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6 results about "Milbemycin" patented technology

The milbemycins are a group of macrolides chemically related to the avermectins and were first isolated in 1972 from Streptomyces hygroscopicus. They are used in veterinary medicine as antiparasitic agents against worms, ticks and fleas.

Synthesis method of miloabalin or acid salt thereof

The invention relates to a synthesis method of milobalin or acid salt thereof, and belongs to the technical field of medicine synthesis. In order to solve the problem that chiral resolution needs to be adopted in the prior art, the invention provides a synthesis method of miloabalin or an acid salt thereof, which comprises the following steps: under the action of an organic strong base, carrying out Michael addition reaction on a compound shown as a formula III and acetonitrile in a non-polar organic solvent at a low temperature of-50 DEG C or below to obtain an intermediate product; under the alkaline condition, the intermediate product is subjected to an oxidation reaction and a hydrolysis reaction under the action of an oxidizing agent, after the reaction is finished, an intermediate product is obtained through acidification, and the intermediate product is subjected to a high-temperature decarboxylation reaction in an aprotic solvent to obtain a compound of a formula VI; and carrying out Hofmann degradation reaction on the compound of formula VI to obtain the compound of formula I miloabalin or miloabalin acid salt. The method has the advantages of high stereoselectivity, no need of chiral resolution operation, avoidance of the problem of large material loss caused by resolution, high chiral purity and high yield.
Owner:ZHEJIANG EAST ASIA PHARM CO LTD

Novel 16-membered macrolide compound as well as preparation method and application thereof in prevention and control of agricultural and forestry pests

The invention relates to a novel 16-membered macrolide compound 13alpha-O-alpha-L-oleandrosyl-23-alpha-hydroxy-25-isopropyl milbemycin beta3, a preparation method of the novel 16-membered macrolide compound 13alpha-O-alpha-L-oleandrosyl-23-alpha-hydroxy-25-isopropyl milbemycin beta3, and an application of the novel 16-membered macrolide compound 13alpha-O-alpha-L-oleandrosyl-23-alpha-hydroxy-25-isopropyl milbemycin
Owner:TAIZHOU VOCATIONAL COLLEGE OF SCI & TECH

Parasite expelling medicine based on milbemycin oxime praziquantel and application of parasite expelling medicine

The invention provides a parasite expelling drug based on milbemycin oxime praziquantel, and the parasite expelling drug comprises the following components in parts by mass: 10-30 parts of modified milbemycin oxime, 20-50 parts of nano-coated praziquantel, 5-15 parts of a compound synergist, 3-8 parts of a flavoring agent, and 2-5 parts of a disintegrating agent. According to the application of the parasite expelling medicine based on milbemycin oxime praziquantel, the medicine is used for preparing a preparation for preventing or treating mixed parasite infection of dogs and cats, and parasites comprise tapeworms, nematodes, flukes and vermiform mites. Through integrated innovation of chemical modification (succinylated milbemycin oxime), a nanotechnology (HPMC-coated praziquantel) and compounding cooperation (febantel-beta cyclodextrin), the comprehensive advantages of broad-spectrum parasite expelling, long-acting stability, safety and low toxicity are achieved, meanwhile, the problems that in the prior art, palatability is poor, the metabolic burden is high, and environmental adaptability is weak are solved, and the application has good application prospects. The composition is suitable for preventing and treating mixed parasite infection of dogs and cats.
Owner:GUANGZHOU BAIYUN SHANBAOSHEN ANIMAL HEALTH PROD CO LTD

A biological pesticide for controlling Phyllotreta striolata (Fabricius)

ActiveCN116458515BBiocideAnimal repellantsPesticide residueMilbemycin
The present invention belongs to the technical field of pesticides, and particularly relates to a biological pesticide for controlling Phyllotreta striolata. A biological pesticide for controlling Phyllotreta striolata, wherein the active ingredient of the biological pesticide is composed of a polyhedrosis virus compounded with emodin, milbemycin or dihydrosanguinarine, and the mass ratio of the polyhedrosis virus to emodin, milbemycin or dihydrosanguinarine is 1-100:100-1. When the polyhedrosis virus in the biological pesticide of the present invention is compounded with emodin, milbemycin or dihydrosanguinarine, it shows a synergistic effect within a certain mass ratio range, can improve the control effect on Phyllotreta striolata, reduce the dosage of the active ingredient, and reduce pesticide residues and control costs.
Owner:桂林市农业科学研究中心

Transaminase mutant and application of transaminase mutant in synthesis of milobalin intermediate DB01

The invention belongs to the field of molecular biology and enzyme engineering, and provides a transaminase mutant which can catalyze resolution of high-concentration 3-ethyl bicyclo [3.2. 0] hept-3-ene-6-ketone to obtain (1R, 5S)-3-ethyl bicyclo [3.2. 0] hept-3-ene-6-ketone (DB01). The method provided by the invention solves the problems of many ketol post-treatment steps, high cost, easy deterioration of a ketone substrate in the separation process and the like in the existing industrial synthesis route, and has a wide market prospect.
Owner:TIANJIN INST OF IND BIOTECH CHINESE ACADEMY OF SCI

Process for the preparation of metabolites of paraconiothyrium cyclothyrioides pf432 and uses thereof

The application discloses a Paraconiothyrium cyclothyrioides PF432 and a preparation method and application of metabolites thereof. The strain is preserved in the China Center for Type Culture Collection, and the preservation number is CCTCC M 20252943. Through liquid fermentation and chromatographic separation, 32 compounds, i.e. compounds 1-21, 22-29 and 30-32, are obtained from fermentation products of ME culture medium, PD culture medium and Gao's No. 1 culture medium of the strain, and the structures are identified through NMR, MS and single crystal X-ray diffraction analysis. Active tests show that the compounds have significant inhibiting effects on Xanthomonas oryzae pv. oryzae and Xanthomonas campestris pv. oryzae, wherein the in-vivo prevention and treatment effects of compounds 10, 15 and 16 on Xanthomonas oryzae pv. oryzae at a concentration of 500 ng / mL are better than that of positive control milbemycins. The application provides new candidate compounds for green prevention and control of plant bacterial diseases.
Owner:ANHUI AGRICULTURAL UNIVERSITY