- Enzyme-like Supramolecular Iridium Catalysis Enabling C?H Bond Borylation of Pyridines with meta-Selectivity
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The use of secondary interactions between substrates and catalysts is a promising strategy to discover selective transition metal catalysts for atom-economy C?H bond functionalization. The most powerful catalysts are found via trial-and-error screening due to the low association constants between the substrate and the catalyst in which small stereo-electronic modifications within them can lead to very different reactivities. To circumvent these limitations and to increase the level of reactivity prediction in these important reactions, we report herein a supramolecular catalyst harnessing Zn???N interactions that binds to pyridine-like substrates as tight as it can be found in some enzymes. The distance and spatial geometry between the active site and the substrate binding site is ideal to target unprecedented meta-selective iridium-catalyzed C?H bond borylations with enzymatic Michaelis–Menten kinetics, besides unique substrate selectivity and dormant reactivity patterns.
- Al-Shehimy, Shaymaa,Gramage-Doria, Rafael,Roisnel, Thierry,Trouvé, Jonathan,Zardi, Paolo
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supporting information
p. 18006 - 18013
(2021/05/07)
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- Azaindazole bipyridine derivative myeloid cell proliferation inhibitor as well as preparation method and application thereof in pharmacy
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The invention provides an azaindazole bipyridine derivative myeloid cell proliferation inhibitor shown as a formula I, wherein R1, R2 and R3 have the meanings defined in the specification of the invention. A compound in formula I can significantly inhibit proliferation and related disordersof myeloid cells represented by MOLM-16, HL-60, and MV-4-11. The formula I or salt thereof or the related pharmaceutical composition provided by the invention has excellent in-vivo and in-vitro inhibitory activity, good druggability, high bioavailability and no obvious damage to organs. Therefore, the compound shown in the formula I or the salt thereof and the related drug combination have huge clinical application prospects.
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Paragraph 0089-0091
(2021/05/01)
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- Azaindole derivative myelocyte proliferation inhibitor, preparation method thereof, and application of inhibitor in pharmacy
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The invention provides an azaindole derivative myeloid proliferation inhibitor as shown in a formula I. In the formula, R1, R2 and R33 are as defined in the specification. The compound shown in the formula I can be used for remarkably inhibiting the proliferation of myeloid cells represented by MOLM-16, HL-60 and MV-4-11 and related diseases of the myeloid cells. The compound shown in the formula I or the salt thereof or the related pharmaceutical composition provided by the invention has excellent in-vivo and in-vitro inhibitory activity, good druggability and high bioavailability, and does not have obvious injury to visceral organs. Therefore, the compound shown in the formula I or the salt thereof and the related pharmaceutical composition have huge clinical application prospects.
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Paragraph 0095-0097
(2021/08/07)
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- WNT PATHWAY MODULATORS
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The present invention relates to dihydropyrazolo[l,5-a]pyrimidine compounds of formula I, defined herein, as WNT pathways modulators, processes for making them, and pharmaceutical compositions comprising them. Methods of treatment of conditions mediated by WNT pathway signalling including cancer, fibrosis, stem cell and diabetic retinopathy, rheumatoid arthritis, psoriasis and myocardial infarction, comprising the compounds of formula I are also provided.
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Paragraph 0365 - 0367
(2015/07/07)
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- SOLID FORMS OF 1-ETHYL-3-(5-(5-FLUOROPYRIDIN-3-YL)-7-(PYRIMIDIN-2-YL)-1H-BENZO[D]IMIDAZOL-2-YL)UREA
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Solid forms of crystalline1-ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)- 1H-benzo[d]imidazol-2-yl)urea, compositions containing solid forms of crystalline 1- ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)-1H-benzo[d]imidazol-2-yl)urea and m
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Page/Page column 55
(2009/07/17)
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- PROCESSES AND INTERMEDIATES FOR PRODUCING AMINOBENZIMIDAZOLE UREAS
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The present invention relates to processes and intermediates for the preparation of compounds useful as inhibitors of bacterial gyrase and Topoisomerase IV (Topo IV).
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Page/Page column 37
(2009/06/27)
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- Imidazo[4,5-c]pyridin-4-one analogues as GABAA receptor ligands
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A compound of formula I, or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chem
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