34 results about "Antimycobacterial" patented technology

The invention relates to biomarkers for diagnosing and / or monitoring tuberculosisin both immunocompetent and immunocompromised individuals, monitoring the responses of individuals to anti-mycobacterial chemotherapy, monitoring the progression of latent tuberculosis to active tuberculosis, differentiating active tuberculosis from latent tuberculosis, and from other clinical conditions that mimic tuberculosis (TB). The invention also relates to methods for diagnosing, treating and monitoring tuberculosis using said biomarkers. The above pertain in all aspects both to pulmonary and extrapulmonary Mycobacterium.tuberculosis infections, with Mycobacterium.tuberculosis being the causative organism in tuberculosis.

The present invention relates to novel benzothiazin derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria.The present invention aims at the generation of new compounds with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance.The solution of the present invention is a compound of the formula Iwherein R1 and R2 are, independently each from other, NO2, CN, CONR7R8, COOR9, CHO, halogen, NR7R8, SO2NR7R8, SR9, OCF3, mono-, di or trifluoromethyl;R3 and R4 are, independently each from other, H, a saturated or unsaturated, linear or branched aliphatic radical having 1-7 chain members, cycloalkyl having 3-6 carbon atoms, benzyl, SR9, OR9;R5 and R6 are, independently each from other, a saturated or unsaturated, halogenated or unhalogenated, linear or branched aliphatic radical having 1-8 chain members, cycloalkyl having 3-6 carbon atoms, phenyl, or R5 and R6 together represent a bivalent radical —(CR92)m—, or R5 and R6 together represent bivalent radicals:wherein m is 1-4, or represent bivalent radicals a saturated or unsaturated mono or polyheterocycles with heteroatoms N, S, O and substituted by (R10)x, wherein x is 1-4;R7, R8 and R9 are, independently each from other H or a saturated or unsaturated, halogenated or unhalogenated, linear or branched aliphatic radical having 1-7 chain members, mono-, di or trifluoromethyl, halogen, phenyl, or R3 and R4 together represent a bivalent radical —(CH2)n— wherein n is 2-7;R10 is H or a saturated or unsaturated, halogenated or unhalogenated, linear or branched aliphatic radical having 1-7 chain members, NO2, NR7R8, CN, CONR7R8, COOR9, CHO, halogen, SO2NR7R8, SR9, OR9, OCF3, mono-, di or trifluoromethyl, benzyl or phenyl.

The invention relates to biomarkers for diagnosing, monitoring and / or treating tuberculosis in both immunocompetent and immunocompromised individuals with or without co-infection with HIV, monitoring the responses of individuals to anti-mycobacterial chemotherapy, monitoring the progression of latent tuberculosis to active tuberculosis, differentiating active tuberculosis from latent tuberculosis, and from other clinical conditions that mimic tuberculosis (TB). The invention also relates to methods for diagnosing, monitoring and / or treating tuberculosis using said biomarkers. The above pertain in all aspects both to pulmonary and extrapulmonary Mycobacterium tuberculosis infections, with Mycobacterium tuberculosis being the causative organism in tuberculosis. The invention therefore finds great utility in assisting with future drug discovery efforts for tuberculosis and also provides proxy clinical end points as well as being an effective predictor of a response to treatment.

Novel pyrrole derivatives of formula (I)and their pharmaceutically acceptable acid addition salts having superior antimycobacterial activity against clinically sensitive as well as resistant strains of Mycobacterium tuberculosis as well as having lesser toxicity compared to known compounds. The use of the novel compounds of formula (I) for treatment of latent tuberculosis including Multi Drug Resistant Tuberculosis (MDR TB). The methods for preparation of the novel compounds, pharmaceutical compositions containing the novel compounds and method of treating MDR TB by administration of compounds of formula (I).

Novel compounds belonging to the class of oxazolidinones possessing potent antimycobacterial properties especially useful in the treatment of acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai. The compound and its pharmaceutically acceptable salts act as antibacterial agents. Also mentioned is a method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial conditions such as Mycobacterium tuberculosis, drug resistant Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai., including administering an antimycobacterially effective amount of the compound and / or pharmaceutically acceptable salts. There is also mentioned a process for the manufacture of the compound or its pharmaceutically acceptable salts.

The present invention provides novel heterocylic amide compounds having useful antimycobacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are alsoprovided.

The invention relates to the field of pharmacy, in particular to the application of antimicrobial peptides in anti-mycobacterium infection drugs. The present invention starts with antimicrobial peptides and develops a series of antimicrobial peptides targeting mycobacteria with special structures and unusual modes of action. The antimicrobial peptides kill bacteria through a membrane destruction mechanism, and bacteria will not develop drug resistance. Antimicrobial peptides, which are the main potential agents for the treatment of tuberculosis, have filled the gap in the absence of new anti-tuberculosis drugs in China for a long time. Therefore, the antimicrobial peptide provided by the present invention can be used to prepare effective drugs against mycobacteria, and is expected to become a potential drug against mycobacterial infection and a main potential drug for treating tuberculosis.

The invention discloses 2-arylamide substituted thiophene imide ester compounds, their preparation method and use, their synthesis method and their use as antibacterial agents in infectious diseases caused by bacteria, especially those caused by mycobacteria. Application in tuberculosis (Tuberculosis, TB). Specifically, the present invention relates to compounds of formula (I), pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising the compounds of the present invention, wherein R 1 , R 2 , R 3 , R 4 , R 5 and Y are as described in the specification. The present invention aims to prepare new compounds with anti-mycobacterial activity, which can be used as potential new drugs for the treatment or prevention of infectious diseases caused by bacteria, especially tuberculosis (TB) diseases caused by Mycobacterium tuberculosis sexual therapy and can be used to overcome problems related to drug resistance.

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.

Substituted benzoxaboroles whose structure comprises Formula (III), wherein R3 is selected from —CH3, —CH2CH3, —CH2═CH2, —CH2CH2CH3, —CH(CH3)2, —CH2CH2═CH2, and cyclopropyl, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, and —CH(CH3)2; compositions containing such compounds, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.

The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and / or their pharmaceutically acceptable salts.

The invention provides for the use of antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit anti-mycobacteria activity, including the mycobacterium causing tuberculosis. Multiple compounds were synthesized and screened for anti-tuberculosis activity. Disclosed herein are a series of compounds with anti-tuberculosis activity, including six leads that completely inhibited bacterial growth at 5 micrograms per ml or less. Three of these compounds were tested to determine MIC and these ranged between 1 and 4 micrograms per ml against both drug susceptible Mycobacterium tuberculosis strains and strains that are multi-drug resistant (MDR) including XDR strains. The compounds developed are derived from parent compound nitazoxanide, which had no inhibitory activity in the stringent testing format used herein. The derivatives were synthesized using a di-nitro-thiophene or 4-Chloro-5-Nitro-thiazole scaffold and R groups connected via a peptide bond (NHCO) to cyclic compounds such as benzene, thiophene or furans. Many of these compounds have broad spectrum activity against Gram positive bacteria including Staphylococcus aureus (MRSA) and Staphylococcus epidermidis. Several of these lead compounds were not toxic for mice at 200 mg / Kg doses administered over a period of three days.