Steroidal antiestrogens and antiandrogens and uses thereof

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;
• and
• administering to said patient an effective amount of a compound having the structural formula:
• an address unit having one of the following different structures:
• 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;
• R15 is O, (H, OH);
• R16 is O, NH;
• and
• R17 through R18 each independently is H, CH3;
• and
• a message unit having the structure:
• wherein:
• R4 is H, C1-C4 alkyl;
• 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, or amine-linked heteroaryls, wherein any 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, and amine-linked heteroaryls may optionally be substituted, independently, with H, CH3, OH, OCH3, OCF3, N(CH3)2, NHCOCH3, aryl, CO2CH3, CONH2, C1-C4 alkyl, (CF2)nF wherein n=1-4, Cl, Br, I, F, O(CH2)rH wherein n=1-4, NO2, NH2, NHCOR4, CO2H, CO2R14, 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, optionally substituted allyl, arylmethyl, alkynyl, or 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, arylmethyl, SO2R6 or S(O)R6, wherein R6 has the definition given above,
• wherein R5 can be in either the E or Z configuration in relation to the 17α-position of the address unit and wherein the compound is dispersed in a pharmaceutically acceptable inert carrier substance.

A compound having the structure

• wherein R1 and R3 can be the same or different and any of the following, either alone or in combination:
• —H, —OH, —OCH3, -alkyl with 7 to 10 carbons (linear, branched, cycloalkyl) with 1 or more carbons replaced singly, multiply or in combination with up to n−1 carbons of N, S, or O and with hydrogen replaced singly or multiply up to replacement of all hydrogen with fluorine, or -alkenyl with 4 to 10 carbons (linear, branched, cycloalkenyl) with 1 or more carbons replaced singly, multiply or in combination with up to n−1 carbons of N, S, and O and with hydrogen replaced singly or multiply up to replacement of all hydrogen with fluorine;
• aralkyl, wherein alkyl is 0, 2 to 10 carbons (linear, branched, cycloalkyl) with 1 or more carbons replaced singly, multiply or a combination of N, S, and O and with hydrogen replaced singly or multiply up to replacement of all hydrogen with fluorine;
• aralkenyl, wherein alkene is 2 to 10 carbons (linear, branched, cycloalkyl) and the alkyl portion of the alkene being 0 to 8 carbons with 1 or more carbons of the alkyl portion replaced singly, multiply or a combination of N, S, and O and with hydrogen replaced singly or multiply up to replacement of all hydrogen with fluorine and configuration is cis or trans;
• or
• aralkynyl, wherein alkynyl is 2 to 10 carbons (linear, branched, cycloalkyl) and the alkyl portion of the alkyne being 0 to 8 carbons with 1 or more carbons of the alkyl portion replaced singly, multiply or a combination of N, S, and O and with hydrogen replaced singly or multiply up to replacement of all hydrogen with fluorine;
• R2 can be any of the following, either alone or in combination:
• hydroxyl, carboxyaryl, carboxyalkyl, alkoxy or ORP, wherein RP is H, CH3, COCH3, CO(CH2)nCH3, CO-aryl, alkyl, cycloalkyl (ether), ester, —COCH3;
• R4 and R5 can be the same or different, and if R4 is hydrogen or alkyl then R5 can be alkyl, aryl, or substituted aryl, heteroaryl, alkyl alcohol, where alkyl is 1 to 10 carbons (linear, branched, cycloalkyl) and wherein hydroxyl group(s) is on any carbon(s) in the alkyl portion, alkyl carbonyl or where alkyl is 1 to 10 carbons (linear, branched, cycloalkyl) and where carbonyl group(s) is on any carbon(s) in the alkyl portion, or fused aromatics, or if R5 is hydrogen or alkyl then R4 can be alkyl where R5 is not hydrogen, aryl, or substituted aryl, heteroaryl, alkyl alcohol and where hydroxyl group(s) is on any carbon(s) in the alkyl portion, alkyl carbonyl and further where carbonyl group(s) is on any carbon(s) in the alkyl portion, or fused aromatics.

A compound having an address unit having the structure:

• wherein:
• R1 is H, CH3, CH2CH3, OH, OCH3, OCH2CH3, C1-C6 alkyl, CH═CH2, CH═CHCH3, CH2-aryl, detectable marker, wherein the detectable marker can be bound directly to the address unit or conjugated thereto via a conjugate;
• R2 is H, CH3, COCH3, CO(CH2)nCH3, CO-aryl, alkyl, cycloalkyl (ether), ester, detectable marker, wherein the detectable marker can be bound directly to the address unit or conjugated thereto via a conjugate;
• and
• R3 is H, CH3, CH2CH3, aryl, heteroaryl, C1-C6 alkyl, alkyl (C1-C6) amides, alkyl (C1-C6) sulfide, alkyl (C1-C6) sulfone, alkyl (C1-C6) sulfoxide, detectable marker, wherein the detectable marker can be bound directly to the address unit or conjugated thereto via a conjugate;
• and
• a message unit having the structure:
• wherein:
• R4 is H, C1-C4 alkyl, detectable marker, wherein the detectable marker can be bound directly to R4 or conjugated thereto via a conjugate;
• R5 is a substituted aryl, detectable marker, 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, aminoalkoxy arene hybrid, or peptidyl hybrid, wherein any substituted 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, aminoalkoxy arene hybrid and peptidyl hybrid, may optionally be substituted, independently, with a detectable marker, H, CH3, OH, OCH3, OCF3, N(CH3)2, NHCOCH3, 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, optionally substituted allyl, arylmethyl, alkynyl, or 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, arylmethyl, SO2R6 or S(O)R6, wherein R6 has the definition given above, and wherein the detectable marker can be bound directly to R5 or conjugated thereto via a conjugate;
• wherein R5 can be in either the E or Z configuration in relation to the 17α-position of said address unit.