5-AZABICYCLO(3.1.0)HEXYLALKYL-2-PIPERIDONES AND -GLUTARIMIDES AS NEUROKININ RECEPTOR ANTAGONISTS

摘要

Compounds of formula (I) and salts thereof, wherein: R1 is C1-C6 alkyl, C3-C7 cycloalkyl, C3-C7 cycloalkyl(C1-C4)alkyl, aryl or aryl(C1-C4)alkyl; wherein the C1-C6 alkyl group is optionally substituted by fluorine and the C3-C7 cycloalkyl or C3-C7 cycloalkyl(C1-C4)alkyl group is optionally substituted in the cycloalkyl ring by up to two substituents each independently selected from halo, C1-C4 alkoxy or halo(C1-C4)alkoxy; R2 is phenyl optionally substituted with one or two halo substituents or is indolyl, thienyl, benzothienyl or naphthyl; R3 is NH2, -NR4SO2(C1-C6 alkyl), -NR4SO2 aryl, -NR4SO2N(R4)2, -NR4CO(C1-C6 alkyl), -NR4CO aryl or a group or formula (a) wherein W is O, NR5, CH(OH), CHCO2H, CHN(R4)2, CHF, CF2, C=O or CH2; R4 is H or C1-C6 alkyl; R5 is H, C1-C6 alkyl, C3-C7 cycloalkyl, C3-C7 cycloalkyl(C1-C6)alkyl, C2-C6 alkanoyl, C4-C8 cycloalkanoyl, C3-C7 cycloalkyl(C2-C6)alkanoyl, aryl CO-, C1-C6 alkyl SO2-, (R4)2NSO2-, C3- C7 cycloalkyl SO2-, C3-C7 cycloalkyl(C1-C6)alkyl-SO2- or aryl SO2; X is CH2 or C=O; m is 0, 1 or 2 with the proviso that m is not O when W is NR5, C=O, or O; and n is an integer of from 1 to 4, are neurokinin receptor antagonists of utility in the treatment of a variety of medical conditions including urinary incontinence, asthma and related conditions.