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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
Applicant: 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
Inventor： 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: A61K47/48 , C07D495/04 , A61K31/437 , C07D471/04 , A61K38/38 , A61K39/44
CPC classification number: A61K47/64 , A61K31/437 , A61K38/385 , A61K39/44 , A61K47/545 , A61K47/60 , A61K47/643 , A61K47/646 , A61K47/65 , A61K47/6803 , A61K47/6851 , C07D471/04
Abstract: 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
Applicant: Patrick Henry Beusker , Franciscus Marinus Hendrikus de Groot , Lutz F. Tietze , Felix Major , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker
Inventor： Patrick Henry Beusker , Franciscus Marinus Hendrikus de Groot , Lutz F. Tietze , Felix Major , Johannes Albertus Frederikus Joosten , Henri Johannes Spijker
IPC: A61K31/5377 , A61K31/545 , A61K31/404 , C07D413/14 , C07D401/14 , C07D403/06 , C07D209/60 , A61K31/454 , C07D403/14 , C07H17/02
CPC classification number: C07D209/60 , A61K31/404 , A61K31/454 , A61K31/5377 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07H17/02
Abstract: 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.
Abstract translation: 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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3.发明申请Triazole-Containing Releasable Linkers, Conjugates Thereof, and Methods of Preparation 有权含三唑的可释放接头，共轭体及其制备方法公开(公告)号：US20080311136A1
公开(公告)日：2008-12-18
申请号：US11997981
申请日：2006-08-03
IPC: A61K47/48 , C07D249/04 , C07K1/00 , C07K16/00
CPC classification number: C07D249/04 , A61K47/56 , A61K47/65 , A61K47/6803 , C07K5/06078 , C07K5/0806
Abstract: This invention relates to compounds comprising one or more therapeutic and/or diagnostic moieties and one or more functional moieties linked together via one or more triazole-containing linkers and to their intermediates and methods of their preparation. The triazole-containing linker may optionally contain one or more conditionally-cleavable or conditionally-transformable moieties and one or more spacer systems in between said moiety/moieties and the one or more therapeutic and/or diagnostic moieties.
Abstract translation: 本发明涉及包含一个或多个治疗和/或诊断部分和通过一个或多个含三唑接头连接在一起的一个或多个功能部分及其中间体及其制备方法的化合物。 含有三唑的接头可以任选地在所述部分/部分之间和一个或多个治疗和/或诊断部分之间含有一个或多个条件可切割或有条件可转化部分和一个或多个间隔体系。
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公开(公告)号：US20150216844A1
公开(公告)日：2015-08-06
申请号：US14174794
申请日：2014-02-06
Applicant: Patrick Henry BEUSKER , Henri Johannes SPIJKER , Johannes Albertus Frederikus JOOSTEN , Tijl HUIJBREGTS , Franciscus Marinus Hendrikus DE GROOT
Inventor： Patrick Henry BEUSKER , Henri Johannes SPIJKER , Johannes Albertus Frederikus JOOSTEN , Tijl HUIJBREGTS , Franciscus Marinus Hendrikus DE GROOT
IPC: A61K31/404 , A61K47/48
CPC classification number: A61K31/404 , A61K47/6803 , A61K47/6851
Abstract: 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.
Abstract translation: 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：US08889868B2
公开(公告)日：2014-11-18
申请号：US13126920
申请日：2009-11-03
Applicant: 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
Inventor： 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: A61K31/4355 , C07D491/048 , A61K31/437 , C07D471/04 , C07D403/14 , C07D403/06 , C07D413/06 , C07D417/06 , C07D495/04
CPC classification number: 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
Abstract: 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.
Abstract translation: 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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Patent Agency Ranking
公开(公告)号：US20130224227A1
公开(公告)日：2013-08-29
申请号：US13642847
申请日：2011-04-21
Applicant: 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
Inventor： 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: A61K47/48 , A61K38/38 , A61K39/44 , A61K31/437
CPC classification number: A61K47/64 , A61K31/437 , A61K38/385 , A61K39/44 , A61K47/545 , A61K47/60 , A61K47/643 , A61K47/646 , A61K47/65 , A61K47/6803 , A61K47/6851 , C07D471/04
Abstract: 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.
Abstract translation: 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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7.发明授权Triazole-containing releasable linkers, conjugates thereof, and methods of preparation 有权含有三唑的可释放接头，其缀合物及其制备方法公开(公告)号：US08158590B2
公开(公告)日：2012-04-17
申请号：US11997981
申请日：2006-08-03
CPC classification number: C07D249/04 , A61K47/56 , A61K47/65 , A61K47/6803 , C07K5/06078 , C07K5/0806
Abstract: This invention relates to compounds comprising one or more therapeutic and/or diagnostic moieties and one or more functional moieties linked together via one or more triazole-containing linkers and to their intermediates and methods of their preparation. The triazole-containing linker may optionally contain one or more conditionally-cleavable or conditionally-transformable moieties and one or more spacer systems in between said moiety/moieties and the one or more therapeutic and/or diagnostic moieties.
Abstract translation: 本发明涉及包含一个或多个治疗和/或诊断部分和通过一个或多个含三唑接头连接在一起的一个或多个功能部分及其中间体及其制备方法的化合物。 含有三唑的接头可以任选地在所述部分/部分之间和一个或多个治疗和/或诊断部分之间含有一个或多个条件可切割或有条件可转化部分和一个或多个间隔体系。
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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
Applicant: Patrick Henry Beusker , Henri Johannes Spijker , Johannes Albertus Frederikus Joosten , Tijl Huijbregts , Franciscus Marinus Hendrikus De Groot
Inventor： Patrick Henry Beusker , Henri Johannes Spijker , Johannes Albertus Frederikus Joosten , Tijl Huijbregts , Franciscus Marinus Hendrikus De Groot
IPC: A61K31/404 , C07D403/06 , C07K16/28 , C07D403/14 , A61P35/00
CPC classification number: C07D403/06 , C07D403/14
Abstract: 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.
Abstract translation: 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
Applicant: 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
Inventor： 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: 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 classification number: 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
Abstract: 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.
Abstract translation: 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：US08680293B2
公开(公告)日：2014-03-25
申请号：US12671609
申请日：2007-08-01
Applicant: Patrick Henry Beusker , Henri Johannes Spijker , Johannes Albertus Frederikus Joosten , Tijl Huijbregts , Franciscus Marinus Hendrikus de Groot
Inventor： Patrick Henry Beusker , Henri Johannes Spijker , Johannes Albertus Frederikus Joosten , Tijl Huijbregts , Franciscus Marinus Hendrikus de Groot
IPC: C07D209/56 , A61K31/40 , A01N43/38 , C07D217/00
CPC classification number: C07D403/06 , C07D403/14
Abstract: 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.
Abstract translation: 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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