Crystalline forms of a factor Xa inhibitor
AssigneeBristol-Myers Squibb Company
InventorsMichael Orwat, Mary Malley, Roxana Schlam, Steven Fabian, Bing-Shiou Yang, Victor Rosso
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Abstract
The instant invention provides crystalline forms of 3-(1-hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one and its solvates thereof; processes for the production of such crystalline forms; pharmaceutical compositions comprising such crystalline forms; and methods of treating thromboembolic disorders with such crystalline forms or such pharmaceutical compositions.
Claims29
Form N-1 of crystalline 3-(1-hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one, which is characterized by unit cell parameters substantially equal to the following:
- Cell dimensions:
- a=9.534(1) Å
- b=9.842(1) Å
- c=13.469(1) Å
- α=87.95(1)
- β=83.18(1)
- γ=70.22(1)
- Space group P-1
- Molecules/asymmetric unit 1
- wherein said crystalline form is at about +22° C.
Form N-3 of crystalline 3-(1-hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one, which is characterized by unit cell parameters substantially equal to the following:
- Cell dimensions:
- a=8.959(3) Å
- b=9.840(2) Å
- c=14.826(6) Å
- α=76.27(2)
- β=86.38(2)
- γ=69.18(2)
- Space group P-1
- Molecules/asymmetric unit 1
- wherein the crystalline form is at about +22° C.
Form H2-2 of crystalline 3-(1-hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one, which is characterized by unit cell parameters substantially equal to the following:
- Cell dimensions:
- a=16.445(2) Å
- b=17.319(1) Å
- c=18.997(2) Å
- α=71.65(1) (1)
- β=78.86(1)
- γ=87.78(1)
- Space group P-1
- Molecules/asymmetric unit 4
- wherein the crystalline form is at about −50° C.
Form DC-4 of crystalline 3-(1-hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one, which is characterized by unit cell parameters substantially equal to the following:
- Cell dimensions:
- a=8.951(2) Å
- b=9.789(3) Å
- c=17.263(4) Å
- α=69.30(2)
- β=83.24(2)
- γ=69.78(2)
- Space group P-1
- Molecules/asymmetric unit 1
- wherein the crystalline form is at about +22° C.
Form EGDA.5-5 of crystalline 3-(1-hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one, which is characterized by unit cell parameters substantially equal to the following:
- Cell dimensions:
- a=9.005(3) Å
- b=9.854(2) Å
- c=16.283(5) Å
- α=84.88(2)
- β=81.95(2)
- γ=68.19(1)
- Space group P-1
- Molecules/asymmetric unit 1
- wherein said crystalline form is at about +22° C.
A process for preparing crystalline forms of Compound (I), comprising a step of slurrying Compound (I) in a solvent selected from:
- polar aprotic solvents and polar protic solvents.
Dependencies are inferred from the claim text.