Branched chain and cycloaliphatic esters of the androstane and oestrane series and pharmaceutical compositions containing same

摘要

There are disclosed branched chain and cycloaliphatic esters of steroids having the formula: or the 5 alpha H analog thereof, where R is H or CH3; R1 is H or CH3; R2 is H or CH3; R3 is H, OH, CH3 or Cl; R4 is H or C1 to C4 alkyl; R5 is H, C1 to C4 alkyl or CF3; R6 is H, C1 to C4 alkyl, C1 to C4 alkoxy, halogen or beta -OH providing that when R6 is beta -OH, the steroid also contains 9 alpha -F and further providing that R1, R2, R3, R4, R5 and R6 represent at least 4 and at most 5 hydrogen atoms, except in the case of a DELTA 1,4-steroid, in which case R1, R2, R3, R4, R5and R6 are all hydrogen; R7 is H or CH3; providing the R8 is -OH or when the steroid has an aromatic ring A and the 3-position is substituted by R9 is where n is 0, 1 or 2; R10 is C1 to C10 alkyl; R11 is H or C1 to C10 alkyl; R12 is an aliphatic group with 1 to 18 carbon atoms, or R10 and R12 taken together with the carbon atom to which they are attached form a C7 to C12 cycloaliphatic group providing the total carbon atom content in the carboxylic acid residue is 8 to 20; ring A is either saturated or has one of the following types of unsaturation: DELTA 1; DELTA 4; DELTA 1,4; DELTA 5(10); DELTA 1,3,5(10), and X is =O, -OH or providing that X is OH or when the steroid has an aromatic ring A. The steroid esters have androgenic, anabolic, oestrogenic or anti-oestrogenic properties depending upon the ring configurations and the substituent(s). Pharmaceutical compositions containing the steroid esters are also disclosed.