Benzo[b]thiophene-2,3-diol | 191031-02-4

• 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: Benzo[b]thiophene-2,3-diol
• 英文别名: 1-benzothiophene-2,3-diol
• CAS: 191031-02-4
• 化学式: C₈H₆O₂S
• 分子量: 166.2
• InChiKey: NAIWWWQDHYGJOQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  68.7
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• [EN] Substituted urea-octatydroindols as antagonists of melanin concentrating hormone receptor 1 (MCH1R)<br/>[FR] UREE-OCTAHYDROINDOLES SUBSTITUES UTILISES EN TANT QU'ANTAGONISTES DU RECEPTEUR 1 DE L'HORMONE CONCENTRANT LA MELANINE (MCH1R)
  申请人：BIOVITRUM AB

  公开号：WO2005051381A1

  公开（公告）日：2005-06-09

  The invention relates to compounds of the general formula (I) wherein R0, R1, R2, R3, R4, R5, R6, R7, R8, R9, Ar, and X are as defined in the description, or a pharmaceutically acceptable salt, hydrates, geometrical isomers, racemates, tautomers, optical isomers, N-oxides and prodrug forms thereof. The compounds may be used for the treatment or prophylaxis of disorders related to the MCH1R receptor and for modulation of appetite. The invention also relates to such use as well as to pharmaceutical formulations comprising a compound of formula (I).

  该发明涉及通式（I）的化合物，其中R0、R1、R2、R3、R4、R5、R6、R7、R8、R9、Ar和X如描述中所定义，或其药学上可接受的盐、水合物、几何异构体、消旋体、互变异构体、光学异构体、N-氧化物及其前药形式。这些化合物可用于治疗或预防与MCH1R受体相关的疾病，并用于调节食欲。该发明还涉及该用途以及包含通式（I）化合物的药物配方。
• [EN] ANTITHROMBOTIC DIAMINES<br/>[FR] DIAMINES ANTITHROMBOTIQUES
  申请人：ELI LILLY AND COMPANY

  公开号：WO1997025033A1

  公开（公告）日：1997-07-17

  (EN) This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula (I) as defined herein. It also provides novel compounds of formula (I), processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula (I).(FR) La présente invention concerne l'utilisation, comme inhibiteurs de thrombine, inhibiteurs de coagulation et agents destinés aux désordres de la thromboembolie, de diamines de formule I telle qu'elle est définie dans la description. L'invention concerne aussi des composés nouveaux de formule I, des procédés et des produits intermédiaires pour leur préparation, et des formulations pharmaceutiques comprenant les composés nouveaux de formule I.

  该应用涉及使用公式（I）所定义的二胺作为凝血酶抑制剂、凝血抑制剂和血栓栓塞疾病药物的用途。它还提供了公式（I）的新化合物、其制备过程和中间体，以及包含公式（I）的新药物配方。
• An improved process for preparing 3-(4-aminoethoxy-benzoyl)benzo beta -thiophenes
  申请人：ELI LILLY AND COMPANY

  公开号：EP0693488A1

  公开（公告）日：1996-01-24

  The invention provides a process for preparing 6-alkoxy-3-(4-alkoxyphenyl)benzo[B]thiophenes in good yield on a manufacturing scale without generating a thick, potentially yield-reducing, paste. The invention also provides methods for converting a-(-alkoxyphenylthio)-4-alkoxyacetophenones into 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-aminoethoxy)-benzoyl]benzo[B]thiophenes via acylation of a dialkoxy benzo[B]thiophene. Each of these preparations relies on an intramolecular cyclization of a dialkoxy acetophenone derivative to yield a benzo[B]thiophene without generating a thick paste that lowers overall yields on a manufacturing scale.

  本发明提供了一种在生产规模上以良好收率制备 6-烷氧基-3-(4-烷氧基苯基)苯并[B]噻吩的工艺，而不会产生粘稠的、可能降低收率的糊状物。本发明还提供了通过二烷氧基苯并[B]噻吩的酰化将 a-(-烷氧基苯硫基)-4-烷氧基苯乙酮转化为 6-羟基-2-(4-羟基苯基)-3-[4-(2-氨基乙氧基)-苯甲酰基]苯并[B]噻吩的方法。上述每种制备方法都依赖于二烷氧基苯乙酮衍生物的分子内环化来生成苯并[B]噻吩，而不会生成浓稠的糊状物，从而降低了生产规模上的总体产量。
• Benzothiophenes with novel basic side chains
  申请人：ELI LILLY AND COMPANY

  公开号：EP0738725A2

  公开（公告）日：1996-10-23

  The present invention provides novel benzothiophene compounds.

  本发明提供了新型苯并噻吩化合物。
• FUSED THIOPHENE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1067128A1

  公开（公告）日：2001-01-10

  Fused thiophene derivatives represented by general formula (I) and interleukin-6 and/or interleukin-12 production inhibitors containing these derivatives as the active ingredient (in general formula (I), each symbol has the meaning as defined in the specification). The fused thiophene derivatives represented by general formula (I) are useful as preventives and/or remedies for various inflammatory diseases, sepsis, multiple myeloma, plasma cell leukemia, osteoporosis, cachexia, psoriasis, nephritis, renal cell cancer, Kaposi's sarcoma, chronic rheumatoid arthritis, hypergamma-globulinemia, Curschmann's disease, intraartial myxoma, diabetes, autoimmune diseases, hepatitis, multiple sclerosis, colon inflammation, graft-versus-host disease and infectious diseases.

  通式(I)代表的融合噻吩衍生物和含有这些衍生物作为活性成分的白细胞介素-6和/或白细胞介素-12产生抑制剂（在通式(I)中，每个符号的含义如说明书中所定义）。通式（I）所代表的融合噻吩衍生物可作为各种炎症、败血症、多发性骨髓瘤、浆细胞白血病、骨质疏松症、恶病质、牛皮癣、肾炎、肾细胞癌的预防和/或治疗药物、卡波西肉瘤、慢性类风湿性关节炎、高丙种球蛋白血症、库希曼病、关节内肌瘤、糖尿病、自身免疫性疾病、肝炎、多发性硬化症、结肠炎、移植物抗宿主病和传染病。