882670-92-0Relevant articles and documents
INHIBITOR OF BRUTON'S TYROSINE KINASE
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, (2021/09/24)
Disclosed herein is a compound of Formula (I) with a Btk inhibitory activity, wherein all the variables are as defined herein. The compound can be used for the treatment of diseases such as autoimmune diseases, xenogeneic immune diseases, cancers or thromboembolic diseases. Also disclosed is a pharmaceutical composition comprising a compound of Formula (I). Futher provided is a compound capable of inhibiting the activity of Bruton's tyrosine kinase by covalent binding.
GCN2 MODULATOR COMPOUNDS
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Paragraph 187; 190; 192-193, (2021/08/27)
The disclosures herein relate to novel compounds of Formula (1): or a salt thereof, wherein X, Y, R1, R2, R3, R4 and R5 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with General Control Nondepressible 2 (GCN2).
PYRIDOPYRIMIDINE COMPOUNDS ACTING AS MTORC 1/2 DOUBLE-KINASE INHIBITORS
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Paragraph 0182-0184, (2020/11/30)
Disclosed are a series of pyridopyrimidine compounds and a use of same in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors, and specifically disclosed is a use of the compounds as shown in formula (IV), tautomers thereof or pharmaceutically acceptable salts thereof in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors.
UREA AND THIOUREA SUBSTITUTED BICYCLES DERIVATIVES AS PESTICIDES
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Page/Page column 60, (2018/02/20)
The present invention relates to compounds of formula (I) a compound of formula (1') as defined herein, to processes for preparing them, to pesticidal, in particular insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and
Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit
Hu, Essa,Tasker, Andrew,White, Ryan D.,Kunz, Roxanne K.,Human, Jason,Chen, Ning,Bürli, Roland,Hungate, Randall,Novak, Perry,Itano, Andrea,Zhang, Xuxia,Yu, Violeta,Nguyen, Yen,Tudor, Yanyan,Plant, Matthew,Flynn, Shaun,Xu, Yang,Meagher, Kristin L.,Whittington, Douglas A.,Ng, Gordon Y.
scheme or table, p. 3065 - 3068 (2009/04/11)
Inhibition of c-Kit has the potential to treat mast cell associated fibrotic diseases. We report the discovery of several aminoquinazoline pyridones that are potent inhibitors of c-Kit with greater than 200-fold selectivity against KDR, p38, Lck, and Src.
Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: Synthesis, SAR, and in vivo anti-inflammatory activity
DiMauro, Erin F.,Newcomb, John,Nunes, Joseph J.,Bemis, Jean E.,Boucher, Christina,Buchanan, John L.,Buckner, William H.,Cee, Victor J.,Chai, Lilly,Deak, Holly L.,Epstein, Linda F.,Faust, Ted,Gallant, Paul,Geuns-Meyer, Stephanie D.,Gore, Anu,Gu, Yan,Henkle, Brad,Hodous, Brian L.,Hsieh, Faye,Huang, Xin,Kim, Joseph L.,Lee, Josie H.,Martin, Matthew W.,Masse, Craig E.,McGowan, David C.,Metz, Daniela,Mohn, Deanna,Morgenstern, Kurt A.,Oliveira-Dos-Santos, Antonio,Patel, Vinod F.,Powers, David,Rose, Paul E.,Schneider, Stephen,Tomlinson, Susan A.,Tudor, Yan-Yan,Turci, Susan M.,Welcher, Andrew A.,White, Ryan D.,Zhao, Huilin,Zhu, Li,Zhu, Xiaotian
, p. 5671 - 5686 (2007/10/03)
The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and natural killer (NK) cells. Genetic evidence in both mice and humans demonstrates that Lck kinase activity is critical for signaling mediated by the T cell receptor (TCR), which leads to normal T cell development and activation. Selective inhibition of Lck is expected to offer a new therapy for the treatment of T-cell-mediated autoimmune and inflammatory disease. Screening of our kinase-preferred collection identified aminoquinazoline 1 as a potent, nonselective inhibitor of Lck and T cell proliferation. In this report, we describe the synthesis and structure-activity relationships of a series of novel aminoquinazolines possessing in vitro mechanism-based potency. Optimized, orally bioavailable compounds 32 and 47 exhibit anti-inflammatory activity (ED50 of 22 and 11 mg/kg, respectively) in the anti-CD3-induced production of interleukin-2 (IL-2) in mice.