1,3-二氢-6,7-二甲氧基-3-(5,6,7,8-四氢-4-甲氧基-6-甲基-1,3-二噁唑并[4,5-g]异喹啉-5-基)异苯并呋喃-1-醇 | 24531-57-5

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 1,3-二氢-6,7-二甲氧基-3-(5,6,7,8-四氢-4-甲氧基-6-甲基-1,3-二噁唑并[4,5-g]异喹啉-5-基)异苯并呋喃-1-醇
• 英文名称: D-1-thio-glucitol
• 英文别名: 1-thio-D-glucitol；1-Thio-D-glucit；thio-sorbitol；thiosorbitol；1-Thio-D-sorbit；1-Thiosorbitol；(2R,3R,4S,5R)-6-sulfanylhexane-1,2,3,4,5-pentol
• CAS: 24531-57-5
• 化学式: C₆H₁₄O₅S
• 分子量: 198.24
• InChiKey: DYIOSHGVFJTOAR-JGWLITMVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.1
• 重原子数：
  12
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  102
• 氢给体数：
  6
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  1,3-二氢-6,7-二甲氧基-3-(5,6,7,8-四氢-4-甲氧基-6-甲基-1,3-二噁唑并[4,5-g]异喹啉-5-基)异苯并呋喃-1-醇 在 乙醇 、 碘 作用下， 生成 disulfide from 1-thio-D-glucitol
  参考文献：
  名称：

  Farlow et al., Journal of the American Chemical Society, 1948, vol. 70, p. 1393

  摘要：

  DOI：
• 作为产物：
  描述：

  葡萄糖 在 cobalt polysulfide 、 水 、 氢气 、 sulfur 作用下， 125.0~150.0 ℃ 、9.81 MPa 条件下， 生成 1,3-二氢-6,7-二甲氧基-3-(5,6,7,8-四氢-4-甲氧基-6-甲基-1,3-二噁唑并[4,5-g]异喹啉-5-基)异苯并呋喃-1-醇
  参考文献：
  名称：

  Farlow et al., Journal of the American Chemical Society, 1948, vol. 70, p. 1393

  摘要：

  DOI：

文献信息

• 1-Thio-D-Glucitol Derivatives
  申请人：Kakinuma Hiroyuki

  公开号：US20080132563A1

  公开（公告）日：2008-06-05

  The present invention provides a 1-thio-D-glucitol compound of the following formula, which shows the action of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt of the compound, or a hydrate of the compound or the salt; and a pharmaceutical comprising such a compound as an active ingredient, especially, a pharmaceutical for preventing or treating diabetes, diabetes-related disease, or diabetic complication. The invention also provides a method for producing the 1-thio-D-glucitol compound and its intermediate.

  本发明提供了以下公式的1-硫代-D-葡萄糖醇化合物，该化合物显示抑制SGLT2活性的作用，该化合物的药用可接受盐或该化合物或盐的水合物；以及包含该化合物作为活性成分的制药品，特别是用于预防或治疗糖尿病、糖尿病相关疾病或糖尿病并发症的制药品。本发明还提供了制备1-硫代-D-葡萄糖醇化合物及其中间体的方法。
• 1-PHENYL 1-THIO-D-GLUCITOL DERIVATIVE
  申请人：Kakinuma Hiroyuki

  公开号：US20100069460A1

  公开（公告）日：2010-03-18

  A 1-phenyl 1-thio-D-glucitol compound represented by formula (I) or the like: or a pharmaceutically acceptable salt thereof or a hydrate thereof, or a pharmaceutical preparation comprising the same as an active ingredient is useful as a novel type of prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which inhibits both SGLT1 and SGLT2 activities to achieve not only suppression of glucose absorption from the digestive tract but also excretion of urinary sugars.

