C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/231, 167/237
C07D 233/54 (2006.01) A61K 31/415 (2006.01) A61K 31/445 (2006.01) C07D 401/04 (2006.01) C07D 401/10 (2006.01) C07D 405/00 (2006.01) C07D 405/06 (2006.01) C07D 413/06 (2006.01) C07D 413/14 (2006.01)
Patent
CA 2027179
ABSTRACT Certain novel imidazole derivatives N-substituted by a vinyl group itself carrying a mevalonic acid derivative or corresponding lactone are inhibitors of HMG-CoA reductase and are useful for lowering blood plasma cholesterol levels. The compounds are of general formula (I): Image (I) in which one of the groups R1 and R2 represents a C1-6alkyl group optionally substituted by one to three halogen atoms and the other represents a phenyl ring optionally substituted by one to five substituents selected from halogen atoms and hydroxyl, C1-3alkyl, C1-3alkoxy, S(O)nC1-3alkyl, (CH2)mNRaRb, (CH2)mNRcCORd and trifluoromethyl groups; R3 represents a phenyl ring optionally substituted by one to five substituents selected from halogen atoms and hydroxyl, C1-3alkyl, C1-3alkoxy, S(O)nC1-3alkyl, (CH2)mNRaRb, (CH2)mNRcCORd and trifluoromethyl groups; with the proviso that at least one of the groups R1, R2 and R3 contains an S(O)nC1-3alkyl, (CH2)mNRaRb or (CH2)mNRcCORd substituent; X represents -CH=CH-; Z represents Image (a) (or) Image (b) and physiologically acceptable solvates, physiologically acceptable acid addition salts thereof when R4 represents hydrogen or a physiologically acceptable and metabolically labile carboxyl protecting group when Z is (a), and quaternary ammonium derivatives thereof.
Kirk Barrie E.
Lester Michael G.
Procopiou Panayiotis A.
Ross Barry C.
Watson Nigel S.
Fetherstonhaugh & Co.
Glaxo Group Limited
Kirk Barrie E.
Lester Michael G.
Procopiou Panayiotis A.
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