IP Library Granted Patent US 8,921,392
Granted Patent B2
US 8,921,392 · App. 13/723,811 · Granted Dec 30, 2014

6-aminoisoquinoline compounds

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Quick Facts
Patent No.
US 8,921,392
App. No.
13/723,811
Granted
Dec 30, 2014
Kind
B2
Abstract

6-Amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided.

Claims (17)

1. A compound according to Formula IV

wherein A is a substituted or unsubstituted chain containing from one to four member atoms selected from the group consisting of carbon, nitrogen, oxygen and sulphur, wherein the chain may be mono- or disubstituted with halogen, cyano, nitro, or C 1 -C 4 alkyl, or the substituted atoms may attach back to the main chain to form a ring;

wherein R 1 and R 2 are, independently, hydrogen, hydroxyl, halogen, or cyano; and

wherein R 3 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, amino, cyano, cycloalkyl, heterocycloalkyl, aryl, C 1 -C 4 alkyl aryl, heteroaryl, C 1 -C 4 alkyl heteroaryl, carbonyl, carbonylamino, thioalkyl, sulfonyl, sulfonylamino, acyl, or carboxyl.

2. The compound of claim 1 , wherein R 1 and R 2 are hydrogen.

3. The compound of claim 1 , wherein A is methylene or ethylene.

4. The compound of claim 1 , wherein A is —O—CH 2 — or —NH—CH 2 —.

5. The compound of claim 1 , wherein R 3 is alkyl, alkoxy, cycloalkyl, heterocycloalkyl, aryl, C 1 -C 4 alkyl aryl, heteroaryl, C 1 -C 4 alkyl heteroaryl, carbonyl, or carbonylamino.

6. The compound of claim 1 , wherein R 3 is aryl.

7. The compound of claim 6 , wherein R 3 is substituted with heteroaryl, acyl, carboxyl, carbonylamino, nitro, amino, cyano, halogen, alkoxy, or hydroxyl.

8. The compound of claim 6 , wherein R 3 is phenyl.

9. The compound of claim 1 , selected from the following:

10. A pharmaceutical composition comprising:

a) the compound according to claim 1 ; and

b) a pharmaceutically acceptable carrier.

11. The composition of claim 10 , wherein the carrier is selected from the group consisting of systemic and topical carriers.

12. The composition of claim 11 , wherein the composition comprises about 0.001% to 10% of the 6-aminoisoquinoline derivative and 90 to 99.999% of the systemic carrier.

Assignments (7)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 24, 2024
From: AERIE PHARMACEUTICALS, INC.
To: ALCON INC.
Reel/Frame 067822/0168 →
RELEASE OF SECURITY INTEREST Recorded Sep 5, 2019
From: DEERFIELD PRIVATE DESIGN FUND III, L.P.
To: AERIE PHARMACEUTICALS, INC.
Reel/Frame 050276/0807 →
RELEASE OF SECURITY INTEREST Recorded Jul 23, 2018
From: DEERFIELD PARTNERS, L.P.; DEERFIELD PRIVATE DESIGN FUND III, L.P.; DEERFIELD SPECIAL SITUATIONS FUND, L.P.; DEERFIELD MANAGEMENT COMPANY, L.P.
To: AERIE PHARMACEUTICALS, INC.
Reel/Frame 046431/0600 →
SECURITY INTEREST Recorded Jul 23, 2018
From: AERIE PHARMACEUTICALS, INC.
To: DEERFIELD PRIVATE DESIGN FUND III, L.P.
Reel/Frame 046432/0307 →
RELEASE OF SECURITY INTEREST Recorded Jul 23, 2018
From: DEERFIELD PARTNERS, L.P.; DEERFIELD PRIVATE DESIGN FUND III, L.P.; DEERFIELD SPECIAL SITUATIONS FUND, L.P.; DEERFIELD MANAGEMENT COMPANY, L.P.
To: AERIE DISTRIBUTION, INC.
Reel/Frame 046431/0500 →
SECURITY INTEREST Recorded Sep 11, 2014
From: AERIE PHARMACEUTICALS, INC.
To: DEERFIELD MANAGEMENT COMPANY, L.P., AS AGENT; DEERFIELD PARTNERS, L.P.; DEERFIELD INTERNATIONAL MASTER FUND, L.P.; DEERFIELD PRIVATE DESIGN FUND III, L.P.; DEERFIELD SPECIAL SITUATIONS FUND, L.P.; DEERFIELD SPECIAL SITUATIONS INTERNATIONAL MASTER FUND, L.P.
Reel/Frame 033726/0043 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 19, 2013
From: DELONG, MITCHELL A.; ROYALTY, SUSAN M.; STURDIVANT, JILL MARIE; HEINTZELMAN, GEOFFREY RICHARD
To: AERIE PHARMACEUTICALS, INC.
Reel/Frame 029832/0455 →