3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxide | 33047-95-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 英文名称: 3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxide
• 英文别名: Dihydrobenzothiazindioxide；3,4-dihydro-2H-1λ6,2-benzothiazine 1,1-dioxide
• CAS: 33047-95-9
• 化学式: C₈H₉NO₂S
• 分子量: 183.231
• InChiKey: VSCYCJOVRGSJBT-UHFFFAOYSA-N

物化性质

• 沸点：
  342.2±45.0 °C(Predicted)
• 密度：
  1.319±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  54.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxide 在 硝酸 作用下， 生成 2,7-dinitro-3,4-dihydro-2H-benzo[e][1,2]thiazine 1,1-dioxide
  参考文献：
  名称：

  Sianesi,E. et al., Chemische Berichte, 1971, vol. 104, p. 1880 - 1891

  摘要：

  DOI：

文献信息

• Inhibitors of bruton's tyrosine kinase
  申请人：Kondru Rama K.

  公开号：US20100016302A1

  公开（公告）日：2010-01-21

  This application discloses 6-Phenyl-imidazo[1,2-a]pyrazine derivatives according to generic Formulae I-V: wherein, variables Q, R, Y 1 , Y 2 , Y 3 , Y 4 , n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.

  该应用程序根据通用公式I-V 揭示了6-苯基咪唑并[1,2-a]吡嗪衍生物： 其中，变量Q、R、Y1、Y2、Y3、Y4、n 和m 如本文所述定义，这些衍生物抑制Btk。本文所披露的化合物可用于调节Btk 的活性并治疗与过度Btk 活性相关的疾病。这些化合物进一步可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，如类风湿性关节炎。还披露了包含公式I-V 化合物和至少一种载体、稀释剂或赋形剂的组合物。
• INHIBITORS OF BURTON'S TYROSINE KINASE
  申请人：Dewdney Nolan James

  公开号：US20100004231A1

  公开（公告）日：2010-01-07

  This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y 1 , Y 2 , Y 2′ , Y 3 , Y 4 , n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.

  该申请披露了根据通用式I-V的5-苯基-1H-吡嗪-2-酮衍生物：其中，变量Q、R、Y1、Y2、Y2'、Y3、Y4、n和m的定义如本文所述，这些衍生物抑制Btk。本文披露的化合物可用于调节Btk的活性并治疗与Btk活性过高有关的疾病。这些化合物进一步可用于治疗与异常B细胞增殖相关的炎症和自身免疫疾病，如类风湿性关节炎。还披露了包含通用式I-V化合物和至少一种载体、稀释剂或赋形剂的组合物。
• [EN] ANALOGS OF FEXARAMINE AND METHODS OF MAKING AND USING<br/>[FR] ANALOGUES DE LA FÉXARAMINE ET PROCÉDÉS DE PRÉPARATION ET D'UTILISATION
  申请人：SALK INST FOR BIOLOGICAL STUDI

  公开号：WO2015138969A1

  公开（公告）日：2015-09-17

  Novel compounds having a formula embodiments of a method of making the same, and of a composition comprising them are disclosed herein. Also disclosed are embodiments of a method of treating or preventing a metabolic disorder in a subject, comprising administering to a subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and treating or preventing a metabolic disorder in the subject. Additionally disclosed are embodiments of a method of treating or preventing inflammation in an intestinal region of a subject, comprising administering to the subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and thereby treating or preventing inflammation in the intestinal region of the subject.

  揭示了具有化合物配方实施例的小说化合物，制备方法的实施例，以及包含它们的组合物。还揭示了一种治疗或预防受试者代谢紊乱的方法实施例，包括向受试者（例如，通过胃肠道）施用所述化合物的一种或多种治疗有效量，从而激活肠道中的FXR受体，并治疗或预防受试者的代谢紊乱。此外还揭示了一种治疗或预防受试者肠道区域炎症的方法实施例，包括向受试者（例如，通过胃肠道）施用所述化合物的一种或多种治疗有效量，从而激活肠道中的FXR受体，并治疗或预防受试者肠道区域的炎症。
• Method of treating diseases and conditions associated with an altered level of amyloid beta peptides and new enolcarboxamide compounds
  申请人：Bornemann Klaus

  公开号：US20050277635A1

  公开（公告）日：2005-12-15

  A method of treating or preventing of a disease or condition associated with an increased level of isoforms of amyloid β peptides (Aβ) and/or with a changed ratio of levels of Aβ isoforms and/or with the formation of plaques containing amyloid β peptide (Aβ) isoforms in a mammal comprising administering to said mammal an therapeutically effective amount of a compound selected from the formulas Ia, Ib wherein V, W, Y, R 2 , R 3 , R 5 , R 6 , L1 and i are defined as in claim 1.

  一种治疗或预防与哺乳动物中淀粉样β肽（Aβ）异构体水平增加、Aβ异构体水平比例改变和/或含有Aβ肽的斑块形成有关的疾病或病症的方法，包括向该哺乳动物投与公式Ia、Ib中选定的化合物的治疗有效量，其中V、W、Y、R2、R3、R5、R6、L1和i的定义如权利要求1所述。
• N,N'-substituted-1,3-diamino-2-hydroxypropane derivatives
  申请人：——

  公开号：US20040171881A1

  公开（公告）日：2004-09-02

  Disclosed are compounds of the formula 1 wherein the variables R N , R C , R 1 , R 25 , R 2 , and R 3 are as defined herein. These compounds have activity as inhibitors of beta-secretase and are therefore useful in treating a variety of discorders such as Alzheimer's Disease.

  本文披露了式1的化合物，其中变量RN、RC、R1、R25、R2和R3的定义如本文所述。这些化合物具有抑制β-分泌酶的活性，因此可用于治疗多种疾病，如阿尔茨海默病。