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US 11,046,662 B2Granted
2-aryl-4-hydroxy-1,3-thiazole derivatives useful as TRPM8-inhibitors in treatment of neuralgia, pain, COPD and asthma
AssigneeDompé Farmaceutici S.P.A.
InventorsAndrea Aramini, Gianluca Bianchini, Laura Brandolini, Andrea Beccari, Samuele Lillini, Giuseppe Nano
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Abstract
The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I). The compounds of the invention are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exacerbated respiratory disorders and urological disorders.
Claims3
A compound of formula (I):
- wherein
- X is oxygen, sulphur, NH, NOH, or NOMe;
- R is a group selected from the group consisting of 3-fluorophenyl, 4-fluorophenyl, 2-bromophenyl, 3-bromophenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-hydroxyphenyl, 3-hydroxyphenyl, 4-hydroxyphenyl, 3-aminophenyl, 4-aminophenyl, 3-methylaminophenyl, 4-methylaminophenyl, thiophen-2yl, 1,2,4-oxadiazol-3yl and 1,2-oxazol-5yl;
- or R is a group selected from the group consisting of furanyl, pyrrolyl, imidazolyl and pyrazolyl, optionally substituted by one or more substituents selected from the group consisting of:
- hydrogen and
- linear or branched C1-C6 alkyl;
- R1 is a group selected from the group consisting of:
- linear or branched C2-C6 alkyl,
- (CH2)m—OR2, wherein m is an integer between 1 and 3 and R2 is selected from hydrogen and linear C1-C3 alkyl,
- C3-C6 cycloalkyl, and
- N(R3)OR4, wherein R3 and R4 are independently hydrogen or linear or branched C1-C3 alkyl, or a pharmaceutically acceptable salt thereof.
8 more elements
Dependencies are inferred from the claim text.