List of works - James J. Crawford

(1R,2R)-N-(1-Cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A Potent and Highly Selective Cathepsin K Inhibitor for the Treatment of Osteoarthritis ⬇️

scientific article published on July 10, 2012

A simple in vitro assay for assessing the reactivity of nitrile containing compounds.

scientific article published in January 2009

Bruton's Tyrosine Kinase Small Molecule Inhibitors Induce a Distinct Pancreatic Toxicity in Rats.

scientific article published on 7 November 2016

Btk-specific inhibition blocks pathogenic plasma cell signatures and myeloid cell-associated damage in IFNα-driven lupus nephritis.

scientific article published on 06 April 2017

Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window

scientific article

Copper/TEMPO catalysed synthesis of nitriles from aldehydes or alcohols using aqueous ammonia and with air as the oxidant

scientific article published on 01 July 2013

Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.

scientific article

Diethylphosphine oxide (DEPO): high-yielding and facile preparation of indolones in water

scientific article published on 01 August 2003

Discovery of GDC-0853, a Potent, Selective, and Non-Covalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development

scientific article published on 19 February 2018

Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties

scientific article

Fast and efficient one step synthesis of dienamides

scientific article published on 16 April 2009

Hippo pathway inhibition by blocking the YAP/TAZ-TEAD interface: a patent review

scientific article published on 02 December 2018

Inhibitors of p21-activated kinases (PAKs).

scientific article published on 3 December 2014

Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.

scientific article

Learning Medicinal Chemistry Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) Rules from Cross-Company Matched Molecular Pairs Analysis (MMPA).

scientific article published on 28 September 2017

Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series

scientific article published on 20 May 2015

LogD Contributions of Substituents Commonly Used in Medicinal Chemistry

scientific article published on 11 December 2019

NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus.

scientific article published on 12 January 2018

Optimized arylomycins are a new class of Gram-negative antibiotics

scientific article published in Nature

Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors

scientific article published on 11 October 2012

Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834

scientific article

Protecting group free, stereocontrolled synthesis of β-halo-enamides

scientific article published on 14 February 2012

RORγ antagonists and inverse agonists: a patent review

scientific article

Rate-Determining and Rate-Limiting Steps in the Clearance and Excretion of a Potent and Selective p21-Activated Kinase Inhibitor: A Case Study of Rapid Hepatic Uptake and Slow Elimination in Rat.

scientific article

Recent progress on nuclear receptor RORγ modulators

scientific article

Remote functionalisation via sodium alkylamidozincate intermediates: access to unusual fluorenone and pyridyl ketone reactivity patterns

scientific article published on 24 February 2011

Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase

scientific article published on 24 July 2018

Single electron transfer (SET) activity of the dialkyl-amido sodium zincate [(TMEDA)·Na(μ-TMP)(μ-tBu)Zn(tBu)] towards TEMPO and chalcone

article

Step-economic synthesis of (+)-crocacin C: a concise crotylboronation/[3,3]-sigmatropic rearrangement approach

scientific article published on 02 August 2012

Streamlined Total Synthesis of Uncialamycin and Its Application to the Synthesis of Designed Analogues for Biological Investigations

scientific article published on 7 June 2016

Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors

scientific article

Synthesis and evaluation of a series of 4-azaindole-containing p21-activated kinase-1 inhibitors.

scientific article published on 15 June 2016

Synthesis of (+)-crocacin D and simplified bioactive analogues.

scientific article published on 10 January 2015

Synthesis of Fused Imidazole-Containing Ring Systems via Dual Oxidative Amination of C(sp(3))-H Bonds

scientific article

The kinase IRAK4 promotes endosomal TLR and immune complex signaling in B cells and plasmacytoid dendritic cells

scientific article published on 02 June 2020

Total synthesis and stereochemistry of uncialamycin

scientific article published on 01 January 2007

p21-Activated kinase inhibitors: a patent review

scientific article

p21-activated kinase inhibitors

scientific article (publication date: 2013)

List of works by James J. Crawford

(1R,2R)-N-(1-Cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A Potent and Highly Selective Cathepsin K Inhibitor for the Treatment of Osteoarthritis ⬇️

A simple in vitro assay for assessing the reactivity of nitrile containing compounds.

Bruton's Tyrosine Kinase Small Molecule Inhibitors Induce a Distinct Pancreatic Toxicity in Rats.

Btk-specific inhibition blocks pathogenic plasma cell signatures and myeloid cell-associated damage in IFNα-driven lupus nephritis.

Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window

Copper/TEMPO catalysed synthesis of nitriles from aldehydes or alcohols using aqueous ammonia and with air as the oxidant

Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.

Diethylphosphine oxide (DEPO): high-yielding and facile preparation of indolones in water

Discovery of GDC-0853, a Potent, Selective, and Non-Covalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development

Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties

Fast and efficient one step synthesis of dienamides

Hippo pathway inhibition by blocking the YAP/TAZ-TEAD interface: a patent review

Inhibitors of p21-activated kinases (PAKs).

Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.

Learning Medicinal Chemistry Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) Rules from Cross-Company Matched Molecular Pairs Analysis (MMPA).

Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series

LogD Contributions of Substituents Commonly Used in Medicinal Chemistry

NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus.

Optimized arylomycins are a new class of Gram-negative antibiotics

Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors

Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834

Protecting group free, stereocontrolled synthesis of β-halo-enamides

RORγ antagonists and inverse agonists: a patent review

Rate-Determining and Rate-Limiting Steps in the Clearance and Excretion of a Potent and Selective p21-Activated Kinase Inhibitor: A Case Study of Rapid Hepatic Uptake and Slow Elimination in Rat.

Recent progress on nuclear receptor RORγ modulators

Remote functionalisation via sodium alkylamidozincate intermediates: access to unusual fluorenone and pyridyl ketone reactivity patterns

Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase

Single electron transfer (SET) activity of the dialkyl-amido sodium zincate [(TMEDA)·Na(μ-TMP)(μ-tBu)Zn(tBu)] towards TEMPO and chalcone

Step-economic synthesis of (+)-crocacin C: a concise crotylboronation/[3,3]-sigmatropic rearrangement approach

Streamlined Total Synthesis of Uncialamycin and Its Application to the Synthesis of Designed Analogues for Biological Investigations

Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors

Synthesis and evaluation of a series of 4-azaindole-containing p21-activated kinase-1 inhibitors.

Synthesis of (+)-crocacin D and simplified bioactive analogues.

Synthesis of Fused Imidazole-Containing Ring Systems via Dual Oxidative Amination of C(sp(3))-H Bonds

The kinase IRAK4 promotes endosomal TLR and immune complex signaling in B cells and plasmacytoid dendritic cells

Total synthesis and stereochemistry of uncialamycin

p21-Activated kinase inhibitors: a patent review

p21-activated kinase inhibitors