3,1-苯并噻嗪-4-酮 | 100911-74-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 中文名称: 3,1-苯并噻嗪-4-酮
• 英文名称: 6-Oxo-4,5-benzo-1,3-thiazin
• 英文别名: 4h-3,1-Benzothiazin-4-one；3,1-benzothiazin-4-one
• CAS: 100911-74-8
• 化学式: C₈H₅NOS
• 分子量: 163.2
• InChiKey: AAYKGHJFMYRXAP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  54.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3,1-苯并噻嗪-4-酮 、 bis-(2,4-dihydroxythiobenzoyl)sulfinyl 在 甲醇 作用下， 反应 3.0h， 生成 2-(2,4-dihydroxythiobenzoyl)-3,1-benzothiazin-4-one
  参考文献：
  名称：

  Kostecka, Malgorzata, Acta poloniae pharmaceutica, 2011, vol. 68, # 1, p. 137 - 141

  摘要：

  DOI：
• 作为产物：
  描述：

  2-甲酰胺基苯甲酸 在 potassium permanganate 、 tetraphosphorus decasulfide 作用下， 生成 3,1-苯并噻嗪-4-酮
  参考文献：
  名称：

  Legrand,L., Bulletin de la Societe Chimique de France, 1960, p. 337 - 343

  摘要：

  DOI：

文献信息

• 2-thio-4h-3,1-benzoxazin-4-one derivatives for use as enzyme inhibitors
  申请人：——

  公开号：US20030176429A1

  公开（公告）日：2003-09-18

  The use of a compound, comprising formula (I) or a salt, ester, amide of prodrug thereof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I) A is an optionally substituted 6-membered aromatic or heteroaromatic ring; and R 1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups.

  化合物的使用，包括式（I）或其盐、酯、酰胺或前药的抑制作用，用于抑制一种首选作用方式是催化酯功能的水解的酶，例如在产品和过程中控制和抑制不需要的酶。这些化合物在医学上也很有用，例如在治疗肥胖和相关疾病方面。该发明还涉及式（I）内的新化合物，以及用于制备它们的方法和含有它们的药物组合物。在式（I）中，A是一个可选择取代的6元芳香环或杂芳环；而R1是支链或非支链的烷基（可由一个或多个氧原子中断），烯基，炔基，环烷基，环烯基，芳基，芳基烷基，还原芳基烷基，芳基烯基，杂芳基，杂芳基烷基，杂芳基烯基，还原芳基，还原杂芳基，还原杂芳基烷基或上述任何一组的取代衍生物。
• Use of non-digestible polymeric foams to sequester ingested materials thereby inhibiting their absorption by the body
  申请人：The Procter & Gamble Company

  公开号：US20030072804A1

  公开（公告）日：2003-04-17

  This disclosure relates to compositions comprising an open-celled polymeric foam wherein the compositions are useful for sequestering lipophilic materials present in the gastrointestinal tract, thereby inhibiting the absorption of such lipophilic materials by the body. The disclosure further relates to compositions comprising the open-celled polymeric foam wherein the compositions are useful for ameliorating side effects associated with the use of lipase inhibitors. In a preferred embodiment, this disclosure relates to compositions comprising polymeric foam materials made from high internal phase emulsions, where such foams are useful for sequestering lipophilic materials. Further disclosed are compositions comprising open-celled polymeric foams wherein the compositions are useful for the purpose of sequestering aqueous and/or hydrophilic materials present in the gastrointestinal tract, thereby ameliorating diarrhea. Kits comprising the compositions and methods of using the compositions and kits are also described.

