- Nickel-Catalyzed Amination of (Hetero)aryl Halides Facilitated by a Catalytic Pyridinium Additive
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An efficient and operationally simple Ni-catalyzed amination protocol has been developed. This methodology features a simple NiII salt, an organic base and catalytic amounts of both a pyridinium additive and Zn metal. A diverse number of (hetero)aryl halides were coupled successfully with primary and secondary alkyl amines, and anilines in good to excellent yields. Similarly, benzophenone imine gave the corresponding N-arylation product in an excellent yield.
- Han, Dongyang,Li, Sasa,Xia, Siqi,Su, Mincong,Jin, Jian
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supporting information
p. 12349 - 12354
(2020/09/09)
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- Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors
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Rational structure-based design has yielded highly potent inhibitors of cathepsin K (Cat K) with excellent physical properties, selectivity profiles, and pharmacokinetics. Compounds with a 3,4-(CH3O)2Ph motif, such as 31, were found to have excellent metabolic stability and absorption profiles. Through metabolite identification studies, a reactive metabolite risk was identified with this motif. Subsequent structure-based design of isoteres culminated in the discovery of an optimized and balanced inhibitor (indazole, 38).
- Crawford, James J.,Kenny, Peter W.,Bowyer, Jonathan,Cook, Calum R.,Finlayson, Jonathan E.,Heyes, Christine,Highton, Adrian J.,Hudson, Julian A.,Martin, Scott,MacFaul, Philip A.,McDermott, Benjamin P.,McGuire, Thomas M.,Morley, Andrew D.,Morris, Jeffrey J.,Page, Ken M.,Ribeiro, Lyn Rosenbrier,Sawney, Helen,Smith, Caroline,Dossetter, Alexander G.,Jestel, Anja,Krapp, Stephan,Steinbacher, Stefan
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supporting information
p. 8827 - 8837,11
(2020/09/16)
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- CYANOCYCLOPROPYLCARBOXAMIDES AS CATHEPSIN INHIBITORS
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The present invention relates to compounds of formula (I) for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.
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Page/Page column 54-55
(2009/03/07)
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- G-PROTEIN COUPLED RECEPTOR AGONISTS
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Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.
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Page/Page column 41
(2008/06/13)
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- N-HYDROXYAMIDE DERIVATIVES AND USE THEREOF
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The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof, in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
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Page/Page column 86
(2008/06/13)
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