(57) (I) [summary] The present invention can be represented by the general formula: R 1 Z 1 ─Het─L 1 ─Ar 1 ─L 2 ─Y (I) [formula, Het, selected from O, N or S saturated and substituted and containing one heteroatom, optionally at least a is an 8 to 10 membered bicyclic ring fully unsaturated or partially saturated R l is aryl, heteroaryl which is optionally substituted There aryl, alkyl, alkenyl, alkynyl, a cycloalkyl or heterocycloalkyl Z 1 represents (O) n S or 4, O direct bond, alkylene chain, NR are L 1, -R 5 -R 6 - join (where alkylene, and is a alkynylene or alkenylene R 6 R 5 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, -C (= Z 3) -NR 4 -, - NR 4 -C (= Z 3) -, - Z 3 -, - C (= O) -, - C (= NOR 4) -, - NR 4 -, - NR 4 -C (= Z 3) -NR 4 -, - SO 2 -NR 4 -, - NR 4 -SO 2 -, - O-C (= O) -, - C (= O) -O -, - NR 4 -C (= O) -O- or -O-C (= O) -NR 4 - be) a L 2 is a direct bond alkylene, alkenylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryldiyl, heterocycloalkylene it is optionally substituted arylene or bond - [C (= O) -N (R 9) -C (R 4) (R l0)]p - join -Z 4 -R 11 - bond -C (= O) -CH 2 Y is, biological isostere of acid or carboxy and represents a bond - -L 3 -L 4 -L 5 or binding - -R 11 -Z 4 -R 11 join - (= O) -C solvates the compounds as well as pharmaceutically acceptable salts and prodrugs thereof and N- oxide prodrugs and their N- oxide active compounds, the corresponding physiologically expressed it in) represents the body about (eg hydrates). The compounds have the ability useful pharmacological properties, to modulate the interaction with the integrin VLA-4 (α4β1) of fibronectin and VCAM-1 in particular.本発明は、一般式(I):R1Z1─Het─L1─Ar1─L2─Y (I)[式中、Hetは、O、SまたはNから選択される少なくとも1個のヘテロ原子を含有する、場合により置換された飽和、部分的飽和または完全不飽和の8~10員二環式環でありRlは、場合により置換されたアリール、ヘテロアリール、アルキル、アルケニル、アルキニル、シクロアルキルまたはヘテロシクロアルキルでありZ1は、直接結合、アルキレン鎖、NR4、OまたはS(O)nを表しL1は、-R5-R6-結合(ここでR5はアルキレン、アルケニレンまたはアルキニレンであり、そしてR6は直接結合、シクロアルキレン、ヘテロシクロアルキレン、アリーレン、ヘテロアリールジイル、-C(=
