SUBSTITUTED PHENETHYLAMINE DERIVATIVES

摘要

The present invention has as its object providing substituted phenethylamine derivatives that function as a motilin receptor antagonist and which are useful as medicines. The invention provides compounds of Formula (1): <CHEM> wherein: Cy is a group of Formula (2): <CHEM> an optionally substituted heterocyclic ring, C3-7cycloalkyl or phenyl; R1, R2, R3, R4 and R5 are hydrogen, halogen, hydroxy, amino, trifluoromethyl or nitrile and at least one of R1, R2, R3, R4 and R5 is halogen, trifluoromethyl or nitrile; R6 is hydrogen, optionally substituted straight-chained or branched C1-3alkyl, amino or hydroxy; R7 is hydrogen, optionally substituted straight-chained or branched C1-3alkyl, optionally substituted amino or hydroxy; R8 is hydrogen, methyl or ethyl; R9 is optionally substituted straight-chained or branched C1-6alkyl, optionally substituted straight-chained or branched C2-6alkenyl, optionally substituted straightchained or branched C2-6alkynyl, C3-7cycloalkyl or optionally substituted phenyl; R20 is hydrogen or straight-chained or branched C1- 3alkyl or R9 and R20 may together form C3-7cycloalkyl; R10 is hydrogen or straight-chained or branched C1- 3alkyl; R11 is hydrogen, optionally substituted straight-chained or branched C1-3alkyl, -CO-N(R14)R15, carboxyl or an optionally substituted heterocyclic ring; R12 is hydroxy or -OR16; R13 is hydrogen, straight-chained or branched C1- 6alkyl, straight-chained or branched C2-6alkenyl, straight-chained or branched C2-6alkynyl or a group of Formula (3): <CHEM> R14 and R15, which may be the same or different, are hydrogen, optionally substituted straight-chained or branched C1-4alkyl, C3-7cycloalkyl, straight-chained or branched C1-4alkyloxy, straight-chained or branched C1-4alkylsulfonyl or a heterocyclic ring, or R14 and R15, as -N(R14)R15, form optionally substituted 3- to 7-membered cyclic amine; R16 is straight-chained C1-4alkyl; R17 is hydrogen or methyl; R18 and R19 together form cycloalkyl or C3-7cycloalkenyl ; X is carbonyl or methylene; Y is carbonyl or methylene; provided that when Cy is 3-indolyl, (i) R11 is an optionally substituted heterocyclic ring; or (ii) R6 is hydrogen, R7 is amino, R8 is methyl, R9 is isopropyl, R20 is hydrogen, R10 is methyl, R11 is carbamoyl, R12 is hydroxy, R13 is tert-butyl, X is carbonyl and Y is carbonyl, and when Cy is cyclohexyl or phenyl, R11 is an optionally substituted heterocyclic ring; or a hydrate or pharmaceutically acceptable salt thereof.