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    ARYL CARBAMATE OLIGOMERS FOR HYDROLYZABLE PRODRUGS AND PRODRUGS COMPRISING SAME
    2.
    发明申请
    ARYL CARBAMATE OLIGOMERS FOR HYDROLYZABLE PRODRUGS AND PRODRUGS COMPRISING SAME 审中-公开
    用于可水解产品的ARYL碳酸酯低聚物和包含其的原料

    公开(公告)号：WO2005016240A2

    公开(公告)日：2005-02-24

    申请号：PCT/US2004/015004

    申请日：2004-05-06

    Applicant: NOBEX CORPORATION ,  EKWURIBE, Nnochiri N. ,  ODENBAUGH, Amy L.

    Inventor： EKWURIBE, Nnochiri N. ,  ODENBAUGH, Amy L.

    IPC: A61K

    CPC classification number: C07C235/48 ,  C07C41/16 ,  C07C41/26 ,  C07C43/23 ,  C07C45/673 ,  C07C45/71 ,  C07C47/575 ,  C07C49/84 ,  C07C271/22 ,  C07C271/28 ,  C07K7/02 ,  C07K7/06 ,  C07C43/2055

    Abstract: The present invention provides a compound having a formula: (I) where R 1 is selected from the group consisting of alkyl, -CH 2 (OC 2 H4)OCH 3 , and -(OC 2 H 4 )OCH 3 ; n is 0-4; Olig is an oligomer having a formula (I) where L is a optional linker moiety selected from the group consisting of CH 2 O , CH 2 OX , OX , C(O) , C(O)X, NH , NHC(O) , XNHC(O) , NHC(O)X , C(O)NH , C(O)NHX , and (I), where X is alkyl 1-6 or is not present, Y is N or O or is not present, and R 3 is alkyl 1-6 ; PAG is a linear or branched polyalkylene glycol moiety; R 2 is an alkyl 1-22 capping moiety if X is present or alkyl 2-22 if X is not present; and q is a number from 1 to the maximum number of branches on PAG; and m is 1-5.

    Abstract translation: 本发明提供具有式（I）的化合物，其中R 1选自烷基，-CH 2（OC 2 H 4）OCH 3和 - （OC 2 H 4）OCH 3; n为0-4; Olig是具有式（I）的低聚物，其中L是选自CH 2 O，CH 2 OX，OX，C（O），C（O）X，NH，NHC（O），XNHC（O） ），NHC（O）X，C（O）NH，C（O）NHX和（I），其中X是烷基1-6或不存在，Y是N或O或不存在，R 3 >是烷基1-6; PAG是直链或支链的聚亚烷基二醇部分; 如果X存在，则R 2为烷基-22封端部分，如果不存在X则为烷基2-22; q是PAG上从1到最大分支数的数字; m为1-5。

    METHODS OF SYNTHESIZING SUBSTANTIALLY MONODISPERSED MIXTURES OF POLYMERS HAVING POLYETHYLENE GLYCOL MOIETIES
    3.
    发明申请
    METHODS OF SYNTHESIZING SUBSTANTIALLY MONODISPERSED MIXTURES OF POLYMERS HAVING POLYETHYLENE GLYCOL MOIETIES 审中-公开
    合成具有聚乙二醇纤维素的聚合物的主要单体混合物的方法

    公开(公告)号：WO2002098949A1

    公开(公告)日：2002-12-12

    申请号：PCT/US2002/017619

    申请日：2002-06-04

    Applicant: NOBEX CORPORATION ,  EKWURIBE, Nnochiri, N. ,  PRICE, Christopher, H. ,  ANSARI, Aslam, M. ,  ODENBAUGH, Amy, L.

    Inventor： EKWURIBE, Nnochiri, N. ,  PRICE, Christopher, H. ,  ANSARI, Aslam, M. ,  ODENBAUGH, Amy, L.

    IPC: C08G65/00

    CPC classification number: C08G65/334 ,  C08L71/02 ,  C08L71/00

    Abstract: Methods of synthesizing a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties include: reacting a substantially monodispersed mixture of compounds having the structure of Formula I: R 1 (OC 2 H 4 )n-O - X + (I) wherein R 1 is H or a lipophilic moiety; n is from 1 to 25; and X + is a positive ion, with a substantially monodispersed mixture of compounds having the structure of Formula II: R 2 (OC 2 H 4 ) m -OMs (II) wherein R 2 is H or a lipophilic moiety; and m is from 1 to 25,under conditions sufficient to provide a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties and having the structure of Formula III: R 2 (OC 2 H 4 ) m+n -OR 1 (III).

    Abstract translation: 合成基本上单分散的包含聚乙二醇部分的聚合物的混合物的方法包括：使具有式I结构的化合物的基本上单分散的混合物：R 1（OC 2 H 4）n O X +（I） 1>是H或亲脂性部分; n为1至25; 并且X +是具有式II结构的化合物的基本上单分散的混合物：R 2（OC 2 H 4）m-OM（II）其中R 2是H或亲油部分; 并且m为1至25，在足以提供包含聚乙二醇部分并且具有式III结构的基本单分散混合物的条件下：R 2（OC 2 H 4）m + n -OR 1（III）。

    MIXTURES OF CALCITONIN DRUG-OLIGOMER CONJUGATES AND METHODS OF USE IN PAIN TREATMENT
    8.
    发明申请
    MIXTURES OF CALCITONIN DRUG-OLIGOMER CONJUGATES AND METHODS OF USE IN PAIN TREATMENT 审中-公开
    卡米酮类药物与低剂量混合物的混合物及其在疼痛治疗中的应用方法

    公开(公告)号：WO2005004792A2

    公开(公告)日：2005-01-20

    申请号：PCT/US2004/016784

    申请日：2004-05-27

    Applicant: NOBEX CORPORATION ,  KOSUTIC, Gordana ,  EKWURIBE, Nnochiri, N. ,  PRICE, Christopher, H. ,  ANSARI, Aslam, M. ,  ODENBAUGH, Amy, L.

    Inventor： KOSUTIC, Gordana ,  EKWURIBE, Nnochiri, N. ,  PRICE, Christopher, H. ,  ANSARI, Aslam, M. ,  ODENBAUGH, Amy, L.

    IPC: A61K

    CPC classification number: A61K38/23 ,  A61K47/60

    Abstract: A mixture of conjugates in which each conjugate in the mixture comprises a calcitonin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may lower serum calcium levels in a subject by 10, 15 or even 20 percent or more. Moreover, the mixture may be more effective at surviving an in vitro model of intestinal digestion than non-conjugated calcitonin. Furthermore, the mixture may exhibit a higher bioavailability than non-conjugated calcitonin. The compositions of this invention are useful in the treatment of various bone disorders and pain.

    Abstract translation: 公开了混合物的混合物，其中混合物中的每个缀合物包含与包含聚亚烷基二醇部分的低聚物偶联的降钙素药物。 该混合物可使受试者中的血清钙水平降低10,15或甚至20％或更多。 此外，混合物在存活肠内消化的体外模型方面比非共轭降钙素更有效。 此外，该混合物可能表现出比非共轭降钙素更高的生物利用度。 本发明的组合物可用于治疗各种骨骼疾病和疼痛。

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