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【專利讓與】用於治療中風的環烯醚萜苷類化合物，其醫藥組合物及其用途

中國醫藥大學 研發成果讓與公告

本校案件

科技部成果公告讓與

公告日期

2021/06/01

發明人代表

中國醫藥大學 生物醫學研究所 徐偉成教授

專利(技術)名稱

用於治療中風的環烯醚萜苷類化合物，其醫藥組合物及其用途

專利國別

美國

專利核准日

2018.07.31

專利證號

US 10,035,791 B2

類型

發明

專利範圍

1. A bicyclic compound represented by:
Figure US10035791-20180731-C00028
wherein —R1 is —OH, —OCH2CH3, a substituent represented by Formula (i), a substituent represented by Formula (ii), a substituent represented by Formula (iii) or a substituent represented by Formula (iv);
Figure US10035791-20180731-C00029
Figure US10035791-20180731-C00030
Figure US10035791-20180731-C00031
Figure US10035791-20180731-C00032
wherein in Formula (ii), R3 is —NH2, —NH3 +Cl−or a substituent represented by Formula (vi):
Figure US10035791-20180731-C00033
wherein R2 is a substituent represented by Formula (vii):
Figure US10035791-20180731-C00034
wherein R4 is a substituent represented by Formula (viii), a substituent represented by Formula (ix) or a substituent represented by Formula (x):
Figure US10035791-20180731-C00035
Figure US10035791-20180731-C00036
Figure US10035791-20180731-C00037
wherein in Formula (viii), R5 is —NH2, —NH3 +Cl−or the substituent represented by Formula (vi);
and in Formula (x), R6 is —H2 +Cl−or the substituent represented by Formula (vi).
2. The bicyclic compound of claim 1 represented by a structural formula of the following table:
Com- pound Structural formula 1
Figure US10035791-20180731-C00038
2
Figure US10035791-20180731-C00039
3
Figure US10035791-20180731-C00040
4
Figure US10035791-20180731-C00041
5
Figure US10035791-20180731-C00042
6
Figure US10035791-20180731-C00043
7
Figure US10035791-20180731-C00044
8
Figure US10035791-20180731-C00045
9
Figure US10035791-20180731-C00046
10
Figure US10035791-20180731-C00047
11
Figure US10035791-20180731-C00048
12
Figure US10035791-20180731-C00049
14
Figure US10035791-20180731-C00050
15
Figure US10035791-20180731-C00051
16
Figure US10035791-20180731-C00052
17
Figure US10035791-20180731-C00053
3. The bicyclic compound of claim 1 represented by a structural formula 1:
Figure US10035791-20180731-C00054
4. The bicyclic compound of claim 1 represented by a structural formula 2:
Figure US10035791-20180731-C00055
5. The bicyclic compound of claim 1 represented by a structural formula 3:
Figure US10035791-20180731-C00056
6. The bicyclic compound of claim 1 represented by a structural formula 4:
Figure US10035791-20180731-C00057
7. The bicyclic compound of claim 1 represented by a structural formula 5:
Figure US10035791-20180731-C00058
8. The bicyclic compound of claim 1 represented by a structural formula 6:
Figure US10035791-20180731-C00059
9. The bicyclic compound of claim 1 represented by a structural formula 7:
Figure US10035791-20180731-C00060
10. The bicyclic compound of claim 1 represented by a structural formula 8:
Figure US10035791-20180731-C00061
11. The bicyclic compound of claim 1 represented by a structural formula 9:
Figure US10035791-20180731-C00062
12. The bicyclic compound of claim 1 represented by a structural formula 10:
Figure US10035791-20180731-C00063
13. The bicyclic compound of claim 1 represented by a structural formula 11:
Figure US10035791-20180731-C00064
14. The bicyclic compound of claim 1 represented by a structural formula 12:
Figure US10035791-20180731-C00065
15. The bicyclic compound of claim 1 represented by a structural formula 14:
Figure US10035791-20180731-C00066
16. The bicyclic compound of claim 1 represented by a structural formula 15:
Figure US10035791-20180731-C00067
17. The bicyclic compound of claim 1 represented by a structural formula 16:
Figure US10035791-20180731-C00068
18. The bicyclic compound of claim 1 represented by a structural formula 17:
Figure US10035791-20180731-C00069
19. A pharmaceutical composition for treating a stroke comprising an effective amount of the bicyclic compound of claim 1 and a pharmaceutically acceptable carrier, wherein the effective amount is from 0.1 mg/kg to 10 mg/kg.
20. A method for treating an ischemic stroke comprising administering an effective amount of the bicyclic compound of claim 1 to a subject in need for a treatment of the stroke.

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