Peter Blomgren
Hoffmann-La Roche
7 Papers
192 Citations
Peter Blomgren is an academic researcher from Hoffmann-La Roche. The author has contributed to research in topics: Bruton's tyrosine kinase & Receptor tyrosine kinase. The author has an hindex of 6, co-authored 7 publications.
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Papers
Design, synthesis, and antiviral properties of 4′-substituted ribonucleosides as inhibitors of hepatitis C virus replication: The discovery of R1479
David Bernard Smith,Joseph Armstrong Martin,Joseph Armstrong Martin,Klaus Klumpp,Stewart J. Baker,Peter Blomgren,Rene Devos,Caroline Granycome,Caroline Granycome,Julie Hang,Hobbs Christopher John,W.R. Jiang,W.R. Jiang,Carl Laxton,Sophie Le Pogam,Vincent Leveque,Han Ma,Graham Maile,JH Merrett,Arkadius Pichota,Keshab Sarma,Mark D. Smith,Steven Swallow,Julian Symons,David R. Vesey,I. Najera,I. Najera,Nick Cammack +27 more
TL;DR: A series of 4'-substituted ribonucleoside derivatives has been prepared and evaluated for inhibition of hepatitis C virus RNA replication in cell culture and the most potent and non-cytotoxic derivative was compound 28 (4'-azidocytidine, R1479).
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Potent and selective Bruton's tyrosine kinase inhibitors: Discovery of GDC-0834.
Wendy B. Young,James Barbosa,Peter Blomgren,Meire Bremer,James J. Crawford,Donna Dambach,Steve Gallion,Sarah G. Hymowitz,Kropf Jeffrey E,Seung H. Lee,Lichuan Liu,Joseph W. Lubach,Jen Macaluso,Pat Maciejewski,Brigitte Maurer,Scott A. Mitchell,Daniel F. Ortwine,Julie Di Paolo,Karin Reif,Heleen Scheerens,Aaron C. Schmitt,C. Gregory Sowell,Xiaojing Wang,Harvey Wong,Jin-Ming Xiong,Jianjun Xu,Zhongdong Zhao,Kevin S. Currie +27 more
TL;DR: In human, 2 was found to be highly labile at the exo-cyclic amide bond that links the tetrahydrobenzothiophene moiety to the central aniline ring, resulting in insufficient parent drug exposure, which informed the back-up program and discovery of improved inhibitors.
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Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.
Scott A. Mitchell,Mihaela Diana Danca,Peter Blomgren,James W. Darrow,Kevin S. Currie,Kropf Jeffrey E,Seung H. Lee,Steven L. Gallion,Jin-Ming Xiong,Douglas A. Pippin,Robert Desimone,David R. Brittelli,David C. Eustice,Aaron Bourret,Melissa Hill-Drzewi,Patricia Maciejewski,Lisa Elkin +16 more
TL;DR: A novel series of imidazo[1,2-a]pyrazine diarylureas that show nanomolar potency for the EphB4 receptor, in addition to potent activity against several other RTKs are reported.
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Discovery of Potent and Selective Tricyclic Inhibitors of Bruton’s Tyrosine Kinase with Improved Druglike Properties
Xiaojing Wang,James Barbosa,Peter Blomgren,Meire Bremer,Jacob Z. Chen,James J. Crawford,Wei Deng,Liming Dong,Charles Eigenbrot,Steve Gallion,Jonathon Hau,Huiyong Hu,Adam R. Johnson,Arna Katewa,Kropf Jeffrey E,Seung H. Lee,Lichuan Liu,Joseph W. Lubach,Jen Macaluso,Pat Maciejewski,Scott A. Mitchell,Daniel F. Ortwine,Julie DiPaolo,Karin Reif,Heleen Scheerens,Aaron C. Schmitt,Harvey Wong,Jin-Ming Xiong,Jianjun Xu,Zhongdong Zhao,Fusheng Zhou,Kevin S. Currie,Wendy B. Young +32 more
TL;DR: A series of novel tricyclic compounds that improved upon the druglike properties of previous chemical matter are devised that are highly potent, selective for Btk, metabolically stable, well tolerated, and efficacious in an animal model of arthritis.
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FRI0049 Preclinical Characterization of GS-9876, A Novel, Oral SYK Inhibitor That Shows Efficacy in Multiple Established Rat Models of Collagen-Induced Arthritis
J. A. Di Paolo,Peter Blomgren,Michael J. Dolton,Randall Mark Jones,Kropf Jeffrey E,Tony Lee,Scott A. Mitchell,Bernard P. Murray,K. Suekawa-Pirrone,Sarah Wise,Jianjun Xu,Zhongdong Zhao,Kevin S. Currie +12 more
TL;DR: GS-9876 is a novel SYK inhibitor that potently inhibits multiple cellular events implicated in RA pathogenesis and displays excellent in vivo efficacy in rat CIA models after once-daily dosing and markedly improved selectivity over competitor SYK programs.
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