- NOVEL SUBSTITUTED-1-H-QUINAZOLINE-2,4-DIONE DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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Disclosed herein are novel substituted-1H-quinazoline-2,4-dione derivatives, a preparation method thereof, and a pharmaceutical composition containing the same. The novel substituted-1H-quinazoline-2,4-dione derivatives are excellent in binding affinity a
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Page/Page column 8
(2009/08/18)
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- NOVEL SUBSTITUTED-1H-QUINAZOLINE-2,4-DIONE DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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Disclosed herein are novel substituted-lH-quinazoline-2,4-dione derivatives, a preparation method thereof, and a pharmaceutical composition containing the same. The novel substituted- lH-quinazoline-2,4-dione derivatives are excellent in binding affinity
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Page/Page column 25
(2008/06/13)
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- Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists
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A 5,7-dichloro-3-phenyl-3-methyl-quinoline-2,4-dione (11a) has been identified in a random screen as a lead for 5-HT6 antagonist. During the lead optimization process, several analogs were synthesized and their biological activities were investigated. Within this series, several compounds display high binding affinity and selectivity for the 5-HT6 receptor. In particular, 3-(4-hydroxyphenyl)-3-methyl-quinoline-2,4-dione (12f) exhibits high affinity (Ki = 12.3 nM) for 5-HT6 receptor with good selectivity over other serotonin and dopamine (D1-D4) receptor subtypes. In a functional adenylyl cyclase stimulation assay, this compound exhibited considerable antagonistic activity (IC50 = 0.61 μM).
- Seong, Churl Min,Park, Woo Kyu,Park, Chul Min,Kong, Jae Yang,Park, No Sang
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p. 738 - 743
(2008/12/23)
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- 3-aryl-3-methyl-quinoline-2,4-diones, preparation method thereof and pharmaceutical composition containing same
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The present invention relates to compounds of 3-aryl-3-methyl-quinoline-2,4-diones , or a pharmaceutically acceptable salt thereof acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of 3-aryl-3-methyl-quinoline-2,4-diones according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders because of its excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors.
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Page/Page column 10
(2008/06/13)
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- 3-aryl--3-methyl-quinoline-2, 4-diones, preparation method thereof, and pharmaceutical composition containing the same
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The present invention relates to compounds of 3-aryl-3-methyl-quinoline-2,4-diones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of 3-aryl-3-methyl-quinoline-2,4-diones according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders because of its excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors.
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Page/Page column 7
(2008/06/13)
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- Oxindole derivative
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An oxindole of Formula 1 or a prodrug thereof, or a pharmaceutically acceptable salt thereof is useful for growth hormone releaser: wherein R1, R2, R3and R4are independently hydrogen, optionally substituted alkyl etc; R5is optionally substituted aryl or optionally substituted heteroaryl; Z is —O— or —NH—; one of W1and W2is hydrogen, alkyl or —Y—CON(R10)R11; the other of W1and W2is n is 1, 2 or 3; m is 0, 1, 2 or 3; Y is single bond or C1-C3alkylene; R6and R7are independently hydrogen, optionally substituted alkyl etc; R8and R9are independently hydrogen, optionally substituted alkyl etc; R10and R11are independently hydrogen, alkyl etc.
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