曲喹达佐 | 108001-60-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 曲喹达佐
• 英文名称: N-(3-nitro-4-quinolyl)-morpholino-carboxamidine
• 英文别名: N-(3-nitro-4-quinolinyl)-4-morpholinecarboxamidine；Troquidazole；N'-(3-nitroquinolin-4-yl)morpholine-4-carboximidamide
• CAS: 108001-60-1
• 化学式: C₁₄H₁₅N₅O₃
• 分子量: 301.305
• InChiKey: UUJSXEHRMRPYEX-UHFFFAOYSA-N

物化性质

• 熔点：
  228-230 °C(Solv: ethanol (64-17-5))
• 沸点：
  471.9±55.0 °C(Predicted)
• 密度：
  1.49±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  110
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  曲喹达佐 生成 4-Morpholinecarboximidamide, N-(3-nitro-4-quinolinyl)-, hydrochloride
  参考文献：
  名称：

  BERENYI, DANIELNE;VARGA, LASZLO;PALLOS, LASZLO;PETOCZ, LUJZA;LADANYI, LAS+

  摘要：

  DOI：
• 作为产物：
  描述：

  morpholine-4-carboxamidine sulfate 、 sodium ethanolate 、 4-氯-3-硝基喹啉 生成 曲喹达佐
  参考文献：
  名称：

  BERENYI, DANIELNE;VARGA, LASZLO;PALLOS, LASZLO;PETOCZ, LUJZA;LADANYI, LAS+

  摘要：

  DOI：

文献信息

• MATRIX METALLOPROTEINASE INHIBITORS
  申请人：Decicco P. Carl

  公开号：US20050025702A1

  公开（公告）日：2005-02-03

  Thus the present invention describes novel compounds comprising: 1-10 targeting moieties; a chelator (Ch); and 0-1 linking groups (Ln) between the targeting moiety and chelator; wherein the targeting moiety is a matrix metalloproteinase inhibitor; and wherein the chelator is capable of conjugating to a cytotoxic radioisotope. The present invention also provides novel compositions of the compounds of the invention, kits, and their uses in treatment of diseases associated with MMPs.

  因此，本发明描述了包括：1-10个靶向基团；一个螯合剂（Ch）；以及靶向基团和螯合剂之间的0-1个连接基团（Ln）的新化合物；其中，靶向基团是一种基质金属蛋白酶抑制剂；螯合剂能够与细胞毒性放射性同位素结合。本发明还提供了该化合物的新组合物、试剂盒以及它们在治疗与基质金属蛋白酶相关疾病中的用途。
• Vitronectin receptor antagonist pharmaceuticals
  申请人：——

  公开号：US20040014964A1

  公开（公告）日：2004-01-22

  The present invention describes novel compounds of the formula: (Q) d —L n —C h , useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.

  本发明描述了新颖化合物的公式：(Q) d-Ln-Ch，用于癌症的诊断和治疗，患者肿瘤成像方法，以及患者癌症治疗的方法。本发明还提供了新颖化合物，用于监测治疗性血管生成和新血管生成的破坏。本发明进一步提供了新颖化合物，用于成像动脉粥样硬化、再狭窄、心肌缺血和心肌再灌注损伤。本发明还提供了新颖化合物，用于类风湿性关节炎的治疗。这些药物由结合到在血管生成期间上调的受体的靶向基团、可选的连接基团和治疗有效的放射性同位素或诊断有效的可成像基团组成。可成像基团是伽马射线或正电子发射放射性同位素、磁共振成像对比剂、X射线对比剂或超声对比剂。
• Stable radiopharmaceutical compositions and methods for preparation thereof
  申请人：——

  公开号：US20020122768A1

  公开（公告）日：2002-09-05

  The present invention provides stable radiopharmaceutical compositions including a therapeutic radionuclide and an effective stabilizing amount of an aromatic stabilizer (e.g., a polyhydroxylated aromatic compound, an aromatic amine, or a hydroxylated aromatic amine), alone or in combination with other antioxidants or stabilizers, to inhibit radiolytic degradation of radiopharmaceuticals. The present invention also provides improved radiopharmaceutical formulations by the use of an aromatic stabilizing agent (e.g., a polyhydroxylated aromatic compound, an aromatic amines, or a hydroxylated aromatic amine), and/or low temperature storage. The present invention also provides processes for making stable radiopharmaceutical compositions. The present invention also provides the use of the pharmaceutical compositions in medical therapy and/or medical diagnosis.

  本发明提供了稳定的放射性药物组合物，包括治疗性放射性核素和有效稳定剂量的芳香稳定剂（例如，多羟基芳香化合物、芳香胺或羟基芳香胺），单独或与其他抗氧化剂或稳定剂组合使用，以抑制放射性降解。本发明还通过使用芳香稳定剂（例如，多羟基芳香化合物、芳香胺或羟基芳香胺）和/或低温储存来提供改进的放射性药物配方。本发明还提供制备稳定的放射性药物组合物的方法。本发明还提供在医疗治疗和/或医疗诊断中使用药物组合物的用途。
• Matrix metalloproteinase inhibitors and uses thereof
  申请人：Bristol-Myers Squibb Pharma Company

  公开号：EP1772452A2

  公开（公告）日：2007-04-11

  The present invention describes novel compounds comprising: 1-10 targeting moieties; a chelator (Ch); and 0-1 linking groups (Ln) between the targeting moiety and chelator; wherein the targeting moiety is a matrix metalloproteinase inhibitor; and wherein the chelator is capable of conjugating to a cytotoxic radioisotope. The present invention also provides novel compositions of the compounds of the invention, kits, and their uses in treatment of diseases associated with MMPs.

  本发明描述的新型化合物包括1-10个靶向分子；螯合剂（Ch）；以及靶向分子和螯合剂之间的0-1个连接基团（Ln）；其中靶向分子是基质金属蛋白酶抑制剂；以及螯合剂能够与细胞毒性放射性同位素共轭。本发明还提供了本发明化合物的新型组合物、试剂盒及其在治疗与 MMPs 相关疾病中的用途。
• Pharmaceuticals for the imaging of angiogenic disorders
  申请人：——

  公开号：US20030180305A1

  公开（公告）日：2003-09-25

  The present invention describes novel compounds of the formula: (Q) d —L n —C h , useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.

  本发明描述了式中的新型化合物： (Q) d -L n -C h , 用于诊断和治疗癌症、患者肿瘤成像方法和患者癌症治疗方法。本发明还提供了用于监测治疗性血管生成治疗和新血管生成血管破坏的新型化合物。这些药物由与血管生成过程中上调的受体结合的靶向分子、任选连接基团和治疗有效的放射性同位素或诊断有效的可成像分子组成。可成像分子是伽马射线或正电子发射的放射性同位素、磁共振成像造影剂、X 射线造影剂或超声造影剂。