Compounds useful as modulators of TRPM8

Patent metadata

Field	Value
Publication number	US-10016418-B2
Application number	US-201615205608-A
Country	US
Kind code	B2
Filing date	Jul 8, 2016
Priority date	Nov 5, 2010
Publication date	Jul 10, 2018
Grant date	Jul 10, 2018

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.

First claim

What is claimed is:

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.

Assignees

• Senomyx Inc
• Seaomyx Inc

Inventors

• Priest Chad
• Noncovich Alain
• Patron Andrew
• Ung Jane

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61P25/04

  Centrally acting analgesics, e.g. opioids · CPC title

• A61P25/02

  for peripheral neuropathies · CPC title