Patent ID: 6414016
Filing Date: 2002-07-02
Classification: A61K,A61P,C07C,C07D,Y10S

Abstract:
A method for relieving or preventing constipation in a human constipated patient or cleansing a bowel of a patient which comprises administering to the patient a therapeutically effective amount of the pharmaceutical composition comprising in an amount sufficient for relieving or preventing constipation in a human constipated patient or cleansing a bowel of a human patient a bi-cyclic compound represented by formula (I): where V1 and V2 are carbon atoms;W1 and W2 are R3 and R4 are hydrogen atoms or one of them is OH; X1 and X2 are hydrogen, lower alkyl or halogen atom, and at least one of these is a halogen atom; Z is an oxygen atom; R2 is a hydrogen atom or alkyl; Y is a saturated or unsaturated C2-10 hydrocarbon chain which is unsubstituted or substituted by oxo, halogen, an alkyl group, hydroxyl or aryl; A is -CH2OH, -COCH2OH, -COOH or its functional derivative; and R1 is a saturated or unsaturated, lower hydrocarbon forming a straight-chain, a branched-chain or a ring, which is unsubstituted or substituted by halogen, oxo, hydroxy, lower alkoxy, lower alkanoyloxy, lower cycloalkyl, lower cycloalkyloxy, aryl, or aryloxy; lower cycloalkyl; lower cycloalkyloxy; aryl or aryloxy, a bond between C-13 and C-14 position can be a double or single bond, and C-15 can have a steric configuration of R, S, or a mixture thereof, and a compound which is a mono-cyclic tautomer of formula (I), wherein in the composition a ratio of the bi-cyclic compound to the mono-cyclic tautomer is at least 1:1.