IP Library Granted Patent US 10,206,922
Granted Patent B2
US 10,206,922 · App. 15/665,595 · Granted Feb 19, 2019

Substituted pyrimidines for treatment of chronic cough, neuronal hypersensitivity underlying chronic cough, neuronal hypersensitivity underlying sub-acute cough and neuronal hypersensitivity underlying acute cough

Inventors: Anthony P. Ford (Palo Alto, CA); Bruce G. McCarthy (San Francisco, CA)
Assignee: Afferent Pharmaceuticals, Inc.
A61K31/505A61K9/0043A61K9/0053A61K9/0095A61K9/10A61K9/107A61K9/20A61K9/2013A61K9/2018A61K9/2027A61K9/2054A61K9/4858C07D239/48A61K47/26
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Quick Facts
Patent No.
US 10,206,922
App. No.
15/665,595
Granted
Feb 19, 2019
Kind
B2
Abstract

Methods for treating cough, chronic cough and urges to cough associated with respiratory diseases with a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 are as defined herein.

Claims (31)

1. A method for treating chronic cough in a patient, the method comprising administering to the patient in need thereof an effective amount of a compound of Formula (I):

or a pharmaceutically acceptable salt thereof,

wherein:

R 1 is hydrogen or C 1 -C 6 alkyl; and

R 2 is alkyl, alkenyl, alkynyl, amino, aminosulfonyl, halo, amido, haloalkyl, alkoxy, hydroxy, haloalkoxy, nitro, hydroxyalkyl, alkoxyalkyl, hydroxyalkoxy, alkynylalkoxy, alkylsulfonyl, arylsulfonyl, carboxyalkyl, cyano or alkylcarbonyl.

2. The method of claim 1 , wherein the chronic cough is idiopathic chronic cough or treatment resistant chronic cough.

3. The method of claim 1 , wherein the chronic cough is daytime chronic cough.

4. The method of claim 1 , wherein the compound of Formula (I), or a pharmaceutically acceptable salt thereof, is administered for about two weeks.

5. The method of claim 1 , wherein R 1 is hydrogen or methyl; and R 2 is alkyl, aminosulfonyl or alkylsulfonyl.

6. The method of claim 1 , wherein R 2 is aminosulfonyl or alkylsulfonyl.

7. The method of claim 1 , wherein the compound of Formula (I) is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

8. The method of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

9. The method of claim 1 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

10. A method for treating neuronal hypersensitivity underlying acute cough, neuronal hypersensitivity underlying sub-acute cough, or neuronal hypersensitivity underlying chronic cough in a patient, the method comprising administering to the patient in need thereof an effective amount of a compound of Formula (I):

or a pharmaceutically acceptable salt thereof,

wherein:

R 1 is hydrogen or C 1 -C 6 alkyl; and

R 2 is alkyl, alkenyl, amino, aminosulfonyl, halo, amido, haloalkyl, alkoxy, hydroxy, haloalkoxy, nitro, hydroxyalkyl, alkoxyalkyl, hydroxyalkoxy, alkynylalkoxy, alkylsulfonyl, arylsulfonyl, carboxyalkyl, cyano or alkylcarbonyl.

11. The method of claim 10 , wherein the chronic cough is idiopathic chronic cough or treatment resistant chronic cough.

12. The method of claim 10 , wherein the chronic cough is daytime chronic cough.

13. The method of claim 10 , wherein the compound of Formula (I), or a pharmaceutically acceptable salt thereof, is administered for about two weeks.

14. The method of claim 10 , wherein the compound is:

15. A method for treating chronic cough in a patient, the method comprising administering to the patient in need thereof an effective amount of a pharmaceutically acceptable salt of the following compound:

16. The method of claim 15 , wherein the chronic cough is refractory chronic cough.

17. The method of claim 15 , wherein the chronic cough is reduced by about 75%.

18. A method for treating neuronal hypersensitivity underlying acute cough, neuronal hypersensitivity underlying sub-acute cough, or neuronal hypersensitivity underlying chronic cough in a patient, the method comprising administering to the patient in need thereof an effective amount of a pharmaceutically acceptable salt of the following compound:

19. The method of claim 18 , wherein the neuronal hypersensitivity underlying chronic cough is refractory chronic cough.

20. The method of claim 18 , wherein the neuronal hypersensitivity underlying chronic cough is reduced by about 75%.

Assignments (4)
CORRECTIVE ASSIGNMENT TO CORRECT THE APPLICATION NUMBER 17197705 PREVIOUSLY RECORDED AT REEL: 061574 FRAME: 0579. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT . Recorded Dec 1, 2022
From: AFFERENT PHARMACEUTICALS, INC.
To: AFFERENT PHARMACEUTICALS, INC.
Reel/Frame 062036/0001 →
CHANGE OF ADDRESS Recorded Sep 30, 2022
From: AFFERENT PHARMACEUTICALS, INC.
To: AFFERENT PHARMACEUTICALS, INC.
Reel/Frame 061574/0579 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 24, 2018
From: FORD, ANTHONY P.; MCCARTHY, BRUCE G.
To: AFFERENT PHARMACEUTICALS INC.
Reel/Frame 045894/0969 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 24, 2018
From: FORD, ANTHONY P.; MCCARTHY, BRUCE G.
To: AFFERENT PHARMACEUTICALS, INC.
Reel/Frame 045895/0521 →
Continuity (4)
Continuation 15013798 · Feb 2, 2016
Continuation 14466713 · Aug 22, 2014
Provisional Application 61869174 · Aug 23, 2013
Related Publication 20170326142A1 · Nov 16, 2017