522 results about "Macrolide Antibiotics" patented technology

A method is provided for the treatment of age-related macular degeneration by administering various antibiotics, such as tetracycline and its derivatives, rifamycin and its derivatives, macrolides, and metronidazole, to a patient in a therapeutically effective amount.

This invention relates to novel macrolides, to the preparation of novel macrolides, to the use of such novel macrolides for preventing, treating, or ameliorating various conditions, and to the use of such novel macrolides as antibacterial agents.

In particular this invention provides for spot-on compositions for the treatment or prophylaxis of parasite infestations in mammals or birds which comprise:

• • (1) a composition comprising
    • (A) an effective amount of a 1-phenylpyrazole derivative; and/or
    • (B) an effective amount of a macrocyclic lactone antihelmintic or antiparasitic agent;
  • (2) an acceptable liquid carrier vehicle; and
  • (3) optionally, a crystallization inhibitor.

The invention also provides for a method of treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal or bird an effective amount of a composition according to the present invention.

The invention belongs to the technical field of the farm chemical, and in particular relates to a plant insecticidal protective agent and an application thereof. The invention provides the plant insecticidal protective agent which is recomposed by food suppressing hydrazine and organic phosphorus (I), pyrethroids insecticides (ii), insect growth regulation agent (III), Macrolides (IV), heterocyclic insecticidal component (V), carbamates (VI) or Nereistoxin pesticide and the application thereof. The recomposed insecticidal composite remarkably improves the insecticidal effect, at least has four acting ways at the same time such as touch out, stomach toxicity, internal absorption and antifeedant so as to adequately protect the plant, favors the delay of the production of the drug resistanceof the insects through different acting ways, and enlarges the pest control spectrum. The composite can be widely applicable to the control of different chewing mouthparts, piercing-sucking mouthparts, lapping mouthparts and rasping mouthparts pests.

This invention provides a process for producing a macrocyclic lactone compound, which comprises cultivating Actinoplanes sp. FERM BP-3832, in the presence of L-proline, L-hydroxyproline or L-nipecotic acid, and then isolating a macrocylic lactone compound from the fermentation broth. The compounds produced by this process include a compound of the following formula:The present invention also relates to a pharmaceutical composition comprising the same, which is useful as immunosuppressive, antimycotic, antitumor agent or the like.

Ocular solutions containing at least one macrolide antibiotic and/or mycophenolic acid provide anti-inflammatory, anti-cell proliferation, anti-cell migration, anti-angiogenesis, antimicrobial, and antifungal effects. In one embodiment, the solution is administered intraocularly after cataract surgery before insertion of a replacement intraocular lens, resulting in reduced posterior capsular opacification which may eliminate the need for a subsequent surgery. The solution may be one that is invasively administered, for example, an irrigation or volume replacement solution containing at least one macrolide antibiotic such as tacrolimus, sirolimus, everolimus, cyclosporine, and ascomycin, or mycophenolic acid. The solution may be one that is non-invasively or topically administered in the form of drops, ointments, gels, creams, etc. and may include eye lubricants and contact lens solutions.

The present invention relates to a method of simultaneously detecting a plurality of agro-veterinary drug residues in bee products. The extracted liquid trichloroacetic acid or perchloric acid and the extracted liquid acetate, phosphate or borate solution are added into a sample; the pH value is controlled between 4.5 and 9.0; the mixed solution is centrifuged, the filtrate is added into a solid phase extraction column to be extracted, the extraction column is eluted and dried, the column is washed by oxalic acid-methanol solution, the volume of the eluent is defined by the aqueous solution of methanol, the eluent is added into liquid chromatography-tandem mass spectrometry to be analyzed and tested, the acquired chromatographic peak is contrasted with the known standard chromatographic peak of the drug, and according to the retention time and the abundance of the mass spectrum ions, the specific name of the detected drug is determined. The method only requires one pre-treatment of the sample, and thus can simultaneously extract 11 classes and more than 60 kinds of veterinary drug residues, such as sulfonamides, quinolones, macrolides, lincomycins, nitroimidazoles, beta-lactams, tetracyclines, chloromycetins, trinethoprims, chlordimeform, triadimenol and the like, the efficiency of analysis is high, and the detection cost is greatly reduced.

