公开(公告)号：US06593292B1

公开(公告)日：2003-07-15

申请号：US09648400

申请日：2000-08-24

申请人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

发明人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

IPC分类号： A61K31496

CPC分类号： C07K7/06 ,  A61K47/54 ,  A61K47/55 ,  A61K47/557 ,  A61K47/62 ,  A61K47/645 ,  A61K47/665 ,  A61K49/0043 ,  A61K49/0056 ,  A61K49/085 ,  A61K49/146 ,  B82Y5/00 ,  C07K7/64

摘要： This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.

摘要翻译： 本发明提供用于增强药物和其它药物穿过上皮组织（包括皮肤，胃肠道，肺上皮等）的递送的组合物和方法。 组合物和方法也可用于穿过内皮组织，包括血脑屏障。 与非共轭化合物相比，组合物和方法使用具有足够的胍基或脒基侧链部分的递送增强转运蛋白，以增强与试剂缀合的化合物跨越组织的一个或多个层的递送。 递送增强聚合物包括例如优选长度在约6和25个残基之间的聚精氨酸分子。

公开(公告)号：US08623833B2

公开(公告)日：2014-01-07

申请号：US12816358

申请日：2010-06-15

申请人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

发明人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

IPC分类号： A61K38/08 ,  A61K38/16 ,  C12P13/10 ,  C07C231/00

CPC分类号： A61K47/48346 ,  A61K31/155 ,  A61K31/337 ,  A61K31/436 ,  A61K31/496 ,  A61K31/573 ,  A61K38/00 ,  A61K38/13 ,  A61K47/54 ,  A61K47/55 ,  A61K47/555 ,  A61K47/557 ,  A61K47/62 ,  A61K47/64 ,  A61K47/645 ,  A61K47/665 ,  A61K49/0043 ,  A61K49/0056 ,  A61K49/085 ,  A61K49/146 ,  B82Y5/00 ,  C07K7/06 ,  C07K7/64

摘要： This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.

摘要翻译： 本发明提供用于增强药物和其它药物穿过上皮组织包括皮肤，胃肠道，肺上皮，眼组织等的递送的组合物和方法。 组合物和方法也可用于穿过内皮组织，包括血脑屏障。 与非共轭化合物相比，组合物和方法使用具有足够的胍基或脒基侧链部分的递送增强转运蛋白，以增强与试剂缀合的化合物跨越组织的一个或多个层的递送。 递送增强聚合物包括例如优选长度在约6和25个残基之间的聚精氨酸分子。

公开(公告)号：US06730293B1

公开(公告)日：2004-05-04

申请号：US09645689

申请日：2000-08-24

申请人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

发明人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

IPC分类号： A61K31765

CPC分类号： C07K7/06 ,  A61K47/54 ,  A61K47/55 ,  A61K47/557 ,  A61K47/645 ,  C07K7/64

摘要： This invention provides compositions and methods for enhancing delivery of glucocorticoids and ascomycins such as hydrocortisone, cyclosporin and FK506 across into and across one or more layers of the skin for the treatment of psoriasis and other inflammatory diseases of the skin.

摘要翻译： 本发明提供用于增强糖皮质激素和阿霉素例如氢化可的松，环孢菌素和FK506的组合物和方法，其跨越皮肤的一层或多层并跨越皮肤的一层或多层，用于治疗皮肤的牛皮癣和其它炎性疾病。

公开(公告)号：US06669951B2

公开(公告)日：2003-12-30

申请号：US09792480

申请日：2001-02-23

申请人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

发明人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

IPC分类号： A61K902

CPC分类号： A61K47/48346 ,  A61K31/155 ,  A61K31/337 ,  A61K31/436 ,  A61K31/496 ,  A61K31/573 ,  A61K38/00 ,  A61K38/13 ,  A61K47/54 ,  A61K47/55 ,  A61K47/555 ,  A61K47/557 ,  A61K47/62 ,  A61K47/64 ,  A61K47/645 ,  A61K47/665 ,  A61K49/0043 ,  A61K49/0056 ,  A61K49/085 ,  A61K49/146 ,  B82Y5/00 ,  C07K7/06 ,  C07K7/64

摘要： This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.

公开(公告)号：US08278264B2

公开(公告)日：2012-10-02

申请号：US11800358

申请日：2007-05-04

申请人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

发明人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

IPC分类号： A61K31/522 ,  A61K38/03 ,  A61K38/13 ,  A61K38/16

CPC分类号： A61K9/0048 ,  A61K31/155 ,  A61K38/00 ,  A61K47/54 ,  A61K47/55 ,  A61K47/555 ,  A61K47/557 ,  A61K47/62 ,  A61K47/64 ,  A61K47/645 ,  A61K47/665 ,  A61K49/0043 ,  A61K49/0056 ,  A61K49/085 ,  A61K49/146 ,  B82Y5/00 ,  C07K7/06 ,  C07K7/64

摘要： This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including into and across ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length (for example, SEQ ID NO:86).

