The Scripps Research Institute

William Marsh Rice University

Research, Incorporated

University of Pennsylvania

Bristol-myers Squibb Compnay

Emory University

Scripps Clinic and Research Foundation

Other

The United States of America As Represented by the Secretary of

Trustees of the University of Penna.

Kyriacos Costa Nicolaou

Dionisios Vourloumis

Ronald L Magolda

Yun He

Peter Emmanuel Maligres

Chan-Kou Hwang

Frank Roschangar

Hans Vallberg

Sacha Ninkovic

Debashis Mandal

Wilhelm Stahl

Erwin Paul Schreiner

Nicolas Winssinger

Nigel Paul King

Francisco Sarabia

Sanjeev Gangwar

Yam B Poudel

Naidu S Chowdari

Adrian Leonard Smith

William E Barnette

Zhen Yang

M Ray Finlay

Wei-Min Dai

Toshio Suzuki

David A Claremon

Nicos A Petasis

Min Lu

Joaquin Pastor

Yuji Ogawa

Maurice Raymond Verschoyle Finlay

Antony Bigot

Erik J Sorensen

Andreas Ritzen

Robert G Bergman

Melpo Christofidou-Solomidou

Rodney K Guy

Erwin Van Meir

Tianhu Li

Emmanuel Pitsinos

Wolfgang A Wrasidlo

Nicholas Simmons

Kiran Kumar Pulukuri

N Paul King

Stephan Rigol

Roman A Valiulin

Philipp M Heretsch

Guido Zuccharello

Robert Discordia

Sebastian V Wendeborn

Steven P Seitz

Anthony Roecker

Kenji Namoto

Robert E Minto

Rohan Diliprao Erande

Derek Rhoades

Xianhai Huang

Ralph F Hirschmann

Karl-Heinz Altmann

Paul A Sprengeler

Yoshihiro Abe

Catherine D Strader

Guo-Qiang Cao

Hiroaki Ueno

Philippe G Nantermet

Trond Ulven

Jeffrey R Aldrich

Wolfgang Wrasidlo

James E Oliver

Golfo Skokotas

Mitsuru Shoji

Soundarapandian M Kumar

Manas R Pattanayak

Yanping Wang

Christopher R H Hale

Manjunath Lamani

Christian Nilewski

Maruice Raymond Verschoyle Finlay

Sotirios Totokotsopoulos

Heraklidia Ioannidou

Abdellatif El Marrouni

David Hepworth

Thomas J Caulfield

Brian E Marron

Aijun Liu

Adrian L Smith

Benjamin Pratt

Jun Yin

Stellios Arseniyadis

Sebastian V Wenderborn

T R Reisine

Robert D Groneberg

Sherrie Pietranico

Joseph M Salvino

Phillipp Klahn

Chalet Tan

David A Clark

Ruofan Li

Quan Cai

Zhaoyong Lu

Jeffrey Pfefferkorn

In one aspect, the present disclosure provides analogs of thailanstatin of the formula wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. 

Derivatives of thailanstatin A, methods of treatment and methods of synthesis thereof

In one aspect, the present disclosure provides disorazole analogs of the formula: Formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided. 

Synthesis of disorazoles and analogs thereof as potent anticancer agents

In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided. 

Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith

In one aspect, the present invention provides novel derivatives of trioxacarin analogs of the formula (I) wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof. 

Total synthesis of trioxacarcin DC-45-A2 and preparation of trioxacarcin analogs

In one aspect, the present disclosure provides new analogs of uncialamycin. The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates which may be used to treat cancer or another disease or disorder.

Derivatives of uncialamycin, methods of synthesis and their use as antitumor agents

In one aspect, the present disclosure provides epothilone analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided. 

Epothilone analogs, methods of synthesis, methods of treatment, and drug conjugates thereof

The invention relates to processes for preparing (S,S)-secoisolariciresinol diglucoside and (R,R)-secoisolariciresinol diglucoside and compositions comprising the same.

Preparation of (S,S)-secoisolariciresinol diglucoside and (R,R)-secoisolariciresinol diglucoside

In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein R, R, R, R, X, X, X, and Aare as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. 

Desacetoxytubulysin H and analogs thereof

In one aspect, the present disclosure provides shishijimicin analogs of the formula: wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, antibody drug conjugates of the compounds are also provided.

Total synthesis of shishijimicin A and analogs thereof

In one aspect, the present invention provides novel derivatives of viridicatumtoxin of the formula wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof. 

Preparation and biological evaluation of viridicatumtoxin analogs

In one aspect, the present disclosure provides new analogs of uncialamycin of formulae (I) and (II). The present disclosure also provides novel synthetic pathways to obtaining uncialamycin and analogs thereof. Additionally, the present disclosure also describes methods of use of uncialamycin and analogs thereof. In another aspect, the present disclosure provides antibody-drug conjugates comprising the compounds of formulae (I) and (II). 

HIF-1 inhibitors and methods of use thereof are provided.

HIF inhibitors

A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.

Chemical synthesis of a highly potent epothilone

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La Jolla, CA, United States of America

Kyriacos Costa Nicolaou