US 2019/0375755 A1 · CRYSTAL FORM OF ACP-196 SALT AND PREPARATION METHOD, PHARMACEUTICAL COMPOSITION, AND USE THEREOF

Abstract

The present invention relates to novel crystalline forms of ACP-196 (acalabrutinib) salts, compared with the known solid form of ACP-196, the crystalline forms of ACP-196 salts of the present invention have advantages in crystallinity, solubility and hygroscopicity. The present invention also relates to the preparation methods for the preparation of the crystalline forms of ACP-196 salts, pharmaceutical compositions thereof and their uses in the preparation of methods for treating and/or preventing diseases mediated by Bruton tyrosine kinase (BTK), such as autoimmune diseases or disorders, xenoimmune diseases or disorders, cancer, including lymphoma and inflammatory diseases or disorders.

Claims23

Dependent claims

1-24. (canceled)

ACP-196 malate Form 1 having the structure shown in the formula (I) below,

wherein, measured using Cu-Kα radiation, the X-ray powder diffraction pattern of the ACP-196 malate Form 1, expressed as 2θ angles, has the following characteristic peaks:
6.2°±0.2°, 8.9°±0.2°, 12.0°±0.2°, 12.4°±0.2°, 16.9°±0.2° and 22.9°±0.2°.

ACP-196 sulfate Form 1 having the structure shown in the formula (V) below,

wherein, measured using Cu-Kα radiation, the X-ray powder diffraction pattern of the ACP-196 sulfate Form 1, expressed as 2θ angles, has the following characteristic peaks:
8.9°±0.2°, 9.7°±0.2°, 17.5°±0.2°, 19.6°±0.2°, 21.9°±0.2° and 23.6°±0.2°.

Dependencies are inferred from the claim text.

Facts

Application

16/487,324Filed 20 Feb 2017

Published

12 Dec 2019

Term ends

Not estimatedThe source records don’t support an estimate.

Classification16 codes

C07D 487/04
In which the condensed system contains two hetero rings: ortho-condensed systems
A61K 31/4985
Having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines: pyrazines or piperazines…
A61P 19/08
Drugs for skeletal disorders: for bone diseases, e.g. rachitism, Paget's disease
A61P 29/00
Non-central analgesic, antipyretic or antiinflammatory agents

Crystal form of acp-196 salt and preparation method, pharmaceutical composition, and use thereof

Life of this patent

Crystal form of acp-196 salt and preparation method, pharmaceutical composition, and use thereof

Life of this patent

Abstract

Claims23