📜2-[(5-Bromo-4-Fluoro-2-Methylphenyl)Amino]-1-Cyclopropylethanone置于草酰氯,Ammonium Acetate,异丙基氯化镁,乙酸酐,溶剂黄146,N,N-二异丙基乙胺体系中,用 四氢呋喃,二氯甲烷,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 2.0H,反应生成司隆色替 参考文献: Processes For Preparing Ask1 Inhibitors[fr] Procédés De Préparation D'Inhibiteurs De L'Ask1 标题: Processes For Preparing Ask1 Inhibitors[fr] Procédés De Préparation D'Inhibiteurs De L'Ask1 摘要:本公开提供了制备式(A)化合物的方法,该化合物具有凋亡信号调节激酶("Ask1")抑制活性,因此在治疗肾病,糖尿病肾病和肾纤维化等疾病方面具有用处.该公开还提供了合成中间体化合物.
专利号:US-2024400552-A1 优先权日:2016-11-11 标题 :Heterocyclic modulators of lipid synthesis 发明人:BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S 权利人:SAGIMET BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by dysregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).
专利号:US-11622968-B2 优先权日:2011-03-08 标 题:Heterocyclic modulators of lipid synthesis 发明人:BUCKLEY DOUGLAS; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S 权利人:SAGIMET BIOSCIENCES INC 摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).
专利号:US-2025017938-A1 优先权日:2023-06-20 标 题:Combination therapies of fasn inhibitors with thyroid hormone receptor agonists 发明人:O'FARRELL ANNE-MARIE; KEMBLE GEORGE; TSAI WEN-WEI 权利人:SAGIMET BIOSCIENCES INC 摘要:Therapeutic combinations of fatty acid synthesis modulators and thyroid hormone receptor agonists are provided. The combinations may be used to treat disorders including metabolic disorders and liver disorders, such as nonalcoholic steatohepatitis/metabolic dysfunction-associated steatohepatitis (NASH/MASH).
专利号:WO-2018151830-A1 优先权日:2017-02-17 标 题:Pyridinyl based apoptosis signal-regulation kinase inhibitors 发明人:JIN BOHAN; DONG QING; HUNG GENE 权利人:FRONTHERA U S PHARMACEUTICALS LLC 摘要:Apoptosis signal-regulating kinase 1 (ASK1) activation and signaling have been reported to play an important role in a broad range of diseases including neurodegenerative, cardiovascular, inflammatory, autoimmunity and metabolic disorders. Disclosed herein is the synthesis of pyridinyl derived therapeutic agents that function as inhibitors of ASK 1 as well as their pharmaceutical compositions and methods of use.
专利号:US-12358903-B2 优先权日:2016-06-13 标题 :FXR (NR1H4) modulating compounds 发明人:BLOMGREN PETER A; CURRIE KEVIN S; FARAND JULIE; 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-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.
1: Ji N, Yang Y, Cai CY, Lei ZN, Wang JQ, Gupta P, Shukla S, Ambudkar SV, Kong D, Chen ZS. Selonsertib (GS-4997), an ASK1 inhibitor, antagonizes multidrug resistance in ABCB1- and ABCG2-overexpressing cancer cells. Cancer Lett. 2019 Jan;440-441:82-93. doi: 10.1016/j.canlet.2018.10.007. Epub 2018 Oct 10. doi: 10.1002/cpt.204. Epub 2015 Sep 29. doi: 10.1159/000369152. Epub 2014 Dec 17.
合成参考文献
参考文献:10.1038/s41401-022-00874-x 摘要:Tong X, Wang Q, Zhao X, Sun Y, Wu X, Yang L, Lu Z, Ou X, Jia J, You H. Histological assessment based on liver biopsy: the value and challenges in NASH drug development. Acta Pharmacologica Sinica. 2022 Feb 14;43(5):1200–9. doi: 10.1038/s41401-022-00874-x. 参考文献:10.1186/s13287-021-02696-w 摘要:Peng L, Chen Y, Shi S, Wen H. Stem cell-derived and circulating exosomal microRNAs as new potential tools for diabetic nephropathy management. Stem Cell Research & Therapy. 2022 Jan 24;13(1):25. doi: 10.1186/s13287-021-02696-w.