(2R-反式)-2-(3,4-二羟基苯基)-3,4-二氢-3-甲氧基-2H-1-苯并吡喃-5,7-二醇 | 65350-86-9

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 黄酮类化合物
• 中文名称: (2R-反式)-2-(3,4-二羟基苯基)-3,4-二氢-3-甲氧基-2H-1-苯并吡喃-5,7-二醇
• 中文别名: 美西达醇
• 英文名称: Meciadanol
• 英文别名: (2R,3S)-2-(3,4-dihydroxyphenyl)-3-methoxy-3,4-dihydro-2H-chromene-5,7-diol
• CAS: 65350-86-9
• 化学式: C₁₆H₁₆O₆
• 分子量: 304.29
• InChiKey: PDHSAQOQVUXZGQ-JKSUJKDBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  99.4
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
  申请人：Scaramuzzino, Giovanni

  公开号：EP1336602A1

  公开（公告）日：2003-08-20

  New pharmaceutical compounds of general formula (I): F-(X)q where q is an integer from 1 to 5, preferably 1; -F is chosen among drugs described in the text, -X is chosen among 4 groups -M, -T, -V and -Y as described in the text. The compounds of general formula (I) are nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without hypotensive side effects and for this reason they are useful for the preparation of medicines for prevention and treatment of inflammatory, ischemic, degenerative and proliferative diseases of musculoskeletal, tegumental, respiratory, gastrointestinal, genito-urinary and central nervous systems.

  通式（I）的新药物化合物：F-（X）q，其中q是1到5的整数，最好是1；-F是在文本中描述的药物中选择的，-X是在文本中描述的4个组-M，-T，-V和-Y中选择的。通式（I）的化合物是硝酸盐前药，可以在体内以受控和选择性的方式释放一氧化氮，而不会产生降压副作用，因此它们非常适用于制备用于预防和治疗肌肉骨骼，皮肤，呼吸，消化，泌尿和中枢神经系统的炎症，缺血，退行性和增生性疾病的药物。
• [EN] POLYPHENOL-PEPTIDE CONJUGATES FOR NUCLEAR-TARGETED DELIVERY<br/>[FR] CONJUGUÉS POLYPHÉNOL-PEPTIDE POUR L'ADMINISTRATION CIBLANT LE NOYAU
  申请人：UNIV WIEN

  公开号：WO2020136240A1

  公开（公告）日：2020-07-02

  The present invention relates to a polyphenol-peptide conjugate composed of: (i) a peptide comprising the amino acid sequence Arg-Arg-X1-Leu, wherein X1 refers to one or two hydrophobic amino acids selected independently from lie, Leu, Val, Phe, Trp, and Met; (ii) at least one polyphenol which is covalently bound to the peptide; and (iii) optionally at least one cargo which, if present, is covalently bound to the peptide. The polyphenol-peptide conjugate can be encapsulated with silica. The invention thus also provides silica particles comprising the polyphenol-peptide conjugate encapsulated by a silica shell. The silica particles allow the efficient cellular uptake and targeted delivery of the polyphenol-peptide conjugate into the cell nucleus, and can therefore advantageously be used for nuclear-targeted gene or drug delivery.

  本发明涉及一种由以下组成的多酚-肽共轭物：（i）包括氨基酸序列Arg-Arg-X1-Leu的肽，其中X1是从lie、Leu、Val、Phe、Trp和Met中独立选择的一个或两个疏水性氨基酸；（ii）至少一种共价结合到肽上的多酚；以及（iii）可选地，至少一种共价结合到肽上的载荷。多酚-肽共轭物可以被硅化物封装。因此，本发明还提供了由硅壳封装的多酚-肽共轭物的硅颗粒。硅颗粒能够有效地被细胞摄取并定向传递到细胞核中，因此可以有利地用于核靶向基因或药物传递。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• HAIR DEFORMATION TREATMENT AGENT
  申请人：Kao Corporation

  公开号：EP3228303A1

  公开（公告）日：2017-10-11

  An agent for hair deforming treatment comprising the following components (A) to (C): (A) glyoxylic acid or a hydrate or salt thereof, (B) a compound represented by the following formula (1): wherein R1 represents H or a methyl group, X represents H, OH, or a methoxy group, Y represents H, O, OH, or a methoxy group, Z represents H, an alkyl group, etc., Rx represents H, O, a methoxy group, etc., Ry represents H, OH, an aromatic hydrocarbon group, etc., and the dashed line optionally represents a double bond, and (C) water, wherein the molar ratio of the content of the component (B) to the content of the component (A), (B)/(A), is 0.01 or more and 5 or less.

  一种用于头发变形处理的制剂，由以下成分(A)至(C)组成： (A) 乙醛酸或其水合物或盐、 (B) 下式(1)所代表的化合物： 其中 R1 代表 H 或甲基，X 代表 H、OH 或甲氧基，Y 代表 H、O、OH 或甲氧基，Z 代表 H、烷基等，Rx 代表 H、O、甲氧基等，Ry 代表 H、OH、芳香烃基等，虚线可选代表双键，以及 (C) 水、 其中，组分（B）的含量与组分（A）的含量的摩尔比，(B)/(A)，为 0.01 或以上，5 或以下。
• POLYPHENOL-PEPTIDE CONJUGATES FOR NUCLEAR-TARGETED DELIVERY
  申请人：Universität Wien

  公开号：EP3673920A1

  公开（公告）日：2020-07-01

  The present invention relates to a polyphenol-peptide conjugate composed of: (i) a peptide comprising the amino acid sequence Arg-Arg-X1-Leu, wherein X1 refers to one or two hydrophobic amino acids selected independently from lie, Leu, Val, Phe, Trp, and Met; (ii) at least one polyphenol which is covalently bound to the peptide; and (iii) optionally at least one cargo which, if present, is covalently bound to the peptide. The polyphenol-peptide conjugate can be encapsulated with silica. The invention thus also provides silica particles comprising the polyphenol-peptide conjugate encapsulated by a silica shell. The silica particles allow the efficient cellular uptake and targeted delivery of the polyphenol-peptide conjugate into the cell nucleus, and can therefore advantageously be used for nuclear-targeted gene or drug delivery.

  本发明涉及一种多酚-多肽共轭物，其组成包括：(i) 包含 Arg-Arg-X1-Leu 氨基酸序列的多肽，其中 X1 指从 lie、Leu、Val、Phe、Trp 和 Met 中独立选出的一个或两个疏水氨基酸；(ii) 至少一种与多肽共价结合的多酚；(iii) 可选的至少一种与多肽共价结合的货物（如果存在）。多酚-肽共轭物可以用二氧化硅封装。因此，本发明还提供了由二氧化硅外壳封装的多酚肽共轭物组成的二氧化硅颗粒。这种二氧化硅颗粒可使多酚多肽共轭物有效地被细胞吸收并定向递送到细胞核中，因此可用于核靶向基因或药物递送。