Search Results - "Cox, Philip B"
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Beyond the Rule of 5: Lessons Learned from AbbVie's Drugs and Compound Collection
Published in Journal of medicinal chemistry (12-04-2018)“…Recently, there has been an increasing focus on the pursuit of targets considered to be less druggable that offer potential for development of promising new…”
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Identification and structure-based drug design of cell-active inhibitors of interleukin 17A at a novel C-terminal site
Published in Scientific reports (26-08-2022)“…Anti-IL17A therapies have proven effective for numerous inflammatory diseases including psoriasis, axial spondylitis and psoriatic arthritis. Modulating and/or…”
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Abbott Physicochemical Tiering (APT)—A unified approach to HTS triage
Published in Bioorganic & medicinal chemistry (15-07-2012)“…An in silico tool has been developed to help prioritize hits from HTS based on multi-parametric physicochemical properties. This Abbott Physicochemical Tiering…”
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Phenols in Pharmaceuticals: Analysis of a Recurring Motif
Published in Journal of medicinal chemistry (26-05-2022)“…Phenols and phenolic ethers are significant scaffolds recurring both in nature and among approved small-molecule pharmaceuticals. This compendium presents the…”
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Contemporary Computational Applications and Tools in Drug Discovery
Published in ACS medicinal chemistry letters (14-07-2022)“…In the past decade or so there has been a dramatic increase in the number of computational applications and tools that have been developed to enable medicinal…”
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Beyond Rule of Five and PROTACs in Modern Drug Discovery: Polarity Reducers, Chameleonicity, and the Evolving Physicochemical Landscape
Published in Journal of medicinal chemistry (11-04-2024)“…Developing orally bioavailable drugs demands an understanding of absorption in early drug development. Traditional methods and physicochemical properties…”
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An Update on the Nitrogen Heterocycle Compositions and Properties of U.S. FDA-Approved Pharmaceuticals (2013–2023)
Published in Journal of medicinal chemistry (25-07-2024)“…This Perspective is a continuation of our analysis of U.S. FDA-approved small-molecule drugs (1938–2012) containing nitrogen heterocycles. In this study we…”
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Design and Synthesis of Pyrrolidine-based Fragments That Sample Three-dimensional Molecular Space
Published in ACS medicinal chemistry letters (09-05-2019)“…Fragment-based drug discovery (FBDD) is a well-established technology for lead compound generation in drug discovery. As this technology has evolved, the…”
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A Structural Analysis of the FDA Green Book-Approved Veterinary Drugs and Roles in Human Medicine
Published in Journal of medicinal chemistry (24-12-2020)“…The FDA Green Book is a list of all drug products that have been approved by the FDA for use in veterinary medicine. The Green Book, as published, lacks…”
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Escaping from Flatland: Substituted Bridged Pyrrolidine Fragments with Inherent Three-Dimensional Character
Published in ACS medicinal chemistry letters (11-06-2020)“…The pressure to deliver new medicines to the patient continues to grow along with increases in compound failure rate, thus putting the current R&D model at…”
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Development of Orally Efficacious Allosteric Inhibitors of TNFα via Fragment-Based Drug Design
Published in Journal of medicinal chemistry (14-01-2021)“…Tumor necrosis factor α (TNFα) is a soluble cytokine that is directly involved in systemic inflammation through the regulation of the intracellular NF-κB and…”
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Beyond the Rule of 5: Lessons Learned from AbbVie’s Drugs and Compound Collection: Miniperspective
Published in Journal of medicinal chemistry (12-04-2018)“…Recently, there has been an increasing focus on the pursuit of targets considered to be less druggable that offer potential for development of promising new…”
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Differential Expression of Prostaglandin E2 Receptors in Porcine Kidney Transplants
Published in Transplantation proceedings (01-07-2019)“…Acute rejection of a kidney allograft results from adaptive immune responses and marked inflammation. The eicosanoid prostaglandin E2 (PGE2) modulates the…”
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Discovery of Antibacterial Biotin Carboxylase Inhibitors by Virtual Screening and Fragment-Based Approaches
Published in ACS chemical biology (19-06-2009)“…As part of our effort to inhibit bacterial fatty acid biosynthesis through the recently validated target biotin carboxylase, we employed a unique combination…”
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Use of Silicon-Based Tethers to Control Diastereofacial Selectivity in Azomethine Ylide Cycloadditions1
Published in Journal of organic chemistry (07-02-1997)“…A novel approach to controlling the diastereofacial selectivity of intramolecular dipolar cycloadditions of azomethine ylides (cf. 9 → 8) by varying the…”
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Development of an Effective Chiral Auxiliary for Hydroxyalkyl Radicals
Published in Journal of organic chemistry (23-08-2002)“…The development of an effective chiral auxiliary for hydroxyalkyl radicals is delineated. Both the 2-tetrahydropyranyl (THP) and…”
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Use of Silicon-Based Tethers to Control Diastereofacial Selectivity in Azomethine Ylide Cycloadditions(1)
Published in Journal of organic chemistry (07-02-1997)“…A novel approach to controlling the diastereofacial selectivity of intramolecular dipolar cycloadditions of azomethine ylides (cf. 9 --> 8) by varying the…”
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4,6-Dichloro-5-nitropyrimidine: a versatile building block for the solid phase synthesis of dihydropteridinones
Published in Tetrahedron letters (14-10-2000)“…This letter describes a novel, flexible, solid phase route to pyrimidine-based heterocycles that utilises commercially available…”
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The solid phase synthesis of unsymmetrical phosphinic acids
Published in Tetrahedron letters (01-01-2001)Get full text
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Auxiliary Induced .rho.-Stereocontrol in Acetaloxyalkyl Radical Addition Reactions
Published in Journal of the American Chemical Society (01-04-1995)Get full text
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