1H-indene-2-acetamide, 2,3-dihydro- | 146737-70-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: 1H-indene-2-acetamide, 2,3-dihydro-
• 英文别名: 2-(2,3-dihydro-1H-inden-2-yl)acetamide；(indan-2-yl)acetamide
• CAS: 146737-70-4
• 化学式: C₁₁H₁₃NO
• 分子量: 175.23
• InChiKey: FXUUGDVQYOENBV-UHFFFAOYSA-N

物化性质

• 沸点：
  383.7±11.0 °C(Predicted)
• 密度：
  1.116±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  43.1
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  1H-indene-2-acetamide, 2,3-dihydro- 在 sodium hydroxide 作用下， 以 四氢呋喃 、 水 为溶剂， 以100%的产率得到2-(2-aminoethyl)indane
  参考文献：
  名称：

  Indan derivative and thromboxane antagonist containing the same

  摘要：

  本发明涉及由式（1）表示的吲哚衍生物或其药学上可接受的盐：##STR1## [其中R.sup.1代表C1到C12烷基，苄基，苯乙烯基，萘基，可选择地取代的苯基或可选择地取代的噻吩基；R.sup.2代表羧基，C1到C4烷氧羰基，##STR2## Y代表--(CH.sub.2).sub.p--（其中p代表0到5的整数），--CO--(CH.sub.2).sub.q .about.，--CH(OH)--(CH.sub.2).sub.q .about.，（其中q代表1到4的整数，符号.about.代表与R.sup.2的连接），氧甲亚甲基或乙烯基；n代表1到4的整数]. 根据本发明的化合物强力拮抗血栓素A.sub.2的作用，因此对于治疗和预防由血栓素A.sub.2引起的疾病如血管病，血管痉挛，哮喘等非常有用。

  公开号：

  US05409956A1
• 作为产物：
  描述：

  2-茚酮 在 10percent Pd/C ammonium hydroxide 、 氢气 、 sodium hydride 、 氯化铵 作用下， 以 四氢呋喃 、 乙酸乙酯 为溶剂， 20.0~100.0 ℃ 、344.75 kPa 条件下， 反应 17.5h， 生成 1H-indene-2-acetamide, 2,3-dihydro-
  参考文献：
  名称：

  Diaminoindanes as Microsomal Triglyceride Transfer Protein Inhibitors

  摘要：

  The synthesis and biological activities of biarylamide-substituted diaminoindanes as microsomal triglyceride transfer protein (MTP) inhibitors are described. One of the more potent compounds, 8aR, inhibited both the secretion of apoB from Hep G2 cells and the MTP-mediated transfer of triglycerides between synthetic acceptor and donor liposomes with IC50 values of 0.7 and 70 nM, respectively. In normolipidemic rats and dogs, oral administration of 8aR dose-dependently reduced both plasma triglycerides and total cholesterol. Moreover, in rats and dogs, 8aR also prevented the postprandial rise in plasma triglycerides following a bolus administration of a fat load. Because MTP inhibitors decrease very low density lipoprotein assembly in the liver, the potential for hepatic lipid accumulation was evaluated. In normolipidemic rats, hepatic cholesterol and triglyceride contents were dose-dependently increased by 8aR. However, hepatic lipid accumulation resulted in negligible change in total liver weight and was reversible after withdrawal of the compound.

  DOI：

  10.1021/jm010294e

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.

  该发明涉及一种治疗高脂血症的药物，其活性成分为一种由通式（1）表示的茚衍生物：##STR1## 其中R.sup.1表示具有1-12个碳原子的烷基基团，苄基，苯乙烯基，萘基，可能被取代的苯基或可能被取代的噻吩基，R.sup.2表示羧基，具有1-4个碳原子的烷氧羰基，##STR2## Y表示--(CH.sub.2).sub.p --（p为0-5的整数），表示--CO--（CH.sub.2).sub.q .about.或--CH(OH)--（CH.sub.2).sub.q .about.（q为1-4的整数，.about.表示与R.sup.2结合），氧甲亚甲基基团或乙烯基团，n为1-4的整数，或其药学上可接受的盐，用于制备治疗高脂血症的药物的这种化合物的使用，以及通过充分利用这种化合物治疗高脂血症的方法。
• Indane modulators of glucocorticoid receptor, AP-1, and/or NF/kB activity and use thereof
  申请人：Duan Jingwu

  公开号：US20070185056A1

  公开（公告）日：2007-08-09

  Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is -A 1 QA 2 -; Q is a bond, —C(═O)—, —OC(O)—, —C(═O)NR 5 —, —SO p —, —SO p NR 5 —, —C(O)O—, —NR 5 C(O)—, —OC(O)NR 5 —, —NR 5 C(O)O—, —S(O) p NR 5 C(O)—, —C(O)NR 5 S(O) p — —NR 5 S(O) p —, or —NR 5 C(═O)NR 6 —. Y is selected from hydrogen, C 1-4 alkyl, OR 16 , substituted C 1-6 alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A 1 and A 2 are independently selected from a bond, C 1-3 alkylene, or C 1-3 alkenylene, and R 1 -R 11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.

