IP Library Granted Patent US 8,153,654
Granted Patent B2
US 8,153,654 · App. 12/009,326 · Granted Apr 10, 2012

6-and 7-amino isoquinoline compounds and methods for making and using the same

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Quick Facts
Patent No.
US 8,153,654
App. No.
12/009,326
Granted
Apr 10, 2012
Kind
B2
Abstract

6- and 7-amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6- and 7-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 (27)

1. A compound of the formula:

or an optical isomer, diastereomer, enantiomer, or pharmaceutically acceptable salt thereof;

wherein R 1 is thienyl;

R 2 and R 3 are independently selected from H and C 1 -C 4 alkyl;

R 4 is H;

R 5 is NH 2 , H, or OH; and

R 7 is H.

2. A compound according to claim 1 , wherein the compound is of the formula

wherein R 1 is thienyl;

R 2 and R 3 are independently selected from H and C 1 -C 4 alkyl;

R 4 is H;

R 5 is NH 2 , H, or OH; and

R 7 is H.

3. A compound according to claim 1 , wherein R 1 is 2-thienyl.

4. A compound according to claim 1 , wherein R 1 is 3-thienyl.

5. A compound according to claim 1 , wherein R 2 and R 3 are both H.

6. A compound according to claim 1 , wherein R 2 and R 3 are both C 1 -C 4 alkyl.

7. A compound according to claim 1 , wherein R 5 is OH.

8. A compound of formula

or an optical isomer, diastereomer, enantiomer, or pharmaceutically acceptable salt thereof.

9. A pharmaceutical composition comprising a compound according to claim 1 and a carrier.

10. A pharmaceutical composition comprising a compound according to claim 8 and a carrier.

11. A method for treating a disease in a mammal comprising administering to a mammal a safe and effective amount of a compound according to claim 1 , wherein the disease comprises at least one of eye disease, bone disorder, obesity, heart disease, hepatic disease, renal disease, pancreatitis, cancer, myocardial infarct, gastric disturbance, hypertension, fertility control, nasal congestion, neurogenic bladder disorder, gastrointestinal disorder and dermatological disorder.

12. A method according to claim 11 , wherein the disease is an eye disease.

13. A method according to claim 12 , wherein the eye disease is glaucoma or a neurodegenerative eye disease.

14. A method according to claim 11 , wherein the compound is

or an optical isomer, diastereomer, enantiomer, or pharmaceutically acceptable salt thereof.

Assignments (6)
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 DISTRIBUTION, INC.
Reel/Frame 046431/0500 →
SECURITY INTEREST Recorded Jul 23, 2018
From: AERIE PHARMACEUTICALS, INC.
To: DEERFIELD PRIVATE DESIGN FUND III, L.P.
Reel/Frame 046432/0307 →
SECURITY AGREEMENT Recorded Mar 4, 2009
From: AERIE PHARMACEUTICALS, INC.
To: ACP IV, LP, (AS COLLATERAL AGENT)
Reel/Frame 022368/0097 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 11, 2008
From: DELONG, MITCHELL A.; STURDIVANT, JILL MARIE; HEINTZELMAN, GEOFFREY RICHARD; ROYALTY, SUSAN M.
To: AERIE PHARMACEUTICALS, INC.
Reel/Frame 020790/0664 →