32 results about "Telithromycin" patented technology

The invention discloses a method for improving erythrocin yield through a negative control gene SACE_3446 on an inactivation saccharopolyspora erythraea chromosome. Saccharopolyspora erythraea is used for producing erythrocin. The erythrocin and derived drugs of the erythrocin such as clarithromycin, azithromycin and telithromycin are used widely in clinic. Erythrocin high-producing strain screening is very important in industrial production. The erythromycin biosynthesis negative control gene SACE_3446 is screened from a saccharopolyspora erythraea TetR family. Compared with erythrocin yield of an original strain, deletion mutants of the saccharopolyspora erythraea SACE_3446 is improved remarkably, the erythrocin is returned to low yield after gene complementation of the SACE_3446, and therefore the SACE_3446 gene is a erythromycin biosynthesis negative control gene. The inactivation saccharopolyspora erythraea SACE_3446 gene can improve the erythrocin yield through a genetic engineering way. Due to the fact that erythromycin biosynthesis gene control is a network system, upstream and downstream control factors acted by SACE_3446 control factors can be found by using the SACE_3446 as an object. The erythrocin yield can also be improved by changing upstream or downstream control factor genes of the saccharopolyspora erythraea SACE_3446 control factors.

The invention discloses a new method for preparing macrolides semi-synthesizing antibiotic tallysomycin. The mother core part uses 6-methoxy bristacin as raw material, which is dewatered on the effect of the base after dewatering, acylating, re-etherification and oxidant, and then it reacts with the carbonyl diimidazole to obtain the intermediate (VI); the lateral chain part uses 3-acetyl pyridine as raw material and is hydrolyzed after bromide and reacting with the hexamine, then it ringed with the potassium sulfocyanide and reacts with the N-(4-bromide butyl)-phthalimide on base condition after the effect of diluted nitric acid and then it is hydrazinolysized to obtain the lateral chain (XIII); the intermediate (VI) reacts with the lateral chain (XIII) to synthesize the tallysomycin.

The present invention discloses applications of azithromycin and telithromycin in anti-Ebola virus infection, wherein the applications comprise applications of azithromycin or/and telithromycin in prevention or treatment of Ebola virus infection or combined applications of azithromycin or/and telithromycin and other anti-virus drugs.

The invention relates to a medicine for curing and radically curing malaria. The weight parts of the components are: 1 to 5 parts of arteannuin ramification and 5 to 100 parts of large ring lactone antibiotic. The arteannuin ramification can be any artesunate medicine, such as arteannuin, artesunate, artemether or dihydro-arteannuin. The large ring lactone antibiotic can be first, second or third generation large ring lactone antibiotic, such as erythrocin, azithromycin, telithromycin and kui erythrocin. The medicine of the invention is low in poison, safe, rapid in effect, high sufficient and can radically cure malaria, which solves the problem that the after-combustion rate and the recurerence rate of the arteannuin ramification medicine is high after curing malaria; furthermore, the invention is high in medicine safety and has the functions of preventing, curing and blocking spreading of malaria, which is not only suitable for the common malaria infected area, but also more suitable for the infected area with multiple drug fastness malaria, thereby being very safe and effective to the children and pregnant women patients.

This invention relates to an eye use transmission system of macrolide type antibiotic hyaluronic acid natrium. The goal of this invention is to provide a macrolide type antibiotic eye use medicine preparation with carrier is hyaluronic acid or its salt. It is used to cure germ eye region infection. The macrolide type antibiotic in this invention includes antibiotic that has 14 yuan,15yuan, 16yuan large ring construction features , for example, natural antibiotic bring by streptomycete erythromycin, josamycin, spiramycin, medemycin etc. and semisynthesis derivant from by structure modification of natural antibiotic, such as roxithromycin, azithromycin, clarithromycin, rokitamycin, telithromycin.

The present invention relates to the process for the preparation of compounds of formula (I) or its pharmaceutically acceptable salts

wherein, R is

The present invention relates to novel polymorphs of Telithromycin designated as Form I, II and III and its process for preparation. Also it provides Telithromycin with at least 99% purity.

The present invention relates to a process for the preparation of erythromysin derivatives, in particular telithromycin of formula (I) and its pharmaceutically acceptable salts, providing the isolated intermediates in crystalline form of superior stability and purity.

