abstract |
REFERS TO COMPOUNDS WITH ALKINE STRUCTURE OF FORMULA (I), WHERE R1 AND R2 ARE INDEPENDENTLY H, ALKYL (C1-C6), CYCLOALKYL (C3-C7), HYDROXY-ALKYL (C2-C4), HYDROXYCYCLOALKYL (C3-C7) ), AMONG OTHERS OR TOGETHER WITH THE N TO WHICH THEY ARE UNITED, THEY FORM A SELECTED HETEROCICLE OF PYRROLIDINE, PIPERIDINE, 8-AZA-BICYCLE [3,2,1] OCTANE, PIPERAZINE, WHERE THE FREE IMINA FUNCTION IS REPLACED WITH R13; AND MORPHOLIN; X IS AN ALKENYLENE OR ALKYNYLENE BRIDGE (C3-C6) OPTIONALLY SUBSTITUTED BY F, Cl, OH, ALKYL (C1-C3) AND CYCLOPROPYL, OR IS AN ETOXY OR ETHYLINIMINE BRIDGE, WHERE THE IMINO GROUP IS OPTIONALLY REPLACED; W AND Z ARE INDEPENDENTLY SINGLE LINK OR AN ALKYLENE BRIDGE (C1-C2); AND, TO THEY ARE INDEPENDENTLY A PHENYL, PYRIDINYL, PYRIMIDYL, PIPERAZINYL, BIVALENT CYCLE, AMONG OTHERS, OPTIONALLY REPLACED WITH R20; B IS Y OR A, WITH PHENYL OR ALKYL (C1-C6), CYCLOALKYL (C3-C7), AMONG OTHERS being preferred. PREFERRED COMPOUNDS ARE: 2 - ((E) -3- {4- [5- (4-CHLORO-PHENYL) -PYRIDIN-2-ILETINYL] -PHENYL} -ALYLAMINO) -PROPAN-1,3-DIOL, (R ) -5- (4-CHLORO-PHENYL) -2- {4- [2- (4-METHYL-PIPERIDIN-1-IL) -PROPOXY-PHENYLETINYL} -PYRIDINE, (R) -1 '- {4- [ 5- (4-CHLORO-PHENYL) -PYRIDIN-2-ILETINYL] -PHENYL} -4-METHYL- [1,3 '] - BIPIPERIDINYL, AMONG OTHERS. IT ALSO REFERS TO A PREPARATION PROCEDURE AND A PHARMACEUTICAL COMPOSITION. THESE COMPOUNDS ARE ANTAGONISTS OF MCH RECEPTORS (MELANIN CONCENTRATING HORMONE) SO THEY ARE APPROPRIATE IN THE TREATMENT OF METABOLIC AND / OR FOOD DISORDERS |