Lista de obras -

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

artículo científico publicado en 2020

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

artículo científico publicado en 2007

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

artículo científico publicado en 2020

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

artículo científico publicado en 2015

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

scientific article published on 23 September 2019

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

artículo científico publicado en 2014

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

article

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

article published in 1999

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

artículo científico publicado en 2013

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

artículo científico publicado en 2016

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

artículo científico publicado en 2008

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

artículo científico publicado en 2017

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

scientific article published on 10 September 2020

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) ⬇️

artículo científico publicado el 19 de junio de 2012

Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265P Mutant Diffuse Large B Cell Lymphoma

scientific article published on 01 November 2019

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

artículo científico publicado en 2011

Enantioselective Narasaka-Heck cyclizations: synthesis of tetrasubstituted nitrogen-bearing stereocenters

artículo científico publicado en 2016

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

artículo científico publicado en 2012

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

artículo científico publicado en 2002

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

artículo científico publicado en 2020

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

artículo científico publicado en 2015

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

artículo científico publicado en 2020

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

scientific article published on 18 July 2019

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

artículo científico publicado en 2018

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

artículo científico

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

article

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

artículo científico publicado en 2007

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) ⬇️

artículo científico publicado el 7 de noviembre de 2012

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

artículo científico publicado el 5 de septiembre de 2012

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

artículo científico publicado en 2014

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

artículo científico publicado en 2018

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

artículo científico publicado en 2013

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

artículo científico publicado en 2017

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

artículo científico publicado en 2016

Practical application of ligand efficiency metrics in lead optimisation

artículo científico publicado en 2018

Reducing the lipophilicity of perfluoroalkyl groups by CF2-F/CF2-Me or CF3/CH3 exchange

artículo científico publicado en 2018

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

artículo científico publicado en 2021

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

scientific article published on 10 February 2020

Sustained wash-resistant receptor activation responses of GPR119 agonists

artículo científico publicado en 2015

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

article

Systematic Investigation of Lipophilicity Modulation by Aliphatic Fluorination Motifs

artículo científico publicado en 2020

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

artículo científico publicado en 2015

The synthesis of azadirachtin: a potent insect antifeedant.

artículo científico publicado en 2008

Total Synthesis of Rapamycin

scientific article published on 01 January 2007

Total synthesis of rapamycin

artículo científico publicado en 2009

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

scientific article published on 30 January 2019

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.

artículo científico publicado en 2012

Lista de obras de

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

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

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

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

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

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

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

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

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

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

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

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

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

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) ⬇️

Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265P Mutant Diffuse Large B Cell Lymphoma

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

Enantioselective Narasaka-Heck cyclizations: synthesis of tetrasubstituted nitrogen-bearing stereocenters

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

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

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

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

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

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

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

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

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

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

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) ⬇️

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

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

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

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

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

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

Practical application of ligand efficiency metrics in lead optimisation

Reducing the lipophilicity of perfluoroalkyl groups by CF2-F/CF2-Me or CF3/CH3 exchange

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

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

Sustained wash-resistant receptor activation responses of GPR119 agonists

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

Systematic Investigation of Lipophilicity Modulation by Aliphatic Fluorination Motifs

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

The synthesis of azadirachtin: a potent insect antifeedant.

Total Synthesis of Rapamycin

Total synthesis of rapamycin

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

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.