发明授权
US6034082A 5-azabicyclo(3.1.0)hexylalkyl-2-piperiodones and --glutarimides as neurokinin receptor antagonists 失效
5-氮杂二环(3.1.0)己基烷基-2-哌啶酮和γ-谷氨酰胺作为神经激肽受体拮抗剂

5-azabicyclo(3.1.0)hexylalkyl-2-piperiodones and --glutarimides as
neurokinin receptor antagonists
摘要:
Compounds of formula (I) ##STR1## and salts thereof, wherein: R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4)alky aryl or aryl(C.sub.1 -C.sub.4)alkyl; wherein the C.sub.1 -C.sub.6 alkyl group is optionally substituted by fluorine and the C.sub.3 -C.sub.7 cycloalkyl or C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.4)alkyl group is optionally substituted in the cycloalkyl ring by up to two substituents each independently selected from halo, C.sub.1 -C.sub.4 alkoxy or halo(C.sub.1 -C.sub.4)alkoxy; R.sup.2 is phenyl optionally substituted with one or two halo substituents or is indolyl, thienyl, benzothienyl or naphthyl; R.sup.3 is NH.sub.2,--NR.sup.4 SO.sub.2 (C.sub.1 -C.sub.6 alkyl), --NR.sup.4 SO.sub.2 aryl, --NR.sup.4 SO.sub.2 N(R.sup.4).sub.2, NR.sup.4 CO(C.sub.1 -C.sub.6 alkyl), --NR.sup.4 CO aryl or a group or formula (a) ##STR2## wherein W is O, NR.sup.5, CH(OH), CHCO.sub.2 H, CHN(R.sup.4).sub.2, CHF, CF.sub.2, C.dbd.O or CH.sub.2 ; R.sup.4 is H or C.sub.1 -C.sub.6 alkyl; R.sup.5 is H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkyl, C.sub.2 -C.sub.6 alkanoyl, C.sub.4 -C.sub.8 cycloalkanoly, C.sub.3 -C.sub.7 cycloalkyl(C.sub.2 -C.sub.6)alkanoyl, aryl CO--, C.sub.1 -C.sub.6 alkylSO.sub.2 --, (R.sup.4).sub.2 NSO.sub.2 --, C.sub.3 -C.sub.7 cycloalkylSO.sub.2 --, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkyl-SO.sub.2 --, or arylSO.sub.2 --; X is CH.sub.2 or C.dbd.O; m is 0, 1 or 2 with the proviso that m is not O when W is NR.sup.5, C.dbd.O, or O; and n is an integer of from 1 to 4. These compounds are neurokinin receptor antagonists of utility in the treatment of a variety of medical conditions including urinary incontinence, asthma and related conditions.
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