11,21-bisphenyl-19-norpregnane derivatives

Details 11,21-bisphenyl-19-norpregnane derivatives 11,21-bisphenyl-19-norpregnane derivatives

1995-05-19

1997-04-15

Prior, Kimberly J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

514176, 514179, 514182, 540106, 540107, 540109, 540116, 552520, 552648, A61K 31565, C07J 100

Patent

active

056209665

ABSTRACT:
The invention relates to a 11,21-bisphenyl-19-norpregnane derivative of formula I ##STR1## wherein R.sub.1 is selected from H, halogen, (1-6C)alkoxy, and NR.sub.5 R.sub.6, R.sub.5 and R.sub.6 being independently hydrogen or (1-6C)alkyl or R.sub.5 and R.sub.6 together are (3-6C)alkylene; R.sub.2 is hydrogen; or R.sub.1 and R.sub.2 together are a (1-3C)alkylenedioxy group, optionally substituted by one or more halogen atoms; R.sub.3 is methyl or ethyl; R.sub.4 is selected from C(O)-NR.sub.5 R.sub.6, SO.sub.n -(1-6C)alkyl optionally substituted by one or more halogen atoms, SO.sub.n -(3-6C)cycloalkyl, n being 1 or 2, SO.sub.2 -NR.sub.5 R.sub.6, 2-oxypyrrolidinyl, and NR.sub.5 R.sub.6 ; R.sub.7 is H or (1-6C)alkyl; R.sub.8 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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