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公开(公告)号：US10376594B2
公开(公告)日：2019-08-13
申请号：US14983858
申请日：2015-12-30
发明人： Marc Stefan Robillard , Hendricus Marie Janssen , Wolter Ten Hoeve , Ronny Mathieu Versteegen , Raffaella Rossin
IPC分类号： C07D257/08 , C07D237/26 , C07C13/263 , C07C33/16 , A61K31/435 , A61K31/502 , A61K31/045 , A61K47/00 , B82Y5/00 , A61K47/68 , A61K31/704 , A61K38/05 , A61K39/395 , A61K47/22 , A61K31/444 , A61K47/54
摘要： 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.
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公开(公告)号：US11857636B2
公开(公告)日：2024-01-02
申请号：US17169217
申请日：2021-02-05
发明人： Marc Stefan Robillard , Hendricus Marie Janssen , Wolter Ten Hoeve , Ronny Mathieu Versteegen , Raffaella Rossin
IPC分类号： C07D257/02 , C07D257/08 , C07D237/26 , C07C33/16 , A61K47/68 , A61K47/54 , B82Y5/00 , A61K31/704 , A61K38/05 , A61K39/395 , A61K47/22 , A61K31/435 , A61K31/444
CPC分类号： 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 , Y02A50/30
摘要： 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.
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公开(公告)号：US11617799B2
公开(公告)日：2023-04-04
申请号：US16312569
申请日：2017-06-27
发明人： Marc Stefan Robillard , Wolter Ten Hoeve , Freek Johannes Maria Hoeben , Ronny Mathieu Versteegen , Hendricus Marie Janssen , Arthur Henry Antoon Marie Van Onzen , Raffaella Rossin
IPC分类号： C07D257/02 , C07D257/08 , C07D237/26 , C07C33/16 , A61K31/495 , A61K31/502 , A61K47/68 , A61K47/54 , C07K16/30 , A61K47/66 , A61K47/60 , A61K47/64 , A61K39/00
摘要： Disclosed is an advancement in provoked chemical cleavage. Thereby the invention provides the use of a diene as a chemically cleavable group attached to a Construct, and the use of a dienophile to provoke the release of the Construct by allowing the diene to react with a dienophile capable of undergoing an inverse electron demand Diels Alder reaction with the diene. The invention includes a kit for releasing a Construct CA bound to a Trigger TR, the kit having a tetrazine and a dienophile, wherein the Trigger is the tetrazine. The invention also includes the use of the formation of a pyridazine by reacting a tetrazine having a Construct CA bound thereto and a dienophile, as a chemical tool for the release, in a chemical, biological or physiological environment, of the Construct.
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公开(公告)号：US10967069B2
公开(公告)日：2021-04-06
申请号：US16512038
申请日：2019-07-15
发明人： Marc Stefan Robillard , Hendricus Marie Janssen , Wolter Ten Hoeve , Ronny Mathieu Versteegen , Raffaella Rossin
IPC分类号： C07D237/26 , C07D257/08 , C07C33/16 , A61K31/704 , A61K31/502 , A61K31/444 , A61K31/435 , A61K47/00 , A61K47/68 , A61K47/44 , A61K47/22 , A61K47/54 , B82Y5/00 , A61K38/05 , A61K39/395
摘要： 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.
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公开(公告)号：US10004810B2
公开(公告)日：2018-06-26
申请号：US15233283
申请日：2016-11-23
IPC分类号： C07D257/08 , C07D237/26 , A61K47/48 , C07C33/16 , B82Y5/00 , A61K31/704 , A61K38/05 , A61K39/395 , A61K47/22 , A61K31/435 , A61K31/444 , A61K47/54 , A61K47/68
CPC分类号： 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
摘要： 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.
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