专利号:US-2024309003-A1 优先权日:2021-05-04 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN; PANDYA BHAUMIK; KAPLAN ALAN 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-9242998-B2 优先权日:2013-02-07 标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C 发明人:HE SHUWEN; DAI XING; PALANI ANANDAN; NARGUND RAVI; LAI ZHONG; ZORN NICOLAS; XIAO DONG; DANG QUN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD 权利人:HE SHUWEN; DAI XING; PALANI ANANDAN; NARGUND RAVI; LAI ZHONG; ZORN NICOLAS; XIAO DONG; DANG QUN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD; MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-8952042-B2 优先权日:2009-08-19 标 题 :FXR (NR1H4) binding and activity modulating compounds 发明人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF 权利人:KREMOSER CLAUS; ABEL ULRICH; STEENECK CHRISTOPH; KINZEL OLAF; PHENEX PHARMACEUTICALS AG 摘要:The present invention relates to compounds of formula (1): n nwhere R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
专利号:US-11739065-B2 优先权日:2016-06-13 标题 :FXR (NR1H4) modulating compounds 发明人:BLOMGREN PETER A; CURRIE KEVIN S; GEGE CHRISTIAN; KROPF JEFFREY E; XU JIANJUN 权利人:GILEAD SCIENCES INC 摘要:The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
专利号:US-9751874-B2 优先权日:2014-12-17 标题:Hydroxy containing FXR (NR1H4) modulating compounds 发明人:GEGE CHRISTIAN; KINZEL OLAF; KREMOSER CLAUS; SCHMITT AARON C 权利人:GILEAD SCIENCES INC 摘要:The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
专利号:US-11225473-B2 优先权日:2019-01-15 标题:FXR (NR1H4) modulating compounds 发明人:BLOMGREN PETER A; CURRIE KEVIN S; FRICK MORIN MAE; HORSTMAN ELIZABETH M; KAPLAN JOSHUA A; KROPF JEFFREY E; WATKINS WILLIAM J 权利人:GILEAD SCIENCES INC 摘要:The present disclosure relates generally to compounds that bind to FXR and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
参考标题:Access To Polysubstituted (Furyl)Methylthioethers Via A Base-Promoted S-H Insertion Reaction Of Conjugated Enynones 作者:Wanqing Wu,Yang Chen,Meng Li,Weigao Hu,Xuemin Lin |发布日期:2019.11.15 摘要:Diverse Functionalized (2-Furyl)Methylthioether Derivatives Via Base-Promoted S-H Insertion Of Conjugated Enynones With Thiophenols Or Thiols Has Been Developed. This Reaction Features Readily Available Starting Materials, High Atom Economy, Broad Substrate Scope, And Versatile Operation. Moreover, The Synthetic Utility Of This Method Has Been Demonstrated By The Efficient Synthesis Of The Cnkspr1 Inhibitor
合成参考文献
摘要:Lubell, W. D.; St-Cyr, D. J.; Dufour-Gallant, J.; Hopewell, R.; Boutard, N.; Kassem, T.; Dörr, A.; Zelli, R., Science of Synthesis Knowledge Updates, (2013) 1, 216. 摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 195.