IP Library Granted Patent US 9,487,498
Granted Patent B2
US 9,487,498 · App. 14/857,308 · Granted Nov 8, 2016

Patent

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: The Johns Hopkins University; Cardioxyl Pharmaceuticals, Inc.
C07D309/12C07C311/48C07C317/14C07C323/67C07D213/74C07D261/10C07D263/58C07D285/125C07D295/096C07D307/82C07D317/14C07D333/62
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Quick Facts
Patent No.
US 9,487,498
App. No.
14/857,308
Granted
Nov 8, 2016
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 (33)

1. A compound of the formula (IV):

wherein:

R 1 is H;

R 2 is H, aralkyl or heterocyclyl;

T is alkyl, substituted alkyl, cycloalkyl, or substituted cycloalkyl; and

Z is an electron withdrawing group;

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein R 2 is H.

3. A method of treating, preventing, delaying the onset of, or delaying the development of a disease or condition that is responsive to nitroxyl therapy, comprising administering to an individual in need thereof a compound of the formula (IV):

wherein:

R 1 is H;

R 2 is H;

T is alkyl, substituted alkyl, cycloalkyl, or substituted cycloalkyl; and

Z is an electron withdrawing group;

or a pharmaceutically acceptable salt thereof.

4. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

5. The method of claim 3 , wherein the disease or condition is a cardiovascular disease or condition.

6. The method of claim 5 , wherein the disease or condition is acute heart failure.

7. The method of claim 3 , wherein the disease or condition implicates ischemia/reperfusion injury.

8. The method of claim 5 , wherein the disease or condition is acute decompensated heart failure.

9. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein R 2 is H, benzyl or tetrahydropyran-2-yl.

10. The compound of claim 2 or a pharmaceutically acceptable salt thereof, wherein T is alkyl having from 1 to 8 carbon atoms, alkyl having from 1 to 8 carbon atoms and substituted by from 1 to 5 substituents, cycloalkyl having from 3 to 8 carbon atoms, or cycloalkyl having from 3 to 8 carbon atoms and substituted by from 1 to 5 substituents.

11. The compound of claim 10 or a pharmaceutically acceptable salt thereof, wherein each substituent is independently selected from halo, nitro, cyano, oxo, alkoxy having from 1 to 8 carbon atoms, acyl having from 1 to 8 carbon atoms, acylamino having from 1 to 8 carbon atoms, amino, hydroxyl, carboxyl, carboxylalkyl having from 1 to 8 carbon atoms, thiol, thioalkyl having from 1 to 8 carbon atoms, and —OS(O) 2 -alkyl having from 1 to 8 carbon atoms.

12. The compound of claim 11 or a pharmaceutically acceptable salt thereof, wherein Z is —F, —Cl, —Br, —I, —CN, —CF 3 , —NO 2 , —SH, —C(O)H, —C(O)alkyl having from 1 to 8 carbon atoms, —C(O)Oalkyl having from 1 to 8 carbon atoms, —C(O)OH, —C(O)Cl, —S(O) 2 OH, —S(O) 2 NHOH, or —NH 3 .

13. The compound of claim 2 or a pharmaceutically acceptable salt thereof, wherein T is a branched alkyl having from 3 to 6 carbon atoms.

14. The compound of claim 13 or a pharmaceutically acceptable salt thereof, wherein Z is —F, —Cl, —Br, —I, —CN, —CF 3 , —NO 2 , —SH, —C(O)H, —C(O)alkyl having from 1 to 8 carbon atoms, —C(O)Oalkyl having from 1 to 8 carbon atoms, —C(O)OH, —C(O)Cl, —S(O) 2 OH, —S(O) 2 NHOH, or —NH 3 .

15. The compound of claim 13 or a pharmaceutically acceptable salt thereof; wherein T is isopropyl, t-butyl or sec-butyl.

16. The compound of claim 15 or a pharmaceutically acceptable salt thereof, wherein Z is —F, —Cl, —Br, —I, —CN, —CF 3 , —NO 2 , —SH, —C(O)H, —C(O)alkyl having from 1 to 8 carbon atoms, —C(O)Oalkyl having from 1 to 8 carbon atoms, —C(O)OH, —C(O)Cl, —S(O) 2 OH, —S(O) 2 N 2 NHOH, or —NH 3 .

17. The compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein Z is —F, —Cl, —Br, —I, —CN, —CF 3 , —NO 2 , —SH, —C(O)H, —C(O)alkyl having from 1 to 8 carbon atoms, —C(O)Oalkyl having from 1 to 8 carbon atoms, —C(O)OH, —C(O)Cl, —S(O) 2 OH, —S(O) 2 NHOH, or —NH 3 .

18. The compound of claim 17 which is:

or a pharmaceutically acceptable salt thereof.

19. The method of claim 3 , wherein for the compound of the formula (IV) or a pharmaceutically acceptable salt thereof T is a branched alkyl having from 3 to 6 carbon atoms.

20. The method of claim 19 , wherein for the compound of the formula (IV) or a pharmaceutically acceptable salt thereof Z is —F, —Cl, —Br, —I, —CN, —CF 3 , —NO 2 , —SH, —C(O)H, —C(O)alkyl having from 1 to 8 carbon atoms, —C(O)Oalkyl having from 1 to 8 carbon atoms, —C(O)OH, —C(O)Cl, —S(O) 2 OH, —S(O) 2 NHOH, or —NH 3 .

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 9, 2022
From: CARDIOXYL PHARMACEUTICALS INC.
To: THE JOHNS HOPKINS UNIVERSITY
Reel/Frame 062041/0565 →
CONFIRMATORY LICENSE Recorded Oct 27, 2017
From: JOHNS HOPKINS UNIVERSITY
To: NATIONAL SCIENCE FOUNDATION
Reel/Frame 044309/0702 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 18, 2015
From: BROOKFIELD, FREDERICK ARTHUR; COURTNEY, STEPHEN MARTIN; FROST, LISA MARIE
To: EVOTEC LTD.
Reel/Frame 036599/0969 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 18, 2015
From: EVOTEC LTD.
To: CARDIOXYL PHARMACEUTICALS
Reel/Frame 036600/0096 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 18, 2015
From: KALISH, VINCENT JACOB
To: CARDIOXYL PHARMACEUTICALS
Reel/Frame 036600/0528 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 18, 2015
From: TOSCANO, JOHN P.; COHEN, ANDREW D.
To: THE JOHNS HOPKINS UNIVERSITY
Reel/Frame 036600/0612 →
Continuity (5)
Continuation 14280133 · May 16, 2014
Continuation 13213480 · Aug 19, 2011
Continuation 11724792 · Mar 16, 2007
Provisional Application 60783556 · Mar 17, 2006
Related Publication 20160002156A1 · Jan 7, 2016