S. Diamond

发表

The Janus Kinase 2 Inhibitor Fedratinib Inhibits Thiamine Uptake: A Putative Mechanism for the Onset of Wernicke’s Encephalopathy

R. Wynn, Phillip C. C. Liu, T. Burn, 2014, Drug Metabolism and Disposition.

A Novel Kinase Inhibitor, INCB28060, Blocks c-MET–Dependent Signaling, Neoplastic Activities, and Cross-Talk with EGFR and HER-3

Qian Wang, Yu Li, Richard Wynn, 2011, Clinical Cancer Research.

Species-Specific Metabolism of SGX523 by Aldehyde Oxidase and the Toxicological Implications

T. Maduskuie, S. Diamond, J. Boer, 2010, Drug Metabolism and Disposition.

Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy

H. Koblish, M. Stubbs, Q. Wang, 2020, The Journal of Pharmacology and Experimental Therapeutics.

Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies

R. Wynn, A. Margulis, H. Koblish, 2018, PloS one.

Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.

P. Scherle, K. Vaddi, M. Covington, 2011, ACS medicinal chemistry letters.

Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.

R. Wynn, P. Scherle, K. Vaddi, 2022, Bioorganic & medicinal chemistry letters.

Parsaclisib Is a Next-Generation PI3Kδ Inhibitor With Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy a

Kathy, Qianqian Wang, H. Koblish, 2020 .

Mass spectrometric and NMR characterization of metabolites of roxifiban, a potent and selective antagonist of the platelet glycoprotein IIb/IIIa receptor

A. Mutlib, J. Shockcor, S. Diamond, 2000, Xenobiotica; the fate of foreign compounds in biological systems.

Preclinical characterization of itacitinib (INCB039110), a novel selective inhibitor of JAK1, for the treatment of inflammatory diseases.

Jun Yu Li, M. Favata, P. Scherle, 2020, European journal of pharmacology.

Discovery of 5,7-Dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-ones as Highly Selective CDK2 Inhibitors.

Yvonne Lo, M. Covington, S. Diamond, 2022, ACS medicinal chemistry letters.

INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).

H. Koblish, P. Scherle, T. Maduskuie, 2019, ACS medicinal chemistry letters.

Metabolism, Excretion, and Pharmacokinetics of [14C]INCB018424, a Selective Janus Tyrosine Kinase 1/2 Inhibitor, in Humans

S. Shepard, J. Rodgers, T. Emm, 2010, Drug Metabolism and Disposition.

Plasma pharmacokinetics and distribution of ruxolitinib into skin following oral and topical administration in minipigs.

S. Diamond, Jennifer J. Harris, S. Yeleswaram, 2020, International journal of pharmaceutics.

Discovery of a novel 2-spiro-proline steroid mimetic scaffold for the potent inhibition of 11β-HSD1.

R. Wynn, P. Scherle, Yanlong Li, 2022, Bioorganic & medicinal chemistry letters.

Discovery and Pharmacological Characterization of a Novel Rodent-Active CCR2 Antagonist, INCB3344

P. Scherle, F. Baribaud, L. Leffet, 2005, The Journal of Immunology.

Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.

P. Scherle, K. Vaddi, Joseph Glenn, 2010, ACS medicinal chemistry letters.

Potent and Selective Biaryl Amide Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).

M. Covington, S. Diamond, E. Behshad, 2022, ACS medicinal chemistry letters.

Discovery of Pyrazolopyridine Derivatives as HPK1 Inhibitors.

M. Covington, S. Diamond, E. Behshad, 2022, ACS medicinal chemistry letters.

Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.

P. Scherle, K. Vaddi, M. Covington, 2010, Bioorganic & medicinal chemistry letters.

Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.

S Diamond, S S Ko, G L Trainor, 2000, Journal of medicinal chemistry.

Expanded-Spectrum Nonnucleoside Reverse Transcriptase Inhibitors Inhibit Clinically Relevant Mutant Variants of Human Immunodeficiency Virus Type 1

Ronald M. Klabe, L. Bacheler, P. Anderson, 1999, Antimicrobial Agents and Chemotherapy.

