IP Library › Patent Application 11550891
Patent Application
App. No. 11/550,891

POLYMORPHIC FORMS OF METHYL (+)-(S) - ALPHA - (2-CHLOROPHENYL)-6, 7-DIHYDROTHIENO [3,2-C]PYRIDINE-5(4H) ACETATE HYDROBROMIDE, CLOPIDOGREL HYDROBROMIDE

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Patent No.
US None
App. No.
11/550,891
Abstract

The invention relates to polymorphic Forms B, C, and D of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide, to pharmaceutical compositions containing the same, and to the method of use thereof for inhibiting platelet aggregation.

Claims (21)

1 . Polymorphic Form B of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide.

2 . Polymorphic Form B of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 1 having an X-ray powder diffraction pattern with a peak at about 20.9 degrees two-theta.

3 . Polymorphic Form B of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 1 having an X-ray powder diffraction pattern with peaks at about 10.4, 14.2, 19.5 and 20.9 degrees two-theta.

4 . Polymorphic Form B of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 1 having an FTIR spectrum with peaks at about 537, 800, 1758, 3488, and 3949 cm −1 .

5 . Polymorphic Form B of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 1 having a melting point of about 140-143° C.

6 . Polymorphic Form B of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 1 having an X-ray powder diffraction pattern substantially as depicted in FIG. 1B .

7 . Polymorphic Form B of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 1 having an FTIR spectrum substantially as depicted in FIG. 3 .

8 . Polymorphic Form C of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide.

9 . Polymorphic Form C of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 8 having an X-ray powder diffraction pattern with a peak at about 22.0 degrees two-theta.

10 . Polymorphic Form C of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 8 having an X-ray powder diffraction pattern with peaks at about 20.6, 22.0, 28.1, and 31.7 degrees two-theta.

11 . Polymorphic Form C of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 8 having an FTIR spectrum with peaks at about 534, 789, 1753, 3639, 3657 and 3959 cm −1 .

12 . Polymorphic Form C of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 8 having a melting point of about 138-148° C.

13 . Polymorphic Form C of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 8 having an X-ray powder diffraction pattern substantially as depicted in FIG. 1C .

14 . Polymorphic Form C of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 8 having an FTIR spectrum substantially as depicted in FIG. 4 .

15 . Polymorphic Form D of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide.

16 . Polymorphic Form D of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 15 having an FTIR spectrum with peaks at about 456, 723, 756, 1647, and 1748 cm −1 .

17 . Polymorphic Form D of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 15 having an X-ray powder diffraction pattern substantially as depicted in FIG. 1D .

18 . Polymorphic Form D of methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate hydrobromide according to claim 15 having an FTIR spectrum substantially as depicted in FIG. 5 .

19 . A pharmaceutical composition comprising a compound according to claim 1 together with a pharmaceutically acceptable carrier, adjuvant, diluent, or vehicle.

20 . A method for inhibiting platelet aggregation which comprises administering to a patient in need thereof an effective amount of a compound according to claim 1 .

21 . A method of reducing atherosclerotic events which comprises administering to a patient in need thereof an effective amount of a compound according to claim 1.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 1, 2007
From: LORIMER, KEITH RICHARD; FUAY NG, ALICIA TEE
To: SANOFI-AVENTIS
Reel/Frame 018945/0121 →