Polymorphs of Acalabrutinib, a Bruton's tyrosine kinase inhibitor

Patent metadata

Field	Value
Publication number	US-12384784-B2
Application number	US-201917279235-A
Country	US
Kind code	B2
Filing date	Sep 24, 2019
Priority date	Sep 25, 2018
Publication date	Aug 12, 2025
Grant date	Aug 12, 2025

Abstract

The present invention discloses novel crystalline polymorphic forms of Acalabrutinib, methods of preparation, pharmaceutical compositions and methods of therapeutic treatment involving polymorphic forms thereof.

First claim

We claim:

1. A crystalline form of acalabrutinib, selected from:
crystalline form-C3 characterized by X-ray powder diffraction (XRPD) pattern peaks at 8.5, 10.0, 11.7, 12.9, 15.3, 17.9, 18.3, 20.1 and 21.6±0.2° 2Θ;
crystalline form-C4 characterized by X-ray powder diffraction (XRPD) pattern peaks at 8.3, 9.9, 12.1, 15.4, 15.9, 16.7, 19.9, 21.5, and 24.4±0.2° 2Θ; and
crystalline form-C5 characterized by X-ray powder diffraction (XRPD) pattern peaks at 7.7, 9.4, 10.8, 13.3, 15.4, 17.3, 22.0, and 23.1±0.2° 2Θ.

2. The crystalline form-C4 of claim 1 , wherein the crystalline form is characterized by a DSC substantially as depicted in FIG. 6 .

3. The crystalline form of claim 1 , wherein the crystalline form C4 contains less than 5% by weight total impurities.

4. The crystalline form of claim 1 , wherein the crystalline form C4 is at least 50% pure.

5. A pharmaceutical composition comprising one or more of a Form-C3, Form-C4 or Form-C5 of acalabrutinib and a pharmaceutically acceptable carrier.

6. The pharmaceutical composition of claim 5 , further comprising one or more pharmaceutically acceptable excipients.

Assignees

• Cipla Ltd

Inventors

• Malhotra Geena
• Pullela Venkata Srinivas
• Pathi Srinivas Laxminarayan
• Chennuru Ramanaiah
• Devarapalli Ramesh
• Mithun Ashok

Classifications

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• C07D487/04 Primary

  Ortho-condensed systems · CPC title