28-01-2021 дата публикации
Номер: US20210023095A1
Автор:
BALBAS Minna Delarae,
Du Xiaohui,
EKSTEROWICZ John,
FANTIN Valeria R.,
McGee Lawrence R.,
MEDINA Julio C.,
REW Yosup,
SUN Daqing,
YAN Xuelei,
ZHOU Haiying,
ZHU Liusheng
Принадлежит:
The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer and hypercortisolism. 2. The compound of or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein{'sup': 1', '3', '6', '3', '3', '4', '3', '6', '3', '3', '4', '3', '3', '4', '3', '4', '6, 'sub': 2', '2', '2', '2', '2', '2, 'Ris —NRS(O)R, —NRS(O)NRR, -alkyNRS(O)R, -alkyNRS(O)NRR, —NRaralkyl, —C(O)NRR, —S(O)NRR, or —S(O)R;'}{'sup': 3', '4', '10', '6, 'sub': 2', '2, 'Rand Rare each independently —H, optionally substituted alkyl, fluoroalkyl, optionally substituted carbocyclyl, optionally substituted carbocyclylalkyl, optionally substituted aryl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl, —C(O)N(R), or —S(O)R;'}{'sup': 3', '4, 'or Rand Rattached to the same N atom are taken together with the N atom to which they are attached to form a substituted or unsubstituted 3-, 4-, 5-, or 6-membered heterocycle;'}{'sup': '5', 'Ris optionally substituted alkyl, fluoroalkyl, optionally substituted carbocyclyl, or optionally substituted heterocyclyl;'}{'sup': '6', 'Ris optionally substituted alkyl, fluoroalkyl, optionally substituted carbocyclyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocyclyl, or optionally substituted heteroaryl;'}{'sup': 7', '8', '5', '3', '4', '3', '4, 'Rand Rare each independently —H, optionally substituted alkyl, fluoroalkyl, halo, —OR, —NRR, —C(O)NRR, —CN, optionally substituted carbocyclyl, or optionally substituted carbocyclylalkyl;'}{'sup': 7', '8', '6, 'sub': '2', 'or Rand Rare taken ...
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