公开(公告)号：US20160214917A1

公开(公告)日：2016-07-28

申请号：US14978924

申请日：2015-12-22

Applicant: SynAffix B.V.

Inventor： Floris Louis VAN DELFT ,  Floris Petrus Johannes Theodorus RUTJES ,  Frederik Jan DOMMERHOLT

IPC: C07C33/16 ,  C07D311/82 ,  G01N21/64 ,  C07C67/347 ,  A61K49/00 ,  G01N33/58 ,  C07D495/04 ,  C07C29/147

CPC classification number: C07C33/16 ,  A61K47/54 ,  A61K49/0052 ,  C07C29/147 ,  C07C29/58 ,  C07C29/62 ,  C07C62/30 ,  C07C67/347 ,  C07C269/06 ,  C07C271/12 ,  C07C271/20 ,  C07C2602/24 ,  C07D311/82 ,  C07D495/04 ,  C07K14/47 ,  G01N21/6428 ,  G01N33/532 ,  G01N33/582 ,  G01N33/585 ,  G01N2021/6439 ,  C07C33/44 ,  C07C69/753

Abstract: The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.

公开(公告)号：US20200048174A1

公开(公告)日：2020-02-13

申请号：US16358272

申请日：2019-03-19

Applicant: SynAffix B.V.

Inventor： Floris Louis VAN DELFT ,  Floris Petrus Johannes Theodorus RUTJES ,  Frederik Jan DOMMERHOLT

IPC: C07C33/16 ,  A61K49/00 ,  C07C29/147 ,  C07C29/58 ,  C07C29/62 ,  C07C67/347 ,  C07C271/12 ,  G01N33/532 ,  G01N33/58 ,  A61K47/54 ,  C07C62/30 ,  C07C269/06 ,  C07C271/20 ,  C07D311/82 ,  C07D495/04 ,  C07K14/47 ,  G01N21/64

Abstract: The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.

公开(公告)号：US20170002012A1

公开(公告)日：2017-01-05

申请号：US15113730

申请日：2015-01-26

Applicant: SYNAFFIX B.V.

Inventor： Floris Louis VAN DELFT ,  Frederik Jan DOMMERHOLT

IPC: C07D487/04 ,  C07C269/06 ,  A61K47/48 ,  C07C271/18 ,  C07H19/10 ,  C07K14/47

CPC classification number: C07D487/04 ,  A61K47/545 ,  A61K47/60 ,  A61K47/6855 ,  C07C269/06 ,  C07C271/18 ,  C07C2602/22 ,  C07C2603/50 ,  C07D225/02 ,  C07D225/08 ,  C07D231/54 ,  C07D249/16 ,  C07D261/20 ,  C07H19/10 ,  C07K14/473

Abstract: A process is provided, comprising reacting a (hetero)aryl 1,3-dipole compound with a (hetero)cycloalkyne, wherein the (hetero)aryl 1,3-dipole compound comprises a 1,3-dipole functional group bonded to a (hetero)aryl group, and wherein the (hetero)aryl 1,3-dipole compound is a (hetero)aryl azide or a (hetero)aryl diazo compound; wherein:(i) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound comprises a substituent(ii) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound is an electron-poor (hetero)aryl groupand wherein the (hetero)cycloalkyne is a (hetero)cyclooctyne or a (hetero)cyclononyne according to Formula (1). The invention also relates to the products obtainable by the process according to the invention.

Abstract translation: 并且其中（杂）环炔是根据式（1）的（杂）环辛炔或（异）环壬炔。 本发明还涉及通过根据本发明的方法可获得的产品。