[EN] alpha -AMINO ACID PHENYL ESTER DERIVATIVES<br/>[FR] DERIVES ESTERS PHENYLIQUES D'ACIDE alpha -AMINE
申请人:AKZO NOBEL NV
公开号:WO2000005196A1
公开(公告)日:2000-02-03
The present invention relates to α-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 α-amino acid phenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.
本发明涉及具有一般式(I)的α-氨基酸苯酯衍生物,其中R1是(C1-3)烷氧基; R2是(C1-3)烷基,(C1-3)烷氧基或(C2-3)烯基; R3是氢,(C1-3)烷基,(C1-3)烷氧基或(C2-3)烯基; R4是(C1-6)烷基; R5和R6分别独立地为(C1-6)烷基,(C2-6)烯基,(C2-6)炔基或芳基烷基,每个基团可以选择性地被(C1-3)烷氧基,(C1-3)烷氧羰基,氰基或NR7R8取代; R7和R8分别是(C1-6)烷基; 或其药学上可接受的盐。本发明还涉及包括所述衍生物的制药组合物,以及将这些α-氨基酸苯酯衍生物用作诱导和维持全身麻醉的催眠剂的用途。