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A kind of toll-like receptor modulator, its pharmaceutical composition, preparation method and application

A composition and drug technology, which can be used in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., and can solve problems such as retrovirus damage

Active Publication Date: 2020-04-24
北京施安泰医药技术开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, a gene encoding a protein similar to TLR10 in humans is present in mice, but the gene appears to have been damaged at one point by a retrovirus in the past

Method used

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  • A kind of toll-like receptor modulator, its pharmaceutical composition, preparation method and application
  • A kind of toll-like receptor modulator, its pharmaceutical composition, preparation method and application
  • A kind of toll-like receptor modulator, its pharmaceutical composition, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] Preparation of 2-(morpholinyl-4-carbonyl)imidazo[1,2-a]quinoxaline-4(5H)-one

[0082]

[0083] first step:

[0084] Dissolve compounds 1a (16.1g, 100mmol) and 1b (19.5g, 100mmol) in ethanol (200ml), heat to reflux, stir and react for 8 hours, check the reaction by TLC, and concentrate under reduced pressure after the reaction is complete. Off-white solid 20.3g, yield 79.0%.

[0085] The second step:

[0086] The compound 1c (20.0g, 77.7mmol) obtained in the first step was dissolved in a mixed solvent of ethanol (100ml) and water (100ml), sodium hydroxide (6.2g, 155.5mmol) was added at room temperature, and the reaction was stirred at 40°C for 6 After the reaction was completed, the ethanol was removed under reduced pressure. The remaining solution was poured into stirred dilute hydrochloric acid to precipitate solids, filtered, the filter cake was washed with water, and dried to obtain 14.8 g of off-white solids with a yield of 83.1%.

[0087] third step:

[0088] The compound 1...

Embodiment 2

[0090] Preparation of the compound 2-(4-methylpiperidinyl-1-carbonyl)imidazo[1,2-a]quinoxaline-4(5H)-one represented by the following formula: prepare according to the method of Example 1 , MS-ESI: m / z=312.3 [M+1].

[0091]

Embodiment 3

[0093] Preparation of the compound 2-(4-piperidinyl-1-carbonyl)imidazo[1,2-a]quinoxalin-4(5H)-one represented by the following formula: prepare according to the method in Example 1, MS -ESI: m / z=298.3 [M+1].

[0094]

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PUM

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Abstract

The invention belongs to the field of pharmaceutical chemistry, particularly relates to compounds with TLR (Toll-like receptor) modulation effect as well as a preparation method and an application ofthe compounds, and provides compounds represented by the following formula X in the description. The compounds of formula X can be used as the TLR modulators and have higher activity. Besides, the compounds have the characteristics of high efficiency, low toxicity, resistance to drug resistance and the like, and have clinical application value. Moreover, synthesis steps of the compounds are simple, so that the compounds have higher economic utilization value.

Description

Technical field [0001] The invention belongs to the field of medicinal chemistry, and specifically relates to a class of compounds with toll-like receptor modulating effects, their pharmaceutical compositions, preparation methods and uses. Background technique [0002] Toll-like receptors (TLR) are an important class of protein molecules involved in non-specific immunity (natural immunity), and they are also a bridge between non-specific immunity and specific immunity. TLR is a single transmembrane non-catalytic protein that can recognize molecules with conserved structures derived from microorganisms. When microorganisms break through the body's physical barriers, such as skin and mucous membranes, TLR can recognize them and activate the body to produce immune cell responses. Toll-like receptors are characterized by an extracellular leucine-rich domain and a cytoplasmic extension of major transmembrane proteins containing conserved regions. The innate immune system can monitor...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04C07D471/14A61K31/4985A61K31/5377A61P31/12A61P35/00A61P37/06A61P37/02A61P25/24
CPCA61P25/24A61P31/12A61P35/00A61P37/02A61P37/06C07D471/14C07D487/04
Inventor 王加维田从凡王霞
Owner 北京施安泰医药技术开发有限公司
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