Pfizer Corporation

Allan Patrick Marchington

Donald Stuart Middleton

Alexander Roderick MacKenzie

Sandra Dora Meadows

Piperidone tachykinin antagonists

The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antagonists.

3-Azetidinylalkylpiperidines or -pyrrolidines as tachykinin antagonists

5-azabicyclo(3.1.0)hexylalkyl-2-piperiodones and --glutarimides as

The present invention provides compounds of the formula (I): ##STR1## and the pharmaceutically acceptable salts thereof, wherein R is C.sub.3 -C.sub.7 cycloalkyl, aryl or C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl being optionally substituted by fluoro, --COOH, --COO(C.sub.1 -C.sub.4) alkyl, C.sub.3 -C.sub.7 cycloalkyl, adamantyl, aryl or het.sup.1, and said C.sub.3 -C.sub.7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, fluoro, fluoro(C.sub.1 -C.sub.4) alkyl and fluoro(C.sub.1 -C.sub.4)alkoxy;

Azetidines

(Azetidin-1-ylalkyl) lactams as tachykinin antagonists

Compounds of the formula: ##STR1## wherein: X is O, NH or NR.sup.1 ; 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)alkyl, 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, indolyl or thienyl; 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 CO(C.sub.1 -C.sub.6 alkyl), --NR.sup.4 CO aryl or a 5 to 7-membered N-linked cyclic group incorporating W in the ring 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 cycloalkanoyl, C.sub.3 -C.sub.7 cycloalkyl(C.sub.2 -C.sub.6)alkanoyl, aryl CO--, C.sub.1 -C.sub.6 alkyl SO.sub.2 --, C.sub.3 -C.sub.7 cycloalkyl SO.sub.2 --, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkyl SO.sub.2 --, aryl-SO.sub.2 -- or (R.sup.6).sub.2 NSO.sub.2 --, wherein each R.sup.6 is independently H or C.sub.1 -C.sub.4 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 0, 1 or 2 with the proviso that m is not 0 when W is NR.sup.5, C.dbd.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.

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Sandwich, United Kingdom

Allan Patrick Marchington