Core B – Medicinal and Process Chemistry

核心 B — 药物和工艺化学

• 批准号: 10513937
• 负责人: Michael George Natchus
• 金额: $ 1054.86万
• 依托单位: EMORY UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2022
• 资助国家: 美国
• 起止时间: 2022-05-16 至 2025-04-30
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/10513937
• 关键词: 2019-nCoV; Academia; Address; Animal Model; Antiviral Therapy; Charge; Chemistry; Clinical; Cyclic GMP; Development; Ensure; FDA approved; Family; Formulation; HIV; Hepatitis B Therapy; Hepatitis B Virus; Institutes; Kilogram; Lamivudine; Licensing; Morbillivirus Infections; Oral; Pharmaceutical Chemistry; Pharmaceutical Preparations; Phase; Phase II Clinical Trials; Plants; Polymerase; Polymorph; Powder dose form; Process; Protease Inhibitor; Records; Research; Respiratory syncytial virus; Ribonucleosides; Roentgen Rays; SARS-CoV-2 infection; Science; Seasons; Solid; Viral; Virus Diseases; Work; analog; antiviral drug development; base; drug candidate; drug development; emtricitabine; first-in-human; high throughput screening; influenzavirus; inhibitor; interest; molnupiravir; novel; operation; preclinical development; professor; programs; research and development; scale up; synergism

Project Summary – Core B The Medicinal Chemistry Core (Core B) of the Antiviral Countermeasures Development Center (AC/DC) will be composed of the combined capacity of the Emory Institute for Drug Development (EIDD) and the research group of Professor Dennis Liotta. This Core will centralize all AC/DC chemistry operations including medicinal chemistry, scale-up synthesis, process development and preformulation profiling into a highly efficient team that will reduce redundant research around chemotypes that are of interest to multiple Projects. It will also interact closely with all AC/DC Projects and Cores to allow for an unprecedented level of synergy and integration throughout the Center. The AC/DC will have a compelling set of leads, early leads and validated hits in its pipeline at various stages of development and optimization at the onset of operations. These compounds present a wide array of chemotypes that will be pursued in parallel, including broadly active ribonucleoside leads, non- nucleoside viral polymerase inhibitor leads, and viral protease inhibitor hits. New validated hits emerging from Core F (HTS) will also be advanced through iterative SAR optimization to ensure an ongoing robust pipeline of drug candidates at various stages of development. Finally, Core B will develop scale-up processes and preformulation profiles to support the advancement of late leads throughout the AC/DC.

项目摘要-核心B 抗病毒对策发展中心(AC/DC)的药物化学核心(核心B)将是 由埃默里药物开发研究所(EIDD)和研究小组的联合能力组成 丹尼斯·利奥塔教授的。该核心将集中所有AC/DC化学操作，包括医疗 化学、放大合成、工艺开发和配方前分析组成一个高效的团队， 将减少围绕多个项目感兴趣的化学类型的重复研究。它还会与 与所有AC/DC项目和核心密切合作，实现前所未有的协同和集成 在整个中心。AC/DC将有一组令人信服的引线、早期引线和验证命中 在运营开始时处于开发和优化的不同阶段。这些化合物表现出广泛的 将并行进行的一系列化学类型，包括广泛活性的核糖核苷前导，非 核苷类病毒聚合酶抑制剂先导，病毒蛋白酶抑制剂命中。新的经验证的命中率从 核心F(HTS)也将通过迭代SAR优化来推进，以确保持续的强大管道 处于不同开发阶段的候选药物。最后，Core B将开发纵向扩展流程，并 配方前配置文件，以支持整个AC/DC中后期引线的推进。