| abstract |
Quinoline derivatives of formula (1) or a pharmaceutically acceptable salt or hydrate, wherein: R1 is H or alkyl; R2 is -R8R9; R8 is a single bond or C1-3 alkyl, optionally substituted one or more times with hydroxy; R9 is aryl or cycloalkyl or heteroaryl, optionally substituted one or more times with hydroxy, alkoxy, or alkoxyalkyl; R3 is H or alkyl or cycloalkyl or cycloalkylalkyl, optionally substituted one or more times with hydroxy or with one or more fluorine atoms; R4 is -NR10R11; R10 and R11 are independently selected from H or alkyl, or R10 and R11 together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocycle ring comprising 3-8 ring members, whose heterocycle ring is not substituted or is substituted one or more times with one or more R12 substituents; R12 is oxo or -R13R14R15, where R13 is a single bond or alkyl; R14 is OC (O) or C (O) O; and R15 is H or alkyl; R5 is an alkyl, cycloalkyl, cycloalkylalkyl, aryl, or aromatic heterocycle group alone or with a fused ring, whose group is not substituted or is substituted one or more times with one or more substituents selected from halogen such as fluorine, alkyl or halogenoalkyl such as fluoroalkyl; R6 represents H or up to 3 substituents independently selected from the list consisting of alkyl, alkenyl, aryl, alkoxy or one of its hydroxylated derivatives, hydroxy, halogen, nitro, cyano, carboxy, carboxyamido, sulfonamido, alkoxycarbonyl, halogenoalkyl such as trifluoromethyl, acyloxy, amino, mono- or di-alkylamino, alkoxyamido, alkoxycarboxylate or one of its esterified derivatives; R7 is H or halogen; a is 1-6; and any of R1, R3, R5, R8, R9, R10, R11 and R12 may optionally be substituted one or more times with halogen, hydroxy, amino, cyano, nitro, carboxy or oxo; with the proviso that the compound is not a compound in which R7 represents H, R5 represents unsubstituted phenyl, and R1, R2, R3, R4, R6 are already selected from one of the combinations indicated in Table 1. Said compounds they are non-peptide antagonists of the NK-2 and NK-3 receptors and are therefore useful for treating and preventing a wide variety of clinical conditions characterized by overstimulation of said receptors. Methods for the preparation of said compounds, pharmaceutical compositions comprising said compounds, and the use thereof in the manufacture of medicaments are also disclosed. |