# US 11,623,917 B2 · Multi-tyrosine kinase inhibitors derivatives and methods of use

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- Number: US 11,623,917 B2
- Document ID: US11623917B2
- Status: Granted
- Kind: B2
- Application number: 17/118,807
- Filed: 2020-12-11
- Published: 2021-04-22
- Granted: 2023-04-11
- Earliest claimed: 2015-06-29
- Assignees: Ontogenesis, LLC
- Applicants: Ontogenesis, LLC
- Inventors: Gerald Horn
- Web page: https://patentgrep.com/patent/US11623917B2

## CPC

- C07D 215/22: attached in position 2 or 4
- C07C 233/57: having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
- C07C 233/60: having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
- C07C 2601/02: with a three-membered ring
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

The present invention is directed to multi-tyrosine kinase inhibitor compounds. The present invention is further directed to compositions comprising those compounds. Finally, the present invention is directed to methods of treating eye conditions including, but not limited to, diabetic background retinopathy, diabetic macular edema, diabetic proliferative retinopathy, diabetic macular edema with proliferative retinopathy, proliferative fibrovascular disease, diabetic macular edema with proliferative fibrovascular disease, retinopathy of prematurity, dry macular degeneration, dry macular degeneration with drusen and wet macular degeneration, using compounds and compositions of the invention.

## Claims

### Claim 1

A method of treating a condition of the eye comprising administering via intravitreal injection or topical application of a therapeutically effective amount of a compound of formula (V):
to a subject in need thereof, wherein X1 and X2 are each, individually a peptide, a protein or absent.

### Claim 2 (depends on 1)

The method of claim 1, wherein the condition is selected from diabetic background retinopathy, diabetic macular edema, diabetic proliferative retinopathy, diabetic macular edema with proliferative retinopathy, neovascular glaucoma, retinopathy of prematurity, proliferative fibrovascular disease, diabetic macular edema with proliferative fibrovascular disease, retinopathy of prematurity, dry macular degeneration, any retinopathies with vascular leakage such as Coat's disease or Bescet's disease, dry macular degeneration with drusen and wet macular degeneration.

### Claim 3 (depends on 1)

The method of claim 1, wherein the condition is diabetic macular edema and wherein proliferative retinopathy is prevented.

### Claim 4 (depends on 1)

The method of claim 1, wherein the condition is diabetic macular edema with proliferative retinopathy and proliferative retinopathy is suppressed.

### Claim 5 (depends on 1)

The method of claim 1, wherein the condition is diabetic macular edema and wherein fibrovascular proliferative disease is prevented.

### Claim 6 (depends on 1)

The method of claim 1, wherein the condition is diabetic macular edema with fibrovascular proliferative disease and wherein fibrovascular proliferative disease is suppressed.

### Claim 7 (depends on 1)

The method of claim 1, wherein the condition is dry macular degeneration or dry macular degeneration with drusen and wherein wet macular degeneration is suppressed or prevented.

### Claim 8

A method of treating a condition of the eye comprising administering via intravitreal injection or topical application of a therapeutically effective amount of a compound of formula (V):
to a subject in need thereof, wherein X1 and X2 are each, individually a peptide, a protein or absent and wherein the administration occurs no more than once every 3 months.

### Claim 9 (depends on 8)

The method of claim 8, wherein the administration occurs no more than once every 6 months.

### Claim 10 (depends on 8)

The method of claim 8, wherein the administration occurs no more than once every 9 months.