3-Fluoro-3-methylcyclooctyne

• 分子结构分类: 有机化合物 - 有机卤素化合物 - 有机氟化物
• 英文名称: 3-Fluoro-3-methylcyclooctyne
• 英文别名: 3-fluoro-3-methylcyclooctyne
• 化学式: C₉H₁₃F
• 分子量: 140.2
• InChiKey: NOBGUCJACVALMY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.78
• 拓扑面积：
  0
• 氢给体数：
  0
• 氢受体数：
  1

文献信息

• [EN] RELEASABLE ANTIBODY CONJUGATES<br/>[FR] CONJUGUÉS D'ANTICORPS LIBÉRABLES
  申请人：QUIAPEG PHARMACEUTICALS AB

  公开号：WO2019171358A1

  公开（公告）日：2019-09-12

  This document provides compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein D is a residue of a cytotoxic or chemotherapeutic compound, which undergoes hydrolysis under physiological conditions to release the cytotoxic or chemotherapeutic compound and which are useful in the treatment of cancer and other diseases.

  本文件提供了化合物的公式(I)，或其药用盐，其中D是细胞毒性或化疗化合物的残基，该残基在生理条件下水解释放出细胞毒性或化疗化合物，并且在癌症和其他疾病的治疗中是有用的。
• Strain-promoted oxidation controlled cycloaddition with high reaction rate
  申请人：Stichting Katholieke Universiteit

  公开号：EP2974744A1

  公开（公告）日：2016-01-20

  The invention provides a the use of a (hetero)cycloalkyne and an oxo-group containing (hetero)1,3-diene for coupling a first system (A) of interest to a second system (A') of interest, wherein a (hetero)cycloalkyne is created in one of the first system (A) of interest and the second system (A') of interest, and wherein an oxo-group containing (hetero)1,3-diene is created in the other system of interest, and allowing the (hetero)cycloalkyne and the oxo-group containing (hetero)1,3-diene to react to form an A-A' conjugate.

  该发明提供了一种使用（杂）环炔和含氧基团的（杂）1,3-二烯将感兴趣的第一系统（A）与感兴趣的第二系统（A'）耦合的方法，其中在感兴趣的第一系统（A）和感兴趣的第二系统（A'）中创建了一个（杂）环炔，而在另一个感兴趣的系统中创建了一个含氧基团的（杂）1,3-二烯，并允许（杂）环炔和含氧基团的（杂）1,3-二烯发生反应形成A-A'共轭物。
• Metabolic labeling and molecular enhancement of biological materials using bioorthogonal reactions
  申请人：The General Hospital Corporation

  公开号：US20170362266A1

  公开（公告）日：2017-12-21

  The present application provides methods of functionalizing an organ or tissue of a mammal by administering a nutrient (e.g., peracetylated N-azido galactosamine Ac4GalNAz) to the mammal or by culturing an organ or tissue in a bioreactor containing such nutrient. The present application also provides methods of selectively functionalizing extracellular matrix (ECM) of an organ or tissue of a mammal by administering a nutrient (e.g., peracetylated N-azido galactosamine Ac4GalNAz) to the mammal. In some aspects, the present application provides a decellularized scaffold of a mammalian organ or tissue comprising an extracellular matrix, wherein the extracellular matrix of the decellularized scaffold is functionalized with a chemical group that is reactive in a bioorthogonal chemical reaction, such as an azide chemical group. The present application also provides biological prosthetic mesh and mammalian organs and tissues for transplantation prepared according to the methods of the application.

  本申请提供了一种通过向哺乳动物投与营养物质（例如，乙酰化N-叠氮基半乳糖氨酸Ac4GalNAz）或在含有这种营养物质的生物反应器中培养器官或组织来功能化哺乳动物器官或组织的方法。本申请还提供了一种通过向哺乳动物投与营养物质（例如，乙酰化N-叠氮基半乳糖氨酸Ac4GalNAz）来选择性地功能化哺乳动物器官或组织的细胞外基质（ECM）的方法。在某些方面，本申请提供了哺乳动物器官或组织的脱细胞支架，其中脱细胞支架的细胞外基质被功能化为在生物正交化学反应中具有反应性的化学基团，例如叠氮基团。本申请还提供了根据本申请的方法制备的生物义肢网和哺乳动物器官和组织用于移植。
• BIOORTHOGONAL MONOMERS CAPABLE OF DIMERIZING AND TARGETING BROMODOMAINS, AND METHODS OF USING SAME
  申请人：Coferon, Inc.

  公开号：US20140243321A1

  公开（公告）日：2014-08-28

  Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.

  本文描述了一种单体，当与一个、两个、三个或更多其他单体在水介质中接触时，能够形成生物上有用的多聚体。在一个方面，这样的单体可以在水介质中（例如在体内）与另一个单体结合形成多聚体（例如二聚体）。考虑到的单体可能包括配体基团、连接元素和连接配体基团和连接元素的连接器元素。在水介质中，这些考虑到的单体可以通过每个连接元素连接在一起，因此可以同时调节一个或多个生物分子，例如调节蛋白质或不同蛋白质上的两个或更多结合域。
• NOVEL FATTY ACIDS AND THEIR USE IN CONJUGATION TO BIOMOLECULES
  申请人：BARNES David Weninger

  公开号：US20160030585A1

  公开（公告）日：2016-02-04

  The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: wherein R 1 , R 2 , R 3 , R 4 , Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

  本发明提供了一种共轭物，其包括通过连接剂与脂肪酸连接的生物分子，其中所述的脂肪酸具有以下的化学式A1、A2或A3：其中，R1、R2、R3、R4、Ak、n、m和p在此定义。本发明还涉及一种制造GDF15共轭物等本发明共轭物的方法，以及其治疗用途，如治疗或预防代谢性疾病或疾病、2型糖尿病、肥胖症、胰腺炎、血脂异常、酒精性和非酒精性脂肪肝病/脂肪性肝炎和其他进行性肝脏疾病、胰岛素抵抗、高胰岛素血症、葡萄糖不耐受、高血糖、代谢综合征、高血压、心血管疾病、动脉粥样硬化、周围动脉疾病、中风、心力衰竭、冠心病、糖尿病并发症（包括但不限于慢性肾脏疾病）、神经病变、胃轻瘫和其他代谢性疾病。本发明还提供了药理活性剂的组合和制药组合物。