公开(公告)号：US09744246B2

公开(公告)日：2017-08-29

申请号：US14124651

申请日：2012-06-06

申请人： David Owen ,  Brian Devlin Kelly ,  Peter Karellas

发明人： David Owen ,  Brian Devlin Kelly ,  Peter Karellas

IPC分类号： A61K47/48 ,  C08G69/10 ,  C08G69/40 ,  C08G83/00

CPC分类号： A61K47/59 ,  A61K47/60 ,  A61K47/65 ,  A61K47/68 ,  C08G69/10 ,  C08G69/40 ,  C08G83/003

摘要： The present invention relates to a macromolecule comprising a dendrimer having surface amino groups to which at least two different terminal groups are attached including a pharmaceutically active agent and a pharmacokinetic modifying agent, the pharmaceutically active agent comprising a hydroxyl group and being attached to the surface amino group of the dendrimer through a diacid linker. Pharmaceutical compositions comprising the macromolecules and methods of treatment using the macromolecules are also described.

公开(公告)号：US20140171375A1

公开(公告)日：2014-06-19

申请号：US14124651

申请日：2012-06-06

申请人： David Owen ,  Brian Devlin Kelly ,  Peter Karellas

发明人： David Owen ,  Brian Devlin Kelly ,  Peter Karellas

IPC分类号： A61K47/48

CPC分类号： A61K47/59 ,  A61K47/60 ,  A61K47/65 ,  A61K47/68 ,  C08G69/10 ,  C08G69/40 ,  C08G83/003

摘要： The present invention relates to a macromolecule comprising a dendrimer having surface amino groups to which at least two different terminal groups are attached including a pharmaceutically active agent and a pharmacokinetic modifying agent, the pharmaceutically active agent comprising a hydroxyl group and being attached to the surface amino group of the dendrimer through a diacid linker. Pharmaceutical compositions comprising the macromolecules and methods of treatment using the macromolecules are also described.

摘要翻译： 本发明涉及包含具有表面氨基的树枝状聚合物的大分子，至少两个不同的末端基团连接到其上，包括药物活性剂和药代动力学改性剂，所述药物活性剂包含羟基并连接到表面氨基 通过二酸连接子的树枝状聚合物组。 还描述了包含大分子的药物组合物和使用大分子的治疗方法。

公开(公告)号：US20090324535A1

公开(公告)日：2009-12-31

申请号：US12161688

申请日：2006-05-15

申请人： Benjamin James Boyd ,  Lisa Michelle Kaminskas ,  Christopher John Hamilton Porter ,  Peter Karellas ,  Guy Yeoman Krippner ,  Pasquale Razzino ,  Brian Devlin Kelly ,  Zemin Wu ,  Sue Pallich

发明人： Benjamin James Boyd ,  Lisa Michelle Kaminskas ,  Christopher John Hamilton Porter ,  Peter Karellas ,  Guy Yeoman Krippner ,  Pasquale Razzino ,  Brian Devlin Kelly ,  Zemin Wu ,  Sue Pallich

IPC分类号： A61K47/48 ,  C08F283/06 ,  A61K38/10 ,  A61K38/16

CPC分类号： C08G65/33396 ,  A61K31/74 ,  A61K31/785 ,  A61K47/59 ,  A61K47/595 ,  A61K47/60 ,  A61K47/645 ,  C08G69/10 ,  C08G83/003

摘要： The present invention relates to a macromolecule having a controlled terminal group stoichiometry, the macromolecule including a surface layer, at least one subsurface layer and at least two terminal groups including: a first terminal group which is a residue of a pharmaceutically active agent, a derivative thereof or precursor therefor; and a second terminal group selected to modify the pharmacokinetics of the pharmaceutically active agent and/or macromolecule, wherein terminal group stoichiometry refers to the number and type of terminal groups.

摘要翻译： 本发明涉及具有受控终端基团化学计量的大分子，所述高分子包括表面层，至少一个地下层和至少两个末端基团，所述末端基团包括：第一末端基团，其为药物活性剂的残基，衍生物 或其前体; 和选择用于改变药物活性剂和/或大分子的药代动力学的第二末端基团，其中末端基团化学计量指的是末端基团的数量和类型。

公开(公告)号：US08337823B2

公开(公告)日：2012-12-25

申请号：US12161688

申请日：2006-05-15

申请人： Benjamin James Boyd ,  Lisa Michelle Kaminskas ,  Christopher John Hamilton Porter ,  Peter Karellas ,  Guy Yeoman Krippner ,  Brian Devlin Kelly ,  Zemin Wu ,  Pasquale Razzino ,  Sue Pallich