摘要翻译： 本发明提供用于增强药物和其它药物穿过上皮组织递送的组合物和方法，包括进入和穿过眼组织等。 组合物和方法也可用于穿过内皮组织，包括血脑屏障。 与非共轭化合物相比，组合物和方法使用具有足够的胍基或脒基侧链部分的递送增强转运蛋白，以增强与试剂缀合的化合物跨越组织的一个或多个层的递送。 递送增强聚合物包括例如优选长度在约6至25个残基之间的聚精氨酸分子（例如SEQ ID NO：86）。

公开(公告)号：US20110206610A1

公开(公告)日：2011-08-25

申请号：US12816358

申请日：2010-06-15

申请人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V.S. Sista ,  Thorsten A. Kirschberg

发明人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V.S. Sista ,  Thorsten A. Kirschberg

IPC分类号： A61K49/00 ,  A61K38/08 ,  A61K38/13 ,  A61K39/395

CPC分类号： A61K47/48346 ,  A61K31/155 ,  A61K31/337 ,  A61K31/436 ,  A61K31/496 ,  A61K31/573 ,  A61K38/00 ,  A61K38/13 ,  A61K47/54 ,  A61K47/55 ,  A61K47/555 ,  A61K47/557 ,  A61K47/62 ,  A61K47/64 ,  A61K47/645 ,  A61K47/665 ,  A61K49/0043 ,  A61K49/0056 ,  A61K49/085 ,  A61K49/146 ,  B82Y5/00 ,  C07K7/06 ,  C07K7/64

摘要： This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.

摘要翻译： 本发明提供用于增强药物和其它药物穿过上皮组织包括皮肤，胃肠道，肺上皮，眼组织等的递送的组合物和方法。 组合物和方法也可用于穿过内皮组织，包括血脑屏障。 与非共轭化合物相比，组合物和方法使用具有足够的胍基或脒基侧链部分的递送增强转运蛋白，以增强与试剂缀合的化合物跨越组织的一个或多个层的递送。 递送增强聚合物包括例如优选长度在约6和25个残基之间的聚精氨酸分子。

公开(公告)号：US06759387B2

公开(公告)日：2004-07-06

申请号：US10209421

申请日：2002-07-30

申请人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

发明人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

IPC分类号： A61K31436

CPC分类号： C07K7/06 ,  A61K47/54 ,  A61K47/55 ,  A61K47/557 ,  A61K47/62 ,  A61K47/645 ,  A61K47/665 ,  A61K49/0043 ,  A61K49/0056 ,  A61K49/085 ,  A61K49/146 ,  B82Y5/00 ,  C07K7/64

摘要： This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length (SEQ ID NO:50).

摘要翻译： 本发明提供用于增强药物和其它药物穿过上皮组织（包括皮肤，胃肠道，肺上皮等）的递送的组合物和方法。 组合物和方法也可用于穿过内皮组织，包括血脑屏障。 与非共轭化合物相比，组合物和方法使用具有足够的胍基或脒基侧链部分的递送增强转运蛋白，以增强与试剂缀合的化合物跨越组织的一个或多个层的递送。 递送增强聚合物包括例如优选长度在约6至25个残基之间的聚精氨酸分子（SEQ ID NO：50）。

公开(公告)号：US20130096069A1

公开(公告)日：2013-04-18

申请号：US13608975

申请日：2012-09-10

申请人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V.S. Sista ,  Thorsten A. Kirschberg

发明人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V.S. Sista ,  Thorsten A. Kirschberg

IPC分类号： A61K9/00

CPC分类号： A61K9/0048 ,  A61K31/155 ,  A61K38/00 ,  A61K47/54 ,  A61K47/55 ,  A61K47/555 ,  A61K47/557 ,  A61K47/62 ,  A61K47/64 ,  A61K47/645 ,  A61K47/665 ,  A61K49/0043 ,  A61K49/0056 ,  A61K49/085 ,  A61K49/146 ,  B82Y5/00 ,  C07K7/06 ,  C07K7/64

摘要： This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including into and across ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.

摘要翻译： 本发明提供用于增强药物和其它药物穿过上皮组织递送的组合物和方法，包括进入和穿过眼组织等。 组合物和方法也可用于穿过内皮组织，包括血脑屏障。 与非共轭化合物相比，组合物和方法使用具有足够的胍基或脒基侧链部分的递送增强转运蛋白，以增强与试剂缀合的化合物跨越组织的一个或多个层的递送。 递送增强聚合物包括例如优选长度在约6和25个残基之间的聚精氨酸分子。

公开(公告)号：US07229961B2

公开(公告)日：2007-06-12

申请号：US10083960

申请日：2002-02-25

申请人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

发明人： Jonathan B. Rothbard ,  Paul A. Wender ,  P. Leo McGrane ,  Lalitha V. S. Sista ,  Thorsten A. Kirschberg

IPC分类号： A61K31/155 ,  A61K31/522 ,  A61K38/03 ,  A61K38/08 ,  A61K38/13 ,  A61K38/16

CPC分类号： A61K9/0048 ,  A61K31/155 ,  A61K38/00 ,  A61K47/54 ,  A61K47/55 ,  A61K47/555 ,  A61K47/557 ,  A61K47/62 ,  A61K47/64 ,  A61K47/645 ,  A61K47/665 ,  A61K49/0043 ,  A61K49/0056 ,  A61K49/085 ,  A61K49/146 ,  B82Y5/00 ,  C07K7/06 ,  C07K7/64

摘要： This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including into and across ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length (SEQ ID NO:86).

摘要翻译： 本发明提供用于增强药物和其它药物穿过上皮组织递送的组合物和方法，包括进入和穿过眼组织等。 组合物和方法也可用于穿过内皮组织，包括血脑屏障。 与非共轭化合物相比，组合物和方法使用具有足够的胍基或脒基侧链部分的递送增强转运蛋白，以增强与试剂缀合的化合物跨越组织的一个或多个层的递送。 递送增强聚合物包括例如优选长度在约6至25个残基之间的聚精氨酸分子（SEQ ID NO：86）。