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    HYDROPHILIC AZADIBENZOCYCLOOCTYNE DERIVATIVES AND METAL-FREE CLICK REACTIONS WITH THESE HYDROPHILIC AZADIBENZOCYCLOOCTYNE DERIVATIVES
    11.
    发明公开
    HYDROPHILIC AZADIBENZOCYCLOOCTYNE DERIVATIVES AND METAL-FREE CLICK REACTIONS WITH THESE HYDROPHILIC AZADIBENZOCYCLOOCTYNE DERIVATIVES 审中-公开

    公开(公告)号：US20240300900A1

    公开(公告)日：2024-09-12

    申请号：US18660802

    申请日：2024-05-10

    Applicant: Roche Diagnostics Operations, Inc.

    Inventor： Frank Bergmann ,  Dieter Heindl ,  Nils Winter

    IPC: C07D225/08 ,  A61K47/54 ,  A61K49/00 ,  A61K51/04

    CPC classification number: C07D225/08 ,  A61K47/545 ,  A61K49/0052 ,  A61K51/044

    Abstract: The invention relates in a first aspect to an azadibenzocyclooctyne derivative according to formula (I) or a salt thereof having specific substituents at the benzo rings of the DIBAC structure and having specific substituents connected to the nitrogen atom of the DIBAC structure. A second aspect of the invention is directed to a conjugate of formula (II), wherein a substituent R6 is connected to the N atom of the 8 membered ring of the DIBAC structure via a linker structure —C(═O)-[L]n-Z—. A third aspect of the invention relates to a method for the modification of a target molecule, wherein a conjugate according to the second aspect is reacted with a target molecule comprising a 1,3-dipole group or a 1,3-(hetero)diene group. In a fourth aspect, the invention is directed to the use of the conjugate according to the second aspect for bioorthogonal labeling and/or modification of a target molecule. A fifth aspect of the invention relates to a modified target molecule comprising the reaction product of a conjugate according to the second aspect and a target molecule comprising a 1,3-dipole group or a 1,3-(hetero)diene group, obtained or obtainable from the method of the third aspect. In a sixth aspect, the invention is related to a kit comprising a modified target molecule according to the fifth aspect as detector reagent and a suitable capture reagent.

    Method for labeling of aldehyde containing target molecules
    12.
    发明授权
    Method for labeling of aldehyde containing target molecules 有权

    公开(公告)号：US11236386B2

    公开(公告)日：2022-02-01

    申请号：US16598685

    申请日：2019-10-10

    Applicant: Roche Diagnostics Operations, Inc.

    Inventor： Frank Bergmann ,  Tobias Oelschlaegel ,  Sebastian Johannes Pomplun

    IPC: C12Q1/6869 ,  C07D295/13 ,  C07D487/04 ,  C07H21/02 ,  C07H21/04 ,  A61K47/68

    Abstract: The present description relates to a method for binding to a target molecule having an aldehyde compound derived from N-(2-aminoethyl)pyrrole, which compound also has a moiety of interest, to compounds (conjugates) obtained by this method, having both the target molecule and the moiety of interest and to novel substances derived from N-(2-aminoethyl)pyrrole. In one embodiment, the compound has the formula of Formula II wherein R1, R2 and R3 independently are H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein R4, R5, R6, R7 and R8 independently are H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or -LM, wherein L is absent or is a linker and M is a moiety of interest selected from a nucleotide, an oligonucleotide, a peptide, a label, a cytotoxic agent, a partner of a binding pair and a functional group, wherein two of R4, R5, R6, R7, and R8 optionally are linked to form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted heterocycloalkyl, and T is a target molecule selected from the group consisting of a solid phase, a polypeptide, a protein, a carbohydrate, a nucleotide and a nucleic acid, with the proviso that at least one of R4, R5, R6, R7 or R8 is -LM.

    SET OF OLIGONUCLEOTIDE PROBES AS WELL AS METHODS AND USES THERETO
    16.
    发明申请
    SET OF OLIGONUCLEOTIDE PROBES AS WELL AS METHODS AND USES THERETO 有权
    作为方法和用途的一组寡核苷酸探针

    公开(公告)号：US20130203628A1

    公开(公告)日：2013-08-08

    申请号：US13862530

    申请日：2013-04-15

    Applicant: ROCHE DIAGNOSTICS OPERATIONS, INC.

    Inventor： Frank Bergmann ,  Walter Eberle ,  Thomas Fischer ,  Herbert von der Eltz

    IPC: C12Q1/68

    CPC classification number: C12Q1/6841 ,  C12Q1/6876 ,  C12Q1/6886 ,  C12Q2565/1025 ,  C12Q2563/107

    Abstract: The present disclosure relates to a set of at least 100 single-stranded oligonucleotide probes directed against (or complementary to) portions of a genomic target sequence of interest. The present disclosure also relates to a method of detecting a genomic target sequence of interest using the set of oligonucleotide probes and a method of generating the set of oligonucleotide probes. Further, the present disclosure relates to a kit comprising the set of oligonucleotide probes and at least one further component.

    Abstract translation: 本公开内容涉及针对感兴趣的基因组靶序列的（或互补）部分的一组至少100个单链寡核苷酸探针。 本公开还涉及使用该组寡核苷酸探针检测感兴趣的基因组靶序列的方法和产生寡核苷酸探针组的方法。 此外，本公开涉及包含该组寡核苷酸探针和至少一种另外的组分的试剂盒。

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