PURPOSE: To obtain the subject new derivative having anti-glucocorticoid activity and usable in treating or preventing glucocorticoid-dependent diseases such as diabetes, hypertension and arteriosclerosis.
CONSTITUTION: This new 11,12-bisphenyl-19-norpregnane derivative (salt) is shown by formula I [R1 is H, a halogen, a 1-6C alkoxy or a group of NR5R6 (R5 and R6 are each H or a 1-6C alkyl, or together form a 3-6C alkylene); R2 is H; R1 and R2 together form a (substituted) alkylenedioxy; R3 is methyl or ethyl; R4 is a group of the formula C(O)-NR5R6, a (substituted) SOn1-6C alkyl ((n) is 1 or 2), an SOn3-6C cycloalkyl, an SO2NR5R6, 2-oxypyrrolidinyl or a group of NR5R6; R7 is H or a 1-6C alkyl; R8 is H or a carboxy-1-oxo-6C alkyl; X is (H, OH), O or NOH]. This compound is obtained by dehydrating a compound of formula II (P is a protected keto group) followed by deprotection and then, as necessary, hydroxylating and hydroxylating or oximating the 3-site.
VOORT HENDRIKUS A A VAN DER (NL)
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