- SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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PROBLEM TO BE SOLVED: To provide a novel compound having an integrin α4 inhibiting action. SOLUTION: A sulfonamide derivative or pharmaceutically acceptable salt thereof has a structure represented by a general formula (I) using specific substituents A an
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Paragraph 0076
(2019/03/28)
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- Discovery of a potent, cell penetrant, and selective p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain chemical probe
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P300/CREB binding protein associated factor (PCAF/KAT2B) and general control nonderepressible 5 (GCN5/KAT2A) are multidomain proteins that have been implicated in retroviral infection, inflammation pathways, and cancer development. However, outside of viral replication, little is known about the dependence of these effects on the C-terminal bromodomain. Herein, we report GSK4027 as a chemical probe for the PCAF/GCN5 bromodomain, together with GSK4028 as an enantiomeric negative control. The probe was optimized from a weakly potent, nonselective pyridazinone hit to deliver high potency for the PCAF/GCN5 bromodomain, high solubility, cellular target engagement, and ≥18000-fold selectivity over the BET family, together with ≥70-fold selectivity over the wider bromodomain families.
- Humphreys, Philip G.,Bamborough, Paul,Chung, Chun-Wa,Craggs, Peter D.,Gordon, Laurie,Grandi, Paola,Hayhow, Thomas G.,Hussain, Jameed,Jones, Katherine L.,Lindon, Matthew,Michon, Anne-Marie,Renaux, Jessica F.,Suckling, Colin J.,Tough, David F.,Prinjha, Rab K.
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supporting information
p. 695 - 709
(2017/02/05)
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- SULFONAMIDE DERIVATIVES AND PHARMACEUTICAL APPLICATIONS THEREOF
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PROBLEM TO BE SOLVED: To provide novel compounds having excellent α4 integrin inhibitory action. SOLUTION: The invention relates to sulfonamide derivatives represented by the general formula (I) in the figure, or pharmaceutically acceptable salts thereof, or prodrugs thereof. (In the formula, a, b, c, d, D, E, R11, B, e, f, g, h and W are as defined herein.) SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
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Paragraph 0065
(2016/10/08)
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- DERIVATIVES OF 2H PYRIDAZIN- 3 -ONES, THEIR PREPARATION AND THEIR USE AS SCD-1 INHIBITORS
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The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: -R1 represents one or more groups such as: trif luoromethyl, halogen such as F, C1, -when n=m=1, W represents CH then Y represents oxygen, -U represents: ? either - (C=O) CH2NH- and is branched at position 4 of pyridazinone, then R2 represents H, ? or -(C=O)NH- and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, - R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enyzme inhibitors for the treatment of obesitz, tzpe-2 diabetes and lipid disorders.
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Page/Page column 47
(2011/02/24)
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- Concurrent Alkylation-Methoxylation of 4,5-Dihalopyridazin-6-ones and Synthesis of 5-Halo-4-hydroxypyridazin-6-ones
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1-Alkyl-5-halo-4-methoxypyridazin-6-ones were synthesized from 1-alkyl-4,5-dihalopyridazin-6-ones by the concurrent alkylation-methoxylation. 1-Alkyl-5-halo-4-hydroxypyridazin-6-ones were also prepared.
- Cho, Su-Dong,Choi, Woo-Yong,Yoon, Yong-Jin
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p. 1579 - 1582
(2007/10/03)
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