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Home / Archives for Recent Patents on Anti-Infective Drug Discovery

Recent Patents on Anti-Infective Drug Discovery

Therapy Of XDR TB with thioridazine a drug beyond patent protection but eligible for patent “as new use”

  • Autores: Amaral L, Molnar J
  • Ano de Publicação: 2010
  • Journal: Recent Patents on Anti-Infective Drug Discovery
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=Therapy+of+XDR-TB+with+thioridazine+a+drug+beyond+patent+protection+but+eligible+for+patent+%E2%80%9Cas+new+use

Mycobacterium tuberculosis that is resistant to Isoniazid (INH) and Rifampin (Rif) and hence, multi-drug resistant (MDR) has progressed to extensive drug resistant (XDR) status. XDR strains of Mycobacterium tuberculosis (XDR Mtb) are resistant, in addition to INH and Rif, to any fluoroquinolone, streptomycin and to any of the injectable anti-TB drugs kanamycin, amikacin and capreomycin.
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Clinical relevance of multiple single-nucleotide polymorphisms in Pneumocystis jirovecii pneumonia: development of a multiplex PCR-single-base-extension.

  • Autores: Amaral L, Dastidar SG, Dutta NK, Karakousis PC, Mazumdar K
  • Ano de Publicação: 2011
  • Journal: Recent Patents on Anti-Infective Drug Discovery
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=New+patentable+use+of+an+old+neuroleptic+compound+thioridazine+to+combat+tuberculosis%3A+a+gene+regulation+perspective

Use of the old antipsychotic phenothiazine thioridazine (THZ) for therapy of multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis (TB) infection is now being seriously considered.
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Targeting the human macrophage with combinations of drugs and inhibitors of Ca2+ and K+ transport to enhance the killing of intracellular multi-drug resistant Mycobacterium tuberculosis (MDR-TB)–a novel, patentable approach to limit the emergence of XDR-TB.

  • Autores: Martins M
  • Ano de Publicação: 2011
  • Journal: Recent Patents on Anti-Infective Drug Discovery
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=Targeting+the+human+macrophage+with+combinations+of+drugs+and+inhibitors+of+Ca(2%2B)+and+K(%2B)+transport+to+enhance+the+killing+of+intracellular+multi-drug+resistant+M.+tuberculosis+(MDR-TB)+-+a+novel%2C+patentable+approach+to+limit+the+emergence+of+XDR-TB

The emergence of resistance in tuberculosis has become a serious problem for the control of this disease. For that reason, new therapeutic strategies that can be implemented in the clinical setting are urgently needed.
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New patentable use of an old neuroleptic compound thioridazine to combat tuberculosis: a gene regulation perspective.

  • Autores: Amaral L, Dastidar SG, Dutta NK, Karakousis PC, Mazumdar K
  • Ano de Publicação: 2011
  • Journal: Recent Patents on Anti-Infective Drug Discovery
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=New+patentable+use+of+an+old+neuroleptic+compound+thioridazine+to+combat+tuberculosis%3A+a+gene+regulation+perspective

Use of the old antipsychotic phenothiazine thioridazine (THZ) for therapy of multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis (TB) infection is now being seriously considered.
Ler mais

Therapy Of XDR TB with thioridazine a drug beyond patent protection but eligible for patent “as new use”

  • Autores: Amaral L, Molnar J
  • Ano de Publicação: 2010
  • Journal: Recent Patents on Anti-Infective Drug Discovery
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=Therapy+of+XDR-TB+with+thioridazine+a+drug+beyond+patent+protection+but+eligible+for+patent+%E2%80%9Cas+new+use%E2%80%9D

Mycobacterium tuberculosis that is resistant to Isoniazid (INH) and Rifampin (Rif) and hence, multi-drug resistant (MDR) has progressed to extensive drug resistant (XDR) status. XDR strains of Mycobacterium tuberculosis (XDR Mtb) are resistant, in addition to INH and Rif, to any fluoroquinolone, streptomycin and to any of the injectable anti-TB drugs kanamycin, amikacin and capreomycin.
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Inhibition of drug efflux in mycobacteria with phenothiazines and other putative efflux inhibitors.

  • Autores: Ainsa JA, Amaral L, Rodrigues L, Viveiros M
  • Ano de Publicação: 2011
  • Journal: Recent Patents on Anti-Infective Drug Discovery
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=Inhibition+of+drug+efflux+in+mycobacteria+with+phenothiazines+and+other+putative+efflux+inhibitors

Mycobacteria are responsible for some of the oldest diseases known to man, usually associated with high morbility and mortality rates. An example is tuberculosis (TB), a major public health problem that accounts for eight million new cases each year.
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Effective therapy with the neuroleptic thioridazine as an adjunct to second line of defence drugs, and the potential that thioridazine offers for new patents that cover a variety of “new uses”.

  • Autores: Amaral L, Jette E, Joseph, Kristiansen, Molnar, Viveiros M
  • Ano de Publicação: 2011
  • Journal: Recent Patents on Anti-Infective Drug Discovery
  • Link: https://apps.webofknowledge.com/full_record.do?product=UA&search_mode=GeneralSearch&qid=16&SID=P2WA5hwy5j35Sqjoq2z&page=1&doc=1

New and active infections of tuberculosis continue to increase globally. Although antibiotic susceptible infections can be readily cured with isoniazide and rifampicin, infections resistant to these two antibiotics, named Multi-Drug Resistant TB (MDR TB), are problematic for therapy, extol high costs in terms of human suffering and finances, and when these MDR infections progress to Extensive Drug Resistant TB (XDR TB) status, they are not only difficult to treat, they produce high levels of mortality regardless of therapeutic modality employed.
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Direct modification of bioactive phenothiazines by exposure to laser radiation.

  • Autores: Amaral L, Andrei IR, Boni M, Fanning S, Martins A, Militaru A, Molnar J, Nastasa V, Pascu A, Pascu ML, Smarandache A, Staicu A, Viveiros M
  • Ano de Publicação: 2011
  • Journal: Recent Patents on Anti-Infective Drug Discovery
  • Link: http://www.ncbi.nlm.nih.gov/pubmed/?term=Direct+modification+of+bioactive+phenothiazines+by+exposure+to+laser+radiation.

Whereas exposure of combinations of a phenothiazine and bacterium to incoherent UV increases the activity of the phenothiazine, exposure of the phenothiazine alone does not yield an increase of its activity. Because the laser beam energy is greater than that produced by the incoherent UV sources, exposure of phenothiazines to specific lasers may yield molecules with altered activities over that of the unexposed parent.
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It is anticipated that as is usually the case, financial motivation will move TZ from its current status potential anti-MDR/XDR agent, to one that will cure MDR and XDR TB. Foreword.

  • Autores: Amaral, Leonard
  • Ano de Publicação: 2011
  • Journal: Recent Patents on Anti-Infective Drug Discovery
  • Link: https://apps.webofknowledge.com/full_record.do?product=UA&search_mode=GeneralSearch&qid=4&SID=2CbhBUDoSw8ZkFBEQLW&page=1&doc=1

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