212573-56-3Relevant academic research and scientific papers
COMPOUND FOR INHIBITING PGE2/EP4 SIGNALING TRANSDUCTION INHIBITING, PREPARATION METHOD THEREFOR, AND MEDICAL USES THEREOF
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, (2022/03/14)
A compound of formula (I), a preparation method therefor, a pharmaceutical composition containing a derivative thereof, and the therapeutic uses thereof, especially inhibiting PGE2/EP4 signalling transduction and the uses thereof for treating cancer, acute or chronic pain, migraine, osteoarthritis, rheumatoid arthritis, gout, bursitis, ankylosing spondylitis, primary dysmenorrhea, tumour or arteriosclerosis.
C6-Selective Direct Arylation of 2-Phenylpyridine via an Activated N-methylpyridinium Salt: A Combined Experimental and Theoretical Study
Yin, Changzhen,Zhong, Kangbao,Li, Wenjing,Yang, Xiao,Sun, Rui,Zhang, Chunchun,Zheng, Xueli,Yuan, Maolin,Li, Ruixiang,Lan, Yu,Fu, Haiyan,Chen, Hua
, p. 3990 - 3998 (2018/09/12)
An elegant pre-activation strategy, based on the formation of N-methylpyridinium iodide salts for C6-selective direct arylation of 2-phenylpyridines using Pd/Cu cooperative catalysis, has been developed. By this methodology, a wide range of unsymmetrical 2, 6-diarylpyridines were synthesized with high reactivity and regioselectivity as well as good functional group tolerance. In particular, challenging substrates bearing electron donating groups (EDGs), such as OMe, NMe2, were also successfully employed in this reaction. Deuterium incorporation studies revealed that the C?H bond acidity is improved significantly in N-methylpyridinium salts compared with their N-Oxide and N-iminopyridinium ylide counterparts, thus solving the long-standing problem associated with previous strategies for the synthesis of diaryl pyridines. Finally, the control experiments and DFT calculations supported a Pd-catalyzed and Cu-mediated mechanism in which a carbenoid copper species that is formed in-situ from N-methylpyridinium salts, participates in a Pd-catalyzed arylation followed by an iodide-promoted N-demethylation process. (Figure presented.).
END CAPPED NUCLEIC ACID MOLECULES
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Paragraph 0097, (2016/07/05)
The disclosure relates to nucleic acids that contain modifications at the 5'-end, 3'-end or 5'-end and 3'-ends, and compounds that can be used to make the modified nucleic acids are disclosed. The modified nucleic acids have improved expression, lower imm
Cushing's syndrome: Development of highly potent and selective CYP11B1 inhibitors of the (pyridylmethyl)pyridine type
Emmerich, Juliette,Hu, Qingzhong,Hanke, Nina,Hartmann, Rolf W.
, p. 6022 - 6032 (2013/09/02)
Potent and selective CYP11B1 inhibitors could be promising therapeutics for the treatment of Cushing's syndrome. Optimization of Ref 1 (5-((1H-imidazol-1- yl)methyl)-2-phenylpyridine) led to compound 44 (5-((5-methylpyridin-3-yl) methyl)-2-phenylpyridine) with a 50-fold improved IC50 value of 2 nM toward human CYP11B1 and an enhanced inhibition of the rat enzyme (IC 50 = 2440 nM) compared to Ref 1 (IC50 > 10000 nM). Furthermore, selectivities over CYP11B2, CYP17, and CYP19 were observed, as well as satisfying metabolic stability not only in human and rat plasma but also in liver S9 fraction. Investigation of cytotoxicity and inhibition of hepatic CYP2A6 and CYP3A4 showed that 44 fulfills first safety criteria and can be considered for further in vivo evaluation in rats.
Synthesis of facial cyclometalated iridium(iii) complexes triggered by tripodal ligands
Moriuchi, Toshiyuki,Mao, Lisheng,Wu, Hsyueh-Liang,Ohmura, Satoshi D.,Watanabe, Masami,Hirao, Toshikazu
, p. 9519 - 9525 (2012/09/11)
The tripodal ligands composed of the 1,3,5-trisubstituted cyclohexyl moiety as a molecular scaffold and 2-phenylpyridyl moieties as a coordination site were designed. The homoleptic cyclometalated fac-Ir(C^N)3 complexes could be obtained by the reaction of IrCl3·nH2O with the designed tripodal ligands. The single crystal X-ray structure determination confirmed the fac configuration and a distorted octahedral geometry with three intramolecular cyclometalated 2-phenylpyridyl ligands surrounding the iridium metal center. Also, the cyclohexyl scaffold was found to serve as a flexible scaffold to induce the fac configuration. The thus-obtained homoleptic cyclometalated fac-Ir(C^N)3 complexes exhibited a broad emission band in the emission spectra at 298 K.
SELECTIVE CYP11B1 INHIBITORS FOR THE TREATMENT OF CORTISOL DEPENDENT DISEASES
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Page/Page column 71, (2012/05/05)
The present invention relates to compounds which selectively inhibit CYP11B1. Preferably, the compounds of the present invention do not substantially inhibit CYP11B2. Moreover, the compounds of the present invention do not substantially inhibit CYP17 and/or CYP19, either. Amongst other applications of the compounds of the present invention, they can be used for the treatment of Cushing's syndrome or metabolic disease.
Calix[6]arene derivatives selectively functionalized at alternate sites on the smaller rim with 2-phenylpyridine and 2-fluorenylpyridine substituents to provide deep cavities
Zeng, Xianshun,Batsanov, Andrei S.,Bryce, Martin R.
, p. 9589 - 9594 (2007/10/03)
The synthesis is described of calix[6]arene derivatives 4, 9, and 14 functionalized at alternate sites on the smaller rim with 4′-(pyrid- 2″-yl)phenylmethoxy, (6′-phenylpyrid-3′-ylmethoxy), and {6′-[2-(9,9-di-n-hexylfluorenyl)]pyrid-3′-ylmethoxy} substitu
Synthesis, crystal structure, and second-order nonlinear optical properties of ruthenium(II) complexes with substituted bipyridine and phenylpyridine ligands
Labat, Laurence,Lamere, Jean-Francois,Sasaki, Isabelle,Lacroix, Pascal G.,Vendier, Laure,Asselberghs, Inge,Perez-Moreno, Javier,Clays, Koen
, p. 3105 - 3113 (2007/10/03)
Two new ruthenium(II) complexes of formula [Ru(bpy)2-(L 1)][PF6] and [Ru(bpy)2(L2)][PF 6]2 are reported. HL1 is a (nitrophenyl) ethenyl-substituted phenylpyridine liga
