James S. Scott

发表

Selective estrogen receptor degraders (SERDs) and covalent antagonists (SERCAs): a patent review (2015-present)

James S. Scott, B. Barlaam, 2021, Expert opinion on therapeutic patents.

Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.

Peter D Smith, A. Rabow, R. A. Norman, 2016, ACS medicinal chemistry letters.

Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.

R. A. Norman, James S. Scott, A. Bailey, 2015, Journal of medicinal chemistry.

Lowering Lipophilicity by Adding Carbon: One-Carbon Bridges of Morpholines and Piperazines.

James S. Scott, S. Degorce, I. Cumming, 2018, Journal of medicinal chemistry.

Achieving improved permeability by hydrogen bond donor modulation in a series of MGAT2 inhibitors

Philip A. MacFaul, Graeme R. Robb, Andrew G. Leach, 2013 .

Multi-step organic synthesis using solid-supported reagents and scavengers: a new paradigm in chemical library generation

Steven V. Ley, R. Ian Storer, Andrew G. Leach, 2000 .

Synthesis of the potent analgesic compound (±)-epibatidine using an orchestrated multi-step sequence of polymer supported reagents

Steven V. Ley, S. Ley, James S. Scott, 1999 .

An Umpolung Approach to Alkene Carboamination: Palladium Catalyzed 1,2-Amino-Acylation, -Carboxylation, -Arylation, -Vinylation, and -Alkynylation.

James S. Scott, J. Bower, A. Faulkner, 2015, Journal of the American Chemical Society.

Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).

James S. Scott, A. Turnbull, F. W. Goldberg, 2014, Journal of medicinal chemistry.

Copper catalyzed Heck-like cyclizations of oxime esters

James S. Scott, J. Bower, Nicholas J. Race, 2014 .

Fragment-Based Design of a Potent MAT2a Inhibitor and in Vivo Evaluation in an MTAP Null Xenograft Model.

S. Tentarelli, M. Vázquez‐Chantada, E. Chiarparin, 2021, Journal of medicinal chemistry.

Skipped Fluorination Motifs: Synthesis of Building Blocks and Comparison of Lipophilicity Trends with Vicinal and Isolated Fluorination Motifs.

E. Chiarparin, James S. Scott, Robert I Troup, 2021, The Journal of organic chemistry.

Synthesis of trans 8-substituted-6-phenyl-6,7,8,9-tetrahydro-3H-pyrazolo [4,3-f]isoquinolines using a Pictet-Spengler approach

James S. Scott, A. Bailey, T. Moss, 2018, Tetrahedron Letters.

Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors

Edward W. Tate, James S. Scott, Charlie N Saunders, 2020, ACS chemical biology.

Lipophilicity trends upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl groups

E. Chiarparin, James S. Scott, J. Graton, 2020, Beilstein journal of organic chemistry.

Stereochemical and mechanistic features of asymmetric Pauson-Khand processes

James S. Scott, W. Kerr, S. Watson, 2000 .

Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.

Hayley S. Brown, D. Laber, James S. Scott, 2014, Journal of medicinal chemistry.

A patent review of MAT2a inhibitors (2018–2021)

James S. Scott, S. Atkinson, L. Evans, 2022, Expert opinion on therapeutic patents.

Discovery of a series of 5-AzaQuinazolines as orally efficacious IRAK4 inhibitors targeting MyD88L265P mutant Diffuse Large B Cell Lymphoma.

A. Bloecher, L. Drew, R. Anjum, 2019, Journal of medicinal chemistry.

Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.

L. Drew, R. Anjum, Yafeng Xue, 2018, Bioorganic & medicinal chemistry.

Virtual Screening in the Cloud Identifies Potent and Selective ROS1 Kinase Inhibitors

J. Sadowski, D. Hargreaves, James S. Scott, 2022, J. Chem. Inf. Model..

Sustained wash-resistant receptor activation responses of GPR119 agonists.

James S. Scott, I. Dale, J. D. Hothersall, 2015, European journal of pharmacology.

Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human.

Hayley S. Brown, D. Laber, James S. Scott, 2013, Bioorganic & medicinal chemistry letters.

A Systematic Investigation of Lipophilicity Modulation by Aliphatic Fluorination Motifs.

E. Chiarparin, James S. Scott, J. Graton, 2020, Journal of medicinal chemistry.

Highly selective entry to the azadirachtin skeleton via a Claisen rearrangement/radical cyclization sequence.

