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New use of rifamycin-quinolizidone dual-target molecule

A technology of rifamycin and quinazinone, which is applied in the field of medicinal chemistry, can solve the problem that no literature records the antibacterial activity of intestinal ammonia-producing flora and the like, and achieve the effects of low resistance frequency, strong antibacterial activity and good application prospect.

Inactive Publication Date: 2017-06-13
TENNOR THERAPEUTICS (SUZHOU) LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, Chinese patent ZL200580031655.4 "Rifamycin Derivatives for Treating Microbial Infection" discloses the compound (R)-3-[(4-{1-[1-(3-carboxy-1-cyclopropyl-7 -Fluoro-9-methyl-4-oxo-4H-quinazin-8-yl)-pyrrolidin-3-yl-cyclopropyl]-methylamino}-piperidin-1-ylimino)-ylidene Methyl]-rifamycin SV, the compound has antimicrobial activity against various bacteria such as Gram-positive bacteria and Escherichia coli, but there is no documented antimicrobial activity against intestinal ammonia-producing flora

Method used

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  • New use of rifamycin-quinolizidone dual-target molecule
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  • New use of rifamycin-quinolizidone dual-target molecule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] This embodiment provides the application of the rifamycin-quinazinone dual target molecule represented by formula I in inhibiting ammonia-producing bacteria in the gastrointestinal tract;

[0020]

[0021] Wherein, the gastrointestinal ammonia-producing bacteria include Bifidobacterium infantis subsp. infantis, Bacteroides fragilis, Clostridium difficile, Clostridium perfringens, Escherichia lentus, Escherichia coli, Helicobacter pylori, Lactobacillus salivarius, Clostridium necrosis, Peptostreptococcus, Morganella morganii, Proteus vulgaris, Salmonella, and Yersinia colitis are a combination of one or more.

[0022] In this embodiment, compound I rifamycin-quinazinone dual target molecule has done a drug sensitivity test on pathogens related to hepatic encephalopathy, and the pathogens include the above-mentioned ammonia-producing bacteria group. Except for the liquid microdilution method for Haemophilus spp., the tests for other bacteria use the agar dilution method consis...

Embodiment 2

[0044] This embodiment provides a prescription and preparation method for a rapid-release oral preparation of the rifamycin-quinazinone dual target molecule represented by formula I.

[0045]

[0046] Weigh the rifamycin-quinazinone dual target molecule and excipients shown in formula I according to the above-mentioned prescription amount. Dissolve povidone K30 (PVP K30) and sodium dodecyl sulfate (SDS) in purified water, stir for 1 hour, and use as a binder for later use; use the rifamycin-quinazinone dual target shown in formula I The molecules, mannitol and sodium starch glycolate (DST) are passed through a 30-mesh sieve, and are added to the granulator, premixed, and the impeller stirring speed is 700 rpm for about 15 minutes. Then use a peristaltic pump to add an appropriate amount of purified water and binder to the granulator mixture at a fixed speed (145-165g / min). The impeller of the granulator stirs at 400rpm for about 1 to 2 minutes. After the binder is added , Contin...

Embodiment 3

[0049] This embodiment provides a method for preparing an injection of the rifamycin-quinazinone dual target molecule represented by formula I.

[0050]

[0051] Under the protection of nitrogen, add mannitol, sodium acetaldehyde sulfoxylate and Tween-80 to an appropriate amount of water for injection, add the rifamycin-quinazinone dual target molecule shown in formula I, and stir at medium speed for 10-15 minutes. Wetting the rifamycin-quinazinone dual target molecule shown in formula I, slowly dripping with 1N NaOH, which took about 175 minutes (fast before and slow afterwards), to the rifamycin-quinazinone shown in formula I The dual target molecules are completely dissolved, filtered by two 0.45+0.22μm microporous membranes, the filtrate is filled into 10mL glass bottles, each containing 3.5mL, the glass bottles are transferred to the freeze dryer for lyophilization, and the cap is ready to be prepared The freeze-dried powder injection of rifamycin-quinazinone dual target mol...

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Abstract

The invention discloses application of a rifamycin-quinolizidone dual-target molecule represented in a formula I in inhibition of ammonia producing floras in gastrointestinal tracts. The rifamycin-quinolizidone dual-target molecule represented in the formula I is similar to an antibacterial spectrum of rifaximin and has relatively strong antibacterial activity to common ammonia producing floras in the gastrointestinal tracts; and meanwhile, the rifamycin-quinolizidone dual-target molecule has the property of low drug resistance frequency and has application prospects in prevention and treatment of infection of hepatic encephalopathy and relevant bacterial genera (types). The formula I is as shown in the specification.

Description

Technical field [0001] The invention belongs to the field of medicinal chemistry, and particularly relates to a new use of a rifamycin-quinazinone dual target molecule. Background technique [0002] Hepatic Encephalopathy (HE) is one of the important complications of acute and chronic end-stage liver disease and cirrhosis, which seriously affects the prognosis and quality of life of patients. Once HE occurs in patients with chronic liver disease, the 1-year survival rate does not exceed 50%, and the 3-year survival rate does not exceed 25%. Among them, the minor type (Minimal Hepatic Encephalopathy, MHE), that is, Covert Hepatic Encephalopathy (CHE), patients often have no clinically significant symptoms, and can only be found through neuropsychological tests. According to statistics, at least 30% of patients with liver cirrhosis can be accompanied by different degrees of HE. A recent survey of 16 Class-A hospitals in 13 provinces and cities in China found that the incidence of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4545A61P31/04A61P1/00A61P1/16A61P25/00
CPCA61K31/4545Y02A50/30
Inventor 马振坤袁鹰刘宇王晓梅
Owner TENNOR THERAPEUTICS (SUZHOU) LTD
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