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    Process for the preparation of N-(haloalkyl)sulfonamide
    1.
    发明授权
    Process for the preparation of N-(haloalkyl)sulfonamide 失效
    制备N-（卤代烷基）磺酰胺的方法

    公开(公告)号：US4265825A

    公开(公告)日：1981-05-05

    申请号：US76111

    申请日：1979-09-17

    申请人： Peter W. Owen ,  Zita K. Harmon ,  Donald A. Tomalia

    发明人： Peter W. Owen ,  Zita K. Harmon ,  Donald A. Tomalia

    IPC分类号： C07C311/00 ,  C07C143/72

    CPC分类号： C07C311/00

    摘要： N-(haloalkyl)sulfonamides represented by the formula ##STR1## wherein R.sub.1 is a C.sub.1 -C.sub.20 aryl, alkaryl, aralkyl or alkyl group; R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen or methyl groups; n is the integer 0 or 1 and X is a chloro, bromo or iodo group, are prepared by reacting an N-(haloalkyl)sulfonyl imide with a C.sub.1 -C.sub.6 alkanol.

    摘要翻译： 由式（I）表示的N-（卤代烷基）磺酰胺其中R 1是C 1 -C 20芳基，烷芳基，芳烷基或烷基; R2，R3和R4各自独立地为氢或甲基; n是整数0或1，X是氯，溴或碘基团，通过使N-（卤代烷基）磺酰亚胺与C 1 -C 6烷醇反应制备。

    Method for preparing 2-alkenyl-2-oxazolines
    2.
    发明授权
    Method for preparing 2-alkenyl-2-oxazolines 失效
    2-链烯基-2-恶唑啉的制备方法

    公开(公告)号：US4376861A

    公开(公告)日：1983-03-15

    申请号：US327299

    申请日：1981-12-03

    申请人： James W. Lalk ,  Gerald C. Kolb ,  Donald A. Tomalia ,  Peter W. Owen

    发明人： James W. Lalk ,  Gerald C. Kolb ,  Donald A. Tomalia ,  Peter W. Owen

    IPC分类号： C07D263/12 ,  C07D263/14

    CPC分类号： C07D263/14 ,  C07D263/12

    摘要： The process comprises the steps of:(A) reacting by contacting an anhydrous or substantially anhydrous 2-alkyl-2-oxazoline with formaldehyde in a molar ratio of at least about 1.5 moles of 2-alkyl-2-oxazoline per mole of formaldehyde, thereby forming 2-(.alpha.-hydroxymethylalkyl)-2-oxazoline,(B) recovering the 2-(.alpha.-hydroxymethylalkyl)-2-oxazoline from the reaction product of step (A), and(C) reacting by contacting the 2-(.alpha.-hydroxymethylalkyl)-2-oxazoline and step B with an alkali or alkaline earth metal hydroxide, thereby forming 2-alkenyl-2-oxazoline.As an example, step A was conducted by reacting 2-ethyl-2-oxazoline (4 moles) having less than 1,000 ppm of water with paraformaldehyde (1 mole) at a reaction temperature of 100.degree. C. for approximately 5.5 hours. The excess oxazoline reactant was removed along with water as "overheads" by fractional distillation of the reaction product, leaving the 2-(.alpha.-hydroxymethylethyl)-2-oxazoline in approximately 96 percent yield. Step C was then conducted by continuously adding the 2-(.alpha.-hydroxymethylethyl)-2-oxazoline to a stirred solution of sodium hydroxide in the mono-methyl ether of triethylene glycol at a temperature of from 100.degree.-105.degree. C. Under these conditions, the 2-isopropenyl-2-oxazoline and water were volatilized and recovered from the overheads. The product yield was approximately 98 percent of theory.

    摘要翻译： 该方法包括以下步骤：（A）使无水或基本上无水的2-烷基-2-恶唑啉与甲醛的摩尔比为至少约1.5摩尔的2-烷基-2-恶唑啉/摩尔甲醛， 从而形成2-（α-羟甲基烷基）-2-恶唑啉，（B）从步骤（A）的反应产物中回收2-（α-羟甲基烷基）-2-恶唑啉，和（C） （α-羟甲基烷基）-2-恶唑啉和步骤B与碱金属或碱土金属氢氧化物反应，从而形成2-链烯基-2-恶唑啉。 作为实例，通过在100℃的反应温度下使具有小于1000ppm水的2-乙基-2-恶唑啉（4摩尔）与多聚甲醛（1摩尔）反应约5.5小时来进行步骤A. 通过反应产物的分馏，将过量的恶唑啉反应物与水一起作为“塔顶馏出物”除去，留下2-（α-羟基甲基乙基）-2-恶唑啉约96％产率。 然后通过将2-（α-羟基甲基乙基）-2-恶唑啉连续加入到三乙二醇的单甲基醚的搅拌的氢氧化钠溶液中，在100〜105℃的温度下进行步骤C.在这些 条件下，将2-异丙烯基-2-恶唑啉和水挥发并从塔顶馏出物中回收。 产品产量约为理论的98％。

