Novel steroidal antiestrogens and antiandrogens and uses thereof

A compound having the structural formula, wherein said compound has a message unit at the 17α-position of an address unit, said formula comprising:

• a) an address unit having one of the following different structures:
• 38
• wherein:
• R10 is H, CH3;
• R11 is H, C1-C4 alkyl;
• R12 is O, (H, OH);
• R13 is H, OH, Cl, Br, I, CH3;
• R14 is H, C1-C4 alkyl;
• R is O, (H, OH);
• R16 is O, NH;
• R17 through R18 each independently is H, CH3;
• and
• b) a message unit having the structure:
• 39
• wherein:
• R4 is H, alkyl (C1-C4);
• R5 is aryl, heteroaryl, fused aryl, —CO-aryl, CO-fused aryl, —CO-heteroaryl, —CO-fused heteroaryl, biaryl, CO-biaryl, ether-linked aryls, ether-linked heteroaryls, amine-linked aryls, amine-linked heteroaryls, wherein any aryl, heteroaryl, fused aryl, fused heteroaryl, biaryl, CO-biaryl, ether-linked aryls, ether-linked heteroaryls, amine-linked aryls, and amine-linked heteroaryls may optionally be substituted, independently, with H, CH3, OH, OCH3, OCF3, NCH3, NCOCH3, aryl, CO2CH3, CONH2, C1-C4 alkyl, (CF2)nF wherein n=1-4, Cl, Br, I, F, O(CH2)nH wherein n=1-4, NO2, NH2, NHCOR4, CO2H, CO2R4. CONHR4. amyl, thioether, SR6, S(O)R6, SO2R6, SO2NR6R7;
• wherein R4 has the definition given above;
• wherein R6 is H, C1-C4 alkyl or perfluoroalkyl, aryl, heteroaryl, or optionally substituted allyl, arylmethyl, alkynyl, alkenyl;
• wherein R7 is H, C1-C4 alkyl or perfluoroalkyl, aryl, heteroaryl, optionally substituted allyl, arylmethyl, OR8 or NHR8;
• wherein R8 is H, C1-C6 alkyl or perfluoroalkyl, aryl, heteroaryl, optionally substituted allyl or arylmethyl, SO2R6 or S(O)R6, wherein R6 has the definition given above;
• and
• wherein R5 can be in either the E or Z configuration in relation to the 17a-position of the address unit.

A method for the prophylaxis or treatment of a prostate disorder in a patient, said method comprising the steps of:

• providing a patient suffering from or believed to be at risk of developing a prostate disorder;
• administering to said patient an effective amount of a compound having the structural formula:
• a) an address unit having the structure:
• 40
• wherein:
• R10 is H, CH3;
• R11 is H, C1-C4 alkyl;
• R12 is O, (H, OH);
• R13 is H, OH, Cl, Br, I, CH3;
• R14 is H, C1-C4 alkyl;
• R is O, (H, OH);
• R16 is O, NH;
• R17 through R18 each independently is H, CH3;
• and
• b) a message unit having the structure:
• 41
• wherein:
• R4 is H, alkyl (C1-C4);
• R5 is aryl, heteroaryl, fused aryl, —CO-aryl, CO-fused aryl, —CO-heteroaryl, —CO-fused heteroaryl, biaryl, CO-biaryl, ether-linked aryls, ether-linked heteroaryls, amine-linked aryls, amine-linked heteroaryls, wherein any aryl, heteroaryl, fused aryl, fused heteroaryl, biaryl, CO-biaryl, ether-linked aryls, ether-linked heteroaryls, amine-linked aryls, and amine-linked heteroaryls may optionally be substituted, independently, with H, CH3, OH, OCH3, OCF3, NCH3, NCOCH3, aryl, CO2CH3, CONH2, C1-C4 alkyl, (CF2)nF wherein n=1-4, Cl, Br, I, F, O(CH2)nH wherein n=1-4, NO2, NH2, NHCOR4, CO2H, CO2R4, CONHR4, amyl, thioether, SR6, S(O)R6, SO2R6, SO2NR6R7;
• wherein R4 has the definition given above;
• wherein R6 is H, C1-C4 alkyl or perfluoroalkyl, aryl, heteroaryl, or optionally substituted allyl, arylmethyl, alkynyl, alkenyl;
• wherein R7 is H, C1-C4 alkyl or perfluoroalkyl, aryl, heteroaryl, optionally substituted allyl, arylmethyl, OR8 or NHR8;
• wherein R8 is H, C1-C6 alkyl or perfluoroalkyl, aryl, heteroaryl, optionally substituted allyl or arylmethyl, SO2R6 or S(O)R6, wherein R6 has the definition given above;
• and
• wherein R5 can be in either the E or Z configuration in relation to the 17a-position of the address unit.