92 results about "Milbemycin" patented technology

The invention includes compositions for transmucosal administration to an animal comprising at least one active agent and a pharmaceutically acceptable carrier. A preferred active agent is selected from the group consisting of meloxicam, carprofen, enrofloxacin, clemastine, diphenhydramine, digoxin, levothyroxine, cyclosporine, ondansetron, lysine, zolpidem, propofol, nitenpyram, ivermectin, milbemycin, and pharmaceutically acceptable salts, solvates and esters thereof. In another embodiment, the invention includes methods of treating or preventing a condition in an animal comprising transmucosally administering a composition comprising a therapeutically or prophylactically effective amount of an active agent and a pharmaceutically acceptable carrier.

PCT No. PCT / NZ96 / 00099 Sec. 371 Date Mar. 25, 1998 Sec. 102(e) Date Mar. 25, 1998 PCT Filed Sep. 19, 1996 PCT Pub. No. WO97 / 11709 PCT Pub. Date Apr. 3, 1997A composition comprising an anthelmintic chosen from the class of macrocyclic lactones including but not limited to the avermectins, ivermectin, doramectin, abamectin, milbemycin and moxidectin, together with a vegetable oil and a co-solvent chosen from the group comprising alcohols having four or more carbons atoms. The compositions of the inventions may be formulated as injections, drenches or for topical administration and are suitable for treating helminthiasis in animals.

Microencapsulated formulations of macrolide lactones (abamectin, milbemectin, milbemycins emamectin, avermectins, ivermectins) wherein the active ingredient is protected from UV-degradation, with exceptional release characteristics resembling those of an emulsion concentrate or, if desired, of long-lasting effect; further with appropriate rheological properties, and with reduced toxicity. The invention provides a unique microencapsulation process for the chemical stability and biological activity of mectins, e.g. abamectin, and provides microcapsules of mectins to be used in formulations CS, WG / CS, ZC, EC / CS and any formulation type containing microcapsules and combination with other biologically active ingredients.

A composition prepared for treating animals suffering from parasites which parasites are known to be susceptible to at least one of the avermectins, milbemycins or salicylanilides, comprises for example ivermectin in an amount of from 0.1 to 10%(w / v), a solvent selected from the group consisting of glycerol formal, propylene glycol, polyethylene glycol and combinations thereof, and a salicylanilide such as closantel in a required dosage amount for the animal to be treated, typically about 2.5 mg / kg live weight of the animal to be treated, a polymeric species selected from the group consisting of polyvinylpyrrolidone and polyoxypropylene / polyoxyethylene block copolymers, the said polymeric species improving the bioavailability of closantel to the extend that blood plasma levels of the said compound greater than about 20 ppm over period of treatment are achievable.

Compounds of formula (I) and salts thereof:Wherein R<1 >represents methyl, ethyl, isopropyl or s-butyl; and R<2 >represents hydrogen or alkyl. R<3 >represents hydrogen, optionally substituted alkanoyl, optionally substituted alkenoyl, optionally substituted alkynoyl, alkylsulfonyl, or alkoxycarbonyl, or R<2 >and R<3 >together with the nitrogen atom to which they are attached form a saturated, optionally substituted 4- to 6-membered heterocyclic ring group. The moiety -a- together with the carbon atom to which it is attached forms a 3- to 6-membered cycloalkyl group. These compounds have anthelmintic, acaricidal and insecticidal activity.

Administration of at least one compound of the family of the avermectins or of the family of the milbemycins, notably ivermectin, is useful for the treatment of ophthalmic pathologies, including ocular rosacea.

The present disclosure describes a formulation including a nanoparticle including a polymer-associated mectin and / or milbemycin compounds with an average diameter of between about 1 nm and about 500 nm; wherein the polymer is a polyelectrolyte, and a dispersant or a wetting agent. The disclosure describes various formulations and formulating agents that can be included in the formulations. Additionally, the disclosure describes application to various plants and pests as well as advantages of the disclosed formulations.

This invention relates to antihelminthic pharmaceutical combinations comprising iodinated aromatic compounds, such as disophenol or nitroxynil, with other pharmaceutical active ingredients targeting the treatment of animals. More specifically, this invention concerns pharmaceutical compositions comprising disophenol or nitroxynil with at least one other pharmaceutical antihelminthic active ingredient, selected from among benzimidazoles, thiabendazole, levamisole or tetramisole salts, avermectins or milbemycins and, even more preferably, levamisole salts selected from between levamisole chloride or phosphate.This invention also relates to medications and a method for treating animals comprising such antihelminthic medications.

