtures, geometrical isomers, tautomers, salts, hydrates, solvates, solid forms or their mixtures are new. X1halo, R1, -SR1 or -OR1; X2H, halo, R2, -SR2 or -OR2; X3halo, R3, -SR3 or -OR3; X4halo, R4, -SR4 or -OR4; X5halo, R5, -SR5 or -OR5; X6halo, R6, -SR6 or -OR6; X7halo, R7, -SR7 or -OR7; X8R8, -SR8 or -OR8; R1, R3, R5, R7H, (cyclo)alkyl, heterocycloalkyl or (hetero)aryl; R2, R4, R6(cyclo)alkyl, heterocycloalkyl or (hetero)aryl; R8alkyl substituted by -COOR12, -CONR12R13, -SO3H or -SO2NR12R13; A : CO, C=N-O-H, C=N-O-R11 or -CR9R10; R9, R10H, OH, alkyl or -OR11; R11alkyl (optionally substituted by (hetero)cycloalkyl or (hetero)aryl); B12C alkyl (unsubstituted, saturated), 2C alkene (unsubstituted) or 2C alkyne; and R12, R13H or alkyl (unsubstituted by substitutents of -COOR12, -CONR12R13, -SO3H or -SO2NR12R13). Provided that compound is not (I), where A is CO, B1 is unsubstituted 2C alkene, X6 and X7 is Cl, and X8 is -OCH2COOH. 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.