- NOVEL HISTONE METHYLTRANSFERASE INHIBITORS
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The present invention relates to novel compounds of formula (I) as defined herein. The compounds are inhibitors of histone methyltransferases of the seven-beta-strand family, in particular of KMT9.
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Page/Page column 30; 84
(2021/04/01)
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- ERBB/BTK INHIBITORS
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Disclosed are compounds inhibiting ErbBs (e. g., EGFR or Her 2), especially mutant forms of ErbBs, and BTK, pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof and pharmaceutical compositions comprising the compounds. The compou
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Page/Page column 102; 60
(2019/08/26)
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- Hofmann-type rearrangement of imides by in situ generation of imide-hypervalent iodines(III) from iodoarenes
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The Hofmann-type rearrangement of aromatic and aliphatic imides using a hypervalent iodine(III) reagent generated in situ from PhI, m-CPBA, and TsOH·H2O proceeded in the presence of a base in alcohol to provide anthranilic acid derivatives and amino acid derivatives in high yields, respectively. This reaction proceeds through a tandem reaction via alcoholysis followed by a Hofmann rearrangement promoted by the formation of an imide-λ3-iodane intermediate.
- Moriyama, Katsuhiko,Ishida, Kazuma,Togo, Hideo
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supporting information; experimental part
p. 946 - 949
(2012/05/05)
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- Protecting-group-free synthesis of a dual CCK1/CCK2 receptor antagonist
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In our pursuit of an efficient, protecting-group-free synthesis of the dual CCK1/CCK2 receptor antagonist 1, we have developed chemoselective conditions for sulfonamide formation reaction in pure water and a PhNMe2 mediated carboxamide formatio
- Liu, Jing,Deng, Xiaohu,Fitzgerald, Anne E.,Sales, Zachary S.,Venkatesan, Hariharan,Mani, Neelakandha S.
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p. 2654 - 2660
(2011/05/08)
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- Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists II: Tuning of receptor selectivity and in vivo efficacy
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In the previous article we demonstrated how certain CCK2R-selective anthranilic amides could be structurally modified to afford high-affinity, selective CCK1R activity. We now describe our efforts at modulating and optimizing the CCK1R and CCK2R affinitie
- Pippel, Marna,Boyce, Kristen,Venkatesan, Hariharan,Phuong, Victor K.,Yan, Wen,Barrett, Terrance D.,Lagaud, Guy,Li, Lina,Morton, Magda F.,Prendergast, Clodagh,Wu, Xiaodong,Shankley, Nigel P.,Rabinowitz, Michael H.
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scheme or table
p. 6376 - 6378
(2010/05/02)
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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 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 8
(2008/06/13)
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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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- SULFONAMIDE COMPOUNDS
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Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.
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Page/Page column 19
(2010/10/20)
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- Quinoxaline compounds
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Certain amidophenyl-sulfonylamino-quinoxaline compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
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Page/Page column 15
(2008/06/13)
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- Synthesis and pharmacological studies at the Gly/NMDA, AMPA and Kainate receptors of new oxazolo[4,5-c]quinolin-4-one derivatives bearing different substituents at position-2 and on the fused benzo ring
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The synthesis and biological evaluation at the Gly/NMDA, AMPA and Kainate receptors of new oxazolo[4,5-c]quinolin-4-one derivatives are reported. Different substituents were introduced at the 2-position (mercapto, carbonyl and methyl groups) and on the fu
- Calabri, Francesca Romana,Colotta, Vittoria,Catarzi, Daniela,Varano, Flavia,Lenzi, Ombretta,Filacchioni, Guido,Costagli, Chiara,Galli, Alessandro
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p. 897 - 907
(2007/10/03)
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