726206-83-3Relevant articles and documents
Immunomodulator
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, (2021/05/22)
The invention discloses an immunomodulator, and particularly relates to a compound for inhibiting IL-17A and application of the compound serving as the immunomodulator in preparation of drugs. The invention discloses application of a compound shown in a formula I or a stereoisomer thereof in preparation of medicines for inhibiting IL-17A, and provides a new choice for clinically screening and/or preparing medicines for treating diseases related to IL-17A activity.
Immunomodulator
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, (2021/02/10)
The invention discloses an immunomodulator, and particularly relates to a compound shown as a formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. Experiments prove that the compound has good IL-17A inhibitory activity, can be used for preparing an IL-17A inhibitor and drugs for preventing and/or treating IL-17A mediated diseases (such as inflammation, autoimmune diseases, infectious diseases, cancers and precancerous syndromes), and provides a new medical possibility for clinical treatment of diseases related to abnormal IL-17A activity.
Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors
Yoshikawa, Kenji,Yoshino, Toshiharu,Yokomizo, Yoshihiro,Uoto, Kouichi,Naito, Hiroyuki,Kawakami, Katsuhiro,Mochizuki, Akiyoshi,Nagata, Tsutomu,Suzuki, Makoto,Kanno, Hideyuki,Takemura, Makoto,Ohta, Toshiharu
, p. 2133 - 2140 (2011/04/24)
We previously reported on a series of cyclohexanediamine derivatives as highly potent factor Xa inhibitors. Herein, we describe the modification of the spacer moiety to discover an alternative scaffold. Ethylenediamine derivatives possessing a substituent at the C1 position in S configuration and phenylenediamine derivatives possessing a substituent at the C5 position demonstrated moderate to strong anti-fXa activity. Further SAR studies led to the identification of compound 30h which showed both good in vitro activity (fXa IC50 = 2.2 nM, PTCT2 = 3.9 μM) and in vivo antithrombotic efficacy.