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US 6,583,174 B1Granted
Composition and method for stabilizing the same
AssigneeSucampo AG
InventorsRyuji Ueno, Tsuyoshi Habe
Life of this patent
Estimating the term…
Abstract
Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.
Claims25
A composition comprising a bi-cyclic compound represented by the formula (I):
- wherein,
- A is —CH2OH, —COCH2OH, —COOH or a functional derivative thereof,
- X1 and X2 are hydrogen atom, lower alkyl or halogen atom;
- V1 and V2 are carbon atoms;
- W1 and W2 are
- wherein R4 and R5 are hydrogen atom, hydroxy, halogen atom, lower alkyl, lower alkoxy or hydroxy (lower) alkyl with the proviso that R4 and R5 are not hydroxy or lower alkoxy at the same time;
- Z is an oxygen atom;
- R1 is a saturated or unsaturated bivalent lower-medium aliphatic hydrocarbon residue which is unsubstituted or substituted with halogen atom, an alkyl group, hydroxy, oxo, aryl or heterocyclic group;
- R2 is a saturated or unsaturated, lower or medium aliphatic hydrocarbon residue which is unsubstituted or substituted with halogen atom, oxo, hydroxy, lower alkyl, lower alkoxy, lower alkanoyloxy, lower cycloalkyl, lower cycloalkyloxy, aryl, aryloxy, heterocyclic group or heterocyclic-oxy group;
- lower cycloalkyl;
- lower cycloalkyloxy;
- aryl, aryloxy, heterocyclic group or heterocyclic-oxy group;
- R3 is a hydrogen atom, a lower alkyl, lower cycloalkyl, aryl or heterocyclic group, and a glyceride, in which the bi-cyclic compound is present in a ratio of at least 50:50 with respect to its tautomeric monocyclic compound.
10 more elements
A method for stabilizing a bi-cyclic compound represented by the formula (I):
- wherein,
- A is —CH2OH, —COCH2OH, —COOH or a functional derivative thereof,
- X1 and X2 are hydrogen atom, lower alkyl or halogen atom;
- V1 and V2 are carbon atoms;
- W1 and W2 are
- wherein R4 and R5 are hydrogen atom, hydroxy, halogen atom, lower alkyl, lower alkoxy or hydroxy (lower) alkyl with the proviso that R4 and R5 are not hydroxy or lower alkoxy at the same time;
- Z is an oxygen atom;
- R1 is a saturated or unsaturated bivalent lower-medium aliphatic hydrocarbon residue which is unsubstituted or substituted with halogen atom, an alkyl group hydroxy, oxo, aryl or heteroyclic group;
- R2 is a saturated or unsaturated, lower or medium aliphatic hydrocarbon residue which is unsubstituted or substituted with halogen atom, oxo, hydroxy, lower alkyl, lower alkoxy, lower alkanoyloxy, lower cycloalkyl, lower cycloalkyloxy, aryl, aryloxy, heterocyclic group or heterocyclic-oxy group;
- lower cycloalkyl;
- lower cycloalkyloxy;
- aryl, aryloxy, heterocyclic group or heterocyclic-oxy group;
- R3 is a hydrogen atom, a lower alkyl, lower cycloalkyl, aryl or heterocyclic group, comprising the step of admixing the same with a glyceride.
10 more elements
Dependencies are inferred from the claim text.