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4-aminoquinoline and 4-aminoquinoline compound and applications of compound

A technology of aminoquinazolines and compounds, applied in the field of medicine, can solve problems such as undiscovered anti-tumor research reports

Inactive Publication Date: 2013-06-26
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] 4-Aminoquinoline compounds were originally reported as immunosuppressants (Bioorganic & Medicinal Chemistry Letters, 1999(9):1819-1824). This type of compound has immune activation antagonism, and no relevant anti-tumor research has been found to report

Method used

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  • 4-aminoquinoline and 4-aminoquinoline compound and applications of compound
  • 4-aminoquinoline and 4-aminoquinoline compound and applications of compound
  • 4-aminoquinoline and 4-aminoquinoline compound and applications of compound

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Embodiment Construction

[0172]The examples are intended to illustrate, not limit, the scope of the invention. The H NMR spectra of the compounds were determined by Bruker ARX-300, and the mass spectra were determined by Agilent 1100 LC / MSD; the reagents used were analytical or chemically pure.

[0173] Ar 1 Preparation of CHO intermediate

[0174] Some aromatic aldehydes are commercially available; others are prepared as follows:

[0175] Method 1: Preparation of 1-substituted benzyl-indole-3-carbaldehydes

[0176]

[0177] Anhydrous potassium carbonate (0.11mol) and indole-3-carbaldehyde (0.1mol) were added to 60mL of DMF, stirred at room temperature for 20 minutes, and ArCH was added to the reaction solution 2 Cl (0.1 mol). After dropping, react at room temperature for 6 h, pour the reaction solution into 300 mL of water, stir for 0.5 h, filter with suction, wash with water, and dry to obtain 1-substituted benzyl-indole-3 carboxaldehyde.

[0178] Method 2: Preparation of 1-substituted benzy...

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Abstract

The invention relates to 4-aminoquinoline and a 4-aminoquinoline compound which are applied to the technical field of medicines and applications of the compound, compounds, configurational isomers and configurational isomer mixtures or pharmacologically acceptable salts and / or hydrates of the compound in the general formula I. The compound provided by the invention has the obvious antitumor activity and can be used for preparing the medicines for treating and / or preventing tumor diseases. In addition, the compound is light in molecular weight, simple to composite and small in toxic and side effects.

Description

technical field [0001] The invention belongs to the technical field of medicine, relates to a new class of 4-aminoquinazoline derivatives, and the use of this class of compounds and another class of 4-aminoquinazoline compounds for the preparation of antitumor drugs, and also relates to the use of the A pharmaceutical composition in which the compound is an active ingredient, and a use in a medicament for treating and / or preventing various cancers and proliferative diseases. Background technique [0002] Malignant tumor is a common and frequently-occurring disease that seriously endangers human health. At present, most of the antineoplastic drugs used clinically are cytotoxic drugs, which have unavoidable shortcomings, such as low selectivity, strong side effects and easy produce drug resistance, etc. Discovering new targeted anticancer drugs with high efficiency, low toxicity and strong specificity has become an important direction in the research and development of antica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/95C07D401/04A61K31/517A61K31/5377A61P35/00
Inventor 宫平翟鑫刘亚婧赵燕芳张锋姜楠
Owner SHENYANG PHARMA UNIVERSITY
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