IP Library Granted Patent US 10,016,418
Granted Patent B2
US 10,016,418 · App. 15/205,608 · Granted Jul 10, 2018

Compounds useful as modulators of TRPM8

Inventors: Chad Priest (Leucadia, CA); Alain Noncovich (San Diego, CA); Andrew Patron (San Marcos, CA); Jane Ung (San Diego, CA)
Assignee: Seaomyx, Inc.
A61K31/497A01N37/18A01N43/10A01N43/40A01N43/56A01N43/60A01N43/76A01N43/78A01N43/80A01N43/90A23L27/88A23L33/10A61K8/42A61K8/49A61K8/494A61K8/4926A61K8/4973A61K8/4986A61K8/69A61K31/165A61K31/381A61K31/415A61K31/4155A61K31/422A61K31/426A61K31/437A61K31/4409A61K31/4436A61Q19/00C07C233/11C07C235/20C07C235/24C07C235/34C07D213/40C07D213/75C07D231/40C07D277/28C07D307/52C07D333/20C07D333/24C07D333/32C07D405/12C07D407/12C07D409/12C07D409/14C07D413/12C07D417/12C07D471/04A23V2002/00A61K2800/10A61K2800/40A61Q1/02A61Q5/02A61Q5/12A61Q9/02A61Q11/00A61Q15/00A61Q17/02A61Q17/04A61Q19/001A61Q19/10C07C2601/14
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Quick Facts
Patent No.
US 10,016,418
App. No.
15/205,608
Granted
Jul 10, 2018
Kind
B2
Abstract

The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.

Claims (37)

1. A composition comprising a compound having structural Formula (II):

or a salt or solvate thereof;

wherein Ar is optionally substituted aryl, optionally substituted carbocyclyl, or optionally substituted pyrrolyl, furanyl, thienyl, pyrazolyl, triazolyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, pyridyl, pyrimidyl, or triazinyl;

X 1 -X 2 is O—CR 2a R 2b , or CR 5 ═CR 6 ;

R 2a , R 2b , R 5 , and R 6 are independently hydrogen or lower alkyl;

Y is oxygen or sulfur;

Z is nitrogen or CR;

n is 0, 1, or 2;

R is hydrogen or lower alkyl;

R 1 is an optionally substituted group selected from the group consisting of pyrrolyl, furanyl, thienyl, and pyrazolyl; and

each R 2 is independently optionally substituted C 1 -C 6 alkyl, optionally substituted C 2 -C 6 alkenyl, C 1 -C 6 alkoxy, hydroxyl, halo, nitro, or cyano,

wherein each optional substituent is selected from the group consisting of C 1 -C 6 alkyl, alkenyl, C 1 -C 6 alkoxy, hydroxyl, halo, nitro, or cyano; or two substituents, together with the atoms to which they are attached, form an optionally substituted carbocyclyl or heterocyclyl containing one or more heteroatom(s) selected from nitrogen, oxygen, and sulfur; and

a carrier.

2. The composition of claim 1 , wherein Y is sulfur.

3. The composition of claim 1 , Z is nitrogen or CR.

4. The composition of claim 1 , wherein n is 0.

5. The composition of claim 1 , wherein R 1 is an optionally substituted group selected from the group consisting of furanyl, thienyl, and pyrazolyl.

6. A composition comprising a compound, wherein the compound selected from the group consisting of:

or a salt or solvate thereof, and

a carrier.

7. A composition comprising a compound, wherein the compound selected from the group consisting of:

or a salt or solvate thereof, and

a carrier.

8. The composition of claim 1 , wherein the compound selected from the group consisting of:

or a salt or solvate thereof.

9. The composition of claim 1 , wherein the compound selected from the group consisting of:

or a salt or solvate thereof.

10. The composition of claim 1 , wherein the compound selected from the group consisting of:

or a salt or solvate thereof.

11. The composition of claim 10 , wherein the composition is an ingestible composition or personal care composition.

12. The composition of claim 11 , wherein the ingestible composition is a food or beverage.

13. The composition of claim 1 , wherein the composition is in form of a solid, semi-solid, plaster, solution, suspension, lotion, cream, foam, gel, paste, emulsion, or a combination thereof.

14. The composition of claim 1 , wherein the compound in the composition is in a concentration ranging from about 0.0001 ppm to 100,000 ppm.

15. The composition of claim 1 , wherein the compound in the composition is in a concentration ranging from about 1 ppm to 500 ppm.

16. The composition of claim 1 , which is a component of a textile product or a packaging material.

17. The composition of claim 1 , wherein the compound is:

or a salt or solvate thereof.

Assignments (2)
MERGER Recorded Oct 16, 2019
From: SENOMYX, INC.
To: FIRMENICH INCORPORATED
Reel/Frame 050733/0195 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 26, 2017
From: PRIEST, CHAD; NONCOVICH, ALAIN; PATRON, ANDREW; UNG, JANE
To: SENOMYX, INC.
Reel/Frame 042149/0680 →
Continuity (4)
Continuation 13883349
Provisional Application 61410634 · Nov 5, 2010
Provisional Application 61443490 · Feb 16, 2011
Related Publication 20160317532A1 · Nov 3, 2016