7-chlorobenzo[b]thiophene-2-carbaldehyde | 477735-67-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻吩类
• 英文名称: 7-chlorobenzo[b]thiophene-2-carbaldehyde
• 英文别名: 7-chloro-1-benzothiophene-2-carbaldehyde；7-Chlorobenzo[b]thiophene-2-carbaldehyde
• CAS: 477735-67-4
• 化学式: C₉H₅ClOS
• 分子量: 196.657
• InChiKey: AMLIAHVNZRIOKN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  45.3
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  7-chlorobenzo[b]thiophene-2-carbaldehyde 在 tris-(dibenzylideneacetone)dipalladium(0) caesium carbonate 、 1,3-双(2,4,6-三甲基苯基)氯化咪唑 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 甲苯 为溶剂， 反应 35.0h， 生成 N-(phenyl(7-phenyl-1-benzothiophen-2-yl)methyl)-3,4-dihydro-2H-1,5-benzodioxepine-7-sulfonamide
  参考文献：
  名称：

  [EN] BENZODIOXEPINE AND BENZODIOXINE COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES
  [FR] BENZODIOXÉPINE ET COMPOSÉS DE BENZODIOXINE QUI INTERAGISSENT AVEC LA PROTÉINE RÉGULATRICE DE LA GLUCOKINASE POUR LE TRAITEMENT DU DIABÈTE

  摘要：

  本发明涉及与葡萄糖激酶调节蛋白相互作用的式I或II的化合物，或其药学上可接受的盐。此外，本发明涉及使用这些化合物或其药学上可接受的盐治疗2型糖尿病和其他涉及葡萄糖激酶调节蛋白的疾病和/或症状的方法，以及含有这些化合物或其药学上可接受的盐的药物组合物。

  公开号：

  WO2012138776A1

文献信息

• [EN] SPIRO-OXADIAZOLINE COMPOUNDS AS AGONISTS OF α-7-NICOTINIC ACETYLCHOLINE RECEPTORS<br/>[FR] COMPOSÉS SPIRO-OXADIAZOLINE EN TANT QU'AGONISTES DES RÉCEPTEURS DE L'ACÉTYLCHOLINE Α-7 NICOTINIQUE
  申请人：FORUM PHARMACEUTICALS INC

  公开号：WO2015066371A1

  公开（公告）日：2015-05-07

  The present invention relates to novel spiro-oxadiazoline compounds that are suitable as agonists or partial agonists of a7-nAChR, and pharmaceutical compositions of the same, methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering a spiro-oxadiazoline cx7-nAChR agonist or partial agonist, to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.

  本发明涉及新型螺环-噁二唑啉化合物，适用作a7-nAChR的激动剂或部分激动剂，以及这些化合物和组合物的制备方法、药物组合物，以及在维持、治疗和/或改善认知功能的方法中使用这些化合物和组合物。具体而言，涉及向需要的患者（例如患有认知缺陷和/或希望增强认知功能的患者）施用螺环-噁二唑啉cx7-nAChR激动剂或部分激动剂的方法，以使其获益。
• DIHYDRO-OXAZOLOBENZODIAZEPINONE COMPOUNDS, A PROCESS FOR THERE PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
  申请人：LING István

  公开号：US20120232065A1

  公开（公告）日：2012-09-13

  Compounds of formula (I): wherein: R 1 represents a hydrogen atom or an alkyl group; R 2 represents an alkyl group; R 3 represents an aryl or heteroaryl group. Medicinal products containing the same which are useful in the treatment or prevention of psychiatric and neurological disorders characterised by cognitive deficits.

  式(I)的化合物：其中：R1代表氢原子或烷基基团；R2代表烷基基团；R3代表芳基或杂环芳基。含有该化合物的药物产品对治疗或预防以认知缺陷为特征的精神疾病和神经系统疾病具有用处。
• Tricyclic Compounds Useful as Inhibitors of Kinases
  申请人：Truchon Jean-Francois

  公开号：US20100048551A1

  公开（公告）日：2010-02-25

  The present invention provides inhibitors of kinases, specifically IκB kinases, JAK1, JAK2, JAK3 and TYK2. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting said kinase activity by administering the compound to a patient in need of treatment for myeloproliferative disorders, cancer or NF-κB-mediated diseases.

  本发明提供了激酶抑制剂，特别是IκB激酶、JAK1、JAK2、JAK3和TYK2的抑制剂。本发明还提供了包含这种抑制性化合物的组合物，并通过将该化合物用于需要治疗骨髓增生性疾病、癌症或NF-κB介导疾病的患者来抑制该激酶活性的方法。
• BENZODIOXEPINE AND BENZODIOXINE COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES
  申请人：Bartberger Michael David

  公开号：US20140155415A1

  公开（公告）日：2014-06-05

  The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

  本发明涉及公式I或II的化合物，或其药学上可接受的盐，其与葡萄糖激酶调节蛋白相互作用。此外，本发明涉及使用这些化合物或其药学上可接受的盐治疗2型糖尿病和其他涉及葡萄糖激酶调节蛋白的疾病和/或状况的方法，以及含有这些化合物或其药学上可接受的盐的制药组合物。
• OXAZOLIDONE COMPOUND, PREPARING METHOD AND APPLICATION THEREOF
  申请人：Shanghai Institute of Materia Medica, Chinese Academy of Sciences

  公开号：EP2947085A1

  公开（公告）日：2015-11-25

  The present invention relates to the field of a pharmaceutical compound, and more specifically, relates to a new oxazolidone compound, an enantiomer, a diastereoisomer and a raceme thereof, and a mixture thereof, and a pharmaceutically acceptable salt thereof, a preparation method thereof, an application thereof as a bioactive substance in a drug. The compound in the present invention has strong anticoagulant activity, does not affect the activity of thrombin, and can reduce the risk of hemorrhage. A pharmacokinetics experiment shows that the compound in the present invention further has good metabolic characteristics, and has a far better oral bioavailability than a positive contrastive agent rivaroxaban.

  本发明涉及一种药物化合物领域，更具体地说，涉及一种新的噁唑烷酮化合物、其对映体、非对映异构体和外消旋体及其混合物、其药学上可接受的盐、其制备方法、其作为生物活性物质在药物中的应用。本发明的化合物具有很强的抗凝血活性，不影响凝血酶的活性，可以降低大出血的风险。药代动力学实验表明，本发明化合物进一步具有良好的代谢特性，其口服生物利用度远远优于阳性对比剂利伐沙班。