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Details for Patent: 5,362,730

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Details for Patent: 5,362,730

Title: Terazosin polymorph and pharmaceutical composition
Abstract:A process for preparing a novel anhydrous crystalline polymorph of anhydrous 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl) piperazine monohydrochloride comprises contacting the known amorphous, crystalline dihydrate, or crystalline anhydrous form I of the compound with a polar organic solvent.
Inventor(s): Bauer; John F. (Lake Bluff, IL), Morley; James A. (Gurnee, IL)
Assignee: Abbott Laboratories (Abbott Park, IL)
Filing Date:Jan 06, 1994
Application Number:08/178,184
Claims:1. A process for the preparation of anhydrous crystalline 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride form II which comprises contacting a material selected from the group consisting of

crystalline 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride dihydrate,

crystalline 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride anhydrate form I, and

amorphous 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride

with an anhydrous polar organic solvent selected from the group consisting of alcohols of one to six carbon atoms, ketones of three to six carbon atoms, and mixtures thereof, followed by removal of the solvent to recover the solid product.

2. The process of claim 1 wherein the step of contacting said material with a polar organic solvent comprises heating crystalline 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride dihydrate under reflux in said solvent.

3. The process of claim 1 wherein the step of contacting said material with a polar organic solvent comprises dissolving said material in said solvent and precipitating the solid product from the resulting solution.

4. The process of claims 1-3 where said organic solvent is selected from the group consisting of C.sub.1 -C.sub.6 alcohols, C.sub.3 -C.sub.6 ketones and mixtures thereof.

5. The anhydrous crystalline polymorph of 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride which is the product of heating 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride dihydrate under reflux in a solvent selected from the group consisting of C.sub.1 -C.sub.6 alcohols, C.sub.3 -C.sub.6 ketones and mixtures thereof, followed by removal of the solvent.

6. The anhydrous crystalline polymorph of 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride which is the product of recrystallizing amorphous 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride dihydrate from a solvent selected from the group consisting of C.sub.1 -C.sub.6 alcohols and C.sub.3 -C.sub.6 ketones and mixtures thereof.

7. The anhydrous crystalline polymorph of 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride which is the product of recrystallizing 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride form I from a solvent selected from the group consisting of C.sub.1 -C.sub.6 alcohols and C.sub.3 -C.sub.6 ketones and mixtures thereof.

8. The anhydrous crystalline polymorph of 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride which is the product of recrystallizing amorphous 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride from a solvent selected from the group consisting of C.sub.1 -C.sub.6 alcohols and C.sub.3 -C.sub.6 ketones and mixtures thereof.

9. A pharmaceutical formulation useful for the treatment of hypertension, benign prostatic hyperplasia or congestive heart failure comprising a therapeutically effective amount of the product of claim 5 in combination with a pharmaceutically acceptable carrier.

10. A pharmaceutical formulation useful for the treatment of hypertension, benign prostatic hyperplasia or congestive heart failure comprising a therapeutically effective amount of the product of claim 6 in combination with a pharmaceutically acceptable carrier.

11. A pharmaceutical formulation useful for the treatment of hypertension, benign prostatic hyperplasia or congestive heart failure comprising a therapeutically effective amount of the product of claim 7 in combination with a pharmaceutically acceptable carrier.

12. A pharmaceutical formulation useful for the treatment of hypertension, benign prostatic hyperplasia or congestive heart failure comprising a therapeutically effective amount of the product of claim 8 in combination with a pharmaceutically acceptable carrier.

13. The anhydrous crystalline polymorph of 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride which is the product of contacting a material selected from the group consisting of

crystalline 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride dihydrate,

crystalline 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride anhydrate form I, and

amorphous 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine monohydrochloride

with an anhydrous polar organic solvent selected from the group consisting of alcohols of one to six carbon atoms, ketones of three to six carbon atoms, and mixtures thereof, followed by removal of the solvent to recover the solid product.
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