-
公开(公告)号:US20230144534A1
公开(公告)日:2023-05-11
申请号:US17948684
申请日:2022-09-20
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
CPC classification number: A61K47/6889 , C07D257/08 , A61K47/555 , A61K47/6897 , C07K16/3046 , A61K47/66 , C07K16/30 , A61K47/60 , A61K47/6817 , A61K47/6415 , C07K2317/626 , A61K2039/505
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:US20210002320A1
公开(公告)日:2021-01-07
申请号:US17023343
申请日:2020-09-16
Applicant: TAGWORKS PHARMACEUTICALS B.V.
IPC: C07H15/252 , G01N33/60 , G01N33/543 , C07C209/62 , C07C205/57 , C07C37/50 , C07C205/20 , C07C29/10 , C07C45/61 , B82Y5/00 , A61K47/54 , A61K47/68 , A61K47/60
Abstract: Disclosed is the use of the reactive components of the inverse electron-demand Diels Alder reaction for chemical masking and unmasking in vitro. This can be applied in complex chemical reactions and, particularly in the synthesis of biomolecules, e.g. on solid supports. The reactice components are a dienophile, particularly a trans-cyclooctene, and a diene, particularly a tetrazine.
-
公开(公告)号:US20150344514A1
公开(公告)日:2015-12-03
申请号:US14646619
申请日:2013-11-22
Applicant: TAGWORKS PHARMACEUTICALS B.V.
IPC: C07H15/252 , G01N33/543 , C07C209/62 , C07C45/61 , C07C37/50 , C07C205/20 , C07C29/10 , G01N33/60 , C07C205/57
CPC classification number: C07H15/252 , A61K47/555 , A61K47/60 , A61K47/6897 , B82Y5/00 , C07C29/10 , C07C37/50 , C07C45/61 , C07C205/20 , C07C205/57 , C07C209/62 , G01N33/54353 , G01N33/60
Abstract: Disclosed is the use of the reactive components of the inverse electron-demand Diels Alder reaction for chemical masking and unmasking in vitro. This can be applied in complex chemical reactions and, particularly in the synthesis of biomolecules, e.g. on solid supports. The reactive components are a dienophile, particularly a trans-cyclooctene, and a diene, particularly a tetrazine.
Abstract translation: 公开了使用反电子需求Diels Alder反应的反应性组分进行化学掩蔽和体外脱膜。 这可以应用于复杂的化学反应,特别是在生物分子的合成中。 固体支撑。 反应性组分是亲二烯体,特别是反式环辛烯,二烯,特别是四嗪。
-
公开(公告)号:US20220356169A1
公开(公告)日:2022-11-10
申请号:US17619794
申请日:2020-06-17
Applicant: Tagworks Pharmaceuticals B.V.
Inventor: Marc Stefan ROBILLARD , Freek Johannes Maria HOEBEN , Raffaella ROSSIN , Ronny Mathieu VERSTEEGEN , Henricus Marie JANSSEN
IPC: C07D401/14 , A61K47/68 , C07D403/14
Abstract: Disclosed herein are tetrazines substituted with groups that result in a high click conjugation yield and high click release yields. In some of several other aspects, the invention relates to combinations and kits having the tetrazines and a dienophile, preferably a trans-cyclooctene. In another aspect, the compounds, combinations, and kits are for use as a medicament.
-
公开(公告)号:US20210162060A1
公开(公告)日:2021-06-03
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: A61K47/68 , C07D237/26 , C07D257/08 , C07C33/16 , A61K47/54 , B82Y5/00 , A61K31/704 , A61K38/05 , A61K39/395 , A61K47/22 , A61K31/435 , A61K31/444
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: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:US20240207434A1
公开(公告)日:2024-06-27
申请号:US18282331
申请日:2022-03-16
Applicant: Tagworks Pharmaceuticals B.V.
Inventor: Wolter TEN HOEVE , Marc Stefan ROBILLARD , Catalina FERRER , Laurens Henri Johan KLEIJN , Ronny Mathieu VERSTEEGEN
CPC classification number: A61K47/6889 , A61K47/54 , A61K47/68031
Abstract: The present invention pertains to improved methods for preparing cyclooctenes and conjugates thereof. In particular, methods for regioselective modification and/or enantiomerically enriching compounds are disclosed. In addition, compounds prepared by these methods are disclosed as well.
-
公开(公告)号:US20230121556A1
公开(公告)日:2023-04-20
申请号:US17619791
申请日:2020-06-17
Inventor: Marc Stefan ROBILLARD , Hannes MIKULA , Wolter TEN HOEVE , Raffaella ROSSIN
Abstract: The invention disclosed herein relates to compounds, combinations, kits, and methods using same, for use in bioorthogonal release reactions. In particular, the compounds, combinations and kits of the invention can be used to achieve fast and efficient click release. Applications of the compounds, combinations, and kits of the invention include both in vitro and in vivo applications.
-
公开(公告)号:US20190336612A1
公开(公告)日:2019-11-07
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: A61K47/68 , C07C33/16 , B82Y5/00 , C07D237/26 , A61K47/54 , A61K31/444 , A61K31/435 , C07D257/08 , A61K31/704 , A61K39/395 , A61K47/22 , A61K38/05
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:US20240091371A1
公开(公告)日:2024-03-21
申请号:US18497645
申请日:2023-10-30
Applicant: Tagworks Pharmaceuticals B.V.
Inventor: Marc Stefan ROBILLARD , Hendricus Marie JANSSEN , Wolter TEN HOEVE , Ronny Mathieu VERSTEEGEN , Raffaella ROSSIN
IPC: A61K47/68 , A61K31/435 , A61K31/444 , A61K31/704 , A61K38/05 , A61K39/395 , A61K47/22 , A61K47/54 , B82Y5/00 , C07C33/16 , C07D237/26 , C07D257/08
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.
-
-
-
-
-
-
-
-
-