公开(公告)号：WO2020256546A1

公开(公告)日：2020-12-24

申请号：PCT/NL2020/050388

申请日：2020-06-17

Applicant: TAGWORKS PHARMACEUTICALS B.V. ,  TECHNISCHE UNIVERSITÄT WIEN

Inventor： ROBILLARD, Marc Stefan ,  MIKULA, Hannes ,  TEN HOEVE, Wolter ,  ROSSIN, Raffaella

IPC: C07C13/263 ,  C07D317/44 ,  A61K47/54

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：WO2014081303A1

公开(公告)日：2014-05-30

申请号：PCT/NL2013/050850

申请日：2013-11-22

Applicant: TAGWORKS PHARMACEUTICALS B.V.

Inventor： ROBILLARD, Marc Stefan ,  VERSTEEGEN, Ronny Mathieu ,  TEN HOEVE, Wolter ,  ROSSIN, Raffaella

IPC: A61K47/48 ,  C07C13/00

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 reactice 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。 该反应组分是亲二烯体，特别是反式环辛烯，二烯，特别是四嗪。

公开(公告)号：WO2022197182A1

公开(公告)日：2022-09-22

申请号：PCT/NL2022/050142

申请日：2022-03-16

Applicant: TAGWORKS PHARMACEUTICALS B.V.

Inventor： TEN HOEVE, Wolter ,  ROBILLARD, Marc Stefan ,  FERRER, Catalina ,  KLEIJN, Laurens Henri Johan ,  VERSTEEGEN, Ronny Mathieu

IPC: A61K47/68 ,  A61P35/00 ,  C07C51/15 ,  C07C51/367 ,  C07C51/64 ,  C07C269/04 ,  C07D207/46 ,  C07K16/30

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：WO2018004338A1

公开(公告)日：2018-01-04

申请号：PCT/NL2017/050427

申请日：2017-06-27

Applicant: TAGWORKS PHARMACEUTICALS B.V.

Inventor： ROBILLARD, Marc Stefan ,  TEN HOEVE, Wolter ,  HOEBEN, Freek Johannes Maria ,  VERSTEEGEN, Ronny Mathieu ,  JANSSEN, Hendricus Marie ,  VAN ONZEN, Arthur Henry Antoon Marie ,  ROSSIN, Raffaella

IPC: A61K47/54 ,  A61K47/69 ,  B82Y5/00 ,  C07D257/08

CPC classification number: A61K47/6889 ,  A61K47/555 ,  A61K47/60 ,  A61K47/6415 ,  A61K47/66 ,  A61K47/6817 ,  A61K47/6897 ,  A61K2039/505 ,  C07D257/08 ,  C07K16/30 ,  C07K16/3046 ,  C07K2317/626 ,  C07K2317/94

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 C A bound to a Trigger T R , the kit comprising 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 comprising a Construct C A bound thereto and a dienophile, as a chemical tool for the release, in a chemical, biological or physiological environment, of said Construct.

Abstract translation: 公开的是引起化学切割的进步。 因此，本发明提供了二烯作为连接到构建体的化学可切割基团的用途，以及使用亲二烯体通过使二烯与能够经历逆电子需求的亲二烯体反应而引发构建体的释放Diels Alder 与二烯反应。 本发明包括用于释放结合触发剂T的构建体C 的试剂盒，所述试剂盒包含四嗪和亲二烯体，其中触发剂是四嗪。 本发明还包括在化学，生物或生理学环境中通过使包含结合于其上的构建体C ^和亲二烯体的四嗪作为释放的化学工具反应形成哒嗪的用途 ，所述构造的

公开(公告)号：WO2014081300A1

公开(公告)日：2014-05-30

申请号：PCT/NL2013/050847

申请日：2013-11-22

Applicant: TAGWORKS PHARMACEUTICALS B.V.

Inventor： ROBILLARD, Marc Stefan ,  TEN HOEVE, Wolter

IPC: A61K47/48 ,  A61P35/00

CPC classification number: A61K47/6911

Abstract: Disclosed is a liposome, comprising a lipid bilayer enclosing a cavity, wherein the bilayer comprises a channel protein releasably linked to an eight-membered non-aromatic cyclic alkenylene group, preferably a cyclooctene group, and more preferably a trans-cyclooctene group. The liposomes are used in a kit comprising the liposome, the liposomal membrane of which comprises a channel protein linked to a Trigger, and an Activator for the Trigger, wherein the Trigger comprises the eight- membered non-aromatic cyclic alkenylene group, and the Activator comprises a diene.

Abstract translation: 公开了一种脂质体，其包含封闭腔的脂质双层，其中所述双层包含可释放地连接到八元非芳族环亚烯基，优选环辛烯基，更优选反式环辛烯基的通道蛋白。 脂质体用于包含脂质体的试剂盒中，其脂质体膜包含与Trigger连接的通道蛋白质和用于触发剂的活化剂，其中触发剂包含八元非芳族环亚烯基和激活剂 包含二烯。