发明人： Benjamin James Boyd ,  Lisa Michelle Kaminskas ,  Christopher John Hamilton Porter ,  Peter Karellas ,  Guy Yeoman Krippner ,  Brian Devlin Kelly ,  Zemin Wu ,  Pasquale Razzino ,  Sue Pallich

IPC分类号： A61K31/74 ,  A61K9/14

CPC分类号： C08G65/33396 ,  A61K31/74 ,  A61K31/785 ,  A61K47/59 ,  A61K47/595 ,  A61K47/60 ,  A61K47/645 ,  C08G69/10 ,  C08G83/003

摘要： The present invention relates to a macromolecule having a controlled terminal group stoichiometry, the macromolecule including a surface layer, at least one subsurface layer and at least two terminal groups including: a first terminal group which is a residue of a pharmaceutically active agent, a derivative thereof or precursor therefor; and a second terminal group selected to modify the pharmacokinetics of the pharmaceutically active agent and/or macromolecule, wherein terminal group stoichiometry refers to the number and type of terminal groups.

摘要翻译： 本发明涉及具有受控终端基团化学计量的大分子，所述高分子包括表面层，至少一个地下层和至少两个末端基团，所述末端基团包括：第一末端基团，其为药物活性剂的残基，衍生物 或其前体; 和选择用于修饰药物活性剂和/或大分子的药代动力学的第二末端基团，其中末端基团化学计量指的是末端基团的数量和类型。

公开(公告)号：US20120302730A1

公开(公告)日：2012-11-29

申请号：US13570058

申请日：2012-08-08

申请人： Guy Yeoman Krippner ,  Gottfried Lichti ,  Pasquale Razzino ,  Brian Devlin Kelly ,  Susanne Pallich ,  Scott Andrew Henderson ,  Angela Michelle Scheppokat ,  Charlotte Claire Williams ,  Christopher John Hamilton Porter ,  Benjamin James Boyd ,  Lisa Michelle Kaminskas ,  Phillip Martin Rendle ,  Ben William Greatrex

发明人： Guy Yeoman Krippner ,  Gottfried Lichti ,  Pasquale Razzino ,  Brian Devlin Kelly ,  Susanne Pallich ,  Scott Andrew Henderson ,  Angela Michelle Scheppokat ,  Charlotte Claire Williams ,  Christopher John Hamilton Porter ,  Benjamin James Boyd ,  Lisa Michelle Kaminskas ,  Phillip Martin Rendle ,  Ben William Greatrex

IPC分类号： C07K1/00 ,  C07K1/06

CPC分类号： C08G83/003 ,  A61K31/785

摘要： The following invention is directed to macromolecules having controlled stoichiometry and topology, processes for their production, and applications for their use. The macromolecules have a controlled functional moiety stoichiometry and include at least one dendritic motif having a surface layer formed from at least one surface building unit and at least one subsurface layer formed from at least one building unit, the surface building unit and building units having a hydrocarbon backbone bearing a carbonyl group and at least one amine group; and at least two different functional moieties on the building unit and/or surface building unit; where functional moiety stoichiometry refers to the number and type of functional moieties.

摘要翻译： 以下发明涉及具有受控化学计量和拓扑结构的大分子，其生产方法及其应用。 大分子具有受控的功能部分化学计量学，并且包括至少一个树突状基序，其具有由至少一个表面构建单元形成的表面层和由至少一个建筑单元形成的至少一个地下层，所述表面建筑单元和建筑单元具有 具有羰基和至少一个胺基的烃主链; 和建筑物单元和/或表面建筑单元上的至少两个不同的功能部分; 功能部分化学计量指功能部分的数量和类型。

公开(公告)号：US08420067B2

公开(公告)日：2013-04-16

申请号：US12377253

申请日：2007-08-10

申请人： Guy Yeoman Krippner ,  Charlotte Claire Williams ,  Brian Devlin Kelly ,  Scott Andrew Henderson ,  Zemin Wu ,  Pasquale Razzino

发明人： Guy Yeoman Krippner ,  Charlotte Claire Williams ,  Brian Devlin Kelly ,  Scott Andrew Henderson ,  Zemin Wu ,  Pasquale Razzino

IPC分类号： A61K38/00 ,  A61K31/74 ,  A61K31/785

CPC分类号： C08G69/10 ,  A61K38/00 ,  A61K47/6885 ,  C07K5/06026 ,  C07K14/001 ,  C08G69/48 ,  C08G83/003

摘要： The present invention relates generally to branched macromolecules bearing functional moieties. In particular, the invention relates to dendrimers, derived from lysine or lysine analogues, bearing a plurality of functional moieties. The invention further relates to the use of such macromolecules, particularly in therapeutic applications, and compositions comprising them.

