1315592-05-2Relevant academic research and scientific papers
ROR [gamma]t inhibitor and application in medicine
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, (2021/07/08)
The invention belongs to the technical field of medicines, and particularly relates to an ROR [gamma]t inhibitor and application in medicines. The invention also relates to a method for preparing the compound and a pharmaceutical composition containing the compound, and application of the compound and the pharmaceutical composition in treatment or prevention of ROR [gamma]t-mediated cancers, inflammations or autoimmune diseases of mammals, especially human beings.
The design and synthesis of novel, potent and orally bioavailable N-aryl piperazine-1-carboxamide CCR2 antagonists with very high hERG selectivity
Cumming, John G.,Bower, Justin F.,Waterson, David,Faull, Alan,Poyser, Philip J.,Turner, Paul,McDermott, Benjamin,Campbell, Andrew D.,Hudson, Julian,James, Michael,Winter, Jon,Wood, Christine
scheme or table, p. 3895 - 3899 (2012/07/03)
A novel N-aryl piperazine-1-carboxamide series of human CCR2 chemokine receptor antagonists was discovered. Early analogues were potent at CCR2 but also inhibited the hERG cardiac ion channel. Structural modifications which decreased lipophilicity and basicity resulted in the identification of a sub-series with an improved margin over hERG. The pharmacological and pharmacokinetic properties of the lead compound from this series, N-(3,4-dichlorophenyl)-4-[(2R)-4-isopropylpiperazine-2-carbonyl] piperazine-1-carboxamide, are described.
