Substituted azaheterocyclecarboxylic acids

Details Substituted azaheterocyclecarboxylic acids Substituted azaheterocyclecarboxylic acids

C - Chemistry, Metallurgy

07

D

C07D 207/16 (2006.01) A61K 31/395 (2006.01) C07D 211/60 (2006.01) C07D 401/04 (2006.01) C07D 403/04 (2006.01) C07D 405/02 (2006.01) C07D 409/02 (2006.01) C07D 411/06 (2006.01) C07D 413/02 (2006.01) C07D 417/04 (2006.01)

Patent

CA 2171637

A compound of the chemical formula (I) and its pharmaceutically accept- able salt, wherein Y is C2-C4 alkylene; Z is a valence bond or C1-C6 alkylene; R1 is substituted or unsubstituted aryl (e.g., phenyl and naphthyl) or heteroaryl (e.g., thienyl and furyl); R2 is hydrogen or C1-C6 alkyl; R3 is hydrogen, hy- droxy or the like; R4 is substituted or unsubstituted benzyl or the like. Typ- ical examples are (2S*,3S*,4S*,5R*)-4-Carboxy-3-[N-(5-Isopropyl-2-methoxy- benzyl)amino]-5-methyl-2-phenylpyrrolidine and (2S*,3S*,5S*)-5-Carboxy-3-[N- (2-methoxy-5-trifluoromethoxybenzyl)amino]-2-phenylpiperidine. The novel sub- stituted azaheterocyclecarboxylic acids in this invention have excellent substance P anatagonistic activity and are thus useful for the treatement of gastrointestinal dis- orders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis or migraine in mammals, especially humans.

Composé de formule chimique (I) et son sel acceptable en pharmacologie. Dans la formule, Y représente C2-C4 alkylène; Z représente une liaison de valence ou C1-C6 alkylène; R1 représente aryle substitué ou non (par exemple phényle et naphtyle) ou hétéroaryle (par exemple thiényle et furyle); R2 représente hydrogène ou C1-C6 alkyle; R3 représente hydrogène, hydroxy ou une substance analogue; R4 représente benzyle substitué ou non ou une substance analogue. Des exemples typiques sont la (2S*,3S*,4S*,5R*)-4-carboxy-3-¢N-(5-isopropyl-2-méthoxy-benzyl)amino!-5-méthyl-2-phénylpy rrolidine et la (2S*,3S*,5S*)-5-carboxy-3-¢N-(2-méthoxy-5-trifluorométhoxybenzyl)amino!-2-phénylpipéridine. Les nouveaux acides azahétérocyclecarboxyliques substitués ci-décrits présentent une excellente activité d'antagonistes vis-à-vis de la substance P et sont utiles dans le traitement de troubles gastro-intestinaux et du système nerveux central, d'allergies, de maladies inflammatoires, d'asthme, de la douleur, des vomissements, ou de la migraine chez les mammifères, notamment chez l'homme.

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