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US 7,919,624 B2Granted
VR1 vanilloid receptor antagonists with a iononic substructure
AssigneePharmeste S.R.L.
InventorsPier Giovanni Baraldi, Pier Andrea Borea, Pierangelo Geppetti, Maria Giovanna Pavani, Francesca Fruttarolo, Marcello Trevisani
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Abstract
The invention provides compounds of formula (I), wherein Y, R, n and X are as defined in the description, a process for their preparation and pharmaceutical compositions containing them. The compounds of formula (I) inhibit the Transient Receptor Potential Vanilloid 1 (TRPV1), which plays a pivotal role in the development of post-inflammatory analgesia, therefore they can be used as analgesic and anti-inflammatory drugs.
Claims27
A compound of formula (I):
- wherein:
- Y is a group of formula
- in which:
- R′ is selected from hydrogen, halogen, hydroxy, (C1-C6)alkyl, (C2-C6)alkenyl, (C3-C6)alkynyl, (C1-C6)alkoxy, (C1-C6)alkylamino, phenyl, naphthyl, phenoxy, naphthoxy or phenylamino;
- R is methyl or hydrogen;
- n is 0 or 1;
- X is selected from phenyl, pyridinyl, naphthyl, quinolinyl and isoquinolinyl;
- with the exclusion of the following compounds:
5 more elements
Dependencies are inferred from the claim text.