844647-17-2Relevant academic research and scientific papers
NOVEL HISTONE METHYLTRANSFERASE INHIBITORS
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Page/Page column 30; 84, (2021/04/01)
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.
ERBB/BTK INHIBITORS
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Page/Page column 102; 60, (2019/08/26)
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
Hofmann-type rearrangement of imides by in situ generation of imide-hypervalent iodines(III) from iodoarenes
Moriyama, Katsuhiko,Ishida, Kazuma,Togo, Hideo
supporting information; experimental part, p. 946 - 949 (2012/05/05)
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.
Protecting-group-free synthesis of a dual CCK1/CCK2 receptor antagonist
Liu, Jing,Deng, Xiaohu,Fitzgerald, Anne E.,Sales, Zachary S.,Venkatesan, Hariharan,Mani, Neelakandha S.
, p. 2654 - 2660 (2011/05/08)
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
Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists II: Tuning of receptor selectivity and in vivo efficacy
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.
scheme or table, p. 6376 - 6378 (2010/05/02)
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
Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists
Seong, Churl Min,Park, Woo Kyu,Park, Chul Min,Kong, Jae Yang,Park, No Sang
, p. 738 - 743 (2008/12/23)
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).
SULFONAMIDE COMPOUNDS
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Page/Page column 19, (2010/10/20)
Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.
3-aryl--3-methyl-quinoline-2, 4-diones, preparation method thereof, and pharmaceutical composition containing the same
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Page/Page column 8, (2008/06/13)
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.
3-aryl-3-methyl-quinoline-2,4-diones, preparation method thereof and pharmaceutical composition containing same
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Page/Page column 10, (2008/06/13)
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.
Quinoxaline compounds
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Page/Page column 15, (2008/06/13)
Certain amidophenyl-sulfonylamino-quinoxaline compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
