Robert Kavash Email & Phone Number

Bethlehem, Pennsylvania, Us

Drug Discovery through Medicinal and Synthetic Organic Chemistry.

Doylestown, Pennsylvania, Us

Drug Discovery through Medicinal and Synthetic Organic Chemstry.Designed and synthesized novel molecular entities for a variety of therapeutic targets.• Jointly led a project that identified orally active small molecule non-peptidic mimics of host defense peptides (HDP’s) for the treatment of malaria.• Led a project with the goal of introducing drug-like properties into an existing series of inhibitors of both M2 wild type and M2-S31N mutant influenza A strains as a strategy towards a new therapeutic agent. Identified a compound with improved safety and pharmacokinetic properties.

Us

Designed, synthesized, and performed CMC product development of novel fully synthetic small molecule non-peptidic mimics of host defense peptides (HDP’s) and other therapeutically relevant small polypeptides.• Analyzed antimalarial screening data to identify potent HDP leads with favorable safety profiles. Championed compound that was subsequently determined to possess in vivo efficacy via a novel mechanism of action. Jointly led the follow-on lead optimization program and designed and synthesized key analogs.• Consulted with process development CMO on GMP synthesis of PMX-30063 (brilacidin), an antibacterial compound that entered Phase II clinical trials.• Jointly led a backup program for heparin reversal agents that resulted in the discovery of compounds with an improved safety profile while broadening the activity profile to also reverse the effect of low molecular weight heparins. Designed and prepared key compounds.• Led and conducted exploratory process development research on heparin reversal compound PMX-60056 (delparantag), which entered Phase I clinical trials. Provided technology transfer to process development CRO and consulted on GMP synthesis.

New Brunswick, Nj, Us

Designed and synthesized novel molecular entities for the treatment of gastrointestinal disorders. • Co-designed and executed backup strategy for delta/mu-opioid receptor modulation project. Identified a compound with significant improvement in properties that met the requirements for selection as a backup candidate for early development.• Discovered a series of novel peripheral dual delta/mu-opioid receptor modulators as therapeutic agents for gastrointestinal disorders. As a co-inventor, solved conceptually and synthetically the problems of cardiovascular (CV) and P-450 inhibition liabilities, which enabled compound JNJ-27018966 to successfully transition into pre-clinical development. The compound, eluxadoline (MuDelta), was approved for marketing as Viberzi® in 2015 for the treatment of diarrhea-predominant Irritable Bowel Syndrome (IBS-D). • Led from conception through design and synthetic execution a small molecule tryptase inhibitor project as a strategy for IBD therapy. Identified lead compound for scale up and further evaluation.

A Johnson and Johnson CompanyDevised and produced novel molecular entities for the treatment of a variety of therapeutic targets.• Co-inventor of TMC-125, a new generation non-nucleoside reverse transcriptase inhibitor currently marketed as Intelence® (etravirine) for the treatment of HIV. Designed and prepared key analogs. Received Janssen Research Foundation Pinnacle Award for this work.• Designed and synthesized key compounds for an anti-obesity project with a strategy of inhibition of the tripeptidyl-peptidase II (TPP II) enzyme. • Designed and synthesized key compounds for an anti–HIV project based on the mechanistic approach of non-nucleoside reverse transcriptase inhibitors. Increased potency from micromolar to nanomolar level against both wild type and mutant strains.

Fort Collins, Co, Us

Professor Anthony Barrett Research Group

Evanston, Il, Us

Professor Anthony Barrett Research Group

Ph. D., Organic Chemistry

M.S., Organic Chemistry

B.S., Chemistry