The invention relates to a semi-synthetic method for preparing a new antibiotic as telithromycin (I), belonging to pharmacy technical field, which comprises using self-manufactured Fe-V-Ti-ZSM-5 of 3-(2-mercaptoglyoxaline-4-radical) pyridine and hydrogen dioxide solution catalysis oxidization desulfhydro method to prepare high-purity side chain key intermediate compound (II), reacting the compound (II) with abomacetin decorated mother ring (III) protected by benzoyl, removing protective radical (benzoyl) to obtain telithromycin. The preparation method has mild conditions, high product yield and eliminated column chromatography separation purification replaced by simple recrystallization purification, to reduce device investment and reduce cost with simple operation and support for industrial production.

The invention provides a novel acylide derivative which has a general formula I or a general formula II or which is an acceptable salt or ester composed of a compound having the general formula I or the general formula II and an inorganic acid or organic acid. The novel acylide derivative according to the embodiment has a novel structure and has excellent antibacterial activity on clinically common sensitive bacteria and drug resistant bacteria, and part of compounds of the novel acylide derivative are as good as or better than telithromycin in inhibitory and bactericidal activity. The existing knowledge about the structure-activity relation of acylides is broken through, the novel acylide derivative having bactericidal activity is provided and is as good as the telithromycin in the market in activity, and the novel acylide derivative is easy to industrially produce. Researches show that targets of the acylides acting on bacterial ribosomes are different from those of ketolides. In total, compared with the prior ketolides having defects, the novel acylide derivative has better market prospect in resisting drug resistant bacteria.

The invention relates to fructose injection of an antibiotic medicine. The fructose injection of the antibiotic medicine consists of antibiotics, fructose and water and also comprises proper additives, wherein the antibiotics comprise gatifloxacin, levofloxacin, ciprofloxacin, pazufloxacin, fleroxacin, sparfloxacin, moxifloxacin, pefloxacin, rufloxacin, lomefloxacin, norfloxacin, caderofloxacin, azithromycin, telithromycin, ornidazole, secnidazole, tinidazole, metronidazole, clindamycin, lincomycin, fluconazole, etimicin, netilmicin, amikacin as well as medicinal acid addition salt, esterification compounds, derivatives and the like; the fructose injection is prepared from the antibiotics; the advantages that the injection is convenient to use and takes effect rapidly are achieved; and compared with the glucose injection, the fructose injection is easier to absorb and utilize, more suitable for antisepsis and anti-inflammation, energy supply and body liquid supplementation of patientssuffering from diabetes, heart diseases and liver diseases, and enlarges the use range.

The invention discloses compound telithromycin nanoemulsion oral liquid. The grain size of the oral liquid ranges from 1nm to 100nm, the compound telithromycin nanoemulsion oral liquid is prepared by raw materials including, by mass percent, from 35 to 45% of surface active agent, from 1 to 5% of cosurfactant, from 4 to 12% of oil phase, from 1 to 3.5% of telithromycin, from 0.1 to 0.3% of bromhexine hydrochloride and the balance deionized water, and the sum of the mass percents of the raw materials is 100%. The telithromycin is the first and the uniquely listed ketolide medicine in the worldat present, and has broad-spectrum antibiotic activity, lower selective drug resistance and cross drug resistance with other ketone antibiotics; and after the telithromycin is compatible with the bromhexine hydrochloride, a high treatment effect in terms of treating respiratory tract infection is realized. Compound telithromycin nanoemulsion remarkably increases activities of two types of medicines, is high in safety, simple in preparation and low in energy consumption, can be produced in a batch manner without special equipment, and has a wide market prospect in the field of medicine.

The invention discloses a prevention and cure chemical agent for sisal hemp mealybug. The chemical agent is prepared from the following raw materials in parts by weight: 1 to 2 parts of kaolin, 0.5 to1.6 parts of konjac glucomannan, 4 to 8 parts of sepiolite, 0.2 to 0.4 part of vegetable oil, 3 to 6 parts of calcium acetate, 4 to 8 parts of potassium dihydrogen phosphate, 2 to 4 parts of biological surfactant, 6 to 15 parts of fungus concentrate, 3 to 5 parts of fatty alcohol-polyoxyethylene ether, 2 to 6 parts of alkyl polyoxyethylene ether, 1 to 3 parts of sucrose fatty acid ester, 0.5 to 1.6 parts of r-amino butyrate, and 0.2 to 0.6 part of telithromycin. After being sprayed, the chemical agent is adhered onto the surface of mealybug, the components of the chemical agent such as the biological surfactant, fatty alcohol-polyoxyethylene ether, alkyl polyoxyethylene ether and the like can damage the shell of the mealybug, so that active ingredients such as the fungus concentrate can enter the body of the mealybug so as to kill the mealybug, and the killing effect is good; and the konjac glucomannan, the kaolin and the sepiolite in the chemical agent wraps the fungus concentrate, so that the chemical effect period can be prolonged.

