Phosphorus-containing isoprenoid derivatives

C - Chemistry – Metallurgy – 07 – F

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C07F 9/38 (2006.01) A61K 31/66 (2006.01) C07C 211/21 (2006.01) C07C 233/03 (2006.01) C07F 9/40 (2006.01) C07F 9/547 (2006.01)

Patent

CA 2115849

ABSTRACT The present invention provides a phosphorus- containing isoprenoid derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is useful as a preventive and therapeutic agent for diseases for which a squalene synthetase inhibiting action is efficacious: Image (I) wherein R1 and R2 each represent a hydrogen atom, a lower alkyl, cycloalkyl, alkenyl or alkynyl group, an aryl group which may be substituted, an arylalkyl group in which the aryl group may be substituted, or a heteroaryl or heteroarylalkyl group; R3 and R4 each represent a hydrogen atom, a lower alkyl group or an alkali metal; Y represents a group represented by the formula: Image (wherein R5 and R6 each represent a hydrogen atom, a lower alkyl group or an alkali metal or a group represented by the formula: - 82 - -CO2R7 (wherein R7 represents a hydrogen atom, a lower alkyl group or an alkali metal); Z represents a group represented by the formula: -(CH2)m- (wherein m is an integer of 0 to 3), a group represented by the formula: -(CH2)p-CH=CH-(CH2)q- (wherein p is 0 or 1 and q is 1 or 2) or a group represented by the formula: Image (wherein R8 represents a hydrogen atom or a lower alkyl group; A represents an alkylene chain which has 1 to 5 carbon atoms and which may have a substituent on each carbon atom; and r is zero or an integer of 1 to 5); and n is zero or an integer of 1 to 5. - 83 -

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