7,8-dihydro-1H-furo[2,3-g]indole | 170728-95-7

• 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: 7,8-dihydro-1H-furo[2,3-g]indole
• CAS: 170728-95-7
• 化学式: C₁₀H₉NO
• 分子量: 159.188
• InChiKey: JGMWGDRTILHBMM-UHFFFAOYSA-N

物化性质

• 沸点：
  342.2±11.0 °C(Predicted)
• 密度：
  1.304±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  25
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  7,8-dihydro-1H-furo[2,3-g]indole 在 盐酸 、 氢氧化钾 、 sodium cyanoborohydride 、 溶剂黄146 作用下， 以 1,4-二氧六环 、 甲醇 、 二氯甲烷 、 二甲基亚砜 为溶剂， 生成 VER-5384
  参考文献：
  名称：

  Indoline derivatives as 5-HT 2C receptor agonists

  摘要：

  A series of 1-(1-indolinyl)-2-propylamines was synthesised and evaluated as 5-HT2C receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for all of the compounds at 5-HT2 receptor subtypes are reported. A number of compounds were found to reduce food intake in rats after oral administration. (C) 2004 Published by Elsevier Ltd.

  DOI：

  10.1016/j.bmcl.2003.05.001
• 作为产物：
  描述：

  2,3-二氢-4-氨基苯并呋喃 在 盐酸 、 sodium tetrahydroborate 、 甲烷磺酸 、 三氟化硼乙醚 、 盐酸羟胺 、 sodium sulfate 作用下， 反应 3.0h， 生成 7,8-dihydro-1H-furo[2,3-g]indole
  参考文献：
  名称：

  Indoline derivatives as 5-HT 2C receptor agonists

  摘要：

  A series of 1-(1-indolinyl)-2-propylamines was synthesised and evaluated as 5-HT2C receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for all of the compounds at 5-HT2 receptor subtypes are reported. A number of compounds were found to reduce food intake in rats after oral administration. (C) 2004 Published by Elsevier Ltd.

  DOI：

  10.1016/j.bmcl.2003.05.001

文献信息

• Condensed indoline derivatives and their use as 5HT, in particular 5HT2c, receptor ligands
  申请人：Roffey Richard Anthony Jonathan

  公开号：US20050187282A1

  公开（公告）日：2005-08-25

  A chemical compound of formula (I) wherein R 1 and R 2 are independently selected from hydrogen and alkyl; R 3 is alkyl; R 4 and R 5 are selected from hydrogen and alkyl; R 6 and R 7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT 2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

  化学式（I）的化合物，其中R1和R2分别选自氢和烷基；R3是烷基；R4和R5选自氢和烷基；R6和R7分别选自氢、卤素、羟基、烷基、芳基、氨基、烷基氨基、二烷基氨基、烷氧基、芳氧基、烷基硫基、烷基亚砜基、硝基、氰基、羧酸酯基、羧酸芳酯基和羧基；A是一个含有一个或多个杂原子的5-或6元环，其中环A的原子除了与环A融合的苯环的不饱和碳原子外，可以是饱和的或不饱和的，以及其药学上可接受的盐、加合物和前药；以及其在治疗中的用途，特别是作为5HT受体的激动剂或拮抗剂，特别是5HT2C受体，例如在治疗中枢神经系统疾病；中枢神经系统损伤；心血管疾病；胃肠道疾病；尿崩症和睡眠呼吸暂停症，特别是用于肥胖症的治疗。
• [EN] SUBSTITUTED INDOLE COMPOUND DERIVATIVES AS DENGUE VIRAL REPLICATION INHIBITORS<br/>[FR] DÉRIVÉS D'INDOLE SUBSTITUÉS UTILISÉS EN TANT QU'INHIBITEURS DE RÉPLICATION DU VIRUS DE LA DENGUE
  申请人：JANSSEN PHARMACEUTICALS INC

  公开号：WO2017167952A1

  公开（公告）日：2017-10-05

  The present invention concerns substituted indole compounds, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.

