专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:US-6872716-B2 优先权日:2000-09-11 标题:Antipsychotic sulfonamide-heterocycles, and methods of use thereof 发明人:WU XINHE; AQUILA BRIAN M; SHAO LIMING; RADEKE HEIKE; CUNY GREGORY D; HAUSKE JAMES R; XIE ROGER L 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.
[参考文献]: Bunta Watanabe, Et Al. Stereospecific Inhibitory Effects Of Ccg-1423 On The Cellular Events Mediated By Myocardin-Related Transcription Factor A. Plos One. 2015 Aug 21;10(8):E0136242.
合成参考文献
参考文献:10.1055/s-0037-1609522 摘要:Synthesis of PF-06424439. Synfacts. 2018 May 17;14(06):0562. doi: 10.1055/s-0037-1609522. 参考文献:10.1055/s-0033-1339575 摘要:Asymmetric Hydrogenation of Cyclic Unsaturated Heterocyclic Acids. Synfacts. 2013 Aug 19;9(09):0965. doi: 10.1055/s-0033-1339575.