4-{2-[(4-Chloro-benzenesulfonylamino)-methyl]-indan-5-yl}-4-oxo-butyric acid | 146737-52-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-{2-[(4-Chloro-benzenesulfonylamino)-methyl]-indan-5-yl}-4-oxo-butyric acid
• 英文别名: 4-[2-[(4-Chlorophenyl)sulfonylaminomethyl]indan-5-yl]-4-oxobutanoic Acid；4-[2-[[(4-chlorophenyl)sulfonylamino]methyl]-2,3-dihydro-1H-inden-5-yl]-4-oxobutanoic acid
• CAS: 146737-52-2
• 化学式: C₂₀H₂₀ClNO₅S
• 分子量: 421.901
• InChiKey: OBDPFCXJMWZWMZ-UHFFFAOYSA-N

物化性质

• 沸点：
  664.6±65.0 °C(predicted)
• 密度：
  1.380±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  28
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  109
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  4-{2-[(4-Chloro-benzenesulfonylamino)-methyl]-indan-5-yl}-4-oxo-butyric acid 在 盐酸 、 sodium hydroxide 、 mercury dichloride 、 锌 作用下， 生成 4-{2-[(4-Chloro-benzenesulfonylamino)-methyl]-indan-5-yl}-butyric acid
  参考文献：
  名称：

  Synthesis and thromboxane A2 antagonistic activity of indane derivatives

  摘要：

  A new series of indane derivatives were prepared and evaluated for their thromboxane A(2) (TXA(2), 1) antagonistic activity. Among these compounds, 24a (Z-335) was found to be a potent TXA(2) antagonist in oral administration. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(99)00014-1
• 作为产物：
  描述：

  2-茚满基乙酸 在 钯 三氯化铝 、 二苯基膦叠氮化物 、 氢气 、 potassium carbonate 、 三乙胺 作用下， 生成 4-{2-[(4-Chloro-benzenesulfonylamino)-methyl]-indan-5-yl}-4-oxo-butyric acid
  参考文献：
  名称：

  Synthesis and thromboxane A2 antagonistic activity of indane derivatives

  摘要：

  A new series of indane derivatives were prepared and evaluated for their thromboxane A(2) (TXA(2), 1) antagonistic activity. Among these compounds, 24a (Z-335) was found to be a potent TXA(2) antagonist in oral administration. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(99)00014-1

文献信息

• Remedy for hyperlipidemia
  申请人：Zeria Pharmaceutical Co., Ltd.

  公开号：US05750524A1

  公开（公告）日：1998-05-12

  The invention relates to a remedy for hyperlipidemia, which comprises, as an active ingredient, an indane derivative represented by the general formula (1): ##STR1## wherein R.sup.1 means an alkyl group having 1-12 carbon atoms, a benzyl group, a styryl group, a naphthyl group, a phenyl group which may be substituted, or a thienyl group which may be substituted, R.sup.2 denotes a carboxyl group, an alkoxycarbonyl group having 1-4 carbon atoms, ##STR2## Y is a group represented by --(CH.sub.2).sub.p -- (p stands for an integer of 0-5), a group represented by --CO--(CH.sub.2).sub.q .about. or --CH(OH)--(CH.sub.2).sub.q .about. (q stands for an integer of 1-4, and .about. means bonding to R.sup.2), an oxymethylene group, or a vinylene group, and n stands for an integer of 1-4, or a pharmaceutically acceptable salt thereof, to use of this compound for the preparation of a remedy for hyperlipidemia, and to a method for treating hyperlipidemia by making good use of this compound.

  本发明涉及一种治疗高脂血症的药物，其包括作为活性成分的吲哚烷衍生物，其通式表示为（1）：其中R1表示具有1-12个碳原子的烷基，苯甲基，苯乙烯基，萘基，取代的苯基或取代的噻吩基，R2表示羧基，具有1-4个碳原子的烷氧羰基，苯氧羰基，氧代亚甲基，乙烯基，Y表示由--（CH2）p--（p为0-5的整数），由--CO--（CH2）q--或--CH（OH）--（CH2）q--（q为1-4的整数，并且. 。表示与R2结合），n表示1-4的整数，或其药学上可接受的盐，以及使用该化合物制备治疗高脂血症的药物的用途和利用该化合物治疗高脂血症的方法。
• HYPERLIPEMIA REMEDY
  申请人：ZERIA PHARMACEUTICAL CO., LTD.

  公开号：EP0773019A1

  公开（公告）日：1997-05-14

  The invention relates to a remedy for hyperlipidemia, which comprises, as an active ingredient, an indane derivative represented by the general formula (1): wherein R1 means an alkyl group having 1-12 carbon atoms, a benzyl group, a styryl group, a naphthyl group, a phenyl group which may be substituted, or a thienyl group which may be substituted, R2 denotes a carboxyl group, an alkoxycarbonyl group having 1-4 carbon atoms, Y is a group represented by -(CH2)p- (p stands for an integer of 0-5), a group represented by -CO-(CH2)q∼ or -CH(OH)-(CH2)q∼ (q stands for an integer of 1-4, and ∼ means bonding to R2), an oxymethylene group, or a vinylene group, and n stands for an integer of 1-4, or a pharmaceutically acceptable salt thereof, to use of this compound for the preparation of a remedy for hyperlipidemia, and to a method for treating hyperlipidemia by making good use of this compound.

  本发明涉及一种治疗高脂血症的药物，其活性成分包括通式(1)代表的茚满衍生物： 其中 R1 表示具有 1-12 个碳原子的烷基、苄基、苯乙烯基、萘基、可被取代的苯基或可被取代的噻吩基，R2 表示羧基、具有 1-4 个碳原子的烷氧羰基、 Y 是-(CH2)p-（p 代表 0-5 的整数）、-CO-(CH2)q∼ 或 -CH(OH)-(CH2)q∼（q 代表 1-4 的整数，∼ 表示与 R2 键合）、氧亚甲基或亚乙烯基所代表的基团、或其药学上可接受的盐，利用该化合物制备治疗高脂血症的药物，以及利用该化合物治疗高脂血症的方法。
• Synthesis and thromboxane A2 antagonistic activity of indane derivatives
  作者：Katsuo Shinozaki、Hiroki Sato、Takeo Iwakuma、Ryuichi Sato、Tadashi Kurimoto、Kiyoshi Yoshida

  DOI：10.1016/s0960-894x(99)00014-1

  日期：1999.2

  A new series of indane derivatives were prepared and evaluated for their thromboxane A(2) (TXA(2), 1) antagonistic activity. Among these compounds, 24a (Z-335) was found to be a potent TXA(2) antagonist in oral administration. (C) 1999 Elsevier Science Ltd. All rights reserved.