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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：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：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：US07705045B2
公开(公告)日：2010-04-27
申请号：US10534777
申请日：2003-11-14
IPC分类号： A61K31/325 , C07C271/42
CPC分类号： C07C271/28 , A61K47/555 , A61K47/65 , A61K47/67 , A61K47/6899 , B82Y5/00 , C07K5/0806
摘要： This invention concerns multiple release spacers and spacer systems, which release multiple leaving groups following a single activation. It concerns compounds comprising a specifier linked to two or more of the same or different leaving groups (L in the figure) via a self-eliminating multiple release spacer or spacer system, which compounds upon a single activation step, in particular removal or transformation of the specifier, release at least two leaving groups.
摘要翻译： 本发明涉及多次释放间隔物和间隔体系，其在单次活化后释放多个离去基团。 它涉及包含通过自消除多重释放间隔物或间隔体系连接到两个或多个相同或不同离去基团（图中为L）的说明符的化合物，其在单个活化步骤，特别是除去或转化 说明符，释放至少两个离开组。
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6.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分类号： A61K47/48 , C07D249/04 , C07K1/00 , C07K16/00
CPC分类号： C07D249/04 , A61K47/56 , A61K47/65 , A61K47/6803 , C07K5/06078 , C07K5/0806
摘要： 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.
摘要翻译： 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：US07223837B2
公开(公告)日：2007-05-29
申请号：US10472921
申请日：2002-03-25
申请人： Franciscus Marinus Hendrikus De Groot , Patrick Henry Beusker , Johannes Wilhelm Scheeren , Dick De Vos , Leonardus Wilhelmus Adriaan Van Berkom , Guuske Frederike Busscher , Antoinette Eugenie Seelen , Ralph Koekkoek , Carsten Albrecht
发明人： Franciscus Marinus Hendrikus De Groot , Patrick Henry Beusker , Johannes Wilhelm Scheeren , Dick De Vos , Leonardus Wilhelmus Adriaan Van Berkom , Guuske Frederike Busscher , Antoinette Eugenie Seelen , Ralph Koekkoek , Carsten Albrecht
IPC分类号： C07K5/08
CPC分类号： B82Y5/00 , A61K47/65 , A61K47/67 , A61K47/6889 , A61K47/6899
摘要： This invention is directed to prodrugs that can be activated at the preferred site of action in order to selectively deliver the corresponding therapeutic parent drugs to target cells or to the target site. This invention will therefore primarily but not exclusively relate to tumor cells as target cells. More specifically the prodrugs are compounds of the formula V—(W)k—(X)l—A—Z, wherein: V is a specifier; (W)k—(X)l—A is an elongated self-elimination spacer system; W and X are each a 1,(4+2n) electronic cascade spacer, being the same or different; A is either a spacer group of formula (Y)m wherein: Y is a 1,(4+2n) electronic cascade spacer, or a group of formula U being a cyclization elimination spacer; Z is a therapeutic drug; k, l and m are integers from 0 (included) to 5 (included); n is an integer of 0 (included) to 10 (included), with the provisos that: —when A is (Y)m: k+l+m≧1, and if k+l+m=1; —when A is U: k+l≧1.
摘要翻译： 本发明涉及可以在优选的作用位点被活化的前药，以便选择性地将相应的治疗性母体药物递送至靶细胞或靶位点。 因此，本发明主要但不完全涉及作为靶细胞的肿瘤细胞。 更具体地，前药是式V-（W） - （X）1-Z-Z的化合物，其中：V是说明符; （W） - （X）1 - A是细长的自消除间隔体系; W和X分别为1（4 + 2n）个电子级联间隔物，相同或不同; A是式（Y）的间隔基团其中：Y是1，（4 + 2n）电子级联间隔基，或者是一组式U是环化消除间隔基; Z是治疗药物; k，l和m是从0（包括）到5（包括）的整数; n是0（包括）到10（包括）的整数，条件是：当A是（Y）m：k + 1 + m> = 1时，如果k + 1 + m = 1; - 当A是U：k + l> = 1。
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8.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分类号： C07D249/04 , A61K47/56 , A61K47/65 , A61K47/6803 , C07K5/06078 , C07K5/0806
摘要： 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.
摘要翻译： 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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