Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds

Patent metadata

Field	Value
Publication number	US-10112920-B2
Application number	US-201715844399-A
Country	US
Kind code	B2
Filing date	Dec 15, 2017
Priority date	Jul 25, 2008
Publication date	Oct 30, 2018
Grant date	Oct 30, 2018

Abstract

Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.

First claim

What is claimed is:

1. A compound selected from:
a dihydrochloride salt of 3-amino-N-(isoquinolin-6-yl)-3-(thiophen-3-yl)propanamide;
a dihydrochloride salt of 3-(dimethylamino)-N-(isoquinolin-6-yl)-2-(thiophen-3-yl)propanamide;
a dihydrochloride salt of 3-amino-N-(isoquinolin-6-yl)-2-(thiophen-3-yl)propanamide; or
a dihydrochloride salt of 4-amino-N-(isoquinolin-6-yl)-4-(thiophen-3-yl)butanamide.

2. A composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.

3. The composition of claim 2 , wherein the carrier is saline buffered to a pH of about 5.5 to about 6.5.

4. A method of treating an eye disease in a subject in need thereof, the method comprising administering to the subject an effective amount of the compound of claim 1 .

5. The method of claim 4 , wherein the eye disease comprises glaucoma.

6. The method of claim 4 , wherein the eye disease comprises a neurodegenerative eye disease.

7. A compound selected from:

or the formula:

R1
R2
R3
R4

H
H
CH 3
H

H
H
H
H

F
H
H
H

Cl
H
H
H

H
H
—OMe
H

Cl
Cl
H
H

—Me
H
H
H

H
H
F
H

CH 3
CH 3
H
H

CH 3
H
H
H

H
H
H
OMe

H
H
H
OH

H
H
H
NH 2 ;

or the formula:

R1
R2
R3
R4
R5
R6

H
H
3-thienyl
Cl
Cl
H

H
H
3-thienyl
H
H
H

H
H
3-thienyl
F
F
H

H
H
C 6 H 6
H
H
H

CH 3
CH 3
C 6 H 6
H
H
H

CH 3
CH 3
C 6 H 6
F
Cl
H

CH 3
CH 3
cyclohexyl
H
H
H

CH 3
CH 3
—CH(CH 3 ) 2
H
H
H

CH 3
CH 3
3-thienyl
CF 3
H
H

CH 3
CH 3
3-thienyl
OCF 3
H
H

CH 3
CH 3
3-thienyl
CN
H
H

CH 3
CH 3
2-pyridyl
H
H
H

CH 3
CH 3
3-pyridyl
H
H
H

CH 3
CH 3
4-pyridyl
H
H
H

CH 3
CH 3
2-thienyl
H
H
H

H
CH 3
3-thienyl
H
H
H

CH 3
CH 3
3-thienyl
NO 2

Assignees

• Aerie Pharmaceuticals Inc

Inventors

• Delong Mitchell A
• Sturdivant Jill Marie
• Royalty Susan M

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P9/12

  Antihypertensives · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title