- CRBN LIGANDS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.
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Paragraph 00420; 00421
(2019/08/20)
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- N-Heterocyclic carbenes derived from imidazo-[1,5-a]pyridines related to natural products: synthesis, structure and potential biological activity of some corresponding gold(I) and silver(I) complexes
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A series of Au(I) complexes (12, 13, 14, 15, 16) and Ag(I) complexes (17, 18, 19, 20) derived from imidazo[1,5-a]pyridin-3-ylidenes were synthesized from AuCl(SMe2) or by reacting silver(I) acetate with 2,5-dimethylimidazo[1,5-a]pyridin-2-ium iodide or imidazo[1,5-a]pyridin-2-ium salts, and were characterized using NMR spectroscopy, mass spectrometry and elemental analyses. In addition, the Au(I) complex 13 and the Ag(I) complex 19 were characterized using single-crystal X-ray diffraction. Using paclitaxel as a standard, all Au(I) and Ag(I) N-heterocyclic carbene complexes were evaluated for their in vitro anti-tumour activity against 12 cell lines using a monolayer cell survival and proliferation assay. The highest anticancer activity was found for complexes 15, 13 and 14 with mean IC50 values of 10.09, 10.42 and 12.28?μM, respectively. Copyright
- Mihorianu, Monica,Franz, M Heiko,Jones, Peter G,Freytag, Matthias,Kelter, Gerhard,Fiebig, Heinz-Herbert,Tamm, Matthias,Neda, Ion
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p. 581 - 589
(2016/07/16)
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- IMIDAZO[1, 5A]PYRIDINE DERIVATIVES AND METHODS FOR TREATING ALDOSTERONE MEDIATED DISEASES
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Compounds of the formula (I) provide pharmacological agents which are inhibitors of the P450 enzyme, aldosterone synthase, and thus may be employed for the treatment of aldosterone mediated conditions. Accordingly, the compounds of formula (I) may be employed for prevention, delay of progression, or treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, fibrosis and remodeling following hypertension and endothelial dysfunction. Preferred are the compounds of formula (I) which are selective inhibitors of aldosterone synthase devoid of undesirable side effects due to general inhibition of cytochrome P450 enzymes.
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- Azines polycycliques. (IV). Synthese de derives sulfures en -3 de l'imidazolpyridine
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La dihydro-2,3 imidazopyridinethione-3 est -preparee aisement a partir de l'aminomethyl-2 pyridine et est ensuite S-alkylee ou -aralkylee.On decrit, dans le cas du derive 3-thiomethyle, la trifluoroacetylation en -1, l'oxydation en methylsulfone et
- Bourdais, Jacques,Rajniakova, Olga,Povazanec, Frantisek
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p. 1351 - 1353
(2007/10/02)
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