5722-94-1Relevant academic research and scientific papers
NOVEL DIOXOLOISOQUINOLINONE DERIVATIVES AND USE THEREOF
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, (2022/02/28)
The present invention relates to novel dioxoisoquinolinone derivative compounds and use thereof. More specifically, the present invention relates to novel dioxoisoquinolinone derivative compounds with inhibition activity of EZH1(Enhancer of zeste homolog 1) and/or EZH2(Enhancer of zeste homolog 2) activity, a pharmaceutically acceptable salt thereof, and/or pharmaceutical compositions comprising the same.
NOVEL HETEROTRICYCLIC DERIVATIVE COMPOUND AND USE OF SAME
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Paragraph 0062-0063, (2022/01/03)
The present disclosure relates to novel heterotricyclic derivative compounds and the use thereof, and more particularly, to novel heterotricyclic derivative compounds having inhibitory activity against EZH1 (enhancer of zeste homolog 1) and/or EZH2 (enhancer of zeste homolog 2) activity, pharmaceutically acceptable salts thereof, or pharmaceutical compositions containing these compounds.
Evidence for a trianion intermediate in the metalation of 4-hydroxy-6,7-dimethoxy-8-methyl-2-naphthoic acid. methodology and application to racemic 5,5′-didesisopropyl-5,5′-dialkylapogossypol derivatives
Le, Tin Thanh,Chau, Nguyet Trang Thanh,Nguyen, Tai Tan,Brien, Josselin,Thai, Trieu Tien,Nourry, Arnaud,Castanet, Anne-Sophie,Nguyen, Kim Phi Phung,Mortier, Jacques
supporting information; body text, p. 601 - 608 (2011/03/20)
The metalation of 4-hydroxy-6,7-dimethoxy-8-methyl-2-naphthoic acid (8) affording trianion 6 is presented and applied to the regioselective efficient construction of a series of 5,5′-didesisopropyl-5,5′- dialkylapogossypol derivatives 3 that are potent pa
DERIVES DU GOSSYPOL ET DE L'APOGOSSYPOL, LEURS PREPARATIONS ET LEURS APPLICTIONS
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Page/Page column 14, (2011/01/05)
Gossypol and apogossypol derivatives of general formula (1), preparation thereof and use thereof.
TROPANE COMPOUNDS
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Page/Page column 387, (2009/05/30)
A compound according to Formula I or II: (I) or (II) wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
Competition of substituents for ortho direction of metalation of veratric acid
Chau, Nguyet Trang Thanh,Nguyen, Thi Huu,Castanet, Anne-Sophie,Nguyen, Kim Phi Phung,Mortier, Jacques
, p. 10552 - 10557 (2008/12/23)
LTMP (5 equiv) metalates randomly veratric acid (1). Under external quench conditions, the thermodynamically more stable lithium 2-lithio-3,4-dimethoxybenzoate (2) reacts with a variety of electrophiles to give versatile building units that are not easily accessible by conventional means. Under in situ quench conditions (LTMP/TMSCl), a reversal of regioselectivity is observed and 6-trimethylsilyl-3,4-dimethoxybenzoic acid (10) is formed predominantly.
A practical synthesis of 3,4-dimethoxy-o-toluic acid
Connolly, Terrence J.,Matchett, Michael,McGarry, Patrick,Sukhtankar, Sunil,Zhu, Jiang
, p. 624 - 627 (2013/09/02)
A streamlined, telescoped process has been developed for the preparation of 3,4-dimethoxy-o-toluic acid, starting with economical and readily available 2,3-dimethoxybenzaldehyde. Catalytic reduction of the aldehyde functional group generated dimethoxytolu
HIV protease inhibitors
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, (2008/06/13)
HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
HIV protease inhibitors
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, (2008/06/13)
HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.
Catechol O-methyltransferase. 12. Affinity Labeling the Active Site with the Oxidation Products of 5,6-Dihydroxyindole
Borchardt, Ronald T.,Bhatia, Pramila
, p. 263 - 271 (2007/10/02)
5,6-Dihydroxyindole (5,6-DHI) and a series of 4- and/or 7-methylated analogues of 5,6-DHI have been synthesized and evaluated for their ability to inactivate purified liver rat catechol O-methyltransferase (COMT).The inactivation of COMT by these agents could be prevented by excluding oxygen from the incubation mixtures, indicating the necessity for their oxidation to the corresponding aminochromes.Substrate protection studies and kinetic studies suggested that the loss of enzyme activity resulted from the modification of a crucial amino acid residue at the active site of COMT through reaction with the quinoid oxidation products.The COMT inhibitory activity of the 4- and/or 7-methylazed analogues of 5,6-DHI argue against a mechanism involving a 1,4 Michael addition reaction at positions 4 or 7 on the aminochrome.Cnsidering the number of potential eletrophilic centers on the basic aminochrome structure, the site of the reaction might change depending on the aromatic substitution pattern.The preferred pathway of reaction may be determined in part by the juxtaposition of the protein nucleophile to the possible sites of attack on the electrophilic ligand but also in part on the reactivity of the electrophilic site which might change with substitution on the aromatic ring.
