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A kind of pharmaceutical composition with HDAC inhibitory activity, preparation method and use thereof

A technology of inhibitory activity and composition, applied in the field of pharmaceutical compositions with HDAC inhibitory activity, can solve problems such as side effects and inability to distinguish tumor cells

Active Publication Date: 2021-10-15
北京华氏精恒医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional anti-tumor drugs cannot distinguish between tumor cells and normal cells, so they often cause serious side effects. Targeted drugs use tumor cells as specific targets and can accurately act on tumors, greatly improving the level of treatment and reducing the cost of treatment. adverse reaction rate

Method used

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  • A kind of pharmaceutical composition with HDAC inhibitory activity, preparation method and use thereof
  • A kind of pharmaceutical composition with HDAC inhibitory activity, preparation method and use thereof
  • A kind of pharmaceutical composition with HDAC inhibitory activity, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0049] The preparation of the pharmaceutical composition can adopt conventional methods in the art. For example, when preparing ordinary tablets, the direct compression method can be adopted, that is, the ingredients are mixed and then compressed; all the components can be granulated and then compressed; or some of the components can be granulated and then mixed with the remaining components for compression. . In addition, the tablet can also be coated by methods commonly used in the art.

[0050] Further, the preparation method of the active ingredient comprises the following steps:

[0051]

[0052] (1) Synthesis of Intermediate IV:

[0053] Reaction of compound II and compound III under the action of a condensing agent in the first reaction solvent in the presence of a base to obtain intermediate IV;

[0054] (2) Synthesis of intermediate V:

[0055] Intermediate IV is reacted in the second reaction solvent under the action of acid to obtain intermediate V;

[0056]...

Embodiment 7～12

[0089] Table 2 embodiment 7~12 pharmaceutical composition component content

[0090]

Embodiment 13～18

[0091] Table 3 embodiment 13~18 pharmaceutical composition component content

[0092]

[0093]

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PUM

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Abstract

The present invention belongs to the field of pharmaceuticals, and in particular relates to a pharmaceutical composition with HDAC inhibitory activity, a preparation method and an application thereof. Based on the total mass of the pharmaceutical composition as 100%, the pharmaceutical composition includes the following mass percentages: Ingredients: active ingredient 1% to 10%; pharmaceutically acceptable excipients 90% to 99%; the active ingredient is a compound with the structure of formula I or a pharmaceutically acceptable salt thereof: in the formula, R 1 Represents substituted phenyl, unsubstituted phenyl, substituted aromatic heterocyclic group or unsubstituted aromatic heterocyclic group; X represents CH or N. The pharmaceutical composition provided by the invention is a novel HDAC inhibitor with high specificity, low side effects, good HDAC inhibitory activity, and achieves the purpose of treating tumors by inhibiting the activity of HDACs, and can be applied to the development of tumor drugs. The prevention and treatment of tumors are of great significance.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a pharmaceutical composition with HDAC inhibitory activity, a preparation method and application thereof. Background technique [0002] Cancer is one of the major diseases that threaten human health. At present, the main treatment methods include drug therapy, surgery therapy and radiation therapy, among which drug therapy is one of the most commonly used treatment methods. Traditional anti-tumor drugs cannot distinguish between tumor cells and normal cells, so they often cause serious side effects. Targeted drugs use tumor cells as specific targets and can accurately act on tumors, greatly improving the level of treatment and reducing the cost of treatment. adverse reaction rate. [0003] Histone deacetylase (HDAC) is one of the epigenetic targets of important research, classified into Zn 2+ Dependence and NAD + Depending on tolerance, histone deacetylases and histone acet...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4709A61K31/498A61P35/00
CPCA61K31/4709A61K31/498A61P35/00
Inventor 霍志强黄巧萍吕永磊唐睿柏小娟戴信敏
Owner 北京华氏精恒医药科技有限公司