- HETEROCYCLIC COMPOUND
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Provided is a heterocyclic compound that may have a GCN2 inhibitory action, and is expected to be useful for the prophylaxis or treatment of GCN2 associated diseases including cancer and the like. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
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Paragraph 1118; 1119
(2019/06/17)
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- 3-(BIARYLOXY) PROPIONIC ACID DERIVATIVE
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A compound of the general formula (I): [wherein, R1 represents a halogen atom, or the like, R2 represents a hydrogen atom, or the like, R3 and R4, each independently, represent a hydrogen atom, a C1-4
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Page/Page column 45
(2012/07/14)
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- 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
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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.
- 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
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experimental part
p. 1222 - 1237
(2010/08/05)
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- AZABENZOXAZOLES FOR THE TREATMENT OF CNS DISORDERS
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The present invention relates to a7 nicotinic receptor agonists of formula (la) or (lb) as described herein and to a method for treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal an a7 nicotinic receptor agonist of formula (la) or (lb). It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant a7nicotinic receptor agonist of formula (la) or (lb).
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Page/Page column 42-43
(2010/11/30)
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