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Serving leading biopharmaceutical companies globally:

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Generated: November 20, 2017

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Title: Crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl] benzenesulfonamide
Abstract:A stable crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide is described. This crystal structure, designated Form B, is more stable, has favorable handling properties and is characterized by its melting point, x-ray and other physical characterizations.
Inventor(s): Talley; John J (Brentwood, MO), Medich; John R (Curnee, IL), McLaughlin; Kathleen T (Arlington Heights, IL), Gaud; Henry T (Evanston, IL), Yonan; Edward E (Carol Stream, IL)
Assignee: G.D. Searle & Co. (Chicago, IL)
Filing Date:Dec 19, 2000
Application Number:09/741,213
Claims:1. A crystalline form of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide having a melting point of about 170-174.degree. C.

2. A form of claim 1 having an IR spectrum with the following peaks: 1170, 925, 844, and 729 cm.sup.-1.

3. A form of claim 1 having an IR spectrum without a significant peak at 723 cm.sup.-1.

4. A form of claim 1 having an x-ray powder diffraction pattern with the following peaks: 12.221, 15.447, 17.081, 19.798 and 23.861.

5. A pharmaceutical composition comprising a therapeutically-effective amount of crystalline Form B of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide in association with at least one pharmaceutically-acceptable carrier, adjuvant or diluent.

6. A method of treating a cyclooxygenase-2 associated disorder in a subject, said method comprising treating the subject having or susceptible to said disorder with a therapeutically-effective amount of the crystalline Form B of 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide.

7. The method of claim 6 for use in treatment of inflammation.

8. The method of claim 6 for use in treatment of arthritis.

9. The method of claim 6 for use in treatment of pain.

10. The method of claim 6 for use in treatment of fever.

11. A method of preparing crystals of claim 1 comprising dissolving 4-[5-methyl-3-phenylisoxazol-4-yl]benzenesulfonamide in an alcohol based solvent system form a solution and slowly cooling the solution.

12. The method of claim 11 wherein the solvent system comprises one or more solvents selected from methanol, isopropanol, aqueous methanol and aqueous ethanol.

13. The method of claim 11 wherein the crystals are recrystallized from a mixture of isopropanol and methanol.
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Serving leading biopharmaceutical companies globally:

Farmers Insurance
Merck
QuintilesIMS
Medtronic
Express Scripts
UBS
Fish and Richardson
Teva
Harvard Business School
Baxter

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