215453-53-5Relevant articles and documents
Mild, General, and Regioselective Synthesis of 2-Aminopyridines from Pyridine N -Oxides via N -(2-Pyridyl)pyridinium Salts
Xiong, Hui,Hoye, Adam T.
, p. 371 - 375 (2022/01/27)
A synthesis of 2-aminopyridines from pyridine N-oxides via their corresponding N-(2-pyridyl)pyridinium salts has been demonstrated and investigated. The reaction sequence features a highly regioselective conversion of the N-oxide into its pyridinium salt
AMINOPYRIDINE COMPOUNDS AND METHODS FOR THE PREPARATION AND USE THEREOF
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Paragraph 0188, (2018/12/02)
The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I and Formula III, as described herein, and pharmaceutically acceptable salts thereof.
Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis
Ndubaku, Chudi O.,Crawford, Terry D.,Chen, Huifen,Boggs, Jason W.,Drobnick, Joy,Harris, Seth F.,Jesudason, Rajiv,McNamara, Erin,Nonomiya, Jim,Sambrone, Amy,Schmidt, Stephen,Smyczek, Tanya,Vitorino, Philip,Wang, Lan,Wu, Ping,Yeung, Stacey,Chen, Jinhua,Chen, Kevin,Ding, Charles Z.,Wang, Tao,Xu, Zijin,Gould, Stephen E.,Murray, Lesley J.,Ye, Weilan
, p. 913 - 918 (2015/08/24)
Diverse biological roles for mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) have necessitated the identification of potent inhibitors in order to study its function in various disease contexts. In particular, compounds that can be used to carry out such studies in vivo would be critical for elucidating the potential for therapeutic intervention. A structure-based design effort coupled with property-guided optimization directed at minimizing the ability of the inhibitors to cross into the CNS led to an advanced compound 13 (GNE-495) that showed excellent potency and good PK and was used to demonstrate in vivo efficacy in a retinal angiogenesis model recapitulating effects that were observed in the inducible Map4k4 knockout mice.
Heterocyclic derivatives and their use as antithrombotic agents
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, (2008/06/13)
The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is O or S; X′ being independently CH or N; and m is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an optionally substituted nitrogen or carbon atom, or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention are therapeutically active and in particular are antithrombotic agents.
Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors
Rewinkel,Lucas,Smit,Noach,Van Dinther,Rood,Jenneboer,Van Boeckel
, p. 2837 - 2842 (2007/10/03)
Replacement of the highly basic benzamidine moiety with moderate basic amino-bicycloaryl moieties in a series of thrombin inhibitors related to NAPAMP provided potent enzyme inhibition and significant improvements in membrane transport and oral bioavailability.