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公开(公告)号：US07425541B2
公开(公告)日：2008-09-16
申请号：US09879442
申请日：2001-06-11
申请人： Vincent Dubois , Ann Marie Fernandez , Sanjeev Gangwar , Evan Lewis , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey Yarranton
发明人： Vincent Dubois , Ann Marie Fernandez , Sanjeev Gangwar , Evan Lewis , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey Yarranton
CPC分类号： A61K47/65
摘要： The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the enzyme Thimet oligopeptidase, or TOP. Also disclosed are methods of designing prodrugs by utilizing TOP-cleavable sequences within the conjugate and methods of treating patients with prodrugs of the invention.
摘要翻译： 本发明的前药是治疗剂的修饰形式，并且包含治疗剂，寡肽，稳定基团和任选的连接基团。 前药可通过Thimet寡肽酶或TOP切割。 还公开了通过利用缀合物内的TOP-可切割序列和用本发明的前药治疗患者的方法来设计前药的方法。
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公开(公告)号：US08034787B2
公开(公告)日：2011-10-11
申请号：US12228636
申请日：2008-08-14
申请人： Vincent Dubois , Ann Marie Fernandez , Sanjeev Gangwar , Evan Lewis , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey T. Yarranton
发明人： Vincent Dubois , Ann Marie Fernandez , Sanjeev Gangwar , Evan Lewis , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey T. Yarranton
CPC分类号： A61K47/65
摘要： The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the enzyme Thimet oligopeptidase, or TOP. Also disclosed are methods of designing prodrugs by utilizing TOP-cleavable sequences within the conjugate and methods of treating patients with prodrugs of the invention.
摘要翻译： 本发明的前药是治疗剂的修饰形式，并且包含治疗剂，寡肽，稳定基团和任选的连接基团。 前药可通过Thimet寡肽酶或TOP切割。 还公开了通过利用缀合物内的TOP-可切割序列和用本发明的前药治疗患者的方法来设计前药的方法。
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公开(公告)号：US20090110753A1
公开(公告)日：2009-04-30
申请号：US12228636
申请日：2008-08-14
申请人： Vincent Dubois , Anne Marie Fernandez , Sanjeev Gangwar , Evan Lewis , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey T. Yarranton
发明人： Vincent Dubois , Anne Marie Fernandez , Sanjeev Gangwar , Evan Lewis , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey T. Yarranton
IPC分类号： A61K33/24 , A61K47/42 , A61K31/437 , A61K31/357 , A61K31/4985 , A61K31/337 , A61K31/704 , A61K31/4353 , A61K31/282 , A61P35/00 , A61K47/48 , A61K38/13 , A61K31/47 , A61K31/407 , A61K31/506 , A61K31/662 , A61K31/513 , A61K31/522 , A61K31/675 , A61K31/7052
CPC分类号： A61K47/65
摘要： The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the enzyme Thimet oligopeptidase, or TOP. Also disclosed are methods of designing prodrugs by utilizing TOP-cleavable sequences within the conjugate and methods of treating patients with prodrugs of the invention.
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公开(公告)号：US07214663B2
公开(公告)日：2007-05-08
申请号：US10311519
申请日：2001-06-11
申请人： Christopher R. Bebbington , Vincent Dubois , Sanjeev Gangwar , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey T. Yarranton
发明人： Christopher R. Bebbington , Vincent Dubois , Sanjeev Gangwar , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey T. Yarranton
CPC分类号： B82Y5/00 , A61K38/00 , A61K47/65 , A61K47/67 , C07K5/0202 , C07K5/0808 , C07K5/081 , C07K5/0812
摘要： The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide of three amino acids, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by a trouase enzyme such as Thimet oligopeptidase. Also disclosed are methods of making and using the prodrug compounds.
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公开(公告)号：US07816317B2
公开(公告)日：2010-10-19
申请号：US11728771
申请日：2007-03-27
申请人： Christopher R. Bebbington , Vincent Dubois , Sanjeev Gangwar , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey T. Yarranton
发明人： Christopher R. Bebbington , Vincent Dubois , Sanjeev Gangwar , Thomas J. Lobl , Matthew H. Nieder , Lesley B. Pickford , Andre Trouet , Geoffrey T. Yarranton
CPC分类号： B82Y5/00 , A61K38/00 , A61K47/65 , A61K47/67 , C07K5/0202 , C07K5/0808 , C07K5/081 , C07K5/0812
摘要： The prodrug of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide of three amino acids, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by a trouase enzyme such as Thimet oligopeptidase. Also disclosed are methods of making and using the prodrug compounds.
