C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/306.2, 260/3
C07D 209/18 (2006.01) C07D 209/12 (2006.01) C07D 209/42 (2006.01) C07D 405/02 (2006.01) C07D 405/06 (2006.01) C07F 9/572 (2006.01)
Patent
CA 1210405
ANALOGS OF MEVALOLACTONE AND DERIVATIVES THEREOF ABSTRACT Compounds of formula I Image (I) wherein one of R and Ro is Image and the other is primary or secondary C1-6alkyl, C3-6cycloalkyl or phenyl-(CH2)m-, wherein R4 is hydrogen, C1-4alkyl, C1-4alkoxy, (except t-butoxy), trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R5 is hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R5a is hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, and m is 1, 2 or 3, with the provisos that both R5 and R5a must be hydrogen when R4 is hydrogen, R5a must be hydrogen when R5 is hydrogen, not more than one of R4 and R5 is trifluoromethyl, not more than one of R4 and R5 is phenoxy and not more than one of R4 and R5 is benzyloxy, R2 is hydrogen, C1-4alkyl, C3-6cyclo- alkyl, C1-4alkoxy, (except t-butoxy), trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, R3 is hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, with the provisos that R3 must be hydrogen when R2 is hydrogen, not more than one of R2 and R3 is trifluoromethyl, not more than one of R2 and R3 is phenoxy, and not more than one of R2 and R3 is benzyloxy, X is -(CH2)n- or -CH=CH- (n=0, 1, 2 or 3), Z is Image II wherein R6 is hydrogen or C1-3alkyl in free acid form or in the form of a physiologically-hydro- lysable and -acceptable ester or a lactone thereof or in salt form. These compounds are indicated for use as pharmaceuticals particularly for inhibiting cholesterol biosynthesis and treating atherosclerosis.
441684
Kirby Eades Gale Baker
Novartis Ag
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