- A radiobrominated tyrosine kinase inhibitor for egfr with l858r/t790m mutations in lung carcinoma
-
Activating double mutations L858R/T790M in the epidermal growth factor receptor (EGFR) region are often observed as the cause of resistance to tyrosine kinase inhibitors (TKIs). Third‐generation EGFR‐TKIs, such as osimertinib and rociletinib (CO‐1686), wa
- Fawwaz, Muammar,Mishiro, Kenji,Nishii, Ryuichi,Makino, Akira,Kiyono, Yasushi,Shiba, Kazuhiro,Kinuya, Seigo,Ogawa, Kazuma
-
-
- Elastic orange emissive single crystals of 1,3-diamino-2,4,5,6-tetrabromobenzene as flexible optical waveguides
-
Single crystals of monoaromatic compounds exhibiting both mechanical softness and optical properties have attracted significant scientific interest in recent years, but they are very scarce. Herein, single crystals of 1,3-diamino-2,4,5,6-tetrabromobenzene
- Bhaktha B. N., Shivakiran,Biradha, Kumar,Choubey, Priyanka S.,Das, Susobhan,Gude, Venkatesh,Reddy, C. Malla
-
p. 9465 - 9472
(2021/08/10)
-
- COMPOSITIONS FOR THE TREATMENT OF PULMONARY FIBROSIS
-
The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.
- -
-
Paragraph 00125-00126
(2018/02/28)
-
- A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFRL858R/T790Mmutant with improved pharmacokinetic properties
-
Structural optimization of pyrido[2,3-d]pyrimidin-7-ones was conducted to yield a series of new selective EGFRT790Minhibitors with improved pharmacokinetic properties. One of the most promising compound 9s potently suppressed EGFRL858R/T790Mkinase and inhibited the proliferation of H1975?cells with IC50values of 2.0?nM and 40?nM, respectively. The compound dose-dependently induced reduction of the phosphorylation of EGFR and downstream activation of ERK in NCI[sbnd]H1975?cells. It also exhibited moderate plasma exposure after oral administration and an oral bioavailability value of 16%. Compound 9s may serve as a promising lead compound for further drug discovery overcoming the acquired resistance of non-small cell lung cancer (NSCLC) patients.
- Yu, Lei,Huang, Minhao,Xu, Tianfeng,Tong, Linjiang,Yan, Xiao-e,Zhang, Zhang,Xu, Yong,Yun, Caihong,Xie, Hua,Ding, Ke,Lu, Xiaoyun
-
supporting information
p. 1107 - 1117
(2016/12/30)
-
- Activated carbon as an efficient support for gold nanoparticles that catalyze the hydrogenation of nitro compounds with molecular hydrogen
-
A catalyst based on activated carbon with deposited gold nanoparticles and impregnated with ethylenediamine for selective hydrogenation of nitroarenes has been suggested.
- Bondarenko, Grigory N.,Beletskaya, Irina P.
-
p. 443 - 445
(2015/12/30)
-
- AMINOPYRIMIDINES AS SYK INHIBITORS
-
The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
- -
-
Page/Page column 259-260
(2011/07/07)
-
- Copper(I)-Induced Bromo-Hydrogen Exchange of 2,3-Dibromoanilines
-
The copper(I)-induced bromine-hydrogen exchange reaction of 2,3-dibromoaniline and 5-substituted 2,3-dibromoanilines in the 2-position has been kinetically studied in water-acetic acid-hydrochloric acid medium at 90 deg C.The dehalogenation reaction is of second order, first order in both substrate and Cu+, and may be interpreted as a reductive substitution, composed of two one-electron steps.The 2,3-dibromophenol was only qualitatively investigated, but gave similar results.
- Liedholm, Brita
-
p. 877 - 884
(2007/10/02)
-