Massachusetts Institute of Technology

Collegium Pharmaceutical, Inc.

Whitehead Institute for Biomedical Research

The Broad Institute, Inc.

Stephen L Buchwald

John P Wolfe

Michael Palucki

Ken Kamikawa

Artis Klapars

Fuk Y Kwong

David W Old

Timothy Manning Swager

Roman V Rariy

Gabriel E Job

Jon Clarence Antilla

Gero Nordmann

Edward J Hennessy

Susan Lindquist

Peter H Seeberger

Obadiah J Plante

Kevin W Anderson

Martina Wolter

Benito Munoz

Jane C Hirsh

Valdas Jurkauskas

Alison B Fleming

Jacopo Zanon

Sivaraman Dandapani

Benjamin Vincent

Jean-Baptiste Langlois

Willmen Youngsaye

Luke Whitesell

Jean-Francois Marcoux

Robert A Singer

Joseph P Sadighi

Whe Yong Lo

Alberto Gutierrez

Robert B Grossman

Kristina A Kreutzer

Richard D Broene

Nancy E Lee

Nicholas C Bruno

Eric R Streiter

Ryo Shintani

Yasunori Moritani

Daniel H Appella

Sven Doye

Seble Wagaw

Alexander M Klibanov

Bradley Lether Pentelute

Georgiy Teverovskiy

Thomas Mackewitz

T Alan Hatton

Partha Pratim Nag

Danilo Zim

Xiaohua Huang

Daniel Tardiff

Joseph M Fox

Jun Pu

Michael Heffernan

Raja Srinivas

Amal Ting

Linda Katherine Molnar

Bruce Tidor

Esther Spaltenstein

Chi Zhang

Jens Bertil Ahman

Martina Uhlenbrock

Jens Ahman

Oliver Fabian Geis

Udo E Lange

Xavier Verdaguer

Scott C Berk

Christopher A Willoughby

Anil Guram

Brett P Fors

Daniel T Cohen

David S Surry

Alexander M Kibanov

Wenliang Huang

Nathan Jui

Malisa Troutman

Andre Chieffi

Barbara J Morgan

Mingjuan Su

O Geis

Edward Hennessy

Disclosed are chemical transformations for the conjugation of unprotected peptide biomolecules. The disclosed chemical transformations relate to methods of selective cysteine and selenocysteine functionalization of unprotected peptide and protein molecules. The processes feature several significant advantages over existing methods of peptide modification, including specificity towards selenocysteine over other nucleophiles (e.g., amines, hydroxyls), excellent functional group tolerance, and mild reaction conditions. Also disclosed are syntheses of arylated cysteine and arylated selenocysteine peptide compounds.

Selective arylation of dichalcogenides in biomolecules

Disclosed are [2.2]paracyclophane-derivative compounds and related polymers that are useful as stable, efficient, blue-light emitting compounds for OLED applications.

[2.2]paracyclophane-derived donor/acceptor-type molecules for OLED applications

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 aspecies,species, or other pathogenic fungal species. The compounds of the invention may inhibit the activity of fungal or protozoan mitochondrial phosphate carrier protein.

Thiohydantoin derivatives and uses thereof

The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and pharmaceutical compositions thereof. The present invention also provides methods and kits using the inventive compounds and pharmaceutical compositions for treating and/or preventing diseases associated with protein aggregation, such as amyloidoses (e.g., Parkinson's disease and Alzheimer's disease), treating and/or preventing neurodegenerative diseases, treating and/or preventing diseases associated with Tar DNA binding protein 43 kDa, reducing or preventing protein aggregation, and/or modulating E3 ubiquitin ligase in a subject in need thereof. 

Benzimidazole derivatives and uses thereof

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 aspecies,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. 

Indazole derivatives and uses thereof

Embodiments described herein relate to compositions including iptycene-based structures and extended iptycene structures. In some embodiments, the compositions may be useful in organic light-emitting diodes (OLEDs), organic photovoltaics, and other devices.

Organic conductive materials and devices

The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods, such as the reaction of Z-X with C(L)(R)(R')in the present of a catalyst and a base, thereby forming C(Z)(R)(R&#x2032;); wherein X represents I, Cl, alkylsulfonate, or arylsulfonate; Z represents optionally substituted aryl, heteroaryl or alkenyl; L represents H or a negative charge; catalyst comprises a copper atom or ion, and a ligand, wherein the ligand is an optionally substituted aryl alcohol, alkyl amine, 1,2-diamine, 1,2-aminoalcohol, 1,2-diol, imidazolium carbene, pyridine, or 1,10-phenanthroline; the ligand is a chelating ligand; and the base represents a Bronsted base; R represents H, optionally substituted alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl; R&#x2032; represents independently for each occurrence H, alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl, formyl, acyl, &#x2014;COR&#x2033;, &#x2014;C(O)N(R), sulfonyl, &#x2014;P(O)(OR&#x2033;), &#x2014;CN, or &#x2014;NO; R&#x2033; represents independently for each occurrence optionally substituted alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl; and C(R&#x2032;)(R) taken together may represent nitrile.

Copper-catalyzed formation of carbon-heteroatom and carbon&#x2014;carbon bonds

An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.

Abuse-deterrent pharmaceutical compositions of opiods and other drugs

Described are palladium precatalysts, and methods of making and using them. The palladium precatalysts show improved stability and improved reactivity in comparison to previously-described palladium precatalysts.

Phosphine-ligated palladium sulfonate palladacycles

One aspect of the present invention relates to ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition metal-catalyzed: aryl amination reactions; aryl amidation reactions; Suzuki couplings; and Sonogashira couplings. In certain embodiments, the invention relates to catalysts and methods of using them that operate in aqueous solvent systems.

Transition-metal-catalyzed carbon-nitrogen and carbon-carbon bond-forming reactions

Ligands for transition metals are disclosed herein, which may be used in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The disclosed methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition-metal-catalyzed cross-coupling reactions.

Ligands for transition-metal-catalyzed cross-couplings, and methods of use thereof

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

Ligands for metals and improved metal-catalyzed processes based thereon

Growing community of inventors

Newton, MA, United States of America

Stephen L Buchwald