摘要翻译： 本发明一般涉及带有官能部分的支链大分子。 特别地，本发明涉及衍生自具有多个功能部分的赖氨酸或赖氨酸类似物的树枝状大分子。 本发明还涉及这种大分子的用途，特别是在治疗应用中的用途，以及包含它们的组合物。

公开(公告)号：US20090118467A1

公开(公告)日：2009-05-07

申请号：US12091233

申请日：2006-10-25

申请人： Guy Yeoman Krippner ,  Gottfried Lichti ,  Pasquale Razzino ,  Brian Devlin Kelly ,  Susanne Pallich ,  Scott Andrew Henderson ,  Angela Michelle Scheppokat ,  Charlotte Claire Williams ,  Christopher John Hamilton Porter ,  Benjamin James Boyd ,  Lisa Michelle Kaminskas ,  Phillip Martin Rendle ,  Ben William Greatrex

发明人： Guy Yeoman Krippner ,  Gottfried Lichti ,  Pasquale Razzino ,  Brian Devlin Kelly ,  Susanne Pallich ,  Scott Andrew Henderson ,  Angela Michelle Scheppokat ,  Charlotte Claire Williams ,  Christopher John Hamilton Porter ,  Benjamin James Boyd ,  Lisa Michelle Kaminskas ,  Phillip Martin Rendle ,  Ben William Greatrex

IPC分类号： C07K5/00

CPC分类号： C08G83/003 ,  A61K31/785

摘要： The following invention is directed to macromolecules having controlled stoichiometry and topology, processes for their production, and applications for their use. The macromolecules have a controlled functional moiety stoichiometry and include at least one dendritic motif having a surface layer formed from at least one surface building unit and at least one subsurface layer formed from at least one building unit, the surface building unit and building units having a hydrocarbon backbone bearing a carbonyl group and at least one amine group; and at least two different functional moieties on the building unit and/or surface building unit; where functional moiety stoichiometry refers to the number and type of functional moieties.

摘要翻译： 以下发明涉及具有受控化学计量和拓扑结构的大分子，其生产方法及其应用。 大分子具有受控的功能部分化学计量学，并且包括至少一个树突状基序，其具有由至少一个表面构建单元形成的表面层和由至少一个建筑单元形成的至少一个地下层，所述表面建筑单元和建筑单元具有 具有羰基和至少一个胺基的烃主链; 和建筑物单元和/或表面建筑单元上的至少两个不同的功能部分; 功能部分化学计量指功能部分的数量和类型。

公开(公告)号：US08586705B2

公开(公告)日：2013-11-19

申请号：US13570058

申请日：2012-08-08

申请人： Guy Yeoman Krippner ,  Gottfried Lichti ,  Pasquale Razzino ,  Brian Devlin Kelly ,  Susanne Pallich ,  Scott Andrew Henderson ,  Angela Michelle Scheppokat ,  Charlotte Claire Williams ,  Christopher John Hamilton Porter ,  Benjamin James Boyd ,  Lisa Michelle Kaminskas ,  Phillip Martin Rendle ,  Ben William Greatrex

发明人： Guy Yeoman Krippner ,  Gottfried Lichti ,  Pasquale Razzino ,  Brian Devlin Kelly ,  Susanne Pallich ,  Scott Andrew Henderson ,  Angela Michelle Scheppokat ,  Charlotte Claire Williams ,  Christopher John Hamilton Porter ,  Benjamin James Boyd ,  Lisa Michelle Kaminskas ,  Phillip Martin Rendle ,  Ben William Greatrex

IPC分类号： A61K38/00 ,  A61K9/00 ,  A61K31/74

CPC分类号： C08G83/003 ,  A61K31/785

摘要： The following invention is directed to macromolecules having controlled stoichiometry and topology, processes for their production, and applications for their use. The macromolecules have a controlled functional moiety stoichiometry and include at least one dendritic motif having a surface layer formed from at least one surface building unit and at least one subsurface layer formed from at least one building unit, the surface building unit and building units having a hydrocarbon backbone bearing a carbonyl group and at least one amine group; and at least two different functional moieties on the building unit and/or surface building unit; where functional moiety stoichiometry refers to the number and type of functional moieties.

