1-(4,4',4''-trichloro-trityl)-1H-imidazole | 37594-47-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: 1-(4,4',4''-trichloro-trityl)-1H-imidazole
• 英文别名: N-([4,4',4"]-Trichlorotrityl)imidazole；1-[Tris(4-chlorophenyl)methyl]imidazole
• CAS: 37594-47-1
• 化学式: C₂₂H₁₅Cl₃N₂
• 分子量: 413.733
• InChiKey: SUDWSRXQRMDEIB-UHFFFAOYSA-N

物化性质

• 沸点：
  522.2±45.0 °C(Predicted)
• 密度：
  1.28±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  6.7
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  17.8
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  咪唑 、 4,4',4'-三氯三苯甲基乙醇 、 N-三苯甲基咪唑 在 三氟甲磺酸三甲基硅酯 作用下， 以 二氯甲烷 为溶剂， 生成 1-(4,4',4''-trichloro-trityl)-1H-imidazole
  参考文献：
  名称：

  Treatment of GLC1A glaucoma with non-steroidal glucocorticoid antagonists

  摘要：

  非甾体糖皮质激素拮抗剂的组合物，用于治疗GLC1A型青光眼的方法已被披露。

  公开号：

  US06051573A1

文献信息

• [EN] PHARMACEUTICAL COMPOSITIONS AND METHODS<br/>[FR] COMPOSITIONS PHARMACEUTIQUES ET MÉTHODES
  申请人：POP TEST ONCOLOGY LLC

  公开号：WO2017023694A1

  公开（公告）日：2017-02-09

  This invention relates the use of Cortisol blockers (e.g., glucocorticoid receptor [GR] antagonists) for the treating or preventing viral infections, treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.

  本发明涉及使用皮质醇阻断剂（例如，糖皮质激素受体[GR]拮抗剂）用于治疗或预防病毒感染，治疗或预防难治性前列腺癌，治疗或预防肿瘤，以及治疗或预防与急性或慢性损伤或疾病相关的感染。
• Pharmaceutical combination of a glucocorticoid receptor antagonist and a cortisol synthesis inhibitor for treating cushing's syndrome
  申请人：Laboratoire HRA Pharma

  公开号：EP2532350A1

  公开（公告）日：2012-12-12

  The invention relates to a method for treating Cushing's syndrome in a patient, which method comprises administering the patient with a pharmaceutical composition comprising a glucocorticoid receptor antagonist, at least twice a day, or an extended-release composition of a glucocorticoid receptor antagonist, or a combination of a glucocorticoid receptor antagonist and a inhibitor of cortisol synthesis.

  本发明涉及一种治疗患者库欣综合征的方法，该方法包括给患者服用一种药物组合物，该药物组合物包含一种糖皮质激素受体拮抗剂，每天至少服用两次，或一种糖皮质激素受体拮抗剂的缓释组合物，或一种糖皮质激素受体拮抗剂和一种皮质醇合成抑制剂的组合物。
• Concomitant administration of glucocorticoid receptor modulators and CYP3A inhibitors
  申请人：Corcept Therapeutics, Inc.

  公开号：US10195214B2

  公开（公告）日：2019-02-05

  Applicant provides methods of treating diseases including Cushing's syndrome and hormone-sensitive cancers by concomitant administration of a glucocorticoid receptor antagonist (GRA) and steroidogenesis inhibitors, and by concomitant administration of a GRA and CYP3A inhibitors. Applicant provides methods of treating diseases including Cushing's syndrome and hormone-sensitive cancers by concomitant administration of mifepristone and ketoconazole. Subjects treated with CYP3A inhibitors or steroidogenesis inhibitors may suffer from toxicity or other serious adverse reactions; concomitant administration of other drugs would be expected to increase the risk of such toxicity and adverse reactions. Applicant has surprisingly found that GRAs may be administered to subjects receiving CYP3A inhibitors or steroidogenesis inhibitors such as ketoconazole without increasing risk adverse reactions; for example, Applicant has found that mifepristone may be concomitantly administered with ketoconazole (a CYP3A inhibitor and a steroidogenesis inhibitor), providing safe concomitant administration of the GRA and ketoconazole. In embodiments, the GRA dose may be reduced.

  申请人提供了通过同时服用糖皮质激素受体拮抗剂（GRA）和类固醇生成抑制剂，以及同时服用GRA和CYP3A抑制剂来治疗包括库欣综合征和激素敏感性癌症在内的疾病的方法。申请人提供了通过同时服用米非司酮和酮康唑治疗包括库欣综合征和激素敏感性癌症在内的疾病的方法。 接受 CYP3A 抑制剂或类固醇生成抑制剂治疗的受试者可能会出现毒性或其他严重的不良反应；同时服用其他药物预计会增加这种毒性和不良反应的风险。申请人令人惊奇地发现，GRA 可用于接受 CYP3A 抑制剂或类固醇生成抑制剂（如酮康唑）的受试者，而不会增加不良反应的风险；例如，申请人发现米非司酮可与酮康唑（一种 CYP3A 抑制剂和一种类固醇生成抑制剂）同时给药，提供 GRA 和酮康唑的安全同时给药。在实施例中，可减少 GRA 的剂量。
• Pharmaceutical compositions and methods
  申请人：Pop Test Oncology LLC

  公开号：US10238666B2

  公开（公告）日：2019-03-26

  This invention relates the use of cortisol blockers (e.g., glucocorticoid receptor [GR] antagonists) for the treating or preventing viral infections, treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.

  本发明涉及皮质醇阻断剂（如糖皮质激素受体[GR]拮抗剂）在治疗或预防病毒感染、治疗或预防耐药前列腺癌、治疗或预防肿瘤以及治疗或预防与急性或慢性损伤或疾病相关的感染方面的用途。
• Glucocorticoid blocking agents for increasing blood-brain barrier permeability
  申请人：——

  公开号：US20020065259A1

  公开（公告）日：2002-05-30

  Glucocorticoid blockers, including glucocorticoid receptor antagonists, are effective to prevent glucocorticoid-induced decrease in permeability of the blood-brain barrier and to increase the permeability of the blood-brain barrier. Administration of glucocorticoid blockers, including glucocorticoid receptor antagonists, concomitant with administration of drugs for treating diseases of the central nervous system increases delivery of such drugs into the central nervous system.

  糖皮质激素受体阻滞剂，包括糖皮质激素受体拮抗剂，可有效防止糖皮质激素引起的血脑屏障通透性降低，并增加血脑屏障的通透性。在服用治疗中枢神经系统疾病的药物的同时服用糖皮质激素阻断剂，包括糖皮质激素受体拮抗剂，可增加这些药物进入中枢神经系统的剂量。