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Patent
Inventiva | Date: 2015-02-19

The invention relates to compounds of formula (I). where R, R_(1), R_(2), n, A and Cy have the meanings indicated in the description. The compounds of formula (I) are Nurr-1 modulators.


The invention relates to compounds of formula I The compounds of formula I are useful for the treatment of diseases where inhibition of the YAP/TAZ-TEAD interaction is required.


Santos R.C.V.,Centro Universitario Franciscano | Santos R.C.V.,Laboratorio Of Nanotecnologia | Lopes L.Q.S.,Centro Universitario Franciscano | Lopes L.Q.S.,Laboratorio Of Nanotecnologia | And 14 more authors.
Journal of Asia-Pacific Entomology | Year: 2014

Paenibacillus larvae and Melissococcus plutonius are the primary bacterial pathogens of honeybees and the causative agents of American and European foulbrood disease (AFB and EFB) respectively. Such diseases have been gaining importance since there are few therapeutic options beyond the reporting of microorganisms resistant to conventional antibiotics. Due to the inefficiency and/or low efficacy of some antibiotics, researches with nanotechnology represent, possibly, new therapeutic strategies. Nanostructured drugs have presented some advantages over the conventional medicines, such as slow, gradual and controlled release, increased bioavailability, and reduced side-effects, among others. In this study, in vitro antimicrobial activity of tea tree oil (TTO) nanoparticles against Paenibacillus species, including P. larvae and M. plutonius strains was evaluated. Minimal inhibitory concentration (MIC) in Mueller-Hinton or KSBHI broth by the microdilution method was assessed. TTO registered MIC values of 0.18-6.25%, while the MIC values obtained for the TTO nanoparticle were of 0.01-0.93%. The possible toxic effect of TTO and TTO nanoparticle has been assessed by the spraying application method in the concentrations higher than the MICs. Bee mortality was evident only in treatment with TTO and the TTO nanoparticles show no toxic effects after 7. days of observation. Our results showed for the first time that TTO nanoencapsulation presented a high activity against Paenibacillus species and M. plutonius strains showing that the use of nanotechnology may represent one alternative way for the treatment or prevention of AFB and EFB. •TTO nanoencapsulation presented a high activity against Paenibacillus species and M. plutonius strains showing that the use of nanotechnology may represent one alternative way for the treatment or prevention of AFB and EFB. © 2014 Korean Society of Applied Entomology, Taiwan Entomological Society and Malaysian Plant Protection Society.


