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Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases

Journal of medicinal chemistry, 2019-09, Vol.62 (17), p.7643-7655

2019

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Enantioselective Addition of Amines to Ketenes Catalyzed by a Planar-Chiral Derivative of PPY: Possible Intervention of Chiral Brønsted-Acid Catalysis

Journal of the American Chemical Society, 2002-08, Vol.124 (34), p.10006-10007

2002

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Synthesis of 4-Substituted Chlorophthalazines, Dihydrobenzoazepinediones, 2-Pyrazolylbenzoic Acid, and 2-Pyrazolylbenzohydrazide via 3-Substituted 3-Hydroxyisoindolin-1-ones

Journal of organic chemistry, 2012-04, Vol.77 (8), p.3887-3906

2012

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A precision therapy against cancers driven by KIT/PDGFRA mutations

Science translational medicine, 2017-11, Vol.9 (414)

2017

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Targeting kinases with precision

Molecular & cellular oncology, 2018-05, Vol.5 (3), p.e1435183-e1435183

2018

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Evolution of a Highly Selective and Potent 2-(Pyridin-2-yl)-1,3,5-triazine Tie-2 Kinase Inhibitor

Journal of medicinal chemistry, 2007-02, Vol.50 (4), p.611-626

2007

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Enantioselective Addition of Alcohols to Ketenes Catalyzed by a Planar-Chiral Azaferrocene: Catalytic Asymmetric Synthesis of Arylpropionic Acids

Journal of the American Chemical Society, 1999-03, Vol.121 (11), p.2637-2638

1999

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Preclinical Evaluation of AMG 900, a Novel Potent and Highly Selective Pan-Aurora Kinase Inhibitor with Activity in Taxane-Resistant Tumor Cell Lines

Cancer research (Chicago, Ill.), 2010-12, Vol.70 (23), p.9846-9854

2010

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Catalytic Asymmetric Staudinger Reactions to Form β-Lactams: An Unanticipated Dependence of Diastereoselectivity on the Choice of the Nitrogen Substituent

Journal of the American Chemical Society, 2005-08, Vol.127 (33), p.11586-11587

2005

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Enantioselective Staudinger Synthesis of β-Lactams Catalyzed by a Planar-Chiral Nucleophile

Journal of the American Chemical Society, 2002-02, Vol.124 (8), p.1578-1579

2002

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Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors

Bioorganic & medicinal chemistry letters, 2007-05, Vol.17 (10), p.2886-2889

2007

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Discovery of a Potent, Selective, and Orally Bioavailable Pyridinyl-Pyrimidine Phthalazine Aurora Kinase Inhibitor

Journal of medicinal chemistry, 2010-09, Vol.53 (17), p.6368-6377

2010

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Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase

Bioorganic & medicinal chemistry letters, 2009-01, Vol.19 (2), p.424-427

2009

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Alkynylpyrimidine Amide Derivatives as Potent, Selective, and Orally Active Inhibitors of Tie-2 Kinase

Journal of medicinal chemistry, 2007-02, Vol.50 (4), p.627-640

2007

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N-(3-(Phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: Structure, synthesis and SAR

Bioorganic & medicinal chemistry, 2008-02, Vol.18 (3), p.1172-1176

2008

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Abstract A112: Drug discovery efforts on the RNA protein methyltransferase METTL3/METTL14

Molecular cancer therapeutics, 2019-12, Vol.18 (12_Supplement), p.A112-A112

2019

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Abstract 791: BLU-285, the first selective inhibitor of PDGFRα D842V and KIT Exon 17 mutants

Cancer research (Chicago, Ill.), 2015-08, Vol.75 (15_Supplement), p.791-791

2015

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First Selective KIT D816V Inhibitor for Patients with Systemic Mastocytosis

Blood, 2014-12, Vol.124 (21), p.3217-3217

2014

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Discovery of Aminoquinazolines as Potent, Orally Bioavailable Inhibitors of Lck: Synthesis, SAR, and in Vivo Anti-Inflammatory Activity

Journal of medicinal chemistry, 2006-09, Vol.49 (19), p.5671-5686

2006

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Abstract 5776: Discovery of AMG 900, a highly selective, orally bioavailable inhibitor of aurora kinases with efficacy in preclinical antitumor models and activity against multidrug-resistant cells

