1419221-80-9Relevant academic research and scientific papers
FUSED BICYCLIC COMPOUND FOR INHIBITING ACTIVITY OF TYROSINE KINASE
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, (2019/06/12)
A fused bicyclic compound having an effect in inhibition of the activity of a tyrosine kinase, and preparation and use thereof are disclosed. In particular, a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydr
The compounds of structure containing conjugated zincon, its pharmaceutical composition and use thereof (by machine translation)
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, (2018/03/24)
The present invention relates to compounds having a structure containing conjugated zincon, its pharmaceutical composition and use, and in particular relates to the general formula (I) or a salt thereof to the compound represented by the, pharmaceutical compositions thereof, and its as BTK inhibitors and/or B cell activation inhibitor, for the prevention or treatment B cell activity with abnormal and/or the use of the BTK-related diseases. The compounds of lymphoma, breast cancer, liver cancer, colon cancer, gastric cancer, such as lung cancer and cervical cancer cell has better lethal effect, note has potential for the treatment of cancer and self-immune diseases related to potential. (by machine translation)
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis
Liu, Jian,Guiadeen, Deodial,Krikorian, Arto,Gao, Xiaolei,Wang, James,Boga, Sobhana Babu,Alhassan, Abdul-Basit,Yu, Younong,Vaccaro, Henry,Liu, Shilan,Yang, Chundao,Wu, Hao,Cooper, Alan,De Man, Jos,Kaptein, Allard,Maloney, Kevin,Hornak, Viktor,Gao, Ying-Duo,Fischmann, Thierry O.,Raaijmakers, Hans,Vu-Pham, Diep,Presland, Jeremy,Mansueto, My,Xu, Zangwei,Leccese, Erica,Zhang-Hoover, Jie,Knemeyer, Ian,Garlisi, Charles G.,Bays, Nathan,Stivers, Peter,Brandish, Philip E.,Hicks, Alexandra,Kim, Ronald,Kozlowski, Joseph A.
, p. 198 - 203 (2016/03/01)
Bruton's tyrosine kinase (BTK) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) pathway. It has become an attractive kinase target for selective B cell inhibition and for the treatment of B cell related diseases. We report a series of compounds based on 8-amino-imidazo[1,5-a]pyrazine that are potent reversible BTK inhibitors with excellent kinase selectivity. Selectivity is achieved through specific interactions of the ligand with the kinase hinge and driven by aminopyridine hydrogen bondings with Ser538 and Asp539, and by hydrophobic interaction of trifluoropyridine in the back pocket. These interactions are evident in the X-ray crystal structure of the lead compounds 1 and 3 in the complex with the BTK enzyme. Our lead compounds show desirable PK profiles and efficacy in the preclinical rat collagen induced arthritis model.
4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
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, (2013/03/26)
The present invention provides 6-5 membered fused pyridine ring compounds according to Formula I or pharmaceutically acceptable salts thereof. or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
