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公开(公告)号：US08680293B2
公开(公告)日：2014-03-25
申请号：US12671609
申请日：2007-08-01
申请人： Patrick Henry Beusker , Henri Johannes Spijker , Johannes Albertus Frederikus Joosten , Tijl Huijbregts , Franciscus Marinus Hendrikus de Groot
发明人： Patrick Henry Beusker , Henri Johannes Spijker , Johannes Albertus Frederikus Joosten , Tijl Huijbregts , Franciscus Marinus Hendrikus de Groot
IPC分类号： C07D209/56 , A61K31/40 , A01N43/38 , C07D217/00
CPC分类号： C07D403/06 , C07D403/14
摘要： This invention relates to novel agents that are analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
摘要翻译： 本发明涉及作为DNA-烷化剂CC-1065的类似物及其缀合物的新型试剂。 此外，本发明涉及制备所述试剂及其共轭物的中间体。 缀合物被设计为在一个或多个活化步骤之后和/或在缀合物控制的速率和时间范围内释放它们的（多个）有效载荷，以选择性递送和/或可控地释放一种或多种所述DNA烷基化剂。 药剂，缀合物和中间体可用于治疗以不期望（细胞）增殖为特征的疾病。 作为实例，本发明的药剂和缀合物可用于治疗肿瘤。
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公开(公告)号：US20110065767A1
公开(公告)日：2011-03-17
申请号：US12671609
申请日：2007-08-01
申请人： Patrick Henry Beusker , Henri Johannes Spijker , Johannes Albertus Frederikus Joosten , Tijl Huijbregts , Franciscus Marinus Hendrikus De Groot
发明人： Patrick Henry Beusker , Henri Johannes Spijker , Johannes Albertus Frederikus Joosten , Tijl Huijbregts , Franciscus Marinus Hendrikus De Groot
IPC分类号： A61K31/404 , C07D403/06 , C07K16/28 , C07D403/14 , A61P35/00
CPC分类号： C07D403/06 , C07D403/14
摘要： This invention relates to novel agents that are analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
摘要翻译： 本发明涉及作为DNA-烷化剂CC-1065的类似物及其缀合物的新型试剂。 此外，本发明涉及制备所述试剂及其共轭物的中间体。 缀合物被设计为在一个或多个活化步骤之后和/或在缀合物控制的速率和时间范围内释放它们的（多个）有效载荷，以选择性递送和/或可控地释放一种或多种所述DNA烷基化剂。 药剂，缀合物和中间体可用于治疗以不期望（细胞）增殖为特征的疾病。 作为实例，本发明的药剂和缀合物可用于治疗肿瘤。
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公开(公告)号：US20110207767A1
公开(公告)日：2011-08-25
申请号：US13126920
申请日：2009-11-03
申请人： Patrick Henry Beusker , Rudy Gerardus Elisabeth Coumans , Ronald Christiaan Elgrtsma , Wiro Michaël Petrus Bernardus Menge , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker , Franciscus Marinus Hendrikus De Groot
发明人： Patrick Henry Beusker , Rudy Gerardus Elisabeth Coumans , Ronald Christiaan Elgrtsma , Wiro Michaël Petrus Bernardus Menge , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker , Franciscus Marinus Hendrikus De Groot
IPC分类号： A61K31/4365 , C07D403/06 , A61K31/404 , C07D471/04 , C07D417/06 , A61K31/427 , A61K31/428 , C07D413/06 , A61K31/423 , A61K31/4192 , A61K31/4184 , C07K16/00 , A61P35/00
CPC分类号： C07D209/60 , A61K31/404 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K47/6803 , C07D403/06 , C07D403/14 , C07D413/06 , C07D417/06 , C07D471/04 , C07D491/048 , C07D495/04
摘要： This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
摘要翻译： 本发明涉及DNA-烷化剂CC-1065及其缀合物的新型类似物。 此外，本发明涉及制备所述试剂和共轭物的中间体。 缀合物被设计为在一个或多个活化步骤之后和/或在缀合物控制的速率和时间范围内释放它们的（多个）有效载荷，以选择性递送和/或可控地释放一种或多种所述DNA烷基化剂。 药剂，缀合物和中间体可用于治疗以不期望（细胞）增殖为特征的疾病。 作为实例，本发明的药剂和缀合物可用于治疗肿瘤。
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公开(公告)号：US20090318668A1
公开(公告)日：2009-12-24
申请号：US12223682
申请日：2007-02-02
申请人： Patrick Henry Beusker , Franciscus Marinus Hendrikus De Groot , Lutz F. Tietze , Felix Major , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker
发明人： Patrick Henry Beusker , Franciscus Marinus Hendrikus De Groot , Lutz F. Tietze , Felix Major , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker
IPC分类号： C07D403/06 , C07D413/14 , C07D401/14 , C07H17/02 , C07K4/00
CPC分类号： C07D209/60 , A61K31/404 , A61K31/454 , A61K31/5377 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07H17/02
摘要： This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
摘要翻译： 本发明涉及DNA结合烷化剂CC-1065及其缀合物的新型类似物。 此外，本发明涉及制备所述试剂及其共轭物的中间体。 缀合物被设计为在一个或多个活化步骤之后和/或在缀合物控制的速率和时间范围内释放它们的（多个）有效载荷，以选择性递送和/或可控地释放一种或多种所述DNA烷基化剂。 药剂，缀合物和中间体可用于治疗以不期望（细胞）增殖为特征的疾病。 作为实例，本发明的药剂和缀合物可用于治疗肿瘤。
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公开(公告)号：US09629924B2
公开(公告)日：2017-04-25
申请号：US13642847
申请日：2011-04-21
