Benzylaminoquinuclidines

Details Benzylaminoquinuclidines Benzylaminoquinuclidines

C - Chemistry, Metallurgy

07

D

C07D 453/02 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 31/695 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2167198

A compound of chemical formula (I) and its pharmaceutically acceptable salt, wherein X and Y are each hydrogen, halogen, C1-C6 alkyl, halosubstituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C6 alkylsulfinyl, C1-C6 alkylsulfonyl or tri C1-C6 alkylsilyl; Ar1 and Ar2 are each aryl optionally substituted by halogen; A is -CO- or -(CH2)-; Z-A- is at 2 or 3 position on the quinuclidine ring; and Z is hydroxy, C1-C6 alkoxy, NR1R2 or the like. Typical examples are (3S,4R,5S,6S)-5-(3,5-bis(trifluoromethyl)benzyloxy)-N-N-dimethyl- 6-diphenylmethyl-1-azabicyclo[2.2.2]octan-3-carboxamide; (3S,4R,5S,6S)-5-(3,5-bis(trifluoromethyl)benzyloxy)-6- dipenylmethyl-1-azabicyclo[2.2.2]octan-3-carboxylic acid. The novel benzyloxyquinuclidines in this invention have substance P antagonistic activity and are thus useful for the treatment of gastrointestinal disorders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis, migraine, urinary incontinence or angiogenesis in mammals, especially humans.

L'invention se rapporte à un composé de la formule chimique (I) et à son sel acceptable du point de vue pharmaceutique, formule dans laquelle X et Y représentent chacun hydrogène, halogène, alkyle C1-C6, alkyle C1-C6 halosubstitué, alcoxy C1-C6, alkylthio C1-C6, alkylsulfinyle C1-C6, alkylsulfonyle C1-C6 ou trialkylsilyle C1-C6; Ar1 et Ar2 représentent chacun aryle éventuellement substitué par halogène; A représente -CO- ou -(CH2)-; Z-A- est en position 2 ou 3 sur le cycle quinuclidine; et Z représente hydroxy, alkoxy C1-C6, NR1R2 ou analogue. Les exemples type sont les suivants: (3S,4R,5S,6S)-5-(3,5-bis(trifluorométhyl)benzyloxy)-N,N-diméthyl-6-diphénylméthyl-1-azabicy clo¢2.2.2!octan-3-carboxamide;(3S,4R,5S,6S)-5-(3,5-bis(trifluorométhyl)benzyloxy)-6-diphényl méthyl-1-azabicyclo¢2.2.2!octan-3-acide carboxylique. Les nouveaux benzyloxyquinuclidines selon l'invention ont une activié antagoniste à l'égard de la substance P et sont donc utiles dans le traitement de troubles gastro-intestinaux, de troubles du système nerveux central, d'allergies, de maladies inflammatoires, de l'asthme, de douleurs, de vomissements, de migraines, de l'incontinence urinaire ou de l'angiogénèse chez les mammifères, en particulier chez l'homme.

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