M
Matthew Weiss
Researcher at Amgen
Publications - 48
Citations - 964
Matthew Weiss is an academic researcher from Amgen. The author has contributed to research in topics: Sulfonamide & Amyloid precursor protein. The author has an hindex of 20, co-authored 48 publications receiving 874 citations.
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Journal ArticleDOI
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.
Jean-Christophe Harmange,Matthew Weiss,Julie Germain,Anthony Polverino,George Borg,James Bready,Danlin Chen,Deborah Choquette,Angela Coxon,Tom DeMelfi,Lucian DiPietro,Nicholas Doerr,Juan Estrada,Julie Flynn,Russell Graceffa,Shawn Harriman,Stephen Kaufman,Daniel S. La,Alexander M. Long,Matthew W. Martin,Sesha Neervannan,Vinod F. Patel,Michele Potashman,Kelly Regal,Philip Roveto,Michael Schrag,Charlie Starnes,Andrew Tasker,Yohannes Teffera,Ling Wang,Ryan White,Douglas A. Whittington,Roger Zanon +32 more
TL;DR: A series of naphthyl-based compounds were synthesized as potential inhibitors of vascular endothelial growth factor (VEGF) receptors and demonstrated significant antitumor efficacy against established HT29 human colon adenocarcinoma xenografts implanted in athymic mice.
Journal ArticleDOI
Novel 2,3-dihydro-1,4-benzoxazines as potent and orally bioavailable inhibitors of tumor-driven angiogenesis.
Daniel S. La,Julie Belzile,James Bready,Angela Coxon,Thomas DeMelfi,Nicholas Doerr,Juan Estrada,Julie Flynn,Shaun Flynn,Russell Graceffa,Shawn Harriman,Jay Larrow,Alexander M. Long,Matthew W. Martin,Michael Morrison,Vinod F. Patel,Philip Roveto,Ling Wang,Matthew Weiss,Douglas A. Whittington,Yohannes Teffera,Zhiyang Zhao,Anthony Polverino,Jean-Christophe Harmange +23 more
TL;DR: 2,3-dihydro-1,4-benzoxazine moiety is reported as a promising platform for generating kinase-based antiangiogenic therapeutic agents and was identified as a potent and selective inhibitor that exhibited efficacy in angiogenic in vivo models.
Journal ArticleDOI
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors.
Matthew Weiss,Jean-Christophe Harmange,Anthony Polverino,David Bauer,Loren Berry,Virginia Berry,George Borg,James Bready,Danlin Chen,Deborah Choquette,Angela Coxon,Tom DeMelfi,Nicholas Doerr,Juan Estrada,Julie Flynn,Russell Graceffa,Shawn Harriman,Stephen Kaufman,Daniel S. La,Alexander M. Long,Sesha Neervannan,Vinod F. Patel,Michele Potashman,Kelly Regal,Philip Roveto,Michael Schrag,Charlie Starnes,Andrew Tasker,Yohannes Teffera,Douglas A. Whittington,Roger Zanon +30 more
TL;DR: Naphthamides 3, 20, and 22 exhibited good pharmacokinetics following oral dosing and showed potent inhibition of VEGF-induced angiogenesis in the rat corneal model, and the inhibitory activity of this series was retained at the cellular level.
Journal ArticleDOI
Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid.
Matthew Weiss,Toni Williamson,Safura Babu-Khan,Michael D. Bartberger,James Brown,Kui Chen,Yuan Cheng,Martin Citron,Michael Croghan,Thomas Dineen,Joel Esmay,Russell Graceffa,Scott Harried,Dean Hickman,Stephen Hitchcock,Daniel B. Horne,Hongbing Huang,Ronke Imbeah-Ampiah,Ted Judd,Matthew R. Kaller,Charles Kreiman,Daniel S. La,Vivian S. W. Li,Patricia Lopez,Steven W. Louie,Holger Monenschein,Thomas T. Nguyen,Lewis D. Pennington,Claire Rattan,Tisha San Miguel,E. Allen Sickmier,Robert C. Wahl,Paul H. Wen,Stephen J. Wood,Qiufen Xue,Bryant Yang,Vinod F. Patel,Wenge Zhong +37 more
TL;DR: This work identified a series of benzodioxolane analogues that possessed improved metabolic stability and increased oral bioavailability and identified an inhibitor which demonstrated robust and sustained reduction of CNS β-amyloid (Aβ) in Sprague-Dawley rats following oral administration.
Journal ArticleDOI
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity.
Russell Graceffa,Alessandro Boezio,Jessica Able,Steven Altmann,Loren Berry,Christiane Boezio,John Butler,Margaret Y. Chu-Moyer,Melanie Cooke,Erin F. DiMauro,Thomas Dineen,Elma Feric Bojic,Robert S. Foti,Robert T. Fremeau,Angel Guzman-Perez,Hua Gao,Hakan Gunaydin,Hongbing Huang,Liyue Huang,Christopher P Ilch,Michael Jarosh,Thomas Kornecook,Charles Kreiman,Daniel S. La,Joseph Ligutti,Benjamin C. Milgram,Min-Hwa Jasmine Lin,Isaac E. Marx,Hanh Nho Nguyen,Emily A. Peterson,Gwen Rescourio,John D. Roberts,Laurie B. Schenkel,Roman Shimanovich,Brian A. Sparling,John Stellwagen,Kristin Taborn,Karina R. Vaida,Jean Wang,John Yeoman,Violeta Yu,Dawn Zhu,Bryan D. Moyer,Matthew Weiss +43 more
TL;DR: A series of atropisomeric quinolinone sulfonamide compounds as sodium channel inhibitors and their preparation are reported, which demonstrate nanomolar inhibition of NaV1.7 and exhibit high levels of selectivity over other sodium channel isoforms.