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Last Updated: December 19, 2025

Claims for Patent: 9,487,525

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Summary for Patent: 9,487,525

Title:	Crystalline forms of (s)-4-amino-n-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7h-pyrrolo[2,3-d]pyrimidin-4-yl) piperidine-4-carboxamide
Abstract:	The present invention discloses certain new solid state forms of (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, processes for preparing such forms, pharmaceutical compositions comprising them, and the use of such forms in therapy.
Inventor(s):	Gary Peter Tomkinson
Assignee:	AstraZeneca AB
Application Number:	US14/394,918
Patent Claims:	1. (S)-4-Amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]-pyrimidin-4-yl)piperidine-4-carboxamide crystalline Form B which is characterized by an X-ray powder diffraction pattern with peaks at about 2-theta=10.0, 12.3, 15.0, 17.1, 19.2 and 24.4°. 2. (S)-4-Amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]-pyrimidin-4-yl)piperidine-4-carboxamide crystalline Form B which is characterized by an X-ray powder diffraction pattern with at least ten peaks at about 2-theta=15.0, 19.2, 12.3, 10.0, 17.1, 24.4, 16.4, 26.0, 15.5, and 23.9°. 3. (S)-4-Amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]-pyrimidin-4-yl)piperidine-4-carboxamide crystalline Form B which is characterized by an X-ray powder diffraction pattern with at least ten peaks at about 2-theta=10.0, 5.0, 15.0, 19.2, 17.1, 12.3, 24.4, 30.2, 32.3, and 23.3°. 4. A pharmaceutical composition comprising (S)-4-Amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]-pyrimidin-4-yl)piperidine-4-carboxamide crystalline Form B, according to claim 1, in association with and a pharmaceutically-acceptable diluent or carrier. 5. A pharmaceutical composition comprising (S)-4-Amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]-pyrimidin-4-yl)piperidine-4-carboxamide crystalline Form B, according to claim 2, in association with and a pharmaceutically-acceptable diluent or carrier. 6. A pharmaceutical composition comprising (S)-4-Amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]-pyrimidin-4-yl)piperidine-4-carboxamide crystalline Form B, according to claim 3, in association with and a pharmaceutically-acceptable diluent or carrier. 7. The pharmaceutical composition according to claim 4, further comprising microcrystalline cellulose, mannitol, croscarmellose sodium and magnesium stearate. 8. The pharmaceutical composition according to claim 5, further comprising microcrystalline cellulose, mannitol, croscarmellose sodium and magnesium stearate. 9. The pharmaceutical composition according to claim 6, further comprising microcrystalline cellulose, mannitol, croscarmellose sodium and magnesium stearate. 10. A pharmaceutical tablet comprising from 0.5 to 2% by weight of magnesium stearate, from 2 to 5% by weight of croscarmellose sodium, from 15 to 60% by weight of crystalline Form B according to claim 1, microcrystalline cellulose and mannitol, wherein the relative weights of microcrystalline cellulose and mannitol within the tablet are in a ratio of from 3:1 to 1:1, and wherein the amount of crystalline Form B within the tablet is from 50 to 500 mg. 11. A pharmaceutical tablet comprising from 0.5 to 2% by weight of magnesium stearate, from 2 to 5% by weight of croscarmellose sodium, from 15 to 60% by weight of crystalline Form B according to claim 2, microcrystalline cellulose and mannitol, wherein the relative weights of microcrystalline cellulose and mannitol within the tablet are in a ratio of from 3:1 to 1:1, and wherein the amount of crystalline Form B within the tablet is from 50 to 500 mg. 12. A pharmaceutical tablet comprising from 0.5 to 2% by weight of magnesium stearate, from 2 to 5% by weight of croscarmellose sodium, from 15 to 60% by weight of crystalline Form B according to claim 3, microcrystalline cellulose and mannitol, wherein the relative weights of microcrystalline cellulose and mannitol within the tablet are in a ratio of from 3:1 to 1:1, and wherein the amount of crystalline Form B within the tablet is from 50 to 500 mg.

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