    Dendritic-antineoplastic drug delivery system
    3.
    发明授权
    Dendritic-antineoplastic drug delivery system 失效

    公开(公告)号：US07005124B2

    公开(公告)日：2006-02-28

    申请号：US10016733

    申请日：2001-10-29

    申请人： Navid Malik ,  Ruth Duncan ,  Donald A. Tomalia ,  Roseita Esfand

    发明人： Navid Malik ,  Ruth Duncan ,  Donald A. Tomalia ,  Roseita Esfand

    IPC分类号： A61K47/48 ,  A61K33/24 ,  A61K31/80

    CPC分类号： B82Y5/00 ,  A61K47/6949 ,  C08G69/00 ,  C08G69/02 ,  C08G83/003 ,  Y10S424/16

    摘要： Antineoplastic dendritic polymer conjugates which are useful drug delivery systems for carrying antineoplastic agents to malignant tumors are prepared by obtaining a dendritic polymer having functional groups which are accessible to an antineoplastic agent capable of interacting with the functional groups, and contacting the dendritic polymer with the antineoplastic agent. The preferred platin-based analogues of the antineoplastic agents conjugated to the dendritic polymer may be administered intravenously, orally, parentally, subcutaneously, intramuscularly, intraarterially or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The antineoplastic dendritic polymer conjugates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, reduced toxicity, and improved anti-tumor activity in vivo.

    Multifunctional nanodevice platform
    4.
    发明授权
    Multifunctional nanodevice platform 失效
    多功能纳米设备平台

    公开(公告)号：US06471968B1

    公开(公告)日：2002-10-29

    申请号：US09570198

    申请日：2000-05-12

    申请人： James R. Baker, Jr. ,  Donald A. Tomalia

    发明人： James R. Baker, Jr. ,  Donald A. Tomalia

    IPC分类号： C07H2104

    CPC分类号： B82Y5/00 ,  A61K41/0057 ,  A61K41/0071 ,  A61K47/6949 ,  C08G83/003

    摘要： The present invention relates to novel therapeutic and diagnostic arrays. More particularly, the present invention is directed to dendrimer based multifunctional compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems generally comprise two or more separate components for targeting, imaging, sensing, and/or triggering release of a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).

    摘要翻译： 本发明涉及新的治疗和诊断阵列。 更具体地，本发明涉及用于疾病诊断和治疗（例如癌症诊断和治疗）的基于树枝状大分子的多功能组合物和系统。 组合物和系统通常包含用于靶向，成像，感测和/或触发治疗或诊断材料释放并监测对细胞或组织（例如肿瘤）的治疗的反应的两个或更多个单独组分。

    Process for preparation of water borne curing agents
    6.
    发明授权
    Process for preparation of water borne curing agents 失效
    水性固化剂的制备方法

    公开(公告)号：US5705573A

    公开(公告)日：1998-01-06

    申请号：US708677

    申请日：1996-09-05

    申请人： Douglas R. Swanson ,  Donald A. Tomalia

    发明人： Douglas R. Swanson ,  Donald A. Tomalia

    IPC分类号： C08F8/00

    CPC分类号： C08F8/32

    摘要： A novel process for preparing poly(2-isopropenyl-2-oxazoline or oxazine) and its methyl methacrylate copolymer, which are useful as water borne curing agents, particularly in the non-stick coating industry. The process converts commercially available poly(methyl methacrylate) into poly(2-isopropenyl-2-oxazoline or oxazine) polymers or copolymers with methyl methacrylate, while circumventing the use of the highly toxic monomer, 2-isopropenyl-2-oxazoline or oxazine. The process involves converting a poly(methacrylic ester) to the corresponding poly(.beta.-hydroxy-N-ethyl or propyl methacrylamide) and activating the ring-forming .beta.-hydroxy-N-ethyl or propyl methacrylamide moiety to form an oxazoline or oxazine ring.

