公开(公告)号：US20170274090A1

公开(公告)日：2017-09-28

申请号：US15461560

申请日：2017-03-17

申请人： SYNTARGA BV

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： A61K31/437 ,  A61K38/38 ,  A61K39/44 ,  C07D471/04

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.

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.

公开(公告)号：US20160052880A1

公开(公告)日：2016-02-25

申请号：US14526462

申请日：2014-10-28

申请人： Syntarga BV

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： C07D209/60 ,  C07D403/06 ,  C07D471/04 ,  C07D413/06 ,  C07D417/06 ,  A61K31/4365 ,  A61K47/48 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/423 ,  A61K31/428 ,  C07D403/14 ,  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。

公开(公告)号：US11052155B2

公开(公告)日：2021-07-06

申请号：US15461560

申请日：2017-03-17

申请人： SYNTARGA BV

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： A61K39/44 ,  A61K47/64 ,  A61K31/437 ,  C07D471/04 ,  A61K47/65 ,  A61K47/60 ,  A61K47/54 ,  A61K38/38 ,  A61K47/68

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.

公开(公告)号：US20180133316A9

公开(公告)日：2018-05-17

申请号：US15461560

申请日：2017-03-17

申请人： SYNTARGA BV

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： A61K39/44 ,  C07D471/04 ,  A61K38/38 ,  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.

公开(公告)号：US20170333567A1

公开(公告)日：2017-11-23

申请号：US15461569

申请日：2017-03-17

申请人： SYNTARGA BV

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： A61K47/64 ,  A61K31/437 ,  A61K38/38 ,  A61K47/68 ,  C07D471/04 ,  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.

公开(公告)号：US20180147289A9

公开(公告)日：2018-05-31

申请号：US15461569

申请日：2017-03-17

申请人： SYNTARGA BV

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： A61K47/64 ,  C07D471/04 ,  A61K39/44 ,  A61K38/38 ,  A61K47/68 ,  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.

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。