923009-49-8Relevant articles and documents
SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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Page/Page column 30; 31, (2018/03/28)
Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
Design, synthesis, and structure-activity relationships of novel spiro-piperidines as acetyl-CoA carboxylase inhibitors
Kamata, Makoto,Yamashita, Tohru,Kina, Asato,Funata, Masaaki,Mizukami, Atsushi,Sasaki, Masako,Tani, Akiyoshi,Funami, Miyuki,Amano, Nobuyuki,Fukatsu, Kohji
scheme or table, p. 3643 - 3647 (2012/07/17)
Spiro-lactone (S)-1 is a potent acetyl-CoA carboxylase (ACC) inhibitor and was found to be metabolically liable in human hepatic microsomes. To remove one of the risk factors in human study by improving the metabolic stability, we focused on modifying the
Design, synthesis, and structure-activity relationships of spirolactones bearing 2-ureidobenzothiophene as acetyl-CoA carboxylases inhibitors
Yamashita, Tohru,Kamata, Makoto,Endo, Satoshi,Yamamoto, Mitsuo,Kakegawa, Keiko,Watanabe, Hiroyuki,Miwa, Katsuhiko,Yamano, Toru,Funata, Masaaki,Sakamoto, Jyun-Ichi,Tani, Akiyoshi,Mol, Clifford D.,Zou, Hua,Dougan, Douglas R.,Sang, BiChing,Snell, Gyorgy,Fukatsu, Kohji
scheme or table, p. 6314 - 6318 (2011/11/29)
The co-crystal structure of the human acetyl-coenzyme A 2 (ACC2) carboxyl transferase domain and the reported compound CP-640186 (1b) suggested that two carbonyl groups are essential for potent ACC2 inhibition. By focusing on enhancing the interactions between the two carbonyl groups and the amino acid residues Gly2162 and Glu2230, we used ligand- and structure-based drug design to discover spirolactones bearing a 2-ureidobenzothiophene moiety
SPIRO-RING COMPOUND
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Page/Page column 40, (2009/12/23)
The present invention aims to provide a compound having an acetyl-CoA carboxylase (ACC) inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom or a substituent; ring P is an optionally substituted 6-membered nitrogen-containing aromatic heterocycle; ring Q is an optionally further substituted 5- to 7-membered nitrogen-containing non-aromatic heterocycle; and ring R is an optionally fused 5- to 7-membered non-aromatic ring, which is further optionally substituted, or a salt thereof.