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Patent
Institute Pasteur Korea | Date: 2015-04-17

The present invention relates to small molecule compounds and their use in the treatment of diseases, in particular viral diseases, in particular hepatitis C virus (HCV).


Grant
Agency: Cordis | Branch: FP7 | Program: CP-SICA | Phase: HEALTH-2007-2.3.4-1 | Award Amount: 4.49M | Year: 2008

Visceral leishmaniasis is caused by the protozoan parasites Leishmania donovani and Leishmania infantum and is a potentially fatal disease in endemic areas around the world. During the infectious cycle, Leishmania alternate between the insect promastigote stage and the vertebrate aflagellate amastigote stage that proliferates inside infected host macrophages provoking the pathology of the disease. This consortium uses a highly interdisciplinary approach to reveal Leishmania signaling molecules associated with amastigote virulence, with the major aim to exploit parasite-specific pathways for anti-leishmanial drug development. We use innovative drug screening concepts not applied previously on parasitic systems. We will utilize visual high-content screening to discover compounds capable to kill intracellular Leishmania amastigotes without deteriorating the host cell. This phenotype-based strategy relies on fluorescent parasites and macrophages as read-outs and will allow simultaneous assessment of anti-leishmanial activity and host cell toxicity under physiological conditions. We will apply a target-based strategy utilizing recombinant Leishmania protein kinases for inhibitor identification and structure-guided drug design. The identification of appropriate target kinases, with only limited homology to their mammalian counterparts will rely on in silico analysis by applying novel bioinformatic tools developed by consortium members, and in vitro assay based on their phospho-transferase activity towards recombinant Leishmania phospho-proteins. The major objectives of this proposal are (i) to screen small molecule and peptide libraries for hit compounds with leishmanicidal activity using phenotype- and target-based strategies, (ii) to identify anti-parasitic lead compounds and assess their pharmacokinetic profiles using cell-culture and experimental infection models for leishmaniasis, and (iii) to initiate lead optimization by structure-based drug design.


Grant
Agency: Cordis | Branch: FP7 | Program: CP-FP | Phase: HEALTH.2010.2.3.2-2 | Award Amount: 8.47M | Year: 2011

Early stage Drug Discovery efforts over the last 5 years have resulted in the identification of a number of promising lead compounds in the fight against TB. These leads need to be further progressed and optimised into candidates for pre-clinical development through the Drug Development progression cascade. Three compound families are of particular interest: 1) InhA Inhibitors, 2) New potent whole cell anti-tubercular compounds with unknown mode of action and 3) new Beta-lactam/Beta-lactamase combinations for TB. A preclinical package is already in place for some of them, but further work is necessary for others in order to justify the progression of a single anti-tubercular family to the more resource intensive stages of preclinical and clinical development. The project will encompass the parallel progression of the three compound families through: A) Lead Optimization Chemistry efforts and MoA studies (Genetic and Proteomic) for whole cell inhibitors, B) In vitro and in vivo evaluation of a new orally bioavailable Beta-lactam alone or in combination with a Beta-lactamase inhibitor to evaluate the sterilising potential of the new drug/s and C) the optimization of an InhA inhibitor for later preclinical development. These efforts will yield candidate molecules for new information rich in vitro assays of antimycobacterial activity (artificial granuloma, activity against slow/non growing cells and activity against clinical isolates) as well as for in vivo safety and efficacy evaluation in different animal models of infection (acute and/or chronic). At this stage a single compound family will be prioritized. Further studies will be performed assessing the potential for shortening treatment in stand alone therapy as well as in combination regimens both in vitro and in vivo. Finally a Clinical Development plan will be put in place for the selected candidate molecule.


Grant
Agency: Cordis | Branch: FP7 | Program: CP-IP | Phase: HEALTH-2009-2.3.2-2 | Award Amount: 19.00M | Year: 2010

With 14.4 million prevalent cases and 1.7 million deaths tuberculosis (TB) remains one of the most serious infectious diseases to date. An estimated 2 billion people are believed to be infected with Mycobacterium tuberculosis and at risk of developing disease. Multi- and extensively drug resistant strains are increasingly appearing in many parts of the world, including Europe. While with current control measures the Millennium Development Goals (MDGs) set for 2015 may be achieved, reaching these would still leave a million people per year dying from TB. Much more effective measures, particularly more effective vaccines will be essential to reach the target of eliminating TB in 2050. Two successive FP5 and FP6 funded projects, Tuberculosis (TB) Vaccine Cluster (2000-2003) and TBVAC (2004-2008), have in the recent decade made significant contributions to the global TB vaccine pipeline, with four vaccines (out of nine globally) being advanced to clinical stages. Both projects strongly contributed to the strengthening and integration of expertise and led to a European focus of excellence that is unique in the area of TB vaccine development. In order to sustain and accelerate the TB vaccine developments and unique integrated excellence of TBVAC, a specific legal entity was created named TuBerculosis Vaccine Initiative (TBVI). The NEWTBVAC proposal is the FP7 successor of TBVAC, and will be coordinated by TBVI. The proposal has the following objectives : 1) To sustain and innovate the current European pipeline with new vaccine discoveries and advance promising candidates to clinical stages; 2) To design new, second generation vaccines based new prime-boost strategies and/or new (combinations of) promising subunit vaccines, that will impact on reduction of disease in exposed individuals; 3) To sustain and innovate discovery, evaluation and testing of new biomarkers, that will be critically important for future monitoring of clinical trials.


The current treatments for visceral leishmaniasis are old and toxic with limited routes of administration. The emergence of drug-resistant Leishmania threatens the efficacy of the existing reservoir of antileishmanials, leading to an urgent need to develop new treatments. It is particularly important to review and understand how the current treatments act against Leishmania in order to identify valid drug targets or essential pathways for next-generation antileishmanials. It is equally important to adapt newly emerging biotechnologies to facilitate the current research on the development of novel antileishmanials in an efficient fashion. This review covers the basic background of the current visceral leishmaniasis treatments with an emphasis on the modes of action. It briefly discusses the role of the immune system in aiding the chemotherapy of leishmaniasis, describes potential new antileishmanial drug targets and pathways, and introduces recent progress on the utilization of high-throughput phenotypic screening assays to identify novel antileishmanial compounds. © 2016 Elsevier B.V.


Patent
QURIENT Co. and Institute Pasteur Korea | Date: 2012-04-20

The present invention refers to: a compound having the general formula (I), wherein n is 0, 1, 2 or; m is 0, 1, 2 or 3; o is 0, 1, 2 or 3; W, X, Y and Z are independently selected from CH, N or N-oxide; A is NR^(4), CO, CS, OP(O)(O), PO, CH_(2), or a heteroarly selected from the group consisting of (a), (b), (c), (d), (e), (f), (g); V is CO, O, S, CH_(2), or NR^(5); as well as its use in treating inflammatory diseases such as asthma, COPD, inflammation post infection, arthritis, atherosclerosis, pain and dermatitis.


Patent
Institute Pasteur Korea | Date: 2014-05-14

The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.


Patent
Institute Pasteur Korea, French Institute of Health and Medical Research | Date: 2014-04-28

The present invention relates to 4H-pyrido[1,2-a]pyrimidin-4-one compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.


The present invention relates to a method of detecting and/or quantifying expression of a target protein candidate in a cell, and to a method of identifying a target protein of a small molecule modulator.


Patent
Institute Pasteur Korea and Qurient Co. | Date: 2014-08-01

The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.

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