# US 2019/0315744 A1 · Crystalline Valbenazine Free Base

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- Number: US 2019/0315744 A1
- Document ID: US20190315744A1
- Status: Published application
- Kind: A1
- Application number: 16/462,358
- Filed: 2017-12-06
- Published: 2019-10-17
- Earliest claimed: 2017-01-10
- Assignees: Sandoz Ltd.
- Applicants: Sandoz AG
- Inventors: Christoph Langes; Stefan Reissmann
- Web page: https://patentgrep.com/patent/US20190315744A1

## CPC

- C07D 471/04: Ortho-condensed systems
- A61P 25/00: Drugs for disorders of the nervous system
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

The present disclosure generally relates to crystalline valbenazine. The present disclosure also generally relates to a pharmaceutical composition comprising crystalline valbenazine, as well of methods of using crystalline valbenazine in the treatment of hyperkinetic disorders, and methods for obtaining such forms.

## Claims

### Claim 1

Crystalline valbenazine.

### Claim 2 (depends on 1)

The crystalline valbenazine according to claim 1, in substantially pure form.

### Claim 3 (depends on 1)

The crystalline valbenazine according to claim 1, characterized by a x-ray powder diffraction pattern comprising four or more 2θ values selected from the group consisting of 6.0±0.2°, 6.8±0.2°, 8.4±0.2°, 10.0±0.2°, 14.2±0.2°, 17.6±0.2°, 18.2±0.2° and 20.3±0.2°, when measured at a temperature of about 22° C. using Cu Kα radiation.

### Claim 4 (depends on 3)

The crystalline valbenazine according to claim 3, having a X-ray diffraction spectrum substantially the same as the X-ray powder diffraction spectrum shown in FIG. 1.

### Claim 5 (depends on 1)

The crystalline valbenazine according to claim 1 having a melting and/or decomposition temperature between 90° C. and 95° C.

### Claim 6 (depends on 1)

A composition comprising at least 95 weight % of crystalline valbenazine according to claim 1, based the weight of the composition.

### Claim 7 (depends on 6)

The composition of claim 6 consisting essentially of crystalline valbenazine characterized by a x-ray powder diffraction pattern comprising four or more 2θ values selected from the group consisting of 6.0±0.2°, 6.8±0.2°, 8.4±0.2°, 10.0±0.2°, 14.2±0.2°, 17.6±0.2°, 18.2±0.2° and 20.3±0.2°, when measured at a temperature of about 22° C. using Cu Kα radiation.

### Claim at position 8

8-9. (canceled)

### Claim 10

A process of making a pharmaceutically acceptable acid addition salt of valbenazine, wherein
a) crystalline valbenazine free base is dissolved in a solvent,
b) the dissolved valbenazine free base is brought into contact with a pharmaceutically acceptable acid, and
c) a solid form of the pharmaceutically acceptable acid addition salt of valbenazine is allowed to form and isolated.

### Claim 11 (depends on 10)

The process according to claim 10, wherein the solid form of the pharmaceutically acceptable acid addition salt of valbenazine is a crystalline solid form.

### Claim 12 (depends on 1)

A process of making crystalline valbenazine according to claim 1, comprising:
allowing valbenazine to crystallize from a solvent comprising diethylether.

### Claim 13 (depends on 12)

The process according to claim 12, wherein the solvent further comprises isopropyl alcohol, dichloromethane, methylethylketone, cyclohexanone, ethylacetate or cyclohexane.

### Claim 14 (depends on 12)

The process according to claim 12, further comprising the step of carbon filtering.

### Claim 15 (depends on 12)

The process according to claim 12, wherein valbenazine is allowed to crystallize at a temperature of from 0° C. to 40° C.