229006-88-6Relevant articles and documents
Synthesis, binding affinity and structure-activity relationships of novel, selective and dual targeting CCR2 and CCR5 receptor antagonists
Junker, Anna,Kokornaczyk, Artur K.,Zweemer, Annelien J. M.,Frehland, Bastian,Schepmann, Dirk,Yamaguchi, Junichiro,Itami, Kenichiro,Faust, Andreas,Hermann, Sven,Wagner, Stefan,Sch?fers, Michael,Koch, Michael,Weiss, Christina,Heitman, Laura H.,Kopka, Klaus,Wünsch, Bernhard
supporting information, p. 2407 - 2422 (2015/03/04)
CCR2 and CCR5 receptors play a key role in the development and progression of several inflammatory, cardiovascular and autoimmune diseases. Therefore, dual targeting of both receptors appeals as a promising strategy for the treatment of such complex, mult
Convenient efficient synthesis of TAK-779, a nonpeptide CCR5 antagonist: Development of preparation of various ammonium salts using trialkylphosphite and N-halogenosuccinimide
Ikemoto, Tomomi,Nishiguchi, Atsuko,Mitsudera, Hiroyuki,Wakimasu, Mitsuhiro,Tomimatsu, Kiminori
, p. 1525 - 1529 (2007/10/03)
A convenient and efficient synthesis of TAK-779 (1a), a nonpeptide CCR5 antagonist, has been achieved. The new methylation of tertiary amine (2) using trimethyl phosphite and N-chlorosuccinimide, followed by the addition of HCl led to ammonium chloride (1a) in 89% isolated yield without requiring a chromatographic method. By this preparation, ammonium methanesulfonate (1e) could be obtained in 75% isolated yield.
Anilide derivative, production and use thereof
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, (2008/06/13)
This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.