# US 2014/0155438 A1 · Polymorphic forms of the sodium salt of 4-tert-butyl-n-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide

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- Number: US 2014/0155438 A1
- Document ID: US20140155438A1
- Status: Published application
- Kind: A1
- Application number: 14/234,277
- Filed: 2012-07-20
- Published: 2014-06-05
- Earliest claimed: 2011-07-22
- Assignees: ChemoCentryx, Inc.
- Inventors: Joanna Bis; David H. Igo; Bert Ho; Deven Shah
- Web page: https://patentgrep.com/patent/US20140155438A1

## CPC

- C07D 213/89: with hetero atoms directly attached to the ring nitrogen atom
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 11/06: Antiasthmatics
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Disclosed are novel polymorphic trihydrated forms of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl] benzenesulfonamide. One embodiment of the present invention is directed to a crystalline form of the sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-25 phenyl]-benzenesulfonamide (hereinafter “Compound A _ crystal-line trihydrate form I”), wherein the crystalline form is characterized by an X-ray powder diffraction pattern comprising diffraction angles (°28), when measured using Cu Ka radiation, at about 4.5, 9.0, 13.6, 13.9, 15.8, 17.8, 18.2, 18.5, 19.1, 19.9, 20A, 21.2, 22.1, 22.7, 24.3, 25.0, 25.6, 26.2, 26.8, 27.3, 27.6, 28.0, 28.8, and 30.8.

## Claims

### Claim 1

A crystalline form of a sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide, wherein the crystalline form is characterized by an X-ray powder diffraction pattern comprising diffraction angles, when measured using Cu Kα radiation, at about 4.5, 9.0, 13.6, 13.9, 15.8, 19.9, 20.4, and 28.0 °2θ.

### Claim 2

A crystalline form of a sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide, wherein the crystalline form is characterized by an X-ray powder diffraction pattern substantially in accordance with FIG. 1.

### Claim 3 (depends on 2)

The crystalline form of claim 2, wherein the crystalline form provides a Raman spectrum containing peaks at about 688, 743, 803, 1125, 1154, 1162, 1286, 1587, 1596, 1656, and 1672 cm−1.

### Claim 4 (depends on 2)

The crystalline form of claim 2, wherein the crystalline form provides a Raman spectrum substantially in accordance with FIG. 3.

### Claim 5 (depends on 2)

A pharmaceutical composition comprising the crystalline form according to claim 2 and a pharmaceutically acceptable carrier.

### Claim 6 (depends on 2)

A method of preparing a pharmaceutical composition comprising admixing the crystalline form according to claim 2 and a pharmaceutically acceptable carrier.

### Claim 7

A crystalline form of a sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide, wherein the crystalline form is characterized by an X-ray powder diffraction pattern comprising diffraction angles, when measured using Cu Kα radiation, at about 4.5, 9.1, 13.6, 13.9, 18.2, 19.9, 22.7, 24.3, 26.8, and 28.0 °2θ.

### Claim 8

A crystalline form of a sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]-benzenesulfonamide, wherein the crystalline form is characterized by an X-ray powder diffraction pattern substantially in accordance with FIG. 2.

### Claim 9 (depends on 8)

The crystalline form of claim 8, wherein the crystalline form provides a Raman spectrum containing peaks at about 668, 743, 1125, 1154, 1286, 1587, 1596, 1612, 1656, and 1673 cm−1.

### Claim 10 (depends on 8)

The crystalline form of claim 8, wherein the crystalline form provides a Raman spectrum substantially in accordance with FIG. 4.

### Claim 11 (depends on 8)

A pharmaceutical composition comprising the crystalline form according to claim 8 and a pharmaceutically acceptable carrier.

### Claim 12 (depends on 8)

A method of preparing a pharmaceutical composition comprising admixing the crystalline form according to claim 8 and a pharmaceutically acceptable carrier.

### Claim 13 (depends on 7)

A pharmaceutical composition comprising the crystalline form according to claim 7 and a pharmaceutically acceptable carrier.

### Claim 14 (depends on 7)

A method of preparing a pharmaceutical composition comprising admixing the crystalline form according to claim 7 and a pharmaceutically acceptable carrier.

### Claim 15 (depends on 1)

A pharmaceutical composition comprising the crystalline form according to claim 1 and a pharmaceutically acceptable carrier.

### Claim 16 (depends on 1)

A method of preparing a pharmaceutical composition comprising admixing the crystalline form according to claim 1 and a pharmaceutically acceptable carrier.