3-(6-Amino-3H-isobenzofuran-1-ylidene)-5-chloro-1,3-dihydro-indol-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 3-(6-Amino-3H-isobenzofuran-1-ylidene)-5-chloro-1,3-dihydro-indol-2-one
• 英文别名: 3-(6-amino-3H-isobenzofuran-1-ylidene)-5-chloro-1,3-dihydroindol-2-one；(3E)-3-(6-amino-3H-2-benzofuran-1-ylidene)-5-chloro-1H-indol-2-one
• 化学式: C₁₆H₁₁ClN₂O₂
• 分子量: 298.729
• InChiKey: LEVMONLZKBUYCH-CCEZHUSRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  21
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  64.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  溴代乙酸酐 、 3-(6-Amino-3H-isobenzofuran-1-ylidene)-5-chloro-1,3-dihydro-indol-2-one 以 四氢呋喃 为溶剂， 以94%的产率得到2-bromo-N-[3-(5-chloro-2-oxo-1,2-dihydro-indol-3-ylidene)-1,3-dihydro-isobenzofuran-5-yl]-acetamide
  参考文献：
  名称：

  (3Z)-3-(2,3-dihydro-1H-inden-1-ylidene)-1,3-dihydro-2H-indol-2-ones as kinase inhibitors

  摘要：

  本发明涉及有机分子，能够调节酪氨酸激酶信号传导，以调控、调节和/或抑制异常细胞增殖。

  公开号：

  US20040019098A1
• 作为产物：
  描述：

  5-氯氧化吲哚 、 6-氨基四氯苯酞 在 盐酸 、 Sodium hexamethyldisilazane 作用下， 以 四氢呋喃 、 乙二醇二甲醚 为溶剂， 以39%的产率得到3-(6-Amino-3H-isobenzofuran-1-ylidene)-5-chloro-1,3-dihydro-indol-2-one
  参考文献：
  名称：

  (3Z)-3-(2,3-dihydro-1H-inden-1-ylidene)-1,3-dihydro-2H-indol-2-ones as kinase inhibitors

  摘要：

  本发明涉及有机分子，能够调节酪氨酸激酶信号传导，以调控、调节和/或抑制异常细胞增殖。

  公开号：

  US20040019098A1

文献信息

• Methods and compositions for intraocular administration to treat ocular conditions
  申请人：ALLERGAN, INC.

  公开号：EP2583679A1

  公开（公告）日：2013-04-24

  Anti-angiogenesis compositions, and methods of using such compositions, useful for injection into the vitreous of human eyes are provided. Such compositions can include TKI component solutions or particles present in a therapeutically effective amount, a viscosity inducing component, and an aqueous carrier component. The compositions have viscosities at about 25° C. of at least about 10 cps or about 100 cps at a shear rate of 0.1/second. In a preferred embodiment, the viscosity at 25° C. is in the range of from about 80,000 cps to about 300,000 cps.

  本研究提供了可用于注射到人眼玻璃体内的抗血管生成组合物和使用此类组合物的方法。此类组合物可包括治疗有效量的 TKI 成分溶液或颗粒、粘度诱导成分和水性载体成分。在 0.1/秒的剪切速率下，组合物在约 25° C 时的粘度至少为约 10 cps 或约 100 cps。在一个优选的实施方案中，25° C 时的粘度范围为约 80,000 cps 至约 300,000 cps。
• Biodegradable intravitreal tyrosine kinase implants
  申请人：Allergan, Inc.

  公开号：US10076492B2

  公开（公告）日：2018-09-18

  Biocompatible intraocular implants include a tyrosine kinase inhibitor and a biodegradable polymer that is effective to facilitate release of the tyrosine kinase inhibitor into the vitreous of an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants can be placed in an eye to treat or reduce the occurrence of one or more ocular conditions.

  生物相容性眼内植入物包括一种酪氨酸激酶抑制剂和一种可生物降解的聚合物，这种聚合物能有效促进酪氨酸激酶抑制剂在眼球玻璃体内长时间释放。植入物的治疗剂可与生物可降解聚合物基质相关联，如基本不含聚乙烯醇的基质。可将植入物植入眼内，以治疗或减少一种或多种眼部疾病的发生。
• Sustained release intraocular implants containing tyrosine kinase inhibitors and related methods
  申请人：Hughes M. Patrick

  公开号：US20050244470A1

  公开（公告）日：2005-11-03

  Biocompatible intraocular implants include a tyrosine kinase inhibitor and a biodegradable polymer that is effective to facilitate release of the tyrosine kinase inhibitor into an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions.

  生物相容性眼内植入物包括酪氨酸激酶抑制剂和生物可降解聚合物，后者可有效促进酪氨酸激酶抑制剂在眼内的长期释放。植入物的治疗剂可与生物可降解聚合物基质相关联，如基本不含聚乙烯醇的基质。植入物可植入眼内，以治疗或减少一种或多种眼部疾病的发生。
• Tyrosine kinase microsphers
  申请人：Hughes M. Patrick

  公开号：US20050244477A1

  公开（公告）日：2005-11-03

  Biocompatible intraocular microspheres include a tyrosine kinase inhibitor and a biodegradable polymer that is effective to facilitate release of the tyrosine kinase inhibitor into the vitreous of an eye for an extended period of time. The therapeutic agents of the microspheres can be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The microspheres can be placed into an eye to treat or reduce the occurrence of one or more ocular conditions.

  生物相容性眼内微球包括一种酪氨酸激酶抑制剂和一种可生物降解的聚合物，可有效促进酪氨酸激酶抑制剂在眼球玻璃体内的长时间释放。微球中的治疗剂可与可生物降解的聚合物基质结合，如基本不含聚乙烯醇的基质。将微球放入眼内可治疗或减少一种或多种眼部疾病的发生。
• (3Z)-3-(3-HYDRO-ISOBENZOFURAN-1-YLIDENE)-1,3-DIHYDRO-2H-INDOL-2-ONES AS KINASE INHIBITORS
  申请人：Allergan, Inc.

  公开号：EP1490356A1

  公开（公告）日：2004-12-29