59034-23-0Relevant academic research and scientific papers
Origin of the defensive secretion of the leaf beetle Chrysomela lapponica
Schulz, Stefan,Gross, Juergen,Hilker, Monika
, p. 9203 - 9212 (1997)
The larvae of the European leaf beetle Chrysomela lapponica use esters of isobutyric acid and (S)-2-methylbutyric acid as defensive secretion. The acids are formed by the larvae from amino acids, as could be shown by experiments with labelled compounds. T
Dual inhibitors of AR and BET and use thereof
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Paragraph 0075; 0082; 0083, (2020/04/17)
The present invention provides a polycyclic compound represented by formula (I) and a use in dual inhibitors of AR and BET. Specifically, the present invention provides the use of a compound represented by formula (I) or optical isomers, solvates, pharmac
Direct Catalytic Asymmetric Cyclopropylphosphonation Reactions of N,N-Dialkyl Groups of Aniline Derivatives by Ru(II)-Pheox Complex
Le, Chi Thi Loan,Ozaki, Seiya,Chanthamath, Soda,Shibatomi, Kazutaka,Iwasa, Seiji
supporting information, p. 4490 - 4494 (2018/08/07)
Novel catalysis involving phosphonomethylation of N-methylaniline and asymmetric cyclopropylphosphonation reactions of N,N-diethylaniline derivatives with diazomethylphosphonates are reported. Optically active cyclopropylphosphonate derivatives were directly synthesized from diazomethylphosphonates and N,N-diethylaniline derivatives catalyzed by a Ru(II)-Pheox complex in one step in good yields and high diastereoselectivities (up to trans/cis = > 99:1) and enantioselectivities (up to 99% ee). D-labeling mechanistic studies of phosphonomethylation and cyclopropylphosphonation suggested that an enamine or iminium intermediate was generated in the reaction process.
Deuterium-modified Abemaciclib derivative
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Paragraph 0359; 0360; 0361; 0362; 0363; 0364; 0365, (2017/08/02)
The invention belongs to the field of medicinal chemistry and specifically relates to a deuterium-modified Abemaciclib derivative, a preparation method of the derivative, a pharmaceutical composition containing the deuterium-modified Abemaciclib derivative, and application of the deuterium-modified Abemaciclib derivative and the pharmaceutical composition in the preparation of a medicine for treating cell proliferative diseases. In comparison with Abemaciclib, some compounds of the invention (especially compounds in the embodiment) have more excellent pharmacokinetic properties. It is expected that clinical dosage will be reduced. Thus, treatment cost is reduced so as to benefit more patients.
Design, synthesis, and biological evaluation of deuterated C-aryl glycoside as a potent and long-acting renal sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes
Xu, Ge,Lv, Binhua,Roberge, Jacques Y.,Xu, Baihua,Du, Jiyan,Dong, Jiajia,Chen, Yuanwei,Peng, Kun,Zhang, Lili,Tang, Xinxing,Feng, Yan,Xu, Min,Fu, Wei,Zhang, Wenbin,Zhu, Liangcheng,Deng, Zhongping,Sheng, Zelin,Welihinda, Ajith,Sun, Xun
, p. 1236 - 1251 (2014/03/21)
SGLT2 inhibitors deuterated at sites susceptible to oxidative metabolism were found to have a slightly longer tmax and half-life (t 1/2), dose-dependent increase in urinary glucose excretion (UGE) in rats, and slightly superior effects on UGE in dogs while retaining similar in vitro inhibitory activities against hSGLT2. In particular, deuterated compound 41 has the potential to be a robust long-acting antidiabetic agent.
DEUTERATED BENZYLBENZENE DERIVATIVES AND METHODS OF USE
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Page/Page column 168, (2010/04/03)
Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by SGLT inhibition.
SULFONAMIDE INHIBITORS OF CARBONIC ANHYDRASE
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Page/Page column 19, (2010/12/29)
The present invention relates to new sulfonamide inhibitors of carbonic anhydrase activity, pharmaceutical compositions thereof, and methods of use thereof.
Diazepines[1,4] annelated with indoline and maleimide from 3-(di)alkylamino-4-(indol-1-yl)maleimides: Mechanism of rearrangement and cyclization
Lakatosh, Sergey A.,Luzikov, Yuri N.,Preobrazhenskaya, Maria N.
, p. 2017 - 2020 (2007/10/03)
The mechanism of cyclization of 3-(di)alkylamino-4-(indol-1-yl)maleimides to diazepine[1,4] derivatives was elucidated using deuterium labeled precursors.
