IP Library Granted Patent US 9,969,684
Granted Patent B2
US 9,969,684 · App. 15/640,342 · Granted May 15, 2018

N-hydroxylsulfonamide derivatives as new physiologically useful nitroxyl donors

Inventors: John P. Toscano (Glen Arm, MD); Frederick Arthur Brookfield (Abingdon, GB); Andrew D. Cohen (Mamaroneck, NY); Stephen Martin Courtney (Abingdon, GB); Lisa Marie Frost (Abingdon, GB); Vincent Jacob Kalish (Annapolis, MD)
Assignees: Cardioxyl Pharmaceuticals, Inc.; The Johns Hopkins University
C07C311/48C07C317/14C07C323/67C07D213/74C07D231/18C07D261/10C07D263/58C07D285/125C07D295/096C07D307/82C07D309/12C07D317/14C07D333/34C07D333/62
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Quick Facts
Patent No.
US 9,969,684
App. No.
15/640,342
Granted
May 15, 2018
Kind
B2
Abstract

The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.

Claims (34)

1. A method for modulating in vivo nitroxyl levels, treating a cardiovascular disease or condition, or treating heart failure, comprising administering to an individual in need thereof

(a) an effective amount of a compound of formula (I)

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is H;

R 2 is H;

R 3 is halo, methylsulfonyl or perfluoromethyl;

R 4 , R 5 , R 6 and R 7 are H; and

halo is F, Cl, Br or I; and

(b) an effective amount of at least one other positive inotropic agent.

2. The method of claim 1 , wherein the other positive inotropic agent is selected from a beta-adrenergic receptor agonist, an inhibitor of phosphodiesterase activity, a calcium-sensitizer, and any combination thereof and the heart failure is acute decompensated heart failure.

3. The method of claim 1 , wherein R 3 is Cl, Br or I.

4. The method of claim 3 , wherein the other positive inotropic agent is selected from a beta-adrenergic receptor agonist, an inhibitor of phosphodiesterase activity, a calcium-sensitizer, and any combination thereof and the heart failure is acute decompensated heart failure.

5. The method of claim 1 , wherein R 3 is methylsulfonyl.

6. The method of claim 5 , wherein the other positive inotropic agent is selected from a beta-adrenergic receptor agonist, an inhibitor of phosphodiesterase activity, a calcium-sensitizer, and any combination thereof and the heart failure is acute decompensated heart failure.

7. The method of claim 1 , wherein R 3 is perfluoromethyl.

8. The method of claim 7 , wherein the other positive inotropic agent is selected from a beta-adrenergic receptor agonist, an inhibitor of phosphodiesterase activity, a calcium-sensitizer, and any combination thereof and the heart failure is acute decompensated heart failure.

9. A method for treating, preventing, delaying the onset of, or delaying the development of heart failure, comprising administering to an individual in need thereof

(a) an effective amount of a compound of formula (I)

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is H;

R 2 is H;

R 3 is halo, methylsulfonyl or perfluoromethyl;

R 4 , R 5 , R 6 and R 7 are H; and

halo is F, Cl, Br or I; and

(b) an effective amount of at least one other positive inotropic agent.

10. The method of claim 9 , wherein the other positive inotropic agent is selected from a beta-adrenergic receptor agonist, an inhibitor of phosphodiesterase activity, a calcium-sensitizer, and any combination thereof and the heart failure is acute decompensated heart failure.

11. The method of claim 9 , wherein R 3 is Cl, Br or I.

12. The method of claim 11 , wherein the other positive inotropic agent is selected from a beta-adrenergic receptor agonist, an inhibitor of phosphodiesterase activity, a calcium-sensitizer, and any combination thereof and the heart failure is acute decompensated heart failure.

13. The method of claim 9 , wherein R 3 is methylsulfonyl.

14. The method of claim 13 , wherein the other positive inotropic agent is selected from a beta-adrenergic receptor agonist, an inhibitor of phosphodiesterase activity, a calcium-sensitizer, and any combination thereof and the heart failure is acute decompensated heart failure.

15. The method of claim 9 , wherein R 3 is perfluoromethyl.

16. The method of claim 15 , wherein the other positive inotropic agent is selected from a beta-adrenergic receptor agonist, an inhibitor of phosphodiesterase activity, a calcium-sensitizer, and any combination thereof and the heart failure is acute decompensated heart failure.

17. The method of claim 1 , wherein the other positive inotropic agent is selected from dopamine, dopexamine, dobutamine, terbutaline, isoproterenol, and any combination thereof.

18. The method of claim 9 , wherein the other positive inotropic agent is selected from dopamine, dopexamine, dobutamine, terbutaline, isoproterenol, and any combination thereof.

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 9, 2022
From: CARDIOXYL PHARMACEUTICALS INC.
To: THE JOHNS HOPKINS UNIVERSITY
Reel/Frame 062041/0565 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2017
From: BROOKFIELD, FREDERICK ARTHUR; COURTNEY, STEPHEN MARTIN; FROST, LISA MARIE
To: EVOTEC LTD.
Reel/Frame 043256/0560 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2017
From: KALISH, VINCENT JACOB
To: CARDIOXYL PHARMACEUTICALS
Reel/Frame 043256/0616 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2017
From: TOSCANO, JOHN P.; COHEN, ANDREW D.
To: THE JOHNS HOPKINS UNIVERSITY
Reel/Frame 043256/0691 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 10, 2017
From: EVOTEC LTD.
To: CARDIOXYL PHARMACEUTICALS
Reel/Frame 043256/0746 →
Continuity (7)
Continuation 15286145 · Oct 5, 2016
Continuation 14857308 · Sep 17, 2015
Continuation 14280133 · May 16, 2014
Continuation 13213480 · Aug 19, 2011
Continuation 11724792 · Mar 16, 2007
Provisional Application 60783556 · Mar 17, 2006
Related Publication 20170305847A1 · Oct 26, 2017