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    • 4. 发明申请
    • HYDROLYSABLE DELIVERY SYSTEM USING CROSS-LINKED POLYMERIC RESINS AS VEHICLES
    • 使用交联聚合树脂作为车辆的可水解输送系统
    • WO9844951A3
    • 1999-01-07
    • PCT/US9806144
    • 1998-03-30
    • MONSANTO COTREMONT SAMUEL J
    • TREMONT SAMUEL J
    • A61K47/48C08F8/00
    • C08F8/32A61K47/58C08F8/30C08F112/14
    • This invention provides a method of preparing a polymeric delivery system for active ingredients. The delivery system is formed either by attaching the active ingredient to a linker through a hydrolyzable covalent bond, then forming a covalent bond between the linker and a portion of the subunits of a cross-linked polymer, or by attaching a linker to a portion of the subunits of a cross-linked polymer, then attaching the active ingredient to the polymer-linker combination through a hydrolyzable covalent bond. The invention also provides a delivery system comprising an active ingredient covalently bonded through a hydrolyzale covalent bond to a linker, which is in turn covalently bonded to a portion of subunits of a cross-linked polymer.
    • 本发明提供了制备用于活性成分的聚合物递送系统的方法。 递送系统通过将活性成分连接到可通过可水解共价键的接头形成,然后在接头与交联聚合物的一部分亚单位之间形成共价键,或通过将接头连接到亚单位的一部分 的交联聚合物,然后通过可水解共价键将活性成分连接到聚合物 - 连接体组合。 本发明还提供一种递送系统,其包含通过可水解共价键共价键合到接头的活性成分,其接着共价键合到交联聚合物的一部分亚单位。
    • 7. 发明申请
    • PROCESS FOR THE PREPARATION OF N-PHOSPHONO-METHYLGLYCINE AND DERIVATIVES THEREOF
    • 制备N-膦酰基甲基甘氨酸及其衍生物的方法
    • WO2005019230A3
    • 2005-08-04
    • PCT/US2004027413
    • 2004-08-23
    • MONSANTO TECHNOLOGY LLCCOLEMAN JAMES PEBNER JERRY RHAUPFEAR ERIC ALENNON PATRICK JSCHAPER JOSEPH ATREMONT SAMUEL JWOLFSON SERGE GBRODSKY PHILIP H
    • COLEMAN JAMES PEBNER JERRY RHAUPFEAR ERIC ALENNON PATRICK JSCHAPER JOSEPH ATREMONT SAMUEL JWOLFSON SERGE GBRODSKY PHILIP H
    • C07F9/28C07F9/38
    • C07F9/3813Y02P20/582
    • N-phosphonomethylamines are produced by reaction of an amine substrate with a halomethylphosphonic acid or salt thereof, a hydroxymethylphosphonic acid or salt thereof, or a dehydrated self-ester dimer, trimer or oligomer of hydroxymethylphosphonic acid. Among the products that may be prepared according to the process are N-phosphonomethylaminocarboxylic acids such as (e.g.) glyphosate, N-phosphonomethylaminoalkanols such as (e.g.) hydroxyethlaminomethylphosphonic acid, and N-acylaminomethylphosphonic acids such as (e.g.) N-carbamylaminomethylphosphonic acid. Certain reactions are conducted with a substantial excess of amine reactant in order to drive the conversion while avoiding excessive formation of bis(N-phosphonomethyl)amine by-products. Other reactions use a secondary amine substrate (such as iminodiacetic acid) and can be conducted at substantial equimolar ratios of halomethylaminomethylphosphonic acid or hydroxyaminomethylphosphonic acid to secondary amine reactant without significant formation of bis(phosphonomethyl)amine by-products. Further disclosed is a process for the preparation of hydroxymethylphosphonic acid self-ester dimers, trimers and oligomers by azeotropic dehydration.
    • N-膦酰基甲基胺通过胺底物与卤代甲基膦酸或其盐,羟甲基膦酸或其盐,或羟甲基膦酸的脱水自酯二聚物,三聚物或低聚物反应而生成。 可以根据该方法制备的产品是N-膦酰基甲基氨基羧酸,例如(例如)草甘膦,N-膦酰基甲基氨基链烷醇例如羟基乙基氨基甲基膦酸和N-酰基氨基甲基膦酸例如N-氨基甲酰基氨基甲基膦酸。 用大量过量的胺反应物进行某些反应以驱动转化,同时避免过量形成双(N-膦酰基甲基)胺副产物。 其他反应使用仲胺底物(如亚氨基二乙酸),并且可以以基本上等摩尔比例的卤代甲基氨基甲基膦酸或羟基氨基甲基膦酸与仲胺反应物进行反应,而不显着形成双(膦酰基甲基)胺副产物。 还公开了通过共沸脱水制备羟甲基膦酸自酯二聚体,三聚体和低聚体的方法。