HETEROCYCLIC COMPOUNDS, USEFUL AS ALLOSTERIC EFFECTORS AT MUSCARINIC RECEPTORS

摘要

Compounds of formula (I) wherein Z represents a methylene group, a methine group, a group of formula ?NH or a group of formula ?N-, and W represents a methylene group, a methine group, a sulfur atom or a group of formula .mu.S?(O)¿v?, where v is 1 or 2; ... is a single or double bond; at least one of Y?1¿, Y?2¿, Y?3¿ and Y?4¿ represents a carboxyl group, a sulfonamide group or a group of formula -(A)¿p?-B?1¿-T?1¿, wherein A is S or O, T?1¿ is a carboxyl group, a thiocarboxy group, a dithiocarboxy group, a sulfonamide group or a tetrazolyl group, B?1¿ is a bond, an optionally substituted alkylene group and p is 0 or 1; the rest of Y?1¿, Y?2¿, Y?3¿ and Y?4¿ are the same or different and are H, halogen, nitro, OH, SH, NH¿2?, optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, aryl, aralkyloxy, aralkylthio and Y?1¿ + Y?2¿ may together be a lactone or keto; one of R?1¿ and R?2¿ is H, alkyl, alkanoyl, aryl, arylcarbonyl, aralkyl, carboxyl, sulfonamide or a group of formula -(O)¿q?-B?2¿-T?2¿, wherein T?2¿ is COOH, sulfonamide or tetrazolyl, B?2¿ is an optionally substituted alkylene, and q is 0 or 1; the other of R?1¿ and R?2¿ is H, alkyl, aryl or aralkyl, or R?1¿ and R?2¿ together represent a group of formula (Ib'), wherein ¢R?10¿, R?11¿ and R?12¿ are the same or different and each is H, OH, halogen, haloalkyl, optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl or alkylsulfonyl!; R?3¿ is H or an amino protecting group; and pharmaceutically acceptable salts and esters thereof are allosteric effectors at muscarinic receptors, and are useful in the treatment and prophylaxis of disorders associated with muscarinic receptors.