131395-17-0Relevant academic research and scientific papers
SULFONYL-SUBSTITUTED BICYCLIC COMPOUND WHICH ACTS AS ROR INHIBITOR
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, (2020/08/16)
Provided is a sulfonyl-substituted bicyclic compound (A) which acts as a RORγ inhibitor, said compound has good RORγ inhibitory activity and is expected to be used for treating diseases mediated by a RORγ receptor in mammals.
Divergent synthesis of photoaffinity probe candidates by click reactions of azido-substituted aryltrifluoromethyldiazirines
Watanabe, Kenji,Tsuda, Junpei,Ochiai, Hidenori,Niwa, Takashi,Hosoya, Takamitsu
, p. 1366 - 1387 (2019/07/31)
Two types of azido-substituted aryltrifluoromethyldiazirine units have been designed and prepared for the divergent synthesis of photoaffinity probe (PAP) candidates. Using these azides, various aryltrifluoromethyldiazirine derivatives have been rendered easily synthesizable by several click reactions, as well as the Staudinger reduction affording the corresponding aniline. The triazole-conjugated aryltrifluoromethyldiazirine derivatives prepared in this study showed normal photoreactivity compared with those reported previously. These results indicate the utility of these azido-substituted aryltrifluoromethyldiazirine units for development of PAPs for target identification of bioactive compounds.
A facile synthesis of isomeric C -(2,2,2-trifluoroethyl)anilines
Trofymchuk, Sergii,Bezdudny, Andrii V.,Pustovit, Yurii M.,Lukin, Oleg,Boyko, Alexander N.,Chekotylo, Alexey,Tolmachev, Andrei A.,Mykhailiuk, Pavel K.
experimental part, p. 1974 - 1976 (2012/08/27)
Three isomers of C-(2,2,2-trifluoroethyl)aniline were prepared on a multigram scale from readily available nitrophenylacetic acids in two steps. First, the carboxy groups of the latter were converted into the trifluoromethyl moieties by treatment with sul
Riluzole series. synthesis and in vivo 'antiglutamate' activity of 6- substituted-2-benzothiazolamines and 3-substituted-2-imino-benzothiazolines
Jimonet, Patrick,Audiau, Fran?ois,Barreau, Michel,Blanchard, Jean-Charles,Boireau, Alain,Bour, Yvette,Coléno, Marie-Annick,Doble, Adam,Doerflinger, Gilles,Do Huu, Claudine,Donat, Marie-Hélène,Duchesne, Jean Marie,Ganil, Pierre,Guérémy, Claude,Honoré, Eliane,Just, Bernard,Kerphirique, Roselyne,Gontier, Sylvie,Hubert, Philippe,Laduron, Pierre M.,Blevec, Joseph Le,Meunier, Mireille,Miquet, Jean-Marie,Nemecek, Conception,Pasquet, Martine,Piot, Odile,Pratt, Jeremy,Rataud, Jean,Reibaud, Michel,Stutzmann, Jean-Marie,Mignani, Serge
, p. 2828 - 2843 (2007/10/03)
Two series of analogues of riluzole, a blocker of excitatory amino acid mediated neurotransmission, have been synthesized: monosubstituted 2- benzothiazolamines and 3-substituted derivatives. Of all the compounds prepared in the first series, only 2-benzothiazolamines bearing alkyl, polyfluoroalkyl, or polyfluoroalkoxy substituents in the 6-position showed potent anticonvulsant activity against administration of glutamic acid in rats. The most active compounds displaying in vivo 'antiglutamate' activity were the 6-OCF3 (riluzole), 6-OCF2CF3, 6-CF3, and 6-CF2CF3 substituted derivatives with ED50 values between 2.5 and 3.2 mg/kg i.p. Among the second series of variously substituted benzothiazolines, compounds as active as riluzole or up to 3 times more potent were identified in two series: benzothiazolines bearing a β-dialkylaminoethyl moiety and compounds with an alkylthioalkyl chain and their corresponding sulfoxides and sulfones. The most potent derivatives were 2-imino-3-(2-methylthio)- and 2-imino-3-(2- methylsulfinyl)-ethyl-6-trifluoromethoxybenzothiazolines (61 and 64, ED50 = 1.0 and 1.1 mg/kg i.p., respectively). In addition, intraperitoneal administration of some of the best benzothiazolines protected mice from mortality produced by hypobaric hypoxia.
Pharmaceutical compositions, 2-benzothiazolamine derivatives, and their preparation
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, (2008/06/13)
Pharmaceutical compositions are disclosed. They are useful for the treatment of medical conditions associated with the effects of glutamate, comprise as active principle, at least one compound of formula: STR1 or a salt thereof, in which either R1 represents polyfluoroalkoxy, 2,2,2-trifluoroethyl, pentafluoroethyl, tert-butyl, trimethylsilyl or trifluoromethylthio and R2 and R3 represent hydrogen, or R1 represents polyfluoroalkoxy, R2 represents hydrogen and R3 represents alkyl, amino, alkoxy, phenyl, phenylalkyl, dimethylamino or dialkylaminoakylthio, or R1 represents polyfluoroalkoxy, R2 represents amino and R3 represents hydrogen, with the exception of 6-trifluoromethoxy-2-benzothiazolamine.
