1,4-Dimethoxy-1-azacyclooct-2-yne

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 1,4-Dimethoxy-1-azacyclooct-2-yne
• 英文别名: 1,4-dimethoxy-1-azacyclooct-2-yne
• 化学式: C₉H₁₅NO₂
• 分子量: 169.22
• InChiKey: NGDAPSOFJLBOPJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.78
• 拓扑面积：
  21.7
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] PROCESS FOR THE CYCLOADDITION OF A HALOGENATED 1,3-DIPOLE COMPOUND WITH A (HETERO)CYCLOALKYNE<br/>[FR] PROCÉDÉ DE CYCLOADDITION D'UN COMPOSÉ 1,3-DIPPOLE HALOGÉNÉ AVEC UN (HÉTÉRO)CYCLOALKYNE
  申请人：SYNAFFIX BV

  公开号：WO2015112016A1

  公开（公告）日：2015-07-30

  The present invention relates to a cycloaddition process comprising the step of reacting a halogenated aliphatic 1,3-dipole compound with a (hetero)cycloalkyne according to Formula (1): Preferably, the (hetero)cycloalkyne according to Formula (1) is a (hetero)cyclooctyne. The invention also relates to the cycloaddition products obtainable by the process according to the invention. The invention further relates to halogenated aliphatic 1,3- dipole compounds, in particular tohalogenated aliphatic 1,3-dipole compounds comprising N-acetylgalactosamine-UDP (GalNAc-UDP),and to halogenated 1,3- dipole compounds comprising (peracylated) N-acetylglucosamine(GlcNAc), N- acetylgalactosamine(GalNAc), N-acetylmannosamine(ManNAc)and N- acetylneuraminic acid(NeuNAc).

  本发明涉及一种环加成过程，包括将卤代脂肪1,3-二极化合物与按照式（1）反应的（杂）环烯烃化合物进行反应的步骤。优选，按照式（1）的（杂）环烯烃化合物是（杂）环辛烯。该发明还涉及根据本发明的方法获得的环加成产物。此外，该发明还涉及卤代脂肪1,3-二极化合物，特别是包括N-乙酰半乳糖氨基葡萄糖醛酸-UDP（GalNAc-UDP）的卤代脂肪1,3-二极化合物，以及包括（过酰化的）N-乙酰葡萄糖胺（GlcNAc）、N-乙酰半乳糖氨基葡萄糖醛酸（GalNAc）、N-乙酰甘露糖氨基葡萄糖醛酸（ManNAc）和N-乙酰神经酸（NeuNAc）的卤代1,3-二极化合物。
• [EN] NOVEL PD-L1 BINDING POLYPEPTIDES FOR IMAGING<br/>[FR] NOUVEAUX POLYPEPTIDES FIXANT PD-L1 POUR L'IMAGERIE
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2016086021A1

  公开（公告）日：2016-06-02

  Provided herein are novel 10Fn3 domains which specifically bind to PD-L1, as well as imaging agents based on the same for diagnostics.

  本文提供了一种新颖的10Fn3结构域，该结构域特异性结合PD-L1，以及基于该结构域的用于诊断的成像剂。
• [EN] PET IMAGING WITH PD-L1 BINDING POLYPEPTIDES<br/>[FR] IMAGERIE PET AVEC DES POLYPEPTIDES DE LIAISON PD-L1
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2017210302A1

  公开（公告）日：2017-12-07

  Provided herein are novel 10Fn3 domains which specifically bind to PD-L1, as well as imaging agents based on the same for diagnostics.

  本文提供了一种新颖的10Fn3结构域，该结构域特异性结合PD-L1，以及基于该结构域的用于诊断的成像剂。
• [EN] IMAGING METHODS USING 18F-RADIOLABELED BIOLOGICS<br/>[FR] MÉTHODES D'IMAGERIE FAISANT INTERVENIR DES SUBSTANCES BIOLOGIQUES RADIOMARQUÉES AU 18F
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2017210335A1

  公开（公告）日：2017-12-07

  The invention relates to water soluble 18F-prosthetic groups and the synthesis and use 18F-labeled biological molecules containing the 18F-prosthetic groups for imaging various processes within the body, for detecting the location of molecules associated with disease pathology, and for monitoring disease progression are disclosed.

  这项发明涉及水溶性的18F-假体基团，以及合成和使用含有这些18F-假体基团的18F标记生物分子，用于成像体内各种过程，检测与疾病病理相关的分子的位置，并监测疾病进展。
• [EN] RELEASABLE CONJUGATES<br/>[FR] CONJUGUÉS LIBÉRABLES
  申请人：QUIAPEG PHARMACEUTICALS AB

  公开号：WO2018163131A1

  公开（公告）日：2018-09-13

  The present application provides compounds of Formula (B), or pharmaceutically acceptable salts thereof, wherein D is a residue of a biologically active drug, which underdo hydrolysis under physiological conditions to release the biologically active drug and which are useful in the treatment of disorders that could be beneficially treated with the drug.

  本申请提供了化合物的公式（B），或其药用盐，其中D是生物活性药物的残留物，在生理条件下经过水解释放出生物活性药物，并且对可能受益于该药物治疗的疾病具有用处。