3-aza and 3-oxa-piperidone tachykinin antagonists

Details 3-aza and 3-oxa-piperidone tachykinin antagonists 3-aza and 3-oxa-piperidone tachykinin antagonists

C - Chemistry, Metallurgy

07

D

C07D 401/14 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07D 403/06 (2006.01) C07D 413/06 (2006.01) C07D 413/14 (2006.01)

Patent

CA 2195924

Compounds of the formula: (see fig. I) wherein: X is O, NH or NR1; R1 is C1-C6 alkyl, C3-C7 cycloalkyl, C3-C7cycloalkyl (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)alkylgroup 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 is phenyl optionally substituted with one or two halo substituents, indolyl or thienyl; R3 is NH2, -NR4 SO2(C1-C6 alkyl), -NR4SO2 aryl, -NR4CO(C1-C6 alkyl), -NR4CO aryl or a 5 to 7-membered N-linked cyclic group incorporating W in the ring 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-C7cycloalkyl(C1-C6)alkyl,C2-C6alkanoyl, 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 (R6)2NSO2-, wherein each R6 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 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.

omposés de formule : (voir fig. I) où : X correspond à O, NH ou NR1; R1 est un alkyle en C1-C6, un cycloalkyle en C3-C7, un alkyle en C1-C4 portant un cycloalkyle en C3-C7, un aryle ou un alkyle en C1-C4 portant un aryle; le groupe alkyle en C1-C6 peut, facultativement, être substitué par un atome de fluor et le cycloalkyle en C3-C7 ou l'alkyle en C1-C4 portant un cycloalkyle en C3-C7 peuvent, facultativement, être substitués, sur le cycloalkyle, par jusqu'à deux substituants choisis indépendamment parmi les halogènes, les alkoxy en C1-C4 ou les haloalkoxy en C1-C4; R

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