News Article | November 14, 2016
Site: www.prnewswire.co.uk

ReportsnReports.com adds "Idiopathic Pulmonary Fibrosis - Pipeline Review, H2 2016" to its store providing comprehensive information on the therapeutics under development for Idiopathic Pulmonary Fibrosis (Respiratory), complete with analysis by stage of development, drug target, mechanism of action (MoA), route of administration (RoA) and molecule type. The guide covers the descriptive pharmacological action of the therapeutics, its complete research and development history and latest news and press releases. Complete report on H2 2016 pipeline review of Idiopathic Pulmonary Fibrosis with 78 market data tables and 15 figures, spread across 260 pages is available at http://www.reportsnreports.com/reports/743476-idiopathic-pulmonary-fibrosis-pipeline-review-h2-2016.html . Idiopathic pulmonary fibrosis (IPF) is a progressive and fatal disease characterized by inflammation and scarring of lung tissue and loss of lung function. Symptoms of IPF include dry cough, shortness of breath, especially during or after physical activity, lasting tiredness and weight loss. Risk factors include smoking, environmental exposure, viral infections, family history and abnormal acid reflux. Treatment includes antioxidants, biological response modulators, anti-fibrotic agents and anticoagulants. Companies discussed in this Idiopathic Pulmonary Fibrosis Pipeline Review, H2 2016 report include AdAlta Pty Ltd., Aeolus Pharmaceuticals, Inc., Afferent Pharmaceuticals, Inc., Apellis Pharmaceuticals Inc, ARMO Biosciences, Inc., Asahi Kasei Pharma Corp., Biogen Inc, Bioneer Corporation, BiOrion Technologies B.V., Bristol-Myers Squibb Company, Celgene Corporation, Chrysalis Pharma SAS, Compugen Ltd., Cynata Therapeutics Limited, F. Hoffmann-La Roche Ltd., FibroGen, Inc., FibroStatin SL, Galapagos NV, GenKyoTex S.A., GlaxoSmithKline Plc, Global Blood Therapeutics, Inc., GNI Group Ltd., HEC Pharm Co., Ltd., Histocell S.L., iBio, Inc., Immunomet Therapeutics, Inc., Inventiva, Isarna Therapeutics GmbH, Kadmon Corporation, LLC, Kasiak Research Private Limited, Kolltan Pharmaceuticals, Inc., Kyorin Pharmaceutical Co., Ltd., Lung Therapeutics Inc, Moerae Matrix, Inc., MorphoSys AG, Novartis AG, Nuevolution AB, Pharmaxis Limited, Promedior, Inc., ProMetic Life Sciences Inc., Pulmatrix, Inc., Respira Therapeutics Inc, Ribomic Inc., Saje Pharma, LLC, Samumed LLC, Sanofi Sorrento Therapeutics, Inc., SPR Biosciences LLC, Teva Pharmaceutical Industries Ltd., Therabron Therapeutics, Inc., Vicore Pharma AB and Yuhan Corporation. The Idiopathic Pulmonary Fibrosis (Respiratory) pipeline guide also reviews of key players involved in therapeutic development for Idiopathic Pulmonary Fibrosis and features dormant and discontinued projects. The guide covers therapeutics under Development by Companies /Universities /Institutes, the molecules developed by Companies in Phase III, Phase II, Phase I, IND/CTA Filed, Preclinical and Discovery stages are 1, 14, 13, 1, 49 and 8 respectively for Similarly, the Universities portfolio in Preclinical and Discovery stages comprises 4 and 3 molecules, respectively for Idiopathic Pulmonary Fibrosis. Idiopathic Pulmonary Fibrosis (Respiratory) pipeline guide helps in identifying and tracking emerging players in the market and their portfolios, enhances decision making capabilities and helps to create effective counter strategies to gain competitive advantage. The guide is built using data and information sourced from Global Markets Direct’s proprietary databases, company/university websites, clinical trial registries, conferences, SEC filings, investor presentations and featured press releases from company/university sites and industry-specific third party sources. Additionally, various dynamic tracking processes ensure that the most recent developments are captured on a real time basis. The report helps in identifying and tracking emerging players in the market and their portfolios, enhances decision making capabilities and helps to create effective counter strategies to gain competitive advantage. Another newly published market research report titled Bronchiectasis - Pipeline Review, H2 2016 provides comprehensive information on the therapeutic development for Bronchiectasis, complete with comparative analysis at various stages, therapeutics assessment by drug target, mechanism of action (MoA), route of administration (RoA) and molecule type, along with latest updates, and featured news and press releases. It also reviews key players involved in the therapeutic development for Bronchiectasis and special features on late-stage and discontinued projects. The report enhances decision making capabilities and help to create effective counter strategies to gain competitive advantage. It strengthens R&D pipelines by identifying new targets and MOAs to produce first-in-class and best-in-class products. Companies Involved in Therapeutics Development are Alitair Pharmaceuticals, Inc., Bayer AG, Grifols, S.A., Insmed Incorporated, Kamada Ltd., Polyphor Ltd., Raptor Pharmaceutical Corp., Recipharm AB, Savara Inc. and Vertex Pharmaceuticals Incorporated. Bronchiectasis Pipeline market research report of 84 pages is available at http://www.reportsnreports.com/reports/743455-bronchiectasis-pipeline-review-h2-2016.html . ReportsnReports.com is your single source for all market research needs. Our database includes 500,000+ market research reports from over 100+ leading global publishers & in-depth market research studies of over 5000 micro markets. With comprehensive information about the publishers and the industries for which they publish market research reports, we help you in your purchase decision by mapping your information needs with our huge collection of reports. Connect With Us on:


