Crystalline forms of a bruton's tyrosine kinase inhibitor

Patent metadata

Field	Value
Publication number	US-2018155352-A1
Application number	US-201815887744-A
Country	US
Kind code	A1
Filing date	Feb 2, 2018
Priority date	Jun 4, 2012
Publication date	Jun 7, 2018
Grant date	—

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.

First claim

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.

Assignees

• Pharmacyclics Llc

Inventors

• Purro Norbert
• Smyth Mark S
• Goldman Erick
• Wirth David D

Classifications

• A61P39/00

  General protective or antinoxious agents · CPC title

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P37/02

  Immunomodulators · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title