Gilead Sciences, Inc.

Isis Pharmaceuticals, Inc.

Threshold Pharmaceuticals, Inc.

Genentech, Inc.

Obi Pharma Inc.

Molecular Templates, Inc.

Carlsbad

Immunogenesis, Inc.

Mark D Matteucci

Jian-Xin Duan

Kuei-Ying Lin

Robert J Jones

Brian C Froehler

Hailong Jiao

Jeff Pudlo

Arnold J Gutierrez

Yeyu Cao

Xiaohong Cai

Jing Yuan Ma

Chris A Buhr

Sundaramoorthi Swaminathan

Rick Wagner

Photon Rao

Norbert W Bischofberger

George Tidmarsh

Nipun Davar

John D Munger

Denise Andersen

Richard W Wagner

Jason G Lewis

Jacob Kaizerman

Tao Chen

Jason Gustaf Lewis

Robert Anthony Mook

Ronald A Hitzeman

Randolph B DePrince

Xiaodong Cao

Charles Praray Hart

Stewart Kroll

Jiancun Zhang

Chung N Chang

Steve Ammons

Bob Jones

Donald Jung

George S Lewis

Kevin L Facchine

John G Curd

Jessica D Sun

Charles P Hart

Provided herein are compounds of formula I: wherein the variables are defined herein, processes of making them, and methods of treating cancer comprising administering such compounds.

Nitrobenzyl derivatives of anti-cancer agents

Provided herein are compounds of formula I, wherein the variables are defined herein, processes of making them, and methods of treating cancer comprising administering such compounds. 

DNA alkylating agents

Provided herein are compounds of formula (I)-(VI): wherein the variables are defined herein, processes of making them, and methods of treating cancer comprising administering such compounds.

Aziridine containing DNA alkylating agents

The present invention provides a new method for making TH-302 and solid forms thereof. The compound in its solid form is an effective anti-cancer agent and may be used in various pharmaceutical compositions, and are particularly effective for the treatment of cancer. The invention also provides a method for preparing such compounds and forms and for treating cancer in a mammal comprising the step of administering a therapeutically effective amount of a solid form of TH-302 thereof.

TH-302 solid forms and methods related thereto

Provided herein are optically active compounds of the formulae (ii); and (III) and pharmaceutical compositions thereof. Also provided herein are processes of making these compounds and resolving the racemic mixture or the enrichment of same with in one of its enantiomers to provide (R)- and (S)-1-(3-(3-N,N-dimethylaminocarbonyl)phenoxyl-4-nitrophenyl)-1-ethyl-N,N'-bis(ethylene)phosphoramidate, and methods of treating cancer comprising administering such compounds. 

(R)- and (S)-1-(3-(3-N,N-dimethylaminocarbonyl)phenoxyl-4-nitrophenyl)-1-ethyl-N,N'-bis (ethylene)phosphoramidate, compositions and methods for their use and preparation

Provided herein are compounds of formula I: wherein the variables are defined herein, processes of making them, and methods of treating cancer comprising administering such compounds. 

Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Phosphoramidate alkylator prodrugs

Cancer can be treated by administration of a hypoxia-activated prodrug, such as TH-302, alone or in combination with other anticancer agents and/or radiation therapy. In combination therapy, the hypoxia-activated prodrug and another anti-cancer agent or radiation therapy may be administered within the same 24-hour period, and administration of the hypoxia-activated prodrug may be completed prior to beginning administration of the other anticancer agent or radiation therapy.

Treatment of cancer using hypoxia activated prodrugs

The present invention provides 2-aminopyridine and 2-pyridone C-nucleosides and oligonucleotides containing the subject nucleosides. The nucleosides are useful in the preparation of the subject oligonucleotides. The oligonucleotides are useful in oligonucleotide-based diagnosis and separation through triplex binding.

2-aminopyridine and 2-pyridone C-nucleosides

Various 14-nitro, 14-amino, and 14-substituted amino camptothecin derivatives are useful in the treatment of cancer and other hyperproliferative diseases. 14-Nitro camptothecin derivatives are conveniently prepared by reacting a camptothecin derivative with fuming nitric acid, optionally employing acetic anhydride as a solvent.

Camptothecin derivatives

Compositions containing, and, methods administering, TH302, are useful in treatment of cancer and other hyper-proliferative diseases.

Phosphoramidate alkylator prodrugs for the treatment of cancer

Growing community of inventors

Burlingame, CA, United States of America

Mark D Matteucci