Quinoline-4-Carboxamide Derivatives as NK-3 and NK-2 Receptor Antagonists

摘要

Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: wherein: R₁ is H or C_1-6 alkyl; R₂ is aryl or C_3-7 cycloalkyl or heteroaryl; R₃ is H or C_1-3 alkyl, optionally substituted by one or more fluorines; R₄ is R₈R₉; R₈ is a single bond, C_1-6 alkyl, or aryl; R₉ is H, COO R₁₀, or NR₁₁R₁₂; R₁₀ is H or C_1-6 alkyl; R₁₁ and R₁₂ are independently selected from H and C_1-6 alkyl; R₅ is branched or linear C_1-6 alkyl, C_3-7 cycloalkyl, C_4-7 cycloalkylalkyl, aryl, or a single or fused ring aromatic heterocyclic group; R₆ represents H or up to three substituents independently selected from the list consisting of: C_1-6 alkyl, C_1-6 alkenyl, aryl, C_1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C_1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- or di-C_1-6 alkylamino; R₇ is H or halo; a is 1-6; and any of R₂, R₅, R₈, R₁₀, R₁₁ and R₁₂ may optionally be substituted one or more times by halo, hydroxy, amino, cyano, nitro, carboxy or oxo; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.