C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 229/12 (2006.01) A61K 31/223 (2006.01) A61P 25/00 (2006.01)
Patent
CA 2337945
The present invention relates to .alpha.-amino acid phenyl ester derivatives having general formula (I) wherein R1 is (C1-3)alkyloxy; R2 is (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R3 is hydrogen, (C1-3)alkyl, (C1-3)alkyloxy or (C2-3)alkenyl; R4 is (C1-6)alkyl; R5 and R6 are independently (C1-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl or aralkyl, each of which may be optionally substituted with (C1-3)alkyloxy, (C1-3)alkyloxycarbonyl, cyano or NR7R8; R7 and R8 are independently (C1-6)alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these .alpha.-amino acid phenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.
La présente invention se rapporte à des dérivés esters phényliques d'acide .alpha.-aminé représentés par la formule générale (I) ou à un sel pharmaceutiquement acceptable de ces dérivés. Dans la formule (I), R¿1? est alkyloxy (C¿1-3?); R¿2? est alkyle (C¿1-3?), alkyloxy (C¿1-3?) ou alcényle (C¿2-3?); R¿3? est hydrogène, alkyle (C¿1-3?), alkyloxy (C¿1-3?) ou alcényle (C¿2-3?); R¿4? est alkyle (C¿1-6?); R¿5? et R¿6? sont indépendamment alkyle (C¿1-6?), alcényle (C¿2-6?), aralkyle ou alkynyle (C¿2-6?), chaque radical pouvant être substitué par alkyloxy (C¿1-3?), alkyloxycarbonyle (C¿1-3?), cyano ou NR¿7?R¿8?; R¿7? et R¿8? sont indépendamment alkyle (C¿1-6?). L'invention se rapporte également à des compositions pharmaceutiques contenant ces dérivés, et à l'utilisation de ces dérivés esters phényliques d'acide .alpha.-aminé en tant que composés hypnotiques pour l'induction et l'entretien d'une anesthésie générale.
Akzo Nobel N.v.
Fetherstonhaugh & Co.
N.v. Organon
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