专利号:US-8598166-B2 优先权日:2008-03-21 标 题:Polysubstituted derivatives of 6-heteroarylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof 发明人:DE PERETTI DANIELLE; EVANNO YANNICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE 权利人:DE PERETTI DANIELLE; EVANNO YANNICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE; SANOFI SA 摘要:Compounds of formula (I): n nwherein R 1 , R 2 , R 3 , R 4 , Het and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
专利号:US-7405310-B2 优先权日:2001-03-05 标 题:Non-nucleoside reverse transcriptase inhibitors 发明人:LINDSTROM STEFAN; SAHLBERG CHRISTER; WALLBERG HANS; KALYANOV GENAIDY; ODEN LOURDES SALVADOR; NAESLUND LOTTA 权利人:MEDIVIR AB 摘要:This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.
专利号:US-11731956-B2 优先权日:2018-10-22 标 题:Substituted 1,2,4-triazoles as intermediates in the synthesis of TYK2 inhibitors
专利号:US-8865898-B2 优先权日:2010-11-30 标题:Nucleoside analog or salt thereof, oligonucleotide analog, gene expression inhibitor, and nucleic-acid probe for detecting gene 发明人:UENO YOSHIHITO 权利人:UENO YOSHIHITO; JAPAN SCIENCE & TECH AGENCY 摘要:A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: n nwherein R 1 , R 2 , and R 3 are the same or different groups, and each of the R 1 , R 2 and R 3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.
专利号:WO-2023071314-A1 优先权日:2021-10-29 标 题:Synthesis, preparation method and use of shp2 and cdk4/6 dual-target inhibitory compound
专利号:US-12331058-B2 优先权日:2021-10-29 标 题:SHP2 and CDK4/6 dual-target inhibitory compound and pharmaceutical composition containing the same 发明人:WU XIAOXING; CHEN XIAOYU; LI WENQIANG; Shu Chengxia; LUO GUANGMEI; YANG KEXIN 权利人:UNIV CHINA PHARMA 摘要:The present invention belongs to the field of medicinal chemistry, and particularly relates to synthesis, a preparation method and the use of an inhibitor containing dual targets SHP2 and CDK4/6, wherein the inhibitor comprises three compounds of general formulas I-III and pharmaceutically acceptable salts, enantiomers, diastereomers, tautomers, solvates, polymorphs or prodrugs thereof. According to the present invention, a class of brand-new SHP2 and CDK4/6 dual-target inhibitors are prepared by means of a pharmacophore fusion and reasonable drug design method, so that the problems of drug resistance, poor drug effect, etc., of the existing SHP2 inhibitor and CDK4/6 inhibitor are solved; the great significance of the present invention is providing the first SHP2 and CDK4/6 dual-target inhibitor, which provides a basis for solving the problem of drug resistance of kinase and phosphatase in the later period.
[参考文献]: N Sundaraganesan, Et Al. Vibrational Spectra And Assignments Of 2-Amino-5-Iodopyridine By Ab Initio Hartree-Fock And Density Functional Methods. Spectrochim Acta A Mol Biomol Spectrosc. 2007 Jul;67(3-4):830-6. [参考文献]: R J Bochis, Et Al. Methyl 6-(Phenylsulfinyl)Imidazo[1,2-A]Pyridine-2-Carbamate, A Potent, New Anthelmintic. J Med Chem. 1978 Feb;21(2):235-7.
合成参考文献
摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 235. 摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 207. 摘要:Kitanosono, T.; Kobayashi, S., Science of Synthesis: Advances in Organoboron Chemistry towards Organic Synthesis, (2019) 1, 303.