61563-27-7Relevant academic research and scientific papers
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
-
Paragraph 00275, (2017/09/27)
The present invention provides compounds, compositions thereof, and methods of using the same.
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
-
Paragraph 00249, (2017/10/06)
The present invention provides compounds, compositions thereof, and methods of using the same.
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
-
Paragraph 00316-00318, (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.
CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
-
Page/Page column 80, (2010/11/27)
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
Heterocyclic compounds
-
Page/Page column 12, (2010/02/14)
The inventive subject matter relates to compounds, pharmaceutical compositions, and kits containing a heterocyclic compound represented by the formula (I) wherein R is an alkyl group optionally having substituent(s) etc., X is an amino group optionally having substituent(s), Y1 and Y2 are nitrogen atoms etc., an isomer or solvate thereof or a pharmaceutically acceptable salt thereof as an active ingredient.
INHIBITORS OF MONOAMINE UPTAKE
-
Page 132, (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.
AMINO ACID DERIVATIVES AND THEIR USE AS THROMBIN INHIBITORS
-
, (2008/06/13)
There is provided compounds of formula I, wherein R 1, R 2, R 3, R x, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.
Benzyl alcohols and their lower alkanecarboxylic acid esters
-
, (2008/06/13)
Benzene derivatives of the general formula STR1 where Hal is halogen, R1 is a hydrocarbon radical of 1 to 18 carbon atoms, R2 is hydrogen or alkyl of 1 to 6 carbon atoms and X is hydrogen or halogen, are prepared by a process in which a toluene derivative of the general formula STR2 is electrochemically oxidized in the presence of an acid of the formula R2 --COOH (III). Novel benzene derivatives of the general formula STR3 where R3 is hydrogen or an R2 --CO-- radical but R1 cannot be methyl if X is hydrogen, and of the general formula STR4 where R4 is a branched or cyclic alkyl radical of 3 to 12 carbon atoms, but R4 cannot be isopropyl if X is hydrogen. The compounds of formulas IV and VI are intermediates for crop protecting agents, e.g. pyrethroids.
Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase
-
, (2008/06/13)
Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase using 7 and/or 8 substituted 1,2,3,4-tetrahydroisoquinoline compounds.
