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The discovery of first-in-class drugs: origins and evolution

Nature reviews. Drug discovery, 2014-08, Vol.13 (8), p.577-587

2014

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Targeted inhibition of the COP9 signalosome for treatment of cancer

Nature communications, 2016-10, Vol.7 (1), p.13166-13166, Article 13166

2016

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Derivation of Rapamycin: Adventures in Natural Product Chemistry

Chimia, 2019-08, Vol.73 (7-8), p.581

2019

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Direct Renin Inhibitors as a New Therapy for Hypertension

Journal of medicinal chemistry, 2010-11, Vol.53 (21), p.7490-7520

2010

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Discovery of 3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a Potent and Selective Inhibitor of Protein Kinase C Isotypes

Journal of medicinal chemistry, 2009-10, Vol.52 (20), p.6193-6196

2009

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Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes

Bioorganic & medicinal chemistry letters, 2012-02, Vol.22 (3), p.1464-1468

2012

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Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV

Bioorganic & medicinal chemistry letters, 2014-02, Vol.24 (3), p.731-736

2014

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Structure of Human Cyclophilin A in Complex with the Novel Immunosuppressant Sanglifehrin A at 1.6 Å Resolution

The Journal of biological chemistry, 2005-06, Vol.280 (23), p.21965-21971

2005

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The macrolide everolimus forms an unusual metabolite in animals and humans: identification of a phosphocholine ester

Drug metabolism and disposition, 2008-08, Vol.36 (8), p.1457

2008

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Small-molecule factor B inhibitor for the treatment of complement-mediated diseases

Proceedings of the National Academy of Sciences - PNAS, 2019-04, Vol.116 (16), p.7926-7931

2019

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Discovery of 4-((2 S ,4 S )-4-Ethoxy-1-((5-methoxy-7-methyl-1 H -indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases

Journal of medicinal chemistry, 2020-06, Vol.63 (11), p.5697-5722

2020

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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

Molecular cancer therapeutics, 2021-12, Vol.20 (12_Supplement), p.P124-P124

2021

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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, 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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Structure–Activity Relationship and Pharmacokinetic Studies of Sotrastaurin (AEB071), a Promising Novel Medicine for Prevention of Graft Rejection and Treatment of Psoriasis

Journal of medicinal chemistry, 2011-09, Vol.54 (17), p.6028-6039

2011

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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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A Novel Class of Oral Direct Renin Inhibitors: Highly Potent 3,5-Disubstituted Piperidines Bearing a Tricyclic P 3 – P 1 Pharmacophore

Journal of medicinal chemistry, 2013-03, Vol.56 (6), p.2196-2206

2013

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SDZ RAD, a new rapamycin derivative: pharmacological properties in vitro and in vivo

Transplantation, 1997-07, Vol.64 (1), p.36

1997

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A Novel Class of Oral Direct Renin Inhibitors: Highly Potent 3,5-Disubstituted Piperidines Bearing a Tricyclic P3 –P1 Pharmacophore

Journal of medicinal chemistry, 2013-03, Vol.56 (6), p.2196-2206

2013

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Sanglifehrin−Cyclophilin Interaction: Degradation Work, Synthetic Macrocyclic Analogues, X-ray Crystal Structure, and Binding Data

Journal of the American Chemical Society, 2003-04, Vol.125 (13), p.3849-3859

2003

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A convergent, highly stereoselective synthesis of a C-11-C-21 subunit of the macbecins

Journal of organic chemistry, 1991-09, Vol.56 (19), p.5496-5498

1991

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SDZ RAD, a new rapamycin derivative: synergism with cyclosporine

Transplantation, 1997-07, Vol.64 (1), p.32

1997

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Erratum to “Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes” [Bioorg. Med. Chem. Lett. 22 (2012) 1464–1468]

Bioorganic & medicinal chemistry letters, 2012-03, Vol.22 (6), p.2359-2359

2012

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The discovery of first-in-class drugs: origins and evolution

Targeted inhibition of the COP9 signalosome for treatment of cancer

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

Derivation of Rapamycin: Adventures in Natural Product Chemistry

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

Direct Renin Inhibitors as a New Therapy for Hypertension

Discovery of 3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a Potent and Selective Inhibitor of Protein Kinase C Isotypes

Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes

Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV

Structure of Human Cyclophilin A in Complex with the Novel Immunosuppressant Sanglifehrin A at 1.6 Å Resolution

The macrolide everolimus forms an unusual metabolite in animals and humans: identification of a phosphocholine ester

Small-molecule factor B inhibitor for the treatment of complement-mediated diseases

Discovery of 4-((2 S ,4 S )-4-Ethoxy-1-((5-methoxy-7-methyl-1 H -indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases

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

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

Structure–Activity Relationship and Pharmacokinetic Studies of Sotrastaurin (AEB071), a Promising Novel Medicine for Prevention of Graft Rejection and Treatment of Psoriasis

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

A Novel Class of Oral Direct Renin Inhibitors: Highly Potent 3,5-Disubstituted Piperidines Bearing a Tricyclic P 3 – P 1 Pharmacophore

SDZ RAD, a new rapamycin derivative: pharmacological properties in vitro and in vivo

A Novel Class of Oral Direct Renin Inhibitors: Highly Potent 3,5-Disubstituted Piperidines Bearing a Tricyclic P3 –P1 Pharmacophore

Sanglifehrin−Cyclophilin Interaction: Degradation Work, Synthetic Macrocyclic Analogues, X-ray Crystal Structure, and Binding Data

A convergent, highly stereoselective synthesis of a C-11-C-21 subunit of the macbecins

SDZ RAD, a new rapamycin derivative: synergism with cyclosporine

Erratum to “Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes” [Bioorg. Med. Chem. Lett. 22 (2012) 1464–1468]

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