Massachusetts Institute of Technology

University of Illinois

Tufts University

Mohammad Movassaghi

Paul Joseph Hergenrother

Nicolas Cedric Boyer

Karen C Morrison

Justin Kim

Joshua Payette

Tony Z Scott

Jaime Cheah

Chase Robert Olsson

Bradley Lether Pentelute

Stephen Paul Lathrop

Alyssa H Antropow

Carly Schissel

Rachel J Buchsbaum

Wen-Tau Timothy Chang

Kun Xu

Matthew W Pompeo

Petra Lindovska

Kyan Anthony D'Angelo

The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.

Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof

The present disclosure provides compounds of Formula I, methods of preparing the compounds, compositions, kits, and methods of using the compounds for treating or preventing microbial infections.

Himastatin derivatives, and processes of preparation thereof, and uses thereof

The present disclosure relates to derivatized agelastatin compounds and methods for the treatment, prevention, or delay of cancer, comprising administering a therapeutically effect amount of the derivatized agelastatin compounds, a pharmaceutically acceptable salt thereof, or a composition thereof to a subject in need thereof. Methods for making the derivatized agelastatin compounds are also provided.

Potent agelastatin derivatives as modulators for cancer invasion and metastasis

A highly convergent biomimetic synthesis of a complex polycyclic scaffold has been successfully implemented. From these efforts, compounds having a structure of Formula (I): or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R-Rand m, n, r, s, t, and u are as defined herein, is provided. Methods of making such compounds are also disclosed as are methods for the treatment of cancer, various infectious diseases, and abnormal cardiovascular function.

Convergent and enantioselective total synthesis of Communesin analogs

The synthesis of various pyrazino[1',2&#x2032;:1,5]pyrrolo[2,3-B]-indole-1,4-dione analogs has been successfully implemented in the present application. From these efforts, compounds having the structure of Formula I-a or Formula I-b: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, are provided herein. These biologically active derivatives have been used to effectively treat various diseases including cancer.

Substituted pyrazino[1',2&#x2032;:1,5]pyrrolo[2,3-b]indole-1,4-diones for cancer treatment

Diazene-directed modular synthesis is described for the preparation Csp2-Csp3 and Csp3-Csp3 linkages where one or more stereogenic quaternary carbon centers are formed. The disclosed methods are directed to the preparation of compounds of Formula (I), or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, from compounds of Formula (II): wherein R-Rand q are as defined independently for each occurrence herein. A wide variety of compounds can be accessed in this manner, including oligocyclotryptamines, where the stereochemistry of each subunit is beneficially secured before fragment coupling.

Diazene directed modular synthesis of compounds with quaternary carbon centers

The synthesis of various pyrazino[1',2&#x2032;:1,5]pyrrolo[2,3-b]-indole-1,4-dione analogs has been successfully implemented in the present application. From these efforts, compounds having the structure of Formula I-c: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein R, R, R-R, R, R, and n are as defined herein, are provided. These biologically active derivatives have been further used to prepare cell-specific drug conjugates effective in treating various diseases including cancer.

Substituted pyrazino[1',2&#x2032;:1 ,5]pyrrolo[2,3-b]indole-1,4-diones for cancer treatment

The present invention, among other things, provides compounds, compositions and methods for treatment of cancer. In some embodiments, the present invention provides methods for treating blood cancer using agelastatin alkaloids.

Compounds, compositions and methods of agelastatin alkaloids

The present application provides, among other things, a compound of Formula I-a and/or I-b, or a pharmaceutically acceptable salt thereof, wherein the variables are defined in the specification. The compounds of the invention are useful for treating various diseases including cancer.

Growing community of inventors

Arlington, MA, United States of America

Mohammad Movassaghi