- 4-PYRIDONE COMPOUND OR SALT THEREOF, AND PHARMACEUTICAL COMPOSITION AND FORMULATION INCLUDING SAME
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An object of the present invention is to provide a compound or a salt thereof having anti-HBV activity, a pharmaceutical composition, an anti-hepatitis B virus agent, a production inhibitor of DNA of a hepatitis B virus, and a production or secretion inhibitor of a hepatitis B surface antigen. According to the present invention, provided are a compound represented by General Formula [1] or a salt thereof: (in the formula, R1 represents a benzothiazolyl group which may be substituted (in which a carbon atom constituting the 6-membered ring of the benzothiazolyl group of R1 is bonded to the nitrogen atom of the pyridone ring); R2 represents a C2-6 alkenyl group which may be substituted, or the like; and R3 represents a hydrogen atom or the like).
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Paragraph 0528; 0532-0536; 0537-0539
(2020/02/08)
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- Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index
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Serine/threonine protein kinases Aurora A, B, and C play essential roles in cell mitosis and cytokinesis. Currently a number of Aurora kinase inhibitors with different isoform selectivities are being evaluated in the clinic. Herein we report the discovery and characterization of 21c (AC014) and 21i (AC081), two structurally novel, potent, kinome-selective pan-Aurora inhibitors. In the human colon cancer cell line HCT-116, both compounds potently inhibit histone H3 phosphorylation and cell proliferation while inducing 8N polyploidy. Both compounds administered intravenously on intermittent schedules displayed potent and durable antitumor activity in a nude rat HCT-116 tumor xenograft model and exhibited good in vivo tolerability. Taken together, these data support further development of both 21c and 21i as potential therapeutic agents for the treatment of solid tumors and hematological malignancies.
- Liu, Gang,Abraham, Sunny,Tran, Lan,Vickers, Troy D.,Xu, Shimin,Hadd, Michael J.,Quiambao, Sheena,Holladay, Mark W.,Hua, Helen,Ford Pulido, Julia M.,Gunawardane, Ruwanthi N.,Davis, Mindy I.,Eichelberger, Shawn R.,Apuy, Julius L.,Gitnick, Dana,Gardner, Michael F.,James, Joyce,Breider, Mike A.,Belli, Barbara,Armstrong, Robert C.,Treiber, Daniel K.
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scheme or table
p. 3250 - 3260
(2012/06/01)
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