The invention discloses a novel method for preparing tulathromycin and relates to a semi-synthetic macrolide antibiotic. The method comprises the following steps: simultaneously protecting 2'-hydroxyl and 6a-amino of desmethyl azithromycin with acetyl, then carrying out oxidation and epoxidation on 4''-hydroxy, then removing the protecting groups under alkaline alcohol solution conditions, and carrying out nucleophilic addition on 4''-epoxy group with n-propylamine to obtain the target compound tulathromycin. Compared with the prior art, the method for preparing tulathromycin has the advantages of simple process, mild conditions, high yield and the like, and is beneficial to industrial production.

There is disclosed the formulation of a poorly soluble macrolide antibiotic, such as clarithromycin together with beta-cyclodextrin, and optionally a dicarboxylic acid wherein the particles of the formulation are prepared using microfluidization techniques in a particle size in the range of from 5 to 15 microns.

A method of combatting atherosclerosis by administering an effective amount of a macrolide antibiotic, for example an azalide such as azithromycin, optionally together with one or more pharmaceutically acceptable carriers or excipients, to a subject.

The present invention relates (a) to new compounds represented by Formula I:

wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, V represents an anti-inflammatory steroid or nonsteroid subunit, or an antineoplastic or antiviral subunit and L represents a linking group covalently linking M and V; (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory/neoplastic/viral diseases and conditions in humans and animals.

Disclosed are mixtures and compositions for controlling invertebrate pests relating to combinations comprising (a) 3-bromo-N-[4-cyano-2-methyl-6-[(methylamino)carbonyl]phenyl]-1-(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxamide, an N-oxide, or a salt thereof, Formula (1) and (b) at least one invertebrate pest control agent selected from neonicotinoids, cholinesterase inhibitors, sodium channel modulators, chitin synthesis inhibitors, ecdysone agonists, lipid biosynthesis inhibitors, macrocyclic lactones, GABA-regulated chloride channel blockers, juvenile hormone mimics, ryanodine receptor ligands, octopamine receptor ligands, mitochondrial electron transport inhibitors, nereistoxin analogs, pyridalyl, flonicamid, pymetrozine, dieldrin, metaflumizone, biological agents, and salts of the foregoing. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a mixture or composition of the invention.

The present disclosure is directed to novel macrolide antibiotics of Formula 1 and pharmaceutically acceptable salts and prodrugs thereof; and the chemical syntheses and medical uses of these novel macrolide antibiotics for the treatment and/or management of infections caused by various aerobic and anaerobic gram-positive and gram-negative microorganisms as well as various mycobacteria.

The present invention provides novel macrolide compounds of the formulas 1 wherein: R is hydroxyl or methoxy; R.sup.1 is selected from the group consisting of hydrogen, hydroxyl, halide, NH.sub.2, OR.sup.9, 2 where R.sup.9 is C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, aryl or heteroaryl and R.sup.10 and R.sup.11 are each independently hydrogen, C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, or aryl; R.sup.2 and R.sup.3 are each independently selected from the group consisting of hydrogen, C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, aryl, alkylaryl, alkenylaryl, alkynylaryl or R.sup.2 and R.sup.3 together form a cycloalkyl or a cycloaryl moiety; R.sup.4 is hydrogen or methyl; R.sup.5 is hydrogen, hydroxyl, oxo, or together with R.sup.6 and the carbons to which they are attached form a cyclic carbonate; R.sup.6 is hydrogen, hydroxyl, OR.sup.12 where R.sup.12 is C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, or together with R.sup.5 and the carbons to which they are attached form a cyclic carbonate; R.sup.7 is methyl, C.sub.3-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl; R.sup.8 is C.sub.1-C.sub.10 alkyl, C.sub.2-C.sub.10 alkenyl, C.sub.2-C.sub.10 alkynyl, alkylaryl, alkenylaryl, alkynylaryl, amidoalkylaryl, amidoalkenylaryl, or amidoalkynylaryl; and, x is a single or a double bond.

