Publication number: 20150353503
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.
Type:
Application
Filed:
September 24, 2013
Publication date:
December 10, 2015
Applicants:
WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH, THE BROAD INSTITUTE, INC., MASSACHUSETTS INSTITUTE OF TECHNOLOGY
Inventors:
Benjamin VINCENT, Luke WHITESELL, Susan L. LINQUIST, Willmen YOUNGSAYE, Stephen L. BUCHWALD, Jean-Baptiste LANGLOIS, Partha P. NAG, Amal TING, Barbara J. MORGAN, Benito MUNOZ, Sivaraman DANDAPANI, Bruce TIDOR, Raja R. SRINIVAS
Publication number: 20150284371
Abstract: This application describes compounds and methods that can inhibit Scavenger receptor class B, type I (SR-BI) activity, which compounds and methods can be used, for example, to mediate high-density lipoprotein (HDL) lipid uptake and treat hepatitis C viral infections. The compounds have the formula: wherein R1 and R2 are independently H, halogen, cyano, haloalkyl, haloalkyloxy or OMe; or R1 and R2 together are —O—CH2— or -0- CF2—O—; R3 is H, halogen, cyano, haloalkyl or haloalkyloxy; R4 is C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkylmethyl or C3-6cycloheteroalkyl, wherein the heteroatom is N or 0; R5 is H or CH3; R6 is C1-6alkyl or C3-6cycloalkyl; and A, B, D and E are each, independently, CH, N, 0 or S, wherein at least one of A, B, D and E is N, and another of A, B, D and E is N, 0 or S.
Type:
Application
Filed:
October 21, 2013
Publication date:
October 8, 2015
Inventors:
Chris Dockendorff, Andrew Germain, Partha Pratim Nag, Willmen Youngsaye, Sivaraman Dandapani, Benito Munoz, Patrick Falloon, Thomas Nieland, Monty Krieger, Miao Yu
Publication number: 20150259298
Abstract: The present invention provides novel compounds (e.g., compounds of Formula (I)), and pharmaceutically acceptable salts, solvates, hydrate, 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 protozoan, or inhibiting the growth of a fungus or protozoan. The fungus may be a Candida species, Sacchawmyces species, or other pathogenic fungal species. The compounds of the invention may inhibit the activity of fungal or protozoan mitochondrial phosphate carrier protein.
Type:
Application
Filed:
October 16, 2013
Publication date:
September 17, 2015
Applicants:
Whitehead Institute for biomedical Research, Massachusetts Institute of Technology, The Broad Institute, Inc.
Inventors:
Benjamin Vincent, Luke Whitesell, Susan L. Lindquist, Willmen Youngsaye, Stephen L. Buchwald, Jean-Baptiste Langlois, Jun Pu, Benito Munoz, Sivaraman Dandapani