41118-21-2Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS WITH AN ROR(GAMMA)T MODULATING ACTIVITY
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Paragraph 0573, (2018/03/06)
The present invention relates to a compound that may have an ROR(gamma)t modulating activity and can thus be useful in the treatment of cancer.
Anti-tumor drug benzodihydropyran (thiopyran) amide compound and its pharmaceutically acceptable salts and preparation method and application
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Paragraph 0053-0055, (2017/03/08)
The invention relates to new compounds benzodihydropyran(thiapyran)amide compounds represented by general formula I, or pharmaceutically acceptable salts of the compounds. The compounds or the pharmaceutically acceptable salts thereof are used as an antit
Design and synthesis of conformationally constrained tri-substituted ureas as potent antagonists of the human glucagon receptor
Liang, Rui,Abrardo, Lauren,Brady, Edward J.,Candelore, Mari Rios,Ding, Victor,Saperstein, Richard,Tota, Laurie M.,Wright, Michael,Mock, Steve,Tamvakopolous, Constantin,Tong, Sharon,Zheng, Song,Zhang, Bei B.,Tata, James R.,Parmee, Emma R.
, p. 587 - 592 (2007/10/03)
A series of conformationally constrained tri-substituted ureas were synthesized, and their potential as glucagon receptor antagonists was evaluated. This effort resulted in the identification of compound 4a, which had a binding IC50 of 4.0 nM a
A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core
Fotsch, Christopher,Biddlecome, Gloria,Biswas, Kaustav,Chen, Jian Jeff,D'Amico, Derin C.,Groneberg, Robert D.,Han, Nianhe Bruce,Hsieh, Feng-Yin,Kamassah, Augustus,Kumar, Gondi,Lester-Zeiner, Dianna,Liu, Qingyian,Mareska, David A.,Riahi, Babak Bobby,Wang, Yueh-Ju Judy,Yang, Kevin,Zhan, James,Zhu, Joe,Johnson, Eileen,Ng, Gordon,Askew, Benny C.
, p. 2071 - 2075 (2007/10/03)
The bradykinin 1 (B1) receptor is upregulated during times of inflammation and is important for maintaining inflamed and chronic pain states. Blocking this receptor has been shown to reverse and/or ameliorate pain and inflammation in animal models. In this report, we describe a new class of B1 receptor antagonists that contain the piperidine acetic acid tetralin core. A structure-activity relationship for these analogs is described in this paper. The most potent compounds from this class have IC50s 20 nM in a B1 receptor functional assay. One of these compounds, 13g, shows modest oral bioavailability in rats.
