1-aryl-2-acylamino-ethane compounds and their use as...

Details 1-aryl-2-acylamino-ethane compounds and their use as... 1-aryl-2-acylamino-ethane compounds and their use as...

C - Chemistry, Metallurgy

07

C

C07C 237/22 (2006.01) A61K 31/16 (2006.01) A61K 31/18 (2006.01) A61K 31/275 (2006.01) A61K 31/33 (2006.01) C07C 255/29 (2006.01) C07C 311/51 (2006.01) C07D 209/08 (2006.01) C07D 209/12 (2006.01) C07D 209/20 (2006.01) C07D 211/22 (2006.01) C07D 211/44 (2006.01) C07D 211/48 (2006.01) C07D 211/58 (2006.01) C07D 213/40 (2006.01) C07D 213/56 (2006.01) C07D 213/70 (2006.01) C07D 215/14 (2006.01) C07D 215/42 (2006.01) C07D 215/46 (2006.01) C07D 223/12 (2006.01) C07D 223/16 (2006.01) C07D 231/38 (2006.01) C07D 233/

Patent

CA 2213080

1-Aryl-2-acylamino-ethane compounds of formula (I), wherein R1 is aryl or heteroaryl; R2 is hydrogen, lower alkyl or aryl-lower alkyl; R3 is hydrogen, lower alkyl, aryl or heteroaryl; R4 is aryl or heteroaryl; X is C1-C7alkylene, C2-C7 alkenyline or C4-C7 alkanedienylene, and Am is an unsubstituted or mono- or di-substituted amino group, a disubstituted amino group being understood as including also an amino group in which the amino nitrogen is bonded into a ring, or a salt thereof, have valuable pharmaceutical properties and are especially effective as NK1 antagonists. They are prepared in a manner known per se.

Composés 1-aryl-2-acylamino-éthane de la formule (I), ou un sel de ceux-ci, dans laquelle R1 représente aryle ou hétéroaryle; R2 représente hydrogène, alkyle inférieur ou aryle-alkyle inférieur; R3 représente hydrogène, alkyle inférieur, aryle ou hétéroaryle; R4 représente aryle ou hétéroaryle; X représente alkylène C1-C7, alcénylène C2-C7 ou alcanediénylène C4-C7, et Am représente un groupe amino non substitué ou mono ou disubstitué, un groupe amino disubstitué s'entendant comme comprenant également un groupe amino dans lequel l'amino azote est lié dans un noyau. Ces composés possèdent des propriétés pharmacologiques précieuses et ils sont notamment efficaces en tant qu'antagonistes des neurokinines 1 (NK1). On les prépare d'une manière connue en soi.

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