S. Ley, James S. Scott, L. Gobbi, 2002, Organic letters.

Clean synthesis of α-bromo ketones and their utilisation in the synthesis of 2-alkoxy-2,3-dihydro-2-aryl-1,4-benzodioxanes, 2-amino-4-aryl-1,3-thiazoles and piperidino-2-amino-1,3-thiazoles using polymer-supported reagents

S. Ley, James S. Scott, J. Scicinski, 1999 .

Clean six-step synthesis of a piperidino-thiomorpholine library using polymer-supported reagents

S. Ley, James S. Scott, J. Habermann, 1998 .

The synthesis of azadirachtin: a potent insect antifeedant.

D. Jennens, M. Göbel, A. Wood, 2008, Chemistry.

Elucidating the mechanism of the photochemical Pauson–Khand reaction: matrix photochemistry of phenylacetylenehexacarbonyldicobalt

James S. Scott, C. Gordon, W. Kerr, 1998 .

Palladium catalyzed cyclizations of oxime esters with 1,1-disubstituted alkenes: synthesis of α,α-disubstituted dihydropyrroles and studies towards an asymmetric protocol.

James S. Scott, J. Bower, A. Faulkner, 2013, Chemical communications.

Identification and optimisation of 3,3-dimethyl-azetidin-2-ones as potent and selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)

S. Steinbacher, M. Augustin, D. Ogg, 2014 .

Total synthesis of parvaquone and the serendipitous discovery of a novel chromium-mediated method for β-lactone formation

James S. Scott, W. Kerr, D. Middlemiss, 1997 .

Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.

Andrew G. Leach, Hayley S. Brown, D. Laber, 2012, Journal of medicinal chemistry.

Total synthesis of rapamycin.

Matthew L. Maddess, S. Marsden, S. Ley, 2009, Chemistry.

Reducing the Lipophilicity of Perfluoroalkyl Groups by CF2-F/CF2-Me or CF3/CH3 Exchange.

E. Chiarparin, James S. Scott, J. Graton, 2018, Journal of medicinal chemistry.

Total synthesis of rapamycin.

Matthew L. Maddess, S. Ley, P. Brennan, 2007, Angewandte Chemie.

Synthesis of 8-substituted-6-phenyl-6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinolines using Pictet-Spengler and Bischler-Napieralski cyclisation methods

James S. Scott, A. Bailey, Robert D. M. Davies, 2018, Tetrahedron Letters.

The brucine N -oxide promoted asymmetric Pauson-Khand reaction

James S. Scott, W. Kerr, S. Watson, 2000 .

Preparation and reaction of desymmetrised cobalt alkyne complexes

James S. Scott, W. Kerr, S. Watson, 2000 .

Studies on Pd/imidazolium salt protocols for aminations of aryl bromides and iodides using lithium hexamethyldisilazide (LHMDS)

S. Caddick, James S. Scott, S. Pearson, 2005 .

Discovery, optimisation and in vivo evaluation of novel GPR119 agonists.

Andrew G. Leach, Hayley S. Brown, James S. Scott, 2011, Bioorganic & medicinal chemistry letters.

Practical synthesis of 3,3-substituted dihydroquinoxalin-2-ones from aryl 1,2-diamines using the Bargellini reaction

James S. Scott, S. Stokes, T. Alanine, 2016 .

Pd-Catalyzed C-H aziridination of 3,3,5,5-tetrasubstituted piperazin-2-ones.

C. A. Roberts, James S. Scott, S. Stokes, 2017, Organic & biomolecular chemistry.

Selective cleavage of ketals and acetals under neutral, anhydrous conditions using triphenylphosphine and carbon tetrabromide

James S. Scott, C. Johnstone, W. Kerr, 1996 .

A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

James S. Scott, B. Barlaam, R. Ducray, 2008, Bioorganic & medicinal chemistry letters.

Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

James S. Scott, B. Barlaam, R. Bradbury, 2007, Bioorganic & medicinal chemistry letters.

Development of a practical Buchwald-Hartwig amine arylation protocol using a conveniently prepared (NHC)Pd(R-allyl)Cl catalyst.

Richard J. Fitzmaurice, S. Caddick, James S. Scott, 2008, Organic & biomolecular chemistry.

Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma.

Nichola L. Davies, A. Ferguson, L. Drew, 2017, Journal of medicinal chemistry.

Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival.

Graeme Walker, Lisa Wissler, Jon Read, 2016, Journal of medicinal chemistry.

Novel acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with reduced acyl glucuronide liability: the discovery of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid (AZD8329).

Martin J Packer, Nidhal Selmi, Andrew Stocker, 2012, Journal of medicinal chemistry.

Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors.

Cristian Bodin, Andrew G Leach, James S. Scott, 2012, Journal of medicinal chemistry.

A Buchwald-Hartwig Protocol to Enable Rapid Linker Exploration of Cereblon E3-Ligase PROTACs.

James S. Scott, Shaun M. Fillery, G. Fairley, 2020, Chemistry.

Abstract 5674: Discovery of AZD9833, an oral small molecule selective degrader of the estrogen receptor (SERD)

James S. Scott, T. Moss, C. Morrow, 2020 .

Practical application of ligand efficiency metrics in lead optimisation.

M. Waring, James S. Scott, 2018, Bioorganic & medicinal chemistry.

Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.

R. Anjum, Yafeng Xue, James S. Scott, 2020, Bioorganic & medicinal chemistry.

Design of pyrazolo-pyrimidines as 11β-HSD1 inhibitors through optimisation of molecular electrostatic potential

James S. Scott, G. Robb, J. Swales, 2015 .

Discovery of AZD9833, a potent and orally bioavailable selective estrogen receptor degrader and antagonist.

O. Delpuech, J. Breed, J. Nissink, 2020, Journal of medicinal chemistry.

Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833.

Paul R. J. Davey, James S. Scott, B. Barlaam, 2020, ACS medicinal chemistry letters.

Discovery of a potent, selective, and orally bioavailable acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor: discovery of 2-[(3S)-1-[5-(cyclohexylcarbamoyl)-6-propylsulfanylpyridin-2-yl]-3-piperidyl]acetic acid (AZD4017).

Martin J Packer, Nidhal Selmi, David Hargreaves, 2012, Journal of medicinal chemistry.

Lowering Lipophilicity by Adding Carbon: AzaSpiroHeptanes, a logD Lowering Twist.

James S. Scott, S. Degorce, M. Bodnarchuk, 2019, ACS medicinal chemistry letters.

Identification and optimisation of a pyrimidopyridone series of IRAK4 inhibitors.

Nichola L. Davies, Yafeng Xue, James S. Scott, 2022, Bioorganic & medicinal chemistry.

Reduction of acyl glucuronidation in a series of acidic 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors: the discovery of AZD6925

James S. Scott, N. Selmi, M. Packer, 2012 .

Optimization of brain penetrant 11β-hydroxysteroid dehydrogenase type I inhibitors and in vivo testing in diet-induced obese mice.

James S. Scott, A. Turnbull, T. Sjögren, 2014, Journal of medicinal chemistry.

Abstract 1042: Preclinical pharmacokinetic and metabolic characterization of the next generation oral SERD AZD9833

James S. Scott, T. Klinowska, D. Mcginnity, 2020 .

Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists.

Paul R. J. Davey, James S. Scott, A. Bailey, 2019, Journal of medicinal chemistry.

Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry.

J. Breed, J. Nissink, Paul R. J. Davey, 2019, ACS medicinal chemistry letters.

Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists.

J. Breed, J. Nissink, Paul R. J. Davey, 2023, Journal of medicinal chemistry.

Optimisation of aqueous solubility in a series of G protein coupled receptor 119 (GPR119) agonists

Andrew G. Leach, Hayley S. Brown, James S. Scott, 2013 .

Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors.

A. Gill, James S. Scott, J. Swales, 2012, Bioorganic & medicinal chemistry letters.

Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).

James S. Scott, A. Turnbull, Frederick W. Goldberg, 2014, Journal of medicinal chemistry.

Free-Wilson and structural approaches to co-optimizing human and rodent isoform potency for 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors.

Andrew G. Leach, James S. Scott, Frederick W. Goldberg, 2012, Journal of medicinal chemistry.

A facile synthesis of 3-trifluoromethyl-1,2,4-oxadiazoles from cyanamides

James S. Scott, D. S. Clarke, K. Goldberg, 2014 .

Oxadiazole isomers: all bioisosteres are not created equal

Andrew G. Leach, James S. Scott, P. Macfaul, 2012 .

A Facile Synthesis of 3‐Trifluoromethyl‐1,2,4‐oxadiazoles from Cyanamides.

James S. Scott, D. S. Clarke, K. Goldberg, 2015 .

Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.

L. Drew, R. Anjum, Yafeng Xue, 2018, Bioorganic & medicinal chemistry.

D. Hargreaves, D. Ogg, James S. Scott, 2012, Journal of medicinal chemistry.

Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.

Andrew G. Leach, Hayley S. Brown, D. Laber, 2014, Journal of medicinal chemistry.