ALKOXY-SUBSTITUTED DIHYDROBENZOPYRAN-2-CARBOXYLATE DERIVATIVES

摘要

This invention encompasses compounds of Formula 1 and the pharmaceutically acceptable salts thereof. wherein R<1> represents alkyl having 2-6 carbon atoms; R<2> represents methyl or ethyl; R<3> represents alkyl having 1 to 5 carbon atoms; W represents (CH2)x where x is 2 to 7, alkylene having 2 to 7 carbon atoms, alkenylene having 3 to 7 carbon atoms, alkynylene having 3 to 7 carbon atoms, or cyclopentyl; R<4> represents hydrogen, alkyl having 2-5 carbon atoms, alkenyl having 2 to 5 carbon atoms, or alkynyl having 2 to 5 carbon atoms; Q represents oxygen or CH2; B represents CH2, C=O or CH-OH; R<5> represents hydrogen, alkyl having 1 to 6 carbon atoms, or R<5> and R<6> together optionally represent a carbon to carbon bond; or R<5> represents alkanoyl having 2 to 4 carbon atoms, carboxy, alkoxycarbonyl, or (CH2)y-CO2R<8> wherein y is 0 to 4 and R<8> is hydrogen or alkyl having 1 to 6 carbon atoms; and A represents -Z-CO2R<7> or -Z-COR<9>R<1><0> wherein R<7> represents hydrogen or alkyl having 1 to 6 carbon atoms, R<9>, R<1><0>, represent hydrogen, alkyl having 1 to 6 carbon atoms, or cycloalkyl having 3 to 6 carbon atoms or NR<9>R<1><0> form a heterocyclic ring, and wherein Z is absent or represents straight or branched chain alkylene or alkenylene having up to 6 carbon atoms. These compounds are selective antagonists of leukotriene B4(LTB4) with little or no antagonism of leukotriene D4 (LTD4) and are useful anti-inflammatory agents for treating inflammatory bowel disease, rheumatoid arthritis, gout and psoriasis.