George D.M.,AbbVie Bioresearch Center | Breinlinger E.C.,AbbVie Bioresearch Center | Friedman M.,AbbVie Bioresearch Center | Zhang Y.,WuXi AppTec | And 11 more authors.
Journal of Medicinal Chemistry | Year: 2015

Protein kinase Cθ (PKCθ) regulates a key step in the activation of T cells. On the basis of its mechanism of action, inhibition of this kinase is hypothesized to serve as an effective therapy for autoimmune diseases such as rheumatoid arthritis (RA), inflammatory bowel disease (IBD), and psoriasis. Herein, the discovery of a small molecule PKCθ inhibitor is described, starting from a fragment hit 1 and advancing to compound 41 through the use of structure-based drug design. Compound 41 demonstrates excellent in vitro activity, good oral pharmacokinetics, and efficacy in both an acute in vivo mechanistic model and a chronic in vivo disease model but suffers from tolerability issues upon chronic dosing. © 2014 American Chemical Society.


Ruzehaji N.,French Institute of Health and Medical Research | Ruzehaji N.,French National Center for Scientific Research | Frantz C.,French Institute of Health and Medical Research | Ponsoye M.,French Institute of Health and Medical Research | And 13 more authors.
Annals of the Rheumatic Diseases | Year: 2016

Background The pathogenesis of systemic sclerosis (SSc) involves a distinctive triad of autoimmune, vascular and inflammatory alterations resulting in fibrosis. Evidence suggests that peroxisome proliferator-activated receptors (PPARs) play an important role in SSc-related fibrosis and their agonists may become effective therapeutic targets. Objective To determine the expression of PPARs in human fibrotic skin and investigate the effects of IVA337, a pan PPAR agonist, in in vitro and in vivo models of fibrosis. Methods The antifibrotic effects of IVA337 were studied using a bleomycin-induced mouse model of dermal fibrosis. The in vivo effect of IVA337 on wound closure and inflammation were studied using an excisional model of wound healing. Results Low levels of PPARa and PPAR? were detected in the skin of patients with SSc compared with controls. In mice, IVA337 was associated with decreased extracellular matrix (ECM) deposition and reduced expression of phosphorylated SMAD2/3-intracellular effector of transforming growth factor (TGF)-ß1. Although the antifibrotic effect of pan PPAR was similar to that of PPAR? agonist alone, a significant downregulation of several markers of inflammation was associated with IVA337. Despite its anti-inflammatory and antifibrotic properties, IVA337 did not interfere with wound closure. In vitro effects of IVA337 included attenuation of transcription of ECM genes and alteration of canonical and non-canonical TGF-ß signalling pathways. Conclusions These findings indicate that simultaneous activation of all three PPAR isoforms exerts a dampening effect on inflammation and fibrosis, making IVA337 a potentially effective therapeutic candidate in the treatment of fibrotic diseases including SSc. © 2016 BMJ Publishing Group Ltd & European League Against Rheumatism.


Volpato A.,Santa Catarina State University | Grosskopf R.K.,Santa Catarina State University | Santos R.C.,Centro Universitario Franciscano | Vaucher R.A.,Centro Universitario Franciscano | And 5 more authors.
Journal of Essential Oil Research | Year: 2015

The aim of this study was to verify in vitro the influence of rosemary, andiroba, and copaiba essential oils on different stages of the cattle tick Rhipicephalus microplus. Female ticks were collected from naturally infected cows and treated in vitro with these essential oils at concentrations of 5% and 10%. All tests were performed in triplicate using positive (amitraz 10%) and negative (untreated) controls. It was possible to observe that rosemary, andiroba, and copaiba essential oils inhibited female reproduction at concentrations of 5% (45.0%, 77.5%, and 71.6%, respectively) and 10% (55.7%, 92.0,% and 86.7%, respectively) compared with amitraz (72.9%). Additionally, andiroba (10%) and copaiba (5% and 10%) oil solutions also had an acaricidal effect (100%), similarly to the positive control. The andiroba and copaiba oils showed an ovicidal effect, which effected hatchability. Rosemary oil showed neither acaricidal nor ovicidal effect. Therefore, based on these results, we were able to show that all oils and concentrations tested may affect tick reproduction by inhibiting tick oviposition and hatchability. In addition, andiroba and copaiba oils exhibited ovicidal and acaricidal effects. © 2015 Taylor & Francis.


