2-methylsulfinyl-naphtho[2,3-b]furan-4,9-dione | 1361227-32-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 萘并呋喃类
• 英文名称: 2-methylsulfinyl-naphtho[2,3-b]furan-4,9-dione
• 英文别名: 2-methylsulfinylbenzo[f][1]benzofuran-4,9-dione
• CAS: 1361227-32-8
• 化学式: C₁₃H₈O₄S
• 分子量: 260.27
• InChiKey: BDVOUHPOXRKREC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  83.6
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2-bromo-naphtho[2,3-b]furan-4,9-dione 在 iron(III) chloride 、 高碘酸 作用下， 以 四氢呋喃 、 水 、 乙腈 为溶剂， 反应 2.19h， 生成 2-methylsulfinyl-naphtho[2,3-b]furan-4,9-dione
  参考文献：
  名称：

  [EN] NOVEL ANPHTHOQUINONES FOR DISEASE THERAPIES
  [FR] NOUVELLES NAPHTOQUINONES À USAGE THÉRAPEUTIQUE

  摘要：

  萘并[2,3-b]呋喃-4,9-二酮和萘并[2,3-b]噻吩-4,9-二酮的制备方法及其用途被公开。还公开了包含这些化合物的药物组合物，用于治疗包括增殖性疾病在内的各种疾病。

  公开号：

  WO2012024818A1

文献信息

• [EN] NOVEL ANPHTHOQUINONES FOR DISEASE THERAPIES<br/>[FR] NOUVELLES NAPHTOQUINONES À USAGE THÉRAPEUTIQUE
  申请人：ZHOUSHAN HAIZHONGZHOU XINSHENG PHARMACEUTICALS CO LTD

  公开号：WO2012024818A1

  公开（公告）日：2012-03-01

  Naphtho[2,3-b]furan-4,9-diones and naphtho[2,3-b]thiophene-4,9-diones, the preparation methods and uses thereof are disclosed. The pharmaceutical compositions comprising such compounds for the treatment of various indications including proliferative diseases are also disclosed.

  萘并[2,3-b]呋喃-4,9-二酮和萘并[2,3-b]噻吩-4,9-二酮的制备方法及其用途被公开。还公开了包含这些化合物的药物组合物，用于治疗包括增殖性疾病在内的各种疾病。
• [EN] NOVEL ESTERS OF 4,9-DIHYDROXY-NAPHTHO[2,3-b]FURANS FOR DISEASE THERAPIES<br/>[FR] NOUVEAUX ESTERS DE 4,9-DIHYDROXY-NAPHTO[2,3-B]FURANNES POUR TRAITEMENT THÉRAPEUTIQUE DE MALADIES
  申请人：ZHOUSHAN HAIZHONGZHOU XINSHENG PHARMACEUTICALS CO LTD

  公开号：WO2012119265A1

  公开（公告）日：2012-09-13

  The present invention discloses esters of 4,9-dihydroxy-naphtho[2,3-b]furans and methods of making and using the same. The present invention also discloses conversion of the esters into therapeutically active 4,9-dihydroxy-naphtho[2,3-b]furans in vivo. The present invention furthermore discloses pharmaceutical compositions comprising the esters of 4,9- dihydroxy-naphtho[2,3-b]furans for the treatment of various indications including proliferative diseases.

  本发明公开了4,9-二羟基萘并[2,3-b]呋喃的酯类及其制造和使用方法。本发明还公开了将这些酯转化为体内治疗活性4,9-二羟基萘并[2,3-b]呋喃的方法。本发明进一步公开了包含4,9-二羟基萘并[2,3-b]呋喃的酯类的药物组合物，用于治疗包括增殖性疾病在内的各种疾病。
• NOVEL ESTERS OF 4, 9-DIHYDROXY-NAPHTHO [2, 3-b] FURANS FOR DISEASE THERAPIES
  申请人：Jiang Zhiwei

  公开号：US20130345176A1

  公开（公告）日：2013-12-26

  The present invention discloses esters of 4,9-dihydroxy-naphtho[2,3-b]furans and methods of making and using the same. The present invention also discloses conversion of the esters into therapeutically active 4,9-dihydroxy-naphtho[2,3-b]furans in vivo. The present invention furthermore discloses pharmaceutical compositions comprising the esters of 4,9-dihydroxy-naphtho[2,3-b]furans for the treatment of various indications including proliferative diseases.

  本发明公开了4,9-二羟基萘并[2,3-b]呋喃的酯类及其制造和使用方法。本发明还公开了将这些酯转化为体内治疗活性4,9-二羟基萘并[2,3-b]呋喃的方法。本发明进一步公开了包含4,9-二羟基萘并[2,3-b]呋喃的酯类的药物组合物，用于治疗包括增殖性疾病在内的各种疾病。
• [EN] TREATMENT OF CANCERS RELATED TO CHRONICALLY ACTIVE RAS<br/>[FR] TRAITEMENT DE CANCERS ASSOCIÉS À UN GÈNE RAS CHRONIQUEMENT ACTIF
  申请人：HANGZHOU YIER BIOTECH CO LTD

  公开号：WO2017079864A1

  公开（公告）日：2017-05-18

  The present invention discloses that naphthofuranquinones and dihydroxynaphthofurans, and derivatives thereof, such as a compound of formula I or II, are effective in deactivating chronically active Ras. The present invention also discloses a method of treating or preventing cancer comprising steps of: 1) identifying a patient suffering from or susceptible to a cancer related to chronically active Ras; and 2) administering a therapeutically effective amount of a compound of formula I or II, or a pharmaceutically acceptable salt thereof. The present invention further discloses a method of treating or preventing cancer comprising steps of: 1) identifying a patient suffering from or susceptible to a cancer related to a K-Ras mutation; and 2) administering a therapeutically effective amount of a compound of formula I or II, or a pharmaceutically acceptable salt thereof.

  本发明揭示了萘呋喹醌和二羟基萘呋喃及其衍生物，例如公式I或II的化合物，在去活化慢性活性Ras方面具有有效性。本发明还揭示了一种治疗或预防癌症的方法，包括以下步骤：1）识别患有或易感患有与慢性活性Ras相关的癌症的患者；和2）给予公式I或II的化合物或其药学上可接受的盐的治疗有效量。本发明还揭示了一种治疗或预防癌症的方法，包括以下步骤：1）识别患有或易感患有与K-Ras突变相关的癌症的患者；和2）给予公式I或II的化合物或其药学上可接受的盐的治疗有效量。
• Naphthoquinones for disease therapies
  申请人：Jiang Zhiwei

  公开号：US08871802B2

  公开（公告）日：2014-10-28

  The present invention discloses novel naphtho[2,3-b]furan-4,9-diones and naphtho[2,3-b]thiophene-4,9-diones and methods of making and using the same. The present invention also discloses pharmaceutical compositions comprising novel naphtho[2,3-b]furan-4,9-dione or naphtho[2,3-b]thiophene-4,9-diones for the treatment of various indications including proliferative diseases.

  本发明揭示了新型萘并[2,3-b]呋喃-4,9-二酮和萘并[2,3-b]噻吩-4,9-二酮及其制备和使用方法。本发明还揭示了包含新型萘并[2,3-b]呋喃-4,9-二酮或萘并[2,3-b]噻吩-4,9-二酮的药物组合物，用于治疗各种疾病，包括增殖性疾病。