- NOVEL 5 OR 8-SUBSTITUTED IMIDAZO [1, 5-a] PYRIDINES AS INDOLEAMINE AND/OR TRYPTOPHANE 2, 3-DIOXYGENASES
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Disclosed herein are 5 or 8-substituted imidazo[l,5-a]pyridines and pharmaceutical compositions comprising at least one such 5 or 8-substituted imidazo[l,5-a]pyridines, processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain 5 or 8- substituted imidazo[l,5-a]pyridines that can be useful for inhibiting indoleamine 2,3- dioxygenase and/or tryptophane 2,3-dioxygenase and for treating diseases or disorders mediated thereby.
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Paragraph 0382
(2016/10/31)
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- PICOLINAMIDE AND PYRIMIDINE-4-CARBOXAMIDE COMPOUNDS, PROCESS FOR PREPARING AND PHAMACEUTICAL COMPOSITION COMPRISING THE SAME
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Provided are picolinamide and pyrimidine-4-carboxamide compounds, a method for preparing the same, a pharmaceutical composition containing the same, and a medical use using the compound as an agent for preventing, regulating, and treating diseases related to regulation of glucocorticoids by using selective inhibitory activity of the compound for an 11β-HSD1 enzyme. The picolinamide and pyrimidine-4-carboxamide compounds of the present invention are selective inhibitors of human-derived 11β-HSD1 enzymes, and are useful in an agent for preventing, regulating, and treating diseases related to glucocorticoid regulation in which human- derived 11β-HSD1 enzymes are involved, for example, metabolic syndromes such as, type 1 and type 2 diabetes, diabetes later complications, latent autoimmune diabetes adult (LAD A), insulin tolerance syndromes, obesity, impaired glucose tolerane (IGT), impaired fasting glucose (IFG), damaged glucose tolerance, dyslipidemia, atherosclerosis, hypertension, etc.
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Page/Page column 83-84
(2011/11/30)
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- Converting core compounds into building blocks: The concept of regiochemically exhaustive functionalization
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In a model study, 3-fluorophenol and 3-fluoropyridine were converted into the each time four possible carboxylic acids by passing through the corresponding organometallic intermediates. As an attempt to generalize the findings reveals, a restricted set of principles and methods suffices to cope with all standard scenarios. The most valuable and versatile tools for the regiochemically exhaustive functionalization of a great variety of substrate patterns are the optionally site-selective metalation (either by reagent/substrate matching or by peripheral coordination control), the use of activating or congesting protective groups and the basicity gradient-driven heavy halogen migration (followed by halogen/metal permutation). Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005.
- Marzi, Elena,Bobbio, Carla,Cottet, Fabrice,Schlosser, Manfred
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p. 2116 - 2123
(2007/10/03)
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