581076-63-3Relevant articles and documents
N-phenyl-2-pyrimidine-amine derivatives
-
, (2017/03/14)
The present invention relates to novel amides and a process for preparing these amides.
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors
Daydé-Cazals, Bénédicte,Fauvel, Bénédicte,Singer, Mathilde,Feneyrolles, Clémence,Bestgen, Benoit,Gassiot, Fanny,Spenlinhauer, Aurélia,Warnault, Pierre,Van Hijfte, Nathalie,Borjini, Nozha,Chevé, Gwéna?l,Yasri, Abdelaziz
, p. 3886 - 3905 (2016/05/24)
Efforts were made to improve a series of potent dual ABL/SRC inhibitors based on a 7-azaindole core with the aim of developing compounds that demonstrate a wider activity on selected oncogenic kinases. Multi-targeted kinase inhibitors (MTKIs) were then derived, focusing on kinases involved in both angiogenesis and tumorigenesis processes. Antiproliferative activity studies using different cellular models led to the discovery of a lead candidate (6z) that combined both antiangiogenic and antitumoral effects. The activity of 6z was assessed against a panel of kinases and cell lines including solid cancers and leukemia cell models to explore its potential therapeutic applications. With its potency and selectivity for oncogenic kinases, 6z was revealed to be a focused MTKI that should have a bright future in fighting a wide range of cancers.
AZAINDOLE DERIVATIVES AS MULTI KINASE INHIBITORS
-
, (2014/07/21)
The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus also includes the preparation of compounds of formula (I), their uses, in particular in the inhibition of protein kinases which are implicated for example in numerous diseases such as cancers or immune system disorders.
Synthesis of new amides of the N-methylpiperazine series
Koroleva,Gusak,Ignatovich,Ermolinskaya
, p. 1556 - 1563 (2012/03/09)
New carboxylic acid amides containing an N-methylpiperazine fragment were synthesized by reactions of 1-methylpiperazine or 3- and 4-(4-methylpiperazin-1- ylmethyl)aniline with 4-chlorobenzoyl chloride and of 4-methyl-3-nitroaniline with 4-(4-methylpiperazin-1-ylmethyl)benzoyl chloride or benzotriazol-1-yl 4-(4-methylpiperazin-1-ylmethyl)benzoate. 4-Chloro-N-[4-(4-methylpiperazin-1- ylmethyl)phenyl]benzamide reacted with imidazole, quinolin-5-amine, and 2-methylquinolin-5-amine to give substituted 4-amino-N-[4-(4- methylpiperazin-1-ylmethyl)phenyl]benzamides. 4-Methyl-3-nitrophenyl-4- methylpiperazin-1-yl-substituted benzamides were reduced with hydrazine hydrate over Raney nickel to obtain N-(3-amino-4-methylphenyl)-4- (4-methylpiperazin-1- ylmethyl)benzamide as key intermediate in the synthesis of antileukemic agent imatinib and its isomer with alternative position of the amide group, 4-[(3-amino-4-methylphenylamino)methyl]phenyl- (4-methylpiperazin-1-yl)} methanone. Pleiades Publishing, Ltd., 2011.
GLEEVEC PROCESS
-
Page/Page column 9-10, (2008/06/13)
The invention provides a process for the production of a pharmaceutical intermediate compound in accordance with the following scheme (formula (I)), wherein R5 is any suitable substituent group; and Z is any suitable leaving group.
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
-
Page/Page column 21-22, (2008/06/13)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, CSK, TrkB, FGFR3, Fes, Lck, B-RAF, C-RAF, MKK6, SAPK2alpha and SAPK2beta kinases.