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US 11,044,931 B2Granted
Low molecular weight modulators of the cold menthol receptor TRPM8 and use thereof
AssigneeBASF SE
InventorsThomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel, Ralf Pelzer
Life of this patent
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Abstract
The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.
Claims10
A substance, wherein the substance is a modulator for use as a mediator of the TRMP8 receptor and is a compound selected from the group consisting of:
- a) compounds of the general formula IA:
- in which:
- a is a C—C single bond or a C—C double bond,
- W is N or CH,
- X and Z, independently of one another, are —O—, —S—, —NR18—, —S(═O)—, or —S(═O)2—,
- Y is selected from straight-chain or branched C1-C8-alkylene groups which optionally carry 1, 2, 3 or 4 identical or different substituents which are selected from NH2, OH, SH, halogen or straight-chain or branched C1-C6-alkoxy groups;
- or X—Y—Z, together with the carbon atom to which they are bonded, form a keto group,
- R11 to R18, independently of one another, are selected from:
- H;
- aryl;
- straight-chain or branched, optionally mono- or polyunsaturated C1-C6-alkyl groups which optionally carry 1, 2, 3 or 4 identical or different substituents which are selected from oxo groups (═O), NH2, OH, SH, halogen or straight-chain or branched C1-C6-alkoxy groups;
- and straight-chain or branched C1-C6-alkyloxy groups which optionally carry 1, 2, 3 or 4 identical or different substituents which are selected from NH2, OH, SH, halogen or straight-chain or branched C1-C6-alkoxy groups;
- or
- R11-R12, together with the carbon atoms to which they are bonded, form a 4-, 5-, 6- or 7-membered, saturated or mono- or polyunsaturated, carbocyclic ring which optionally carries 1, 2, 3, 4 or 5 identical or different substituents which are selected from straight-chain or branched C1-C6-alkyl groups, and oxo groups (═O);
- or
- b) compounds of the general formula IB;
- in which:
- b is a C—C single bond or a C—C double bond,
- V is —CH2— or carbonyl;
- W, X, Y, Z and R11 to R18 have the meanings given above;
- U is —CH2— or —O—;
- and
- where U and V are not simultaneously —CH2—;
- or
- c) of the general formula IC:
- a, X, Y, Z and R11 to R18 have the meanings given above;
- U is —CH2— or a chemical bond;
- and V is —CH2— or carbonyl;
- where U and V are optionally not simultaneously —CH2—;
- wherein the modulator is not
27 more elements
Dependencies are inferred from the claim text.