3-{[2-(methylsulfonyl)hydrazinyl]carbonyl}-1-[2-oxo-2-(thiophen-2-yl)ethyl] pyridinium chloride | 357625-50-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-{[2-(methylsulfonyl)hydrazinyl]carbonyl}-1-[2-oxo-2-(thiophen-2-yl)ethyl] pyridinium chloride
• 英文别名: TRC4186；Pyridinium, 3-((2-(methylsulfonyl)hydrazino)carbonyl)-1-(2-oxo-2-(2-thienyl)ethyl)-, chloride；N'-methylsulfonyl-1-(2-oxo-2-thiophen-2-ylethyl)pyridin-1-ium-3-carbohydrazide;chloride
• CAS: 357625-50-4
• 化学式: C₁₃H₁₄N₃O₄S₂*Cl
• 分子量: 375.857
• InChiKey: QWXKHFBZAGOZJM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.88
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  133
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  3-{[2-(methylsulfonyl)hydrazinyl]carbonyl}-1-[2-oxo-2-(thiophen-2-yl)ethyl] pyridinium chloride 在 palladium 10% on activated carbon 氢气 、 三乙胺 作用下， 以 甲醇 为溶剂， 20.0 ℃ 、5.0 kPa 条件下， 反应 50.0h， 生成 N'-(methylsulfonyl)-1-[2-oxo-2-(thiophen-2-yl)ethyl]-1,4,5,6-tetrahydropyridine-3-carbohydrazide
  参考文献：
  名称：

  [EN] PIPERIDINE DERIVATIVES USEFUL FOR TREATMENT OF DIEBETES
  [FR] NOUVEAUX COMPOSÉS HÉTÉROCYCLIQUES

  摘要：

  公开号：

  WO2010128528A9
• 作为产物：
  描述：

  烟酸甲酯 在 吡啶 、 一水合肼 作用下， 以 N,N-二甲基甲酰胺 、 异丙醇 为溶剂， 反应 23.0h， 生成 3-{[2-(methylsulfonyl)hydrazinyl]carbonyl}-1-[2-oxo-2-(thiophen-2-yl)ethyl] pyridinium chloride
  参考文献：
  名称：

  [EN] NOVEL PYRIDINIUM COMPOUNDS
  [FR] NOUVEAUX COMPOSÉS DE PYRIDINIUM

  摘要：

  本发明涉及新型吡啶盐化合物，其异构体、立体异构体、对映异构体、构象体、互变异构体、多晶型、水合物和溶剂化合物。本发明还涵盖了制备新化合物的方法和所述化合物的药物组合物。该发明还涉及上述化合物用于制备用作药物的药物的用途。

  公开号：

  WO2016162785A1

文献信息

• NOVEL HETEROCYCLIC COMPOUNDS
  申请人：Dutt Chaitanya

  公开号：US20120046317A1

  公开（公告）日：2012-02-23

  The present invention relates to a new class of heterocyclic compounds and pharmaceutically acceptable salts thereof, process for preparing the same, pharmaceutical composition containing these compounds and to their use in treatment of diseases caused due to formation and accumulation of AGEs (Advanced Glycation end products). The compounds of the present invention are useful for the treatment of diabetic and aging-related complications caused by formation and accumulation of AGEs, such as neuropathy, nephropathy, microangiopathy, retinopathy, hypertension, heart failure, atherosclerosis, Alzheimer's disease & dermatological disorders.

  本发明涉及一种新的杂环化合物及其药学上可接受的盐，制备该化合物的过程，含有这些化合物的药物组合物以及它们在治疗由于AGEs（高级糖基化终产物）的形成和积累引起的疾病中的应用。本发明的化合物对于治疗由于AGEs的形成和积累引起的糖尿病和衰老相关并发症非常有用，例如神经病变、肾病、小血管病、视网膜病、高血压、心力衰竭、动脉粥样硬化、阿尔茨海默病和皮肤病。
• [EN] IN-SITU SYNTHESIS OF 3-SUBSTITUTED PYRIDINIUM COMPOUNDS<br/>[FR] SYNTHÈSE IN-SITU DE COMPOSÉS À BASE DE PYRIDINIUM 3-SUBSTITUÉS
  申请人：TORRENT PHARMACEUTICALS LTD

  公开号：WO2022238921A1

  公开（公告）日：2022-11-17

  Present invention relates to an in-situ and improved process for the preparation of 3-[2-(methylsulfonyl)hydrazinyl]carbonyl}- 1-[2-oxo-2- (thiophen-2-yl)ethyl]pyridinium salts or salt-cocrystal.

