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公开(公告)号：WO2012156918A1
公开(公告)日：2012-11-22
申请号：PCT/IB2012/052445
申请日：2012-05-16
Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V. , ROBILLARD, Marc, Stefan , JANSSEN, Henricus, Marie , TEN HOEVE, Wolter , VERSTEEGEN, Ronny, Mathieu
Inventor： ROBILLARD, Marc, Stefan , JANSSEN, Henricus, Marie , TEN HOEVE, Wolter , VERSTEEGEN, Ronny, Mathieu
IPC: A61K47/48
CPC classification number: A61K47/6803 , A61K31/435 , A61K31/444 , A61K31/704 , A61K38/05 , A61K39/3955 , A61K39/39558 , A61K47/22 , A61K47/545 , A61K47/555 , A61K47/558 , A61K47/6897 , B82Y5/00 , C07C33/16 , C07D237/26 , C07D257/08 , Y02A50/471
Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.
Abstract translation: 本发明涉及用于治疗剂的前药活化方法，其中使用对彼此具有生物正交反应性的非生物活性化学基团。 本发明还涉及包含至少一种前药和至少一种活化剂的前药盒，其中所述前药包含药物和第一生物正交反应性组（所述触发剂），并且其中所述活化剂包含第二生物正交反应性组 。 本发明还涉及上述方法和试剂盒中使用的靶向治疗剂。 本发明特别涉及抗体 - 药物偶联物和双特异性和三特异性抗体衍生物。
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Patent Agency Ranking2.发明申请PRETARGETING KIT FOR IMAGING OR THERAPY COMPRISING A TRANS - CYCLOOCTENE DIENOPHILE AND A DIENE 审中-公开用于成像或治疗包装转子 - 胆固醇和二苯胺的预备套件
公开(公告)号：WO2012153254A1
公开(公告)日：2012-11-15
申请号：PCT/IB2012/052260
申请日：2012-05-07
Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V. , ROBILLARD, Marc Stefan , LUB, Johan , ROSSIN, Raffaella , VAN DEN BOSCH, Sandra Martina , VERSTEEGEN, Ronny Mathieu
Inventor： ROBILLARD, Marc Stefan , LUB, Johan , ROSSIN, Raffaella , VAN DEN BOSCH, Sandra Martina , VERSTEEGEN, Ronny Mathieu
CPC classification number: A61K51/1093 , A61K47/6897 , A61K49/106 , A61K51/041 , A61K51/0495 , A61K51/0497 , B82Y5/00 , C07D207/46 , C07D235/02 , C07D245/02 , C07D249/16
Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels- Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has a flattened structure as a result of the position of at least two exocyclic bonds.
Abstract translation: 描述了用于靶向医学成像和/或治疗剂的预靶向方法和相关试剂盒，其中使用对彼此显示出生物正交反应性的非生物反应性化学基团。 本发明涉及使用[4 + 2]反电子需求（复古）Diels-Alder化学来提供预瞄准探针和效应探针之间的耦合。 为此目的，这些探针中的一个包括电子缺乏四嗪或其它合适的二烯，另一个是由于至少两个环外键的位置而具有扁平结构的E-环辛烯。
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公开(公告)号：WO2012049624A1
公开(公告)日：2012-04-19
申请号：PCT/IB2011/054481
申请日：2011-10-11
Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V. , LUB, Johan , TEN HOEVE, Wolter , ROSSIN, Raffaella , VAN DEN BOSCH, Sandra Martina , ROBILLARD, Marc Stefan
Inventor： LUB, Johan , TEN HOEVE, Wolter , ROSSIN, Raffaella , VAN DEN BOSCH, Sandra Martina , ROBILLARD, Marc Stefan
CPC classification number: A61K51/1093 , A61K47/4813 , A61K47/48215 , A61K47/48723 , A61K47/6889 , A61K47/6891 , A61K49/16 , A61K51/0495 , A61K51/10 , B82Y5/00
Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistryin providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has one or more axial substituents.
Abstract translation: 描述了用于靶向医学成像和/或治疗剂的预靶向方法和相关试剂盒，其中使用对彼此显示出生物正交反应性的非生物反应性化学基团。 本发明涉及使用[4 + 2]反电子需求（复古）Diels-Alder化学，提供预瞄准探针和效应探针之间的耦合。 为此目的，这些探针中的一个包括电子缺乏四嗪或其它合适的二烯，另一个是具有一个或多个轴取代基的E-环辛烯。
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公开(公告)号：WO2012156919A1
公开(公告)日：2012-11-22
申请号：PCT/IB2012/052446
申请日：2012-05-16
Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V. , ROBILLARD, Marc, Stefan , JANSSEN, Henricus, Marie , TEN HOEVE, Wolter , VERSTEEGEN, Ronny, Mathieu , ROSSIN, Raffaella
Inventor： ROBILLARD, Marc, Stefan , JANSSEN, Henricus, Marie , TEN HOEVE, Wolter , VERSTEEGEN, Ronny, Mathieu , ROSSIN, Raffaella
IPC: A61K47/48
CPC classification number: A61K47/6803 , A61K31/435 , A61K31/444 , A61K31/704 , A61K38/05 , A61K39/3955 , A61K39/39558 , A61K47/22 , A61K47/545 , A61K47/555 , A61K47/558 , A61K47/6897 , B82Y5/00 , C07C33/16 , C07D237/26 , C07D257/08 , Y02A50/471
Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi-and trispecific antibody derivatives.
