C
Celia D’Arienzo
Researcher at Bristol-Myers Squibb
Publications - 61
Citations - 2246
Celia D’Arienzo is an academic researcher from Bristol-Myers Squibb. The author has contributed to research in topics: In vivo & Prodrug. The author has an hindex of 26, co-authored 60 publications receiving 1822 citations.
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Journal ArticleDOI
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
Stephen T. Wrobleski,Moslin Ryan M,Shuqun Lin,Yanlei Zhang,Steven H. Spergel,James Kempson,Tokarski John S,Joann Strnad,Adriana Zupa-Fernandez,Lihong Cheng,David J. Shuster,Kathleen M. Gillooly,Xiaoxia Yang,Elizabeth M. Heimrich,Kim W. McIntyre,Charu Chaudhry,Javed Khan,Max Ruzanov,Jeffrey Tredup,Dawn Mulligan,Dianlin Xie,Huadong Sun,Christine Huang,Celia D’Arienzo,Nelly Aranibar,Manoj Chiney,Anjaneya Chimalakonda,William J. Pitts,Louis J. Lombardo,Percy H. Carter,James R. Burke,David S. Weinstein +31 more
TL;DR: The late stage optimization efforts including a structure-guided design and water displacement strategy that led to the discovery of BMS-986165 as a high affinity JH2 ligand and potent allosteric inhibitor of TYK2 are reported.
Journal ArticleDOI
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Rajeev S. Bhide,Zhen-Wei Cai,Yong-Zheng Zhang,Ligang Qian,Donna D. Wei,Stephanie Barbosa,Louis J. Lombardo,Robert M. Borzilleri,Xiaoping Zheng,Laurence I. Wu,Joel C. Barrish,Soong-Hoon Kim,Kenneth J. Leavitt,Arvind Mathur,Leslie Leith,Sam T. Chao,Barri Wautlet,Steven Mortillo,Robert Jeyaseelan,Daniel W. Kukral,John T. Hunt,Amrita Kamath,Aberra Fura,Viral Vyas,Punit Marathe,Celia D’Arienzo,George M. Derbin,Joseph Fargnoli +27 more
TL;DR: A series of substituted 4-(4-fluoro-1H-indol-5-yloxy)pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of vascular endothelial growth factor receptor-2 kinase is reported.
Journal ArticleDOI
Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215).
Zhen-Wei Cai,Yong-Zheng Zhang,Robert M. Borzilleri,Ligang Qian,Stephanie Barbosa,Donna D. Wei,Xiaoping Zheng,Lawrence Wu,Junying Fan,Zhongping Shi,Barri Wautlet,Steve Mortillo,Robert Jeyaseelan,Daniel W. Kukral,Amrita Kamath,Punit Marathe,Celia D’Arienzo,George M. Derbin,Joel C. Barrish,Jeffrey A. Robl,John T. Hunt,Louis J. Lombardo,Joseph Fargnoli,Rajeev S. Bhide +23 more
TL;DR: A series of amino acid ester prodrugs of the dual VEGFR-2/FGFR-1 kinase inhibitor 1 was prepared in an effort to improve the aqueous solubility and oral bioavailability of the parent compound.
Journal ArticleDOI
Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities.
Kyoung S. Kim,Liping Zhang,Robert J. Schmidt,Zhen-Wei Cai,Donna D. Wei,David K. Williams,Louis J. Lombardo,George L. Trainor,Dianlin Xie,Yaquan Zhang,Yongmi An,John S. Sack,John S. Tokarski,Celia D’Arienzo,Amrita Kamath,Punit Marathe,Yueping Zhang,Jonathan Lippy,Robert Jeyaseelan,Barri Wautlet,Benjamin J. Henley,Johnni Gullo-Brown,Veeraswamy Manne,John T. Hunt,Joseph Fargnoli,Robert M. Borzilleri +25 more
TL;DR: Conformationally constrained 2-pyridone analogue 2 is a potent Met kinase inhibitor that possesses a favorable pharmacokinetic profile in mice and demonstrates significant in vivo antitumor activity in the GTL-16 human gastric carcinoma xenograft model.
Journal ArticleDOI
Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain.
James R. Burke,Lihong Cheng,Kathleen M. Gillooly,Joann Strnad,Adriana Zupa-Fernandez,Ian M. Catlett,Yifan Zhang,Elizabeth M. Heimrich,Kim W. McIntyre,Mark D. Cunningham,Julie Carman,Xiadi Zhou,Dana Banas,Charu Chaudhry,Sha Li,Celia D’Arienzo,Anjaneya Chimalakonda,Xiaoxia Yang,Jenny Xie,Jian Pang,Qihong Zhao,Shawn M. Rose,Jinwen Huang,Moslin Ryan M,Stephen T. Wrobleski,David S. Weinstein,Luisa Salter-Cid +26 more
TL;DR: BMS-986165 is a potent oral agent that similarly blocks receptor-stimulated activation of TYK2 allosterically and with high selectivity and potency afforded through optimized binding to a regulatory domain of the protein.