Patent EA-004809-B1 (EA)
Title: 5-chloro-3-(4-methanesulfonylphenyl)-6'-methyl-[2,3']bipyridinyl in pure crystalline form and process for synthesis
Inventor: CROCKER LOUIS S
IPC: A61P25/00
Filed: 2001-05-22
Abstract: 1. A polymorphic form of the compound of formula A: A which is designated Form V. 2. The polymorphic form according to Claim 1 characterized as having an x-ray powder diffraction pattern peak position, Cu K alpha, at about 13.7 angstroms. 3. The polymorphic form according to Claim 2 further characterized as having at least one x-ray powder diffraction pattern peak position, CuK alpha, at about: 7.2, 6.9, 6.7, 5.8, 5.7, 5.0, 4.9, 4.8, 4.7, 4.5, 4.2, 4.0, 3.9, 3.8, 3.7, 3.6, 3.4, 3.3, 3.1, 3.0, 2.9 or 2.8 angstroms. 4. The polymorphic form according to Claim 1 characterized as having a DSC extrapolated onset melting temperature of about 133.9 degree C. 5. The polymorphic form according to Claim 1 characterized as having a DSC peak melting temperature of about 134.5 degree C. 6. The polymorphic form according to Claim 1 in substantially pure form. 7. A pharmaceutical composition comprising a non-toxic therapeutically effective amount of a polymorphic form according to Claim 1 and a pharmaceutically acceptable carrier. 8. A method of treating an inflammatory disease susceptible to treatment with an non-steroidal anti-inflammatory agent comprising administering to a patient in need of such treatment a non-toxic therapeutically effective amount of a polymorphic form according to Claim 1. 9. A method of treating a cyclooxygenase mediated disease advantageously treated by an active agent that selectively inhibits cyclooxygenase-2 in preference to cyclooxygenase-1 comprising administering to a patient in need of such treatment a non-toxic therapeutically effective amount of a polymorphic form according to Claim 1. 10. A method for treating an illness selected from the group consisting of: (a) rheumatic fever, (b) symptoms associated with influenza or other viral infections, common cold, (c) low back and neck pain, (d) dysmenorrhea, (e) headache, (f) toothache, (g) sprains and strains, (h) myositis, (i) neuralgia, (j) synovitis, (k) arthritis, including rheumatoid arthritis, degenerative joint diseases (osteoarthritis), gout andanlcylosing spondylitis, (1) bursitis, (m) burns, (n) injuries, and (o) following surgical and dental procedures, comprising administering to a patient in need of such treatment a non-toxic therapeutically effective amount of a polymorphic form according to Claim 1. 11. A process for making a Form V polymorph of structural formula A: comprising: combining polymorph I, II, III or IV of Compound A with isopropyl acetate; heating to an elevated temperature less than about 75 degree C; and cooling to a low temperature to produce the Form V polymorph. 12. The process according to Claim 11 further comprising isolating the Form V polymorph. 13. The process according to Claim 12 wherein isolating the Form V polymorph is by filtration. 14. The process according to Claim 11 wherein the elevated temperature is about 35-70 degree C. 15. The process according to Claim 14 wherein the elevated temperature is about 50-65 degree C. 16. The process according to Claim 11 wherein the low temperature is about 0-30 degree C. 17. The process according to Claim 16 wherein the low temperature is about 10-20 degree C. 18. The process according to Claim 11 wherein the elevated temperature is about 50-65 degree C and the low temperature is about 10-20 degree C.