JAK inhibitors having a specific particle size distribution
AssigneeElanco US Inc.
InventorStephen Stirm
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Abstract
The present disclosure provides compositions of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(cyclopropylsulfonyl)azetidin-3-yl)acetonitrile having a specific acceptance value and/or particle size distribution, pharmaceutical compositions comprising the same, methods of using the same, and processes for making the same.
Claims16
A tablet comprising substantially polymorphically pure crystalline 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(cyclopropylsulfonyl) azetidin-3-yl)acetonitrile, wherein the tablet has an Acceptance Value of 5 or lower,
- wherein the polymorphically pure crystalline 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(cyclopropylsulfonyl) azetidin-3-yl)acetonitrile is in the form of particles having a particle size distribution characterized by d50 of 15-30 μm, a d90 of 50-80 μm, a dv90 of ≤80 μm, and a dv50 of ≤30 μm, and
- wherein the substantially polymorphically pure crystalline 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(cyclopropylsulfonyl) azetidin-3-yl)acetonitrile is characterized by the X-ray powder diffraction pattern comprising a peak at 5.34°, 10.68°, 14.26°, 16.06°, 16.39°, 16.48°, 18.26°, 18.65°, 21.05°, 21.76°, 22.68°, or 26.75° (±0.2° 2θ).
A composition comprising particles of substantially polymorphically pure crystalline 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(cyclopropylsulfonyl) azetidin-3-yl)acetonitrile, wherein the particles have a particle size distribution characterized by d50 of 15-30 μm, a d90 of 50-80 μm, a dv90 of ≤80 μm, and a dv50 of ≤30 μm, wherein the substantially polymorphically pure crystalline 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(cyclopropylsulfonyl) azetidin-3-yl)acetonitrile is characterized by the X-ray powder diffraction pattern comprising a peak at 5.34°, 10.68°, 14.26°, 16.06°, 16.39°, 16.48° 18.26°, 18.65°, 21.05°, 21.76°, 22.68°, or 26.75° (±0.2° 2θ).
Dependencies are inferred from the claim text.