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:EP-1836163-B1 优先权日:2004-12-23 标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin 发明人:BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER 权利人:NOVARTIS AG 摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.
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-2025026766-A1 优先权日:2022-01-12 标题 :Thiazolopyridyl Amide Derivatives as DNA Polymerase Theta Inhibitors 发明人:LI JING; XU WENQING; WANG ZHIWEI 权利人:BEIGENE LTD 摘要:The present invention relates to compounds containing thiazolopyridyl amide structure, the process for their synthesis, as well as the use of such compounds for inhibiting DNA Polymerase Theta (Pol Theta), and in the treatment of various diseases including cancers.
摘要:Krishnamoorthy, R., Science of Synthesis Knowledge Updates, (2013) 1, 455. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 132. 摘要:Zhang, M.; Su, W., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 1, 96.