Cyclic ketal derivatives

Details Cyclic ketal derivatives Cyclic ketal derivatives

C - Chemistry, Metallurgy

07

H

C07H 19/01 (2006.01) A61K 31/34 (2006.01) A61K 31/70 (2006.01) C07D 493/08 (2006.01) C07H 9/04 (2006.01)

Patent

CA 2131010

2131010 9318040 PCTABS00025 Compounds are described of formula (I), wherein R1 represents a hydroxyl group or a group selected from -OCOCH=ECHCH(CH3)(CH2)3CH3, -OCOCH=ECHC(CH3)=ECHCH(CH3)CH2CH3 or -OCO-X-CH2CH(CH3)CH2CH3 [where X is -CH=ECHCH(CH3)-, -CH2CH(OH)CH(CH3)-, -CH=ECHC(OH)(CH3)-, -CH2CH(OH)CH2- or -CH2CH2CH(CH3)-]; R2 represents a hydroxyl group; R3 represents a group selected from (1) (where R7 is a hydrogen atom or an acetyl group), -C(CH3)=ECHCH(CH2R8)CH2Ph (where R8 is a hydrogen or a hydroxyl group), -C(CH2OH)=ZCHCH(CH3)CH2Ph, -C(=CH2)CH(OH)CH(CH2OH)CH2Ph, -C(=CH2)CH(NHCOCH3)CH(CH3)CH2Ph, -C(CH2NHCOCH3)=ECHCH(CH3)CH2Ph and (2); R4 and R5 may each independently represent a hydrogen atom or a methyl group; R6 represents a tetrazole ring linked via the ring carbon atom to the rest of the molecule and optionally substituted at one of the ring nitrogen atoms by a C1-4alkyl group; and salts thereof. 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 inventions 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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