Cyclic ketal derivatives

Details Cyclic ketal derivatives Cyclic ketal derivatives

1993-10-26

1995-04-25

Chan, Nicky

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

549363, A61K 31335, C07D31100

Patent

active

054099501

ABSTRACT:
Compounds are described of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom, a hydroxyl group or a group selected from --OCOCH.dbd.CHCH(CH.sub.3)(CH.sub.2).sub.3 CH.sub.3, --OCOCH.dbd.CHC(CH.sub.3).dbd.CHCH(CH.sub.3)--CH.sub.2 CH.sub.3, or --OCO--X--CH.sub.2 CH(CH.sub.3)CH.sub.2 CH.sub.3 [where X is --CH.dbd.CHCH(CH.sub.3)--, --CH.sub.2 CH(OH)CH(CH.sub.3)--, --CH.dbd.CHC(OH)(CH.sub.3)--, --CH.sub.2 CH(OH)CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH(CH.sub.3)--)];
R.sub.2 represents a hydrogen atom or a hydroxyl group;
R.sub.3 represents a group selected from --C(.dbd.CH.sub.2)CH(OR.sub.7)CH(CH.sub.3)CH.sub.2 Ph (where R.sub.7 is a hydrogen atom or an acetyl group), --C(CH.sub.3).dbd.CHCH(CH.sub.2 R.sub.8)CH.sub.2 Ph (where R.sub.8 is a hydrogen or a hydroxyl group), --C(CH.sub.2 OH).dbd.CHCH(CH.sub.3)CH.sub.2 Ph, --C(.dbd.CH.sub.2)CH(OH)CH(CH.sub.2 OH)CH.sub.2 Ph, --C(.dbd.CH.sub.2)CH(NHCOCH.sub.3)CH(CH.sub.3)CH.sub.2 Ph, --C(CH.sub.2 NHCOCH.sub.3).dbd.CHCH(CH.sub.3)CH.sub.2 Ph or ##STR2## R.sub.4, R.sub.5 and R.sub.6 may each independently represent a hydrogen atom or a methyl group and salts thereof; with the proviso that when either of R.sub.1 and R.sub.2 represents a hydrogen atom R.sub.3 is a group selected from --C(.dbd.CH.sub.2)CH(OR.sub.7)CH(CH.sub.3)CH.sub.2 Ph and --C(CH.sub.3).dbd.CHCH(CH.sub.3)CH.sub.2 Ph and when both of R.sub.1 and R.sub.2 represent hydrogen atoms R.sub.3 represents --C(CH.sub.3).dbd.CHCH(CH.sub.3)CH.sub.2 Ph.
These compounds inhibit the enzyme squalene synthase and/or are intermediates for the preparation of compounds which inhibit the enzyme squalene synthase. Compounds of the invention may be formulated for use in a variety of conditions where a lowering of the level of blood plasma cholesterol in animals would be beneficial and for use in combating fungal infections in animals.

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