6-氯-9-(3-N-(2-氯乙基氨)丙氨基-2-甲氧基吖啶二盐酸盐 | 17870-45-0

• 物质功能分类: 医药中间体 - 原料药中间体
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 6-氯-9-(3-N-(2-氯乙基氨)丙氨基-2-甲氧基吖啶二盐酸盐
• 英文名称: 6-Chloro-9-[3-(2-chloroethylamino)propylamino]-2-methoxyacridine dihydrochloride
• 英文别名: N-(2-chloroethyl)-N'-(6-chloro-2-methoxyacridin-9-yl)propane-1,3-diamine;dihydrochloride
• CAS: 17870-45-0；17070-45-0
• 化学式: C19H21Cl2N3O.2ClH
• mdl: MFCD00013320
• 分子量: 451.2
• InChiKey: LMEMIKWTNPWYMI-UHFFFAOYSA-N

物化性质

• 熔点：
  261-262 °C
• 溶解度：
  可溶于DMSO
• 物理描述：
  Icr 191 appears as yellow crystalline or chunky solid. (NTP, 1992)

计算性质

• 辛醇/水分配系数(LogP)：
  3.79
• 重原子数：
  27
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.315
• 拓扑面积：
  55.3
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 危险等级：
  6.1(b)

文献信息

• METHYLLACTAM RING COMPOUND AND PHARMACEUTICAL USE THEREOF
  申请人：Japan Tobacco Inc.

  公开号：US20190352284A1

  公开（公告）日：2019-11-21

  An object of the present invention is to provide a methyllactam ring compound that has an SGLT1 inhibitory activity and is useful for a drug, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof. A compound of Formula [I]: or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof is provided.

  本发明的一个目的是提供一种具有SGLT1抑制活性且适用于药物的甲基乳酰胺环化合物，或其药用盐，包括它的药物组合物以及其药用。提供一种化合物的公式[I]：或其药用盐，包括它的药物组合物以及其药用。
• PYRAZOLE COMPOUNDS SUBSTITUTED WITH HETEROARYL AND PHARMACEUTICAL USE THEREOF
  申请人：Japan Tobacco Inc.

  公开号：US20190330193A1

  公开（公告）日：2019-10-31

  Pyrazole compounds substituted with heteroaryl or pharmaceutically acceptable salts thereof that have an SGLT1 inhibitory activity and are useful for a drug, pharmaceutical compositions comprising the same, and pharmaceutical use thereof are disclosed. Specifically, a compound of Formula [X]: wherein R 1 is hydrogen or halogen, R 2 is C 1-6 alkyl or halo-C 1-6 alkyl, Ring Het is substituted pyridyl or optionally substituted pyrazinyl, pyrimidinyl, or pyridazinyl, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof is provided.

  揭示了具有SGLT1抑制活性的以杂环芳基取代的吡唑化合物或其药学可接受的盐，用作药物，包括它们的药物组合物，以及其药用。具体地，提供了以下式[X]的化合物：其中R1为氢或卤素，R2为C1-6烷基或卤代C1-6烷基，环Het为取代的吡啶基或可选择取代的吡嗪基、嘧啶基或吡啉基，或其药学可接受的盐，包括它的药物组合物和药用。
• CHRONIC KIDNEY DISEASE TREATMENT OR PREVENTION METHOD
  申请人：Japan Tobacco Inc.

  公开号：EP4026562A1

  公开（公告）日：2022-07-13

  One aim of the present invention is to treat or prevent chronic kidney disease. Provided is a treatment or prophylactic pharmaceutical composition for chronic kidney disease, that contains an SGLT1-inhibiting compound or a pharmaceutically acceptable salt thereof.

  本发明的一个目的是治疗或预防慢性肾脏疾病。提供了一种用于慢性肾脏疾病的治疗或预防性药物组合物，其含有一种SGLT1抑制化合物或其药学上可接受的盐。
• THERAPEUTIC OR PROPHYLACTIC METHOD FOR DIABETES USING COMBINATION MEDICINE
  申请人：Japan Tobacco Inc.

  公开号：EP4026564A1

  公开（公告）日：2022-07-13

  One purpose of the present invention is to provide therapy or prophylaxis of diabetes, obesity, or diabetic complications. The present invention provides a therapeutic or prophylactic medicine that is for diabetes, obesity, or diabetic complications, and that is characterized by combinational use of an SGLT1 inhibitor and at least one drug selected from SGLT2 inhibitors and DPP4 inhibitors; and a therapeutic or prophylactic method that is for diabetes, obesity, or diabetic complications, and that is characterized by administering an SGLT1 inhibitor and at least one drug selected from SGLT2 inhibitors and DPP4 inhibitors.

  本发明的一个目的是提供糖尿病、肥胖症或糖尿病并发症的治疗或预防。本发明提供了一种治疗或预防糖尿病、肥胖症或糖尿病并发症的药物，其特点是联合使用SGLT1抑制剂和至少一种从SGLT2抑制剂和DPP4抑制剂中选择的药物；以及一种治疗或预防糖尿病、肥胖症或糖尿病并发症的治疗方法，其特点是给予SGLT1抑制剂和至少一种从SGLT2抑制剂和DPP4抑制剂中选择的药物。
• Process for the manufacture of keto gulonic acid
  申请人：F. HOFFMANN-LA ROCHE AG

  公开号：EP0213591A2

  公开（公告）日：1987-03-11

  The invention relates to a process for producing 2-keto-L-gulonic acid, which comprises converting L-sorbose and/or D-sorbitol into 2-keto-L-gulonic acid with the aid of a microorganism or its cell free extract, said microorganism belonging to the species Gluconobacter oxydans capable of producing 2-keto-L-gulonic acid and having a high activity of L-sorbose dehydrogenase to convert L-sorbose into L-sorbosone. Specific microorganisms useful in such process are also part of the invention.

  本发明涉及一种生产2-酮-L-古洛糖酸的工艺，该工艺包括借助微生物或其无细胞提取物将L-山梨糖和/或D-山梨醇转化为2-酮-L-古洛糖酸，所述微生物属于能够生产2-酮-L-古洛糖酸的葡萄糖杆菌（Gluconobacter oxydans），并具有较高的L-山梨糖脱氢酶活性，可将L-山梨糖转化为L-山梨糖醇。本发明还包括用于这种工艺的特定微生物。