# US 10,766,907 B2 · Crystalline forms of therapeutic compounds and uses thereof

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- Number: US 10,766,907 B2
- Document ID: US10766907B2
- Status: Granted
- Kind: B2
- Application number: 16/513,505
- Filed: 2019-07-16
- Published: 2019-11-07
- Granted: 2020-09-08
- Earliest claimed: 2016-09-08
- Assignees: Kala Pharmaceuticals, Inc.
- Applicants: Kala Pharmaceuticals, Inc.
- Inventors: Minh Ngoc Nguyen; Winston Zapanta Ong
- Web page: https://patentgrep.com/patent/US10766907B2

## CPC

- C07D 491/107: with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- 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

Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.

## Claims

### Claim 1

A method of treating a disease comprising administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising a crystalline form of Compound 1:
wherein the crystalline form has an X-ray powder diffraction (XRPD) pattern comprising peaks at 8.5-9.5 degrees 2θ, 18-19 degrees 2θ, 19-19.5 degrees 2θ, and 25.0-25.5 degrees 2θ; and
wherein the disease is a proliferative disease, cancer, or an ocular disease.

### Claim 2 (depends on 1)

The method of claim 1, wherein the crystalline form is a hydrate.

### Claim 3 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition comprises the crystalline form of claim 1 and a pharmaceutically acceptable carrier.

### Claim 4 (depends on 3)

The method of claim 3, wherein the pharmaceutical composition is suitable for topical administration.

### Claim 5 (depends on 3)

The method of claim 3, wherein the pharmaceutical composition is suitable for injection.

### Claim 6 (depends on 3)

The method of claim 3, wherein the pharmaceutical composition is suitable for delivery to the eye.

### Claim 7 (depends on 1)

The method of claim 1, wherein the disease is a proliferative disease.

### Claim 8 (depends on 1)

The method of claim 1, wherein the disease is cancer.

### Claim 9 (depends on 1)

The method of claim 1, wherein the disease is an ocular disease.

### Claim 10 (depends on 9)

The method of claim 9, wherein the disease is retinopathy.

### Claim 11 (depends on 9)

The method of claim 9, wherein the disease is age-related macular degeneration (AMD).

### Claim 12 (depends on 9)

The method of claim 9, wherein the disease is corneal neovascularization.

### Claim 13

A method of inhibiting growth factor signaling comprising administering to a subject a therapeutically effective amount of a pharmaceutical composition comprising a crystalline form of Compound 1:
wherein the crystalline form has an X-ray powder diffraction (XRPD) pattern comprising peaks at 8.5-9.5 degrees 2θ, 18-19 degrees 2θ, 19-19.5 degrees 2θ, and 25.0-25.5 degrees 2θ.

### Claim 14 (depends on 13)

The method of claim 13, wherein the crystalline form is a hydrate.

### Claim 15 (depends on 1, 13)

The method of claim 13, wherein the pharmaceutical composition comprises the crystalline form of claim 1 and a pharmaceutically acceptable carrier.

### Claim 16 (depends on 15)

The method of claim 15, wherein the pharmaceutical composition is suitable for topical administration.

### Claim 17 (depends on 15)

The method of claim 15, wherein the pharmaceutical composition is suitable for injection.

### Claim 18 (depends on 15)

The method of claim 15, wherein the pharmaceutical composition is suitable for delivery to the eye.

### Claim 19 (depends on 15)

The method of claim 15, wherein the growth factor signaling is associated with an ocular disease.