专利号:US-2009076268-A1 优先权日:2007-09-14 标 题:Facile assembly of fused benzofuro-heterocycles 发明人:FITZGERALD ANNE E; LIU JING; MANI NEELAKANDHA S 权利人:FITZGERALD ANNE E; LIU JING; MANI NEELAKANDHA S 摘要:This invention concerns the synthesis of polycyclic structural components of pharmacological compounds, including the synthesis of fused benzofuro-heterocycles, through selective palladium-catalyzed cross-coupling and intramolecular cyclization.
专利号:US-10947203-B2 优先权日:2016-03-25 标题 :1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane X receptor 发明人:CHEN TAOSHENG; LIN WENWEI; WANG YUEMING 权利人:ST JUDE CHILDRENS RES HOSPITAL; ST JUDE CHILDRENS RSEARCH HOSPITAL 摘要:In an aspect, the invention relates to 1,4,5-substituted 1,2,3-triazole and 1,2,4,5-substituted imidazoles having a structure represented by a formula: n nwhich are modulators the pregnane X receptor (“PXRâ€?); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of modulating an adverse drug reaction in a mammal using the compounds and pharmaceutical compositions; methods of treatment of a disorder of uncontrolled cellular proliferation, such as a cancer, using the compounds and pharmaceutical compositions; methods of modulating pregnane X receptor activity in a mammal using the compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:WO-2013134527-A1 优先权日:2012-03-07 标 题:Synthesis of polycyclic alkaloids and their use as tgr5 agonists
专利号:EP-2828263-A1 优先权日:2012-03-07 标题 :Synthesis of polycyclic alkaloids and their use as tgr5 agonists
专利号:US-6872745-B2 优先权日:2000-04-14 标 题 :Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis 发明人:JOHNSON JR THEODORE O; HUA YE; LUU HIEP T; DRAGOVICH PETER S 权利人:AGOURON PHARMA 摘要:Compounds of the formula: n n nwhere the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:US-7671085-B2 优先权日:2002-11-15 标 题 :Non-steroidal farnesoid X receptor modulators and methods for the use thereof 发明人:DOWNES MICHAEL R; EVANS RONALD M 权利人:SALK INST FOR BIOLOGICAL STUDI 摘要:The efficient regulation of cholesterol synthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR would be an important step in further deconvoluting FXR physiology. In accordance with the present invention, the identification of novel potent FXR activators is described. Two derivatives of invention compounds, bearing stilbene or biaryl moieties, contain members that are the most potent FXR agonists reported to date in cell-based assays. These compounds are useful as chemical tools to further define the physiological role of FXR as well as therapeutic leads for the treatment of diseases linked to cholesterol, bile acids and their metabolism and homeostasis.
参考文献:10.1007/s11426-024-2248-y 摘要:Zhan F, Lou W, Zheng H, Li G, She Y. Tetra-coordinated difluoroboron TADF emitter for sky-blue organic light-emitting diodes with 27.4% external quantum efficiency. Sci. China Chem. 2024 Dec 23;68(3):1026–34. doi: 10.1007/s11426-024-2248-y.