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US 11,597,702 B2Granted
Substituted pyrazoles FFA4/GPR120 receptor agonists
AssigneeGolgi Neurosciences S.R.L.
InventorsDomenica Torino, Francesco Piscitelli, Valentina Cusano, Rocco Vitalone, Andrew Griffin, Russell Thomas, Paolo Pevarello, Ali Munaim Yousif
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Abstract
Disclosed are compounds of formula (I) or a pharmaceutically acceptable salt thereof: These compounds have FFA4/GPR120 receptor (FFA4) agonistic properties. Also disclosed are pharmaceutical compositions including these compounds, chemical processes for preparing them and their use in the treatment or prophylaxis of diseases associated with FFA4 receptor activity in animals, in particular humans.
Claims9
A compound of formula (I) or a pharmaceutically acceptable salt thereof:
- including any stereochemically isomeric form thereof, wherein:
- X is a methylene group, unsubstituted or substituted by a methyl group or one or more halogen atoms;
- Y is selected from:
- —O—;
- —NR8—, wherein R8 is hydrogen or C1-C6 alkyl;
- —S—;
- —SO— and —SO2—;
- W is a single bond;
- Z is —CR9—, wherein R9 is hydrogen, halogen, C1-C6 alkyl, C1-C4 hydroxyalkyl;
- R1 is selected from hydrogen;
- C1-C6 alkyl and C3-C10 cycloalkyl;
- R2 is CN or trifluoromethyl;
- R3 is aryl;
- hetaryl;
- benzyl;
- C1-C4 alkyl or C3-C10 cycloalkyl;
- which can be unsubstituted or substituted by one or more substituents selected from halogen, C1-C4 alkyl (unsubstituted or substituted by halogen), C1-C4 alkyloxy (unsubstituted or substituted by halogens), CN and R12SO2—, wherein R12 is a C1-C6 alkyl or cycloalkyl;
- each of R4, R6 and R7 is independently selected from the group consisting of hydrogen;
- halogen;
- CN;
- C1-C6 alkyl (unsubstituted or substituted by halogen or hydroxyl);
- C1- C4 alkyloxy (unsubstituted or substituted by halogen or hydroxyl);
- —CONH2;
- —NHCOCH3 and —NO2;
- R5 is —(CH2)n—OH, wherein n is 1-3;
- or
- R6 and R7, taken together with the aromatic ring to which they are bound, form a group:
- with the proviso that the compound of formula (I) is not:
- 5-[(4-cyanophenoxy)methyl]-3-methyl-1-phenyl-pyrazole-4-carbonitrile,
- 5-[[2-chloro-4-(hydroxymethyl)phenoxy]methyl]3-methyl-1-phenyl-pyrazole-4-carbonitrile;
- 5-[(2-chloro-4-cyano-phenoxy)methyl]-3-methyl-1-phenyl-pyrazole-4-carbonitrile;
- and
- 3-methyl-5-(phenoxymethyl)-1-phenyl-pyrazole-4-carbonitrile.
30 more elements
Dependencies are inferred from the claim text.