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Claims for Patent: 5,354,760

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Claims for Patent: 5,354,760

Title: Crystalline Tiagabine monohydrate, its preparation and use
Abstract:The invention provides crystalline Tiagabine hydrochloride monohydrate, process for its preparation, compositions containing the same and its therapeutic use as anti-epileptic agent.
Inventor(s): Petersen; Henning (Lyngby, DK), Nielsen; Peter (Herlev, DK), Cain; Michael (Grayslake, IL), Patel; Subhash (Chicago, IL)
Assignee: Novo Nordisk A/S (Bagsvaerd, DK)
Application Number:07/857,038
Patent Claims: 1. Crystalline R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride monohydrate having a differential scanning calorimetry profile with an onset from about 80.8.degree. C. to about 83.0.degree. C.

2. Crystalline R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride monohydrate, having substantially the same X-ray diffractogram as set out in FIG. 1 and substantially the same IR spectrum, in KBr, as set out in FIG. 3.

3. A process for the preparation of crystalline R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3enyl)nipecotic acid hydrochloride monohydrate, which process comprises forming an aqueous solution of R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride and crystallizing said R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride monohydrate from solution by precipitation or recrystallization from water.

4. A process for the preparation of crystalline R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride monohydrate comprising acid catalyzed hydrolysis of the ethyl ester of R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride in an aqueous solution followed by crystallization of R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride monohydrate from the aqueous solution by precipitation or recrystallization from water.

5. A pharmaceutical composition comprising an effective anti-epileptic amount of crystalline R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride monohydrate having a differential scanning calorimetry profile with an onset from about 80.8.degree. C. to about 83.0.degree. C. together with a pharmaceutically acceptable carrier or diluent.

6. The pharmaceutical composition according to claim 5 in the form of an oral dosage unit containing from 1 to 200 mg of R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride monohydrate having a differential scanning calorimetry profile with an onset from about 80.8.degree. C. to about 83.0.degree. C.

7. A pharmaceutical composition comprising an effective anti-epileptic amount of crystalline R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride monohydrate having substantially the same X-ray diffractogram as set out in FIG. 1 and substantially the same IR spectrum, in KBr, as set out in FIG. 3 together with a pharmaceutically acceptable carrier or diluent.

8. A method of treating epilepsy in a mammal comprising administering to the mammal an effective amount of crystalline R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride monohydrate having a differential scanning calorimetry profile with an onset from about 80.8.degree. C. to about 83.0.degree. C.

9. A method of treating epilepsy in a mammal comprising administering to the mammal a pharmaceutical composition comprising an effective anti-epileptic amount of crystalline R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride monohydrate having a differential scanning calorimetry profile with an onset from about 80.8.degree. C. to about 83.0.degree. C. together with a pharmaceutically acceptable carrier or diluent.

10. A method of treating epilepsy in a mammal comprising administering to the mammal an effective amount of crystalline R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride monohydrate having substantially the same X-ray diffractogram as set out in FIG. 1 and substantially the same IR spectrum, in KBr, as set out in FIG. 3.

11. A method of treating epilepsy in a mammal comprising administering to the mammal a pharmaceutical composition comprising an effective anti-epileptic amount of crystalline R(-)-N-(4,4-di(3-methylthien-2-yl)-but-3-enyl)nipecotic acid hydrochloride monohydrate having substantially the same X-ray diffractogram as set out in FIG. 1 and substantially the same IR spectrum, in KBr, as set out in FIG. 3 together with a pharmaceutically acceptable carrier or diluent.
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