LGD-3303 | 917891-35-1

• 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
• 英文名称: LGD-3303
• 英文别名: 9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3,6-dihydro-pyrrolo[3,2-f]quinolin-7-one；9-Chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3h-pyrrolo(3,2-f)quinolin-7(6h)-one；9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-6H-pyrrolo[3,2-f]quinolin-7-one
• CAS: 917891-35-1
• 化学式: C₁₆H₁₄ClF₃N₂O
• 分子量: 342.748
• InChiKey: OMXGOGXEWUCLFI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  34
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  (+/-)-9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoro-ethyl)-1,2,3,6-tetrahydro-pyrrolo[3,2-f]-quinolin-7-one 在 2,3-二氯-5,6-二氰基-1,4-苯醌 作用下， 以 乙酸乙酯 为溶剂， 反应 0.5h， 以62%的产率得到LGD-3303
  参考文献：
  名称：

  Androgen Receptor Modulator Compounds and Methods

  摘要：

  本文提供了结合雄激素受体和/或调节雄激素受体活性的化合物，以及制备和使用这些化合物的方法。还提供了包括这些化合物的组合物和制备和使用这些组合物的方法。

  公开号：

  US20090030027A1

文献信息

• Androgen receptor modulator compounds and methods
  申请人：Pedram Bijan

  公开号：US20120165362A1

  公开（公告）日：2012-06-28

  Provided herein are compounds that bind to androgen receptors and/or modulate activity of androgen receptors, and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.

  本文提供了结合雄激素受体和/或调节雄激素受体活性的化合物，以及制备和使用这些化合物的方法。还提供了包括这些化合物的组合物以及制备和使用这些组合物的方法。
• Methods of reducing mammographic breast density and/or breast cancer risk
  申请人：Havah Therapeutics Pty Ltd.

  公开号：US10064874B2

  公开（公告）日：2018-09-04

  The present disclosure is directed to generally methods and/or compositions for treating mammographic breast density and/or breast stiffness in a patient in need thereof, such as a pre-menopausal, a peri-menopausal or a post-memopausal patient, comprising the administration of an effective amount of androgenic agent and an effective amount of an aromatase inhibitor. The present disclosure is also directed to methods and/or compositions for reducing breast pain. The present disclosure is also directed to method and/or compositions for reducing elasticity and/or decreasing mechano-transduction on the genome of breast cells. The present disclosure is also directed to methods and/or compositions for stabilizing and/or increasing the levels of androgen receptor expression in breast tissue.

  本公开总体上涉及治疗有需要的患者（如绝经前、围绝经期或绝经后患者）的乳房X线摄影乳房密度和/或乳房僵硬的方法和/或组合物，包括施用有效量的雄激素制剂和有效量的芳香化酶抑制剂。本公开还涉及减少乳房疼痛的方法和/或组合物。本公开内容还涉及降低弹性和/或降低乳腺细胞基因组机械传导的方法和/或组合物。本公开内容还涉及稳定和/或增加乳腺组织中雄激素受体表达水平的方法和/或组合物。
• Anti-tumor therapy
  申请人：The University of Chicago

  公开号：US10421971B2

  公开（公告）日：2019-09-24

  Compositions, kits and methods for treating cancer in a subject in need thereof are disclosed involving one or more genes the suppression of which renders the cancer chemosensitive and/or radiosensitive.

  本研究公开了用于治疗所需对象癌症的组合物、试剂盒和方法，这些组合物、试剂盒和方法涉及一种或多种基因，抑制这些基因可使癌症具有化疗敏感性和/或放射敏感性。
• Prognostic and predictive breast cancer signature
  申请人：The University of Chicago

  公开号：US10679730B2

  公开（公告）日：2020-06-09

  Embodiments of the invention are directed to methods of determining the prognosis of a breast cancer patient by evaluating a specified set of genes. Specifically, methods may comprise calculating a prognosis score based on a particular algorithm. Also disclosed are compositions, kits and methods for treating cancer in a subject in need thereof are disclosed involving one or more upstream activators and/or downstream effectors of TET1.

  本发明的实施方案涉及通过评估一组特定基因来确定乳腺癌患者预后的方法。具体而言，方法可包括根据特定算法计算预后评分。本发明还公开了用于治疗癌症的组合物、试剂盒和方法，这些组合物、试剂盒和方法涉及TET1的一个或多个上游激活剂和/或下游效应物。
• Methods and compositions for the treatment of cancer cachexia
  申请人：Ohio State Innovation Foundation

  公开号：US11529323B2

  公开（公告）日：2022-12-20

  In one aspect, the disclosure relates to methods and compositions for treatment of cancer cachexia. In a further aspect, the composition is a pharmaceutical composition comprising a class I/IIB HDAC inhibitor and an androgen. In a still further aspect, the method of treatment comprises administering a class I/IIB HDAC inhibitor and an androgen to a subject or patient who has been diagnosed as having cancer cachexia. In some aspects, the class I/IIB HDAC inhibitor is a compound known as AR-42.

  在一个方面，本公开涉及治疗癌症恶病质的方法和组合物。在另一个方面，组合物是一种药物组合物，包含I/IIB类HDAC抑制剂和雄激素。在更进一步的方面，治疗方法包括向已被诊断为癌症恶病质的受试者或患者施用I/IIB类HDAC抑制剂和雄激素。在某些方面，I/IIB类HDAC抑制剂是一种称为AR-42的化合物。