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Nucleoside compound, pharmaceutically acceptable salt, composition and application thereof

A technology of nucleoside compounds and compositions, applied in the field of nucleoside compounds, pharmaceutically acceptable salts and compositions, can solve the problems of cat pain, easy recurrence and the like, and achieve the effect of excellent anti-feline calicivirus effect

Active Publication Date: 2021-06-11
嘉兴金派特生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no targeted drug for feline stomatitis caused by feline calicivirus. Hormones or antibiotics are commonly used as supportive therapy, which is prone to relapse. In severe cases, full-mouth tooth extraction is used for treatment, which brings great pain to cats.

Method used

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  • Nucleoside compound, pharmaceutically acceptable salt, composition and application thereof
  • Nucleoside compound, pharmaceutically acceptable salt, composition and application thereof
  • Nucleoside compound, pharmaceutically acceptable salt, composition and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0088]

[0089] N-bromosuccinimide (NBS) (122 mg) was added to a mixture of compound a (0.20 g) and DMF (2 mL), and the mixture was stirred at 10-20° C. for 1 hour. LCMS monitoring showed that the target Ms was generated, and the reaction solution was prepared and purified. Compound a-1 (0.20 g, 78.5% yield, 99.7% purity) was obtained as a white solid. 1 HNMR: (400MHz, DMSO-d6): δ7.98(s,H),7.06(s,1H),6.25(s,1H),5.20(s,1H),4.93(m,1H),4.53(dd ,1H),4.05(m,1H),3.93(m,1H),3.64-3.67(m,1H),3.48-3.51(m,1H).

[0090]

[0091] Add Zn(CN) to the mixed solution of compound a-1 (0.50g) and DMF (2mL) 2 (0.67g, 5.71mmol, 362μL, 5.99eq), CuI (18.2mg, 95.3μmol, 0.10eq) and Pd(PPh 3 ) 4 (441mg, 381μmol, 0.40eq), under nitrogen protection, then the reaction solution was stirred at 140°C for 2 hours. LCMS showed the generation of target Ms. The reaction solution was filtered, and 10 mL of water was added to the filtrate, followed by extraction with dichloromethane (20 mL*2). After li...

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Abstract

The invention relates to a nucleoside compound, a pharmaceutically acceptable salt, a composition and an application thereof. The nucleoside compound has a structure shown as a formula (I) shown in the description. The nucleoside compound has a better anti-feline calicivirus effect, and therefore, the nucleoside compound disclosed by the invention has the potential of preparing the medicine for treating or preventing the diseases (such as cat stomatitis) caused by the feline calicivirus.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to nucleoside compounds, pharmaceutically acceptable salts, compositions and applications thereof. Background technique [0002] Feline calicivirus is a non-enveloped, single-stranded RNA virus with a spherical capsid. It is highly contagious and can cause moderate, self-limiting acute oral problems and upper respiratory tract diseases. It is the most infectious upper respiratory tract disease in cats. One of the common pathogens. At present, there is no targeted medicine for feline stomatitis caused by feline calicivirus. Hormone or antibiotics are generally used as supportive therapy, which is prone to relapse. In severe cases, full-mouth tooth extraction is used for treatment, which brings great pain to cats. Therefore, there is an urgent need for a series of effective anti-calicivirus compounds. Contents of the invention [0003] Based on this, it is necessary to...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/7068A61K31/53A61P31/14
CPCC07D487/04A61K31/7068A61K31/53A61P31/14A61K2300/00Y02A50/30
Inventor 不公告发明人
Owner 嘉兴金派特生物科技有限公司
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