摘要翻译： 以下发明涉及具有受控化学计量和拓扑结构的大分子，其生产方法及其应用。 大分子具有受控的功能部分化学计量学，并且包括至少一个树突状基序，其具有由至少一个表面构建单元形成的表面层和由至少一个建筑单元形成的至少一个地下层，所述表面建筑单元和建筑单元具有 具有羰基和至少一个胺基的烃主链; 和建筑物单元和/或表面建筑单元上的至少两个不同的功能部分; 功能部分化学计量指功能部分的数量和类型。

公开(公告)号：US20100292148A1

公开(公告)日：2010-11-18

申请号：US12377253

申请日：2007-08-10

申请人： Guy Yeoman Krippner ,  Charlotte Claire Williams ,  Brian Devlin Kelly ,  Scott Andrew Henderson ,  Zemin Wu ,  Pasquale Razzino

发明人： Guy Yeoman Krippner ,  Charlotte Claire Williams ,  Brian Devlin Kelly ,  Scott Andrew Henderson ,  Zemin Wu ,  Pasquale Razzino

IPC分类号： A61K38/34 ,  C07K14/47 ,  A61K38/17 ,  A61P35/00 ,  A61P23/00 ,  A61P31/04 ,  A61P31/10 ,  A61P31/12 ,  A61P33/02 ,  A61P11/08 ,  A61P11/10 ,  A61P37/06 ,  A61P19/02 ,  A61P25/08 ,  A61P7/10 ,  A61P37/04 ,  A61P19/10 ,  C07K14/765 ,  A61K38/38 ,  C07K14/685 ,  A61K38/10 ,  C07K7/08 ,  C07D475/08 ,  A61K38/05 ,  C07K5/11 ,  A61K38/07

CPC分类号： C08G69/10 ,  A61K38/00 ,  A61K47/6885 ,  C07K5/06026 ,  C07K14/001 ,  C08G69/48 ,  C08G83/003

摘要： The present invention relates generally to branched macromolecules bearing functional moieties. In particular, the invention relates to dendrimers, derived from lysine or lysine analogues, bearing a plurality of functional moieties. The invention further relates to the use of such macromolecules, particularly in therapeutic applications, and compositions comprising them.

摘要翻译： 本发明一般涉及带有官能部分的支链大分子。 特别地，本发明涉及衍生自具有多个功能部分的赖氨酸或赖氨酸类似物的树枝状大分子。 本发明还涉及这种大分子的用途，特别是在治疗应用中的用途，以及包含它们的组合物。

公开(公告)号：US08258259B2

公开(公告)日：2012-09-04

申请号：US12091233

申请日：2006-10-25

申请人： Guy Yeoman Krippner ,  Gottfried Lichti ,  Pasquale Razzino ,  Brian Devlin Kelly ,  Susanne Pallich ,  Scott Andrew Henderson ,  Angela Michelle Scheppokat ,  Charlotte Claire Williams ,  Christopher John Hamilton Porter ,  Benjamin James Boyd ,  Lisa Michelle Kaminskas ,  Phillip Martin Rendle ,  Ben William Greatrex

发明人： Guy Yeoman Krippner ,  Gottfried Lichti ,  Pasquale Razzino ,  Brian Devlin Kelly ,  Susanne Pallich ,  Scott Andrew Henderson ,  Angela Michelle Scheppokat ,  Charlotte Claire Williams ,  Christopher John Hamilton Porter ,  Benjamin James Boyd ,  Lisa Michelle Kaminskas ,  Phillip Martin Rendle ,  Ben William Greatrex

IPC分类号： C07K7/00 ,  A61K31/74 ,  A61K9/00

CPC分类号： C08G83/003 ,  A61K31/785

摘要： The following invention is directed to macromolecules having controlled stoichiometry and topology, processes for their production, and applications for their use. The macromolecules have a controlled functional moiety stoichiometry and include at least one dendritic motif having a surface layer formed from at least one surface building unit and at least one subsurface layer formed from at least one building unit, the surface building unit and building units having a hydrocarbon backbone bearing a carbonyl group and at least one amine group; and at least two different functional moieties on the building unit and/or surface building unit; where functional moiety stoichiometry refers to the number and type of functional moieties.

摘要翻译： 以下发明涉及具有受控化学计量和拓扑结构的大分子，其生产方法及其应用。 大分子具有受控的功能部分化学计量学，并且包括至少一个树突状基序，其具有由至少一个表面构建单元形成的表面层和由至少一个建筑单元形成的至少一个地下层，所述表面建筑单元和建筑单元具有 具有羰基和至少一个胺基的烃主链; 和建筑物单元和/或表面建筑单元上的至少两个不同的功能部分; 功能部分化学计量指功能部分的数量和类型。