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Proteolysis targeting chimeras (PROTACs) in ‘beyond rule-of-five’ chemical space: Recent progress and future challenges

Bioorganic & medicinal chemistry letters, 2019-07, Vol.29 (13), p.1555-1564

2019

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Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279

Journal of medicinal chemistry, 2023-08, Vol.66 (15), p.10473-10496

2023

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Discovery of the First Clinical Protein Degrader for the Treatment of Autoimmune Indications: Orally Bioavailable and Selective IRAK4 Degrader KT-474

Journal of medicinal chemistry, 2024-10, Vol.67 (20), p.18017-18021

Edmondson, Scott D.

2024

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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}- N -methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs

Journal of medicinal chemistry, 2021-10, Vol.64 (19), p.14498-14512

2021

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Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase

Journal of medicinal chemistry, 2020-09, Vol.63 (18), p.10460-10473

2020

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Design, Synthesis, and Evaluation of Conformationally Restricted Acetanilides as Potent and Selective β3 Adrenergic Receptor Agonists for the Treatment of Overactive Bladder

Journal of medicinal chemistry, 2014-02, Vol.57 (4), p.1437-1453

2014

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Crystal Structure of Human Phosphodiesterase 3B: Atomic Basis for Substrate and Inhibitor Specificity

Biochemistry (Easton), 2004-05, Vol.43 (20), p.6091-6100

2004

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Novel potent and selective pyrazolylpyrimidine-based SYK inhibitors

Bioorganic & medicinal chemistry letters, 2020-11, Vol.30 (22), p.127523-127523, Article 127523

2020

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Potent and selective TYK2-JH1 inhibitors highly efficacious in rodent model of psoriasis

Bioorganic & medicinal chemistry letters, 2022-10, Vol.73, p.128891-128891, Article 128891

2022

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Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors

Bioorganic & medicinal chemistry letters, 2023-07, Vol.91, p.129352-129352, Article 129352

2023

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Identification of a novel series of azabenzimidazole-derived inhibitors of spleen tyrosine kinase

Bioorganic & medicinal chemistry letters, 2020-09, Vol.30 (18), p.127393-127393, Article 127393

2020

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Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants

Bioorganic & medicinal chemistry letters, 2020-08, Vol.30 (16), p.127072-127072, Article 127072

2020

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Optimization of a series of potent, selective and orally bioavailable SYK inhibitors

Bioorganic & medicinal chemistry letters, 2020-10, Vol.30 (19), p.127433, Article 127433

2020

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Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors

Bioorganic & medicinal chemistry letters, 2006-10, Vol.16 (20), p.5373-5377

2006

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Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with in Vivo Activity in Rodents

ACS medicinal chemistry letters, 2017-01, Vol.8 (1), p.96-101

2017

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Discovery of phenyl acetamides as potent and selective GPR119 agonists

Bioorganic & medicinal chemistry letters, 2017-03, Vol.27 (5), p.1124-1128

2017

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Investigation of piperazine benzamides as human β3 adrenergic receptor agonists for the treatment of overactive bladder

Bioorganic & medicinal chemistry letters, 2017-02, Vol.27 (4), p.1094-1098

2017

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Discovery of benzamides as potent human β3 adrenergic receptor agonists

Bioorganic & medicinal chemistry letters, 2016-01, Vol.26 (1), p.55-59

2016

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Investigation of piperazine benzamides as human β 3 adrenergic receptor agonists for the treatment of overactive bladder

Bioorganic & medicinal chemistry letters, 2017-02, Vol.27 (4), p.1094-1098

2017

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Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors

Bioorganic & medicinal chemistry, 2008-04, Vol.18 (7), p.2409-2413

2008

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Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes

ACS medicinal chemistry letters, 2016-12, Vol.7 (12), p.1107-1111

2016

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Palladium-Catalyzed Coupling of Vinylogous Amides with Aryl Halides: Applications to the Synthesis of Heterocycles

Organic letters, 2000-04, Vol.2 (8), p.1109-1112

2000

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Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes

ACS medicinal chemistry letters, 2015-08, Vol.6 (8), p.936-941

2015

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Proteolysis targeting chimeras (PROTACs) in ‘beyond rule-of-five’ chemical space: Recent progress and future challenges

Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279

Discovery of the First Clinical Protein Degrader for the Treatment of Autoimmune Indications: Orally Bioavailable and Selective IRAK4 Degrader KT-474

Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}- N -methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs

Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase

Design, Synthesis, and Evaluation of Conformationally Restricted Acetanilides as Potent and Selective β3 Adrenergic Receptor Agonists for the Treatment of Overactive Bladder

Crystal Structure of Human Phosphodiesterase 3B: Atomic Basis for Substrate and Inhibitor Specificity

Novel potent and selective pyrazolylpyrimidine-based SYK inhibitors

Potent and selective TYK2-JH1 inhibitors highly efficacious in rodent model of psoriasis

Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors

Identification of a novel series of azabenzimidazole-derived inhibitors of spleen tyrosine kinase

Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants

Optimization of a series of potent, selective and orally bioavailable SYK inhibitors

Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder

Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors

Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with in Vivo Activity in Rodents

Discovery of phenyl acetamides as potent and selective GPR119 agonists

Investigation of piperazine benzamides as human β3 adrenergic receptor agonists for the treatment of overactive bladder

Discovery of benzamides as potent human β3 adrenergic receptor agonists

Investigation of piperazine benzamides as human β 3 adrenergic receptor agonists for the treatment of overactive bladder

Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors

(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]- pyridin-6-ylphenyl)butanamide: A Selective α-Amino Amide Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes

Palladium-Catalyzed Coupling of Vinylogous Amides with Aryl Halides: Applications to the Synthesis of Heterocycles

Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes

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