thieno<2,3-c>isoquinoline | 7078-18-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 英文名称: thieno<2,3-c>isoquinoline
• 英文别名: Thieno[2,3-c]isoquinoline
• CAS: 7078-18-4
• 化学式: C₁₁H₇NS
• 分子量: 185.249
• InChiKey: PKHHCZYTAHQZJN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  41.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  2-甲酰基苯硼酸 、 (3-碘噻吩-2-基)氨基甲酸叔丁酯 在 四(三苯基膦)钯 盐酸 、 sodium carbonate 作用下， 生成 thieno<2,3-c>isoquinoline
  参考文献：
  名称：

  Yang, Youhua; Hoernfeldt, Anna-Britta; Gronowitz, Salo, Journal of Heterocyclic Chemistry, 1989, vol. 26, p. 865 - 868

  摘要：

  DOI：

文献信息

• Macrocyclic Compounds As Antiviral Agents
  申请人：Harper Steven

  公开号：US20100183551A1

  公开（公告）日：2010-07-22

  A class of macrocyclic compounds of formula (I), wherein R 1 , R 3 , R 4 , R a , R b , A, Z, Y, X, M, W, n and m are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes 5 for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection. Formula (I):

  提供一类宏环化合物的化学式（I），其中R1、R3、R4、Ra、Rb、A、Z、Y、X、M、W、n和m如下所定义，这些化合物可作为病毒蛋白酶的抑制剂，特别是对乙型肝炎病毒（HCV）NS3蛋白酶的抑制剂。还提供了合成和使用这类宏环化合物用于治疗或预防HCV感染的方法。化学式（I）：
• Thieno[2,3-c] isoquinolines for use as inhibitors of PARP
  申请人：Pellicciari Roberto

  公开号：US20060094746A1

  公开（公告）日：2006-05-04

  The present invention relates to compounds for the inhibition of poly(ADP-ribose) polymerase (PARP). In some embodiments, the compounds have the Formula: wherein the constituent variables are as defined herein. The invention further provides methods for the use of the compounds disclosed herein.

  本发明涉及用于抑制聚(ADP-核糖)聚合酶（PARP）的化合物。在某些实施例中，该化合物具有以下式子：其中组成变量如本文所定义。本发明还提供了使用所披露的化合物的方法。
• THERAPEUTIC BENEFIT OF SUBOPTIMALLY ADMINISTERED CHEMICAL COMPOUNDS
  申请人：BROWN Dennis M.

  公开号：US20160045502A1

  公开（公告）日：2016-02-18

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to mustard-based alkylating agents such as uracil mustard and analogs, derivatives, or prodrugs thereof, including 6-methyluracil mustard and 6-ethyluracil mustard.

  本发明描述了一种改善先前受到治疗性能不佳限制的治疗剂的治疗效果的方法和组合物，通过改善单药疗法的功效或减少副作用。这种方法和组合物特别适用于芥子碱基烷基化剂，例如尿嘧啶芥和其类似物、衍生物或前药，包括6-甲基尿嘧啶芥和6-乙基尿嘧啶芥。
• Thieno(2,3-C) Isoquinolines for use as inhibitors of Parp
  申请人：SMITHKLINE BEECHAM PLC

  公开号：EP1464646A1

  公开（公告）日：2004-10-06

  Heterocyclic derivatives, including derivatives of thieno[2,3-c]isoquinolin-3-one and their use in therapy as inhibitors of poly(ADP-ribose) polymerase (PARP), for use in the prevention and treatment of tissue damage due to ischaemia and reperfusion, degenerative diseases, inflammatory diseases, tumour diseases, leukaemia and/or sarcoma.

  杂环衍生物，包括噻吩并[2,3-c]异喹啉-3-酮的衍生物及其作为多（ADP-核糖）聚合酶（PARP）抑制剂的治疗用途，用于预防和治疗缺血和再灌注、退行性疾病、炎症性疾病、肿瘤疾病、白血病和/或肉瘤引起的组织损伤。
• Use of substituted hexitols including dianhydrogalactitol and analogs to treat neoplastic disease and cancer stem and cancer stem cells including glioblastoma multiforme and medulloblastoma
  申请人：Del Mar Pharmaceuticals (BC) Ltd.

  公开号：US10201521B2

  公开（公告）日：2019-02-12

  The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of glioblastoma multiforme and medulloblastoma. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N7 methylation. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is active against tumors that are refractory to temozolomide; the drug acts independently of the MGMT repair mechanism.

  二氢半乳糖醇的使用为治疗多形性胶质母细胞瘤和髓母细胞瘤提供了一种新的治疗方法。二氢半乳糖醇是一种 DNA 烷基化剂，可产生 N7 甲基化。Dianhydrogalactitol 能有效抑制癌症干细胞的生长，并对替莫唑胺难治性肿瘤有效；该药物的作用不受 MGMT 修复机制的影响。