Novel choline cocrystal of epalrestat

A technology of co-crystallization and choline dihydrogen, which is applied in the direction of medical preparations containing active ingredients, metabolic diseases, extracellular fluid diseases, etc., can solve the problem that there is no way to predict the co-crystal characteristics of compounds, and it takes a lot of time, issues of effort and resources
CN102216281BInactive Publication Date: 2014-11-05BIONEVIA PHARMACEUTICALS INC
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
BIONEVIA PHARMACEUTICALS INC
Publication Date
2014-11-05
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a novel choline cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and / or prevent various conditions, including treating and / or preventing diabetic complications, treating and / or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients.
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Description

[0001] Cross References to Related Applications

[0002] Pursuant to 35 U.S.C. §119, this application claims priority to US Provisional Application US 61 / 094,904, filed September 6, 2008, which is incorporated herein by reference. technical field

[0003] The present invention relates to novel choline cocrystals of 5-[(1Z,2E)-2-methyl-3-phenylpropenylene]-4-oxo-2-thioxo-3-thiazolidineacetic acid, such The preparation method of the new co-crystal, the pharmaceutical composition containing the new choline co-crystal and the method of treating and / or preventing various diseases by administering the new choline co-crystal. Background technique

[0004] The common name of the compound 5-[(1Z,2E)-2-methyl-3-phenylpropenylene]-4-oxo-2-thio-3-thiazolidineacetic acid (shown below) is "according to parerestat", which is an active pharmaceutical ingredient ("API") known to have beneficial therapeutic activity, for example as an aldose reductase inhibitor:

[0005]

[0006] The pre...

Claims

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