((4aR,8aS)-1-(4-fluorophenyl)-6-((2-isopropyl-2H-1,2,3-triazol-4-yl)sulfonyl)-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(thiazol-4-yl)methanone | 1781245-13-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: ((4aR,8aS)-1-(4-fluorophenyl)-6-((2-isopropyl-2H-1,2,3-triazol-4-yl)sulfonyl)-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(thiazol-4-yl)methanone
• 英文别名: CORT125329；Zavacorilant；[(4aR,8aS)-1-(4-fluorophenyl)-6-(2-propan-2-yltriazol-4-yl)sulfonyl-4,5,7,8,8a,9-hexahydropyrazolo[3,4-g]isoquinolin-4a-yl]-(1,3-thiazol-4-yl)methanone
• CAS: 1781245-13-3
• 化学式: C₂₅H₂₆FN₇O₃S₂
• 分子量: 555.657
• InChiKey: DUHWKWNCLIALLV-BVZFJXPGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  38
• 可旋转键数：
  6
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  153
• 氢给体数：
  0
• 氢受体数：
  10

文献信息

• OCTAHYDRO FUSED AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS
  申请人：Corcept Therapeutics, Inc.

  公开号：US20150148341A1

  公开（公告）日：2015-05-28

  The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.

  本发明提供了八氢融合的阿扎德卡林化合物以及将这些化合物用作糖皮质激素受体调节剂的方法。
• Octahydro fused azadecalin glucocorticoid receptor modulators
  申请人：Corcept Therapeutics, Inc.

  公开号：US10323034B2

  公开（公告）日：2019-06-18

  The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.

  本发明提供了八氢融合氮杂十环素化合物以及将这些化合物用作糖皮质激素受体调节剂的方法。
• EP3560493B1
  申请人：——

  公开号：EP3560493B1

  公开（公告）日：2021-03-31
• [EN] OCTAHYDRO FUSED AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS<br/>[FR] MODULATEURS DE RECEPTEURS DE GLUCOCORTICOIDE AZADECALINE FUSIONNEE OCTAHYDRO
  申请人：CORCEPT THERAPEUTICS INC

  公开号：WO2015077530A1

  公开（公告）日：2015-05-28

  The present invention provides octahydro fused azadecalin compounds having glucocorticoid receptor binding affinity and modulatory activity for pharmaceutical use. Also provided are pharmaceutical compositions containing an effective amount of the fused azadecalin compounds and methods of using the compositions for the-treatment of a glucocorticoid receptor mediated disorder in a subject.
• [EN] METHOD OF NORMALIZING THE NEUTROPHIL TO LYMPHOCYTE RATIO IN CANCER PATIENTS WITH A SELECTIVE GLUCOCORTICOID RECEPTOR ANTAGONIST<br/>[FR] PROCÉDÉ DE NORMALISATION DU RAPPORT ENTRE LES NEUTROPHILES ET LES LYMPHOCYTES CHEZ DES PATIENTS CANCÉREUX AU MOYEN D'UN ANTAGONISTE SÉLECTIF DES RÉCEPTEURS AUX GLUCOCORTICOÏDES
  申请人：CORCEPT THERAPEUTICS INC

  公开号：WO2021076565A1

  公开（公告）日：2021-04-22

  Methods for treating a cancer patient with a neutrophil-to-lymphocyte ratio (NLR) greater than 3 are disclosed, comprising administering a nonsteroidal glucocorticoid receptor antagonist (GRA) to such a cancer patient, effective to reduce the patient's NLR. The methods include administering a nonsteroidal GRA and a cancer treatment to such a cancer patient, effective to reduce the patient's NLR and enhance the treatment of the cancer patient. The GRA may be orally administered. The nonsteroidal GRA may be a nonsteroidal compound comprising a heteroaryl ketone fused azadecalin structure (e.g., relacorilant) or an octahydro fused azadecalin structure (e.g., exicorilant). The cancer treatment may include chemotherapy, immunotherapy, radiation therapy, administration of an anti-angiogenic agent, administration of a growth factor inhibitor, and surgery. The methods may enhance the cancer treatment, improve the prognosis of the cancer patient, improve the survival of the cancer patient, and provide beneficial clinical effects and advantages to the patient.