Immunomodulating heterocyclic compounds

摘要

Compounds of formula (I) are inhibitors of CD80 and useful in immunomodulation therapy: wherein R₁ and R₃ independently represent H; F; CI; Br; -NO₂; -CN; C₁-C₆ alkyl optionally substituted by F or Cl; or C₁-C₆ alkoxy optionally substituted by F; R₄ represents a carboxylic acid group (-COOH) or an ester thereof, or -C(-O)NR₆R₇, -NR₇C(-O)R₆, -NR₇C(-O)OR₆, -NHC(-O)NR₇R₆ or -NHC(-S)NR₇R₆ wherein R₆ represents H, or a radical of formula -(Alk)_m-Q wherein m is 0 or 1, Alk is an optionally substituted divalent straight or branched C₁-C₁₂ alkylene, or C₂-C₁₂ alkenylene, or C₂-C₁₂ alkynylene radical or a divalent C₃-C₁₂ carbocyclic radical, any of which radicals may contain one or more -O-, -S- or -N(R₈)- links wherein R₈, represents H or C₁-C₄ alkyl, C₃-C₄ alkenyl, C₃-C₄ alkynyl, or C₃-C₆ cycloalkyl, and Q represents H; -NR₉R₁₀ wherein R₉ and R₁₀ independently represents H; C₁-C₄ alkyl; C₃-C₄ alkenyl; C₃-C₄ alkynyl; C₃-C₆ cycloalkyl; an ester group; an optionally substituted carbocyclic or heterocyclic group; or R₉ and R₁₀ form a ring when taken together with the nitrogen to which they are attached, which ring is optionally substituted; and R₇ represents H or C₁-C₆ alkyl; or when taken together with the atom or atoms to which they are attached R₆ and R₇ form an optionally substituted monocyclic heterocyclic ring having 5, 6 or 7 ring atoms; and X represents a bond or a divalent radical of formula -(Z)_n-(Alk)- or -(Alk)-(Z)_n- wherein Z represents -O-, -S- or -NH-, Alk is as defined in relation to R₆, and n is 0 or 1.