  本发明涉及一种原位改进的制备3-[2-(甲磺酰基)肼基]羰基}-1-[2-氧代-2-(噻吩-2-基)乙基]吡啶盐或盐-共晶的方法。
• Novel compounds for the management of aging-related and diabetic vascular complications, process for their preparation and therapeutic uses thereof
  申请人：——

  公开号：US20010018524A1

  公开（公告）日：2001-08-30

  Novel compounds of the pyridinium series useful for the management of diabetes and aging-related vascular complications, including kidney disease, nerve damage, atherosclerosis, retinopathy, dermatological disorders and discoloration of teeth, by breaking preformed AGE, of the general formula I, or pharmaceutically acceptable salts thereof, 1 wherein, R 1 , R 2 , R 3 , X and m are as defined in the specification. Also disclosed is a method for preparation of the compounds of general formula (I) and pharmaceutical composition containing one or more compounds as defined above as active ingredients. Also disclosed is a method of treatment of a diabetic patient by administering the compounds as defined above, either singly or in combination with drugs for antidiabetic therapy.

  本发明涉及一系列新的吡啶系列化合物，可用于管理糖尿病和与衰老相关的血管并发症，包括肾脏疾病、神经损伤、动脉硬化、视网膜病变、皮肤疾病和牙齿变色，通过破坏预先形成的AGE，其通式为I，或其药学上可接受的盐，其中，R1、R2、R3、X和m如规范中所定义。本发明还公开了一种制备通式（I）化合物的方法和含有一种或多种上述化合物作为活性成分的制药组合物。本发明还公开了一种通过单独或与抗糖尿病治疗药物联合使用上述化合物治疗糖尿病患者的方法。
• Composition and method for use of pyridinium derivatives in cosmetic and therapeutic applications
  申请人：Torrent Pharmaceuticals Ltd

  公开号：EP1304101A1

  公开（公告）日：2003-04-23

  The invention discloses a new class of compounds particularly pyridinium derivatives, which have been found to exhibit triple function of a free radical scavenger (antioxidant), AGE breaker and AGE inhibitor, and cosmetic composition comprising these compounds contained in a cosmetically acceptable carrier. The invention also discloses a method of cosmetic application by applying such composition. The invention further discloses a pharmaceutical composition, comprising said compounds useful in scavenging free radicals from the body cells of a mammal, a method of scavenging free radicals from the body cells of a mammal and a method of treating of diseases caused by accumulation of free radicals in the body cells of a mammal by administering a composition made with the compounds of the invention. The invention in addition, also discloses composition and method for inhibiting AGE in a mammal by use of the compounds of the same group.

  本发明公开了一类新化合物，特别是吡啶鎓衍生物，它们被发现具有自由基清除剂（抗氧化剂）、AGE 破坏剂和 AGE 抑制剂的三重功能，还公开了包含在化妆品可接受载体中的这些化合物的化妆品组合物。本发明还公开了一种通过施用此类组合物进行美容的方法。本发明进一步公开了一种药物组合物，其中包含有助于清除哺乳动物体细胞中自由基的所述化合物；一种清除哺乳动物体细胞中自由基的方法；以及一种通过施用用本发明化合物制成的组合物治疗哺乳动物体细胞中自由基积累引起的疾病的方法。此外，本发明还公开了通过使用同组化合物抑制哺乳动物体内 AGE 的组合物和方法。
• Pharmaceutical combinations comprising specified age breaker and further drugs, i.a. antihypertensive drugs, antidiabetic drugs etc.
  申请人：Torrent Pharmaceuticals Ltd.

  公开号：EP2659933A1

  公开（公告）日：2013-11-06

  The present invention relates to a combination, such as a combined preparation or pharmaceutical composition comprising: (a) compound of formula (I), and/or (II) or a pharmaceutically acceptable salt thereof; (b) at least one therapeutic agent selected from the group consisting of: an antihypertensive agent; an antidiabetics agent; a hypolipidemic agent; an antiplatelet agent; an antiobesity agent; an antithrombotic agent; an agent for diabetic vascular complications; and an agent for treatment of heart failure; or a pharmaceutically acceptable salts thereof, optionally in presence of a pharmaceutically acceptable carrier for separate, simultaneous or sequential use. The present invention also relates to a use of such combination for the treatment of mammal including human being. R1, R2, R3, R1, R2, R3, R4, R5, X, Y, A and B and m are as defined in the specification.

  本发明涉及一种组合物，如一种组合制剂或药物组合物，其包含：(a) 式(I)和/或(II)化合物或其药学上可接受的盐；(b) 至少一种选自以下组别的治疗剂：抗高血压药；抗糖尿病药；降血脂药；抗血小板药；抗肥胖药；抗血栓药；治疗糖尿病血管并发症药；治疗心力衰竭药；或其药学上可接受的盐，可选择与药学上可接受的载体一起单独、同时或连续使用。本发明还涉及将此类组合物用于治疗包括人类在内的哺乳动物。 R1、R2、R3、R1、R2、R3、R4、R5、X、Y、A 和 B 以及 m 如说明书中所定义。