439607-87-1Relevant academic research and scientific papers
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.
NOVEL PIPERAZINES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF
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Page/Page column 80, (2008/06/13)
Disclosed are novel piperazine derivatives that act as agonists of the α7 nAChR. Also disclosed are phannaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.
Pharmaceutical compositions for CNS and other disorders
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Page 17, (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.
Pharmaceutical composition for the treatment of CNS and other disorders
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, (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 pharma
Benzoxazoline and benzimidazoline derivatives as novel aldose reductase inhibitors, part 2: Lead optimization
Nakao, Kazuya,Asao, Masaaki,Shirai, Hiroki,Saito, Kiyoshi,Moriya, Tamon,Iwata, Hiroshi,Matsumoto, Mamoru,Matsuoka, Yuzo,Shimizu, Ryo
, p. 631 - 642 (2007/10/03)
We designed novel aldose reductase inhibitors, benzoxazoline and benzimidazoline derivatives, based on lead evolution from spiroquinazolinones. In order to optimize in vivo activity in the lens, variously substituted derivatives were synthesized. The relationship between structure and in vitro activity was also analyzed by comparative molecular field analysis. The optimized compound exhibited high potency in the lens.
