New 1-aryloxy-3-pyrrol-1-yl-propan-2-one derivatives are cytosolic phospholipase A2 inhibitors, useful for prophylactic or therapeutic treatment of diseases caused by increased activity of phospholipase A2, preferably e.g. pain and fever

摘要

1-aryloxy-3-pyrrol-1-yl-propan-2-one derivatives (I) are new. 1-aryloxy-3-pyrrol-1-yl-propan-2-one derivatives of formula (I), their enantiomers, diastereomers, salts and/or esters are new. R1 : COR2; R2 : D1-E; D1 : 1-8C alkyl, 2-8C alkenyl, 2-8C alkynyl, aryl, T-aryl, T-aryl-G or aryl-G; T, G : 1-8C alkyl, 2-8C alkenyl or 2-8C alkynyl; E : OR3 or CN; R3 : H or 1-6C alkyl; either R4, R5 : H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl or R6-COOH; or R4+R5+C to which R4 and R5 are bonded : 5-6-membered (hetero)aromatic ring (optionally substituted by 1 or 2 R7); R6 : 1-6C alkyl, 2-6C alkenyl or 2-6C alkynyl; R7 : 1-6C alkyl, halo, CF 3, CN or COOH; Q : R8, OR8 or SR8; R8 : 1-16C alkyl, 2-16C alkenyl or 2-16C alkynyl (all linear and all optionally interrupted by 1 or 2 O, S or aryl (optionally substituted by 1 or 2 R9 and 1-2 1-6C alkyl, and optionally interrupted)), H or aryl (optionally substituted by 1 or 2 R9); Ar1 : aryl (optionally substituted by 1 or 2 R9); and R9 : 1-6C alkyl, halo, OR6, SR6 or CF 3. An independent claim is also included for preparing (I). [Image] ACTIVITY : Antiinflammatory; Analgesic; Antipyretic; Antiallergic; Antiasthmatic; Antipsoriatic; Cerebroprotective; Vasotropic; Neuroprotective; Nootropic; Dermatological; Antirheumatic; Anticoagulant; Thrombolytic; Immunosuppressive; Antibacterial; Virucide; Cytostatic. MECHANISM OF ACTION : Cytosolic phospholipase A2 inhibitor. Test details are described but no results given.