6-苄氧基-2-苯噁唑啉酮 | 158822-84-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶唑类
• 中文名称: 6-苄氧基-2-苯噁唑啉酮
• 中文别名: 6-苄氧基-2-苯并唑酮；6-苄氧基-2-苯并噁唑酮
• 英文名称: 6-(benzyloxy)benzo[d]oxazol-2(3H)-one
• 英文别名: 6-Benzyloxy-2-benzoxazolinone；6-phenylmethoxy-3H-1,3-benzoxazol-2-one
• CAS: 158822-84-5
• 化学式: C₁₄H₁₁NO₃
• mdl: MFCD07369766
• 分子量: 241.246
• InChiKey: JVUPJESJQYCFOB-UHFFFAOYSA-N

物化性质

• 熔点：
  181-186 °C(lit.)

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.071
• 拓扑面积：
  47.6
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 安全说明：
  S22,S24/25
• WGK Germany：
  3

反应信息

• 作为反应物：
  描述：

  6-苄氧基-2-苯噁唑啉酮 在 水 、 sodium hydroxide 作用下， 以 甲醇 为溶剂， 以49%的产率得到2-amino-5-(benzyloxy)phenol
  参考文献：
  名称：

  WO2019217591A5

  摘要：

  公开号：

  WO2019217591A5
• 作为产物：
  描述：

  6-羟基-2-苯并噁唑啉酮 、 溴甲苯 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 2.0h， 生成 6-苄氧基-2-苯噁唑啉酮
  参考文献：
  名称：

  [EN] AMINE-LINKED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN DEGRADATION
  [FR] DÉGRONIMÈRES DE C3-GLUTARIMIDE LIÉS À UNE AMINE POUR LA DÉGRADATION DE PROTÉINES CIBLES

  摘要：

  这项发明提供了胺连接的C3-戊二酰亚胺Degronimers和Degrons，用于治疗应用，如本文进一步描述的，以及它们的使用方法、组合物以及它们的制备方法。

  公开号：

  WO2017197051A1

文献信息

• HETEROARYLAMIDE LOWER CARBOXYLIC ACID DERIVATIVE
  申请人：Machinaga Nobuo

  公开号：US20090324581A1

  公开（公告）日：2009-12-31

  To provide a novel compound which has S1P receptor agonistic activity, exhibits excellent immunosuppressing effect, gives less adverse side effects, and can be orally administered. The invention provides a compound represented by general formula (I) (wherein A is a single bond, —O—, or —CH 2 —; R 1 represents a hydrogen atom or a C 1 -C 6 alkyl group, and V represents any one group selected from among the following groups (1) to (3): (1) -G 1 -, (2) -G 2 -N(R 2 )-G 3 -, and (3) a group represented by formula 2, wherein each of Z 1 and Z 2 represents a hydrogen atom or a C 1 -C 6 alkyl group, Z 3 represents a hydrogen or the like, Q represents —CH 2 —O— or the like, and Y represents a group represented by formula 3, a salt thereof, or a solvate thereof.

  提供一种新型化合物，具有S1P受体激动活性，表现出优异的免疫抑制效果，产生较少的不良副作用，并可口服。本发明提供一种由通式（I）表示的化合物（其中A是单键，-O-或-CH2-；R1表示氢原子或C1-C6烷基基团，V表示从以下组（1）至（3）中选择的任一组：（1）-G1-，（2）-G2-N（R2）-G3-，以及（3）由式2表示的组，其中Z1和Z2分别表示氢原子或C1-C6烷基基团，Z3表示氢或类似物，Q表示-CH2-O-或类似物，Y表示由式3表示的基团，其盐或溶剂化物。
• Anti-MSR1 antibodies and methods of use thereof
  申请人：REGENERON PHARMACEUTICALS, INC.

  公开号：US11377502B2

  公开（公告）日：2022-07-05

  Provided herein are antibodies and antigen-binding fragments that bind MSR1 and methods of use thereof. According to certain embodiments, the antibodies bind human MSR1 with high affinity. In certain embodiments, the antibodies bind MSR1 without blocking, or blocking less than 90%, of modified LDL binding to MSR1. In some embodiments, the antibodies bind cell surface expressed-MSR1 and are internalized. The antibodies of the invention may be fully human antibodies. The invention includes anti-MSR1 antibodies, or antigen-binding fragments thereof, conjugated to drugs or therapeutic compounds.

  本文提供了结合 MSR1 的抗体和抗原结合片段及其使用方法。根据某些实施方案，抗体以高亲和力结合人 MSR1。在某些实施方案中，抗体结合 MSR1 而不阻断或阻断少于 90% 的修饰低密度脂蛋白与 MSR1 的结合。在某些实施方案中，抗体与细胞表面表达的 MSR1 结合并被内化。本发明的抗体可以是全人源抗体。本发明包括与药物或治疗化合物结合的抗MSR1抗体或其抗原结合片段。
• WO2019217591A5
  申请人：——

  公开号：WO2019217591A5

  公开（公告）日：2022-06-01
• Structure-activity relationships of benzoxazolinones with respect to auxin-induced growth and auxin-binding protein
  作者：Masako Hoshi-Sakoda、Kenji Usui、Kozo Ishizuka、Seiji Kosemura、Shosuke Yamamura、Koji Hasegawa

  DOI：10.1016/0031-9422(94)85050-x

  日期：——

  The structure-activity relationships of the naturally occurring auxin-inhibiting substance, 6-methoxy-2-benzoxazolinone, isolated from maize shoots, and its artificial analogues with respect to auxin activity and membrane-bound auxin-binding protein, were studied. 6-Isobutoxy-2-benzoxazolinone strongly inhibited auxin (1-naphthylacetic acid, NAA)-induced growth of etiolated maize coleoptile segments. 6-Isopropoxy-2-benzoxazolinone, 6-ethoxy-2-benzoxazolinone and 6-methoxy-2-benzoxazolinone showed significant inhibitory activity. However, 2-benzoxazolinone and 6-benzyloxy-2-benzoxazolinone did not inhibit auxin-induced growth. On the basis of these data, it seemed reasonable to assume that the auxin-inhibitory activity was enhanced by increasing the side chain length at position C-6 on the 2-benzoxazolinone, although the attachment of a ring at C-6 destroyed activity. Competition by benzoxazolinones with an alkoxy group at C-6 with H-3-NAA at auxin-binding protein(s) isolated from endoplasmic reticulum (ER) membrane of maize shoots showed a positive correlation with their physiological effects. However, since the inhibitory activity of the benzoxazolinones for auxin-receptor(s) binding was small compared with their physiological activity, the benzoxazolinones may contribute to inhibition of auxin-induced growth through interference with other auxin-receptors.
• AMINE-LINKED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN DEGRADATION
  申请人：C4 Therapeutics, Inc.

  公开号：EP3455219A1

  公开（公告）日：2019-03-20