# US 11,026,935 B2 · Free base crystalline form of a complement component C5a receptor

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- Number: US 11,026,935 B2
- Document ID: US11026935B2
- Status: Granted
- Kind: B2
- Application number: 17/091,019
- Filed: 2020-11-06
- Published: 2021-05-13
- Granted: 2021-06-08
- Earliest claimed: 2019-11-08
- Assignees: ChemoCentryx, Inc.
- Applicants: Chemocentryx, Inc.
- Inventors: Rajinder Singh; Kwok Yau; Yibin Zeng; Penglie Zhang; Rebecca M. Lui; Antoni Krasinski
- Web page: https://patentgrep.com/patent/US11026935B2

## CPC

- A61K 31/451: having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
- A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/00: Drugs for immunological or allergic disorders
- C07D 211/60: Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

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

## Claims

### Claim 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).

### Claim 2 (depends on 1)

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).

### Claim 3 (depends on 1)

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

### Claim 4 (depends on 1)

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.

### Claim 5 (depends on 1)

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).

### Claim 6 (depends on 1)

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

### Claim 7 (depends on 1)

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

### Claim 8 (depends on 1)

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

### Claim 9 (depends on 8)

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.