Free base crystalline form of a complement component C5a receptor

Patent metadata

Field	Value
Publication number	US-11026935-B2
Application number	US-202017091019-A
Country	US
Kind code	B2
Filing date	Nov 6, 2020
Priority date	Nov 8, 2019
Publication date	Jun 8, 2021
Grant date	Jun 8, 2021

Abstract

Provided herein is a free base crystalline form of a complement component 5a receptor having the formula of Compound 1Also provided herein are pharmaceutical compositions and methods of treatment using the crystalline free base form of Compound 1 described herein.

First claim

What is claimed is:

1. A free base crystalline form of Compound 1

characterized by an X-ray powder diffraction (XRPD) pattern comprising peaks at 8.1, 8.4, 14.1, 16.9, and 19.0 degrees 2θ (±0.2 degrees 2θ).

2. The free base crystalline form of claim 1 , further characterized by XRPD peaks at 12.4, 15.2, 16.1, 24.4, and 24.7 degrees 2θ (±0.2 degrees 2θ).

3. The free base crystalline form of claim 1 , characterized by an X-ray powder diffraction pattern in accordance with FIG. 1 .

4. The free base crystalline form of claim 1 , further characterized by a differential scanning calorimetry thermogram (DSC) comprising an endothermic peak at around 216° C.

5. The free base crystalline form of claim 1 , further characterized by a melting point onset of about 213° C. as determined by differential scanning calorimetry thermogram (DSC).

6. The free base crystalline form of claim 1 , further characterized by a DSC in accordance with FIG. 2 .

7. A pharmaceutical composition comprising the free base crystalline form of Compound 1 according to claim 1 and at least one pharmaceutically acceptable excipient.

8. An aqueous suspension comprising the free base crystalline form of Compound 1 according to claim 1 and at least one excipient.

9. The aqueous suspension of claim 8 , wherein the at least one excipient is at least one suspending agent and/or at least one wetting agent.

Assignees

• Chemocentryx Inc

Inventors

• Singh Rajinder
• Yau Kwok
• Zeng Yibin
• Zhang Penglie
• Lui Rebecca M
• Krasinski Antoni

Classifications

• C07D211/60 Primary

  Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals · CPC title

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61K31/675

  having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate · CPC title