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Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors

Journal of medicinal chemistry, 2017-03, Vol.60 (5), p.1946-1958

2017

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Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway

Journal of medicinal chemistry, 2019-05, Vol.62 (9), p.4656-4668

2019

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Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: Design, synthesis and structure–activity relationship studies

Bioorganic & medicinal chemistry letters, 2004-09, Vol.14 (18), p.4607-4613

2004

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Diastereoselective and Enantioselective Intramolecular Amino−Zinc−Enolate Carbometalation Reactions. A New Polysubstituted Pyrrolidines Synthesis

Journal of organic chemistry, 1998-04, Vol.63 (8), p.2442-2450

1998

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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors

Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16173-16203

2022

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Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C

Cancer discovery, 2022-06, Vol.12 (6), p.1500-1517

2022

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Small-molecule factor D inhibitors targeting the alternative complement pathway

Nature chemical biology, 2016-12, Vol.12 (12), p.1105

2016

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Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 2: Metabolism-directed optimization studies towards orally bioavailable derivatives

Bioorganic & medicinal chemistry letters, 2004-09, Vol.14 (18), p.4615-4621

2004

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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS G12C for the Treatment of Solid Tumors

Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16173-16203

2022

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A sensitive fluorescence intensity assay for deubiquitinating proteases using ubiquitin-rhodamine110-glycine as substrate

Analytical biochemistry, 2007-12, Vol.371 (2), p.201-207

2007

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Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach

Journal of medicinal chemistry, 2020-08, Vol.63 (15), p.8088-8113

2020

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Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo

Journal of medicinal chemistry, 2017-07, Vol.60 (13), p.5717-5735

2017

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trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker

Bioorganic & medicinal chemistry letters, 2015-04, Vol.25 (8), p.1782-1786

2015

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Discovery and Design of First Benzylamine-Based Ligands Binding to an Unlocked Conformation of the Complement Factor D

ACS medicinal chemistry letters, 2018-05, Vol.9 (5), p.490-495

2018

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Fluorescence Lifetime-Based Competitive Binding Assays for Measuring the Binding Potency of Protease Inhibitors In Vitro

Journal of biomolecular screening, 2014-07, Vol.19 (6), p.870-877

2014

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Abstract 4026: JDQ443, a covalent inhibitor of KRASG12C with a novel binding mode, shows broad antitumor activity in KRASG12C preclinical models as a single agent and in combination with inhibitors of SHP2, MEK or CDK4/6

Cancer research (Chicago, Ill.), 2022-06, Vol.82 (12_Supplement), p.4026-4026

2022

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The Discovery of Novel Potent trans-3,4-Disubstituted Pyrrolidine Inhibitors of the Human Aspartic Protease Renin from in Silico Three-Dimensional (3D) Pharmacophore Searches

Journal of medicinal chemistry, 2013-03, Vol.56 (6), p.2207-2217

2013

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trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker

Bioorganic & medicinal chemistry letters, 2015-04, Vol.25 (8), p.1787-1791

2015

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β-Glycosidase inhibitors mimicking the pyranoside boat conformation

Chemical communications (Cambridge, England), 2000-01 (19), p.1829-1830

2000

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Synthesis and Evaluation as Glycosidase Inhibitors of Isoquinuclidines Mimicking a Distorted β-Mannopyranoside

Helvetica chimica acta, 2003-11, Vol.86 (11), p.3787-3817

2003

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Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1

Bioorganic & medicinal chemistry letters, 2004-09, Vol.14 (18), p.4623-4626

2004

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Isoquinuclidine Mimics of β-D-Glucopyranosides: Differences and Similarities in the Mechanism of Action of some β-D-Glucosidases and a β-D-Mannosidase

Helvetica chimica acta, 2003-11, Vol.86 (11), p.3818-3835

2003

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Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives

Bioorganic & medicinal chemistry letters, 2004-09, Vol.14 (18), p.4627-4631

2004

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Amino Zinc Enolate Carbocyclization Reactions. New Access to Polysubstituted Piperidine Derivatives

Journal of organic chemistry, 1998-02, Vol.63 (3), p.566-574

1998

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Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors

Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway

Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: Design, synthesis and structure–activity relationship studies

Diastereoselective and Enantioselective Intramolecular Amino−Zinc−Enolate Carbometalation Reactions. A New Polysubstituted Pyrrolidines Synthesis

JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors

Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C

Small-molecule factor D inhibitors targeting the alternative complement pathway

Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 2: Metabolism-directed optimization studies towards orally bioavailable derivatives

Abstract P124: JDQ443, a covalent irreversible inhibitor of KRAS G12C, exhibits a novel binding mode and demonstrates potent anti-tumor activity and favorable pharmacokinetic properties in preclinical models

JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS G12C for the Treatment of Solid Tumors

A sensitive fluorescence intensity assay for deubiquitinating proteases using ubiquitin-rhodamine110-glycine as substrate

Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach

Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo

trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker

Discovery and Design of First Benzylamine-Based Ligands Binding to an Unlocked Conformation of the Complement Factor D

Fluorescence Lifetime-Based Competitive Binding Assays for Measuring the Binding Potency of Protease Inhibitors In Vitro

Abstract 4026: JDQ443, a covalent inhibitor of KRASG12C with a novel binding mode, shows broad antitumor activity in KRASG12C preclinical models as a single agent and in combination with inhibitors of SHP2, MEK or CDK4/6

The Discovery of Novel Potent trans-3,4-Disubstituted Pyrrolidine Inhibitors of the Human Aspartic Protease Renin from in Silico Three-Dimensional (3D) Pharmacophore Searches

trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker

β-Glycosidase inhibitors mimicking the pyranoside boat conformation

Synthesis and Evaluation as Glycosidase Inhibitors of Isoquinuclidines Mimicking a Distorted β-Mannopyranoside

Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1

Isoquinuclidine Mimics of β-D-Glucopyranosides: Differences and Similarities in the Mechanism of Action of some β-D-Glucosidases and a β-D-Mannosidase

Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives

Amino Zinc Enolate Carbocyclization Reactions. New Access to Polysubstituted Piperidine Derivatives

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