Pyrazole analogs of mevalonolactone and derivatives thereof,...

C - Chemistry – Metallurgy – 07 – D

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C07D 231/12 (2006.01) A61K 31/415 (2006.01) C07D 405/02 (2006.01) C07D 405/06 (2006.01)

Patent

CA 1249283

PYRAZOLE ANALOGS OF MEVALONOLACTONE AND DERIVATIVES THEREOF, PROCESSESFOR THEIR PRODUCTION AND THEIR USE Abstract of the Disclosure Compounds of formula I Image I wherein R1 is C1-6 alkyl, each of R2 and R5 is independently hydrogen, C1-4 alkyl, C1-4 alkoxy (except t-butoxy), trifluoromethyl, fluoro, chloro, phenyl, phenoxy or benzyloxy, each of R3 and R6 is independently hydrogen, C1-3 alkyl, C1-3 alkoxy, trifluoromethyl, fluoro, chloro, phenoxy or benzyloxy, each of R4 and R7 is independently hydrogen, C1-3 alkyl, C1-2 alkoxy, fluoro or chloro, with the proviso that there may only be a single trifluoromethyl, phenoxy or benzyloxy substituent in each of rings A and B, X is -(CH2)m- or -(CH2)qCH=CH(CH2)q- wherein m is 0, 1, 2 or 3 and both q's are 0 or one is 0 and the other is 1, Image wherein R10 is hydrogen or C1-3 alkyl, with the general proviso that the -X-Z' group is in the 4- or 5-position of the pyrazole ring and is ortho to R1; in free acid form or in the form of an ester or ?-lactone thereof or in salt form, which are indicated for use as hypolipoproteinemic- and anti-atherosclerotic agents.

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