ANALOGS OF MEVALOLACTONE AND DERIVATIVES THEREOF,PROCESSES FOR THEIR PRODUCTION,PHARMACEUTICAL COMPOSITIONS CONTAINIG THEM AND THEIR USE AS PHARMACEUTICALS

摘要

Cpds. of formula (I) and their esters, delta-lactones and salts are new. In (I) (one of R and R' is R4, R5, R5aC6H2 and the other is p- or s-(1-6C)alkyl, (3-6C) cycloalkyl or Ph-(CH2)m; R4 is H, 1-4C alkyl, 1-4C alkoxy (except tBuO), CF3, F, Cl, PhO or PhCH2O; R5 is H, 1-3C alkyl, 1-3C alkoxy, CF3, F, Cl, PhO or PhCH2O; R5a is H, Me, Et, MeO, EtO, F or Cl; m is 1, 2 or 3; R2 is H, 1-4C alkyl, 3-6C cycloalkyl, 1-4C alkoxy (except tBuO), CF3, F, Cl, PhO or PhCH2O; R3 is H, 1-3C alkyl, 1-3C alkoxy, CF3, F, Cl, PhO or PhCH2O; X is (CH2)n or vinylene; n is 1, 2 or 3; and R6 is H or 1-3C alkyl. Provided that (1) R5 and R5a are H when R4 is H; (2) R5a is H when R5 is H; (3) only 1 of R4 and R5 may be CF3 or PhO or PhCH2O; (4) R3 is H when R2 is H; and (5) only 1 of R2 and R3 may be CF3 or PhO or PhCH2O). Some intermediates to (I) are also new and claimed. Dosage of (I) is 1-2000 mg daily.