31 results about "Antituberculars" patented technology

The invention relates to a new compound antitubercular preparation containing gatifloxacin, and a preparation method thereof. The compound antitubercular preparation comprises rifampicin, isoniazide, pyrazinamide and gatifloxacin. Each unit of preparation contains 100-150mg of rifampicin, 60-120mg of isoniazide, 200-400mg of pyrazinamide and 100-200mg of gatifloxacin. The addition of gatifloxacin in the preparation can shorten the course of treatment of tuberculosis and improve the treatment effect; and degradation of the rifampicin can be reduced through dry method granulating tabletting, thus improving the bioavailability of rifampicin and improving the curative effect of the medicament. The compound preparation can be prepared into common tablets, double-layer coated-core tablets or pellet-core tablets.

A derivative of β-carboline alkaloid harmine, 10,12-diheptanoyl-11-hydroxy-3-methyl-β-carboline, prepared by a Friedel-Crafts acylation of harmine is reported as a novel potent antitubercular drug.

The invention discloses a semi-synthetic aminoglycoside antibiotic of 1-N-acetyl micronomicin, and pharmaceutically acceptable salt and a preparation method thereof. The preparation method of 1-N-acetyl micronomicin comprises the following steps: the formylation protection is carried out on C2'-NH2 and C3-NH2 of micronomicin basic groups, the 3,-2-two-N-formoxyl micronomicin, the acetylation reaction is then carried out to obtain 1-N-acetyl-3,-2-two-N-formoxyl micronomicin, the obtained products are subject to hydrolysis reaction in alkali solution, and the 1-N-acetyl micronomicin is obtained through formylation protection for removing 2'-NH2 and 3-NH2. The 1-N-acetyl micronomicin has the advantages that in-vitro antitubercular bacteria and antibiotic activity experiments prove that the 1-N-acetyl micronomicin has higher antibiotic activity to mycobacterium tuberculosis gram-positive bacteria and negative bacteria, in addition, the toxicity of medicine on ears and kidneys is greatly reduced, and higher clinical application value is realized.

The invention relates to a new compound antitubercular preparation containing gatifloxacin, and a preparation method thereof. The compound antitubercular preparation comprises rifampicin, isoniazide, pyrazinamide and gatifloxacin. Each unit of preparation contains 100-150mg of rifampicin, 60-120mg of isoniazide, 200-400mg of pyrazinamide and 100-200mg of gatifloxacin. The addition of gatifloxacin in the preparation can shorten the course of treatment of tuberculosis and improve the treatment effect; and degradation of the rifampicin can be reduced through dry method granulating tabletting, thus improving the bioavailability of rifampicin and improving the curative effect of the medicament. The compound preparation can be prepared into common tablets, double-layer coated-core tablets or pellet-core tablets.

A steroidal compound n-hexyl-p-stigmasteryloxy-benzoate is reported as a novel potent antitubercular drug.

The invention relates to a radiolabeled irradiation anthranone or naphtho dianthrone compound, which has the specific affinity capability in biosome necrotic tissues and simultaneously comprises chemical elements or isotopes with unstable nucleus. Radiation can be emitted out in a period when the compound is decayed to the stable state, and the radiation is sufficient to damage the adjacent tubercle bacillus for target radiation treatment, so the antitubercular treatment possibility is improved. The compound has a special advantage that the drug resistance tuberculosis can be treated through single-time or multi-time dosage of the radiolabeled irradiation anthranone or naphtha dianthrone compound.

An antimycobacterial combination and composition for treating tuberculosis are described. The compounds used are N-(3-[[4-(3-trifluoromethylphenyl)piperazinyl]methyl]-2-methyl-5-phenyl-pyrrolyl)-4-pyridylcarboxamide of formula (I) or a pharmaceutically acceptable non-toxic salt thereofand an amount of one or more first line antitubercular drugs.

The invention discloses an isoniazid thiadiazine thione derivative, which solves the problem that the existing derivative has poor lipid solubility of active ingredient, and can not dissolve in water or can not highly disperse. The structure of the derivative can be presented by INH-THTT-R-THTT-INH, wherein ING represents the structure of isoniazid of antitubercular drug, THTT is a ring structure, and R is linear chain, non-linear chain or annular alkyl compound containing two primary amines (including alkyl structures of different substituent groups). The derivative can be prepared into highly-dispersed drug delivery system, including the dosage form of liposome, solid lipid nanospheres, niosomes, micro emulsion and the like. The derivative can not only improve the lipid solubility of isoniazid, but also hydrolyze and release isoniazid active compound in vivo, increases the penetrability of isoniazid cell, reduces the tolerance of isoniazid during therapy and improves the curative effect.

A steroidal compound n-hexyl-p-stigmasteryloxy-benzoate is reported as a novel potent antitubercular drug.

Invention provides antitubercular compounds selected from propargylated 1,2,3 triazoles of Formula I, wherein, X is sulfur(S) or a sulphone (A), n, m represent independently an integer O or 1, with the provision that when ‘n’ is 1, ‘m’ is 1; R1 is hydrogen; C1-C6 linear or branched alkyl group optionally substituted with aryl group; halogen; or aryl group optionally substituted with —OCH3, halogen, and nitro; R2 and R3 are selected from the group consisting of hydrogen, C1-C6 alkyl optionally substituted with heterocyclic ring of 5 to 6 ring atoms containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, which may be substituted with alkyl, arylalkyl, linear or branched alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or allyl or propargyl groups consisting of 1 to 6 carbon atoms; Z is C1-C6 alkyl optionally substituted with heterocyclic ring of 1 to 6 ring atoms, containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, which may be substituted with arylalkyl, linear or branched alkenyl, substituted alkenyl, alkynyl, substituted alkynyl allyl or propargyl groups consisting of 1 to 6 carbon atoms; with the provision that when ‘m’ is 1, and ‘n’ is zero; R1 is selected from the group consisting of hydrogen, halogen; C1-C6 linear or branched alkyl group optionally substituted with aryl group or aryl group optionally substituted with —OCH3, halogen, and nitro, R2 and R3 are selected from the group consisting of hydrogen, C1-C6 alkyl optionally substituted with heterocyclic ring of 5 to 6 ring atoms containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, which may be substituted with alkyl, arylalkyl, linear or branched alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or allyl or propargyl groups consisting of 1 to 6 carbon atoms; Z is selected from the group consisting of halogen, C1-C6 linear or branched alkyl group optionally substituted with heterocyclic ring of 1 to 6 ring atoms, containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, wherein the heterocyclic ring may further be substituted with halogen, alkyl, arylalkyl.

The invention discloses an application of clinafloxacin amino derivatives and medicinal salts thereof in preparing antitubercular medicaments. In the structural general formula of the clinafloxacin amino derivatives, R is -(CH2)nNR<1>R<2>, -CH(CH2CH2XCH3)NH2, 2-pyrrolidyl or -OR3; n is 0 or 1; R1 and R2 are separately hydrogen, methyl, 2-hydroxyethyl, (R)-1-ethyl-2-hydroxyethyl, 2-aminoethyl, 3-(dimethylamino)propyl, hydroxyl, amino, methylamino, methoxyl or thiourea group; X is S or SO2; R3 is methyl or isobutyl; the compounds have certain inhibitory effect on standard sensitive strains, clinically isolated sensitive strains and clinically isolated drug-resistant strains of mycobacterium tuberculosis, the antitubercular activity of a part of compounds is stronger than that of ofloxacin and clinafloxacin and weaker than that of moxifloxacin, thus providing a new research direction for the antitubercular medicaments, and being beneficial to clinical treatment of tuberculosis.