摘要翻译： 本发明的前药是治疗剂的修饰形式，并且包含治疗剂，三个氨基酸的寡肽，稳定基团和任选的连接基团。 前药可以被诸如Thimet寡肽酶的木瓜酶切割。 还公开了制备和使用前药化合物的方法。
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公开(公告)号：US07329507B2
公开(公告)日：2008-02-12
申请号：US11540466
申请日：2006-09-29
申请人： Lesley B. Pickford , Sanjeev Gangwar , Thomas J. Lobl , Matthew H. Nieder , Geoffrey T. Yarranton
发明人： Lesley B. Pickford , Sanjeev Gangwar , Thomas J. Lobl , Matthew H. Nieder , Geoffrey T. Yarranton
CPC分类号： A61K38/06 , A61K38/07 , A61K47/64 , A61K47/65 , C07K5/0808 , C07K5/101 , C07K5/1024
摘要： The compounds of the invention are modified forms of therapeutic agents. A typical prodrug compound of the invention comprises a therapeutic agent, an oligopeptide having an isoleucine residue, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by an enzyme associated with the target cell. Methods of making and using the compounds are also disclosed.
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公开(公告)号：US07115573B2
公开(公告)日：2006-10-03
申请号：US10311411
申请日：2001-06-11
申请人： Lesley B. Pickford , Sanjeev Gangwar , Thomas J. Lobl , Matthew H. Nieder , Geoffrey T. Yarranton
发明人： Lesley B. Pickford , Sanjeev Gangwar , Thomas J. Lobl , Matthew H. Nieder , Geoffrey T. Yarranton
CPC分类号： A61K38/06 , A61K38/07 , A61K47/64 , A61K47/65 , C07K5/0808 , C07K5/101 , C07K5/1024
摘要： The compounds of the invention are modified forms of therapeutic agents. A typical prodrug compound of the invention comprises a therapeutic agent, an oligopeptide having an isoleucine residue, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by an enzyme associated with the target cell. Methods of making and using the compounds are also disclosed.
摘要翻译： 本发明的化合物是治疗剂的修饰形式。 本发明的典型前药化合物包含治疗剂，具有异亮氨酸残基的寡肽，稳定基团和任选的连接基团。 前药可通过与靶细胞相关的酶切割。 还公开了制备和使用化合物的方法。
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公开(公告)号：US07696313B2
公开(公告)日：2010-04-13
申请号：US12009031
申请日：2008-01-16
申请人： Lesley B. Pickford , Sanjeev Gangwar , Thomas J. Lobl , Matthew H. Nieder , Geoffrey T. Yarranton
发明人： Lesley B. Pickford , Sanjeev Gangwar , Thomas J. Lobl , Matthew H. Nieder , Geoffrey T. Yarranton
CPC分类号： A61K38/06 , A61K38/07 , A61K47/64 , A61K47/65 , C07K5/0808 , C07K5/101 , C07K5/1024
摘要： The compounds of the invention are modified forms of therapeutic agents. A typical prodrug compound of the invention comprises a therapeutic agent, an oligopeptide having an isoleucine residue, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by an enzyme associated with the target cell. Methods of making and using the compounds are also disclosed.
摘要翻译： 本发明的化合物是治疗剂的修饰形式。 本发明的典型前药化合物包含治疗剂，具有异亮氨酸残基的寡肽，稳定基团和任选的连接基团。 前药可通过与靶细胞相关的酶切割。 还公开了制备和使用化合物的方法。
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公开(公告)号：US20080255248A1
公开(公告)日：2008-10-16
申请号：US12009031
申请日：2008-01-16
申请人： Lesley B. Pickford , Sanjeev Gangwar , Thomas J. Lobl , Matthew H. Nieder , Geoffrey T. Yarranton
发明人： Lesley B. Pickford , Sanjeev Gangwar , Thomas J. Lobl , Matthew H. Nieder , Geoffrey T. Yarranton
CPC分类号： A61K38/06 , A61K38/07 , A61K47/64 , A61K47/65 , C07K5/0808 , C07K5/101 , C07K5/1024
摘要： The compounds of the invention are modified forms of therapeutic agents. A typical prodrug compound of the invention comprises a therapeutic agent, an oligopeptide having an isoleucine residue, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by an enzyme associated with the target cell. Methods of making and using the compounds are also disclosed.
摘要翻译： 本发明的化合物是治疗剂的修饰形式。 本发明的典型前药化合物包含治疗剂，具有异亮氨酸残基的寡肽，稳定基团和任选的连接基团。 前药可通过与靶细胞相关的酶切割。 还公开了制备和使用化合物的方法。
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公开(公告)号：US20090136980A1
公开(公告)日：2009-05-28
申请号：US11986096
申请日：2007-11-20
申请人： Christopher R. Bebbington , Matthew H. Nieder , Pina M. Cardarelli , Sanjeev Gangwar , Lesley B. Pickford , Chin Pan
发明人： Christopher R. Bebbington , Matthew H. Nieder , Pina M. Cardarelli , Sanjeev Gangwar , Lesley B. Pickford , Chin Pan
IPC分类号： C12Q1/37
CPC分类号： G01N33/57492 , A61K47/65 , C12Q1/37 , G01N2333/70596 , G01N2500/00
摘要： The compounds of the invention are modified forms of therapeutic agents. A typical prodrug compound of the invention comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the CD10 enzyme. Methods of treatment using the prodrug and methods of designing the prodrug are also disclosed.
摘要翻译： 本发明的化合物是治疗剂的修饰形式。 本发明的典型前药化合物包含治疗剂，寡肽，稳定基团和任选的连接基团。 前药可被CD10酶切割。 还公开了使用前药的治疗方法和设计前药的方法。
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