申请人:——
公开号:US20040059109A1
公开(公告)日:2004-03-25
The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I, Formula (I) wherein R
1
is (C
1-3
)alkyloxy, (C
1-3
)alkyloxy(C
1-3
)alkyl, (C
1-3
)alkylthio, (C
1-3
)alkylthio(C
1-3
)alkyl, (C
1-3
)alkylsulfinyl, (C
1-3
)alkylsulfinyl(C
1-3
)alkyl, (C
1-3
)alkylsulfonyl, (C
1-3
)alkylsulfonyl(C
1-3
)alkyl, (C
1-3
)alkyloxycarbonyl,
(CH
2
)
n
—CO—NR
8
R
9? or
(CH2)
n
—NR
8
R
9?; n is 0, 1 or 2; R
2
is hydrogen or
(C
1-3?)alkyl; R
3
is (C
1-3
)alkyl or
(C
1-3
)alkyloxy(C
1-3?)alkyl; R
4
is (C
1-3
)alkyloxy(C
1-3
)alkyl; or R
3
and R
4
form together with the nitrogen atom to which they are bound a 5-, 6-, or 7-membered ring, optionally containing a further heteroatom selected from O and S, and which ring may optionally contain a double bond and be optionally substituted with (C
1-3
)alkyl or (C
1-3
)alkyloxy; R
5
and R
6
are independently (C
1-3
)alkyl; R
7
is hydrogen, (C
1-3
)alkyl, (C
1-3
)alkyloxy or (C
2-3
)alkenyl; R
8
and R
9
are independently (C
1-3
)alkyl; or R
8
and R
9
form together with the nitrogen atom to which they are bound a 5-, 6-, or 7-membered, optionally containing a further heteroatom selected from O and S, and which ring may optionally contain a double bond; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.
1
本发明涉及具有一般式I的丙氨酸2,6-二烷氧基苯酯衍生物,式(I)其中,R1是(C1-3)烷氧基、(C1-3)烷氧基(C1-3)烷基、(C1-3)烷基硫醚、(C1-3)烷基硫醚(C1-3)烷基、(C1-3)烷基亚磺酰、(C1-3)烷基亚磺酰(C1-3)烷基、(C1-3)烷基磺酰、(C1-3)烷基磺酰(C1-3)烷基、(C1-3)烷氧羰基、(CH2)n—CO—NR8R9或(CH2)n—NR8R9;n为0、1或2;R2是氢或(C1-3)烷基;R3是(C1-3)烷基或(C1-3)烷氧基(C1-3)烷基;R4是(C1-3)烷氧基(C1-3)烷基;或R3和R4与它们所结合的氮原子一起形成一个5、6或7元环,可选地含有进一步从O和S中选择的杂原子,并且该环可以可选地含有双键并被(C1-3)烷基或(C1-3)烷氧基取代;R5和R6独立地是(C1-3)烷基;R7是氢、(C1-3)烷基、(C1-3)烷氧基或(C2-3)烯基;R8和R9独立地是(C1-3)烷基;或者R8和R9与它们所结合的氮原子一起形成一个5、6或7元环,可选地含有进一步从O和S中选择的杂原子,并且该环可以可选地含有双键;或其药学上可接受的盐。本发明还涉及包含上述衍生物的制药组合物,以及将这些丙氨酸2,6-二烷氧基苯酯衍生物用作诱导和维持全身麻醉的催眠药的用途。