- Self-Replication and Amplification of Enantiomeric Excess of Chiral Multifunctionalized Large Molecules by Asymmetric Autocatalysis
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Self-replication of large chiral molecular architectures is one of the great challenges and interests in synthetic, systems, and prebiotic chemistry. Described herein is a new chemical system in which large chiral multifunctionalized molecules possess asymmetric autocatalytic self-replicating and self-improving abilities, that is, improvement of their enantioenrichment in addition to the diastereomeric ratio. The large chiral multifunctionalized molecules catalyze the production of themselves with the same structure, including the chirality of newly formed asymmetric carbon atoms, in the reaction of the corresponding achiral aldehydes and reagent. The chirality of the large multifunctionalized molecules controlled the enantioselectivity of the reaction in a highly selective manner to construct multiple asymmetric stereogenic centers in a single reaction.
- Kawasaki, Tsuneomi,Nakaoda, Mai,Takahashi, Yutaro,Kanto, Yusuke,Kuruhara, Nanako,Hosoi, Kenji,Sato, Itaru,Matsumoto, Arimasa,Soai, Kenso
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- Design and synthesis of diazine-based panobinostat analogues for HDAC8 inhibition
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Guided by computational analysis, herein we report the design, synthesis and evaluation of four novel diazine-based histone deacetylase inhibitors (HDACis). The targets of interest (TOI) are analogues of panobinostat, one of the most potent and versatile HDACi reported. By simply replacing the phenyl core of panobinostat with that of a diazine derivative, docking studies against HDAC2 and HDAC8 revealed that the four analogues exhibit inhibition activities comparable to that of panobinostat. Multistep syntheses afforded the visualized targets TOI1, TOI2, TOI3-rev and TOI4 whose biological evaluation confirmed the strength of HDAC8 inhibition with TOI4 displaying the greatest efficacy at varying concentrations. The results of this study lay the foundation for future design strategies toward more potent HDACis for HDAC8 isozymes and further therapeutic applications for neuroblastoma.
- Balasubramaniam, Sivaraman,Vijayan, Sajith,Goldman, Liam V.,May, Xavier A.,Dodson, Kyra,Adhikari, Sweta,Rivas, Fatima,Watkins, Davita L.,Stoddard, Shana V.
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p. 628 - 637
(2020/05/18)
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- 2 -Chloro -5-aldehyde pyrimidine and preparation method thereof
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The invention discloses 2-chloro-5-aldehyde pyrimidine and a preparation method thereof. The preparation method comprises the following steps: step 1, adding Arnold salt into a solvent to obtain an arnold salt solution, the chemical structural formula of the Arnold salt is as shown in the specification (I); and step 2, adding chloroformamidine hydrochloride and an alkali into the Arnold salt solution to carry out ring-closing reaction so as to obtain the 2-chloro-5-aldehyde pyrimidine.
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Paragraph 0052-0071
(2019/07/04)
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- Preparation method of 2-chloro-5-aldehyde pyrimidine
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The invention discloses a preparation method of 2-chloro-5-aldehyde pyrimidine. The preparation method includes the steps: a) performing hydrolysis reaction on 2-methoxyl-5-aldehyde pyrimidine servingas an initial raw material under acidic conditions to obtain 2-hydroxy-5-aldehyde pyrimidine, namely, a compound I; b) performing nucleophilic substitution reaction on the compound I and phosphorus oxychloride to obtain the 2-chloro-5-aldehyde pyrimidine, namely, a compound II. The preparation method is short in synthetic route, simple and convenient in operation, high in product yield and low insynthesis cost, raw materials are low in cost and easy to obtain, and industrial production requirements are met.
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Paragraph 0059-0095
(2019/03/08)
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- NUCLEIC ACID-BINDING PHOTOPROBES AND USES THEREOF
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The present invention relates to photoactivatable compounds and methods of use thereof for determining binding site and other structural information about RNA transcripts. The invention also provides methods of identifying RNA transcripts that bind compounds and are thus druggable, methods of screening drug candidates, and methods of determining drug binding sites and/or accessible or reactive sites on a target RNA.
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Paragraph 0050
(2019/06/17)
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- COMPOUNDS AND METHODS FOR MODULATING RNA FUNCTION
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 0076; 00629
(2018/02/28)
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- cGAS ANTAGONIST COMPOUNDS
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Disclosed are novel compounds of Formula (I) that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
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Paragraph 0231
(2017/11/06)
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- COMPOUNDS AND METHODS OF TREATING RNA-MEDIATED DISEASES
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Sheet 105/122
(2017/12/27)
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- FGFR4 INHIBITORS
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Methods, compounds, pharmaceutical compositions, and methods of preparing medicaments for treating hepatocellular carcinoma having an altered FGFR4 and/or FGF19 status.
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Page/Page column 60; 61
(2016/10/31)
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