5-乙酰基-3(4-氟苯基)-异噁唑 | 889938-97-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 5-乙酰基-3(4-氟苯基)-异噁唑
• 英文名称: 1-(3-(4-fluorophenyl)isoxazol-5-yl)ethanone
• 英文别名: 1-[3-(4-fluorophenyl)-1,2-oxazol-5-yl]ethanone
• CAS: 889938-97-0
• 化学式: C₁₁H₈FNO₂
• 分子量: 205.188
• InChiKey: FYOVARWWAUYDFV-UHFFFAOYSA-N

物化性质

• 沸点：
  369.1±32.0 °C(Predicted)
• 密度：
  1.232±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  43.1
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-碘吡啶 、 5-乙酰基-3(4-氟苯基)-异噁唑 在 正丁基锂 作用下， 以 四氢呋喃 为溶剂， 反应 2.17h， 以29%的产率得到3-(4-fluorophenyl)-5-(1-(pyridin-4-yl)ethyl)isoxazole
  参考文献：
  名称：

  [EN] PYRIDINE DERIVATIVES
  [FR] DÉRIVÉS PYRIDINES

  摘要：

  本申请提供了新型的吡啶化合物及其药用可接受的盐或前药。同时，还提供了制备这些化合物的方法。这些化合物通过向患者施用一种或多种化合物的治疗有效量，用于抑制CYP 17活性。通过这样做，这些化合物有效地治疗与CPY17活性相关的病症。可以使用这些化合物治疗多种病症，包括以异常细胞增殖为特征的疾病。在一个实施例中，所述疾病为癌症，如前列腺癌。

  公开号：

  WO2013049559A1
• 作为产物：
  描述：

  syn-4-氟苯甲醛肟 在 戴斯-马丁氧化剂 作用下， 以 二氯甲烷 为溶剂， 反应 20.0h， 生成 5-乙酰基-3(4-氟苯基)-异噁唑
  参考文献：
  名称：

  [EN] PYRIDINE DERIVATIVES
  [FR] DÉRIVÉS PYRIDINES

  摘要：

  本申请提供了新型的吡啶化合物及其药用可接受的盐或前药。同时，还提供了制备这些化合物的方法。这些化合物通过向患者施用一种或多种化合物的治疗有效量，用于抑制CYP 17活性。通过这样做，这些化合物有效地治疗与CPY17活性相关的病症。可以使用这些化合物治疗多种病症，包括以异常细胞增殖为特征的疾病。在一个实施例中，所述疾病为癌症，如前列腺癌。

  公开号：

  WO2013049559A1

文献信息

• [EN] IMIDAZOLE DERIVATIVES AS CYP17 INHIBITORS FOR THE TREATMENT OF CANCER<br/>[FR] DÉRIVÉS IMIDAZOLES EN TANT QU'INHIBITEURS DE CYP17 POUR LE TRAITEMENT DU CANCER
  申请人：ENDO PHARMACEUTICALS INC

  公开号：WO2013049565A1

  公开（公告）日：2013-04-04

  The present application provides novel imidazole compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP 17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.

  本申请提供了新型咪唑化合物及其药用盐。还提供了制备这些化合物的方法。通过向患者投与一种或多种化合物的治疗有效量，这些化合物对抑制CYP 17活性是有用的。通过这样做，这些化合物在治疗与CPY17活性相关的疾病方面是有效的。可以使用这些化合物治疗各种疾病，包括以异常细胞增殖为特征的疾病。在一个实施例中，该疾病是癌症，如前列腺癌。
• PYRIDINE DERIVATIVES
  申请人：Asana BioSciences, LLC

  公开号：US20170073339A1

  公开（公告）日：2017-03-16

  The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CYP17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.

  本申请提供了新型吡啶化合物及其药学上可接受的盐或前药。还提供了制备这些化合物的方法。通过向患者投入一种或多种化合物的治疗有效剂量，这些化合物可用于抑制CYP17活性。通过这样做，这些化合物可有效治疗与CYP17活性有关的疾病。这些化合物可用于治疗多种疾病，包括以异常细胞增殖为特征的疾病。在一种实施方式中，该疾病是癌症，如前列腺癌。
• Pyridine Derivatives
  申请人：Endo Pharmaceuticals Inc.

  公开号：US20130085148A1

  公开（公告）日：2013-04-04

  The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.

  本申请提供了新型吡啶化合物及其药学上可接受的盐或前药。同时还提供了制备这些化合物的方法。这些化合物可以通过向患者投予治疗有效量的一个或多个化合物来抑制CYP17活性。通过这样做，这些化合物对于治疗与CPY17活性相关的疾病是有效的。这些化合物可以用于治疗各种疾病，包括以异常细胞增殖为特征的疾病。在一个实施例中，该疾病是癌症，如前列腺癌。
• Imidazole Derivatives
  申请人：Endo Pharmaceuticals Inc.

  公开号：US20130085164A1

  公开（公告）日：2013-04-04

  The present application provides novel imidazole compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.

  本申请提供了新型咪唑化合物及其药学上可以接受的盐。还提供了制备这些化合物的方法。这些化合物可通过向患者投予治疗有效量的一个或多个化合物来抑制CYP17活性。通过这样做，这些化合物对治疗与CPY17活性相关的疾病是有效的。这些化合物可用于治疗各种疾病，包括以异常细胞增殖为特征的疾病。在一种实施例中，该疾病是癌症，如前列腺癌。
• Pyridine derivatives
  申请人：Endo Pharmaceuticals, Inc.

  公开号：US08809372B2

  公开（公告）日：2014-08-19

  The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CYP17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.

  本申请提供了新型吡啶化合物及其药学上可接受的盐或前药。还提供了制备这些化合物的方法。这些化合物可通过向患者投予治疗有效量的一个或多个化合物来抑制CYP17活性。通过这样做，这些化合物可有效治疗与CYP17活性有关的疾病。这些化合物可用于治疗多种疾病，包括以异常细胞增殖为特征的疾病。在一个实施例中，该疾病是癌症，如前列腺癌。