- Target protein degradation inducing compound, preparation method thereof and pharmaceutical composition for preventing or treating targeted protein related diseases containing the same as an active ingredient
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The present invention relates to a degraducer for inducing the decomposition of target protein, a producing method thereof, and a pharmaceutical composition for preventing or treating target protein-related diseases by containing the degraducer as an active ingredient. A novel compound represented by chemical formula 1, ULB-L-PTM, by the present invention, as a degraducer compound inducing the decomposition of target protein using cereblon E3 ubiquitin ligase, is able to significantly achieve a target protein degradation-inducing activity with an excellent binding activity of a cereblon E3 ubiquitin ligase binder thereby, being able to achieve an excellent protein degradation activity by targeting protein or polypeptide related to various diseases. The bromodomain-containing pharmaceutical composition for preventing or treating protein-related diseases or conditions contains the novel compound represented by chemical formula 1 as an active ingredient and has a useful effect of providing a health functional food composition for prevention or improvement.(AA) Example 22 (nM, 24h)COPYRIGHT KIPO 2020
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Paragraph 0970; 0972-0974
(2020/05/01)
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- Synthesis of Cyclic and Acyclic Nucleoside Phosphonates and Sulfonamides Derived from 6-(Thiophen-2-yl)-7-fluoro-7-deazapurine
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Ribonuclosides derived from 6-hetaryl-7-dezapurines are potent cytostatics, but their mechanism of action is unknown. Here we designed and synthesized a series of cyclic and acyclic nucleoside phosphonates, as well as carboxy, cyano, sulfo, and sulfonamide acyclic analogues derived from 6-thiophen-2-yl-7-deazapurine and 7-fluoro-6-thiophen-2-yl-7-deazapurine as ribonucleoside monophosphate mimics. None of these analogues exerted significant cytotoxic and antiviral activity.
- Malnuit, Vincent,Smoleń, Sabina,Tichy, Michal,Po?tová Slavětínská, Lenka,Hocek, Michal
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p. 5409 - 5423
(2019/08/30)
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- AMINO SULFONYL COMPOUNDS
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Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
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Paragraph 0496; 0497
(2018/06/12)
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- Containing oligomeric ethylene oxide unit and its preparation method for compound silicon nitrile class, use in lithium batteries
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The invention provides silicone-nitrile compounds containing low polyoxyethylene units, which as shown in formula I, as well as a preparation method for the compounds and application of the compounds in a lithium battery. A nitrile group has characteristic capable of improving a dielectric constant of the substances; the nitrile group is introduced into organic silicon by the compounds, so that oxidation resistance and salt dissolving capacity of an organic silicon-based material are improved; meanwhile, high safety of an organic silicon solvent containing the low polyoxyethylene (EO) unit and ability of assisting propylene carbonate (PC) to form a film are retained. The silicone-nitrile compounds containing low polyoxyethylene units disclosed by the invention can be used as an ethylene carbonate-based or propylene carbonate-based cosolvent for being applied to the lithium battery. Compared with the conventional lithium battery electrolyte material, the silicone-nitrile compounds disclosed by the invention have a higher dielectric constant, a simpler molecular structure, and a simpler and more economical synthesis process.
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Paragraph 0030-0032
(2017/02/09)
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- SYNTHESIS AND TRANSFORMATION OF OXYGEN-CONTAINING MONO- AND DINITRILES. I. REACTION OF β-CHLOROPROPIONITRILES WITH DIOLS
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In the reaction of β-chloropropionitrile with diols 7-11-membered oxygen-containing mono- and dinitriles were synthesized in ratios of 3:2 respectively, irrespective of the ratio of the initial components.Alkaline hydrolysis of oxygen-containing mononitriles with a weak solution of hydrogen peroxide leads to the formation of the corresponding amides, while alkaline hydrolysis of the oxygen-containing dinitriles leads to two products (amidonitriles and diamides).
- Movsumzade, E. M.,Rasulbekova, T. I.,Kulieva, D. A.,Aliev, G. R.,Movsumzade, S. M.
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p. 2132 - 2135
(2007/10/02)
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