US2018155352A1PendingUtilityA1

Crystalline forms of a bruton's tyrosine kinase inhibitor

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Assignee: PHARMACYCLICS LLCPriority: Jun 4, 2012Filed: Feb 2, 2018Published: Jun 7, 2018
Est. expiryJun 4, 2032(~5.9 yrs left)· nominal 20-yr term from priority
A61P 39/00A61P 37/00A61P 43/00A61P 37/02A61P 3/10A61P 35/00A61P 7/06A61P 7/02A61P 9/00A61P 37/06A61P 35/02A61P 29/00A61P 27/02A61P 21/04A61P 19/08A61P 1/16A61P 13/12A61P 11/04A61P 17/00A61P 17/06A61P 11/02A61P 13/10A61P 15/02A61P 1/02A61P 15/00A61P 19/02A61P 11/00A61P 13/08A61P 1/00A61P 11/06A61K 9/4858C07D 487/04B65D 75/36A61K 9/2013A61J 1/035A61K 31/519A61K 9/2054C07B 2200/13A61K 45/06A61K 9/4866A61K 9/0053A61K 9/4825A61K 9/2018A61K 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

exact text as granted — not AI-modified
1 - 13 . (canceled) 
     
     
         14 . A crystalline form 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 that has an X-ray powder diffraction (XRPD) pattern comprising 2-Theta peaks at about 7.0°, about 14.0°, and about 18.2°. 
     
     
         15 . The crystalline form of  claim 14 , wherein the XRPD pattern further comprises a 2-Theta peak at about 15.7°. 
     
     
         16 . The crystalline form of  claim 15 , wherein the XRPD pattern further comprises a 2-Theta peak at about 19.1°. 
     
     
         17 . The crystalline form of  claim 16 , wherein the XRPD pattern further comprises a 2-Theta peak at about 19.5°. 
     
     
         18 . The crystalline form of  claim 17 , wherein the XRPD pattern further comprises a 2-Theta peak at about 20.3°. 
     
     
         19 . The crystalline form of  claim 18 , wherein the XRPD pattern further comprises a 2-Theta peak at about 22.10°. 
     
     
         20 . The crystalline form of  claim 19 , wherein the XRPD pattern further comprises a 2-Theta peak at about 22.9°. 
     
     
         21 . The crystalline form of  claim 14 , wherein the crystalline form is unsolvated. 
     
     
         22 . The crystalline form of  claim 15 , wherein the crystalline form is unsolvated. 
     
     
         23 . The crystalline form of  claim 16 , wherein the crystalline form is unsolvated. 
     
     
         24 . The crystalline form of  claim 17 , wherein the crystalline form is unsolvated. 
     
     
         25 . The crystalline form of  claim 18 , wherein the crystalline form is unsolvated. 
     
     
         26 . The crystalline form of  claim 19 , wherein the crystalline form is unsolvated. 
     
     
         27 . The crystalline form of  claim 20 , wherein the crystalline form is unsolvated.

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