1-[3-(Indan-2-yloxy)-4-methoxyphenyl]ethanone | 115898-73-2

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-[3-(Indan-2-yloxy)-4-methoxyphenyl]ethanone
• 英文别名: 3-(2-indanyloxy)-4-methoxyacetophenone；1-{3-[(2,3-Dihydro-1H-inden-2-yl)oxy]-4-methoxyphenyl}ethan-1-one；1-[3-(2,3-dihydro-1H-inden-2-yloxy)-4-methoxyphenyl]ethanone
• CAS: 115898-73-2
• 化学式: C₁₈H₁₈O₃
• 分子量: 282.339
• InChiKey: YDTATDYYXUTOEQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  35.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-[3-(Indan-2-yloxy)-4-methoxyphenyl]ethanone 、 碳酸二乙酯 在 sodium hydride 作用下， 反应 1.0h， 生成 ethyl 3-(3-(2-indanyloxy)-4-methoxyphenyl)-3-oxopropanoate
  参考文献：
  名称：

  EP2172458

  摘要：

  公开号：

文献信息

• Pyrazolone Derivative
  申请人：Gomi Noriaki

  公开号：US20100324091A1

  公开（公告）日：2010-12-23

  A pyrazolone derivative represented by formula (I) below: wherein R 1 to R 3 are the same as defined in claims; or an optical isomer, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof is provided. The novel pyrazolone derivative according to the present invention has a PAI-1 production inhibitory activity, a tissue fibrosis inhibitory activity, and a fibrolytic activity, and is effective for preventing and/or treating tissue fibrotic diseases (lung fibrosis, kidney fibrosis, etc.) and diseases of which a pathological thrombus becomes the cause, such as ischemic cardiac diseases (cardiac infarction and angina pectoris), atrial thrombus, lung embolism, deep thrombophlebitis, disseminated intravascular clotting, ischemic brain diseases (brain infarction, brain hemorrhage), and arterial sclerosis. In addition, a pharmaceutical agent for preventing and/or treating the disease conditions or the symptoms mediated by plasminogen activator inhibitor-1, comprising the novel pyrazolone derivative according to the present invention is also provided.

  本发明提供了一种由以下式（I）表示的吡唑酮衍生物：其中，R1至R3与权利要求中定义的相同；或其光学异构体、药学上可接受的盐或其水合物或溶剂化物。根据本发明，这种新型的吡唑酮衍生物具有PAI-1生产抑制活性、组织纤维化抑制活性和纤溶活性，对于预防和/或治疗组织纤维化疾病（肺纤维化、肾脏纤维化等）以及由病理性血栓引起的疾病（缺血性心脏病（心肌梗死和心绞痛）、心房血栓、肺栓塞、深静脉血栓性炎症、弥漫性血管内凝血、缺血性脑疾病（脑梗死、脑出血）和动脉硬化）非常有效。此外，本发明还提供了一种用于预防和/或治疗由纤溶酶原激活剂抑制物-1介导的疾病状况或症状的药物制剂，其包括根据本发明的新型吡唑酮衍生物。
• 2-PHENYLMORPHOLIN-5-ONE DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
  申请人：Nikken Chemicals Company, Limited

  公开号：EP0924204A1

  公开（公告）日：1999-06-23

  A 2-phenylmorpholin-5-one derivative having the formula (I): wherein R1 represents a C1 to C8 alkyl group, a C3 to C7 cycloalkyl group or an indanyl group, R2 represents a C1 to C4 alkyl group, R3 represents a hydrogen atom, a C1 to C5 alkyl group, etc., R4 represents a hydrogen atom, a C1 to C6 alkyl group, etc., R5, R6 represent a hydrogen atom, a C1 to C5 alkyl group, etc., an optical isomer thereof or a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof and a pharmaceutical composition containing the same. The above compound has a strong type IV phosphodiesterase (PDE) inhibitory activity and has bronchodilater and antiinflammatory effects.

  具有式(I)的2-苯基吗啉-5-酮衍生物： 其中 R1 代表 C1 至 C8 烷基、C3 至 C7 环烷基或茚基，R2 代表 C1 至 C4 烷基，R3 代表氢原子、C1 至 C5 烷基等，R4 代表氢原子、C1 至 C6 烷基等，R5、R6 代表氢原子、C1 至 C5 烷基等、 其光学异构体或其药理学上可接受的盐，或其水合物或溶液，以及含有上述物质的药物组合物。 上述化合物具有很强的 IV 型磷酸二酯酶（PDE）抑制活性，并具有支气管扩张和抗炎作用。
• 6-PHENYLTETRAHYDRO-1,3-OXAZIN-2-ONE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME
  申请人：Nikken Chemicals Company, Limited

  公开号：EP0928789A1

  公开（公告）日：1999-07-14

  A 6-phenyltetrahydro-1,3-oxazin-2-one derivative having the formula (I): wherein, R1 is an unsubstituted or substituted C1 to C8 alkyl group; an unsubstituted or substituted C3 to C7 cycloalkyl group;, etc., R2 is a C1 to C4 alkyl group, R3 is H; an unsubstituted or substituted C1 to C5 alkyl group; etc., R4 is H; an unsubstituted or substituted C1 to C6 alkyl group, and R5 and R6 are independently a hydrogen atom; an unsubstituted or substituted C1 to C5 alkyl group; etc. an optical isomer thereof, or a pharmacologically acceptable salt thereof, or a hydrate or a solvate thereof and pharmaceutical compositions containing the same, in particular a drug for the prevention or treatment of inflammatory diseases and a drug for asthma. The above 6-phenyltetrahydro-1,3-oxazin-2-one derivative has a strong type IV PDE inhibitory activity and has a bronchiodilator and antiinflammatory effects.

