6-vinylnicotinic acid | 1211579-10-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 6-vinylnicotinic acid
• 英文别名: 6-ethenylpyridine-3-carboxylic acid
• CAS: 1211579-10-0
• 化学式: C₈H₇NO₂
• 分子量: 149.149
• InChiKey: HCAXAGYQQYQNTF-UHFFFAOYSA-N

物化性质

• 沸点：
  312.7±30.0 °C(Predicted)
• 密度：
  1.231±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  50.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  6-vinylnicotinic acid 在 palladium-carbon 4-二甲氨基吡啶 作用下， 以 乙醇 、 水 、 N,N-二甲基甲酰胺 为溶剂， 生成 6-ethyl-N-[4-(2-furyl)-5-(tetrahydropyran-4-carbonyl)thiazol-2-yl]pyridine-3-carboxamide
  参考文献：
  名称：

  THERAPEUTIC AGENT FOR ANXIETY DISORDERS

  摘要：

  提供一种治疗和/或预防焦虑症的药剂，其包含一种噻唑衍生物作为活性成分，该噻唑衍生物的化学式为（I），其中R1代表芳基或类似物，R2代表吡啶基或类似物，或其药学上可接受的盐等。

  公开号：

  US20120172362A1
• 作为产物：
  描述：

  6-氯烟酸甲酯 在 二氯双(三邻甲苯膦)合钯(II) 、 lithium hydroxide monohydrate 、 lithium chloride 作用下， 以 甲醇 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 生成 6-vinylnicotinic acid
  参考文献：
  名称：

  THERAPEUTIC AGENT FOR ANXIETY DISORDERS

  摘要：

  公开号：

  EP2474544B1

文献信息

• FUNCTIONALISING REAGENTS AND THEIR USES
  申请人：Watts Andrew Graham

  公开号：US20120101254A1

  公开（公告）日：2012-04-26

  Reagents and methods for functionalising polypeptides with moieties poly (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalising reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalising reagent is covalently linked to a poly (alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly (alkylene glycol) molecule and/or the glycan group.

  本发明揭示了用于将多元(烷基乙二醇)分子和糖基与多肽进行官能化的试剂和方法，其基于一种官能化试剂，其包括具有乙烯基取代基的含氮杂环芳香环，其能够与自然存在或已经引入多肽中的一个或多个巯基反应，例如通过使用一个或多个半胱氨酸残基的巯基。官能化试剂与多元(烷基乙二醇)分子（例如聚乙二醇(PEG)分子）或糖基共价连接，使得多肽中的乙烯基与巯基之间的反应共价连接多肽和多元(烷基乙二醇)分子和/或糖基。
• FUNCTIONALIZING REAGENTS AND THEIR USES
  申请人：Glythera Limited

  公开号：US20140364586A1

  公开（公告）日：2014-12-11

  Reagents and methods for functionalizing polypeptides with moieties (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group.

  本文披露了一种功能化试剂和方法，用于将（烷基二醇）分子和糖基与多肽功能化。该方法基于一种功能化试剂，该试剂包含一个含氮杂环芳香环，具有一个乙烯基取代基，能够与多肽中天然存在或已引入的一个或多个巯基反应，例如使用一个或多个半胱氨酸残基的巯基。功能化试剂与多（烷基二醇）分子（例如聚乙二醇（PEG）分子）或糖基共价连接，因此，多肽中乙烯基和巯基之间的反应将多肽共价连接到多（烷基二醇）分子和/或糖基上。
• Thiol-functionalising reagents and their uses
  申请人：Glythera Limited

  公开号：EP2886132A1

  公开（公告）日：2015-06-24

  Reagents and methods for functionalising polypeptides with moieties poly(alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalising reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalising reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group.

  本发明公开了用聚(烷二醇)分子和聚糖基团使多肽功能化的试剂和方法，这些试剂和方法基于一种功能化试剂，该试剂包括一个含氮杂环芳香环，该芳香环具有乙烯基取代基，能够与多肽中天然存在或引入的一个或多个硫醇基反应，例如通过使用一个或多个半胱氨酸残基的硫醇基。官能化试剂与聚(烷二醇)分子（如聚乙二醇（PEG）分子）或聚糖基团共价连接，使乙烯基与多肽中的硫醇基团反应，将多肽与聚(烷二醇)分子和/或聚糖基团共价连接。
• Therapeutic agent for motor disorders
  申请人：KYOWA HAKKO KIRIN CO., LTD.

  公开号：US10407440B2

  公开（公告）日：2019-09-10

  Provided are an agent for the treatment and/or prophylaxis of a movement disorder, the agent for the treatment and/or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and/or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and/or prophylaxis wherein the movement disorder is a side effect of L-DOPA and/or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R1 represents aryl and the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof as an active ingredient.

  提供了一种用于治疗和/或预防运动障碍的制剂，该制剂用于治疗和/或预防运动障碍，其中运动障碍是锥体外系综合征，该制剂用于治疗和/或预防运动障碍，其中运动障碍是运动迟缓、步态障碍、肌张力障碍、运动障碍或迟发性运动障碍、治疗和/或预防运动障碍的药物，其中运动障碍是 L-DOPA 和/或多巴胺受体激动剂治疗的副作用等，每种药物都含有式（I）代表的噻唑衍生物，其中 R1 代表芳基等，R2 代表吡啶基等，或其药学上可接受的盐作为活性成分。
• Materials and methods relating to linkers for use in protein drug conjugates
  申请人：Iksuda Therapeutics Limited

  公开号：US11285220B2

  公开（公告）日：2022-03-29

  The present invention relates to protein drug conjugates, methods of manufacturing the same and their use in therapy. In particular, the present invention relates to protein drug conjugates comprising a globular protein, an improved linker and a drug for use in targeted drug delivery applications.

  本发明涉及蛋白质药物共轭物、制造方法及其在治疗中的应用。特别是，本发明涉及由球状蛋白质、改良连接体和药物组成的蛋白质药物共轭物，可用于靶向给药应用。