862274-39-3Relevant academic research and scientific papers
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.
NIACIN RECEPTOR AGONISTS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Page/Page column 32-33, (2008/12/05)
The present invention encompasses compounds of Formula (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also
INDAZOLE DERIVATIVES AS INHIBITORS OF HORMONE-SENSITIVE LIPASES
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Page/Page column 33-34, (2008/06/13)
The invention relates to indazole derivatives of general formula (I) or (II), with the meanings as given in the description, the pharmaceutically-acceptable salts and use thereof as medicaments.
Indazole derivatives as inhibitors of hormone sensitive lipase
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Page/Page column 11, (2008/06/13)
The present invention relates to indazole derivatives of the general formulae I or II having the meanings indicated in the description, to the pharmaceutically useful salts thereof and the use thereof as drugs.