DPC 817: a Cytidine Nucleoside Analog with Activity against Zidovudine- and Lamivudine-Resistant Viral Variants

L. Bacheler, M. Otto, M. Rayner, 2002, Antimicrobial Agents and Chemotherapy.

In Vitro and In Vivo Effects of the Arylamine Human Immunodeficiency Virus Protease Inhibitor 4R-(4α,5α,6β,7β)-1-[(3-(1-Imidazoylcarbamoyl)phenyl)methyl]-3-[(3-aminophenyl)methyl]hexahydro-5,6-dihydroxy-4,7-bis(phenylmethyl)-2H-1,3-diazepin-2-one (SD894) on Rat Hepatic Cytochrome P450 2B and 3A

S. Diamond, D. Christ, M. Grubb, 1997 .

Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.

D. J. Rogier, P. Scherle, R. Devraj, 2011, Bioorganic & medicinal chemistry letters.

DPC 681 and DPC 684: Potent, Selective Inhibitors of Human Immunodeficiency Virus Protease Active against Clinically Relevant Mutant Variants

L. Bacheler, R. Klabe, G. Harris, 2001, Antimicrobial Agents and Chemotherapy.

Impact on Creatinine Renal Clearance by the Interplay of Multiple Renal Transporters: A Case Study with INCB039110

Bill Williams, Yan Zhang, S. Diamond, 2015, Drug Metabolism and Disposition.

Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

Lixin Shao, Michael Xia, D. J. Rogier, 2011, ACS medicinal chemistry letters.

Discovery and Pharmacological Characterization of a Novel Rodent-Active CCR2 Antagonist, INCB3344

P. Scherle, F. Baribaud, T. Burn, 2005, The Journal of Immunology.

Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.

M. Covington, S. Diamond, S. Yeleswaram, 2022, ACS medicinal chemistry letters.

Roles of UGT, P450, and Gut Microbiota in the Metabolism of Epacadostat in Humans

Kevin J. Bowman, A. Combs, W. Frietze, 2016, Drug Metabolism and Disposition.

INCB040093 Is a Novel PI3Kδ Inhibitor for the Treatment of B Cell Lymphoid Malignancies

Jun Yu Li, Qianqian Wang, B. Rumberger, 2018, The Journal of Pharmacology and Experimental Therapeutics.

INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models

R. Wynn, H. Koblish, Yue Zhang, 2020, PloS one.

The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies

Jun Yu Li, R. Wynn, X. Liu, 2018, Clinical Cancer Research.

Interaction of ritonavir on tissue distribution of a [(14)c]L-valinamide, a potent human immunodeficiency virus-1 protease inhibitor, in rats using quantitative whole-body autoradiography.

S. Diamond, D. Christ, L. Gan, 2002, Drug metabolism and disposition: the biological fate of chemicals.

Microsoft Word-26861637-file00

Bill Williams, Yan Zhang, S. Diamond, 2015 .

Effects of Epacadostat on Brain Extracellular Fluid Concentrations of Serotonin—an Intracerebral Microdialysis Study in Sprague-Dawley Rats

Kevin J. Bowman, J. Maleski, Yan Zhang, 2019, Drug Metabolism and Disposition.

THE CHIMPANZEE (PAN TROGLODYTES) AS A PHARMACOKINETIC MODEL FOR SELECTION OF DRUG CANDIDATES: MODEL CHARACTERIZATION AND APPLICATION

K. He, H. Wong, S. Diamond, 2004, Drug Metabolism and Disposition.

Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.

R. Wynn, H. Koblish, Yue Zhang, 2021, Journal of medicinal chemistry.

4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.

L. Bacheler, C. Weigelt, A. Cocuzza, 2001, Bioorganic & medicinal chemistry letters.

1 The translational landscape of SARS-CoV-2 and infected cells 1 2 3

J. Dougherty, S. Brody, A. Horani, 2020 .

In Vitro Interactions of Epacadostat and its Major Metabolites with Human Efflux and Uptake Transporters: Implications for Pharmacokinetics and Drug Interactions

Qiang Zhang, Yan Zhang, S. Diamond, 2017, Drug Metabolism and Disposition.

Induction of cytochromes P-450 2B and 3A in mice following the dietary administration of the novel cognitive enhancer linopirdine.

S. Diamond, D. Christ, J. O'Neil, 1994, Drug metabolism and disposition: the biological fate of chemicals.

Species-specific, P450- and sulfotransferase-mediated novel ring contraction of a naphthyridine-N-oxide compound in cynomolgus monkey.

A. Mutlib, S. Unger, Barry C. Johnson, 2007, Chemical research in toxicology.

Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach.

April Horsey, L. Leffet, M. Covington, 2023, ACS Medicinal Chemistry Letters.

Characterization of a Novel Rodent-Active Discovery and Pharmacological

P. Scherle, F. Baribaud, L. Leffet, 2013 .