| abstract |
The present invention relates to certain substituted 17β-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), especially those of formula (IG) wherein R?1 and R1¿ are: i) independently hydrogen or lower alkyl and the bond between the carbons bearing R?1 and R2¿ is a single or a double bond, or ii) taken together are a -CH¿2?- group to form a cyclopropane ring, and the bond between the carbons bearing R?1 and R2¿ is a single bond; R3c is hydrogen; R4c is hydrogen, lower alkyl, lower cycloalkyl, lower alkenyl, alkanoyl of 2-6 carbons, -(CH¿2?)mCO2R?16¿, -(CH¿2)mAr?a, -(CH¿2?)n'CONR?17R18¿, -(CH¿2?)n'NR?17R18¿ or -(CH¿2?)n'OR?16¿, wherein R16 is hydrogen, lower alkyl or lower alkenyl; R?17 and R18¿ are independly hydrogen, lower alkyl lower cycloalkyl or lower alkenyl; Ara is an aromatic group of 6 to 12 carbons; n' is 0 or an integer from 1 to 5; m is an integer from 1 to 5; R?19 and R20¿ are independently hydrogen or lower alkyl, or taken together R?19 and R20¿ form a carbonyl group(=O); R5c is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, or NR21R22, wherein R?21 and R22¿ are independently hydrogen, lower alkyl or lower alkenyl; and pharmaceutically acceptable salts thereof, their preparation, medical use and pharmaceutical formulations. |