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Claims for Patent: 6,414,016

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Claims for Patent: 6,414,016

Title: Anti-constipation composition
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): ##STR1## where X.sub.1 and X.sub.2 are preferably both fluorine atoms. The composition can be used to treat constipation without substantive side-effects, such as stomachache.
Inventor(s): Ueno; Ryuji (Potomac, MD)
Assignee: Sucampo, A.G. (Zurich, GH)
Application Number:09/655,760
Patent Claims: 1. 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): ##STR28##

where V.sub.1 and V.sub.2 are carbon atoms;

W.sub.1 and W.sub.2 are ##STR29##

R.sub.3 and R.sub.4 are hydrogen atoms or one of them is OH;

X.sub.1 and X.sub.2 are hydrogen, lower alkyl or halogen atom, and at least one of these is a halogen atom;

Z is an oxygen atom;

R.sub.2 is a hydrogen atom or alkyl;

Y is a saturated or unsaturated C.sub.2-10 hydrocarbon chain which is unsubstituted or substituted by oxo, halogen, an alkyl group, hydroxyl or aryl;

A is -CH.sub.2 OH, -COCH.sub.2 OH, -COOH or its functional derivative; and

R.sub.1 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.

2. 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 bi-cyclic compound represented by the following Formula (I); ##STR30##

where V.sub.1 and V.sub.2 are carbon atoms;

W.sub.1 and W.sub.2 are ##STR31##

R.sub.3 and R.sub.4 are hydrogen atoms or one of them is OH;

X.sub.1 and X.sub.2 are hydrogen, lower alkyl or halogen atom, and at least one of these is a halogen atom;

Z is an oxygen atom;

R.sub.2 is a hydrogen atom or alkyl;

Y is a saturated or unsaturated C.sub.2-10 hydrocarbon chain which is unsubstituted or substituted by oxo, halogen, an alkyl group, hydroxyl or aryl;

A is -CH.sub.2 OH, -COCH.sub.2 OH, -COOH or its functional derivative; and

R.sub.1 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,

C-15 can have a steric configuration of R, S, or a mixture thereof,

a compound which is a mono-cyclic tautomer of formula (I);

and a medium chain fatty acid triglyceride,

wherein in the composition a ratio of the bi-cyclic compound to the monocyclic tautomer is at least 1:1.

3. The method according to claim 1, wherein in the composition a ratio of bi-cyclic/mono-cyclic structure is at least 20:1.

4. The method according to claim 1, wherein A is -COOH, W.sub.1 is a ketone, R.sub.2 is a hydrogen atom, and X.sub.1 and X.sub.2 are fluorine atoms.

5. The method according to claim 1, wherein A is COOH; Y is (CH.sub.2).sub.6 ; W.sub.1 is .dbd.O; R.sub.3 and R.sub.4 are hydrogen atoms; X.sub.1 and X.sub.2 are fluorine atoms; and R.sub.1 is (CH.sub.2).sub.3 CH.sub.3.

6. The method according to claims 2, wherein the ratio of bi-cyclic/mono-cyclic structure is at least 20:1.

7. The method according to claim 2, wherein A is -COOH, W.sub.1 is a ketone, and X.sub.1 and X.sub.2 are fluorine atoms.

8. The method according to claim 2, wherein A is COOH; Y is (CH.sub.2).sub.6 ; W.sub.1 is .dbd.O; R.sub.3 and R.sub.4 are hydrogen atoms; X.sub.1 and X.sub.2 are fluorine atoms; and R.sub.1 is (CH.sub.2).sub.3 CH.sub.3.

9. The method according to claim 2, wherein the medium chain fatty acid triglyceride is present in an amount of 1-1,000,000 parts by weight based on one part by weight of the bi-cyclic structure.

10. The method according to claim 9, wherein the medium chain fatty acid triglyceride is present in an amount of 5-500,000 parts by weight based on one part by weight of the bi-cyclic structure.

11. The method according to claim 9, wherein the medium chain fatty acid triglyceride is present in an amount of 10-200,000 parts by weight based on one part by weight of the bi-cyclic structure.

12. The method according to claim 2, wherein the medium chain fatty acid triglyceride is a triglyceride of a fatty acid having 6-14 carbon atoms.

13. The method according to claim 2, wherein the medium chain fatty acid triglyceride is caprylic acid triglyceride and/or capric triglyceride.
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