Jeanene E. Tickner

Early Development of Ibuzatrelvir: Navigating Polymorph and Crystallization Challenges in a Protecting Group-Free Direct Amidation and Amidation-Dehydration Sequence

María González‐Esguevillas, Aaron F. Baldwin, Pablo J. Cabrera, Yanfei Guan et autres

Abstract Ibuzatrelvir is an orally bioavailable, next-generation clinical candidate developed for the treatment of COVID-19 infections. It was identified during the pandemic, prior to the approval of PAXLOVID, and displays a more favorable pharmacokinetic profile than nirmatrelvir. Consequently, the initial development of …

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The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A3 receptor

Michael P. DeNinno, Hiroko Masamune, Lois K. Chenard, Kenneth J. DiRico et autres

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3‘-Aminoadenosine-5‘-uronamides: Discovery of the First Highly Selective Agonist at the Human Adenosine A 3 Receptor

Michael P. DeNinno, Hiroko Masamune, Lois K. Chenard, Kenneth J. DiRico et autres

Selective adenosine A(3) agonists have potential utility for the prevention of perioperative myocardial ischemic injury. Herein, we report on the discovery and synthesis of compound 7. This amino nucleoside agonist possesses unprecedented levels of selectivity for the human adenosine A(3) receptor.

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Discovery of micromolar PDE IV inhibitors that exhibit much reduced affinity for the [3H]rolipram binding site: 3-norbornyloxy-4-methoxyphenylmethylene oxindoles

Hiroko Masamune, John B. Cheng, Kelvin Cooper, James F. Eggier et autres

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LTD4 Receptor binding activity of novel pyridine chromanols: qualitative correlation with pKa

Hiroko Masamune, James F. Eggler, Anthony Marfat, Lawrence S. Melvin et autres

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Synthesis and pharmacological profile of two novel heterocyclic chromanols, CP-80,798 and CP-85,958, as potent LTD4 receptor antagonists

E. G. ANDREWS, G.W. Antognoli, R Breslow, Michael P. Carta et autres

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Synthesis and in vitro profile of 7-substituted quinoline chromanols as novel, non-acidic LTB4 antagonists

Hiroko Masamune, R Breslow, John B. Cheng, Maryrose J. Conklyn et autres

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