# US 2019/0314331 A1 · Nonracemic mixtures and uses thereof

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- Number: US 2019/0314331 A1
- Document ID: US20190314331A1
- Status: Published application
- Kind: A1
- Application number: 16/452,880
- Filed: 2019-06-26
- Published: 2019-10-17
- Earliest claimed: 2017-12-05
- Assignees: Sunovion Pharmaceuticals Inc.
- Applicants: Sunovion Pharmaceuticals Inc.
- Inventors: Seth Cabot Hopkins; Kenneth Stephen Koblan; John R. Snoonian; Harold Scott Wilkinson
- Web page: https://patentgrep.com/patent/US20190314331A1

## CPC

- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61P 25/24: Antidepressants
- 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

## Abstract

Provided are compositions comprising unequal mixtures of (R)-amisulpride and (S)-amisulpride, or pharmaceutically acceptable salts thereof, where the amount of (R)-amisulpride is greater than the amount of (S)-amisulpride, compositions and medicaments comprising the same used for the treatment of various diseases and disorders, and methods of using same for the treatment of various diseases and disorders, including, but not limited to, dosage regimens. In addition, provided are various formulations thereof, including, but not limited to, formulations employing polymorphs of enantiomeric amisulpride.

## Claims

### Claim at position 1

1-52. (canceled)

### Claim 53

A composition comprising:
(R)-(+)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base; and
(S)-(−)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base;
wherein the combined amount of (R)-(+)-amisulpride and (S)-(−)-amisulpride, or pharmaceutically acceptable salts thereof, is about 200 mg to about 600 mg by weight of free base; and
wherein the enantiomeric ratio of (R)-(+)-amisulpride to (S)-(−)-amisulpride in the composition is about 65:35 to about 85:15 by weight of free base.

### Claim 54 (depends on 53)

The composition of claim 53 wherein the enantiomeric ratio of (R)-(+)-amisulpride to (S)-(−)-amisulpride is about 75:25 to about 85:15 by weight of free base.

### Claim 55 (depends on 53)

The composition of claim 53 wherein the enantiomeric ratio of (R)-(+)-amisulpride to (S)-(−)-amisulpride is about 80:20 to about 85:15 by weight of free base.

### Claim 56 (depends on 53)

The composition of claim 53 wherein the enantiomeric ratio of (R)-(+)-amisulpride to (S)-(−)-amisulpride is about 85:15 by weight of free base.

### Claim 57 (depends on 53)

The composition of claim 53 wherein the combined amount of (R)-(+)-amisulpride and (S)-(−)-amisulpride, or pharmaceutically acceptable salts thereof, is about 200 mg to about 400 mg by weight of free base.

### Claim 58 (depends on 53)

The composition of claim 53 wherein the combined amount of (R)-(+)-amisulpride and (S)-(−)-amisulpride, or pharmaceutically acceptable salts thereof, is about 200 mg by weight of free base.

### Claim 59 (depends on 53)

The composition of claim 53 wherein the combined amount of (R)-(+)-amisulpride and (S)-(−)-amisulpride, or pharmaceutically acceptable salts thereof, is about 400 mg by weight of free base.

### Claim 60 (depends on 53)

The composition of claim 53 wherein the composition comprises:
about 170 mg to about 340 mg of (R)-(+)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base; and
about 30 mg to about 60 mg (S)-(−)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base.

### Claim 61 (depends on 53)

The composition of claim 53 wherein the composition comprises:
about 170 mg of (R)-(+)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base; and
about 30 mg of (S)-(−)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base.

### Claim 62 (depends on 53)

The composition of claim 53 wherein the composition comprises:
about 340 mg of (R)-(+)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base; and
about 60 mg of (S)-(−)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base.

### Claim 63 (depends on 53)

The composition of claim 53 wherein the (R)-(+)-amisulpride is crystalline (R)-(+)-amisulpride of crystal Form A; and the (S)-(−)-amisulpride is crystalline (S)-(−)-amisulpride of crystal Form A′;
wherein Form A is characterized by a powder x-ray diffraction pattern comprising peaks, in terms of 2-theta, at 7.0±0.2°, 9.7±0.2°, and 15.4±0.2°; and
Form A′ is characterized by a powder x-ray diffraction pattern comprising peaks, in terms of 2-theta, at 7.0±0.2°, 9.7±0.2°, and 15.4±0.2°.

### Claim 64

A composition comprising:
(R)-(+)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base; and
(S)-(−)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base;
wherein the combined amount of (R)-(+)-amisulpride and (S)-(−)-amisulpride, or pharmaceutically acceptable salts thereof, is about 200 mg to about 400 mg by weight of free base; and
wherein the enantiomeric ratio of (R)-(+)-amisulpride to (S)-(−)-amisulpride in the composition is about 85:15 by weight of free base.

### Claim 65 (depends on 64)

The composition of claim 64 wherein the composition comprises:
about 170 mg of (R)-(+)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base; and
about 30 mg of (S)-(−)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base.

### Claim 66 (depends on 64)

The composition of claim 64 wherein the composition comprises:
about 340 mg of (R)-(+)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base; and
about 60 mg of (S)-(−)-amisulpride, or a pharmaceutically acceptable salt thereof, by weight of free base.

### Claim 67 (depends on 64)

The composition of claim 64 wherein the (R)-(+)-amisulpride is crystalline (R)-(+)-amisulpride of crystal Form A; and the (S)-(−)-amisulpride is crystalline (S)-(−)-amisulpride of crystal Form A′;
wherein Form A is characterized by a powder x-ray diffraction pattern comprising peaks, in terms of 2-theta, at 7.0±0.2°, 9.7±0.2°, and 15.4±0.2°; and
Form A′ is characterized by a powder x-ray diffraction pattern comprising peaks, in terms of 2-theta, at 7.0±0.2°, 9.7±0.2°, and 15.4±0.2°.