1141878-75-2Relevant academic research and scientific papers
BENZOXAZINONE DERIVATIVE
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Page/Page column 66; 67, (2010/08/07)
[PROBLEMS] To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases. [MEANS FOR SOLVING PROBLEMS] The compound, which is for use as an active ingredient, is represented by the formula (I): [wherein R1 represents optionally halogenated C1-6 alkyl, etc.; R2 represents, e.g., a group represented by the formula (II-1) or (II-4) (wherein W represents C1-6 alkylene, etc. and R represents C1-6 alkyl, etc.); R3 represents hydrogen, C1-6 alkyl, etc.; X represents -O-, -NH-, etc.; and Y1, Y2, Y3, and Y4 each independently represents -CH-, -N-, etc.].
Discovery of novel benzoxazinones as potent and orally active long chain fatty acid elongase 6 inhibitors
Mizutani, Takashi,Ishikawa, Shiho,Nagase, Tsuyoshi,Takahashi, Hidekazu,Fujimura, Takashi,Sasaki, Takahide,Nagumo, Akira,Shimamura, Ken,Miyamoto, Yasuhisa,Kitazawa, Hidefumi,Kanesaka, Maki,Yoshimoto, Ryo,Aragane, Katsumi,Tokita, Shigeru,Sato, Nagaaki
experimental part, p. 7289 - 7300 (2010/06/16)
A series of benzoxazinones was synthesized and evaluated as novel long chain fatty acid elongase 6 (ELOVL6) inhibitors. Exploration of the SAR of the UHTS lead 1a led to the identification of (S)-1y that possesses a unique chiral quarternary center and a