申请人： Patrick Henry Beusker , Rudy Gerardus Elisabeth Coumans , Ronald Christiaan Elgersma , Wiro Michael Petrus Bernardus Menge , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker , Franciscus Marinus Hendrikus De Groot
发明人： Patrick Henry Beusker , Rudy Gerardus Elisabeth Coumans , Ronald Christiaan Elgersma , Wiro Michael Petrus Bernardus Menge , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker , Franciscus Marinus Hendrikus De Groot
IPC分类号： A61K47/48 , C07D495/04 , A61K31/437 , C07D471/04 , A61K38/38 , A61K39/44
CPC分类号： A61K47/64 , A61K31/437 , A61K38/385 , A61K39/44 , A61K47/545 , A61K47/60 , A61K47/643 , A61K47/646 , A61K47/65 , A61K47/6803 , A61K47/6851 , C07D471/04
摘要： This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
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公开(公告)号：US08940784B2
公开(公告)日：2015-01-27
申请号：US12223682
申请日：2007-02-02
申请人： Patrick Henry Beusker , Franciscus Marinus Hendrikus de Groot , Lutz F. Tietze , Felix Major , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker
发明人： Patrick Henry Beusker , Franciscus Marinus Hendrikus de Groot , Lutz F. Tietze , Felix Major , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker
IPC分类号： A61K31/5377 , A61K31/545 , A61K31/404 , C07D413/14 , C07D401/14 , C07D403/06 , C07D209/60 , A61K31/454 , C07D403/14 , C07H17/02
CPC分类号： C07D209/60 , A61K31/404 , A61K31/454 , A61K31/5377 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07H17/02
摘要： This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
摘要翻译： 本发明涉及DNA结合烷化剂CC-1065及其缀合物的新型类似物。 此外，本发明涉及制备所述试剂及其共轭物的中间体。 缀合物被设计为在一个或多个活化步骤之后和/或在缀合物控制的速率和时间范围内释放它们的（多个）有效载荷，以选择性递送和/或可控地释放一种或多种所述DNA烷基化剂。 药剂，缀合物和中间体可用于治疗以不期望（细胞）增殖为特征的疾病。 作为实例，本发明的药剂和缀合物可用于治疗肿瘤。
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公开(公告)号：US08889868B2
公开(公告)日：2014-11-18
申请号：US13126920
申请日：2009-11-03
申请人： Patrick Henry Beusker , Rudy Gerardus Elisabeth Coumans , Ronald Christiaan Elgersma , Wiro Michaël Petrus Bernardus Menge , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker , Franciscus Marinus Hendrikus de Groot
发明人： Patrick Henry Beusker , Rudy Gerardus Elisabeth Coumans , Ronald Christiaan Elgersma , Wiro Michaël Petrus Bernardus Menge , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker , Franciscus Marinus Hendrikus de Groot
IPC分类号： A61K31/4355 , C07D491/048 , A61K31/437 , C07D471/04 , C07D403/14 , C07D403/06 , C07D413/06 , C07D417/06 , C07D495/04
CPC分类号： C07D209/60 , A61K31/404 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K47/6803 , C07D403/06 , C07D403/14 , C07D413/06 , C07D417/06 , C07D471/04 , C07D491/048 , C07D495/04
摘要： This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
摘要翻译： 本发明涉及DNA-烷化剂CC-1065及其缀合物的新型类似物。 此外，本发明涉及制备所述试剂和共轭物的中间体。 缀合物被设计为在一个或多个活化步骤之后和/或在缀合物控制的速率和时间范围内释放它们的（多个）有效载荷，以选择性递送和/或可控地释放一种或多种所述DNA烷基化剂。 药剂，缀合物和中间体可用于治疗以不期望（细胞）增殖为特征的疾病。 作为实例，本发明的药剂和缀合物可用于治疗肿瘤。
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公开(公告)号：US20130224227A1
公开(公告)日：2013-08-29
申请号：US13642847
申请日：2011-04-21
申请人： Patrick Henry Beusker , Rudy Gerardus Elisabeth Coumans , Ronald Christiaan Elgersma , Wiro Michael Petrus Bernardus Menge , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker , Franciscus Marinus Hendrikus de Groot
发明人： Patrick Henry Beusker , Rudy Gerardus Elisabeth Coumans , Ronald Christiaan Elgersma , Wiro Michael Petrus Bernardus Menge , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker , Franciscus Marinus Hendrikus de Groot
IPC分类号： A61K47/48 , A61K38/38 , A61K39/44 , A61K31/437
CPC分类号： A61K47/64 , A61K31/437 , A61K38/385 , A61K39/44 , A61K47/545 , A61K47/60 , A61K47/643 , A61K47/646 , A61K47/65 , A61K47/6803 , A61K47/6851 , C07D471/04
摘要： This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
摘要翻译： 本发明涉及DNA-烷化剂CC-1065及其缀合物的新型类似物。 此外，本发明涉及制备所述试剂和共轭物的中间体。 缀合物被设计为在一个或多个活化步骤之后和/或在缀合物控制的速率和时间范围内释放它们的（多个）有效载荷，以选择性递送和/或可控地释放一种或多种所述DNA烷基化剂。 药剂，缀合物和中间体可用于治疗以不期望（细胞）增殖为特征的疾病。 作为实例，本发明的药剂和缀合物可用于治疗肿瘤。
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