The invention provides a preparation method of milbemycin oxime. The preparation method of milbemycin oxime comprises the following steps: extracting milbemycins, namely taking milbe mycelia obtained through fermentation as a raw material, extracting, concentrating, extracting, concentrating, extracting again and concentrating again, so as to obtain milbemycin; preparing milbemycin ketone, namely taking the milbemycin as a raw material, establishing an oxidation reaction system, after reaction is finished, filtering, concentrating, extracting and concentrating the reaction system, so as to obtain an intermediate product milbemycin ketone; synthesizing milbemycin oxime, namely dissolving milbemycin ketone with methanol and dioxane, dropwise adding hydroxylamine hydrochloride solution and reacting, concentrating the reaction system, extracting, drying and concentrating, so as to obtain a milbemycin oxime crude product; and purifying milbemycin oxime, namely crystallizing the milbemycin oxime crude product with a mixed solvent of trichloromethane and normal heptane, dissolving a crystalline product with ethanol, dropwise adding into water while stirring for carrying out crystallization, filtering, and drying, so that the milbemycin oxime finished product is obtained. The preparation method of the milbemycin oxime has the advantages that productivity is greatly improved, and cost is obviously reduced, so that the preparation method provided by the invention is obviously better than an existing preparation method.

Compounds of the milbemycin family or derivatives thereof are formulated into pharmaceutical compositions useful for the treatment of dermatological conditions in humans, in particular rosacea.

A spot-on pesticide composition for animals, specifically mammals, namely dogs, which composition comprises a combination of a pyrethroid and a macrocyclic lactone selected from avermectin, ivermectin, selamectin, moxidectin, milbemycin and any combination thereof, and optionally fipronil and / or an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area.

The present invention provides an anthelmintic composition including an avermectin or milbemycin, together with triclabendazole, and a predetermined quantity of rheology modifier, such as Laponite or xanthan gum, sufficient to render the anthelmintic composition suitable as an oral drench.

The invention provides a synthetic method for milbemycin oxime. The method comprises the following steps that 1, an oxidation reaction is performed, wherein milbemycins is used as raw materials, pypocholoride or chlorite is used as an oxidizing agent, piperidines free radical of nitroxide is used as a catalyst, a halide is used as a promoter, all the materials are subjected to the reaction in a dichloromethane solvent at the temperature being minus 5-15 DEG C for 0.5-4 h, and postprocessing is performed on a reaction product to obtain an intermediate product of milbemycin ketone; 2, an oximation reaction is performed, wherein methyl alcohol and 1,4-dioxane are used as a reactive solvent, hydroxylamine hydrochloride is used as an oximation reagent, the reaction is performed at the temperature being 25-35 DEG C for 10-16 h, and postprocessing and purification are performed to obtain milbemycin oxime. According to the method, industrial production of the milbemycin oxime is achieved in China for the first time, and the yield of the obtained product is higher than that of similar products both at home and abroad. Due to the fact that the pypocholoride is used as the oxidizing agent, pyridine nitroxide free radical is used as a catalyst, conditions are mild, few side reactions exist, the yield is high, and the cost is low.

The present invention relates to methods of treating a mycobacterial infection. In particular, this invention relates to methods, uses and compounds for use in treating mycobacterial infections, including tuberculosis. For example, the compounds may be an avermectin or a milbemycin. The avermectin or milbemycin may be selected from, but not limited to, one or more of ivermectin, moxidectin or selamectin. Exemplary microbial infections that may be treated include, but are not limited to, infections caused by Mycobacterium tuberculosis, Mycobacterium bovis, other mycobacteria of the tuberculosis complex, and non-tuberculous mycobacteria, including Mycobacterium ulcerans.

Double compartment skincare products confine a first compartment containing an anhydrous composition including an active ingredient, and a second compartment, wherein the active ingredient is selected from among compounds of the avermectin family and compounds of the milbemycin family, and are useful as medicaments for the treatment and / or prevention of dermatological conditions / afflictions.

The invention relates to milbemycins producing recombinant streptomyces. In comparison with corresponding wild streptomyces or start streptomyces generating the recombinant streptomyces, the milbemycins producing recombinant streptomyces is characterized in that at least one of the following genes of the recombinant streptomyces is inactivated: gene mpca5 with code SEQ ID NO:8 or amino acid sequence with at least 80% of sequence identity, gene mpca3 with code SEQ ID NO:9 or amino acid sequence with at least 80% of sequence identity, gene mpca4 with code SEQ ID NO:10 or amino acid sequence with at least 80% of sequence identity and gene mpca5 with code SEQ ID NO:11 or amino acid sequence with at least 80% of sequence identity. The invention also relates to a method for generating the recombinant streptomyces and a method for producing milbemycins by use of the recombinant streptomyces.

