439608-30-7Relevant academic research and scientific papers
HMOX1 inducers
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, (2020/09/18)
The present invention is related to compounds of structure (I) as heme oxygenase 1 (HMOX 1) inducers. The present invention is also related a method of controlling the activity or the amount, or both the activity and the amount, of heme-oxygenase 1 in a mammalian subject. The definitions of the variables are provided herein.
Preparation method for methylthio-substituted benzo[d]oxazole derivative
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, (2017/08/31)
The invention discloses a preparation method for a methylthio-substituted benzo[d]oxazole derivative, i.e., 5-methyl-2-(methylthio)benzo[d]oxazole. According to the invention, 2-nitro-4-methylphenol is used as a starting raw material and undergoes reduction, ring closure and methylation so as to obtain the methylthio-substituted benzo[d]oxazole derivative. The prepared derivative is an important medical intermediate.
Regioselective thiolation of arenes and heteroarenes: C-H functionalization strategy for C-S bond formation
Varun, Begur Vasanthkumar,Prabhu, Kandikere Ramaiah
supporting information, p. 9655 - 9668 (2015/01/16)
A facile transition-metal-free oxidative cross-dehydrogenative coupling reaction involving selective formation of a C-S bond leading to the synthesis of arylthiobenzoxazoles, heteroarylthiobenzoxazoles, and arylthiobenzothiazoles has been described. This highly regioselective C-H functionalization reaction with electron-rich aromatic systems including heteroaromatics is achieved by reversing the reactivity of sulfur in the presence of a suitable oxidant and strong acid. (Chemical Equation Presented).
Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2] nonane (CP-810,123), a novel α7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: Synthesis, SAR development, and in vivo efficacy in cognition models
O'Donnell, Christopher J.,Rogers, Bruce N.,Bronk, Brian S.,Bryce, Dianne K.,Coe, Jotham W.,Cook, Karen K.,Duplantier, Allen J.,Evrard, Edelweiss,Hajós, Mihaly,Hoffmann, William E.,Hurst, Raymond S.,Maklad, Noha,Mather, Robert J.,McLean, Stafford,Nedza, Frank M.,O'Neill, Brian T.,Peng, Langu,Qian, Weimin,Rottas, Melinda M.,Sands, Steven B.,Schmidt, Anne W.,Shrikhande, Alka V.,Spracklin, Douglas K.,Wong, Diane F.,Zhang, Andy,Zhang, Lei
experimental part, p. 1222 - 1237 (2010/08/05)
A novel α7 nAChR agonist, 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4- diazabicyclo[3.2.2]nonane (24, CP-810,123), has been identified as a potential treatment for cognitive deficits associated with psychiatric or neurological conditions including schizophrenia and Alzheimer's disease. Compound 24 is a potent and selective compound with excellent pharmaceutical properties. In rodent, the compound displays high oral bioavailability and excellent brain penetration affording high levels of receptor occupancy and in vivo efficacy in auditory sensory gating and novel object recognition. The structural diversity of this compound and its preclinical in vitro and in vivo package support the hypothesis that α7 nAChR agonists may have potential as a pharmacotherapy for the treatment of cognitive deficits in schizophrenia. 2009 American Chemical Society.
5-PYRIDINONE SUBSTITUTED INDAZOLES
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Page/Page column 62-63, (2009/04/24)
5-pyridinone substituted indazoles of the formula and methods of their use are presented.
Pharmaceutical compositions for CNS and other disorders
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Page 23, (2008/06/13)
The present invention relates to a method of treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant α7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant α7 nicotinic receptor agonist.
