60986-80-3Relevant academic research and scientific papers
Isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists
Nakamura, Masayuki,Kurihara, Hideki,Suzuki, Gentaroh,Mitsuya, Morihiro,Ohkubo, Mitsuru,Ohta, Hisashi
scheme or table, p. 726 - 729 (2010/05/18)
This Letter describes the synthesis and evaluation of mGluR7 antagonists in the isoxazolopyridone series. In the course of modification in this class, novel solid support synthesis of the isoxazolopyridone scaffold was developed. Subsequent chemical modification led to the identification of several potent derivatives with improved physicochemical properties compared to a hit compound 1. Among these, 2 showed good oral bioavailability and brain penetrability, suggesting that 2 may be useful for in vivo study to elucidate the role of mGluR7.
Process for the preparation of substituted isoxazolo[4,5-c]pyridin-4-(5H)-ones
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, (2008/06/13)
An improved process for the preparation of substituted isoxazolo[4,5-c]pyridin-4(5H)-ones which are either useful as intermediates in the preparation of compounds having pharmaceutical activity or as hypolipidemic agents which comprises cyclizing a corresponding 5-(2-amino-2-phenyl- or substituted phenyl-ethenyl)-3-substituted-N-alkyl isoxazole-4-carboxamide under acidic conditions.
Substituted hydroxy pyridones
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, (2008/06/13)
Substituted hydroxy pyridones, e.g., 3-(α-iminobenzyl)-4-hydroxy-6-phenyl-1-methyl-2(1H)-pyridone, are prepared by reducing corresponding isoxazolo[4,5-c]pyridin-4(5H)-ones and are useful as minor tranquilizers and sleep inducers.
Substituted hydroxy pyridones
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, (2008/06/13)
Substituted hydroxy pyridones, e.g., 3-(α-N-methyliminobenzyl)-4-hydroxy-6-phenyl-1-methyl-2(1H)-pyridone, are prepared by reacting a corresponding substituted hydroxy pyridone carbonyl with an alkyl amine, and are useful as minor tranquilizers, sleep inducers, muscle relaxants, and neuroleptics.
Substituted pyrido[3,4-e]oxazine diones and their therapeutic use
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, (2008/06/13)
Substituted pyrido[3,4-e]oxazine diones, e.g., 6-methyl-4,7-diphenyl-2H-pyrido[3,4-e]-1,3-oxazine-2,5-dione are useful as minor tranquilizers, sleep inducers and muscle relaxants.