The invention discloses a milbemycins tree trunk injection liquid which is prepared from 0.5-30 percent of milbemycins, 5-20 percent of surfactant and 70-98 percent of solvent. The milbemycins tree trunk injection liquid is applied by adopting a trunk injection application technology, has a good prevention and control effect on various diseases of trees, and particularly has high prevention and control effects on pine wood nematode diseases. The milbemycins tree trunk injection liquid is efficient, economic and environmentally-friendly, and is an agent special for preventing and controlling tree diseases.

The present disclosure describes a formulation including a nanoparticle including a polymer-associated mectin and / or milbemycin compounds with an average diameter of between about 1 nm and about 500 nm; wherein the polymer is a polyelectrolyte, and a dispersant or a wetting agent. The disclosure describes various formulations and formulating agents that can be included in the formulations. Additionally, the disclosure describes application to various plants and pests as well as advantages of the disclosed formulations.

The invention discloses a gene cluster for regulating and controlling synthesis of milbemycins, recombinant streptomyces as well as a preparation method and application of the recombinant streptomyces, belongs to the technical field of bioengineering and provides the gene cluster for synthesis of the milbemycins aiming to the problem of difficulty in separation and purification of the milbemycinsat present. The gene cluster includes a kelC gene, a kelD gene and a kelE gene. The invention also provides the recombinant streptomyces, relative to an original strain for producing the recombinant streptomyces, at least one of the kelC gene, the kelD gene and the kelE gene in a genome is inactivated. The invention also provides a construction method of the recombinant streptomyces and a method of using the recombinant streptomyces to produce the milbemycins. The gene cluster is suitable for production and purification of the milbemycins.

An anti-parasiticidal composition presented as a topical “pour-on” product for treating animals infected by parasites which are known to be susceptible to salicylanilides, especially closantel, alone or together with at least one other anti parasitic compound of the avermectin or milbemycin type and offers enhanced bioavailability of the salicylanilide by provision of a delivery system comprising at least 20% (v / v) of one or more alcohols, and optionally including a polymeric moiety selected from the group consisting of polyvinylpyrrolidone (PVP), polyoxypropylene / polyoxyethylene block copolymers (poloxamer), and polyethylene glycols (PEG), thereby improving the bioavailability of e.g. closantel (as assessed with respect to blood plasma levels of closantel).

This invention provides for novel antiparasitic and pesticidal derivatives of avermectin and milbemycin compounds in which two avermectin or milbemycin members are linked together by a chemical linker. The resulting compounds may be used in veterinary compositions which are used in treating, controlling and preventing of endo- and ectoparasite infections and infestations in animals or for combating pests in plants or plant propagation material.

The use of compounds of the milbemycin class as inhibitors of efflux pumps in microbes or other cells is described, along with pharmaceutical compositions incorporating a milbemycin. Also described is a method of screening for compounds which inhibit a CDR1, CDR2, BEN, or FLU1 efflux pump or a pump with components having a high level of protein level sequence similarity with the components of those efflux pumps.

This present invention relates to a method for the purification of milbemycins which comprises washing a milbemycin with a base. According to the method, impurities can be easily removed without using an industrially troublesome technique such as chromatography.

The invention relates to a preparation method of a milbemycin oxime intermediate II. The preparation method comprises the step of reacting milbemycins (I) with pypocholoride as an oxidant in the presence of a catalyst and bromide to generate the milbemycin oxime intermediate II. The preparation method provided by the invention is simple in process operation, high in yield, low in cost, and is very suitable for industrial production. The formula I and the formula II are shown in the description, wherein R is equal to CH3 or C2H5.

The present invention relates to microcapsules comprising the macrolides abamectin, mibamectin, milbemycin, emamectin, ivermectin and generally mectins, wherein the active ingredients are protected from UV degraded, with specific release profile similar to emulsifiable concentrates or if desired with long acting; also with suitable rheological properties and reduced toxicity. The present invention provides a unique microencapsulation method for the chemical stability and biological activity of mectins such as abamectin and provides for CS, WG / CS, ZC, EC / CS formulations and any formulation comprising microcapsules Mectins microcapsules in type and in combination with other biologically active ingredients.

Veterinarian composition comprising an organic salt of levamisole in combination with at least one avermectine and / or milbemycine. A veterinarian formulation comprising of organics salts of levamisole, more specifically to the disophenolat salt of levamisole and the nitroxynil-salt of levamisole with avermectines and milbemycines and its use in treatment of helminthiasis in mammals, in particular in bovines, swines, caprines, equines, ovines, canines and felines.

The invention discloses a method and a fermentation medium for producing milbemycins through streptomyces fermentation. The fermentation level of milbemycins can be improved by improving the medium and fermentation process, so as to significantly improve the yield of the milbemycins and to reduce production cost; and the method is simple and easy to implement, and is applicable to industrial production.