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Vimseltinib: A Precision CSF1R Therapy for Tenosynovial Giant Cell Tumors and Diseases Promoted by Macrophages

Molecular cancer therapeutics, 2021-11, Vol.20 (11), p.2098-2109

2021

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Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT)

Bioorganic & medicinal chemistry letters, 2022-10, Vol.74, p.128928-128928, Article 128928

2022

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Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors

Bioorganic & medicinal chemistry letters, 2022-10, Vol.74, p.128929-128929, Article 128929

2022

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Discovery of 1‑(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3‑d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a Pan-RAF Inhibitor with Minimal Paradoxical Activation and Activity against BRAF or RAS Mutant Tumor Cells

Journal of medicinal chemistry, 2015-05, Vol.58 (10), p.4165-4179

2015

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Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2

Molecular cancer therapeutics, 2015-09, Vol.14 (9), p.2023-2034

2015

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Single Integration Optimization of Linear Time-Varying Switched Systems

IEEE transactions on automatic control, 2012-06, Vol.57 (6), p.1592-1597

2012

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Volltext

Synthesis and Biochemical Evaluation of 3-Fluoromethyl-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Journal of medicinal chemistry, 1999-09, Vol.42 (18), p.3588-3601

1999

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Enantiospecific Synthesis of 3-Fluoromethyl-, 3-Hydroxymethyl-, and 3-Chloromethyl-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Journal of medicinal chemistry, 1999-10, Vol.42 (21), p.4351-4361

1999

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Synthesis and Evaluation of 4-Fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Journal of medicinal chemistry, 2001-08, Vol.44 (17), p.2849-2856

2001

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Synthesis and Evaluation of 3-Trifluoromethyl-7-substituted- 1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Journal of medicinal chemistry, 1999-08, Vol.42 (17), p.3315-3323

1999

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The Rational Synthesis of Chlorins via Rearrangement of Porphodimethenes: Influence of β-Substituents on the Regioselectivity and Stereoselectivity of Pyrroline Ring Formation

Journal of organic chemistry, 2002-06, Vol.67 (13), p.4536-4546

2002

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CRHR1 receptor binding and lipophilicity of pyrrolopyrimidines, potential nonpeptide corticotropin-releasing hormone type 1 receptor antagonists

Bioorganic & medicinal chemistry, 2002, Vol.10 (1), p.175-183

2002

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Abstract B129: Preclinical studies with DCC-3116, an ULK kinase inhibitor designed to inhibit autophagy as a potential strategy to address mutant RAS cancers

Molecular cancer therapeutics, 2019-12, Vol.18 (12_Supplement), p.B129-B129

2019

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Synthesis and Evaluation of 3-Trifluoromethyl-7-substituted-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Journal of medicinal chemistry, 2002-05, Vol.45 (11), p.2347-2347

2002

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Synthesis and Evaluation of 4-Fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Journal of medicinal chemistry, 2002-05, Vol.45 (11), p.2348-2348

2002

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Abstract 4033: Pan-exon mutant KIT inhibitor DCC-3009 demonstrates tumor regressions in preclinical gastrointestinal stromal tumor models

Cancer research (Chicago, Ill.), 2023-04, Vol.83 (7_Supplement), p.4033-4033

2023

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Synthesis and Biochemical Evaluation of 3-Fluoromethyl-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Journal of medicinal chemistry, 2002-05, Vol.45 (11), p.2347-2347

2002

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Examination of the Role of the Acidic Hydrogen in Imparting Selectivity of 7-(Aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) Toward Inhibition of Phenylethanolamine N-Methyltransferase vs the α2-Adrenoceptor1a

Journal of medicinal chemistry, 1997-12, Vol.40 (25), p.3997-4005

1997

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Fast Sample-Based Planning for Dynamic Systems by Zero-Control Linearization-Based Steering

Robotics Research, p.453-469

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Fast approximate path coordinate motion primitives for autonomous driving

