Anti-constipation composition
AssigneeSucampo AG
InventorRyuji Ueno
Life of this patent
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Abstract
An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation without substantive side-effects, such as stomachache.
Claims11
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 a sulfur atom;
- R2 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 is a double or single bond, and
- C-15 has a steric configuration of R, S, or a mixture thereof.
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 a hi-cyclic compound represented by the following 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 a sulfur 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 is a double or single bond,
- C-15 has can have a steric configuration of R, S, or a mixture thereof, and medium chain fatty acid triglyceride.
Dependencies are inferred from the claim text.