CN101641339B - 用于预防和治疗心血管疾病的化合物 - Google Patents
用于预防和治疗心血管疾病的化合物 Download PDFInfo
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- CN101641339B CN101641339B CN2007800523498A CN200780052349A CN101641339B CN 101641339 B CN101641339 B CN 101641339B CN 2007800523498 A CN2007800523498 A CN 2007800523498A CN 200780052349 A CN200780052349 A CN 200780052349A CN 101641339 B CN101641339 B CN 101641339B
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- dimethoxy
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- dihydroquinazoline
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- 0 CC(C*(C)C*(*)**=[N+][O-])*(C)* Chemical compound CC(C*(C)C*(*)**=[N+][O-])*(C)* 0.000 description 4
- SQBKNGXWWBLWCX-UHFFFAOYSA-N COc(c(OC)c1)cc2c1N=C(c(cc1)ccc1N(CCO)CCO)NC2=O Chemical compound COc(c(OC)c1)cc2c1N=C(c(cc1)ccc1N(CCO)CCO)NC2=O SQBKNGXWWBLWCX-UHFFFAOYSA-N 0.000 description 1
- KTACWZKZFWVPAU-UHFFFAOYSA-N COc(cc1OC)cc(N=C(c(cc2)ccc2N(CCO)CCO)N2)c1C2=O Chemical compound COc(cc1OC)cc(N=C(c(cc2)ccc2N(CCO)CCO)N2)c1C2=O KTACWZKZFWVPAU-UHFFFAOYSA-N 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N OC(c1ccccc1)=O Chemical compound OC(c1ccccc1)=O WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
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Abstract
Description
实施例 编号 | 化合物名称 | 对ApoA-I mRNA水 平的作用 |
38 | 3-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)-1,1-二甲基脲 | 活性 |
37 | 1-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)-3-苯基脲 | 活性 |
36 | 1-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)-3-(4-甲氧基苯基)脲 | 活性 |
实施例 编号 | 化合物名称 | 对ApoA-I mRNA水 平的作用 |
35 | 1-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)-3-甲基脲 | 活性 |
34 | N-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)异丁酰胺 | 活性 |
33 | N-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)苯甲酰胺 | 活性 |
32 | N-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)乙酰胺 | 活性 |
31 | N-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)-4-甲氧基苯甲酰胺 | 活性 |
30 | N-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)-4-甲基苯磺酰胺 | 活性 |
29 | N-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)苯磺酰胺 | 活性 |
28 | 环己基氨甲酸2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹 唑啉-2-基)-2,6-二甲基苯氧基)乙基酯 | 活性 |
27 | N-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)-4-甲基苯甲酰胺 | 活性 |
26 | 甲基氨甲酸2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑 啉-2-基)-2,6-二甲基-苯氧基)乙基酯 | 活性 |
25 | 丙基氨甲酸2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑 啉-2-基)-2,6-二甲基-苯氧基)乙基酯 | 活性 |
24 | N-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)甲磺酰胺 | 活性 |
实施例 编号 | 化合物名称 | 对ApoA-I mRNA水 平的作用 |
23 | 4-氯-N-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)苯磺酰胺 | 活性 |
22 | N-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)-4-甲氧基苯磺酰胺 | 活性 |
21 | N1-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)-N2-甲基邻苯二甲酰胺 | 活性 |
20 | 4-氯-N-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)苯磺酰胺 | 活性 |
18 | 2-(4-(2-氨基乙氧基)-3,5-二甲基苯基)-5,7-二甲氧基喹 唑啉-4(3H)-酮 | 活性 |