  本公开涉及包含开孔聚合泡沫的组合物，其中的组合物可用于封闭存在于胃肠道中的亲脂性物质，从而抑制人体对此类亲脂性物质的吸收。本公开进一步涉及包含开孔聚合物泡沫的组合物，其中该组合物可用于改善与使用脂肪酶抑制剂相关的副作用。在一个优选的实施方案中，本公开涉及包含由高内相乳液制成的聚合物泡沫材料的组合物，其中这种泡沫可用于封存亲脂材料。进一步公开的是由开孔聚合物泡沫组成的组合物，其中的组合物可用于封闭胃肠道中的水性和/或亲水性物质，从而改善腹泻。还描述了包含这些组合物的试剂盒以及使用这些组合物和试剂盒的方法。
• Compositions, methods, and kits useful for the alleviation of gastrointestinal effects
  申请人：——

  公开号：US20040126424A1

  公开（公告）日：2004-07-01

  This disclosure relates to compositions suitable for a variety of treatments, including ameliorating the undesirable side effects associated with compounds such as lipase inhibitors (e.g., anal leakage of undigested fat or oil). In particular, one embodiment of the present invention relates to compositions that are suitable for administration to an animal for the purpose of stiffening one or more lipophilic substances present in the gastrointestinal tract of the animal. The stiffening agents have a complete melting point of about 33° C. or greater. Various kits comprising the compositions are also described herein. Also disclosed are methods of stiffening lipophilic substances present in the gastrointestinal tract of an animal are provided, wherein the methods comprise administering a composition comprising a safe and effective amount of a stiffening agent to the animal, wherein the stiffening agent is described herein and has a complete melting point of about 33° C. or greater. The methods also include those selected from treating gastrointestinal distress, treating fecal urgency, treating obesity, treating hyperlipidemia, treating diarrhea, inhibiting anal leakage, reducing levels of toxic substances, reducing blood cholesterol levels, inducing satiety, effecting weight loss, effecting weight control, treating Type II Diabetes, delaying onset of Type II Diabetes, preventing Type II Diabetes, and combinations thereof, the methods comprising administering a composition comprising a safe and effective amount of the stiffening agent to the animal, as well as a safe and effective amount of a lipase inhibitor.

  本公开涉及适用于各种治疗的组合物，包括改善与脂肪酶抑制剂等化合物相关的不良副作用（如未消化脂肪或油的肛门渗漏）。特别是，本发明的一个实施方案涉及适用于动物的组合物，其目的是使动物胃肠道中的一种或多种亲脂物质变硬。硬化剂的完全熔点约为 33 摄氏度或更高。本文还描述了包含这些组合物的各种试剂盒。 还公开了使存在于动物胃肠道中的亲脂性物质变硬的方法，其中方法包括向动物施用包含安全有效量的变硬剂的组合物，其中变硬剂如本文所述，具有约33℃或更高的完全熔点。这些方法还包括选自治疗肠胃不适、治疗排便急迫症、治疗肥胖症、治疗高脂血症、治疗腹泻、抑制肛门渗漏、降低有毒物质水平、降低血液胆固醇水平、诱导饱腹感、减轻体重、控制体重、治疗 II 型糖尿病、延缓衰老、控制体重的方法、治疗 II 型糖尿病、延迟 II 型糖尿病的发病、预防 II 型糖尿病及其组合，这些方法包括向动物施用包含安全有效量的硬化剂以及安全有效量的脂肪酶抑制剂的组合物。
• [EN] ORTHO-CARBONYL AMINO-SUBSTITUTED BENZENE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USE THEREOF<br/>[FR] DÉRIVÉ DE BENZÈNE SUBSTITUÉ PAR ORTHO-CARBONYL AMINO, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION<br/>[ZH] 一类邻位羰基氨基取代苯衍生物、其制备方法和用途
  申请人：INST MATERIA MEDICA CAMS

  公开号：WO2020199945A1

  公开（公告）日：2020-10-08

  本发明涉及医药技术领域，公开了具有式(I)所示的化合物及其制备方法、药物组合物和用途。具体的说，本发明进一步公开了含有如式(I)所示化合物、药学上可接受的盐及其药物组合物，他们能抑制人吲哚胺2，3-双加氧酶(IDO)和/或人色氨酸2，3-双加氧酶(TDO)的酶活性的作用，在制备用于治疗和/或预防与IDO/TDO活性过高或者过度表达有关的疾病或病症药物中的用途，如治疗肿瘤药物。本发明化合物具有较强的IDO抑制活性。(I)
• Process for the synthesis of 3-thio-4-quinolone derivatives and intermediate compounds for use therein, and their use as medicaments
  申请人：The Boots Company PLC

  公开号：EP0317149B1

  公开（公告）日：1991-11-06