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    Hydrophobic taxane derivatives
    1.
    发明授权
    Hydrophobic taxane derivatives 失效
    疏水紫杉烷衍生物

    公开(公告)号：US06291690B1

    公开(公告)日：2001-09-18

    申请号：US09567366

    申请日：2000-05-09

    申请人： Eric Mayhew ,  J. Craig Franklin ,  Suresh Bhatia ,  Paul A. Harmon ,  Andrew S. Janoff

    发明人： Eric Mayhew ,  J. Craig Franklin ,  Suresh Bhatia ,  Paul A. Harmon ,  Andrew S. Janoff

    IPC分类号： C07D30514

    CPC分类号： B82Y5/00 ,  A61K9/127 ,  C07D305/14 ,  C07F9/65512

    摘要： This invention provides a taxane derivative of the formula: wherein a hydrophobic organic moiety is attached to a taxane. R and R1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.

    摘要翻译： 本发明提供下式的紫杉烷衍生物：其中疏水性有机部分连接于紫杉烷。 R和R 1各自独立地为H或疏水性有机部分，只要R和R 1中的至少一个不为H.将疏水性有机部分连接到紫杉烷以获得紫杉烷衍生物通常稳定该衍生物的缔合 其中包含脂质体脂质的脂质，其中施用衍生物 - 载体缔合的动物血浆中的载体。 本文还提供含有紫杉烷衍生物和药学上可接受的介质的组合物; 理想地，培养基还含有脂质载体，并且该衍生物与载体相关联。 本文还提供了将紫杉烷衍生物施用于动物，例如患有癌症的动物的方法。

    Hydrophobic taxane derivatives
    3.
    发明授权
    Hydrophobic taxane derivatives 失效
    疏水紫杉烷衍生物

    公开(公告)号：US5580899A

    公开(公告)日：1996-12-03

    申请号：US474888

    申请日：1995-06-07

    申请人： Eric Mayhew ,  J. Craig Franklin ,  Suresh Bhatia ,  Paul A. Harmon ,  Andrew S. Janoff

    发明人： Eric Mayhew ,  J. Craig Franklin ,  Suresh Bhatia ,  Paul A. Harmon ,  Andrew S. Janoff

    IPC分类号： A61K9/127 ,  A61K31/335 ,  A61K31/337 ,  A61K31/66 ,  A61P35/00 ,  C07D305/14 ,  C07F9/655

    CPC分类号： B82Y5/00 ,  A61K9/127 ,  C07D305/14 ,  C07F9/65512

    摘要： This invention provides a taxane derivative of the formula: ##STR1## wherein a hydrophobic organic moiety is attached to a taxane. R and R.sup.1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R.sup.1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.

    摘要翻译： 本发明提供下式的紫杉烷衍生物：其中疏水性有机部分连接于紫杉烷。 R和R 1各自独立地为H或疏水性有机部分，只要R和R 1中的至少一个不为H.将疏水性有机部分连接到紫杉烷以获得紫杉烷衍生物通常稳定该衍生物的缔合 其中包含脂质体脂质的脂质，其中施用衍生物 - 载体缔合的动物血浆中的载体。 本文还提供含有紫杉烷衍生物和药学上可接受的介质的组合物; 理想地，培养基还含有脂质载体，并且该衍生物与载体相关联。 本文还提供了将紫杉烷衍生物施用于动物，例如患有癌症的动物的方法。

    Preparation of liposomal taxanes
    4.
    发明授权
    Preparation of liposomal taxanes 失效
    脂质体紫杉烷的制备

    公开(公告)号：US6118011A

    公开(公告)日：2000-09-12

    申请号：US753650

    申请日：1996-11-27

    申请人： Eric Mayhew ,  J. Craig Franklin ,  Suresh Bhatia ,  Paul A. Harmon ,  Andrew S. Janoff

    发明人： Eric Mayhew ,  J. Craig Franklin ,  Suresh Bhatia ,  Paul A. Harmon ,  Andrew S. Janoff

    IPC分类号： A61K9/127 ,  A61K31/335 ,  A61K31/337 ,  A61K31/66 ,  A61P35/00 ,  C07D305/14 ,  C07F9/655

    CPC分类号： B82Y5/00 ,  A61K9/127 ,  C07D305/14 ,  C07F9/65512

    摘要： This invention provides a taxane derivative of the formula: ##STR1## wherein a hydrophobic organic moiety is attached to a taxane. R and R.sup.1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R.sup.1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.

    摘要翻译： 本发明提供下式的紫杉烷衍生物：其中疏水性有机部分连接于紫杉烷。 R和R 1各自独立地为H或疏水性有机部分，只要R和R 1中的至少一个不为H.将疏水性有机部分连接到紫杉烷以获得紫杉烷衍生物通常稳定该衍生物的缔合 其中包含脂质体脂质的脂质，其中施用衍生物 - 载体缔合的动物血浆中的载体。 本文还提供含有紫杉烷衍生物和药学上可接受的介质的组合物; 理想地，培养基还含有脂质载体，并且该衍生物与载体相关联。 本文还提供了将紫杉烷衍生物施用于动物，例如患有癌症的动物的方法。

    Synthesis of hydrophobic taxane derivatives
    5.
    发明授权
    Synthesis of hydrophobic taxane derivatives 失效
    疏水性紫杉烷衍生物的合成

    公开(公告)号：US5939567A

    公开(公告)日：1999-08-17

    申请号：US988120

    申请日：1997-12-10

    申请人： Eric Mayhew ,  J. Craig Franklin ,  Suresh Bhatia ,  Paul A. Harmon ,  Andrew S. Janoff

    发明人： Eric Mayhew ,  J. Craig Franklin ,  Suresh Bhatia ,  Paul A. Harmon ,  Andrew S. Janoff

    IPC分类号： A61K9/127 ,  A61K31/335 ,  A61K31/337 ,  A61K31/66 ,  A61P35/00 ,  C07D305/14 ,  C07F9/655

    CPC分类号： B82Y5/00 ,  A61K9/127 ,  C07D305/14 ,  C07F9/65512

    摘要： This invention provides a taxane derivative of the formula: ##STR1## wherein a hydrophobic organic moiety is attached to a taxane. R and R.sup.1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R.sup.1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.

    摘要翻译： 本发明提供下式的紫杉烷衍生物：其中疏水性有机部分连接于紫杉烷。 R和R 1各自独立地为H或疏水性有机部分，只要R和R 1中的至少一个不为H.将疏水性有机部分连接到紫杉烷以获得紫杉烷衍生物通常稳定该衍生物的缔合 其中包含脂质体脂质的脂质，其中施用衍生物 - 载体缔合的动物血浆中的载体。 本文还提供含有紫杉烷衍生物和药学上可接受的介质的组合物; 理想地，培养基还含有脂质载体，并且该衍生物与载体相关联。 本文还提供了将紫杉烷衍生物施用于动物，例如患有癌症的动物的方法。