University of Iowa Research Foundation

University of Nebraska

The United States of America, as Represented by the Secretary, Department of Health and Human Services

University of Connecticut

The United States of America

The United States of America, National Institute of Health

David Wiemer

Jeffrey D Neighbors

John A Beutler

Raymond J Hohl

Sarah Holstein

Andrew J Wiemer

Beverly L Davidson

Thomas Turbyville

John Kodet

Craig Kuder

Rocky J Barney

Karlyne Reilly

A Beutler John

Disclosed herein are inhibitors of the GGDPS enzyme, and methods for their use in treating or preventing diseases, such as multiple myeloma. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are described.

Triazole bisphosphonate geranylgeranyl diphosphate synthase inhibitors

The invention provides a compound of formula I: or a salt thereof, wherein R-Rhave any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful in immunotherapy as a potential treatment, or co-treatment, for cancer or infectious diseases.

Phosphonamidate butyrophilin ligands

Disclosed herein are inhibitors of the GGDPS enzyme, and methods for their use in treating or preventing diseases, such as multiple myeloma. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are described. 

The invention provides a drug conjugate comprising: 1) a therapeutic agent that comprises a phosphate, phosphonate, carboxy, or phosphoramidate group, and 2) a fluorescent group linked to the phosphate, phosphonate, carboxy, or phosphoramidate group to form the corresponding ester and salts thereof. The conjugates are useful for therapy and as probes. The invention also provides therapeutic methods for treating diseases with conjugates of the invention as well as methods for determining optimal dosages of a conjugate or a therapeutic agent for a given patient using a conjugate of the invention.

Fluorescent prodrugs

The invention provides novel pyrophosphate synthase inhibitors of formula I and formula II as well salts thereof; the invention also provides compositions comprising such inhibitors and methods for their use. 

Therapeutic bisphosphonates

The invention provides a compound of formula (I): wherein R-Rhave any of the values defined in the specification. The compounds are useful for the treatment of cancer and other diseases. 

Schweinfurthin analogues

Disclosed is a method for preventing or treating an undesirable condition in a subject carrying cells homozygous null for the neurofibromatosis type 1 gene or subjects that are haploinsufficient for the neurofibromatosis type 1 gene, the method comprising administering to a subject in need thereof an effective amount of a schweinfurthin or schweinfurthin analog or derivative, or a pharmaceutically acceptable salt, prodrug, hydrate, or solvate thereof. Also disclosed is a new schweinfurthin compound of the formula. 

Schweinfurthins and uses thereof

The invention provides fluorescent schweinfurthin analogs of formula (I) which are useful as probes and for the treatment of cancer and other diseases. 

Methods and intermediates for preparing enantiomerically enriched Schweinfurthin analogs which are useful for the treatment of cancer, as well as novel Schweinfurthin analogs having anti-cancer activity, compositions comprising such analogs and therapeutic methods comprising administering such analogs.

The invention provides novel pyrophosphate synthase inhibitors of formula I as well as compositions comprising such inhibitors and methods for their use.

Geranylgeranyl pyrophosphate synthase inhibitors

The present invention provides compounds useful for the detection of the enzyme tripeptidyl protease I (TPP-1). The invention also provides methods of making such compounds, methods of using such compounds, and kits and compositions containing such compounds. In one embodiment, Gly-L-Pro-L-Ser-1-anthraquinonylhydrazide, in combination with p-anisaldehyde, is used to detect TPP-1.

Growing community of inventors

Iowa City, IA, United States of America

David Wiemer