公开(公告)号：US10376594B2

公开(公告)日：2019-08-13

申请号：US14983858

申请日：2015-12-30

Applicant: TAGWORKS PHARMACEUTICALS B.V.

Inventor： Marc Stefan Robillard ,  Hendricus Marie Janssen ,  Wolter Ten Hoeve ,  Ronny Mathieu Versteegen ,  Raffaella Rossin

IPC: 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

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.

公开(公告)号：US12186405B2

公开(公告)日：2025-01-07

申请号：US17948684

申请日：2022-09-20

Applicant: TAGWORKS PHARMACEUTICALS B.V.

Inventor： Marc Stefan Robillard ,  Wolter Ten Hoeve ,  Freek Johannes Maria Hoeben ,  Ronny Mathieu Versteegen ,  Henricus Marie Janssen ,  Arthur Henry Antoon Marie Van Onzen ,  Raffaella Rossin

IPC: C07D257/02 ,  A61K31/495 ,  A61K31/502 ,  A61K47/54 ,  A61K47/60 ,  A61K47/64 ,  A61K47/66 ,  A61K47/68 ,  C07C33/16 ,  C07D237/26 ,  C07D257/08 ,  C07K16/30 ,  A61K39/00

Abstract: 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.

公开(公告)号：US11857636B2

公开(公告)日：2024-01-02

申请号：US17169217

申请日：2021-02-05

Applicant: TAGWORKS PHARMACEUTICALS B.V.

Inventor： Marc Stefan Robillard ,  Hendricus Marie Janssen ,  Wolter Ten Hoeve ,  Ronny Mathieu Versteegen ,  Raffaella Rossin

IPC: 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 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 ,  Y02A50/30

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.

公开(公告)号：US11617799B2

公开(公告)日：2023-04-04

申请号：US16312569

申请日：2017-06-27

Applicant: Tagworks Pharmaceuticals B.V. ,  Syncom B.V.

Inventor： 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: 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

Abstract: 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.

公开(公告)号：US10967069B2

公开(公告)日：2021-04-06

申请号：US16512038

申请日：2019-07-15

Applicant: TAGWORKS PHARMACEUTICALS B.V.

Inventor： Marc Stefan Robillard ,  Hendricus Marie Janssen ,  Wolter Ten Hoeve ,  Ronny Mathieu Versteegen ,  Raffaella Rossin

IPC: 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

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.

公开(公告)号：US10004810B2

公开(公告)日：2018-06-26

申请号：US15233283

申请日：2016-11-23

Applicant: TAGWORKS PHARMACEUTICALS B.V.

Inventor： Marc Stefan Robillard ,  Hendricus Marie Janssen ,  Wolter Ten Hoeve ,  Ronny Mathieu Versteegen

IPC: 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 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.