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Cerilliant
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US Army
QuintilesIMS
Dow
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AstraZeneca
Novartis
Accenture

Generated: February 18, 2018

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Claims for Patent: 5,958,951

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Summary for Patent: 5,958,951
Title: Modified form of the R(-)-N-(4,4-di(3-methylthien-2-yl)but-3-enyl)-nipecotic acid hydrochloride
Abstract:The present invention provides R(-)-N-(4,4-di(3-methylthien-2-yl)but-3-enyl)-nipecotic acid hydrochloride in its pure and stable anhydrous form.
Inventor(s): Ahrndt; Preben (.O slashed.lstykke, DK), Petersen; Henning B.o slashed.rge (Lyngby, DK), Chang; Vincent H. (Lake Forest, IL), Allen; Kimberly Ann (Silver Lake, WI), Cain; Michael H. (Grayslake, IL)
Assignee: Novo Nordiskials (Bagsvoerd, DK)
Application Number:08/872,380
Patent Claims: 1. Anhydrous crystalline R(-)-N-(4,4-di(3-methylthien-2yl)but-3-enyl)nipecotic acid hydrochloride having substantially the following X-ray powder diffraction peaks obtained with KBr: 6.4, 11.3, 13.0, 13.9, 15.0, 18.7, 19.4, 22.5 and 23.7.

2. Anhydrous crystalline R(-)-N-(4,4-di(3-methylthien-2yl)but-3-enyl)nipecotic acid hydrochloride substantially free of bound organic solvent and having substantially the following X-ray powder diffraction peaks obtained with KBr: 6.4, 11.3, 13.0, 13.9, 15.0, 18.7, 19.4, 22.5 and 23.7.

3. A process for the preparation of anhydrous crystalline R(-)-N-(4,4-di(3-methylthien-2yl)but-3-enyl)nipecotic acid hydrochloride having substantially the following X-ray powder diffraction peaks obtained with KBr: 6.4, 11.3, 13.0, 13.9, 15.0, 18.7, 19.4, 22.5 and 23.7 which process comprises

a) dissolving tiagabine hydrochloride in an aqueous hydrochloric acid solution, and

b) precipitating tiagabine hydrochloride from the aqueous hydrochloric acid solution.

4. A pharmaceutical composition comprising a therapeutically effective amount of a crystalline salt according to claim 1 together with a pharmaceutically acceptable carrier or diluent.

5. The pharmaceutical composition according to claim 4 in the form of a dosage unit containing about 1.0-1500 mg of the active ingredients.

6. A method of inhibiting GABA uptake in a mammal in need of such treatment comprising administering an effective amount of a crystalline salt according to claim 1.

7. A method of inhibiting GABA uptake in a mammal in need of such treatment comprising administering a pharmaceutical composition according to claim 4.

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