Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties
    6.
    发明授权
    Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties 有权
    合成具有聚乙二醇部分的聚合物的基本单分散混合物的方法

    公开(公告)号:US06835802B2

    公开(公告)日:2004-12-28

    申请号:US09873731

    申请日:2001-06-04

    IPC分类号: C08G6534

    摘要: 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: R1(OC2H4)n—O−X+  (I) wherein R1 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: R2(OC2H4)m—OMs  (II) wherein R2 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: R2(OC2H4)m+n—OR1  (III).

    摘要翻译: 合成包含聚乙二醇部分的基本上单分散的聚合物混合物的方法包括:使具有式I结构的化合物的基本上单分散的混合物:其中R 1为H或亲油部分; n为1至25; 并且X +是正离子,其具有具有式II结构的化合物的基本上单分散的混合物:其中R 2是H或亲脂性部分; 并且m为1至25,在足以提供包含聚乙二醇部分并具有式III结构的聚合物的基本上单分散混合物的条件下:

    Mixtures of calcitonin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
    7.
    发明授权
    Mixtures of calcitonin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same 失效
    包含聚亚烷基二醇的降钙素药物 - 低聚物共轭物的混合物及其制备方法及其制备方法

    公开(公告)号:US06713452B2

    公开(公告)日:2004-03-30

    申请号:US09873777

    申请日:2001-06-04

    IPC分类号: A61K3823

    CPC分类号: C07K14/585 A61K47/60

    摘要: 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.

    摘要翻译: 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时可能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。

    Mixtures of growth hormone drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
    9.
    发明授权
    Mixtures of growth hormone drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same 失效
    包含聚亚烷基二醇的生长激素药物 - 低聚物缀合物的混合物及其制备方法及其制备方法

    公开(公告)号:US06828305B2

    公开(公告)日:2004-12-07

    申请号:US09873757

    申请日:2001-06-04

    IPC分类号: A61K3827

    CPC分类号: C07K14/61 A61K38/27 A61K47/60

    摘要: Mixtures of conjugates in which each conjugate in the mixture comprises a growth hormone drug coupled to an oligomer that includes a polyalkylene glycol moiety wherein the mixtures have a molecular weight distribution with a standard deviation of less than about 22 Daltons are disclosed. Methods of treating growth hormone deficiency in a subject in need of such treatment and methods of accelerating the growth rate of an animal arc also disclosed. Processes for synthesizing substantially monodispersed mixtures of conjugates wherein each conjugate comprises a growth hormone drug coupled to an oligomer that comprises a polyethylene glycol moiety are further provided.

    摘要翻译: 缀合物的混合物,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生长激素药物,其中所述混合物具有小于约22道尔顿的标准偏差的分子量分布。 还公开了在需要这种治疗的受试者中治疗生长激素缺乏的方法和加速动物弧的生长速率的方法。 用于合成基本上单分散的缀合物混合物的方法,其中每个缀合物包含与包含聚乙二醇部分的低聚物偶联的生长激素药物。

    Substantially monodispersed mixtures of polymers having polyethylene glycol moieties
    10.
    发明授权
    Substantially monodispersed mixtures of polymers having polyethylene glycol moieties 有权
    具有聚乙二醇部分的聚合物的基本单分散混合物

    公开(公告)号:US07119162B2

    公开(公告)日:2006-10-10

    申请号:US10977973

    申请日:2004-10-29

    IPC分类号: C08G65/34

    摘要: 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: R1(OC2H4)n—O−X+   (I) wherein R1 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: R2(OC2H4)m—OMs   (II) wherein R2 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: R2(OC2H4)m+n—OR1 .   (III) Substantially monodispersed mixtures of polymers comprising polyethylene glycol moieties are also disclosed.

    摘要翻译: 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:<?in-line-formula description =“In-Line Formulas”end =“lead” (O 2 H 4) (I)<?in-line-formula description =“In-line formula”end =“tail”?>其中R 1是H或亲油部分; n为1至25; 并且X + +是正离子,其具有具有式II结构的化合物的基本上单分散的混合物:<?in-line-formula description =“In-line Formulas”end =“lead”? (II)H 2 -OMs(II)&lt;&lt;&lt;&lt; 2-in-line-formula description =“In-line Formulas”end =“tail”?>其中R 2是H或亲脂性部分; 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结构的基本上单分散的聚合物混合物的条件下:<?在线公式描述=“在线公式”末端=“铅 (○2 H 4)m + n - 或 - 1个/ SUP>。 (III)<?in-line-formula description =“In-line Formulas”end =“tail”?>还公开了包含聚乙二醇部分的聚合物的基本上单分散的混合物。