恩氯米芬盐酸盐 | 14158-65-7

• 物质功能分类: 有机原料 - 羧酸类化合物及衍生物
• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 中文名称: 恩氯米芬盐酸盐
• 英文名称: trans-Clomiphene Hydrochloride
• 英文别名: 2-[4-[(E)-2-chloro-1,2-diphenylethenyl]phenoxy]-N,N-diethylethanamine;hydrochloride
• CAS: 14158-65-7
• 化学式: C26H29Cl2NO
• mdl: MFCD08060093
• 分子量: 442.4
• InChiKey: KKBZGZWPJGOGJF-BTKVJIOYSA-N

物化性质

• 熔点：
  156.6-158 °C
• 溶解度：
  在水中的溶解度为10mg/mL，澄清

计算性质

• 辛醇/水分配系数(LogP)：
  6.47
• 重原子数：
  30
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  12.5
• 氢给体数：
  1
• 氢受体数：
  2

制备方法与用途

用途

恩氯米芬盐酸盐可用于卵巢功能障碍、睾酮缺乏、男性性腺功能减退症和2型糖尿病的相关研究。

作用

恩氯米芬盐酸盐是一种有效的可口服非甾体雌激素受体拮抗剂，具有显著的抗雌激素作用。

文献信息

• Trans-Clomiphene Formulations and Uses Thereof
  申请人：REPROS THERAPEUTICS INC.

  公开号：US20150202167A1

  公开（公告）日：2015-07-23

  The present invention provides iraws-clomiphene and pharmaceutically acceptable salts and solvates thereof, characterized in that trans-clomiphene is in particulate form having a specific size range. The invention is also directed to pharmaceutical compositions comprising or formulated using trans-clomiphene or pharmaceutically acceptable salts and solvates having a specified size range and their use in treating disorders including secondary hypogonadism, type 2 diabetes, elevated cholesterol, elevated triglycerides, wasting, lipodystrophy, female and male infertility, benign prostate hypertrophy, prostate cancer, breast cancer, ovarian cancer and endometrial cancer.

  本发明提供了具有特定粒度范围的颗粒状反式克罗米芬和药学上可接受的盐和溶剂化物，该发明还涉及包含或制备使用具有特定粒度范围的反式克罗米芬或药学上可接受的盐和溶剂化物的药物组合物，并将其用于治疗包括继发性性腺功能减退症、2型糖尿病、高胆固醇、高甘油三酯、消耗症、脂肪萎缩症、女性和男性不孕症、良性前列腺增生、前列腺癌、乳腺癌、卵巢癌和子宫内膜癌等疾病。
• Methods and compositions with trans-clomiphene for treating wasting and lipodystrophy
  申请人：ZONAGEN, INC.

  公开号：US20040171697A1

  公开（公告）日：2004-09-02

  The present invention discloses compositions and methods useful for treating wasting, especially a loss of muscle mass. The present invention also discloses compositions and methods useful for treating lipodystrophy. The compositions and methods of the present invention are particularly beneficial to HIV-infected individuals.

  本发明公开了用于治疗消瘦，特别是肌肉质量丧失的组合物和方法。本发明还公开了用于治疗脂肪营养不良的组合物和方法。本发明的组合物和方法尤其有益于艾滋病毒感染者。
• DOSING REGIMES FOR TRANS-CLOMIPHENE
  申请人：Podolski Joseph S.

  公开号：US20090215907A1

  公开（公告）日：2009-08-27

  The present invention relates to the use of compositions comprising trans-clomiphene for treating men with hypogonadism. The invention is also directed to methods for treating males with hypogonadism and disorders related thereto, including reduction of muscle mass, limitation of body performance capacity, reduction of bone density, reduction of libido, reduction of potency, reduction of benign prostatic hyperplasia and infertility.
• Trans-Clomiphene for Metabolic Syndrome
  申请人：van As Andrew

  公开号：US20120022167A1

  公开（公告）日：2012-01-26

  The present invention relates to the administration of compositions comprising an antiestrogen, preferably trans-clomiphene, for treating metabolic syndrome in a subject. The invention is also directed to methods for reducing fasting glucose levels in a subject by administering a composition comprising an antiestrogen, preferably trans-clomiphene.
• TRANS-CLOMIPHENE METABOLITES AND USES THEREOF
  申请人：Podolski Joseph S.

  公开号：US20140163114A1

  公开（公告）日：2014-06-12

  The present invention relates to substantially pure metabolites of irara-clomiphene. The invention is also directed to pharmaceutical compositions comprising these metabolites and their use in treating disorders including secondary hypogonadism, type 2 diabetes, elevated cholesterol, elevated triglycerides, wasting, lipodystrophy, female and male infertility, benign prostate hypertrophy, prostate cancer, breast cancer, ovarian cancer and endometrial cancer.