5-Hydroperoxy-6,8,11,14-eicosatetraenoic acid

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: 5-Hydroperoxy-6,8,11,14-eicosatetraenoic acid
• 英文别名: (6E,8E,11E,14E)-5-hydroperoxyicosa-6,8,11,14-tetraenoic acid
• 化学式: C₂₀H₃₂O₄
• 分子量: 336.5
• InChiKey: JNUUNUQHXIOFDA-SSTLJLGOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  24
• 可旋转键数：
  15
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  66.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  (5E,8E,11E,14E)-(114C)icosa-5,8,11,14-tetraenoic acid 生成 5-Hydroperoxy-6,8,11,14-eicosatetraenoic acid
  参考文献：
  名称：

  KIMURA, YOSHIYUKI;OKUDA, HIROMICHI;OKUDA, TAKUO;HATANO, TSUTOMU;ARICHI, S+, J. NATUR. PROD., 50,(1987) N 3, 392-399

  摘要：

  DOI：

文献信息

• 5-Lipoxygenase-Activating Protein Inhibitor
  申请人：SCHAAB Kevin Murray

  公开号：US20090291981A1

  公开（公告）日：2009-11-26

  Described herein is the FLAP inhibitor 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxy-pyridin-3-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid, or a pharmaceutically acceptable salt thereof. Also described are methods of preparing the FLAP inhibitor, or a pharmaceutically acceptable salt thereof, including solvates, and polymorphs thereof. Also described herein are pharmaceutical compositions suitable for administration to a mammal that include the FLAP inhibitor, or a pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.

  描述了一种FLAP抑制剂：3-[3-叔丁基硫基-1-[4-(6-乙氧基-吡啶-3-基)-苄基]-5-(5-甲基-吡啶-2-基甲氧基)-1H-吲哚-2-基]-2,2-二甲基丙酸，或其药用可接受盐。还描述了制备该FLAP抑制剂的方法，或其药用可接受盐，包括水合物和其多晶型。还描述了适合给予哺乳动物的药物组合物，包括FLAP抑制剂，或其药用可接受盐，以及使用此类药物组合物治疗呼吸系统疾病或疾病的方法，以及治疗其他白三烯依赖性或白三烯介导的条件或疾病的方法。
• Oxaindene derivatives and a process for preparing them as well as medicaments containing them and the use of them
  申请人：EGIS GYOGYSZERGYAR RT.

  公开号：EP0751137A1

  公开（公告）日：1997-01-02

  A subject-matter of the invention are oxaindene derivatives of general formula wherein R1represents a C1-4-alkyl, C1-4-alkoxy or C3-6-cycloalkyl group, R2stands for hydrogen or a C1-4-alkyl or C3-6-cycloalkyl group, R3represents hydrogen or a C1-4-alkyl, C1-4-alkoxy or benzyloxy group, Xmeans hydrogen, an aliphatic C1-4-acyl or benzoyl or naphthoyl group, optionally substituted by 1 or more nitro or C1-4-alkoxy group(s) or a group of formula in which latter R7stands for a C1-4-alkylene group    and R5 and R6each represents a C1-4-alkyl group    or R5 and R6together with the nitrogen atom to which they are attached form a piperidyl or morpholinyl group, A and Btogether form an ethylene or a vinylene group    and nis 1, 2 or 3, and their stereoisomers and their mixtures as well as acid addition salts of these compounds. Moreover there are provided for a process for preparing these compounds, medicaments containing them and the use of these compounds. They have a strong 5-lipoxygenase enzyme inhibiting activity.

