Patent
Indazole derivatives and uses thereof
Benjamin Vincent,Luke Whitesell,Susan Lindquist,Willmen Youngsaye,Stephen L. Buchwald,Jean-Baptiste Langlois,Partha Pratim Nag,Amal Ting,Barbara Morgan,Benito Munoz,Sivaraman Dandapani,Bruce Tidor,Raja Srinivas +12 more
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TLDR
In this article, the authors proposed a method for treating and/or preventing a fungal or protozoan infection, inhibiting the activity of an enzyme, killing a fungus, or stopping the growth of a fungus or a protozoon.Abstract:
The present invention provides novel compounds (e.g., compounds of Formula (I)), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits comprising the inventive compounds, or compositions thereof, for treating and/or preventing a fungal or protozoan infection, inhibiting the activity of a fungal or protozoan enzyme, killing a fungus or protozoon, or inhibiting the growth of a fungus or protozoon. The fungus may be a Candida species, Aspergillus species, or other pathogenic fungal species. The compounds of the invention may inhibit the activity of fungal or protozoan cytochrome b and/or fungal or protozoan Hsp90. The present invention also provides synthetic methods of the inventive compounds.read more
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Patent
Heterocyclic inhibitors of PTPN11
TL;DR: In this paper, new compounds and compounds based on pyrazolopyrazines and their application as pharmaceuticals for the treatment of disease are presented. But none of them are suitable as inhibitors of PTPN11.
Patent
Substituted benzylindazoles for use as bub1 kinase inhibitors in the treatment of hyperproliferative diseases
Hitchcock Marion,Anne Mengel,Pütter Vera,Gerhard Siemeister,Antje Margret Wengner,Briem Hans,Eis Knut,Volker Schulze,Amaury Ernesto Fernandez-Montalvan,Prechtl Stefan,Holton Simon,Fanghänel Jörg,Lienau Philip,Cornelia Preusse,Mark Jean Gnoth +14 more
TL;DR: In this paper, the authors describe compounds of formula (I) which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals, which are used as drugs.
Patent
Benzyl substituted indazoles as bub1 inhibitors
Anne Mengel,Hans-Georg Lerchen,Manfred Möwes,Thomas Müller,Lars Bärfacker,Marion Hitchcock,Arwed Cleve,Joachim Kuhnke,Briem Hans,Gerhard Siemeister,Bone Wilhelm,Amaury Ernesto Fernandez-Montalvan,Jens Schröder,Mönning Ursula,Holton Simon +14 more
Patent
Novel 3-(isoxazol-3-yl)-pyrazolo[3,4-d]pyrimidin-4-amine compound, which is ret kinase inhibitor
TL;DR: In this paper, a novel 3-(isoxazol-3-yl)-pyrazolo[3,4-d]pyrimidin-4-amine compound, a preparation method for the compound, and a pharmaceutical use of the compound to be used in the prevention and treatment of various cancer diseases caused by the activity of RET kinases.
Patent
Heterocyclic compounds as ret kinase inhibitors
Allan M. Jordan,Rebecca Newton,Bohdan Waszkowycz,Jonathan Mark Sutton,George Hynd,Silvia Paoletta,Euan Alexander Fraser Fordyce +6 more
TL;DR: In this article, the authors describe compounds of Formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, bonds a, b, c and d, X 1, X 2, X 3, X 4, R 2, and R 3 are each as defined herein.
References
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Journal ArticleDOI
Epidemiology of Invasive Candidiasis: a Persistent Public Health Problem
TL;DR: Improved non-culture-based diagnostics are needed to expand the potential for preemptive (or early directed) therapy and improve diagnostic, preventive, and therapeutic strategies is necessary to reduce the considerable morbidity and mortality associated with IC.
Journal ArticleDOI
The changing epidemiology of resistance.
TL;DR: Some of the new mechanisms and recent trends in the global spread of multidrug resistant (MDR) bacteria are reviewed, with the emergence of community-associated methicillin-resistant Staphylococcus aureus blurring the distinction between hospital and community strains.
Journal ArticleDOI
Resistance of Candida species to antifungal agents: molecular mechanisms and clinical consequences
Dominique Sanglard,Frank C. Odds +1 more
TL;DR: Recent large-scale surveys of yeasts isolated from blood cultures, based on standardised methodology and resistance definitions, do not support the view that antifungal resistance in pathogenic yeasts constitutes a significant or growing therapeutic problem.
Journal ArticleDOI
A New Palladium Precatalyst Allows for the Fast Suzuki-Miyaura Coupling Reactions of Unstable Polyfluorophenyl and 2-Heteroaryl Boronic Acids
TL;DR: In this article, a precatalyst was developed for Suzuki−Miyaura reactions of a wide range of (hetero)aryl chlorides, bromides, and triflates with polyfluorophenyl, 2-furan and 2-thiophene, and their analogues.
Journal ArticleDOI
Resistance of Candida albicans to Fluconazole During Treatment of Oropharyngeal Candidiasis in a Patient with AIDS: Documentation by In Vitro Susceptibility Testing and DNA Subtype Analysis
Spencer W. Redding,J. Smith,J. Smith,G. Farinacci,G. Farinacci,M. Rinaldi,M. Rinaldi,Annette W. Fothergill,J. Rhine-Chalberg,J. Rhine-Chalberg,M. A. Pfaller,M. A. Pfaller +11 more
TL;DR: In vitro susceptibility testing of isolates obtained during these successive episodes of infection revealed the development of resistance to fluconazole, and molecular epidemiologic techniques confirmed the persistence of the same Candida albicans strain throughout all 12 episodes.