公开(公告)号：EP3108886A2

公开(公告)日：2016-12-28

申请号：EP16176625.8

申请日：2011-04-21

申请人： Syntarga B.V.

发明人： BEUSKER, Patrick Henry ,  COUMANS, Rudy Gerardus Elisabeth ,  ELGERSMA, Ronald Christiaan ,  MENGE, Wiro Michael Petrus Bernardus ,  JOOSTEN, Johannes Albertus Frederikus ,  SPIJKER, Henri Johannes ,  GROOT de, Franciscus Marinus Hendrikus

IPC分类号： A61K31/437 ,  A61P35/00 ,  A61K47/48 ,  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.

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。 缀合物被设计成在一个或多个活化步骤之后和/或在由缀合物控制的速率和时间范围内释放它们的（多重）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：EP3056203B1

公开(公告)日：2017-12-13

申请号：EP16154533.0

申请日：2011-04-21

申请人： Syntarga B.V.

发明人： BEUSKER, Patrick Henry ,  COUMANS, Rudy Gerardus Elisabeth ,  ELGERSMA, Ronald Christiaan ,  MENGE, Wiro Michael Petrus Bernardus ,  JOOSTEN, Johannes Albertus Frederikus ,  SPIJKER, Henri Johannes ,  GROOT de, Franciscus Marinus Hendrikus

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61K47/68 ,  A61P35/00

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 conjugates of the DNA-alkylating agent CC-1065. 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 conjugates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the conjugates of this invention may be used to treat a tumor.

公开(公告)号：EP3108886A3

公开(公告)日：2017-03-22

申请号：EP16176625.8

申请日：2011-04-21

申请人： Syntarga B.V.

发明人： BEUSKER, Patrick Henry ,  COUMANS, Rudy Gerardus Elisabeth ,  ELGERSMA, Ronald Christiaan ,  MENGE, Wiro Michael Petrus Bernardus ,  JOOSTEN, Johannes Albertus Frederikus ,  SPIJKER, Henri Johannes ,  GROOT de, Franciscus Marinus Hendrikus

IPC分类号： A61K31/437 ,  A61P35/00 ,  A61K47/48 ,  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.

摘要翻译： 本发明涉及DNA-烷化剂CC-1065的新型缀合物。 缀合物被设计成在一个或多个活化步骤之后和/或在由缀合物控制的速率和时间范围内释放它们的（多重）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。 缀合物可用于治疗以不期望（细胞）增殖为特征的疾病。 作为实例，本发明的缀合物可用于治疗肿瘤。

公开(公告)号：EP2173739B1

公开(公告)日：2013-07-31

申请号：EP07808517.2

申请日：2007-08-01

申请人： Syntarga B.V.

发明人： BEUSKER, Patrick Henry ,  SPIJKER, Henri Johannes ,  JOOSTEN, Johannes Albertus Frederikus ,  HUIJBREGTS, Tijl ,  DE GROOT, Franciscus Marinus Hendrikus

IPC分类号： C07D403/06 ,  C07D403/14 ,  A61K31/403 ,  A61P35/00

CPC分类号： C07D403/06 ,  C07D403/14

公开(公告)号：EP2344478A2

公开(公告)日：2011-07-20

申请号：EP09748515.5

申请日：2009-11-03

申请人： Syntarga B.V.

发明人： BEUSKER, Patrick Henry ,  COUMANS, Rudy Gerardus Elisabeth ,  ELGERSMA, Ronald Christiaan ,  MENGE, Wiro Michaël Petrus Bernardus ,  JOOSTEN, Johannes Albertus Frederikus ,  SPIJKER, Henri Johannes ,  DE GROOT, Franciscus Marinus Hendrikus

IPC分类号： C07D403/06

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。 缀合物被设计成在一个或多个活化步骤之后和/或在由缀合物控制的速率和时间范围内释放它们的（多重）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：EP2344478B1

公开(公告)日：2017-09-27

申请号：EP09748515.5

申请日：2009-11-03

申请人： Syntarga B.V.

发明人： BEUSKER, Patrick Henry ,  COUMANS, Rudy Gerardus Elisabeth ,  ELGERSMA, Ronald Christiaan ,  MENGE, Wiro Michaël Petrus Bernardus ,  JOOSTEN, Johannes Albertus Frederikus ,  SPIJKER, Henri Johannes ,  DE GROOT, Franciscus Marinus Hendrikus

IPC分类号： C07D209/60 ,  C07D403/06 ,  C07D403/14 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4365

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

公开(公告)号：EP3056203A1

公开(公告)日：2016-08-17

申请号：EP16154533.0

申请日：2011-04-21

申请人： Syntarga B.V.

发明人： BEUSKER, Patrick Henry ,  COUMANS, Rudy Gerardus Elisabeth ,  ELGERSMA, Ronald Christiaan ,  MENGE, Wiro Michael Petrus Bernardus ,  JOOSTEN, Johannes Albertus Frederikus ,  SPIJKER, Henri Johannes ,  GROOT de, Franciscus Marinus Hendrikus

IPC分类号： A61K31/437 ,  A61P35/00 ,  A61K47/48 ,  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 conjugates of the DNA-alkylating agent CC-1065. 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 conjugates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, 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的新型缀合物。 缀合物被设计成在一个或多个活化步骤之后和/或在由缀合物控制的速率和时间范围内释放它们的（多重）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。 缀合物可用于治疗以不期望（细胞）增殖为特征的疾病。 作为实例，本发明的缀合物可用于治疗肿瘤。

公开(公告)号：EP2173739A1

公开(公告)日：2010-04-14

申请号：EP07808517.2

申请日：2007-08-01

申请人： Syntarga B.V.

发明人： BEUSKER, Patrick Henry ,  SPIJKER, Henri Johannes ,  JOOSTEN, Johannes Albertus Frederikus ,  HUIJBREGTS, Tijl ,  DE GROOT, Franciscus Marinus Hendrikus

IPC分类号： C07D403/06 ,  C07D403/14 ,  A61K31/403 ,  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.