392277-22-4Relevant academic research and scientific papers
ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
-
Paragraph 00264, (2016/04/09)
Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for
Pyrroloquinoline Derivatives And Their Use As Protein Kinases Inhibitors
-
Page/Page column 31, (2009/03/07)
The present invention relates to inhibitors of protein kinases of formula I: which can be used in the treatment of various diseases, notably cancer, inflammation or disorders of the central nervous system. It also relates to pharmaceutical compositions containing the compounds according to the invention and their use in therapy.
An efficient and practical method for highly chemoselective hydrogenation of nitrobenzylamines to aminobenzylamine hydrochlorides
Cheng, Chuanjie,Wang, Xinyan,Xing, Lixin,Liu, Bo,Zhu, Rui,Hu, Yuefei
, p. 1775 - 1780 (2008/02/11)
Aqueous hydrochloric acid proved to be a very reliable modulator for adjusting the reactivity of palladium on carbon. Thus an efficient and practical method for the highly chemoselective hydrogenation of N,N- dialkylnitrobenzylamines to amino-N,N-dialkylbenzylamine hydrochlorides was established. The method features convenient performance, easy work-up and high efficiency
AMIDE DERIVATIVES
-
Page/Page column 73, (2008/06/13)
The invention concerns a compound of the Formula I (A chemical formula should be inserted here - please see paper copy enclosed herewith) wherein m is 0-2 and each R1 is a group such as hydroxy, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is halogeno, trifluoromethyl or (1-6C)alkyl; R3 is hydrogen, halogeno or (1-6C)alkyl; and R4 is (3-6C)cycloalkyl;or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by cytokines.
Process development of 4-[N-methyl-N-(tetrahydropyran-4-yl)aminomethyl]aniline dihydrochloride: A key intermediate for TAK-779, a small-molecule nonpeptide CCR5 antagonist
Hashimoto, Hideo,Ikemoto, Tomomi,Itoh, Tatsuya,Maruyama, Hideaki,Hanaoka, Tadashi,Wakimasu, Mitsuhiro,Mitsudera, Hiroyuki,Tomimatsu, Kiminori
, p. 70 - 73 (2013/09/06)
A new and efficient synthesis of 4-[N-methyl-N-(tetrahydropyran-4-yl)aminomethyl]aniline dihydrochloride, a key intermediate for the CCR5 antagonist TAK-779, is described. Reductive alkylation of methylamine with tetrahydro-4H-pyran-4-one followed by alkylation of N-methyl-N-(tetrahydropyran-4-yl)amine with 4-nitrobenzylbromide and reduction of N-(4-nitrobenzyl)-N-(tetrahydropyran-4-yl)amine results in a 78% isolated yield from the starting materials by a scalable method, using only commercially available reagents.