  一种由公式（I）或类似物表示的1-苯基1-硫代-D-葡萄糖醇化合物，或其药学上可接受的盐或水合物，或包含其作为活性成分的制药制剂，可用作一种新型的预防或治疗糖尿病、糖尿病相关疾病或糖尿病并发症的药物。该药物不仅抑制消化道中的葡萄糖吸收，还能促进尿糖的排泄，通过同时抑制SGLT1和SGLT2活性来实现。
• EXTERNAL DERMAL COMPOSITION FOR ANTI-AGEING AND METHOD FOR PRODUCING THE SAME
  申请人：HAYASHIBARA CO., LTD.

  公开号：US20150342854A1

  公开（公告）日：2015-12-03

  The present invention has an object to provide an external dermal composition for anti-ageing, which prevents or improves apparent skin problems such as wrinkles, fine wrinkles, blemishes, and saggings caused by increasing age or ageing; and maintains or improves the barrier function and the hyaluronic acid production in the skin. The object is solved by providing an external dermal composition for anti-ageing, which contains an aqueous medium as a base material and one or more ingredients selected from L-ascorbic acid, derivatives thereof, and their salts as an effective ingredient(s).

  本发明的目的是提供一种用于抗衰老的外用皮肤组成物，该组成物可以预防或改善因年龄增长或衰老引起的皮肤问题，如皱纹、细纹、斑点和下垂，并维持或改善皮肤的屏障功能和透明质酸的产生。本发明通过提供一种外用皮肤组成物来实现该目的，该组成物包含水性介质作为基材料，并含有一种或多种从L-抗坏血酸、其衍生物和它们的盐中选择的成分作为有效成分。
• Pharmaceutical compositions
  申请人：Taisho Pharmaceutical Co., Ltd.

  公开号：EP2601949A2

  公开（公告）日：2013-06-12

  A pharmaceutical composition comprising a combination of (A) (1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol and (B) at least one member of the group consisting of insulin secretagogues, insulin sensitizers, insulins, dipeptidyl peptidase IV inhibitors, α-glucosidase inhibitors, and GLP-1 mimetics, has superior efficacy in preventing or treating diabetes mellitus, diseases associated with diabetes mellitus, or complications of diabetes mellitus and yet it causes no appreciable side effects.

  一种药物组合物，包含(A)(1S)-1,5-脱水-1-[5-(4-乙氧基苄基)-2-甲氧基-4-甲基苯基]-1-硫代-D-葡萄糖醇和(B)胰岛素促泌剂、胰岛素增敏剂、胰岛素、二肽基肽酶 IV 抑制剂、α-葡萄糖苷酶抑制剂和 GLP-1 拟效物组成的组中的至少一种成员的组合、二肽基肽酶 IV 抑制剂、α-葡萄糖苷酶抑制剂和 GLP-1 拟效物组成的组中的至少一种，在预防或治疗糖尿病、糖尿病相关疾病或糖尿病并发症方面具有卓越的疗效，而且不会产生明显的副作用。
• Pharmaceutical compositions with (1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol and a further antidiabetic agent
  申请人：Taisho Pharmaceutical Co., Ltd.

  公开号：EP2829271A2

  公开（公告）日：2015-01-28

  A pharmaceutical composition comprising a combination of (A) (1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol and (B) at least one member of the group consisting ofdipeptidyl peptidase IV inhibitors, insulin sensitizers, insulins, α-glucosidase inhibitors, and GLP-1 mimetics, has superior efficacy in preventing or treating diabetes mellitus, diseases associated with diabetes mellitus, or complications of diabetes mellitus and yet it causes no appreciable side effects.

  一种药物组合物，包含(A)(1S)-1,5-脱水-1-[5-(4-乙氧基苄基)-2-甲氧基-4-甲基苯基]-1-硫代-D-葡萄糖醇和(B)由二肽基肽酶 IV 抑制剂、胰岛素增敏剂、胰岛素、α-葡萄糖苷酶抑制剂和 GLP-1 拟效物组成的组中的至少一种成员的组合、胰岛素、α-葡萄糖苷酶抑制剂和 GLP-1 模仿剂组成的组中的至少一种，在预防或治疗糖尿病、糖尿病相关疾病或糖尿病并发症方面具有卓越的疗效，而且不会产生明显的副作用。