Richard Hartz Email & Phone Number

Princeton, New Jersey, United States

Cardiovascular Disease Programs• Led a medicinal chemistry team to rapidly complete lead optimization studies on a HTS hit for an early phase heart failure program to reach a go/no go decision.• Investigated multiple chemotypes with the aid of artificial intelligence (AI)/machine learning (ML) to identify compounds with suitable potency, kinase selectivity, and drug-like properties for a kinase inhibitor program (SGK1) for heart failure. This led to the discovery of compounds with… Show more Cardiovascular Disease Programs• Led a medicinal chemistry team to rapidly complete lead optimization studies on a HTS hit for an early phase heart failure program to reach a go/no go decision.• Investigated multiple chemotypes with the aid of artificial intelligence (AI)/machine learning (ML) to identify compounds with suitable potency, kinase selectivity, and drug-like properties for a kinase inhibitor program (SGK1) for heart failure. This led to the discovery of compounds with excellent cell potency. Show less

Dual αvβ6/αvβ1 Integrin Inhibitors for Fibrosis• Investigated the SAR of dual αvβ6/αvβ1 integrin inhibitors for potential use in the treatment of liver or lung fibrosis leading to compounds with desirable potency and in vitro properties. Lead compounds were advanced into rodent pharmacokinetic (PK) studies and exhibited low clearance and acceptable oral bioavailability.Galectin-3 Inhibitors for Fibrosis• Proposed and synthesized novel thiodisaccharide mimics as galectin-3… Show more Dual αvβ6/αvβ1 Integrin Inhibitors for Fibrosis• Investigated the SAR of dual αvβ6/αvβ1 integrin inhibitors for potential use in the treatment of liver or lung fibrosis leading to compounds with desirable potency and in vitro properties. Lead compounds were advanced into rodent pharmacokinetic (PK) studies and exhibited low clearance and acceptable oral bioavailability.Galectin-3 Inhibitors for Fibrosis• Proposed and synthesized novel thiodisaccharide mimics as galectin-3 inhibitors for potential use in the treatment of liver or lung fibrosis. A lead compound was evaluated in a mouse bile-duct ligation model for liver fibrosis.HIV-1 Maturation Inhibitors• Designed and synthesized betulinic acid derived HIV-1 maturation inhibitors for HIV/AIDS with excellent antiviral potency across wild-type and a panel of naturally occurring polymorphic and mutant viruses resulting in the discovery of a key compound that was evaluated as a potential clinical candidate.mGluR5 Positive Allosteric Modulators for Schizophrenia• Conducted lead optimization studies on a HTS hit to identify novel mGlu-R5 positive allosteric modulators with improved potency and in vitro properties.Glycogen Synthase Kinase-3 (GSK-3) Inhibitors for Alzheimer’s Disease• Designed and synthesized GSK-3 inhibitors from three chemotypes in collaboration with the CADD/X-ray crystallography group resulting in the discovery of highly potent imidazo[1,2-b]pyridazine and pyrimidine-based analogues. Lead compounds were orally active in a triple transgenic mouse Alzheimer’s disease model.Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for Neuropathic Pain• Initiated follow-up SAR optimization on HTS hits from three chemotypes for the AAK1 inhibitor program resulting in the discovery of a lead aryl-amide based proof-of-concept AAK1 inhibitor. These results contributed to the discovery of a first-in-class clinical compound (BMS-986176/LX9211) for neuropathic pain. Show less

Corticotropin Releasing Factor-1 (CRF1) Receptor Antagonists for Anxiety/Depression• Discovered two pyrazinone-based corticotropin releasing factor-1 (CRF1) receptor antagonist clinical candidates for the treatment of anxiety/depression by optimizing the potency and PK properties of compounds in this chemotype, including optimization to minimize the formation of reactive metabolites.• Designed and synthesized prodrugs of a lead CRF1 receptor antagonist leading to improved oral… Show more Corticotropin Releasing Factor-1 (CRF1) Receptor Antagonists for Anxiety/Depression• Discovered two pyrazinone-based corticotropin releasing factor-1 (CRF1) receptor antagonist clinical candidates for the treatment of anxiety/depression by optimizing the potency and PK properties of compounds in this chemotype, including optimization to minimize the formation of reactive metabolites.• Designed and synthesized prodrugs of a lead CRF1 receptor antagonist leading to improved oral bioavailability. Show less

• Corticotropin Releasing Factor-1 (CRF1) Receptor Antagonists for Anxiety/Depression

• Corticotropin Releasing Factor-1 (CRF1) Receptor Antagonists for Anxiety/Depression

Ann Arbor, Michigan

Advisor: Professor William R. RoushCompleted the first total synthesis of the antitumor antibiotic olivomycin A.

Doctor Of Philosophy (Ph.D.), Organic Chemistry

Advisor: Professor Amos B. Smith, III Natural product synthesis

Bachelor Of Science (B.S.), Chemistry