    摘要翻译： 制备聚（2-异丙烯基-2-恶唑啉或恶嗪）及其甲基丙烯酸甲酯共​​聚物的新方法，其可用作水性固化剂，特别是在不粘涂料工业中。 该方法将市售的聚（甲基丙烯酸甲酯）转化成聚（2-异丙烯基-2-恶唑啉或恶嗪）聚合物或与甲基丙烯酸甲酯共​​聚物，同时避免使用高毒性单体2-异丙烯基-2-恶唑啉或恶嗪。 该方法包括将聚（甲基丙烯酸酯）转化为相应的聚（β-羟基-N-乙基或丙基甲基丙烯酰胺）并活化成环β-羟基-N-乙基或丙基甲基丙烯酰胺部分以形成恶唑啉或恶嗪环 。

    Removal of 2-isopropenyl-2-oxazoline monomer
    9.
    发明授权
    Removal of 2-isopropenyl-2-oxazoline monomer 失效
    去除2-异丙烯基-2-恶唑啉单体

    公开(公告)号：US4357464A

    公开(公告)日：1982-11-02

    申请号：US254246

    申请日：1981-04-15

    申请人： Donald A. Tomalia ,  Timothy J. Adaway

    发明人： Donald A. Tomalia ,  Timothy J. Adaway

    IPC分类号： C08F6/00 ,  C08F6/10

    CPC分类号： C08F6/006

    摘要： The level of residual 2-isopropenyl-2-oxazoline monomer in polymers prepared therefrom can be reduced by reaction of the protonated salt of the monomer with a variety of nucleophiles. The products of the reaction with the monomer are much less toxic than the 2-isopropenyl-2-oxazoline and the utility of the polymer is thereby enhanced. The reaction product of 2-isopropenyl-2-oxazoline and H.sub.2 SO.sub.3 is itself novel and useful.

    摘要翻译： 由其制备的聚合物中残留的2-异丙烯基-2-恶唑啉单体的水平可以通过单体的质子化盐与各种亲核试剂的反应来降低。 与单体的反应产物的毒性远低于2-异丙烯基-2-恶唑啉，从而提高了聚合物的用途。 2-异丙烯基-2-恶唑啉和H 2 SO 3的反应产物本身是新颖的和有用的。

    Vinyl substituted cyclic polyethers and addition polymers thereof
    10.
    发明授权
    Vinyl substituted cyclic polyethers and addition polymers thereof 失效
    乙烯基取代的环状聚醚及其加成聚合物

    公开(公告)号：US4351933A

    公开(公告)日：1982-09-28

    申请号：US271745

    申请日：1981-06-08

    申请人： Thomas A. Chamberlin ,  Donald A. Tomalia

    发明人： Thomas A. Chamberlin ,  Donald A. Tomalia

    IPC分类号： B01D53/14 ,  B01J45/00 ,  C02F1/28 ,  C07D323/00 ,  C08F16/26 ,  C08F20/28 ,  C08F20/22 ,  C08F20/26

    CPC分类号： B01J45/00 ,  B01D53/1493 ,  C02F1/285 ,  C07D323/00 ,  C08F16/26 ,  C08F20/28

    摘要： Compounds represented by the formula: ##STR1## and addition polymers thereof where m is an integer from 2 to about 10, X-- is chlorine, hydroxy, carboxy or:--AC--R).dbd.CH.sub.2--R is hydrogen or methyl, --R--' is an ethylene or propylene group and--AC--R).dbd.CH.sub.2is one of: ##STR2## These compounds and their addition polymers form complexes with alkali metal or alkaline earth metal salts and permit the concentration of aqueous solutions of said salts. For example, a compound of the formula: ##STR3## is polymerized with an azobis (isobutyronitrile) catalyst to form addition polymers of the repeating unit ##STR4## When cross-linked, rendering it water-insoluble, such an addition polymer concentrates an aqueous solution of sodium chloride when contacted with same at about 0.degree. C.

    摘要翻译： 由下式表示的化合物及其加成聚合物，其中m为2至约10的整数，X-为氯，羟基，羧基或：-AC-R）= CH 2 -R为氢或甲基，-R - '是乙烯或丙烯基，-AC-R）= CH 2是以下之一：这些化合物及其加成聚合物与碱金属或碱土金属盐形成络合物，并允许浓度为 说盐。 例如，下式的化合物与偶氮二（异丁腈）催化剂聚合以形成重复单元的加成聚合物。当交联时，使其不溶于水，这种加成聚合物将水 氯化钠在约0℃下与其接触时的溶液