US2019248799A1PendingUtilityA1

Crystalline forms of a bruton's tyrosine kinase inhibitor

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Assignee: PHARMACYCLICS LLCPriority: Jun 4, 2012Filed: Apr 24, 2019Published: Aug 15, 2019
Est. expiryJun 4, 2032(~5.9 yrs left)· nominal 20-yr term from priority
A61P 39/00A61P 7/06A61P 43/00A61P 37/02A61P 37/00A61P 37/06A61P 3/10A61P 35/00A61P 7/02A61P 35/02A61P 9/00A61P 29/00A61P 27/02A61P 19/02A61P 1/16A61P 1/02A61P 11/02A61P 17/06A61P 1/00A61P 15/00A61P 11/06A61P 11/04A61P 21/04A61P 15/02A61P 13/10A61P 17/00A61P 13/08A61P 13/12A61P 19/08A61P 11/00A61K 45/06A61K 9/2013C07D 487/04A61K 31/519A61K 9/4858B65D 75/36A61K 9/2054A61K 9/4866A61K 9/2018C07B 2200/13A61J 1/035A61K 9/0053A61K 9/4825A61K 2300/00
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Claims

Abstract

Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Claims

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1 - 13 . (canceled) 
     
     
         14 . A pharmaceutical formulation for oral administration comprising:
 (a) about 40 mg to about 200 mg of 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one;   (b) about 40 wt % to about 50 wt % of one or more diluents; and   (c) about 0.2 wt % to about 1.0 wt % of one or more lubricants.

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