POLYMER CONJUGATES OF PROTEIN KINASE C INHIBITORS
    4.
    发明申请
    POLYMER CONJUGATES OF PROTEIN KINASE C INHIBITORS 审中-公开
    蛋白激酶C抑制剂的聚合物结合

    公开(公告)号:WO03037384A3

    公开(公告)日:2003-08-28

    申请号:PCT/US0234666

    申请日:2002-10-29

    CPC classification number: A61K47/60

    Abstract: The invention provides polymer conjugates of protein kinase C (PKC) inhibitors comprising a polymer, such as poly(ethylene glycol), covalently attached to a PKC inhibitor, such as a bisindolylmaleimide molecule. The linkage between the polymer and the PKC inhibitor is preferably hydrolytically degradable. The invention also includes a pharmaceutical composition comprising a polymer conjugate of a PKC inhibitor and a method of treating any condition responsive to a PKC inhibitor by administering a polymer conjugate of the invention.

    Abstract translation: 本发明提供蛋白激酶C(PKC)抑制剂的聚合物缀合物,其包含共价连接到PKC抑制剂如双吲哚基马来酰亚胺分子的聚(乙二醇)等聚合物。 聚合物和PKC抑制剂之间的连接优选是可水解降解的。 本发明还包括药物组合物,其包含PKC抑制剂的聚合物缀合物和通过施用本发明的聚合物缀合物来治疗对PKC抑制剂有反应的任何病症的方法。

    BRANCHED POLYMERS AND THEIR CONJUGATES
    5.
    发明申请
    BRANCHED POLYMERS AND THEIR CONJUGATES 审中-公开
    支化聚合物及其共轭物

    公开(公告)号:WO2003040211A2

    公开(公告)日:2003-05-15

    申请号:PCT/US2002/035759

    申请日:2002-11-07

    Abstract: 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.

    Abstract translation: 本发明涉及包含至少两个聚合物臂(例如聚乙二醇)的支化反应性水溶性聚合物,所述聚合物臂通过杂原子连接与中心脂族烃核心分子连接。 支化聚合物带有至少一个官能团,用于与生物活性剂反应形成生物活性缀合物。 支化聚合物的官能团可以直接连接到脂族烃核上或经由插入的键例如杂原子,亚烷基-O-亚烷基-O-, - 亚烷基-O-亚烷基 - , - 芳基 - O-,-O-芳基 - ,(-O-亚烷基 - )m或( - 亚烷基-O-)m连接,其中m是1-10。

    MULTI-ARM POLYPEPTIDE-POLY(ETHYLENE GLYCOL) BLOCK COPOLYMERS AS DRUG DELIVERY VEHICLES
    7.
    发明申请
    MULTI-ARM POLYPEPTIDE-POLY(ETHYLENE GLYCOL) BLOCK COPOLYMERS AS DRUG DELIVERY VEHICLES 审中-公开
    作为药物递送车辆的多臂多肽 - 聚(乙烯甘油)嵌段共聚物

    公开(公告)号:WO2004060977A1

    公开(公告)日:2004-07-22

    申请号:PCT/US2003/041332

    申请日:2003-12-24

    Abstract: The invention provides a mufti-arm block copolymer for use in delivering a variety of bioactive agents. The copolymer of the invention contains a central core from which extend multiple (3 or more) copolymer arms. Each copolymer arm possesses an inner polypeptide segment and an outer hydrophilic polymer segment. Thus, the overall structure of the copolymer comprises an inner core region that includes the central core and the inner polypeptide segment, while the outer core region is hydrophilic in nature. The mufti-arm copolymer of the invention is particularly useful for delivery of biologically active agents that can be entrapped within the inner core region.

    Abstract translation: 本发明提供了用于递送各种生物活性剂的多臂嵌段共聚物。 本发明的共聚物含有中心核,多个(3个或更多个)共聚物臂可从中心芯延伸。 每个共聚物臂具有内部多肽片段和外部亲水性聚合物片段。 因此,共聚物的总体结构包括内核区域,其包含中心核心和内部多肽区段,而外核区域本质上是亲水性的。 本发明的三臂共聚物特别可用于递送可被包埋在内芯区内的生物活性剂。

    WATER-SOLUBLE POLYMER CONJUGATES OF RETINOIC ACID
    9.
    发明申请
    WATER-SOLUBLE POLYMER CONJUGATES OF RETINOIC ACID 审中-公开
    水溶性聚合物的重组酸

    公开(公告)号:WO2003037385A1

    公开(公告)日:2003-05-08

    申请号:PCT/US2002/036421

    申请日:2002-10-30

    CPC classification number: A61K9/0075 A61K9/1641 A61K47/60 Y02A50/406

    Abstract: The present invention provides water-soluble polymer conjugates of retinoic acid. The conjugates of the invention are prepared by covalent attachment of a water-soluble and non-peptidic polymer such as polyethylene glycol to a retinoid such as retinoic acid. The polymer portion of the conjugate may be linear (i.e., prepared using an end-capped or methoxy PEG or a linear bifunctional PEG), branched or forked. The conjugates of the invention are water soluble, and are, in particular, useful for inhalation therapy of conditions of the respiratory tract responsive to retinoid therapy.

    Abstract translation: 本发明提供视黄酸的水溶性聚合物共轭物。 本发明的缀合物通过将水溶性和非肽类聚合物如聚乙二醇共价连接到类视黄醇如维甲酸来制备。 缀合物的聚合物部分可以是线性的(即使用端封端或甲氧基PEG或线性双功能PEG制备),分支或分叉。 本发明的缀合物是水溶性的,特别是用于对类视黄醇治疗有效的呼吸道病症的吸入治疗。

    POLYMER CONJUGATES OF PROTEIN KINASE C INHIBITORS
    10.
    发明申请
    POLYMER CONJUGATES OF PROTEIN KINASE C INHIBITORS 审中-公开
    蛋白激酶C抑制剂的聚合物共轭物

    公开(公告)号:WO2003037384A2

    公开(公告)日:2003-05-08

    申请号:PCT/US2002/034666

    申请日:2002-10-29

    CPC classification number: A61K47/60

    Abstract: The invention provides polymer conjugates of protein kinase C (PKC) inhibitors comprising a polymer, such as poly(ethylene glycol), covalently attached to a PKC inhibitor, such as a bisindolylmaleimide molecule. The linkage between the polymer and the PKC inhibitor is preferably hydrolytically degradable. The invention also includes a pharmaceutical composition comprising a polymer conjugate of a PKC inhibitor and a method of treating any condition responsive to a PKC inhibitor by administering a polymer conjugate of the invention.

    Abstract translation: 本发明提供蛋白激酶C(PKC)抑制剂的聚合物缀合物,其包含共价连接至PKC抑制剂如双吲哚基马来酰亚胺分子的聚合物(例如聚(乙二醇))。 聚合物和PKC抑制剂之间的连接优选是可水解降解的。 本发明还包括药物组合物,其包含PKC抑制剂的聚合物缀合物和通过施用本发明的聚合物缀合物来治疗对PKC抑制剂有响应的任何病症的方法。

Patent Agency Ranking