Pazinato R.,Santa Catarina State University | Klauck V.,Santa Catarina State University | Volpato A.,Santa Catarina State University | Tonin A.A.,Federal University of Santa Maria | And 10 more authors.
Experimental and Applied Acarology | Year: 2014

The aim of this study was to verify the influence of tea tree oil (TTO) (Melaleuca alternifolia) tested in its pure and nanostructured (TTO nanoparticles) forms on the reproduction of female Rhipicephalus microplus. For our purpose, female ticks were collected from naturally infected animals and treated in vitro with TTO (1, 5, and 10 %) and TTO nanoparticles (0.075, 0.375, and 0.75 %). In order to validate the tests, they were performed in triplicate using positive (amitraz) and negative (untreated) controls. It was possible to observe that pure TTO (5 and 10 %) and TTO nanoparticles (0.375 and 0.75 %) showed 100 % reproductive inhibition on female ticks. Additionally, pure TTO (1 %) also showed an acaricide effect (70 %), similarly to the positive control (78.3 %). This is the first study demonstrating the activity of pure TTO and TTO nanoparticles on female ticks. Therefore, based on these results, we were able to show that both forms and all concentrations of M. alternifolia affected tick reproduction by inhibiting egg laying and hatching. We were also able to show that TTO nanoparticles potentiated the inhibitor effect of pure TTO on the reproduction of R. microplus. © 2013 Springer Science+Business Media Dordrecht.


The present invention relates to a method of treatment of a mucopolysaccharidosis with 4-methyl-2-oxo-2H-1-benzopyran-7-yl-5-thio--D-xylopyranoside.