  提供了一种新型的非甾体化合物，可用于治疗与糖皮质激素受体、AP-1和/或NF-κB活性调节相关的疾病，包括肥胖、糖尿病、炎症性和免疫性疾病，其具有以下结构的化学式（I）： 或其对映体、非对映体、药用可接受的盐或水合物，其中X为-A 1 QA 2 -；Q为键，—C(═O)—，—OC(O)—，—C(═O)NR 5 —，—SO p —，—SO p NR 5 —，—C(O)O—，—NR 5 C(O)—，—OC(O)NR 5 —，—NR 5 C(O)O—，—S(O) p NR 5 C(O)—，—C(O)NR 5 S(O) p —，—NR 5 S(O) p —，或—NR 5 C(═O)NR 6 —。Y从氢、C 1-4 烷基、OR 16 、取代的C 1-6 烷基、环烷基、芳基、杂环烷基和杂芳基中选择。A 1 和A 2 独立选择自键、C 1-3 烷基或C 1-3 烯基，R 1 -R 11 在此定义。还提供了包含所述化合物的药物组合物、组合物和治疗肥胖、糖尿病和炎症性或免疫相关疾病的方法。
• [EN] 2-(6-AMINO-PYRIDIN-3-YL)-2-HYDROXYETHYLAMINE DERIVATIVES AS BETA 2-ADRENOCEPTORS AGONISTS<br/>[FR] DERIVES DE 2-(6-AMINO-PYRIDINE-3-YL)-2-HYDROXYETHYLAMINE UTILISES COMME AGONISTES DES RECEPTEURS BETA 2-ADRENERGIQUES
  申请人：PFIZER LTD

  公开号：WO2004108676A1

  公开（公告）日：2004-12-16

  The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

  该发明涉及公式（1）的化合物，以及用于制备、用于制备的中间体、含有和用途的过程。根据本发明的化合物在许多疾病、紊乱和状况中特别有用，特别是在炎症性、过敏性和呼吸系统疾病、紊乱和状况中。
• Indan derivative and thromboxane antagonist containing the same
  申请人：Zeria Pharmaceutical Co., Ltd.

  公开号：US05409956A1

  公开（公告）日：1995-04-25

  The present invention relates to indan derivatives represented by the formula (1) or pharmaceutically acceptable salts thereof: ##STR1## [wherein R.sup.1 represents C1 to C12 alkyl, benzyl, styryl, naphthyl, optionally substituted phenyl or optionally substituted thienyl; R.sup.2 represents carboxyl, C1 to C4 alkoxycarbonyl, ##STR2## Y represents --(CH.sub.2).sub.p -- (wherein p represents an integer of 0 to 5), --CO--(CH.sub.2).sub.q .about., --CH(OH)--(CH.sub.2).sub.q .about., (wherein q represents an integer of 1 to 4, and the symbol .about. represents a linkage to R.sup.2), oxymethylene or ethylene; and n represents an integer of 1 to 4]. The compounds according to the present invention potently antagonize the action of thromboxane A.sub.2, and therefore useful for the treatment and prevention of diseases caused by thromboxane A.sub.2 such as angiosis, vasospasm, asthma and the like.

  本发明涉及由式（1）表示的吲哚衍生物或其药学上可接受的盐：##STR1## [其中R.sup.1代表C1到C12烷基，苄基，苯乙烯基，萘基，可选择地取代的苯基或可选择地取代的噻吩基；R.sup.2代表羧基，C1到C4烷氧羰基，##STR2## Y代表--(CH.sub.2).sub.p--（其中p代表0到5的整数），--CO--(CH.sub.2).sub.q .about.，--CH(OH)--(CH.sub.2).sub.q .about.，（其中q代表1到4的整数，符号.about.代表与R.sup.2的连接），氧甲亚甲基或乙烯基；n代表1到4的整数]. 根据本发明的化合物强力拮抗血栓素A.sub.2的作用，因此对于治疗和预防由血栓素A.sub.2引起的疾病如血管病，血管痉挛，哮喘等非常有用。
• INDANE MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
  申请人：Duan Jingwu

  公开号：US20090325961A1

  公开（公告）日：2009-12-31

  Novel non-steroidal compounds are provided that are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases having the structure of formula (I): or enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, where X is A 1 QA 2 -; Q is a bond, —C(═O)—, —OC(O)—, —C(═O)NR 5 —, —SO p —, —SO p NR 5 —, —C(O)O—, —NR 5 C(O)—, —OC(O)NR 5 —, —NR 5 C(O)O—, —S(O) p NR 5 C(O)—, —C(O)NR 5 S(O) p — —NR 5 S(O) p —, or —NR 5 C(═O)NR 6 —. Y is selected from hydrogen, C 1-6 alkyl, OR 16 , substituted C 1-6 alkyl, cycloalkyl, aryl, heterocyclo and heteroaryl. A 1 and A 2 are independently selected from a bond, C 1-3 alkylene, or C 1-3 alkenylene, and R 1 -R 11 are defined herein. Also provided are pharmaceutical compositions, combinations, and methods of treating obesity, diabetes and inflammatory- or immune-associated diseases comprising said compounds.

  本发明提供了一些新型非类固醇化合物，其可用于治疗与糖皮质激素受体、AP-1和/或NF-κB活性调节有关的疾病，包括肥胖症、糖尿病、炎症和免疫性疾病，其结构式为(I)：或其对映异构体、顺异构体或药学上可接受的盐或水合物，其中X为A1QA2-；Q为键，—C（═O）—，—OC（O）—，—C（═O）NR5—，—SOp—，—SOpNR5—，—C（O）O—，—NR5C（O）—，—OC（O）NR5—，—NR5C（O）O—，—S（O）pNR5C（O）—，—C（O）NR5S（O）p—，—NR5S（O）p—或—NR5C（═O）NR6—。Y选自氢、C1-6烷基、OR16、取代的C1-6烷基、环烷基、芳基、杂环烷基和杂环芳基。A1和A2独立地选自键、C1-3烷基或C1-3烯基，R1-R11在此定义。还提供了包含上述化合物的药物组合物和治疗肥胖症、糖尿病和炎症或免疫相关疾病的方法。