申请人:Samjin Pharmaceutical Co., Ltd.
公开号:US20030092910A1
公开(公告)日:2003-05-15
The present invention relates to a novel compound of the general formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, which have strong antimumor activities and very low toxicity.
1
wherein R
1
and R
2
are independently hydrogen, C
1
-C
4
alkyl, C
1
-C
4
alkylcarboxyl, C
1
-C
4
alkylcarbonyl, C
1
-C
4
alkoxy, C
1
-C
4
hydroxyalkyl, C
1
-C
4
aminoalkyl or C
1
-C
4
hydroxyiminoalkyl, or R
1
and R
2
are fused to form C
3
-C
4
unsaturated ring;
R
3
, R
4
, R
5
, R
6
and R
7
are independently hydrogen, halogen, hydroxy, nitro, amino, C
1
-C
4
alkyl, C
1
-C
4
alkylcarboxyl, C
1
-C
4
alkylcarbonyl, C
1
-C
4
alkoxy or C
1
-C
4
thioalkoxy;
R
8
is C
1
-C
4
alkyl;
Y is oxygen, sulphur, amino, substituted amino or C
1
-C
4
thioalkyl;
Z is C
1
-C
4
alkoxy, C
1
-C
4
alkyl C
1
-C
4
alkylamino or C
1
-C
4
thioalkoxy;
X
1
and X
2
are independently carbon or nitrogen; and
—N═C— and —C═Y— may form a single bond or a double bond provided that if —N═C— forms a single bond, —C═Y— forms a double bond, and if —C═Y— forms a single bond, —N═C— forms a double bond and R
8
is nonexistent.
本发明涉及一种新型化合物,其通式为(I),及其药学上可接受的酸盐,并涉及其制备方法,该化合物具有很强的抗肿瘤活性和极低的毒性。其中R1和R2独立地为氢、C1-C4烷基、C1-C4烷基羧基、C1-C4烷基羰基、C1-C4烷氧基、C1-C4羟基烷基、C1-C4氨基烷基或C1-C4羟基亚烷基,或者R1和R2融合形成C3-C4不饱和环;R3、R4、R5、R6和R7独立地为氢、卤素、羟基、硝基、氨基、C1-C4烷基、C1-C4烷基羧基、C1-C4烷基羰基、C1-C4烷氧基或C1-C4硫氧基;R8为C1-C4烷基;Y为氧、硫、氨基、取代氨基或C1-C4硫代烷基;Z为C1-C4烷氧基、C1-C4烷基、C1-C4烷基氨基或C1-C4硫代烷氧基;X1和X2独立地为碳或氮;且-N═C—和—C═Y—可以形成单键或双键,条件是如果—N═C—形成单键,则—C═Y—形成双键,如果—C═Y—形成单键,则—N═C—形成双键,且R8不存在。