Receive press releases from IQ4I Research & Consultancy Pvt. Ltd.: By Email This pipeline analysis gives comprehensive insights on drugs being developed for the treatment of NASH & their various stages of development in 144 slide decks. This pipeline focuses on novel pharmacologic drugs & regenerative medicines covering small molecules, antibodies, stem cell therapies, recombinant proteins and RNA-based therapeutics. Boston, MA, February 24, 2017 --( This report enables Pharmaceutical/Biotech companies, Academic institutes, Individual researchers, Investors, Medical technology companies, Service providers and other associated stake holders to identify and analyze the available licensing/collaborative commercial opportunities in the Non-alcoholic steatohepataitis (NASH) drugs market. The report also provides strategic insights on some of the molecules that are yet to be launched in the next few years. Some of the key sections covered in the report are given below: *Epidemiology -In this section, epidemiology of NASH is reviewed to understand potential significance and impact of the disease. -Global & US prevalence rates. *Hot Targets, Mechanisms & Therapies -In this section, various NASH associated targets, mechanism and upcoming therapies are discussed. Also, covers novel targets in early research for NASH along with disease progression biomarkers associated with NASH (Inflammatory, apoptosis, fibrosis). *Market analysis -In market analysis section, global NASH drugs market is indicated along with the estimated Peak sales ($) of leading clinical stage drugs forecasted from 2019-2025. -Forecasting model for NASH market. -NASH market dynamics -NASH Market and estimated Peak sales of 8 clinical candidates (OCA-Intercept, Aramchol-Galmed, -GR-MD-02-Gilead, Cenicriviroc-Tobira, Simtuzumab-Gilead, Remo Biphasic-Avolynt, IVA 337- Inventiva Pharma, GFT505-Genfit) -NASH related deals analysis with financials (upfront, milestones and royalties) -Funding scenario in NASH market *Pipeline Analysis -Pipeline analysis was carried to get deeper insights on various treatment modalities in discovery, preclinical & development section, pipelines from major companies were identified and Potential targets were reported along with Mechanism of action, Current development status & nature of molecule. Pipeline analysis by developmental stage (Discovery to Clinical development) -Pipeline analysis by modalities --Monoclonal Antibodies pipeline analysis --RNA-therapeutics pipeline analysis --Recombinant protein pipeline analysis -Pipeline analysis by leading players & Target analysis -Drug analysis based on mechanism (Anti-Inflammatory, Anti-fibrotic & Metabolic) *Key Players Analysis -The key player’s analysis section provides an in-depth understanding of various companies working on Nonalcoholic steatohepatitis (NASH) and their Pipelines with development phase as well as understanding partnering strategies such as deals entered by the company. -Global key players overview -Global key players Pipeline data (Discovery, Pre-clinical & Clinical development) -Global key players deals (Collaborations, Licensing, Service agreements, grants, funds) Boston, MA, February 24, 2017 --( PR.com )-- “Non-alcoholic steatohepataitis (NASH) Pipeline Analysis” gives comprehensive insights on the various drugs being developed for the treatment of NASH. The report covers all the drugs that are in various phases of development (Discovery, Preclinical & Clinical). The pipeline focuses on novel pharmacologic drugs & regenerative medicines covering small molecules, antibodies, stem cell therapies, recombinant proteins and RNA-based therapeutics, but excludes symptom relief drugs, generic combinations and supplemental drugs. The report also covers some of the hot targets in research for NASH treatments and NASH related biomarkers.This report enables Pharmaceutical/Biotech companies, Academic institutes, Individual researchers, Investors, Medical technology companies, Service providers and other associated stake holders to identify and analyze the available licensing/collaborative commercial opportunities in the Non-alcoholic steatohepataitis (NASH) drugs market. The report also provides strategic insights on some of the molecules that are yet to be launched in the next few years.Some of the key sections covered in the report are given below:*Epidemiology-In this section, epidemiology of NASH is reviewed to understand potential significance and impact of the disease.-Global & US prevalence rates.*Hot Targets, Mechanisms & Therapies-In this section, various NASH associated targets, mechanism and upcoming therapies are discussed. Also, covers novel targets in early research for NASH along with disease progression biomarkers associated with NASH (Inflammatory, apoptosis, fibrosis).*Market analysis-In market analysis section, global NASH drugs market is indicated along with the estimated Peak sales ($) of leading clinical stage drugs forecasted from 2019-2025.-Forecasting model for NASH market.-NASH market dynamics-NASH Market and estimated Peak sales of 8 clinical candidates (OCA-Intercept, Aramchol-Galmed,-GR-MD-02-Gilead, Cenicriviroc-Tobira, Simtuzumab-Gilead, Remo Biphasic-Avolynt, IVA 337- Inventiva Pharma, GFT505-Genfit)-NASH related deals analysis with financials (upfront, milestones and royalties)-Funding scenario in NASH market*Pipeline Analysis-Pipeline analysis was carried to get deeper insights on various treatment modalities in discovery, preclinical & development section, pipelines from major companies were identified and Potential targets were reported along with Mechanism of action, Current development status & nature of molecule. Pipeline analysis by developmental stage (Discovery to Clinical development)-Pipeline analysis by modalities--Monoclonal Antibodies pipeline analysis--RNA-therapeutics pipeline analysis--Recombinant protein pipeline analysis-Pipeline analysis by leading players & Target analysis-Drug analysis based on mechanism (Anti-Inflammatory, Anti-fibrotic & Metabolic)*Key Players Analysis-The key player’s analysis section provides an in-depth understanding of various companies working on Nonalcoholic steatohepatitis (NASH) and their Pipelines with development phase as well as understanding partnering strategies such as deals entered by the company.-Global key players overview-Global key players Pipeline data (Discovery, Pre-clinical & Clinical development)-Global key players deals (Collaborations, Licensing, Service agreements, grants, funds) Click here to view the list of recent Press Releases from IQ4I Research & Consultancy Pvt. Ltd.

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