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    2,4-pentadienoic acid derivatives having retinoid-like biological activity
    41.
    发明授权
    2,4-pentadienoic acid derivatives having retinoid-like biological activity 失效
    具有类视黄醇样生物活性的2,4-戊二烯酸衍生物

    公开(公告)号：US6034242A

    公开(公告)日：2000-03-07

    申请号：US165917

    申请日：1998-10-02

    申请人： Vidyasagar Vuligonda ,  Roshantha A. Chandraratna

    发明人： Vidyasagar Vuligonda ,  Roshantha A. Chandraratna

    IPC分类号： A61K31/35 ,  A61K31/20 ,  A61K31/23 ,  A61K31/38 ,  A61K31/47 ,  A61P17/00 ,  A61P43/00 ,  C07C57/50 ,  C07C69/618 ,  C07C215/02 ,  C07C215/18 ,  C07C311/58 ,  C07C335/06 ,  C07C403/00 ,  C07D277/22 ,  C07D311/58 ,  C07D333/54 ,  C07D335/06 ,  C07D215/06 ,  C07D215/12

    CPC分类号： C07D333/54 ,  A61K31/20 ,  A61K31/23 ,  C07C57/50 ,  C07C69/618 ,  C07D311/58 ,  C07D335/06

    摘要： Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is NR.sub.5 ; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lover alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CO.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, have retinoid like biological activity.

    摘要翻译： 式1的化合物，其中Z选自式3中所示的基团，Y是任选被一个或两个R 4基团取代的碳原子数为3至8的环烷基或环烯基，所述基团任选被一个或两个R 4基团取代 ，二价Y基团被相邻碳上的Z和-CR1 = CR1-CR1 = CR1基团取代; X是NR5; R1和R2独立地为H，低级烷基或氟代烷基; R3是氢，有情人烷基，Cl或Br; R4是低级烷基，氟烷基或卤素; R5是H或低级烷基，B是氢，COOH或其可药用盐，COOR8，CO9R10，-CH2OH，CH2OR11，CH2OCOR11，CHO，CH（OR12）2，CHOR13O，-COR7，CR7（OR12） CR 7OR 13 O或三低级烷基甲硅烷基，其中R 7为含有1至5个碳的烷基，环烷基或烯基，R 8为碳原子数1至10的烷基，碳原子数为5至10的环烷基或烷基具有的三甲基甲硅烷基烷基 1至10个碳，或R8为苯基或低级烷基苯基，R9和R10独立地为氢，1-10个碳原子的烷基或5-10个碳原子的环烷基，或苯基或低级烷基苯基，R11为低级烷基， 苯基或低级烷基苯基，R12为低级烷基，R13为2-5个碳原子的二价烷基，具有类视黄醇类生物活性。

    Process for the selective preparation of monohydroxyalkylated amines
    49.
    发明授权
    Process for the selective preparation of monohydroxyalkylated amines 失效
    选择性制备单羟基烷基化胺的方法

    公开(公告)号：US4223138A

    公开(公告)日：1980-09-16

    申请号：US891562

    申请日：1978-03-29

    申请人： Rudiger Schubart

    发明人： Rudiger Schubart

    IPC分类号： C07C215/06 ,  C07C67/00 ,  C07C213/00 ,  C07C213/04 ,  C07C215/02 ,  C07C217/08 ,  C07D211/58 ,  C07D295/088 ,  C07C89/02

    CPC分类号： C07D295/088 ,  C07D211/58

    摘要： A process for the preparation of an aminoethanol is described wherein an amine is vaporized in a collection vessel and the vapors are caused to pass upwardly through a defined reaction zone into a condensation zone where they are condensed and caused to flow downwardly into the reaction zone. In the reaction zone the flow toward the collection zone is retarded and, while retarded, epoxide reactant is directed thereagainst. The aminoethanol so formed is removed into the collection zone such as by directing condensed amine thereagainst.

    摘要翻译： 描述了制备氨基乙醇的方法，其中胺在收集容器中蒸发，并使蒸气向上通过限定的反应区进入冷凝区，在冷凝区中冷凝并使其向下流入反应区。 在反应区域中，朝向收集区的流动被延迟，并且在延迟时，环氧化物反应物被引导到其上。 如此形成的氨基乙醇被除去到收集区，例如通过在其上引入缩合胺。

    Branched polymers
    50.
    发明授权
    Branched polymers 有权
    支链聚合物

    公开(公告)号：US08809453B2

    公开(公告)日：2014-08-19

    申请号：US13865912

    申请日：2013-04-18

    申请人： Nektar Therapeutics

    发明人： Michael David Bentley ,  Xuan Zhao ,  Xiaoming Shen ,  William Dudley Battle, III

    IPC分类号： C08G63/91 ,  C08G63/48 ,  C07C215/02

    CPC分类号： C08G65/48 ,  A61K47/60 ,  A61K47/6901 ,  C07K17/08 ,  C08G65/329 ,  C08G65/3322 ,  C08L2203/02 ,  C12N9/96

    摘要： The present invention is directed to branched reactive water-soluble polymers comprising at least two polymer arms, such as poly(ethylene glycol), attached to a central aliphatic hydrocarbon core molecule through heteroatom linkages. The branched polymers bear at least one functional group for reacting with a biologically active agent to form a biologically active conjugate. The functional group of the branched polymer can be directly attached to the aliphatic hydrocarbon core or via an intervening linkage, such as a heteroatom, -alkylene-, —O-alkylene-O—, -alkylene-O-alkylene-, -aryl-O—, —O-aryl-, (—O-alkylene-)m, or (-alkylene-O—)m linkage, wherein m is 1-10.

    摘要翻译： 本发明涉及包含通过杂原子键连接到中心脂族烃核心分子的至少两个聚合物臂（例如聚（乙二醇））的支链反应性水溶性聚合物。 支链聚合物具有至少一个用于与生物活性剂反应以形成生物活性缀合物的官能团。 支链聚合物的官能团可以直接连接到脂族烃核心上或通过插入键如杂原子， - 亚烷基 - ， - - 亚烷基-O-， - 亚烷基-O-亚烷基 - ， - 芳基 - O-，-O-芳基 - ，（ - - 亚烷基 - ）m或（ - 亚烷基-O-）m键，其中m为1-10。