  本发明涉及替代吲哚化合物，使用该化合物预防或治疗登革病毒感染的方法，并且还涉及将该化合物用作药物，更好地用作治疗或预防登革病毒感染的药物。本发明还涉及药物组合物或混合制剂的化合物，以及用作药物的组合物或制剂，更好地用于预防或治疗登革病毒感染。该发明还涉及化合物的制备过程。
• Indoline derivatives, method of preparation and use
  申请人：Glaxo Group Limited

  公开号：US05633276A1

  公开（公告）日：1997-05-27

  A compound of formula (I) ##STR1## wherein, R.sup.1 is hydrogen, halogen or C.sub.1-6 alkyl; R.sup.2 is a group of formula --CR.sup.3 R.sup.4 (CH.sub.2).sub.p NR.sup.5 COR.sup.6 ; R.sup.3, R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or C.sub.l-6 alkyl; R.sup.6 is C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; n is an integer of 2, 3 or 4; p is an integer of 1, 2, 3 or 4; and pharmaceutically acceptable salts and solvates thereof. A compound of formula (I) is useful in the treatment of conditions associated with a disturbed functioning of the melatonin system.

  公式（I）的化合物##STR1##其中，R.sup.1是氢、卤素或C.sub.1-6烷基；R.sup.2是公式--CR.sup.3R.sup.4(CH.sub.2).sub.pNR.sup.5COR.sup.6的基团；R.sup.3、R.sup.4和R.sup.5可以相同也可以不同，是氢或C.sub.l-6烷基；R.sup.6是C.sub.1-6烷基或C.sub.3-7环烷基；n是2、3或4的整数；p是1、2、3或4的整数；以及其药学上可接受的盐和溶剂合物。公式（I）的化合物在治疗与褪黑素系统功能紊乱相关的疾病方面具有用处。
• Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands
  申请人：Roffey Richard Anthony Jonathan

  公开号：US20050192334A1

  公开（公告）日：2005-09-01

  A chemical compound of formula (I) wherein R 1 and R 2 are independently selected from hydrogen and alkyl; R 3 is alkyl; R 4 and R 5 are selected from hydrogen and alkyl; R 6 and R 7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT 2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

  化学式为（I）的化合物，其中R1和R2独立地选自氢和烷基；R3为烷基；R4和R5选自氢和烷基；R6和R7独立地选自氢、卤素、羟基、烷基、芳基、氨基、烷基氨基、二烷基氨基、烷氧基、芳氧基、烷硫基、烷基亚砜基、硝基、氰基、羧基酯基、芳羧基酯基和羧基；A是一个5-或6-成员环，可选地含有一个或多个杂原子，其中环A的原子除与环A融合的苯环的不饱和碳原子外，均为饱和或不饱和的，以及其药学上可接受的盐、加合物和前药；以及其在治疗中的使用，特别是作为5HT受体的激动剂或拮抗剂，特别是5HT2C受体，例如在中枢神经系统疾病、中枢神经系统损伤、心血管疾病、胃肠道疾病、尿崩症和睡眠呼吸暂停症的治疗中，特别是用于肥胖症的治疗。
• Condensed indoline derivatives and their use as 5HT , in particular 5hHT2c, receptor ligands
  申请人：Roffey Anthony Jonathan Richard

  公开号：US20070105889A1

  公开（公告）日：2007-05-10

  A chemical compound of formula (I) wherein R 1 and R 2 are independently selected from hydrogen and alkyl; R 3 is alkyl; R 4 and R 5 are selected from hydrogen and alkyl; R 6 and R 7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT 2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

  化学式为（I）的化合物，其中R1和R2分别选自氢和烷基；R3为烷基；R4和R5选自氢和烷基；R6和R7分别选自氢、卤素、羟基、烷基、芳基、氨基、烷基氨基、二烷基氨基、烷氧基、芳氧基、烷硫基、烷基亚砜基、硝基、氰基、羧甲氧基、羧芳氧基和羧基；A是一个5或6元环，可以包含一个或多个杂原子，环A的原子，除了与环A融合的苯环的不饱和碳原子外，都是饱和或不饱和的，并且其药物可接受的盐、加成物和前药；以及其在治疗中的应用，特别是作为5HT受体的激动剂或拮抗剂，特别是5HT2C受体，例如在中枢神经系统疾病的治疗中；中枢神经系统损伤；心血管疾病；胃肠道疾病；尿崩症和睡眠呼吸暂停症，特别是用于肥胖症的治疗。