IP Library Granted Patent US 9,045,505
Granted Patent B2
US 9,045,505 · App. 12/732,909 · Granted Jun 2, 2015

Nitric oxide donors

View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,045,505
App. No.
12/732,909
Granted
Jun 2, 2015
Kind
B2
Abstract

The invention relates to novel NO donors which are targeted to the mitochondria. The NO donor compounds of the invention allow NO to be selectively provided to the mitochondria.

Claims (26)

1. A compound comprising a lipophilic cation linked by a linker group to a thionitrite moiety, wherein the compound has the structure of the general formula I and the lipophilic cation is capable of mitochondrially targeting the thionitrite moiety,

wherein L is the linker group and X − is an anion, and the linker group is selected from the group consisting of

(a) (C 1-30 ) alkylene,

(b) (C 1-x ) alkylene-NR—(C 1-y ) alkylene, wherein R is H, alkyl, or aryl,

(c) (C 1-x ) alkylene-NR—C(═O)—(C 1-y ) alkylene, wherein R is H, alkyl, or aryl,

(d) (C 1-x ) alkylene-C(═O)—NR—(C 1-y ) alkylene, wherein R is H, alkyl, or aryl,

(e) (C 1-x ) alkylene-O—(C 1-y )alkylene,

(f) (C 1-x ) alkylene-O—C(═O)—(C 1-y ) alkylene,

(g) (C 1-x ) alkylene-S—(C 1-y ) alkylene, or

(h) (C 1-x ) alkylene-aryl(C 1-y ) alkylene,

wherein x +y =30; and wherein each alkylene is optionally substituted with one or more functional groups independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthio, alkylsulfinyl, alkylsulfonyl, carboxyalkyl, cyano, oxy, amino, alkylamino, aminocarbonyl, alkoxycarbonyl, aryloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, aralkylaminocarbonyl, alkylcarbonylamino, arylcarbonylamino, aralkylcarbonylamino, alkylcarbonyl, heterocyclocarbonyl, aminosulfonyl, alkylaminosulfonyl, alkylsulfonyl, and heterocyclosulfonyl, or the substituent groups of adjacent carbon atoms in the linker group can be taken together with the carbon atoms to which they are attached to form a carbocycle or a heterocycle.

2. A compound of claim 1 wherein the anion is an anion derived from an acid selected from the group comprising hydrochloric, hydrobromic, hydroiodic, sulfuric, sulfurous, nitric, nitrous, phosphoric, phosphorous, alkylsulfonic or arylsulfonic acid.

3. A compound of claim 1 wherein the compound is of formula (II)

wherein n is from 0 to 27X, is an anion and R 1 and R 2 are independently selected from the group comprising hydrogen, alkyl and aryl.

4. A compound of claim 1 wherein the compound is of formula (III)

wherein n is from 0 to 27, X − is an anion and R 1 , R 2 , R 3 and R 4 are independently selected from the group comprising hydrogen, alkyl and aryl.

5. A compound of claim 1 wherein the compound is of formula (IV)

wherein n is from 0 to 27X, is an anion and R 1 , R 2 and R 3 are independently selected from the group comprising hydrogen, alkyl and aryl.

6. A compound of claim 1 wherein the compound is formula (V)

wherein n is from 0 to 27X, is an anion and R 1 , R 2 , R 3 , R 4 and R 5 are independently selected from the group comprising hydrogen, alkyl and aryl.

7. A compound of claim 1 wherein the compound is of formula (VI)

wherein n is from 0 to 27X, is an anion and R 1 , R 2 , R 3 and R 4 are independently selected from the group comprising hydrogen, alkyl and aryl.

8. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 with one or more pharmaceutically acceptable excipients, carriers or diluents.

9. A method for generating NO in the mitochondria of a subject comprising administering to the subject, a therapeutically effective amount of a compound of claim 1 or a pharmaceutical composition comprising same.

10. A method for S-nitrosylating proteins in the mitochondria of a subject comprising administering to the subject, a therapeutically effective amount of a compound of claim 1 or a pharmaceutical composition comprising same.

11. A compound selected from the group comprising:

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 2, 2018
From: MEDICAL RESEARCH COUNCIL
To: UNITED KINGDOM RESEARCH AND INNOVATION
Reel/Frame 046469/0108 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 10, 2017
From: UNIVERSITY OF OTAGO
To: MEDICAL RESEARCH COUNCIL
Reel/Frame 042954/0352 →