专利号:WO-2025128848-A1 优先权日:2023-12-12 标题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK 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 ('TREM2'). 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:WO-2023081730-A1 优先权日:2021-11-03 标 题:4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide derivatives as cannabinoid cb2 receptor modulators for the treatment of cancer 发明人:ELZEIN ELFATIH; LIU JIWEN 权利人:TEON THERAPEUTICS INC 摘要:The present invention relates to 82 specific 4-hydroxy-2-oxo-1,2- dihydro-1,8-naphthyridine-3-carboxamide derivatives as cannabinoid CB2 receptor modulators for the treatment of cancer, e.g. to 6-(4- fluorophenyl)-4-hydroxy-1-(2-(4-methylpiperazin-1-yl)ethyl)-2-oxo-N- (spiro[2.3]hexan-5-yl)-1,2-dihydro-1,8-naphthyridine-3-carboxamide (example 1, compound 1) The present description discloses the synthesis and characterisation of the 82 claimed compounds as well as biological assays thereof.
专利号:CN-119390677-A 优先权日:2024-12-06 标题 :Synthesis method of bicyclo-ethanol
1: Zhen YZ, Li NR, He HW, Zhao SS, Zhang GL, Hao XF, Shao RG. Protective effect of bicyclol against bile duct ligation-induced hepatic fibrosis in rats. World J Gastroenterol. 2015 Jun 21;21(23):7155-64. doi: 10.3748/wjg.v21.i23.7155. 2: Chen X, Zhang J, Han C, Dai H, Kong X, Xu L, Xia Q, Zhang M, Zhang J. A sexual dimorphism influences bicyclol-induced hepatic heat shock factor 1 activation and hepatoprotection. Mol Pharmacol. 2015 Jul;88(1):38-47. doi: 10.1124/mol.114.097584. Epub 2015 Apr 21. doi: 10.1016/j.brainresbull.2013.11.001. Epub 2013 Nov 16. 5: Yao XM, Li Y, Li HW, Cheng XY, Lin AB, Qu JG. Bicyclol attenuates tetracycline-induced fatty liver associated with inhibition of hepatic ER stress and apoptosis in mice. Can J Physiol Pharmacol. 2016 Jan;94(1):1-8. doi: 10.1139/cjpp-2015-0074. Epub 2015 Sep 22. doi: 10.1080/10286020.2015.1131678. Epub 2016 Jan 8. doi: 10.1016/j.brainres.2013.06.032. Epub 2013 Jul 10. doi: 10.1007/s40261-013-0136-3. doi: 10.1016/j.ejphar.2016.09.002. Epub 2016 Sep 3. doi: 10.1016/j.ejps.2015.06.020. Epub 2015 Jun 24. doi: 10.5588/ijtld.14.0579. Epub 2012 Jan 28. doi: 10.1631/jzus.B1200263.
合成参考文献
摘要:Hu W, Zhang CZ, Li Y. [Resolution of racemic anti-hepatitis drug ( +/- ) -bicyclol]. Yao Xue Xue Bao. 2006 Mar;41(3):221–4. 摘要:Tang T, Li Y. [Protective effect of bicyclol against acute fatty liver induced by tetracycline in mice]. Yao Xue Xue Bao. 2008 Jan;43(1):23–8. 参考文献:10.1016/j.ejphar.2008.02.059 摘要:Zhao J, Chen H, Li Y. Protective effect of bicyclol on acute alcohol-induced liver injury in mice. Eur J Pharmacol. 2008 May 31;586(1-3):322–31. doi: 10.1016/j.ejphar.2008.02.059. 参考文献:10.1038/aps.2009.194 摘要:Bao X, Liu G. Bicyclol protects HepG2 cells against D-galactosamine-induced apoptosis through inducing heat shock protein 27 and mitochondria associated pathway. Acta Pharmacologica Sinica. 2010 Feb 05;31(2):219–26. doi: 10.1038/aps.2009.194.