- 2-[BIS(4-FLUOROPHENYL)METHYL]-2,7-DIAZASPIRO[4.5]DECAN-10-ONE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF THE HUMAN DOPAMINE-ACTIVE-TRANSPORTER (DAT) PROTEIN FOR THE TREATMENT OF E.G. ATTENTION DEFICIT DISORDER (ADD)
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The present invention provides compounds of formula (I) and in particular 2-[bis(4-fluorophenyl)methyl]-2,7- diazaspiro[4.5]decan-10-one derivatives and related compounds as inhibitors of human dopamine-active-transporter (DAT) protein for the treatment of sexual dysfunction, affective disorders, anxiety, depression, chronic fatigue, Tourette syndrome, Angelman syndrome, attention deficit disorder (ADD), attention deficit hyperactivity disorder (ADHD), obesity, pain, obsessive-compulsive disorder, movement disorders, CNS disorders, sleep disorders, narcolepsy, conduct disorder, substance abuse (including smoking cessation), eating disorders, and impulse control disorders.
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Page/Page column 84
(2016/04/09)
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- Design, synthesis, and structure-activity relationships of spirolactones bearing 2-ureidobenzothiophene as acetyl-CoA carboxylases inhibitors
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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
- 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
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p. 6314 - 6318
(2011/11/29)
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