卡洛芬杂质H(EP) | 92841-23-1

• 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
• 中文名称: 卡洛芬杂质H(EP)
• 英文名称: 6-chloro-2-ethyl-9H-carbazole
• CAS: 92841-23-1
• 化学式: C₁₄H₁₂ClN
• 分子量: 229.709
• InChiKey: MVPBNCKQNLUXLA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  15.8
• 氢给体数：
  1
• 氢受体数：
  0

反应信息

• 作为产物：
  描述：

  卡洛芬 在 potassium phosphate 、 1,3,7,9-tetrapropyl-1H,9H-pyrimido[5,4-g]pteridine-2,4,6,8-tetraone 、 水 作用下， 以 乙腈 为溶剂， 反应 24.0h， 以58%的产率得到卡洛芬杂质H(EP)
  参考文献：
  名称：

  药物相关和天然脂肪族羧酸的光介导加氢和氘代脱羧作用

  摘要：

  在此，我们报道了由有机嘧啶蝶啶光氧化还原催化剂催化的不同伯、仲和叔羧酸的光介导加氢和氘代脱羧反应。通过实验统计设计 (DoE) 优化反应。在优化的反应条件下，实现了市售非甾体抗炎药（NSAID）片剂和克级的转化。本申请的范围包括伯、仲和叔脂肪族生物活性羧酸。通过使用D 2 O作为廉价的氘源，实现了高达95%的氘掺入。讨论了敏感性评估以及有助于阐明反应机制的实验。

  DOI：

  10.1021/acs.joc.2c01664

文献信息

• [EN] GAMMA SECRETASE MODULATORS<br/>[FR] MODULATEURS DE LA GAMMA-SÉCRÉTASE
  申请人：AMGEN INC

  公开号：WO2009075874A1

  公开（公告）日：2009-06-18

  The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

  本发明提供了作为γ-分泌酶调节剂的化合物，因此可用于治疗可通过调节γ-分泌酶治疗的疾病，如阿尔茨海默病。还提供了含有此类化合物的药物组合物以及制备此类化合物的过程。
• NITROSATED NONSTEROIDAL ANTIINFLAMMATORY COMPOUNDS, COMPOSITIONS AND METHODS OF USE
  申请人：EARL Richard A.

  公开号：US20100093671A1

  公开（公告）日：2010-04-15

  The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.

  该发明描述了新型亚硝酰化非甾体抗炎药（NSAIDs）及其药学上可接受的盐，并且描述了至少包含一种亚硝酰化NSAID和可选的至少一种化合物的新型组合物，该化合物捐赠、转移或释放一氧化氮，刺激内源性一氧化氮的合成，提高内源性内皮源性松弛因子的水平或是一氧化氮合酶的底物，并/或至少包含一种治疗剂。该发明还提供了至少包含一种亚硝酰化NSAID和至少一种化合物的新型组合物，该化合物捐赠、转移或释放一氧化氮，提高内源性内皮源性松弛因子的水平，刺激内源性一氧化氮的合成或是一氧化氮合酶的底物，并/或至少包含一种治疗剂。该发明还提供了至少包含一种亚硝酰化NSAID，可选的至少一种一氧化氮供体和/或至少一种治疗剂的新型试剂盒。该发明还提供了治疗炎症、疼痛和发热的方法；治疗胃肠道疾病的方法；促进伤口愈合的方法；治疗和/或预防使用非甾体抗炎化合物导致的胃肠道、肾脏和/或呼吸道毒性的方法；治疗炎症性疾病状态和/或疾病的方法；以及治疗和/或预防眼科疾病和/或疾病的方法。
• ESTER-SUBSTITUTED THIENOTRIAZOLODIAZEPINE COMPOUNDS AND THEIR MEDICINAL USE
  申请人：Yoshitomi Pharmaceutical Industries, Ltd.

  公开号：EP0316456A1

  公开（公告）日：1989-05-24

  Ester-substituted thienotriazolodiazepine compoundsre- presented by general formula (1) (wherein Ar represents pyridyl, phenyl or phenyl having one to three same or different substituents R1 and R3, which may be the same or different, each represents hydrogen or C1-4 alkyl, R2 represents hydrogen, C1-4 alkyl ortrifluoromethyl, and R represents C1-18 straight or branched-chain alkyl, C2-18 straight or branched-chain alkenyl, aryl, aryl having one to three same or different substituents, aralkyl, aralkyl having one or more same or different substituents on the aromatic ring or alkyl chain, aralkyl fused with a heterocyclic ring, aralkenyl, aralkenyl having one to three same or different substituents, heteroarylalkyl, or optionally substituted indenylalkyl), pharmaceutically acceptable salts thereof, and their medicinal use are disclosed. These compounds are useful as drugs for treating various diseases induced by thrombocyte activator.

  由通式(1)表示的酯取代的噻吩三唑并二氮杂卓化合物 (其中 Ar 代表吡啶基、苯基或具有一至三个相同或不同取代基的苯基，R1 和 R3 可以相同或不同，各自代表氢或 C1-4 烷基，R2 代表氢、C1-4 烷基或三氟甲基，R 代表 C1-18 直链或支链烷基、C2-18 直链或支链烯基、芳基、具有一至三个相同或不同取代基的芳基、烷基、在芳香环或烷基链上具有一个或多个相同或不同取代基的烷基、与杂环融合的烷基、芳烯基、具有一至三个相同或不同取代基的芳烯基、杂芳烷基或任选取代的茚基烷基）、其药学上可接受的盐及其药用用途均已公开。这些化合物可作为治疗血小板活化剂诱发的各种疾病的药物。
• US5028603A
  申请人：——

  公开号：US5028603A

  公开（公告）日：1991-07-02
• US8304409B2
  申请人：——

  公开号：US8304409B2

  公开（公告）日：2012-11-06