4-acetyl-2,3,5,6-tetrahydro-1,4-thiazine 1,1-dioxine | 23863-20-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻嗪类
• 英文名称: 4-acetyl-2,3,5,6-tetrahydro-1,4-thiazine 1,1-dioxine
• 英文别名: 4-Acetylthiomorpholin-1,1-dioxid；4-acetyl-thiomorpholine 1,1-dioxide；1-(1,1-Dioxidothiomorpholino)ethanone；1-(1,1-dioxo-1,4-thiazinan-4-yl)ethanone
• CAS: 23863-20-9
• 化学式: C₆H₁₁NO₃S
• 分子量: 177.224
• InChiKey: ZIXYYCBQOVEADB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.1
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  62.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  N-acetylthiomorpholine 在 双氧水 作用下， 以 乙酸酐 、 溶剂黄146 为溶剂， 生成 4-acetyl-2,3,5,6-tetrahydro-1,4-thiazine 1,1-dioxine
  参考文献：
  名称：

  Maillard,J. et al., Chimica Therapeutica, 1969, vol. 4, p. 80 - 88

  摘要：

  DOI：

文献信息

• Bicyclic pyrrolyl amides as glucogen phosphorylase inhibitors
  申请人：——

  公开号：US20030232875A1

  公开（公告）日：2003-12-18

  Heterocyclic amide derivatives, of formula (I): wherein —X-Y-Z- is selected from —S—CR 4 ═CR 5 —, —CR 4 ═CR 5 —S—, —O—CR 4 ═CR 5 —, —CR 4 ═CR 5 —O—, —N═CR 4 —S—, —S—CR 4 ═N—, —NR 6 —CR 4 ═CR 5 — and —CR 4 ═CR 5 —NR 6 —; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof; (with provisos); possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.

  杂环酰胺衍生物的化学式（I）：其中—X-Y-Z-选择自—S—CR4═CR5—，—CR4═CR5—S—，—O—CR4═CR5—，—CR4═CR5—O—，—N═CR4—S—，—S—CR4═N—，—NR6—CR4═CR5—和—CR4═CR5—NR6—；或其药学上可接受的盐或体内可水解酯；（附带条件）；具有糖原磷酸化酶抑制活性，因此在治疗与糖原磷酸化酶活性增加相关的疾病状态中具有价值。描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。
• [EN] TETRAHYDROISOQUINOLINE DERIVED PRMT5-INHIBITORS<br/>[FR] INHIBITEURS DE PRMT5 DÉRIVÉS DE TÉTRAHYDROISOQUINOLÉINE
  申请人：CTXT PTY LTD

  公开号：WO2016034673A1

  公开（公告）日：2016-03-10

  A compound of formula I wherein: n is 1 or 2: p is 0 or 1; R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.

  式I的化合物，其中：n为1或2；p为0或1；R1可选地为一个或多个卤素或甲基基团；R2a和R2b分别选自以下组：(i) F；(ii) H；(iii) Me；和(iv) CH2OH；R2c和R2d分别选自以下组：(i) F；(ii) H；(iii) Me；和(iv) CH2OH；R3a和R3b分别选自H和Me；R4为H或Me；R5为H或Me；R6a和R6b分别选自H和Me；A为(i)可选地取代的苯基；(ii)可选地取代的萘基；或(iii)可选地取代的C5-12杂环基。
• GPR40 AGONISTS IN ANTI-DIABETIC DRUG COMBINATIONS
  申请人：Janssen Pharmaceutica NV

  公开号：US20170290800A1

  公开（公告）日：2017-10-12

  Disclosed are compositions comprising (a) a GPR40 agonist and (b) an SGLT2 inhibitor, and methods for treating of disorders that are affected by the modulation of the GPR40 receptor and SGLT2 transporter. Such GPR40 compounds are represented by Formula (I) as follows: wherein ring W, R 1 , R 2 , R 3 , R 5 , R 6 , A, and Z, are defined herein.

  本文披露了包含（a）GPR40激动剂和（b）SGLT2抑制剂的组合物，以及治疗受GPR40受体和SGLT2转运蛋白调节影响的疾病的方法。这些GPR40化合物由以下式（I）表示： 其中环W，R1，R2，R3，R5，R6，A和Z在此处被定义。
• [EN] BENZIMIDAZOLES FOR USE IN THE TREATMENT OF CANCER AND INFLAMMATORY DISEASES<br/>[FR] BENZIMIDAZOLES POUR UNE UTILISATION DANS LE TRAITEMENT DU CANCER ET DES MALADIES INFLAMMATOIRES
  申请人：CAPELLA THERAPEUTICS INC

  公开号：WO2017053537A1

  公开（公告）日：2017-03-30

  Provided herein are methods for treating, preventing, or ameliorating one or more symptoms of a condition, disorder, or disease mediated by a lipid kinase or a protein kinase with benzimidazoles, for example, of Formula I or II, and pharmaceutical compositions thereof. Also provided herein are benzimidazoles, and pharmaceutical compositions thereof; and methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.

  本文提供了使用苯并咪唑类化合物治疗、预防或改善由脂质激酶或蛋白激酶介导的疾病、紊乱或症状的方法，例如公式I或II的苯并咪唑类化合物及其药物组合物。本文还提供了苯并咪唑类化合物及其药物组合物，以及它们用于治疗、预防或改善增生性疾病症状的方法。
• 2,3,4,9-Tetrahydro-1H-carbazoles
  申请人：Bayer Schering Pharma Aktiengesellschaft

  公开号：EP1975159A1

  公开（公告）日：2008-10-01

  The present invention relates to 2,3,4,9-tetrahydro-1 H-carbazoles of the general formula I, in which Q, X, W, R1, R2, R3, R4 and R5 have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.

  本发明涉及通式I的2,3,4,9-四氢-1H-咔唑， 其中Q、X、W、R1、R2、R3、R4和R5的含义如描述中所定义。 根据本发明的化合物是有效的FSH拮抗剂，可用于男性或女性的生育控制，或用于骨质疏松症的预防和/或治疗。

表征谱图