Purdue Research Foundation

University of Rochester

Research Corporation Technologies, Inc.

University of Minnesota

Terrapin Technologies, Inc.

Indiana University

University of New York

Richard F Borch

Therese K Schmalbach

Lawrence M Kauvar

Matthew H Lyttle

Amy S Morgan

Ronald R Valente

Stanley L Hem

Harm Hogenesch

James P Schmidt

Gregory W Canute

Marcy Hernick

Carolee Flader

Hugo Garrido-Hernandez

Irene A George

Sandra C Tobias

Mark R Kelley

Richard Anthony Gibbs

Michelle Martin Clark

Kristin M Fries

Farid Fouad

Rodney L Nyland, Ii

Rodney L Ii Nyland

The invention described herein pertains to compounds and conjugates, to compositions, complexes and formulations comprising the compounds and/or conjugates, and to methods of use of the compounds, conjugates and their compositions, complexes and formulations in vaccines and vaccinations and generating immune responses.

Immunogenic compositions and reagents for preparing

This application describes quinone derivatives which target the redox site of Ape1/Ref1. Also included in the invention are pharmaceutical formulations containing the derivatives and therapeutic uses of the derivatives.

Quinone derivatives, pharmaceutical compositions, and uses thereof

Described herein are neutral prodrugs of phosphorus-containing inhibitors of farnesyl transferase that include one or more phosphate fragments or analogs of phosphate fragments. Analogs of phosphate fragments include various linkers other than oxygen connecting the phosphate fragment to the remaining portion of the drug, such as but not limited to linkers forming phosphoramidates, phosphonates, difluorophosphonates, phosphordiamidates, and the like.

Prodrugs and conjugates of prenylation inhibitors

The invention provides a compound of formula I: wherein R, R, R, R, and Rhave any of the values defined in the specification, as well as pharmaceutical compositions comprising such compounds or salts. The compounds are useful for treating cancer in animals.

Phosphoramide compounds

Novel phosphoramidate derivatives of hydroxy functional or amino functional compounds, including amino acids, peptides, peptidomimetics and nucleotide analogs, are described. The compounds enable enhanced intracellular delivery of drugs as their corresponding phosphate esters or amides. Described phosphoramidate compounds exhibit antiproliferative activity. Pharmaceutical formulations are provided for treatment of cancers.

Phosphoramidates and methods therefor

Compounds of the formula ##STR1## and the esters, amides, amide/esters and salts thereof, wherein YCO is .gamma.-glu or .beta.-asp;

Metabolic effects of certain glutathione analogs

A method to potentiate the effect of a chemotherapeutic agent in a tumor cell, which method comprises administering to said tumor cell, along with said chemotherapeutic agent, a potentiating amount of a compound of the formula: ##STR1## or an amide, ester or hybrid amide/ester thereof, wherein X is a hydrocarbon radical optionally substituted on any aromatic moiety contained therein; Y--CO is .gamma.-Glu or .beta.-Asp and AA.sub.C is an amino acid, preferably glycine, phenylglycine, .beta.-alanine, alanine or phenylalanine is disclosed. Similar compounds can also be used to selectively exert cytotoxicity versus target cells as compared to nontarget cells and also to elevate the production of GM progenitors in bone marrow of mammalian subjects.

Target-selective protocols based on mimics

Bone marrow stimulation by certain glutathione analogs

Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are each (C.sub.2 -C.sub.6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are H and Ar is a heteroaromatic ring and the pharmaceutically acceptable salts thereof.

Phosphoramidates useful as antitumor agents

Compounds of the formula: ##STR1## which is further defined herein, possess anti-tumor activity.

A process for preventing or ameliorating the myelosuppression which can occur in a mammal such as a human cancer patient being treated with a platinum-free antineoplastic drug is provided, comprising administering an effective dosage of a dithiocarbamate compound to said mammal, preferably subsequent to administration of the cytotoxic drug.

Growing community of inventors

Pittsford, NY, United States of America

Richard F Borch