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Pyrimidine and triazine compound preparation method and application

A kind of compound, the technology of hydrate, applied in the new pyrimidine and triazine compound, the pharmaceutical composition containing the compound, the preparation treatment and/or the medicine field of preventing cancer and other proliferative diseases

Inactive Publication Date: 2012-09-12
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Abnormal regulation mechanism of mTOR can lead to abnormal proliferation and differentiation of tumor cells

Method used

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  • Pyrimidine and triazine compound preparation method and application
  • Pyrimidine and triazine compound preparation method and application
  • Pyrimidine and triazine compound preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0188] Embodiment 1: ( E )-4,4'-[6-[2-[1-(3-chlorobenzyl)-1 H -Indol-3-yl]methylidenehydrazino]-[1,3,5]-triazine-2,4-diyl]dimorpholine

[0189] ESI-MS [M+H] (m / z):534 ; m.p.129-130℃; 1 H NMR (300 MHz, DMSO) δ 10.59 (s, 1H), 8.46 (d, J = 7.7 Hz, 1H), 8.27 (s, 1H), 7.87 (s, 1H), 7.49 (d, J = 8.1 Hz, 1H), 7.34 (m, 3H), 7.16 (m, 3H), 5.45 (s, 2H), 3.73 (s, 8H), 3.64 (s, 8H).

Embodiment 2

[0190] Embodiment 2: ( E )-4,4'-[6-[2-[1-(4-methylbenzyl)-1 H -Indol-3-yl]methylidenehydrazino]-[1,3,5]-triazine-2,4-diyl]dimorpholine

[0191] ESI-MS [M+H] (m / z): 513.26 m.p.:137-139℃; 1H NMR (300 MHz, DMSO) δ 10.58 (s, 1H), 8.45 (d, J = 7.4 Hz, 1H), 8.26 (s, 1H), 7.84 (s, 1H), 7.46 (d, J = 8.0 Hz, 1H), 7.38 (d, J = 8.3 Hz, 2H), 7.32-7.02 (m, 4H), 5.43 (s, 2H), 3.73 (s, 8H), 3.64 (s, 8H), 1.06 (s, 3H).

Embodiment 3

[0192] Embodiment 3: ( E )-4,4'-[6-[2-[1-(3,4-dichlorobenzyl)-1 H -Indol-3-yl]methylidenehydrazino]-[1,3,5]-triazine-2,4-diyl]dimorpholine

[0193] ESI-MS [M+H] (m / z): 567.17; m.p. 135-137℃; 1 H NMR (300 MHz, DMSO) δ 10.60 (s, 1H), 8.47 (d, J = 7.7 Hz, 1H), 8.27 (s, 1H), 7.87 (s, 1H), 7.56 (dd, J = 9.4, 5.0 Hz, 2H), 7.49 (d, J = 8.1 Hz, 1H), 7.30-7.04 (m, 3H), 5.45 (s, 2H), 3.74 (s, 8H), 3.65 (s, 8H).

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Abstract

The present invention relates to pyrimidine and triazine compounds represented as a general formula I, geometric isomers, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, wherein substituents R1, R2, R3 and X have the meanings defined in the description. The invention further relates to uses of the compounds represented as the general formula I in preparing medicine for treating and / or preventing cancer and other hyperplasia diseases.

Description

technical field [0001] The present invention relates to novel pyrimidine and triazine compounds, their geometric isomers and their pharmaceutically acceptable salts, hydrates, solvates or prodrugs, their preparation methods and pharmaceutical compositions containing the compounds. The present invention also relates to the use of pyrimidine and triazine compounds in the preparation of medicines for treating and / or preventing cancer and other proliferative diseases. Background technique [0002] Malignant tumor is a disease that seriously endangers human life and health. With the change of external factors such as environmental pollution, the number of cancer cases in the world is increasing year by year. According to the statistics of the World Health Organization (WHO), about 10 million people are diagnosed every year in the world. Cancer patients, 7 million people died of related diseases caused by tumors, so malignant tumors have become the second major killer of human bei...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/12A61K31/5377A61K31/506A61K31/53A61P35/00
Inventor 宫平赵燕芳刘亚婧翟鑫朱五福
Owner SHENYANG PHARMA UNIVERSITY
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