专利号:US-10975069-B2 优先权日:2014-04-01 标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof 发明人:HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN 权利人:UNIV WASHINGTON 摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
专利号:US-6365772-B1 优先权日:1995-05-30 标题 :Facile synthesis of phosphonomethylglycine from phosphonomethyliminodiacetic acid 发明人:CULLEN BARRY A; PARKER BRIAN A 权利人:HAMPSHIRE CHEMICAL CORP 摘要:A process for the preparation of phosphonomethylglycine in nearly quantitative yields which eliminates the use of a noble metal co-catalyst and its concomitant problems. The oxygen-containing gas is replaced with the much more chemically active hydrogen peroxide, which in combination with activated carbon, oxidizes the PMIDA to PMG in very high yield. The amount of oxidant allowed to react with PMIDA is a function of the concentration of oxygen in the gaseous reaction products, and is controlled by monitoring that concentration. In another embodiment, the oxidizing agent is an oxygen-containing gas. In either case, the concentration of oxygen in the gaseous reaction product is monitored to determine the end point of the reaction.
专利号:US-7220884-B2 优先权日:2004-02-10 标 题 :Hydroaminomethylation of olefins 发明人:BRIGGS JOHN R; WHITEKER GREGORY T; KLOSIN JERZY 权利人:DOW GLOBAL TECHNOLOGIES INC 摘要:The present invention relates to a method comprising the step of contacting under hydroaminomethylation conditions, an olefin, an amine, a rhodium-phosphorous ligand, and synthesis gas (syngas). In particular, it has been discovered that, under some circumstances, a neutral rhodium-monodentate phosphite ligand is prescribed. The invention provides a simple way of making, in high yields and regiospecificity, a variety of products, including pharmacologically active products such as ibutilide, terfenadine, and fexofenadine, and derivatives thereof.
专利号:WO-9638455-A1 优先权日:1995-05-30 标题:Facile synthesis of phosphonomethylglycine from phosphonomethyliminodiacetic acid
专利号:AU-698565-B2 优先权日:1995-05-30 标 题 :Facile synthesis of phosphonomethylglycine from phosphonomethyliminodiacetic acid
专利号:CN-1191539-A 优先权日:1995-05-30 标 题:A Simple Method for the Synthesis of Phosphonomethylglycine from Phosphonomethyliminodiacetic Acid