Cancer research (Chicago, Ill.), 2010-04, Vol.70 (8_Supplement), p.5776-5776

2010

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Enantioselective staudinger synthesis of β-lactams catalyzed by a planar-chiral nucleophile1

Journal of the American Chemical Society, 2002, Vol.124 (8), p.1578-1579

2002

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Enantioselective Addition of Amines to Ketenes Catalyzed by a Planar-Chiral Derivative of PPY: Possible Intervention of Chiral Broensted-Acid Catalysis

ChemInform, 2003-02, Vol.34 (5), p.no-no

2003

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ChemInform Abstract: Enantioselective Staudinger Synthesis of β-Lactams Catalyzed by a Planar-Chiral Nucleophile

ChemInform, 2002-07, Vol.33 (28), p.no-no

2002

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Catalytic Asymmetric Staudinger Reactions to Form β-Lactams: An Unanticipated Dependence of Diastereoselectivity on the Choice of the Nitrogen Substituent

ChemInform, 2005-12, Vol.36 (51), p.no-no

2005

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Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases

Enantioselective Addition of Amines to Ketenes Catalyzed by a Planar-Chiral Derivative of PPY: Possible Intervention of Chiral Brønsted-Acid Catalysis

Synthesis of 4-Substituted Chlorophthalazines, Dihydrobenzoazepinediones, 2-Pyrazolylbenzoic Acid, and 2-Pyrazolylbenzohydrazide via 3-Substituted 3-Hydroxyisoindolin-1-ones

A precision therapy against cancers driven by KIT/PDGFRA mutations

Targeting kinases with precision

Evolution of a Highly Selective and Potent 2-(Pyridin-2-yl)-1,3,5-triazine Tie-2 Kinase Inhibitor

Enantioselective Addition of Alcohols to Ketenes Catalyzed by a Planar-Chiral Azaferrocene: Catalytic Asymmetric Synthesis of Arylpropionic Acids

Preclinical Evaluation of AMG 900, a Novel Potent and Highly Selective Pan-Aurora Kinase Inhibitor with Activity in Taxane-Resistant Tumor Cell Lines

Catalytic Asymmetric Staudinger Reactions to Form β-Lactams: An Unanticipated Dependence of Diastereoselectivity on the Choice of the Nitrogen Substituent

Enantioselective Staudinger Synthesis of β-Lactams Catalyzed by a Planar-Chiral Nucleophile

Discovery of N‑(4-(3-(2-Aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), A Highly Selective, Orally Bioavailable Inhibitor of Aurora Kinases with Activity against Multidrug-Resistant Cancer Cell Lines

Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors

Discovery of a Potent, Selective, and Orally Bioavailable Pyridinyl-Pyrimidine Phthalazine Aurora Kinase Inhibitor

Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase

Alkynylpyrimidine Amide Derivatives as Potent, Selective, and Orally Active Inhibitors of Tie-2 Kinase

N-(3-(Phenylcarbamoyl)arylpyrimidine)-5-carboxamides as potent and selective inhibitors of Lck: Structure, synthesis and SAR

Abstract A112: Drug discovery efforts on the RNA protein methyltransferase METTL3/METTL14

Abstract 791: BLU-285, the first selective inhibitor of PDGFRα D842V and KIT Exon 17 mutants

First Selective KIT D816V Inhibitor for Patients with Systemic Mastocytosis

Discovery of Aminoquinazolines as Potent, Orally Bioavailable Inhibitors of Lck: Synthesis, SAR, and in Vivo Anti-Inflammatory Activity

Abstract 5776: Discovery of AMG 900, a highly selective, orally bioavailable inhibitor of aurora kinases with efficacy in preclinical antitumor models and activity against multidrug-resistant cells

Enantioselective staudinger synthesis of β-lactams catalyzed by a planar-chiral nucleophile1

Enantioselective Addition of Amines to Ketenes Catalyzed by a Planar-Chiral Derivative of PPY: Possible Intervention of Chiral Broensted-Acid Catalysis

ChemInform Abstract: Enantioselective Staudinger Synthesis of β-Lactams Catalyzed by a Planar-Chiral Nucleophile

Catalytic Asymmetric Staudinger Reactions to Form β-Lactams: An Unanticipated Dependence of Diastereoselectivity on the Choice of the Nitrogen Substituent

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