7364-27-4Relevant articles and documents
Discovery of isatin and 1H-indazol-3-ol derivatives as D-amino acid oxidase (DAAO) inhibitors
Szilágyi, Bence,Kovács, Péter,Ferenczy, Gy?rgy G.,Rácz, Anita,Németh, Krisztina,Visy, Júlia,Szabó, Pál,Ilas, Janez,Balogh, Gy?rgy T.,Monostory, Katalin,Vincze, István,Tábi, Tamás,Sz?k?, éva,Keser?, Gy?rgy M.
, p. 1579 - 1587 (2018/02/23)
D-Amino acid oxidase (DAAO) is a potential target in the treatment of schizophrenia as its inhibition increases brain D-serine level and thus contributes to NMDA receptor activation. Inhibitors of DAAO were sought testing [6+5] type heterocycles and identified isatin derivatives as micromolar DAAO inhibitors. A pharmacophore and structure-activity relationship analysis of isatins and reported DAAO inhibitors led us to investigate 1H-indazol-3-ol derivatives and nanomolar inhibitors were identified. The series was further characterized by pKa and isothermal titration calorimetry measurements. Representative compounds exhibited beneficial properties in in vitro metabolic stability and PAMPA assays. 6-fluoro-1H-indazol-3-ol (37) significantly increased plasma D-serine level in an in vivo study on mice. These results show that the 1H-indazol-3-ol series represents a novel class of DAAO inhibitors with the potential to develop drug candidates.
ISOINDOLINONE COMPOUNDS AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS
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Page/Page column 75; 76, (2015/11/02)
The present invention relates to isoindolinone compounds. The isoindolinone compounds are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the u
NOVEL 1-SUBSTITUTED INDAZOLE DERIVATIVE
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Paragraph 0228-0230, (2014/05/08)
A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and