申请人:——
公开号:US20020187994A1
公开(公告)日:2002-12-12
A compound of formula
1
wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H
2
or F
2
;
A is N or C(R
2
); G is N or C(R
3
); D is N or C(R
4
);
with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO;
R
1
is hydrogen or C
1
to C
4
alkyl;
R
2
, R
3
, and R
4
are independently hydrogen, halogen, C
1
-C
4
alkyl, C
2
-C
4
alkenyl, C
2
-C
4
alkynyl, aryl, heteroaryl, OH, OC
1
-C
4
alkyl, CO
2
R
1
, —CN, —NO
2
, —NR
5
R
6
, —CF
3
, —OSO
2
CF
3
or R
2
and R
3
, or R
3
and R
4
respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C
1
-C
4
alkyl, C
2
-C
4
alkenyl, C
2
-C
4
alkynyl, aryl, heteroaryl, OH, OC
1
-C
4
alkyl, CO
2
R
1
, —CN, —NO
2
, —NR
5
R
6
, —CF
3
, —OSO
2
CF
3
; R
5
and R
6
are independently hydrogen, C
1
-C
4
alkyl, C(O)R
7
, C(O)NHR
8
, C(O)OR
9
, SO
2
R
10
or may together be (CH
2
)
j
Q(CH
2
)
k
where Q is O, S, NR
11
, or a bond; j is 2 to 7, k is 0 to 2; R
7
, R
8
, R
9
, R
10
, and R
11
are independently C
1
-C
4
alkyl, aryl, or heteroaryl, or an enantiomer thereof,
and the pharmaceutically acceptable salts thereof, processes for preparing them, composition containing them, and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.
化合物的化学式为1,其中n为0或1;m为0或1;p为0或1;X为氧或硫;Y为CH、N或NO;W为氧、H2或F2;A为N或C(R2);G为N或C(R3);D为N或C(R4);但是A、G和D中最多只有一个是氮,但Y、A、G和D中至少有一个是氮或NO;R1为氢或C1到C4烷基;R2、R3和R4独立地为氢、卤素、C1-C4烷基、C2-C4烯基、C2-C4炔基、芳基、杂环芳基、OH、OC1-C4烷基、CO2R1、-CN、-NO2、-NR5R6、-CF3、-OSO2CF3或R2和R3,或R3和R4可以分别形成另一个共用A和G或G和D的六元芳香或杂芳香环,其中包含零到两个氮原子,并且取代有以下一个或两个取代基:独立地为氢、卤素、C1-C4烷基、C2-C4烯基、C2-C4炔基、芳基、杂环芳基、OH、OC1-C4烷基、CO2R1、-CN、-NO2、-NR5R6、-CF3、-OSO2CF3;R5和R6独立地为氢、C1-C4烷基、C(O)R7、C(O)NHR8、C(O)OR9、SO2R10或可以共同为(CH2)jQ(CH2)k,其中Q为O、S、NR11或键;j为2到7,k为0到2;R7、R8、R9、R10和R11独立地为C1-C4烷基、芳基或杂环芳基,或其对映体,以及其药学上可接受的盐,制备它们的过程,包含它们的组合物以及它们在治疗中的应用,特别是在治疗或预防精神障碍和智力障碍方面。