56302-41-1Relevant academic research and scientific papers
PEPTIDES, COMPOUNDS, COMPOSITIONS AND METHODS FOR INHIBITING SOX9 DIMERIZATION
-
Paragraph 0097; 00147-00149, (2021/05/29)
The present application provides SOX9 dimerization inhibitor compounds, compositions, and methods of use thereof. In certain aspects, the SOX9 dimerization inhibitor is a peptide comprising a portion of the SOX9 dimerization motif and a TAT protein to support cell entry which is c-terminal to the SOX9 dimerization motif as set forth in SEQ ID NO:3. In other aspects, the SOX9 dimerization inhibitor is a compound of the general formula I (The applicant is kindly asked to please insert chemical structure here) where one A is H and the other is: (please insert second chemical structure here), and the remaining substituents are as defined in the application.
Tuneable Copper Catalysed Transfer Hydrogenation of Nitrobenzenes to Aniline or Azo Derivatives
Moran, Maria Jesus,Martina, Katia,Baricco, Francesca,Tagliapietra, Silvia,Manzoli, Maela,Cravotto, Giancarlo
supporting information, p. 2689 - 2700 (2020/05/18)
A highly versatile and flexible copper nanoparticle (Cu(0) NPs) catalytic system has been developed for the controlled and selective transfer hydrogenation of nitroarene. Interestingly, the final catalytic product is strongly dependent on the nature of the hydrogen donor source. The yield of nitrobenzene reduction to aniline increased from 20% to an almost quantitative yield over a range of alcohols, diols and aminoalcohols. In glycerol at 130 °C aniline was isolated in 93% yield. In ethanolamine, the reaction was conveniently performed at a lower temperature (55 °C) and gave selectively substituted azobenzene (92% yield). Experimental studies provide support for a reaction pathway in which the Cu(0) NPs catalysed transfer hydrogenation of nitrobenzene to aniline proceeds via the condensation route. The high chemoselectivity of both protocols has been proved in experiments on a panel of variously substituted nitroarenes. Enabling technologies, microwaves and ultrasound, used both separately and in combination, have successfully increased the reaction rate and reaction yield. (Figure presented.).
Design, synthesis and biological evaluation of novel 2-phenyl pyrimidine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors
Li, Xinyu,Shi, Binyu,Teng, Yu,Cheng, Yu,Yang, Huizhu,Li, Jiurong,Wang, Lianjian,He, Siying,You, Qidong,Xiang, Hua
, p. 294 - 299 (2019/03/02)
BTK is an effective target for the treatment of B-cell malignant tumors and autoimmune diseases. In this work, a series of 2-phenyl pyrimidine derivatives were prepared and their preliminary in vitro activities on B-cell leukemia cells as well as the BTK enzyme were determined. The results showed that compound 11g displayed the best inhibitory activity on BTK with an inhibition rate of 82.76% at 100 nM and excellent anti-proliferation activity on three B-cell leukemia lines (IC50 = 3.66 μM, 6.98 μM, and 5.39 μM against HL60, Raji and Ramos, respectively). Besides, the flow cytometry analysis results indicated that 11g inhibited the proliferation of the Raji cells in a dose- and time-dependent manner, and blocked the Ramos cells at the G0/G1 phase, which is in accordance with the positive control ibrutinib. The mechanism investigation demonstrated that 11g could inhibit the phosphorylation of BTK and its downstream substrate phospholipase γ2 (PLCγ2). All these results showed that 11g was a promising lead compound that merited further optimization as a novel class of BTK inhibitor for the treatment of B-cell lymphoblastic leukemia.
2-phenylpyrimidine compounds, preparation method and medical application
-
Paragraph 0098; 0099; 0109; 0110; 0111, (2018/06/15)
The invention belongs to the field of medicines and particularly relates to 2-phenylpyrimidine compounds and pharmacologically-acceptable salts thereof and an isotope marker. The invention also discloses a pharmaceutical composition containing the substances and application of the pharmaceutical composition for treating diseases related with protein kinase activity, such as cancer and inflammation. (The formula is shown in the description).
TYK2 INHIBITORS, USES, AND METHODS FOR PRODUCTION THEREOF
-
, (2018/09/28)
The present invention provides compounds useful as inhibitors of Tyrosine Kinase 2 (Tyk2), solid forms and compositions thereof, methods of producing the same, and methods of using the same in the treatment of Tyk2-mediated diseases.
Synthesis and Characterization of a Bidirectional Photoswitchable Antagonist Toolbox for Real-Time GPCR Photopharmacology
Hauwert, Niels J.,Mocking, Tamara A. M.,Da Costa Pereira, Daniel,Kooistra, Albert J.,Wijnen, Lisa M.,Vreeker, Gerda C. M.,Verweij, Eléonore W. E.,De Boer, Albertus H.,Smit, Martine J.,De Graaf, Chris,Vischer, Henry F.,De Esch, Iwan J. P.,Wijtmans, Maikel,Leurs, Rob
supporting information, p. 4232 - 4243 (2018/04/05)
Noninvasive methods to modulate G protein-coupled receptors (GPCRs) with temporal and spatial precision are in great demand. Photopharmacology uses photons to control in situ the biological properties of photoswitchable small-molecule ligands, which bodes
Environmentally benign selective hydrogenation of α,β-unsaturated aldehydes and reduction of aromatic nitro compounds using Cu based bimetallic nanoparticles supported on multiwalled carbon nanotubes and mesoporous carbon
Hareesh,Minchitha,Venkatesh,Nagaraju,Kathyayini
, p. 82359 - 82369 (2016/09/09)
Bimetallic catalysts of Cu with Fe, Co, Ni, Zn or Ru supported on multiwalled carbon nanotubes (MWCNT) and mesoporous carbon (MC) were prepared by in situ reduction of CuCl2 and the metal chlorides using NaBH4. The catalytic activity of these materials was investigated in the hydrogenation of α,β-unsaturated aldehydes and reduction of aromatic nitro compounds using different hydrogen sources. Cu-Ni and Cu-Ru supported on MWCNT catalysts were found to be better than MC supported catalysts in terms of yield of the expected product and recyclability. Among the different hydrogen sources used, molecular H2 was found to be the best for the hydrogenation of α,β-unsaturated aldehydes to corresponding alcohols (conversion 83-86%, selectivity 72-78%), whereas NaBH4 was the best for the reduction of aromatic nitro compounds to corresponding amines (conversion 100%, selectivity 98%). The reaction conditions were optimised for good yield and selectivity of the product. Generality of the catalysts was also investigated in the reduction of different α,β-unsaturated aldehydes and aromatic nitro compounds. The relationship between catalytic activity and physico-chemical properties was investigated by characterising the catalytic materials using powder X-ray diffraction (powder XRD), X-ray photoelectron spectroscopy (XPS), Brunauer-Emmett-Teller (BET) surface area, scanning electron microscopy (SEM)-energy dispersive X-ray spectroscopy (EDS) and transmission electron microscopy (TEM).
SUBSTITUTED PYRIDAZINE CARBOXAMIDE COMPOUNDS AS KINASE INHIBITOR COMPOUNDS
-
Page/Page column 39, (2010/01/12)
Pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
Novel Cyclic Urea Derivatives, Preparation Thereof and Pharmaceutical Use Thereof as Kinase Inhibitors
-
Page/Page column 47, (2009/04/24)
Compounds of formula (I): wherein Ra, Rb, R, X1 and X2 are as defined in the disclosure, pharmaceutical compositions comprising said compounds, processes for making and methods of using the same are provided.