Abstract translation: 本发明涉及用于治疗剂的前药活化方法，其中使用对彼此具有生物正交反应性的非生物活性化学基团。 本发明还涉及包含至少一种前药和至少一种活化剂的前药盒，其中所述前药包含药物和第一生物正交反应性组（所述触发剂），并且其中所述活化剂包含第二生物正交反应性组 。 本发明还涉及上述方法和试剂盒中使用的靶向治疗剂。 本发明特别涉及抗体 - 药物偶联物和双和三特异性抗体衍生物。
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公开(公告)号：WO2012156920A1
公开(公告)日：2012-11-22
申请号：PCT/IB2012/052447
申请日：2012-05-16
Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V. , ROBILLARD, Marc, Stefan , TEN HOEVE, Wolter , VERSTEEGEN, Ronny, Mathieu , ROSSIN, Raffaella , HOEBEN, Freek, Johannes, Maria
Inventor： ROBILLARD, Marc, Stefan , TEN HOEVE, Wolter , VERSTEEGEN, Ronny, Mathieu , ROSSIN, Raffaella , HOEBEN, Freek, Johannes, Maria
IPC: A61K47/48
CPC classification number: A61K47/6803 , A61K31/435 , A61K31/444 , A61K31/704 , A61K38/05 , A61K39/3955 , A61K39/39558 , A61K47/22 , A61K47/545 , A61K47/555 , A61K47/558 , A61K47/6897 , B82Y5/00 , C07C33/16 , C07D237/26 , C07D257/08 , Y02A50/471
Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.
Abstract translation: 本发明涉及用于治疗的前药活化方法，其中使用由彼此表现出生物正交反应性的非生物反应性化学基团组成。 本发明还涉及包含至少一种前药和至少一种活化剂的前药药盒，其中前药包含药物和第一生物正交反应性基团（触发剂），并且其中活化剂包含第二生物正交反应性基团 。 本发明还涉及在上述方法和试剂盒中使用的靶向治疗剂。 本发明特别涉及抗体 - 药物偶联物和双和三特异性抗体衍生物。
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公开(公告)号：WO2012085789A1
公开(公告)日：2012-06-28
申请号：PCT/IB2011/055730
申请日：2011-12-16
Applicant: KONINKLIJKE PHILIPS ELECTRONICS N.V. , ROSSIN, Raffaella , LAEPPCHEN, Tilman , VAN DEN BOSCH, Sandra Martina , ROBILLARD, Marc Stefan , VERSTEEGEN, Ronny Mathieu
Inventor： ROSSIN, Raffaella , LAEPPCHEN, Tilman , VAN DEN BOSCH, Sandra Martina , ROBILLARD, Marc Stefan , VERSTEEGEN, Ronny Mathieu
CPC classification number: A61K51/044 , A61K31/495 , A61K45/06 , A61K47/4873 , A61K47/48746 , A61K47/6893 , A61K47/6897 , A61K51/0495 , A61K51/1027 , A61K51/1045 , A61K51/1093 , B82Y5/00
Abstract: Described is a method, and a combination of agents for used therein, by which an agent administered to a subject can be rapidly cleared from circulation. This is achieved by providing an Administration Agent (e.g. a probe for pretargeting) with a reactive group and providing a Clearing Agent with another reactive group, said reactive groups forming a bio-orthogonally reactive pair. Preferably, the reactive pair comprises a cyclooctene or cyclooctyn as one reactant, and a diene as the other reactant. The method and combination can be used for the removal of any bindable molecule from circulation, such as an excess of a pre-targeting probe in the course of a pre-targeting method, a targeting or imaging agent delivered, or the removal of any biomolecule already present in circulation.
Abstract translation: 描述了一种方法，以及其中使用的试剂的组合，通过其可以将施用于受试者的药剂迅速地从循环中清除。 这通过提供与反应性基团的给药剂（例如用于预靶向的探针）并向澄清剂提供另一反应性基团来实现，所述反应性基团形成生物正交反应性对。 优选地，反应性对包括作为一种反应物的环辛烯或环辛烯，和作为其它反应物的二烯。 该方法和组合可用于从循环中除去任何可结合的分子，例如在预靶向法，靶向或成像剂递送过程中过量的预靶向探针，或去除任何生物分子 已经流通。
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