61563-28-8Relevant academic research and scientific papers
2 - Chloro -3 - methyl benzoic acid and intermediate preparation method (by machine translation)
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Paragraph 0079; 0086; 0087, (2018/10/11)
The invention discloses a 2 - chloro - 3 - methyl benzoic acid and intermediate preparation method. A 2 - chloro - 3 - methyl benzoic acid and intermediate preparation method, comprising the following steps, in the oxygen pressure is 0.1 mpa - 0.8 mpa under the condition of, under the action of the catalyst and promoter, the 2, 6 - dimethyl chlorobenzene to carry out oxidation reaction, can be; wherein said 2, 6 - dimethyl chlorobenzene and the oxygen molar amount ratio of 1: 1.8 - 1: 2.2. The 2 - chloro - 3 - methyl benzoic acid, in order to industrially easily available raw materials for the reaction, after treatment is simple, high yield, purity is good, small pollution to the environment, is more suitable for industrial. (by machine translation)
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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Paragraph 00276, (2017/09/27)
The present invention provides compounds, compositions thereof, and methods of using the same.
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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Paragraph 00250, (2017/10/06)
The present invention provides compounds, compositions thereof, and methods of using the same.
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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Paragraph 00316; 00319; 00320, (2017/10/06)
The present invention provides compounds, compositions thereof, and methods of using the same.
Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL)
Borkin, Dmitry,Pollock, Jonathan,Kempinska, Katarzyna,Purohit, Trupta,Li, Xiaoqin,Wen, Bo,Zhao, Ting,Miao, Hongzhi,Shukla, Shirish,He, Miao,Sun, Duxin,Cierpicki, Tomasz,Grembecka, Jolanta
, p. 892 - 913 (2016/02/23)
Development of potent small molecule inhibitors of protein-protein interactions with optimized druglike properties represents a challenging task in lead optimization process. Here, we report synthesis and structure-based optimization of new thienopyrimidine class of compounds, which block the protein-protein interaction between menin and MLL fusion proteins that plays an important role in acute leukemias with MLL translocations. We performed simultaneous optimization of both activity and druglike properties through systematic exploration of substituents introduced to the indole ring of lead compound 1 (MI-136) to identify compounds suitable for in vivo studies in mice. This work resulted in the identification of compound 27 (MI-538), which showed significantly increased activity, selectivity, polarity, and pharmacokinetic profile over 1 and demonstrated a pronounced effect in a mouse model of MLL leukemia. This study, which reports detailed structure-activity and structure-property relationships for the menin-MLL inhibitors, demonstrates challenges in optimizing inhibitors of protein-protein interactions for potential therapeutic applications.
INHIBITORS OF MONOAMINE UPTAKE
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Page 133, (2010/02/07)
N,N-disubstituted 4-amino-piperidines of the general Formula (I) are inhibitors of the uptake of serotonin and/or norepinephrine and/or dopamine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.
Synthesis of 9,10-dihydrosilaanthracenes with substituents ortho to the silicon and methylene bridges
Bedard, Thomas C.,Corey, Joyce Y.,Lange, Lura D.,Rath, Nigam P.
, p. 261 - 272 (2007/10/02)
The generation of 9,10-dihydrosilaanthracenes with substituents on benzo ring carbons, specifically in the 4,5-positions adjacent to the methylene bridge, has been developed.Attempts to prepare the 1,8-isomer where the substituents are adjacent to the silicon bridge are also described.The diarylmethane precursors to the substituted 9,10-dihydrosilaanthracenes required the synthesis of 2,3-dihalotoluenes as well as isomeric 2,6-disubstituted benzaldehydes which were then condensed to diarylmethanols through the Grignard reagents.Ring closure to the 4,5-dimethyl-9,9-dialkyl-9,10-dihydro-9-silaanthracene, I, required the use of Rieke magnesium.The structure of I (alkyl = iPr) was determined and demonstrates that the introduction of substituents adjacent to the methylene bridge causes the dihydrosilaanthracene framework to become nearly planar with a dihedral (or butterfly) angle of 170 deg C.
Vilsmeier reaction studies on some α,β-unsaturated alkenones
Sreenivasulu, M.,Rao, G. S. Krishna
, p. 494 - 495 (2007/10/02)
α,β-Unsaturated alkenones (1a-g) are converted into chlorobenzenemono-, di- and tricarboxaldehydes (2a-h) under Vilsmeier reaction conditions.Besides six known chlorobenzaldehydes the route affords, in a one-pot reaction, two new members of this class of compounds, 3-methyl-(2d) and 3,5-dimethyl-(2h)-2-chlorobenzaldehydes.
Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase
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, (2008/06/13)
Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase using 7 and/or 8 substituted 1,2,3,4-tetrahydroisoquinoline compounds.
