71022-90-7Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AS INHIBITORS OF HPK1
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Page/Page column 203, (2021/01/29)
This disclosure relates to heterocyclics as inhibitors of HPK1, in particular relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising said compound that useful for treatment of HPK1 mediated diseases and conditions such as cancer. (I)
A Suite of “Minimalist” Photo-Crosslinkers for Live-Cell Imaging and Chemical Proteomics: Case Study with BRD4 Inhibitors
Pan, Sijun,Jang, Se-Young,Wang, Danyang,Liew, Si Si,Li, Zhengqiu,Lee, Jun-Seok,Yao, Shao Q.
supporting information, p. 11816 - 11821 (2017/09/06)
Affinity-based probes (AfBPs) provide a powerful tool for large-scale chemoproteomic studies of drug–target interactions. The development of high-quality probes capable of recapitulating genuine drug–target engagement, however, could be challenging. “Mini
DEUTERATED DIAMINOPYRIMIDINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH COMPOUNDS
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Paragraph 0097; 0103, (2016/05/09)
The present invention related to deuterated diaminopyrimidine compounds and pharmaceutical compositions comprising such compounds. In particular, disclosed are the deuterated diaminopyrimidine compounds shown as formula (I), and the pharmaceutical compositions comprising such compounds or crystal form, pharmaceutically acceptable salts, hydrates or solvates thereof. The compounds of the present invention can be used for treating and/or preventing protein kinase-associated diseases, such as cell proliferative disease, cancer, immune disease and the like.
Aminoheteroaryl benzamides as kinase inhibitors
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Page/Page column 222; 223, (2016/02/15)
The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
Further studies on bis-charged tetraazacyclophanes as potent inhibitors of small conductance Ca2+-activated K+ channels
Yang, Donglai,Arifhodzic, Lejla,Ganellin, C. Robin,Jenkinson, Donald H.
supporting information, p. 907 - 923 (2013/07/27)
Previously, quinolinium-based tetraazacyclophanes, such as UCL 1684 and UCL 1848, have been shown to be extraordinarily sensitive to changes in chemical structure (especially to the size of the cyclophane system) with respect to activity as potent non-peptidic blockers of the small conductance Ca 2+-activated K+ ion channels (SKCa). The present work has sought to optimize the structure of the linking chains in UCL 1848. We report the synthesis and SKCa channel-blocking activity of 29 analogues of UCL 1848 in which the central CH2 of UCL 1848 is replaced by other groups X or Y = O, S, CF2, CO, CHOH, CC, CHCH, CHMe to explore whether subtle changes in bond length or flexibility can improve potency still further. The possibility of improving potency by introducing ring substituents has also been explored by synthesizing and testing 25 analogues of UCL 1684 and UCL 1848 with substituents (NO2, NH2, CF 3, F, Cl, CH3, OCH3, OCF3, OH) in the 5, 6 or 7 positions of the aminoquinolinium rings. As in our earlier work, each compound was assayed for inhibition of the afterhyperpolarization (AHP) in rat sympathetic neurons, an action mediated by the SK3 subtype of the SK Ca channel. One of the new compounds (39, R7 = Cl, UCL 2053) is twice as potent as UCL 1848 and UCL 1684: seven are comparable in activity.
Inhibitors of the mevalonate pathway of streptococcus pneumoniae
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Page/Page column 11, (2011/08/04)
Compounds and related methods as can be used for selective mevalonate pathway inhibitors.
Mevalonate analogues as substrates of enzymes in the isoprenoid biosynthetic pathway of Streptococcus pneumoniae
Kudoh, Takashi,Park, Chan Sun,Lefurgy, Scott T.,Sun, Meihao,Michels, Theodore,Leyh, Thomas S.,Silverman, Richard B.
experimental part, p. 1124 - 1134 (2010/04/26)
Survival of the human pathogen Streptococcus pneumoniae requires a functional mevalonate pathway, which produces isopentenyl diphosphate, the essential building block of isoprenoids. Flux through this pathway appears to be regulated at the mevalonate kina
An efficient approach to asymmetric synthesis of dipeptide β-turn mimetics: Indolizidinone amino acids
Wang, Wei,Xiong, Chiyi,Hruby, Victor J
, p. 3159 - 3161 (2007/10/03)
Azabicyclo[X.Y.0] alkane amino acids are rigid dipeptide β-turn mimetics with great potential applications for drug discovery. The lack of efficient methods to synthesize these compounds is a major bottleneck in this field. Herein we report an efficient a
A New Approach towards Synthesis of Linear Natural Phenolic Products
Singh, Serjinder,Singh, Iqbal
, p. 586 - 588 (2007/10/02)
A repetitive strategy for the synthesis of linear natural phenolic products involving reaction of two lithium enolate molecules of t-butyl acetate with esters of dicarboxylic acids is reported.