  一种具有式（I）的 6-苯基四氢-1,3-恶嗪-2-酮衍生物： 其中，R1 是未取代或取代的 C1 至 C8 烷基；未取代或取代的 C3 至 C7 环烷基；等等，R2 是 C1 至 C4 烷基，R3 是 H；未取代或取代的 C1 至 C5 烷基；等等、R4为H；未取代或取代的C1至C6烷基，R5和R6独立地为氢原子；未取代或取代的C1至C5烷基；等，其光学异构体，或其药理学上可接受的盐，或其水合物或溶液，以及含有上述物质的药物组合物，特别是一种预防或治疗炎症性疾病的药物和一种治疗哮喘的药物。 上述 6-苯基四氢-1,3-恶嗪-2-酮衍生物具有很强的 IV 型 PDE 抑制活性，并具有支气管扩张和抗炎作用。
• PYRAZOLONE DERIVATIVE
  申请人：Kowa Company, Ltd.

  公开号：EP2172458A1

  公开（公告）日：2010-04-07

  A pyrazolone derivative represented by formula (I) below: wherein R1 to R3 are the same as defined in claims; or an optical isomer, a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof is provided. The novel pyrazolone derivative according to the present invention has a PAI-1 production inhibitory activity, a tissue fibrosis inhibitory activity, and a fibrolytic activity, and is effective for preventing and/or treating tissue fibrotic diseases (lung fibrosis, kidney fibrosis, etc.) and diseases of which a pathological thrombus becomes the cause, such as ischemic cardiac diseases (cardiac infarction and angina pectoris), atrial thrombus, lung embolism, deep thrombophlebitis, disseminated intravascular clotting, ischemic brain diseases (brain infarction, brain hemorrhage), and arterial sclerosis. In addition, a pharmaceutical agent for preventing and/or treating the disease conditions or the symptoms mediated by plasminogen activator inhibitor-1, comprising the novel pyrazolone derivative according to the present invention is also provided.

  下式（I）所代表的吡唑酮衍生物： 其中 R1 至 R3 与权利要求中定义的相同；或其光学异构体、药学上可接受的盐或其水合物或溶液。根据本发明的新型吡唑酮衍生物具有 PAI-1 生成抑制活性、组织纤维化抑制活性和纤维分解活性，可有效预防和/或治疗组织纤维化疾病（肺纤维化、肾纤维化等）和病理血栓形成疾病。例如缺血性心脏病（心肌梗塞和心绞痛）、心房血栓、肺栓塞、深部血栓性静脉炎、弥散性血管内凝血、缺血性脑部疾病（脑梗塞、脑出血）和动脉硬化。此外，还提供了一种用于预防和/或治疗由纤溶酶原激活剂抑制剂-1介导的疾病症状的药剂，其中包含根据本发明的新型吡唑酮衍生物。
• [DE] THIAZOL-DERIVATE ALS SELEKTIVE INHIBITOREN DER PDE-IV<br/>[EN] THIAZOLE DERIVATIVES USEFUL AS SELECTIVE INHIBITORS OF PDE-IV<br/>[FR] NOUVEAUX DERIVES DE THIAZOL S'UTILISANT COMME INHIBITEURS SELECTIFS DE LA PDE-IV
  申请人：BYK GULDEN LOMBERG CHEMISCHE FABRIK GMBH

  公开号：WO1998008844A1

  公开（公告）日：1998-03-05

  (DE) Verbindungen der Formel (I), worin R1, R2, R3, R4 und n die in der Beschreibung angegebenen Bedeutungen haben, sind neue wirksame Bronchialtherapeutika.(EN) Compounds having the formula (I), in which R1, R2, R3, R4 and n have the meanings given in the description, are new effective bronchotherapeutic agents.(FR) L'invention concerne des composés de la formule (I) dans laquelle R1, R2, R3, R4 et n ont la signification mentionnée dans la description. Ces composés sont de nouveaux agents thérapeutiques bronchiques actifs.

  将以下英文文本翻译成中文：仅返回翻译后的中文文本， （DE）Verbindungen der Formel (I), worin R1, R2, R3, R4 und n die in der Beschreibung angegebenen Bedeutungen haben, sind neue wirksame Bronchialtherapeutika. (EN) Compounds having the formula (I), in which R1, R2, R3, R4 and n have the meanings given in the description, are new effective bronchotherapeutic agents. (FR) L'invention concerne des composés de la formule (I) dans laquelle R1, R2, R3, R4 et n ont la signification mentionnée dans la description. Ces composés sont de nouveaux agents thérapeutiques bronchiques actifs.