GB9601680D0 — Therapeutic agents

USPTO Abstract

Compounds of the formula: <CHEM> wherein: X is O, NH or NR<1>; R<1> 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; R<2> is phenyl optionally substituted with one or two halo substituents, indolyl or thienyl; R<3> is NH2, -NR<4> SO2(C1-C6 alkyl), -NR<4>SO2 aryl, -NR<4>CO(C1-C6 alkyl), -NR<4>CO aryl or a 5 to 7-membered N-linked cyclic group incorporating W in the ring wherein W is O, NR<5>, CH(OH), CHCO2H, CHN(R<4>)2, CHF, CF2, C = O or CH2; R<4> is H or C1-C6 alkyl; R<5> 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-, C3-C7 cycloalkyl SO2-, C3-C7 cycloalkyl(C1-C6)alkyl SO2-, aryl-SO2- or (R<6>)2NSO2-, wherein each R<6> is independently H or C1-C4 alkyl or the two groups may be joined to form with the nitrogen atom to which they are attached, a pyrrolidinyl, piperidino, morphlino or piperazinyl group; m is O, 1 or 2 with the proviso that m is not O when W is NR<5>, 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.