328232-52-6Relevant academic research and scientific papers
Discovery of trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide, a potent and orally active neuropeptide Y Y5 receptor antagonist
Haga, Yuji,Sakamoto, Toshihiro,Shibata, Takunobu,Nonoshita, Katsumasa,Ishikawa, Makoto,Suga, Takuya,Takahashi, Hirobumi,Takahashi, Toshiyuki,Takahashi, Hidekazu,Ando, Makoto,Murai, Takashi,Gomori, Akira,Oda, Zenjun,Kitazawa, Hidefumi,Mitobe, Yuko,Kanesaka, Maki,Ohe, Tomoyuki,Iwaasa, Hisashi,Ishii, Yasuyuki,Ishihara, Akane,Kanatani, Akio,Fukami, Takehiro
experimental part, p. 6971 - 6982 (2010/02/28)
A series of trans-3-oxospiro[(aza)isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide derivatives were synthesized to identify potent NPY Y5 receptor antagonists. Of the compounds, 21j showed high Y5 binding affinity, metabolic stability and brain and cerebrospinal fluid (CSF) penetration, and low susceptibility to P-glycoprotein transporters. Oral administration of 21j significantly inhibited the Y5 agonist-induced food intake in rats with a minimum effective dose of 1 mg/kg. This compound was selected for proof-of-concept studies in human clinical trials.
Spiro compounds
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, (2008/06/13)
Compounds of the general formula (I): wherein Ar1represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.
Novel spiro compounds
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, (2008/06/13)
Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.