2017 IEEE 56th Annual Conference on Decision and Control (CDC), 2017, p.837-842

2017

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Power Network Regulation Benchmark for Switched-Mode Optimal Control

IFAC-PapersOnLine, 2015, Vol.48 (27), p.280-285

2015

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Synthesis and Evaluation of 4-Fluoro-8-substituted-2,3,4,5-tetrahydro-1 H -2-benzazapines as Selective Inhibitors of Phenylethanolamine N -Methyltransferase versus the α 2 -Adrenoceptor

Journal of medicinal chemistry, 2002-05, Vol.45 (11), p.2348-2348

2002

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Synthesis and Evaluation of 3-Trifluoromethyl-7-substituted-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N -Methyltransferase versus the α 2 -Adrenoceptor

Journal of medicinal chemistry, 2002-05, Vol.45 (11), p.2347-2347

2002

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Synthesis and Evaluation of 4-Fluoro-8-substituted-2,3,4,5-tetrahydro-1 H -2-benzazapines as Selective Inhibitors of Phenylethanolamine N -Methyltransferase versus the α 2 -Adrenoceptor

Journal of medicinal chemistry, 2001-08, Vol.44 (17), p.2849-2856

2001

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Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants

Vimseltinib: A Precision CSF1R Therapy for Tenosynovial Giant Cell Tumors and Diseases Promoted by Macrophages

Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT)

Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors

Discovery of 1‑(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3‑d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a Pan-RAF Inhibitor with Minimal Paradoxical Activation and Activity against BRAF or RAS Mutant Tumor Cells

Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2

Single Integration Optimization of Linear Time-Varying Switched Systems

Synthesis and Biochemical Evaluation of 3-Fluoromethyl-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Enantiospecific Synthesis of 3-Fluoromethyl-, 3-Hydroxymethyl-, and 3-Chloromethyl-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Synthesis and Evaluation of 4-Fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Synthesis and Evaluation of 3-Trifluoromethyl-7-substituted- 1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

The Rational Synthesis of Chlorins via Rearrangement of Porphodimethenes: Influence of β-Substituents on the Regioselectivity and Stereoselectivity of Pyrroline Ring Formation

CRHR1 receptor binding and lipophilicity of pyrrolopyrimidines, potential nonpeptide corticotropin-releasing hormone type 1 receptor antagonists

Abstract B129: Preclinical studies with DCC-3116, an ULK kinase inhibitor designed to inhibit autophagy as a potential strategy to address mutant RAS cancers

Synthesis and Evaluation of 3-Trifluoromethyl-7-substituted-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Synthesis and Evaluation of 4-Fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Abstract 4033: Pan-exon mutant KIT inhibitor DCC-3009 demonstrates tumor regressions in preclinical gastrointestinal stromal tumor models

Synthesis and Biochemical Evaluation of 3-Fluoromethyl-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N-Methyltransferase versus the α2-Adrenoceptor

Examination of the Role of the Acidic Hydrogen in Imparting Selectivity of 7-(Aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) Toward Inhibition of Phenylethanolamine N-Methyltransferase vs the α2-Adrenoceptor1a

Fast Sample-Based Planning for Dynamic Systems by Zero-Control Linearization-Based Steering

Fast approximate path coordinate motion primitives for autonomous driving

Power Network Regulation Benchmark for Switched-Mode Optimal Control

Synthesis and Evaluation of 4-Fluoro-8-substituted-2,3,4,5-tetrahydro-1 H -2-benzazapines as Selective Inhibitors of Phenylethanolamine N -Methyltransferase versus the α 2 -Adrenoceptor

Synthesis and Evaluation of 3-Trifluoromethyl-7-substituted-1,2,3,4-tetrahydroisoquinolines as Selective Inhibitors of Phenylethanolamine N -Methyltransferase versus the α 2 -Adrenoceptor

Synthesis and Evaluation of 4-Fluoro-8-substituted-2,3,4,5-tetrahydro-1 H -2-benzazapines as Selective Inhibitors of Phenylethanolamine N -Methyltransferase versus the α 2 -Adrenoceptor

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