Biochemical binding of RET9 and VEGFR2 inhibitors

Patent metadata

Field	Value
Publication number	US-11401260-B2
Application number	US-201816757305-A
Country	US
Kind code	B2
Filing date	Oct 19, 2018
Priority date	Oct 20, 2017
Publication date	Aug 2, 2022
Grant date	Aug 2, 2022

Abstract

Provided herein are compounds, compositions, and pharmaceutical compositions of Formula (I). Also provided herein are methods of using compounds of Formula (I) to treat proliferative diseases, ocular diseases, dermatological diseases, inflammatory diseases, autoimmune diseases, autoinflammatory diseases, and metabolic diseases. Also provided herein are methods of using the compounds of Formula (I) as therapeutics, e.g., in the treatment and/or prevention of diseases associated with growth factor activity or angiogenesis. In some embodiments, the disease being treated is a proliferative disease.

First claim

What is claimed is:

1. A compound, wherein the compound is: a compound of Formula I:

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein the compound is:

3. The compound of claim 1 , wherein the compound is a pharmaceutically acceptable salt of

4. A pharmaceutical composition, comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

5. The pharmaceutical composition of claim 4 , wherein the composition is suitable for delivery to an eye of a subject.

6. A method of preparing a compound of Formula (I),

or a pharmaceutically acceptable salt thereof,

wherein the method comprises contacting a compound of Formula (X),

or a salt thereof,
wherein X is a halogen,

with a compound of Formula (Y),

or a salt thereof,
wherein R is an amine protecting group,

to form the compound of Formula (I), or a pharmaceutically acceptable salt thereof.

7. The method of claim 6 , wherein X is Cl or F.

8. The method of claim 6 , wherein R is tert-Butyloxycarbonyl.

Assignees

• Kala Pharmaceuticals Inc

Inventors

• Nowak Pawel Wojciech
• Ong Winston Z

Classifications

• C07D401/14 Primary

  containing three or more hetero rings · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61K9/0048

  Eye, e.g. artificial tears · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title

• A61P27/02

  Ophthalmic agents · CPC title