L-761,000 | 176045-83-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: L-761,000
• 英文别名: 4-(1-(4-Bromobenzyl)-5-methoxy-2-methyl-1H-indol-3-yl)-3-methylbutanoic acid；4-[1-[(4-bromophenyl)methyl]-5-methoxy-2-methylindol-3-yl]-3-methylbutanoic acid
• CAS: 176045-83-3
• 化学式: C₂₂H₂₄BrNO₃
• 分子量: 430.341
• InChiKey: AXFSURYONUFFTK-UHFFFAOYSA-N

物化性质

• 沸点：
  602.4±55.0 °C(Predicted)
• 密度：
  1.33±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  27
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  51.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  L-761,000 在 lithium hydroxide 、 双氧水 、 三甲基乙酰氯 、 双(三甲基硅烷基)氨基钾 作用下， 以 四氢呋喃 为溶剂， 生成 L-761,066
  参考文献：
  名称：

  Synthesis and biological evaluation of both enantiomers of L-761,000 as inhibitors of cyclooxygenase 1 and 2

  摘要：

  Both enantiomers of L-761,000 were prepared and evaluated for their cyclooxygenase activities.

  DOI：

  10.1016/0960-894x(96)00101-1
• 作为产物：
  描述：

  (1-(4-Bromobenzyl)-5-methoxy-2-methyl-1H-indol-3-yl) acetaldehyde 在 sodium hydroxide 、 copper(l) iodide 、 三甲基氯硅烷 作用下， 以 四氢呋喃 、 甲醇 、 乙醚 、 甲苯 为溶剂， 反应 2.0h， 生成 L-761,000
  参考文献：
  名称：

  Synthesis and biological evaluation of both enantiomers of L-761,000 as inhibitors of cyclooxygenase 1 and 2

  摘要：

  Both enantiomers of L-761,000 were prepared and evaluated for their cyclooxygenase activities.

  DOI：

  10.1016/0960-894x(96)00101-1

文献信息

• N-benzyl indol-3-yl butanoic acid derivatives as cyclooxygenase
  申请人：Merck Frosst Canada, Inc.

  公开号：US05639780A1

  公开（公告）日：1997-06-17

  The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

  这项发明涵盖了化合物I的新颖结构，可用于治疗环氧合酶-2介导的疾病。该发明还涵盖了用于治疗环氧合酶-2介导疾病的某些药物组合物，其中包括化合物I。
• Degradable implantable medical devices
  申请人：Elixir Medical Corporation

  公开号：US10350093B2

  公开（公告）日：2019-07-16

  Devices and methods are provided for an implantable medical device which is degradable over a clinically relevant period of time. The medical devices may have the form of implants, graft implants, vascular implants, non vascular implants, wound closure implants, sutures, drug delivery implants, biologic delivery implants, urinary tract implants, inter-uterine implants, organ implants, bone implants including bone plates, bone screws, dental implants, spinal disks, or the like. In preferred embodiments, the implantable medical device comprises an implantable luminal prosthesis, such as vascular and non-vascular stents and stents grafts.

  本发明提供了可在临床相关时间内降解的植入式医疗器械的设备和方法。这些医疗器械可以是植入物、移植植入物、血管植入物、非血管植入物、伤口闭合植入物、缝合线、给药植入物、生物给药植入物、泌尿道植入物、子宫间植入物、器官植入物、骨植入物（包括骨板、骨螺钉）、牙科植入物、椎间盘或类似物。在优选的实施方案中，植入式医疗器械包括植入式管腔假体，如血管和非血管支架和支架移植物。
• Combinations of an endothelin receptor antagonist and an antiepileptic compound having pain alleviating properties or analgesic
  申请人：——

  公开号：US20030232787A1

  公开（公告）日：2003-12-18

  The present invention is a novel combination effective for alleviating pain comprising a pain alleviating effective amount of an endothelin receptor antagonist or a pharmaceutically acceptable salt thereof and from 1 to 3 compounds independently selected from the group consisting of antiepileptic compounds having pain alleviating properties and analgesics, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising same. The administration of endothelin receptor antagonists in these novel combinations results in an improved reduction in the frequency and severity of pain. The incidence of unwanted side effects can be reduced by these novel combinations in comparison to using higher doses of a single agent treatment to achieve a similar therapeutic effect. The present invention is also directed to methods of using effective amounts of the novel combinations and pharmaceutical compositions thereof to treat pain in mammals, including a human.

  本发明是一种有效缓解疼痛的新型复方制剂，它包含缓解疼痛有效量的内皮素受体拮抗剂或其药学上可接受的盐，以及1至3种独立选自具有缓解疼痛特性的抗癫痫化合物和镇痛剂及其药学上可接受的盐组成的化合物，以及包含这些化合物的药物组合物。在这些新型组合物中施用内皮素受体拮抗剂，可有效降低疼痛的频率和严重程度。与使用较大剂量的单药治疗以达到类似的治疗效果相比，这些新型组合物可以降低不希望出现的副作用的发生率。本发明还涉及使用有效量的新型组合物及其药物组合物治疗哺乳动物（包括人类）疼痛的方法。
• DEGRADABLE IMPLANTABLE MEDICAL DEVICES
  申请人：Elixir Medical Corporation

  公开号：US20200188142A1

  公开（公告）日：2020-06-18

  Devices and methods are provided for an implantable medical device which is degradable over a clinically relevant period of time. The medical devices may have the form of implants, graft implants, vascular implants, non vascular implants, wound closure implants, sutures, drug delivery implants, biologic delivery implants, urinary tract implants, inter-uterine implants, organ implants, bone implants including bone plates, bone screws, dental implants, spinal disks, or the like. In preferred embodiments, the implantable medical device comprises an implantable luminal prosthesis, such as vascular and non-vascular stents and stents grafts.
• US5639780A
  申请人：——

  公开号：US5639780A

  公开（公告）日：1997-06-17