专利号:US-2012165520-A1 优先权日:2010-12-23 标题:Process for the synthesis of prodrugs of opioids 发明人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 权利人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 摘要:The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-9828340-B2 优先权日:2013-02-21 标题 :Asymmetric synthesis of a substituted pyrrolidine-2-carboxamide 发明人:FISHLOCK DANIEL; GU CHEN; SHU LIANHE; REGE PANKAJ DEVDATTA; SARMA KESHAB 权利人:HOFFMANN LA ROCHE 摘要:The invention relates to a process for the preparation of 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid of the formula (I) n nas well as intermediates thereof and pharmaceutical preparations thereof, comprising the step of reacting a compound of the formula (IV) with a compound of the formula (V), as defined in the specification, in the presence of a chiral silver- or copper catalyst.
专利号:US-8933227-B2 优先权日:2009-08-14 标题 :Selective synthesis of functionalized pyrimidines 发明人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN 权利人:LINZ GUENTER; KRAEMER GERD; KUSSEROW SABRINA; SCHNAUBELT JUERGEN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to a process for making 2,4-differentiated 5-trifluoromethyl pyrimidines and 2-amino-5-trifluoromethyl-pyrimidine derivatives, which compounds are useful in the preparation of pharmacologically active compounds.
专利号:US-2018370905-A1 优先权日:2013-04-05 标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same
专利号:WO-2024041503-A1 优先权日:2022-08-22 标 题:Compounds targeting y220c mutant of p53 发明人:LI SUJING; LI AMIN; ZHENG QIAN; Dang Chaojie; FAN XINRUI; LONG WEI; WANG YANPING 权利人:JACOBIO PHARMACEUTICALS CO LTD 摘要:The present invention discloses compounds of formula (I) which can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. Also provided are processes for the synthesis and use of the compounds of formula (I).
参考文献:10.1007/s11696-024-03708-8 摘要:Wang K, Zhao D, Jin M, Li Y, Sun L, Zhu Y, Wang C, Li S, Wang Y, Miao Q, Chen X, Zhao Y, Hou Y. Multigram-scale synthesis of volasertib, an inhibitor of polo-like kinases in clinical evaluation. Chem. Pap. 2024 Oct 10;78(17):8965–77. doi: 10.1007/s11696-024-03708-8. 参考文献:10.1007/s11814-024-00366-0 摘要:Khuu QC, Le PD, Luu LC, Trinh HTT, Wolf SE, Nguyen TA. Additive-Induced Polymorphism of a Model Amino Acid Crystal. Korean J. Chem. Eng. 2024 Dec 23;42(4):885–900. doi: 10.1007/s11814-024-00366-0.