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-9861636-B2 优先权日:2014-04-29 标题 :Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors 发明人:HE WEI 权利人:HE WEI; ZHEJIANG DTRM BIOPHARMA CO LTD 摘要:Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.
专利号:US-2023295141-A1 优先权日:2022-03-17 标 题:Fxr small molecule agonist, the preparation and use thereof 发明人:ZHAO YISHUANG; ZHANG ZHENWEI; WU GUOHUI; YANG SHENGSHENG 权利人:CASCADE PHARMACEUTICALS INC 摘要:The present invention discloses an FXR (farnesoid X receptor) small molecule agonist, the structure of which is shown in formula I, and a preparation method thereof. In the formula, the definition of each substituent is as described in the specification and claims. The compound of the present invention has advantages, such as high FXR agonistic activity, convenience in synthesis, easy availability of raw materials, and can be used as a medicine for the treatment of FXR-related diseases.
专利号:US-2010010219-A1 优先权日:2006-12-07 标 题 :Method for producing pyrrolidine compound 发明人:HARADA KAZUHITO; ITO TAKASHI 权利人:JAPAN TOBACCO INC 摘要:Provided is a method capable of efficiently producing a compound having a superior HSD1 inhibitory action and a compound useful as a synthetic intermediate therefor, with superior achievability of asymmetric synthesis (i.e., superior selectivity), superior yield, superior safety and superior industrial workability at a low cost. n A method of producing a compound represented by the following formula [8]: n n n n n n n n n n or a salt thereof, or a solvate thereof, from a compound represented by the following formula [2]: n n n n n n n n n n or a reactive derivative thereof, or a salt thereof, or a solvate thereof.
参考标题:Rh(III)-Catalyzed Regio- And Chemoselective [4 + 1]-Annulation Of Azoxy Compounds With Diazoesters For The Synthesis Of 2H-Indazoles: Roles Of The Azoxy Oxygen Atom 作者:Zhen Long,Zhigang Wang,Danni Zhou,Danyang Wan,Jingsong You |发布日期:2017.6.2 摘要:Tandem C-H Alkylation/intramolecular Decarboxylative Cyclization Of Azoxy Compounds With Diazoesters For The Synthesis Of 3-Acyl-2H-Indazoles Is Disclosed. The Azoxy Instead Of The Azo Group Enables A Distinct Approach For Cyclative Capture, Leading To A [4 + 1]-Annulation Rather Than A Classic [4 + 2] Manner. The Azoxy Oxygen Atom Is Traceless After Annulation, And Further Removal From The Product Is
合成参考文献
摘要:Kwiecień, H., Science of Synthesis Knowledge Updates, (2018) 3, 155. 摘要:Adak, L.; Ghosh, T.; Ranu, B. C., Science of Synthesis: Cross-Dehydrogenative Coupling, (2023) nan, 414.