The invention discloses an insecticide acaricide taking an oligose and macrolides composition as a synergist, and in particular relates to a synergism composition capable of enhancing the insecticiding effect of the insecticide acaricide. The composition comprises oligose and a macrolides insecticide; the macrolides insecticide is abamectin, pleocidin, emamectin benzoate or ivermectin; the oligose is pectic oligosaccharide, sodium alginate oligosaccharides or chitosan oligosaccharide; the mass part ratio of the oligose to the macrolides insecticide is (1-30):(1-10). The synergism composition can enhance the insecticidal efficacy of the insecticide acaricide and realize the synergism effect with other insecticide acaricides.

The present inventions relates to a method of increasing beef production in cattle with feed additives, comprising feeding cattle with feed, comprising an effective amount of an ionophore in combination with a macrolide antibiotic, and thereafter feeding cattle with feed, comprising zilpaterol and essentially no ionophore or macrolide antibiotic for the succeeding about 20 to 40 days.

The invention discloses a method for preparing macrolide antibiotics molecular engram polymer microspheres, which is characterized by comprising the following steps: dissolving a dispersant, namely polyvinyl alcohol or hydroxyethyl cellulose into secondary distilled water to prepare a water-phase dispersion liquid; dissolving engram molecules and functional monomers into an organic solvent to prepare an oil-phase mixture; adding the oil-phase mixture into the water-phase dispersion liquid under the action of stirring, adding an initiator, namely azo-bis-iso-butyrynitrile into the mixture, performing thermal initiation polymerization on the mixture in water bath, and obtaining polymer microspheres; and adopting an ultrasonic extraction method to elute the engram molecules in a butyl acetate aqueous solution or a methanol solution of acetic acid, using distilled water to wash the engram molecules, and performing vacuum drying on the engram molecules to obtain the macrolide antibiotics molecular engram polymer microspheres. Through the method, the macrolide antibiotics molecular engram polymer microspheres are prepared in water phases and are recognized in the water phases; the reorganization result is close to that obtained by a natural biological molecular recognition system; and the invention provides a method for recognizing, separating and analyzing hydrophilic medicaments .

The invention discloses a harmless treatment method of macrolide antibiotic residues, which belongs to the technical field of solid waste treatment. The method comprises the following steps: firstly, inversely and mechanically stirring effectively broken sclertium, and then harmlessly treating the macrolide antibiotic residues with selectomycin harmless treatment microbial inoculum. The treated antibiotic residues can be used as vegetable fertilizer additive to promote the vegetable growth and solve the problem of environmental pollution caused by macrolide antibiotic residues, thus the method realizes the comprehensive utilization of resources and has better economic benefits.

Ocular solutions containing at least one macrolide antibiotic and/or mycophenolic acid provide anti-inflammatory, anti-cell proliferation, anti-cell migration, anti-angiogenesis, antimicrobial, and antifungal effects. In one embodiment, the solution is administered intraocularly after cataract surgery before insertion of a replacement intraocular lens, resulting in reduced posterior capsular opacification which may eliminate the need for a subsequent surgery. The solution may be one that is invasively administered, for example, an irrigation or volume replacement solution containing at least one macrolide antibiotic such as tacrolimus, sirolimus, everolimus, cyclosporine, and ascomycin, or mycophenolic acid. The solution may be one that is non-invasively or topically administered in the form of drops, ointments, gels, creams, etc. and may include eye lubricants and contact lens solutions. The solution may contain a supratherapeutic concentration of agent(s) so that a therapeutic concentration of a topically administered solution accumulates in a diseased ocular structure sufficient to treat the disease. The agent(s) may be formulated with polymers or other components for extended or slow release to provide a substantially constant concentration over the course of treatment.

The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof:

which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

The invention relates to a lindenrane-type dimerization sesquiterpenoids (structural format I and II) separated from chloranthus plant, a preparation method and applications thereof on medicament in curing type 2 diabetes mellitus, adiposity and other complications caused thereby. In the formula I and II, R1-R17 is hydrogen or oxygen or hydroxy group or acyl (acetyl, angelica acyl, hydroxyl angelica acyl, tigloxyl, senecioyl, hydroxyl senecioyl, carboxyl senecioyl and 1, 4-carboxybutyryl group) or double bond or alkyl (methyl) or macrolide can be formed between R16 and R17, wherein X is oxygenor nitrogen. The biological experiment proves that the compound has stronger insulin-sensitizing activity.