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Triazine compound or pharmaceutically acceptable salt, isomer, pharmaceutical composition and application thereof

A compound and triazine technology, applied in the field of preparation of triazine compounds, can solve the problems of not finding hERG inhibition, mutagenicity/cleavage and phototoxicity, etc., and achieve lower single dose and better treatment. effect, the effect of increasing blood concentration

Pending Publication Date: 2022-05-27
YAOKANG ZHONGTUO (JIANGSU) PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, no safety concerns such as hERG inhibition, mutagenicity / crackogenicity, and phototoxicity were found in in vitro studies of S-217622

Method used

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  • Triazine compound or pharmaceutically acceptable salt, isomer, pharmaceutical composition and application thereof
  • Triazine compound or pharmaceutically acceptable salt, isomer, pharmaceutical composition and application thereof
  • Triazine compound or pharmaceutically acceptable salt, isomer, pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1: Synthesis of Compound S1

[0047]

[0048] Step 1: Synthesis of deuterated compound 4a

[0049]

[0050] (1) Compound 1 (37.2g, 0.2mol) was suspended in water (190ml) and concentrated hydrochloric acid (50ml, 0.6mol), at 0°C, NaNO 2 Aqueous solution (13.80g, 0.2mol, 32.20mL) was added dropwise to the above solution, then stirred for 30min, filtered, pre-cooled NaBF 4 (24.20 g, 0.22 mol) in an aqueous solution (90 ml) was added to the above filtrate and stirred at 0°C for 40 min. The stirring was stopped, filtered, and the filter cake was washed with cold ethanol and diethyl ether. The filter cake was collected and dried to obtain the diazonium salt (22.5 g, 0.097 mol). Dissolve the diazonium salt in CHCl 3 (231 mL), KOAc (15.15 g, 0.155 mol) was added to the above solution, stirred at room temperature, monitored by TLC, the reaction was complete, and the stirring was stopped. Add water (200ml) to quench the reaction, extract with DCM (100mL × 3), co...

Embodiment 2

[0069] Example 2: Synthesis of Compound S2

[0070]

[0071] The synthesis method is as in Example 1, only need to replace the corresponding raw material. 1 H NMR (300MHz, DMSO-d 6 ,DCl inD 2 O)δ9.32(1H,s),8.42(1H,s),7.77(1H,s),7.46(1H,m),5.36(2H,s),5.08(2H,s),4.18(3H, s),3.94(1H,s).MS(ESI,m / z):534(M + +1).

Embodiment 3

[0072] Example 3: Synthesis of Compound S3

[0073]

[0074] The synthesis method is as in Example 1, only need to replace the corresponding raw material. 1 H NMR (300MHz, DMSO-d 6 ,DCl inD 2 O)δ9.32(1H,s),8.42(1H,s),7.77(1H,s),7.46(1H,m),5.36(2H,s),5.08(2H,s),4.18(3H, s),3.94(2H,s).MS(ESI,m / z):533(M + +1).

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PUM

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Abstract

The invention discloses a triazine compound with a structure as shown in a general formula I or pharmaceutically acceptable salt, isomer, metabolite, prodrug, solvate or hydrate, pharmaceutical composition and application thereof. The triazine compound provided by the invention overcomes the defects of single structure, lack of non-covalent high-efficiency small-molecule inhibitors and the like of the existing anti-coronavirus drugs, has good inhibitory activity on 3C-like cysteine protease, has excellent pharmacokinetic properties, and has a good treatment effect on infectious diseases.

Description

technical field [0001] The invention belongs to the field of innovative medicinal chemistry, and relates to a triazine compound, its preparation method, pharmaceutical composition and application. Background technique [0002] Coronaviruses (CoVs) are a family of enveloped positive-strand RNA pathogenic viruses that cause acute and chronic diseases, including central nervous system disease, the common cold, lower respiratory tract infections, and diarrhea. HCoV-229E and HCoV-OC43 are the first zoonotic strains identified since 1995. In 2003, the severe acute respiratory syndrome coronavirus, now named SARS-CoV-1, caused the first global human coronavirus pandemic, resulting in more than 8,000 people with progressive respiratory failure and 916 deaths (case fatality ratio 10-15). %). In the following eight years, zoonotic coronaviruses HCoV-NL64 and HCoV-HKU1 with significantly reduced lethality were discovered. In 2012, the Middle East respiratory syndrome coronavirus (MER...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/14A61K31/53A61P31/14
CPCC07D403/14A61P31/14Y02P20/55
Inventor 蒋晟肖易倍郭炳华张阔军刘春河
Owner YAOKANG ZHONGTUO (JIANGSU) PHARMA TECH CO LTD
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