864864-17-5Relevant academic research and scientific papers
Discovery and biological profile of isoindolinone derivatives as novel metabotropic glutamate receptor 1 antagonists: A potential treatment for psychotic disorders
Ito, Satoru,Hirata, Yukari,Nagatomi, Yasushi,Satoh, Atsushi,Suzuki, Gentaroh,Kimura, Toshifumi,Satow, Akio,Maehara, Shunsuke,Hikichi, Hirohiko,Hata, Mikiko,Ohta, Hisashi,Kawamoto, Hiroshi
scheme or table, p. 5310 - 5313 (2010/04/26)
We describe here the discovery and biological profile of a series of isoindolinone derivatives as developed mGluR1 antagonists. Our combined strategy of rapid parallel synthesis and conventional medicinal optimization successfully led to N-cyclopropyl 22 and N-isopropyl isoindolinone analogs 21 and 23 with improved in vivo DMPK profiles. Moreover the most advanced analog 23 showed an oral antipsychotic-like effect at a dose of 1 mg/kg in an animal model.
DIARYL-SUBSTITUTED FIVE-MEMBERED HETEROCYCLE DERIVATIVE
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, (2010/11/24)
The present invention provides the compounds represented by formula (I): (I) or pharmaceutical salts thereof, wherein: X 1 represents oxygen atoms and the like, X 2 represents nitrogen atoms and the like, X 3 represents nitrogen atoms and the like, X 4 represents nitrogen atoms and the like, R 1 represents formula (II-1): wherein X 5 represents sulfur atoms and the like, A 1 represents carbon atoms and the like, A 2 represents nitrogen atoms and the like and A ring represents phenyl group and the like, having mGluR1 inhibiting effect, and being usefull for preventing or treating convulsion, acute pain, inflammatory pain, chronic pain, brain disorder such as cerebral infarction or transient ischemick attack, psychotic disorder such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorder.
