Substituted 1-phenyl-3-pyrazolecarboxamides active on neurotensin receptors, their preparation and pharmaceutical compositions containing them
The invention relates to compounds of the formula I, in which: -R1 represents a group chosen from: -T-CN; -C(NH2)=NOH; -C(=NOH)NH(CH2)rNR5R6; -T-C(NR12R13)=NR14; -C(NH2)=NO(CH2)rNR5R6; -T-CONRaRb; -T-CONR7Rc; -Y-CO2R7; -ORd; -T-NR5R6, on condition that R5 and R6 do not simultaneously represent hydro...
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Zusammenfassung: | The invention relates to compounds of the formula I, in which: -R1 represents a group chosen from: -T-CN; -C(NH2)=NOH; -C(=NOH)NH(CH2)rNR5R6; -T-C(NR12R13)=NR14; -C(NH2)=NO(CH2)rNR5R6; -T-CONRaRb; -T-CONR7Rc; -Y-CO2R7; -ORd; -T-NR5R6, on condition that R5 and R6 do not simultaneously represent hydrogen when T represents a direct bond; -T-N(R7)CORe; -SO2NRaRb; -T-N(R7)SO2R'7; -T-NR27R28; -R2 and R3 each independently represent hydrogen, a (C1-C6) alkyl, a (C3-C8)cycloalkylmethyl, a (C3-C8)-cycloalkyl, a halogen, a nitro, a trifluoromethyl, a group -OR4, a group -NR5R6, a l-pyrrolyl, a cyano, a carbamoyl; -or R2 and R3 together constitute a trimethylene, tetramethylene or pentamethylene group; -R4 represents hydrogen; a (C1-C6)alkyl; a (C3-C4)-alkenyl; a (C3-C8)cycloalkylene; a (C3-C8)cyclo-alkylmethyl; a (C1-C4)alkoxy(C1-C4)alkylene; a benzyl; - the group -NH-AA(OH) represents the residue of an amino acid formula II, where Xa is hydrogen and X'a is hydrogen, a (C1-C5)-alkyl or a non-aromatic C3-C15 carbocyclic radical; or alternatively, Xa and X'a, together with the carbon atom to which they are attached, form a non-aromatic C3-C15 carbocycle; its salts and its quaternary ammonium salts formed with acyclic or cyclic tertiary amines and its solvates. Application: Compounds having a great affinity for the neurokine receptors. |
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