4,6-dimethyl-2,3-dihydro-1H-indol-2-one | 290820-93-8

• 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: 4,6-dimethyl-2,3-dihydro-1H-indol-2-one
• 英文别名: 4,6-dimethyl-1,3-dihydroindol-2-one
• CAS: 290820-93-8
• 化学式: C₁₀H₁₁NO
• mdl: MFCD11847071
• 分子量: 161.2
• InChiKey: GRDBADCLUZAZKI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• [EN] SUBSTITUTED 5-HYDROXYOXINDOLES AND THEIR USE AS ANALGESICS AND FEVER REDUCERS<br/>[FR] 5-HYDROXYOXINDOLES SUBSTITUÉS ET LEUR UTILISATION EN TANT QU'ANALGÉSIQUES ET RÉDUCTEURS DE FIÈVRE
  申请人：CARAFE DRUG INNOVATION LLC

  公开号：WO2016179157A1

  公开（公告）日：2016-11-10

  The present invention provides compounds and compositions which are useful in methods for modulating pain and fevers in a subject. These compounds are of the structure of formula (I), wherein Rx-R4, X, Y, and Z are defined herein, or a pharmaceutically acceptable salt, solvate, or prodrug thereof to the subject. In one embodiment, the compound is 5-hydroxy-7-methyloxindole.

  本发明提供了一些化合物和组合物，可用于调节受体体内的疼痛和发烧。这些化合物的结构为公式（I），其中Rx-R4，X，Y和Z在此定义，或其药学上可接受的盐，溶剂或前药，用于治疗受体体内的疼痛和发烧。在一种实施例中，该化合物是5-羟基-7-甲氧基吲哚。
• 2-AMINOBENZAMIDE DERIVATIVE
  申请人：Kuramochi Takahiro

  公开号：US20090233900A1

  公开（公告）日：2009-09-17

  To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation. The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.

  本发明提供了一种基于对辣椒素受体VR1激活的抑制作用的新型优良药剂，用于治疗或预防伤害性疼痛、神经病理性疼痛、癌症疼痛、头痛、膀胱功能障碍等疾病。本发明通过确认一种苯甲酰胺衍生物，其特征在于其苯环上的单环在酰胺基氮原子上被紧缩，其低烷基氨基或邻位于酰胺基的环基取代的氨基具有对VR1激活的强抑制作用和优良的药理作用，从而发现它可以成为治疗或预防伤害性疼痛、神经病理性疼痛、癌症疼痛、头痛、膀胱功能障碍等VR1相关疾病的优良药剂。
• 2-AMINOBENZAMIDE DERIVATIVES AS VANILLOID RECEPTOR 1 (VR1) INHIBITORS USEFUL FOR THE TREATMENT OF PAIN OR BLADDER FUNCTION DISORDER
  申请人：Astellas Pharma Inc.

  公开号：EP1955697B1

  公开（公告）日：2012-05-02
• SUBSTITUTED 5-HYDROXYOXINDOLES AND THEIR USE AS ANALGESICS AND FEVER REDUCERS
  申请人：CARAFE DRUG INNOVATION, LLC

  公开号：US20180256543A1

  公开（公告）日：2018-09-13

  The present invention provides compounds and compositions which are useful in methods for modulating pain and fevers in a subject. These compounds are of the structure of formula (I), wherein Rx-R4, X, Y, and Z are defined herein, or a pharmaceutically acceptable salt, solvate, or prodrug thereof to the subject. In one embodiment, the compound is 5-hydroxy-7-methyloxindole.
• US6316429B1
  申请人：——

  公开号：US6316429B1

  公开（公告）日：2001-11-13