D
Derek J. Norris
Researcher at Bristol-Myers Squibb
Publications - 63
Citations - 4895
Derek J. Norris is an academic researcher from Bristol-Myers Squibb. The author has contributed to research in topics: Cancer & Tricyclic. The author has an hindex of 23, co-authored 62 publications receiving 4667 citations.
Papers
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Journal ArticleDOI
Overriding Imatinib Resistance with a Novel ABL Kinase Inhibitor
TL;DR: BMS-354825 is an orally bioavailable ABL kinase inhibitor with two-log increased potency relative to imatinib that retains activity against 14 of 15 imatinIB-resistant BCR-ABL mutants and illustrates how molecular insight into kinase inhibitors resistance can guide the design of second-generation targeted therapies.
Journal ArticleDOI
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
Louis J. Lombardo,Francis Y. Lee,Ping Chen,Derek J. Norris,Joel C. Barrish,Kamelia Behnia,Stephen Castaneda,Cornelius Lyndon A M,Jagabandhu Das,Arthur M. Doweyko,Craig Fairchild,John T. Hunt,Ivan Inigo,Kathy A. Johnston,Amrita Kamath,David Kan,Herbert E. Klei,Punit Marathe,Suhong Pang,Russell Peterson,Sidney Pitt,Gary L. Schieven,Robert J. Schmidt,John S. Tokarski,Mei-Li Wen,John Wityak,Robert M. Borzilleri +26 more
TL;DR: Compound 13 was orally active in a K562 xenograft model of chronic myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels.
Journal ArticleDOI
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.
Jagabandhu Das,Ping Chen,Derek J. Norris,Ramesh Padmanabha,James Lin,Robert V. Moquin,Zhongqi Shen,Lynda S. Cook,Arthur M. Doweyko,Sidney Pitt,Suhong Pang,Ding Ren Shen,Qiong Fang,Henry F. De Fex,Kim W. McIntyre,David J. Shuster,Kathleen M. Gillooly,Kamelia Behnia,Gary L. Schieven,John Wityak,Joel C. Barrish +20 more
TL;DR: Molecular modeling was used to construct a putative binding model for Lck inhibition by Dasatinib and 12m, and the framework of key hydrogen-bond interactions proposed was in agreement with the subsequent, published crystal structure of 2 bound to structurally similar Abl kinase.
Patent
Cyclic protein tyrosine kinase inhibitors
Jagabandhu Das,Ramesh Padmanabha,Ping Chen,Derek J. Norris,Arthur M. Doweyko,Joel C. Barrish,John Wityak +6 more
TL;DR: In this paper, novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
Patent
Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
Bang-Chi Chen,Ping Chen,John Hynes,Peter A. Kiener,Katerina Leftheris,Malinda Longphre,Derek J. Norris,Chennagiri R. Pandit,Steven H. Spergel,John S. Tokarski,Stephen T. Wrobleski,Hong Wu,Rulin Zhao +12 more
TL;DR: In this paper, the use of a compound for treating a respiratory disease in a mammal wherein the compound is a cannabinoid receptor modulator is disclosed, and compounds useful as CBR modulators for treating respiratory and non-respiratory leukocyte activation associated diseases comprise compounds of formula (I), in which A and B are nitrogen or carbon, provided only one of a and B is nitrogen; and R1-R6 are as defined in the specification, wherein R2 with R5 may form a ring, and/or two R4 groups may form six-membered a