The invention provides a fructose injection of an antibiotic drug. The injection is composed of antibiotics, fructose and water. The injection also can contain proper additives. The antibiotic comprise gatifloxacin, levofloxacin, ofloxacin, ciprofloxacin, pazufloxacin, fleroxacin, sparfloxacin, moxifloxacin, pefloxacin, rufloxacin, lomefloxacin, norfloxacin, caderofloxacin, azithromycin, telithromycin, ornidazole, secnidazole, tinidazole, metronidazole, clindamycin, lincomycin, fluconazole, etimicin, netilmicin, amikacin and medicinal acid additive salts, esterified compounds, derivatives and the like. The antibiotics are prepared into the fructose injection. Besides the advantages of convenience in use and quickness to take effect of the injection, compared with a gluconic infection, the injection provided by the invention is more easily absorbed and utilized, is more suitable for preventing bacteria and diminishing inflammation, supplying energy and supplementing body fluids for patients with diabetes, heart disease and liver disease, so that the application range of the injection is expanded.

The invention discloses a method of preparing ketolide macrolide antibiotics. The method of preparing ketolide macrolide antibiotics comprises the following steps: S1, performing a reaction on a side chain with triphosgene to generate isocyanate; S2, performing butt-joint of isocyanate obtained in the step 1 with isocyanate and performing cyclization to generate an oxazolone compound; and S3, removing a hydroxyl protective group from the oxazolone compound obtained in the step 2 to obtain telithromycin. The method disclosed by the invention does not use an unstable carbonyl imidazole intermediate, so that impurities of macrolide structures are prevented from being generated, and relatively high reaction yield and better product purity are obtained.

The invention relates to feed and in particular relates to an insecticidal composition capable of being compounded with a macrolide compound. Specifically, the insecticidal composition contains active ingredients A and B, and the balance of aids, composition components and auxiliary components needed in the process of preparing related formulations of pesticides, wherein the active ingredient A is selected from novel telithromycin, and the active ingredient B is selected from emamectin benzoate. The compound composition experiment discovers that an obvious synergistic effect can be achieved between the two active ingredients, the insecticidal efficiency is greatly improved, and compared with that of a single agent, the pest control effect of the insecticidal composition disclosed by the invention is generally improved by about 10-15%. Moreover, the fast-acting property is greatly improved, the lasting period is long, the repeated usage frequency and dosage of the pesticides are less, the agricultural cost is reduced, and the environmental pollution is alleviated.

The present invention relates to stable amorphous 3-De[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribohexopyranosyl)oxy]-11,12-dideoxy-6-O-methyl-3-oxo-12,11-[oxycarbonyl[[4-[4-(3-pyridinyl)-1H-imidazol-1-yl]butyl]imino]]erythromycin (telithromycin), methods for the preparation thereof, the use of stable amorphous telithromycin in the treatment of bacterial infections and to pharmaceutical compositions comprising stable amorphous telithromycin.

This disclosure provides a method of potentiating the efficacy of certain antibiotics by administering a therapeutically effect amount of the antibiotic in combination with SPR741. In certain embodiments the antibiotic is retapamulin, telithromycin, or aztreonam. The disclosure also provides a method of treating a bacterial infection by administering SPR741 in combination with a second antibioticand pharmaceutical compositions comprising SPR741 and a second antibiotic.

A fructose injection of an antibiotic drug comprises antibiotics, fructose and water and can contain proper additives. The antibiotics comprise gatifloxacin, levofloxacin, ofloxacin, ciprofloxacin, pazufloxacin, fleroxacin, sparfloxacin, moxifloxacin, pefloxacin, rufloxacin, lomefloxacin, norfloxacin, cadrofloxacin, azithromycin, telithromycin, ornidazole, secnidazole, tinidazole, metronidazole, clindamycin, lincomycin, fluconazole, etimicin, netilmicin, amikacin as well as pharmaceutical acid added salts, esters and derivatives thereof. The antibiotics are prepared into the fructose injection, beside injection advantages of being convenient to use and taking effect quickly, compared with glucose injections, the injection is easier to absorb and utilize and more suitable for antisepsis andanti-inflammation, energy supply and body fluid supplement use for patients suffering from diabetes, heart disease and hepatopathy, and the use range of the injection is enlarged.