Pharmaceutical composition comprising a crystal form of (S)-4-(8-amino-3-(1-(but-2-ynoyl) pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide
DC
First Claim
1. A solid pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and 95-105 mg of a crystal form of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide characterized by a reflection X-ray powder diffraction pattern comprising peaks at 6.4°
- ±
0.2°
2θ
, 8.6°
±
0.2°
2θ
, 10.5°
±
0.2°
2θ
, 11.6°
±
0.2°
2θ and
15.7°
±
0.2°
2θ
.
1 Assignment
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Accused Products
Abstract
In some embodiments, the invention relates to crystalline solid forms, including hydrates, polymorphs, and salt forms, of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention relates to amorphous solid forms of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention also relates to pharmaceutical compositions containing the solid forms, and methods for treating conditions or disorders by administering to a subject a pharmaceutical composition that includes the forms, including pharmaceutical compositions and methods for overcoming the effects of acid reducing agents.
19 Citations
28 Claims
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1. A solid pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and 95-105 mg of a crystal form of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide characterized by a reflection X-ray powder diffraction pattern comprising peaks at 6.4°
- ±
0.2°
2θ
, 8.6°
±
0.2°
2θ
, 10.5°
±
0.2°
2θ
, 11.6°
±
0.2°
2θ and
15.7°
±
0.2°
2θ
. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13)
- ±
-
14. A method for inhibiting Bruton'"'"'s tyrosine kinase activity in a human, comprising orally administering to said human twice daily a solid pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and 95-105 mg of a crystal form of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide characterized by a reflection X-ray powder diffraction pattern comprising peaks at 6.4°
- ±
0.2°
2θ
, 8.6°
±
0.2°
2θ
, 10.5°
±
0.2°
2θ
, 11.6°
±
0.2°
2θ and
15.7°
±
0.2°
2θ
. - View Dependent Claims (15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28)
- ±
Specification
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- Resources
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Current AssigneeAcerta Pharma B.V. (Astrazeneca PLC)
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Original AssigneeAcerta Pharma B.V. (Astrazeneca PLC)
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InventorsBlatter, Fritz, Ingallinera, Tim, Barf, Tjeerd, Aret, Edwin, Krejsa, Cecile, Evarts, Jerry
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Primary Examiner(s)Willis, Douglas M
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Application NumberUS15/707,508Publication NumberTime in Patent Office470 DaysField of Search514249, 544350US Class CurrentCPC Class CodesA61K 31/4985 Pyrazines or piperazines or...A61K 45/06 Mixtures of active ingredie...A61K 47/36 Polysaccharides; Derivative...A61P 1/04 for ulcers, gastritis or re...A61P 13/08 of the prostateA61P 13/12 of the kidneysA61P 17/00 Drugs for dermatological di...A61P 17/04 AntipruriticsA61P 17/06 AntipsoriaticsA61P 19/00 Drugs for skeletal disordersA61P 19/02 for joint disorders, e.g. a...A61P 21/00 Drugs for disorders of the ...A61P 27/02 Ophthalmic agentsA61P 29/00 Non-central analgesic, anti...A61P 3/10 for hyperglycaemia, e.g. an...A61P 31/04 Antibacterial agentsA61P 31/18 for HIVA61P 35/00 Antineoplastic agentsA61P 35/02 specific for leukemiaA61P 37/02 ImmunomodulatorsView All