18 | N1-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)-N2-甲基邻苯二甲酰胺 | 活性 |
17 | 2-(4-氨基-3,5-二甲基苯基)-5,7-二甲氧基喹唑啉 -4(3H)-酮 | 活性 |
16 | 5,7-二甲氧基-2-(4-甲氧基-3,5-二甲基苯基)喹唑啉 -4(3H)-酮 | 活性 |
15 | 2-(2-氯-6-甲基吡啶-4-基)-5,7-二甲氧基喹唑啉-4(3H)- 酮 | 活性 |
14 | 2-(4-(2-羟基乙氧基)-3,5-二甲基苯基)-5,7-二甲氧基吡 啶并[2,3-d]嘧啶-4(3H)-酮 | 活性 |
13 | 2-(4-((4-乙基哌嗪-1-基)甲基)苯基)-5,7-二甲氧基喹唑 啉-4(3H)-酮 | 活性 |
12 | 2-(2,3-二氢苯并[b][1,4]二噁烯-6-基)-6,7-二甲氧基喹 唑啉-4(3H)-酮 | 活性 |
实施例 编号 | 化合物名称 | 对ApoA-I mRNA水 平的作用 |
11 | 2-(4-(双(2-羟基乙基)氨基)苯基)-6,7-二甲氧基喹唑啉 -4(3H)-酮 | 活性 |
10 | 2-(4-(双(2-羟基乙基)氨基)苯基)-5,7-二甲氧基喹唑啉 -4(3H)-酮 | 活性 |
9 | 2-(4-羟基-3-甲氧基苯基)-5,7-二甲氧基喹唑啉-4(3H)- 酮 | 活性 |
8 | 3-(3,5-二甲基-4-(2-(4-甲基哌嗪-1-基)乙氧基)苯 基)-6,8-二甲氧基异喹啉-1(2H)-酮 | 活性 |
7 | 2-(4-(2-羟基乙氧基)-3,5-二甲基苯基)-5,7-二甲氧基喹 唑啉-4(3H)-酮 | 活性 |
6 | 7-(4-羟基-3,5-二甲基苯基)-2,4-二甲氧基-1,6-萘啶 -5(6H)-酮 | 活性 |
5 | 3-(4-(2-羟基-2-甲基丙氧基)-3,5-二甲基苯基)-6,8-二 甲氧基异喹啉-1(2H)-酮 | 活性 |
4 | 2-(4-羟基-3,5-二甲基苯基)-5,7-二甲氧基喹唑啉 -4(3H)-酮 | 活性 |
3 | 3-(4-羟基-3,5-二甲基苯基)-7-(吗啉代基甲基)异喹啉 -1(2H)-酮 | 活性 |
2 | 3-(4-(2-羟基乙氧基)-3,5-二甲基苯基)-6,8-二甲氧基异 喹啉-1(2H)-酮 | 活性 |
1 | 3-(4-羟基-3,5-二甲基苯基)-6,8-二甲氧基异喹啉 -1(2H)-酮 | 活性 |
实施例 编号 | 化合物名称 | EC50 蛋白质 (μM) |
20 | 4-氯-N-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)苯磺酰胺 | 0.32 |
18 | 2-(4-(2-氨基乙氧基)-3,5-二甲基苯基)-5,7-二甲氧基喹 唑啉-4(3H)-酮 | 7.22 |
18 | N1-(2-(4-(5,7-二甲氧基-4-氧代-3,4-二氢喹唑啉-2- 基)-2,6-二甲基苯氧基)乙基)-N2-甲基邻苯二甲酰胺 | 7.29 |
17 | 2-(4-氨基-3,5-二甲基苯基)-5,7-二甲氧基喹唑啉 -4(3H)-酮 | 7.63 |
16 | 5,7-二甲氧基-2-(4-甲氧基-3,5-二甲基苯基)喹唑啉 -4(3H)-酮 | 16.46 |
15 | 2-(2-氯-6-甲基吡啶-4-基)-5,7-二甲氧基喹唑啉-4(3H)- 酮 | 3.96 |
14 | 2-(4-(2-羟基乙氧基)-3,5-二甲基苯基)-5,7-二甲氧基吡 啶并[2,3-d]嘧啶-4(3H)-酮 | 9.20 |
13 | 2-(4-((4-乙基哌嗪-1-基)甲基)苯基)-5,7-二甲氧基喹唑 啉-4(3H)-酮 | 13.72 |
实施例 编号 | 化合物名称 | EC50 蛋白质 (μM) |
12 | 2-(2,3-二氢苯并[b][1,4]二噁烯-6-基)-6,7-二甲氧基喹 唑啉-4(3H)-酮 | 9.07 |
11 | 2-(4-(双(2-羟基乙基)氨基)苯基)-6,7-二甲氧基喹唑啉 -4(3H)-酮 | 13.30 |
10 | 2-(4-(双(2-羟基乙基)氨基)苯基)-5,7-二甲氧基喹唑啉 -4(3H)-酮 | 12.11 |
9 | 2-(4-羟基-3-甲氧基苯基)-5,7-二甲氧基喹唑啉-4(3H)- 酮 | 12.08 |
8 | 3-(3,5-二甲基-4-(2-(4-甲基哌嗪-1-基)乙氧基)苯 基)-6,8-二甲氧基异喹啉-1(2H)-酮 | 2.82 |
7 | 2-(4-(2-羟基乙氧基)-3,5-二甲基苯基)-5,7-二甲氧基喹 唑啉-4(3H)-酮 | 12.16 |
6 | 7-(4-羟基-3,5-二甲基苯基)-2,4-二甲氧基-1,6-萘啶 -5(6H)-酮 | 6.52 |
5 | 3-(4-(2-羟基-2-甲基丙氧基)-3,5-二甲基苯基)-6,8-二甲 氧基异喹啉-1(2H)-酮 | 6.27 |
4 | 2-(4-羟基-3,5-二甲基苯基)-5,7-二甲氧基喹唑啉 -4(3H)-酮 | 7.93 |
3 | 3-(4-羟基-3,5-二甲基苯基)-7-(吗啉代基甲基)异喹啉 -1(2H)-酮 | 11.09 |
2 | 3-(4-(2-羟基乙氧基)-3,5-二甲基苯基)-6,8-二甲氧基异 喹啉-1(2H)-酮 | 11.35 |
1 | 3-(4-羟基-3,5-二甲基苯基)-6,8-二甲氧基异喹啉 -1(2H)-酮 | 5.42 |
2-(4-羟基-苯基)-吡喃并[2,3-b]吡啶-4-酮 | 179.47 |
Claims (11)
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EP0210342A2 (de) * | 1985-05-03 | 1987-02-04 | Dr. Karl Thomae GmbH | Arzneimittel, enthaltend Pyridinone mit antithrombotischer Wirkung |
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US10131640B2 (en) | 2009-03-18 | 2018-11-20 | Resverlogix Corp. | Anti-inflammatory agents |
US10111885B2 (en) | 2015-03-13 | 2018-10-30 | Resverlogix Corp. | Compositions and therapeutic methods for the treatment of complement-associated diseases |
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