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
LEHR, MATTHIAS, PROF. DR.,Matthias, Prof. Dr. Lehr,ARNSMANN, MARTINA,Martina Arnsmann
申请号：
DE102012017516
公开号：
DE102012017516A1
申请日:
2012.09.05
申请国别(地区):
DE
年份:
2014
代理人:
摘要：
Die vorliegende Erfindung betrifft neue heteroarylsubstituierte Acetonderivate, die das Enzym Phospholipase A2hemmen, sowie pharmazeutische Mittel umfassend diese Verbindungen.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.
