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DERIVATIVES OF 11,21-BISPHENYL-19-NORPREGNAN, METHOD OF OBTAINING THEM AND PHARMACEUTICAL COMPOSITION CONTAINING SUCH DERIVATIVES
DERIVATIVES OF 11,21-BISPHENYL-19-NORPREGNAN, METHOD OF OBTAINING THEM AND PHARMACEUTICAL COMPOSITION CONTAINING SUCH DERIVATIVES
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机译:11,21-双联苯胺-19-北半乳聚糖的衍生物,获得它们的方法和包含此类衍生物的药物组合物
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摘要
The invention relates to a 11,21-bisphenyl-19-norpregnane derivative of formula I CHEM wherein R1 is selected from H, halogen, (1-6C)alkoxy, and NR5R6, R5 and R6 being independently hydrogen or (1-6C)alkyl or R5 and R6 together are (3-6C)alkylene; R2 is hydrogen; or R1 and R2 together are a (1-3C)alkylenedioxy group, optionally substituted by one or more halogen atoms; R3 is methyl or ethyl; R4 is selected from C(O)-NR5R6, SOn-(1-6C)alkyl optionally substituted by one or more halogen atoms, SOn-(3-6C)cycloalkyl, n being 1 or 2, SO2-NR5R6, 2-oxypyrrolidinyl, and NR5R6; R7 is H or (1-6C)alkyl; R8 is H or carboxy-1-oxo(1-6C)alkyl; and X is selected from (H,OH), O, and NOH; 11 or a pharmaceutically acceptable salt thereof. The compounds of the invention have anti-glucocorticoid activity and can be used in treating or preventing glucocorticoid-dependent diseases.
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机译:本发明涉及式I 的11,21-联苯-19-降戊烯基衍生物,其中R 1选自H,卤素,(1-6C)烷氧基和NR 5 R 6,R 5和R 6独立地为氢或(1- 6C)烷基或R5和R6一起是(3-6C)亚烷基; R 2是氢; R 1和R 2一起是(1-3C)亚烷基二氧基,其任选地被一个或多个卤素原子取代; R3是甲基或乙基; R4选自C(O)-NR5R6,任选被一个或多个卤素原子取代的SOn-(1-6C)烷基,SOn-(3-6C)环烷基,n为1或2,SO2-NR5R6、2-氧吡咯烷基和NR5R6; R7是H或(1-6C)烷基; R8是H或羧基-1-氧代(1-6C)烷基; X选自(H,OH),O和NOH; 11或其药学上可接受的盐。本发明的化合物具有抗糖皮质激素活性,可用于治疗或预防糖皮质激素依赖性疾病。
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