  本发明的主题是一种一般公式的氧吲哚衍生物，其中R1代表C1-4-烷基、C1-4-烷氧基或C3-6-环烷基，R2代表氢或C1-4-烷基或C3-6-环烷基，R3代表氢或C1-4-烷基、C1-4-烷氧基或苄氧基，X代表氢、脂肪族C1-4-酰基或苯甲酰基或萘甲酰基，可选择地被1个或多个硝基或C1-4-烷氧基取代，或者是一个公式中的基团，其中R7代表C1-4-烷基烯基，R5和R6各自代表C1-4-烷基基团，或者R5和R6与它们连接的氮原子一起形成哌啶基或吗啡啉基，A和B一起形成乙烯或乙烯基基团，n为1、2或3，以及它们的立体异构体和它们的混合物，以及这些化合物的酸盐。此外还提供了一种制备这些化合物的方法，包含它们的药物以及这些化合物的用途。它们具有强大的5-脂氧酶酶抑制活性。
• 5-LIPOXYGENASE ACTIVATING PROTEIN (FLAP) INHIBITOR
  申请人：REWOLINSKI Melissa Virginia

  公开号：US20100075934A1

  公开（公告）日：2010-03-25

  Described herein are methods for the synthesis of 3-[5-(pyridin-2-ylmethoxy)-3-(2-methyl-2-propylthio)-1-[4-(2-methoxypyridin-5-yl)benzyl]-indol-2-yl]-2,2-dimethyl-propionic acid, pharmaceutically acceptable salts, pharmaceutically acceptable solvates thereof. Also described are pharmaceutical compositions suitable for oral administration to a mammal that include, as well as methods of using such oral pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.

  本文描述了一种合成3-[5-(吡啶-2-基甲氧基)-3-(2-甲基-2-丙基硫)-1-[4-(2-甲氧基吡啶-5-基)苯基]-吲哚-2-基]-2,2-二甲基丙酸及其药学上可接受的盐和可接受的溶剂的方法。还描述了适用于口服给哺乳动物的药物组合物，以及使用这种口服药物组合物治疗呼吸道疾病或疾病以及其他白三烯依赖性或白三烯介导的疾病或疾病的方法。
• 5-LIPOXYGENASE-ACTIVATING PROTEIN INHIBITOR
  申请人：Schaab Kevin Murray

  公开号：US20110160249A1

  公开（公告）日：2011-06-30

  A pharmaceutically acceptable salt comprising 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxy-pyridin-3-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionate as the anion and a cation selected from Na + , K + , Li + , Ca 2+ , NH 4 + , the protonated form of dicyclohexylamine, the protonated form of N-methyl-D-glucamine, the protonated form of tris(hydroxymethyl)methylamine, the protonated form of arginine, and the protonated form of lysine is disclosed, along with formulations and methods of using the same.

  本发明涉及一种药物可接受的盐，其包括3-[3-叔丁基磺酰基-1-[4-(6-乙氧基吡啶-3-基)-苄基]-5-(5-甲基吡啶-2-基甲氧基)-1H-吲哚-2-基]-2,2-二甲基丙酸根离子和从Na+、K+、Li+、Ca2+、NH4+、二环己基胺质子化形式、N-甲基-D-葡萄糖胺质子化形式、三羟甲基甲基胺质子化形式、精氨酸质子化形式和赖氨酸质子化形式中选择的阳离子，以及使用它们的制剂和方法。
• Pyridinylmethylamino-arylic acids
  申请人：THE UPJOHN COMPANY

  公开号：EP0114734A2

  公开（公告）日：1984-08-01

  Compounds of the formula and their pharmacologically acceptable acid addition salts, wherein Y1 is 0, S, NR or a bond, R2 is hydrogen or a substituent, and Q1 is optionally esterified or salified carboxyl, CH2OH, CH20H, CH2SH, NR or tetrazolyl, can have utility as thromboxane synthetase and/or 5-lipoxygenase inhibitors.

  式中的化合物及其药学上可接受的酸加成盐 及其药理学上可接受的酸加成盐，其中 Y1 是 0、S、NR 或键，R2 是氢或取代基，Q1 是任选酯化或盐化的羧基、CH2OH、CH20H、CH2SH、NR 或四唑基，可用作血栓素合成酶和/或 5-脂氧合酶抑制剂。