T. D. Owens

发表

New Synthetic Technology for Efficient Construction of α-Hydroxy-β-amino Amides via the Passerini Reaction1

Andrew Nguyen, J. E. Semple, O. Levy, 2000 .

Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties.

D. Siev, J. E. Semple, N. K. Minami, 2000, Bioorganic & medicinal chemistry letters.

Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties.

R. Nutt, S. Tamura, A. Tulinsky, 1996, Journal of medicinal chemistry.

Covalent Kinase Inhibitors for Cancer

T. D. Owens, Yan Lou, 2017 .

Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis.

A. Kuglstatter, D. Davis, Jaehyeon Park, 2015, Journal of medicinal chemistry.

Targeting Interleukin-2-inducible T-cell Kinase (ITK) and Resting Lymphocyte Kinase (RLK) Using a Novel Covalent Inhibitor PRN694

J. M. Bradshaw, A. Johnson, P. Porcu, 2014, The Journal of Biological Chemistry.

Synthesis of Enantiomerically Pure N-tert-Butanesulfinyl Imines (tert-Butanesulfinimines) by the Direct Condensation of tert-Butanesulfinamide with Aldehydes and Ketones

J. Ellman, T. D. Owens, Guangcheng Liu, 1999 .

The preparation and utility of bis(sulfinyl)imidoamidine ligands for the copper-catalyzed Diels-Alder reaction.

A. Souers, J. Ellman, T. D. Owens, 2003, Journal of Organic Chemistry.

Co‐inhibition of immunoproteasome subunits LMP2 and LMP7 is required to block autoimmunity

J. M. Bradshaw, M. Lindstrom, M. Groettrup, 2018, EMBO reports.

Phase 1 clinical trial evaluating safety, exposure and pharmacodynamics of BTK inhibitor tolebrutinib (PRN2246, SAR442168)

A. Redfern, Patrick F. Smith, S. Gourlay, 2021, Clinical and translational science.

N-tert-butanesulfinyl imines: versatile intermediates for the asymmetric synthesis of amines.

J. Ellman, Jonathan A Ellman, Tony P Tang, 2002, Accounts of chemical research.

Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.

A. Kuglstatter, D. Davis, R. Kondru, 2015, Bioorganic & medicinal chemistry letters.

Mitigation of reactive metabolite formation for a series of 3-amino-2-pyridone inhibitors of Bruton's tyrosine kinase (BTK).

P. Wovkulich, P. Di Lello, D. Fry, 2017, Bioorganic & medicinal chemistry letters.

Concise total synthesis of the prolyl endopeptidase inhibitor eurystatin A via a novel Passerini reaction–deprotection–acyl migration strategy

R. Nutt, J. E. Semple, T. D. Owens, 2001 .

Synthesis, Utility, and Structure of Novel Bis(sulfinyl)imidoamidine Ligands for Asymmetric Lewis Acid Catalysis

A. Oliver, J. Ellman, F. Hollander, 2001 .

Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.

A. Kuglstatter, R. Kondru, D. Goldstein, 2012, Journal of medicinal chemistry.

Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: synthesis of potent, selective P3-lactam thrombin inhibitors containing P4-o-alkoxycarbonylbenzylsulfonamide residues.

J. E. Semple, T. D. Owens, 1998, Bioorganic & medicinal chemistry letters.

Discovery of Reversible Covalent Bruton's Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib).

J. M. Bradshaw, E. Verner, D. Goldstein, 2022, Journal of medicinal chemistry.

Preclinical Efficacy and Anti-Inflammatory Mechanisms of Action of the Bruton Tyrosine Kinase Inhibitor Rilzabrutinib for Immune-Mediated Disease

J. M. Bradshaw, D. Goldstein, C. Langrish, 2021, The Journal of Immunology.

Prolonged and tunable residence time using reversible covalent kinase inhibitors

J. M. Bradshaw, Jack Taunton, Sergei Romanov, 2015, Nature chemical biology.

Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.

J. M. Bradshaw, M. Gerritsen, E. Venetsanakos, 2017, Journal of medicinal chemistry.

A Small Molecule Inhibitor of ITK and RLK Impairs Th1 Differentiation and Prevents Colitis Disease Progression

J. M. Bradshaw, J. Funk, L. Berg, 2015, The Journal of Immunology.

RN486, a Selective Bruton's Tyrosine Kinase Inhibitor, Abrogates Immune Hypersensitivity Responses and Arthritis in Rodents

Daigen Xu, J. Demartino, S. Narula, 2012, Journal of Pharmacology and Experimental Therapeutics.

Inhibiteurs de la tyrosine kinase

D. Goldstein, T. D. Owens, 2016 .

New Synthetic Technology for Efficient Construction of α‐Hydroxy‐β‐amino Amides via the Passerini Reaction.

J. E. Semple, O. Levy, T. D. Owens, 2001 .

The Irreversible Covalent Fibroblast Growth Factor Receptor Inhibitor PRN1371 Exhibits Sustained Inhibition of FGFR after Drug Clearance

J. M. Bradshaw, M. Gerritsen, E. Venetsanakos, 2017, Molecular Cancer Therapeutics.

JPET #187740 RN486 [6-Cyclopropyl-8-fluoro-2-(2-hydroxymethyl-3-{1-methyl-5-[5-(4-methyl- piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-pyridin-3-yl}-phenyl)-2H- isoquinolin-1-one], a Selective Bruton’s Tyrosine Kinase (Btk) Inhibitor, Abrogates Immune Hypersensitivity Responses and Arthritis

Daigen Xu, J. Demartino, S. Narula, 2011 .

Synthesis and crystal structure of a unique and homochiral N,S-bonded N,N'-bis(tert-butanesulfinyl)amidinate rhodium(I) complex.

A. Souers, A. Oliver, J. Ellman, 2001, Inorganic chemistry.

Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties.

R. Nutt, S. Tamura, A. Tulinsky, 1996, Journal of medicinal chemistry.

A Small Molecule Inhibitor of ITK and RLK Impairs Th1 Differentiation and Prevents Colitis Disease Progression

J. M. Bradshaw, J. Funk, L. Berg, 2015, Journal of Immunology.

Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.

Johannes C. Hermann, John Menke, A. Kuglstatter, 2013, Journal of medicinal chemistry.

RN486, a Selective Bruton's Tyrosine Kinase Inhibitor, Abrogates Immune Hypersensitivity Responses and Arthritis in Rodents

Daigen Xu, S. Narula, D. Srinivasan, 2012, Journal of Pharmacology and Experimental Therapeutics.

Ibrutinib, a Carboxylic Acid Amide Inhibitor of Bruton's Tyrosine Kinase

T. D. Owens, 2016 .

The Preparation and Utility of Bis(sulfinyl)imidoamidine Ligands for the Copper‐Catalyzed Diels—Alder Reaction.

A. Souers, J. Ellman, T. D. Owens, 2003 .