(3E)-6-chloro-3-[hydroxy-(pyridin-2-ylamino)methylidene]-2-methyl-1,1-dioxothieno[2,3-e]thiazin-4-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并噻嗪类
• 英文名称: (3E)-6-chloro-3-[hydroxy-(pyridin-2-ylamino)methylidene]-2-methyl-1,1-dioxothieno[2,3-e]thiazin-4-one
• 化学式: C₁₃H₁₀ClN₃O₄S₂
• 分子量: 371.8
• InChiKey: OXROWJKCGCOJDO-JLHYYAGUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  136
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• NITROXIDE MODIFIED NON-STEROIDAL ANTI-INFLAMMATORY COMPOUNDS AND USES THEREOF IN THE TREATMENT AND PREVENTION OF DISEASES OR DISORDERS
  申请人：Wink David A.

  公开号：US20120263650A1

  公开（公告）日：2012-10-18

  Disclosed are nitroxide modified NSAID compounds of the formula (I) or a pharmaceutically acceptable salt or enantiomer thereof: in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , and n are defined herein and pharmaceutical compositions thereof. Further disclosed is a method of treating or preventing various disorders, such as inflammation, cancer, diabetes, a cardiovascular disorder, weight gain, polyps, and/or chronic pain, in a patient comprising administering an effective amount of a compound or pharmaceutically acceptable salt or enantiomer of formula (I). A method of imaging the compound or pharmaceutically acceptable salt or enantiomer of formula (I) in the body of the animal is also provided.

  揭示了具有以下结构式（I）的硝基氧自由基修饰的NSAID化合物或其药用盐或对映体：其中R1、R2、R3、R4、R5、R6、R7、R8、R9、R10、R11和n在此处被定义，并其药物组合物。进一步揭示了一种治疗或预防各种疾病的方法，如炎症、癌症、糖尿病、心血管疾病、体重增加、息肉和/或慢性疼痛，在患者中包括给予化合物或结构式（I）的药用盐或对映体的有效量。还提供了一种在动物体内成像化合物或结构式（I）的药用盐或对映体的方法。
• Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods of making and use thereof
  申请人：KemPharm, Inc.

  公开号：US10463660B2

  公开（公告）日：2019-11-05

  The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxymorphone (4,5-α-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxymorphone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxymorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

  本技术提供了由芳基羧酸和例如非甾体抗炎药与羟吗啡酮（4,5-α-环氧-3,14-二羟基-17-甲基吗啡南-6-酮）化学共轭形成羟吗啡酮的新型原药/组合物的组合物，包括苯甲酸盐、水杨酸盐、丙酸盐、非那西丁酸盐和醋酸盐，它们具有降低羟吗啡酮滥用可能性的作用。本技术还提供了治疗病人的方法、医药包和合成本技术共轭物的方法。
• Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone, prodrugs, methods of making and use thereof
  申请人：KemPharm, Inc.

  公开号：US10544153B2

  公开（公告）日：2020-01-28

  The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxycodone (4,5-α-epoxy-14-hydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxycodone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxycodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

  本技术提供了由芳基羧酸和例如非甾体抗炎药与羟考酮（4,5-α-环氧-14-羟基-17-甲基吗啡烷-6-酮）化学共轭形成羟考酮的新型原药/组合物的组合物，包括苯甲酸盐、水杨酸盐、丙酸盐、非那西丁酸盐和醋酸盐，它们具有降低羟考酮滥用可能性的作用。本技术还提供了治疗病人的方法、医药包和合成本技术共轭物的方法。
• Compositions of pharmaceutical actives containing diethylene glycol monoethyl ether or other alkyl derivatives
  申请人：THEMIS MEDICARE LIMITED

  公开号：US10940205B2

  公开（公告）日：2021-03-09

  The present invention relates to pharmaceutical compositions of various pharmaceutical actives, especially lyophilic and hydrophilic actives containing Diethylene glycol monoethyl ether or other alkyl derivatives thereof as a primary vehicle and/or to pharmaceutical compositions utilizing Diethylene glycol monoethyl ether or other alkyl derivatives thereof as a primary vehicle or as a solvent system in preparation of such pharmaceutical compositions. The pharmaceutical compositions of the present invention are safe, non-toxic, exhibits enhanced physical stability compared to conventional formulations containing such pharmaceutical actives and are suitable for use as injectables for intravenous and intramuscular administration, as well as for use as a preformed solution/liquid for filling in and preparation of capsules, tablets, nasal sprays, gargles, dermal applications, gels, topicals, liquid oral dosage forms and other dosage forms.

  本发明涉及各种药物活性物质的药物组合物，特别是含有二乙二醇单乙醚或其 他烷基衍生物作为主要载体的冻干和亲水活性物质，和/或涉及利用二乙二醇单乙醚或其 他烷基衍生物作为主要载体或作为制备此类药物组合物的溶剂系统的药物组合物。本发明的药物组合物安全、无毒，与含有此类药物活性成分的传统制剂相比，具有更强的物理稳定性，适合用作静脉注射和肌肉注射的注射剂，也适合用作预制溶液/液体，用于填充和制备胶囊、片剂、鼻腔喷雾剂、漱口水、皮肤应用、凝胶、外用药、口服液剂型和其他剂型。
• Method of using a cox-2 inhibitor and a topoisomerase II inhibitor as a combination therapy in the treatment of neoplasia
  申请人：Masferrer L Jaime

  公开号：US20060105961A1

  公开（公告）日：2006-05-18

  The present invention provides compositions and methods to treat, prevent or inhibit a neoplasia or a neoplasia-related disorder in a mammal using a combination of a COX-2 inhibitor and a topoisomerase II inhibitor.

  本发明提供了使用 COX-2 抑制剂和拓扑异构酶 II 抑制剂组合治疗、预防或抑制哺乳动物肿瘤或肿瘤相关疾病的组合物和方法。