📜N-甲氧基-N-甲基烟酰胺置于1,2-双(二苯基膦基)苯,三异丁基铝,Bis(Dibenzylideneacetone)-Palladium(0)体系中,用 正己烷 用作溶剂,化学反应 6.0H,以79%的收率获得n-甲基烟酰胺 参考文献:Dealkoxylation Of N-Alkoxyamides Without An External Reductant Driven By Pd/al Cooperative Catalysis 标题:Dealkoxylation Of N-Alkoxyamides Without An External Reductant Driven By Pd/al Cooperative Catalysis 摘要:Lewis酸辅助钯催化的n-烷氧基酰胺脱烷氧化反应在无外部还原剂的情况下实现. Doi:10.1039/d0Ob01815E
专利号:US-8653282-B2 优先权日:2007-10-18 标 题:Preparation of dihydrothieno [3,2-D] pyrimidines and intermediates used therein 发明人:FRUTOS ROGELIO; KRISHNAMURTHY DHILEEPKUMAR; MULDER JASON ALAN; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; TAMPONE THOMAS G 权利人:FRUTOS ROGELIO; KRISHNAMURTHY DHILEEPKUMAR; MULDER JASON ALAN; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; TAMPONE THOMAS G; BOEHRINGER INGELHEIM INT 摘要:The invention relates to improved methods of preparing dihydrothienopyrimidines of formula 1, and intermediates thereof, (I) wherein X is SO or SO 2 , preferably SO, and wherein R A , R 1 , R 2 , R 3 , R 4 and R 5 have the meanings given in the description. The methods according to this invention are more suitable for large-scale synthesis of said compounds than prior methods because the new synthetic process avoids distillation and chromatographic purification between steps and results in a higher overall yield of the desired product.
专利号:US-2023135239-A1 优先权日:2021-11-04 标 题 :Drug for treating severe acute respiratory syndrome caused by coronavirus and complications thereof and use of the drug 发明人:YU WENQIANG; LI ZHENYAN; XU JIANQING; LI WEI; LIAN CHENG 权利人:SHANGHAI PUBLIC HEALTH CLINICAL CT; SHANGHAI YIZHE BIOTECHNOLOGY CO LTD 摘要:The present invention discloses a drug for treating severe acute respiratory syndrome caused by coronavirus and the complications thereof and the use of the drug, and specifically the use of an agent in the preparation of a drug for treating severe acute respiratory syndrome caused by coronavirus and the complications thereof. The above-mentioned agent is at least one of hyaluronic acid synthesis inhibitor, hyaluronidase, hyaluronidase inhibitor, hyaluronic acid receptor inhibitor, and anticoagulant. The present invention is based on the discovery of an important pathogenic mechanism of severe acute respiratory syndrome-related coronavirus 2 that a sequence homologous to human in severe acute respiratory syndrome-related coronavirus 2, named HIS (Human Insert Sequence), can specifically activate hyaluronic acid synthase HAS and other inflammatory factors, and then it is found from clinical samples that the content of hyaluronic acid in the serum of a patient with severe COVID-19 is significantly higher than that in a patient with mild COVID-19. The above-mentioned agent is used for the first time for treating coronavirus and complications, and it is verified that a hyaluronic acid synthesis inhibitor can reduce the content of hyaluronic acid, thus the adjustment of hyaluronic acid level has good application value in the treatment and/or prevention of conditions caused by coronavirus.
专利号:US-8981092-B2 优先权日:2008-09-19 标题 :Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity 发明人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO 权利人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO; NERVIANO MEDICAL SCIENCES SRL 摘要:Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, n nor pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
专利号:US-7354923-B2 优先权日:2001-08-10 标 题 :Piperazine melanocortin-specific compounds 发明人:SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH 权利人:PALATIN TECHNOLOGIES INC 摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure: n nand stereoisomer and pharmaceutically acceptable salts thereof, where X is CH 2 or Câ•?O, R 1 , R 2 , and R 3 are as described in the specification, preferably where R 3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R 3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.
专利号:WO-2018191771-A1 优先权日:2017-04-18 标题 :Detection and treatment of congenital malformations 发明人:DUNWOODIE SALLY; SPARROW DUNCAN; STOCKER ROLAND; SHI HONGJUN 权利人:VICTOR CHANG CARDIAC RES INSTITUTE 摘要:The invention relates to a method of preventing or treating a congenital malformation in an unborn offspring of a subject, the method comprising administering to the subject a therapeutically effective amount of NAD or an intermediate of NAD synthesis.
专利号:US-2024216412-A1 优先权日:2022-11-22 标 题 :Oxidized nicotinamide adenine dinucleotide (nad+) precursor treatment for heart failure alleviation independent of mitochondrial protein deacetylation 发明人:TIAN RONG; WALKER MATTHEW 权利人:UNIV WASHINGTON 摘要:The current disclosure provides provides boosting intracellular NAD + with nicotinamide riboside chloride (NR) to protect from cardiac dysfunction, NR being a natural NAD + precursor that bypasses nicotinamide phosphoribosyltransferase (NAMPT) to stimulate intracellular NAD + synthesis.
摘要:HANSCH,C ET AL. (1995) 摘要:Yoshikai, N., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 274. 参考文献:10.1007/bf00171061 摘要:Martel F, Martins MJ, Azevedo I. Inward transport of 3H-MPP+ in freshly isolated rat hepatocytes: evidence for interaction with catecholamines. Naunyn Schmiedebergs Arch Pharmacol. 1996 Aug;354(3):305–11. doi: 10.1007/bf00171061.