- Design and synthesis of 1-(1-benzothiophen-7-yl)-1H-pyrazole, a novel series of G protein-coupled receptor 52 (GPR52) agonists
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G-protein-coupled receptor 52 (GPR52) is classified as an orphan Gs-coupled G-protein-coupled receptor. GPR52 cancels dopamine D2 receptor signaling and activates dopamine D1/N-methyl-D-aspartate receptors via intracellular cAMP accumulation. Therefore, G
- Nakahata, Takashi,Tokumaru, Kazuyuki,Ito, Yoshiteru,Ishii, Naoki,Setoh, Masaki,Shimizu, Yuji,Harasawa, Toshiya,Aoyama, Kazunobu,Hamada, Teruki,Kori, Masakuni,Aso, Kazuyoshi
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p. 1598 - 1608
(2018/02/27)
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- AMIDE COMPOUND
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A compound represented by the formula (I) wherein ring Cy1 is a 5-membered aromatic heterocycle optionally further substituted besides a group represented by -A-B, ring Cy2 is an optionally substituted benzene ring, ring Cy3 is an optionally substituted 5-membered aromatic heterocycle, ring Cy4 is an optionally substituted 6-membered aromatic ring, A is -CONRa- or -NRaCO-, Ra is a hydrogen atom or a substituent, B is a hydrogen atom or an optionally substituted C1-6 alkyl-group, X is an optionally substituted C1-2 alkylene, -Y-, -Y-CH2- or - CH2-Y-, Y is an oxygen atom, -NRb- or -S(O)m-, Rb is a hydrogen atom or a substituent, and m is 0, 1 or 2, provided that N-methyl-4-[2-[3,4,5-trimethoxyphenyl)amino]-1,3-benzoxazol-7-yl]thiophene-2-carboxamide is excluded, or a salt thereof, has an agonistic action on GPR52, and is useful as an agent for the prophylaxis or treatment of schizophrenia and the like.
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Page/Page column 64
(2012/11/13)
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- AMIDE COMPOUND
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A compound having GPR52 agonist activity or a salt thereof is provided. The compound can be provided as a preventive/therapeutic agent for schizophrenia or the like. The compound is represented by the following formula: wherein A represents —CONRa— or —NRaCO—, Ra represents a hydrogen atom or the like,B represents a hydrogen atom or the like,a ring Cy1 represents a six-membered aromatic ring which may have one or more substituents in addition to a group represented by -A-B,a ring Cy2 represents a six-membered ring which may be substituted with a halogen atom or the like,a ring Cy3 represents a five- or six-membered ring which may have one or more substituents;X represents C1-2 alkylene or the like,m represents an integer of 0 to 2, anda ring Cy4 represents a six-membered aromatic ring which may have one or more substituents.
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Page/Page column 68
(2010/03/04)
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