17-Pyrimidinylandrostane

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: 17-Pyrimidinylandrostane
• 英文别名: 2-[(8R,9S,10S,13S,14S)-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pyrimidine
• 化学式: C₂₃H₃₄N₂
• 分子量: 338.5
• InChiKey: FDDWDOPVPCHNMU-SXUIBZKYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7
• 重原子数：
  25
• 可旋转键数：
  1
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• Estra-1,3,5(10),16-tetraene-3-carboxamide derivatives, processes for their preparation, pharmaceutical preparations comprising them and their use for preparing medicaments
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20140249119A1

  公开（公告）日：2014-09-04

  The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis.

  这项发明涉及AKR1C3抑制剂以及它们的制备过程，以及它们用于治疗和/或预防疾病的用途，还包括它们用于制备用于治疗和/或预防疾病的药物，特别是出血性疾病和子宫内膜异位症。
• ESTRA-1,3,5(10),16-TETRAENE-3-CARBOXAMIDES FOR INHIBITION OF 17.BETA.-HYDROXYSTEROID DEHYDROGENASE (AKR1 C3)
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20160024142A1

  公开（公告）日：2016-01-28

  The invention relates to AKR1C3 inhibitors of formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of bleeding disorders and endometriosis.

  该发明涉及式(I)的AKR1C3抑制剂，以及其制备方法，用于治疗和/或预防疾病，以及用于生产治疗和/或预防疾病的药物，特别是出血性疾病和子宫内膜异位症。
• 3-SUBSTITUTED ESTRA-1,3,5(10),16-TETRAENE DERIVATIVES, METHODS FOR THE PRODUCTION THEREOF, PHARMACEUTICAL PREPARATIONS CONTAINING SAME, AND USE THEREOF FOR THE PRODUCTION OF MEDICAMENTS
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20150210734A1

  公开（公告）日：2015-07-30

  The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis.

  这项发明涉及AKR1C3抑制剂及其制备方法，以及它们用于治疗和/或预防疾病的用途，还包括它们用于制备用于治疗和/或预防疾病的药物的用途，特别是用于出血障碍和子宫内膜异位症的治疗。
• [EN] 3-NITROGEN OR SULPHUR SUBSTITUTED OESTRA-1,3,5(10),16-TETRAENE AKR1C3 INHIBITORS<br/>[FR] INHIBITEURS D'AKR1C3 DE TYPE ŒSTRA-1,3,5(10),16-TÉTRAÈNE SUBSTITUÉS PAR UN 3-AZOTE OU SOUFRE
  申请人：BAYER PHARMA AG

  公开号：WO2016037956A1

  公开（公告）日：2016-03-17

  The invention relates to AKR1C3 inhibitors of formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of bleeding disorders and endometriosis.

  该发明涉及式(I)的AKR1C3抑制剂，以及其制备方法，用于治疗和/或预防疾病的用途，以及用于生产治疗和/或预防疾病的药物的用途，特别是用于出血性疾病和子宫内膜异位症的治疗。
• NOVEL STEROIDAL 17-BETA HETEROARYL COMPOUNDS AS INHIBITORS OF AKR1C3
  申请人：Bayer Pharma Aktiengesellschaft

  公开号：EP3421483A1

  公开（公告）日：2019-01-02

  The invention relates to novel steroidal 17-beta heteroaryl compounds as AKR1C3 inhibitors, to the use thereof for the treatment and/or prophylaxis of diseases and to the use thereof for the production of medicaments for treatment and/or prophylaxis of diseases, especially of gynecological disorders, hyperproliferative disorders, metabolic disorders, or inflammatory disorders as well as prostate cancer including castration-resistant prostate cancer as a sole agent or in combination with other active ingredients.

  这项发明涉及一种新颖的类固醇17-β杂环芳基化合物，作为AKR1C3抑制剂的用途，用于治疗和/或预防疾病，并用于制备治疗和/或预防疾病的药物，特别是治疗妇科疾病、高增殖性疾病、代谢性疾病或炎症性疾病以及包括去势抵抗性前列腺癌在内的前列腺癌，作为单一药剂或与其他活性成分组合使用。