Heterocyclic analogs of mevalonolactone and derivatives...

C - Chemistry – Metallurgy – 07 – D

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167/207, 260/326

C07D 207/337 (2006.01) C07D 307/54 (2006.01) C07D 333/24 (2006.01)

Patent

CA 1278794

Case 600-7035 HETEROCYCLIC ANALOGS OF MEVALONOLACTONE AND DERIVATIVES THEREOF, PROCESSES FOR THEIR PRODUCTION AND THEIR USE AS PHARMACEUTICALS Abstract of the Disclosure Compounds of formula Image I wherein Ra is a group -X-Z, Rb is R2, Rc is R3, Rd is R4 and Y is a group Image or Ra is R1, Rb is a group -X-Z, Rc is R2, Rd is R3 and Y is O,S or a group Image R1, R2, R3 and R4 independently are C1-6alkyl not containing an asymmetric carbon atom, C3-7cycloalkyl or a ring Image or in the case of R3 and R4 additionally hydrogen, or for R3 when Y is O or S Image = Image whereby R17 is hydrogen or C1-3alkyl and R18 and R19 are independently hydrogen C1-3alkyl or phenyl; each R5 is independently hydrogen, C1-3alkyl, n-butyl, i-butyl, t-butyl, C1-3alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, bromo, phenyl, phenoxy or benzyloxy; each R6 is independently hydrogen, C1-3alkyl, C1-3alkoxy, trifluoromethyl, fluoro, chloro, bromo, phenoxy or benzyloxy, and each R7 is independently hydrogen, C1-2alkyl, C1-2alkoxy, fluoro or chloro, 600-7035 with the proviso that there may only be one each of tri- fluoromethyl, phenoxy or benzyloxy in each ring A present, X is (CH2)m or (CH2) CH=CH-(CH2)q, m is 0, 1, 2 or 3 and both q's are 0 or one is 0 and the other is 1, z is Image II wherein R9 is hydrogen or C1-3alkyl, in free acid form, or in the form of an ester or .delta.-lactone thereof or in salt form as appropriate, which compounds are indicated for use as pharmaceuticals in particular as hypolipoproteinemic and anti-atherosclerotic agents.

521333

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