Fused heterocyclic compounds and analogs thereof, modulators of nuclear hormone receptor function

A compound having the following formula Id, or a salt thereof:

• wherein the symbols have the following meanings and are, for each occurrence, independently selected:
• G is an aryl or heterocyclo group, where said group is mono- or polycyclic, and which is optionally substituted at one or more positions;
• Z is 0;
• n=1 or 2;
• A1 is CR7;
• A2 is CR7;
• Y is J-J′-J” where J is (CR7R7′)n and n=0-3, J′ is a bond or O, S, S═O, SO2, NH, NR7, C═O, OC═O, NR1C═O, CR7R7′, C═CR8R8′, R2P═O, R2P═S, R2OP═O, R2NHP═O, OP═OOR2, OP═ONHR2, OP═OR2, OSO2, C═NR7, NHNH, NHNR6, NR6NH, N═N, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo or aryl or substituted aryl, and J″ is (CR7R7′)n and n=0-3, where Y is not a bond;
• W is CR7R7′-CR7R7′, CR8═CR8′CR7R7′-C═O, NR9—CR7R7′, N═CR8, N═N, NR9—NR9′, S—CR7R7′, SO—CR7R7′, SO2—CR7R7′, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, or aryl or substituted aryl;
• Q1 is H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycloalkyl or substituted heterocycloalkyl, arylalkyl or substituted arylalkyl, alkynyl or substituted alkynyl, aryl or substituted aryl, heterocyclo (e.g., heteroaryl) or substituted heterocyclo (e.g., substituted heteroaryl), halo, CN, R1OC═O, R4C═O, R5R6NC═O, HOCR7R7′, nitro, R1OCH2, R1O, NH2, C═OSR1, SO2R1 or NR4R5;
• Q2 is H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycloalkyl or substituted heterocycloalkyl, arylalkyl or substituted arylalkyl, alkynyl or substituted alkynyl, aryl or substituted aryl, heterocyclo (e.g., heteroaryl) or substituted heterocyclo (e.g., substituted heteroaryl), halo, CN, R1OC═O, R4C═O, R5R6NC═O, HOCR7R7′, nitro, R1OCH2, R1O, NH2, C═OSR1, SO2R1 or NR4R5;
• L is a bond;
• R1 and R1′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkyalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl;
• R2 is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl;
• R3 and R3′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, halo, CN, hydroxylamine, hydroxamide, alkoxy or substituted alkoxy, amino, NR1R2, thiol, alkylthio or substituted alkylthio;
• R4 is H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, R1C═O, R1NHC═O, R1OC═O;
• SO2OR1, or SO2NR1R1′;
• R5 is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, R1C═O, R1NHC═O, SO2R1, SO2OR1, or SO2NR1R1′;
• R6 is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, CN, OH, OR1, R1C═O, R1NHC═O, SO2R1, SO2OR1, or SO2NR1R1′;
• R7 and R7 are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, halo, N3, CN, OR1, O(C═O)R1, O(C═O)NHR1, O(C═O)OR1, nitro, hydroxylamine, hydroxylamide, amino, SR1, SeR1, NHR4, NR2R5, NOR1, thiol, alkylthio or substituted alkylthio, R1C═O, R1OC═O, R1NHC═O, SO2R1, SOR1, PO3R1R−1, R1R1′ NC═O, C═OSR1, SO2R1, SO2OR1, SO2NR1R1′, OSO2-aryl, OSO2— (substituted aryl), OSO2-heterocyclo, OSO2— (substituted heterocyclo), or COCl;
• R8 and R8′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkyalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, nitro, halo, CN, OR1, amino, NHR4, NR2R5, NOR1, alkylthio or substituted alkylthio, C═OSR1, R1OC═O, R1C═O, R1NHC═O, R1R1′ NC═O, SO2OR1, S═OR1, SO2R1, PO3R1R1′, or SO2NR1R1′;
• and
• R9 and R9′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, CN, OH, OR1, R1C═O, R1OC═O, R1NHC═O, SO2OR1, or SO2NR1R1;
• with the proviso that when A1 and A2 are CH;
• Y is O, CH2 or NH;
• W is CH2—CH2 or CH═CH;
• Q2 is H or CH2OH;
• and Q1 is H or CH2OH, then (i) G-L is not pyridinyl, phenyl, dichlorophenyl, bromophenyl or methoxyphenyl when E is CH(OH) or CH(OCH3) and (ii) G-L is not methoxyphenyl or phenyl substituted with —OCH2CH2—SB where SB is dimethylamino, diethylamino, piperidinyl, morpholinyl, or pyrrolidinyl when E is CH2.

A method of modulating the function of a nuclear hormone receptor which comprises administering to a mammalian species an effective nuclear hormone receptor modulating amount of a compound of the following formula I:

• wherein the symbols have the following meanings, and are, for each occurrence, independently selected:
• G is an aryl or heterocyclo group, where said group is mono- or polycyclic, and which is optionally substituted at one or more positions;
• Z is O, S, NH, or NR5;
• E and M are selected such that
• (i) E is CR7R7′ and M is C-Q2;
• or
• (ii) E is C═CR10R10′ and M is N or C-Q2;
• A1 is CR7 or N;
• A2 is CR7 or N;
• Y is J-J′-J″ where J is (CR7R7′)n and n=0-3, J′ is a bond or O, S, S═O, SO2, NH, NR7, C═O, OC═O, NR1C═O, CR7R7′, C═CR R8′R2P═O, R2P═S, R2OP═O, R2NHP═O, OP═OOR2, OP═ONHR2, OP═OR2, OSO2, C═NR7, NHNH, NHNR5, NR5NH, N═N, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo or aryl or substituted aryl, and J″ is (CR7R7′)n and n=0-3, where Y is not a bond;
• W is CR7R7′-CR7R7′, CR8═CR8′, CR7R7′—C═O, NR9CR7R7′, N═CR8, N═N, NR9—NR9′, S—CR7R7′, SO—CR7R7′, SO2—CR7R7′, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, or aryl or substituted aryl;
• Q1 is H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycloalkyl or substituted heterocycloalkyl, arylalkyl or substituted arylalkyl, alkynyl or substituted alkynyl, aryl or substituted aryl, heterocyclo (e.g., heteroaryl) or substituted heterocyclo (e.g., substituted heteroaryl), halo, CN, R1OC═O, R4C═O, R5R6NC═O, HOCR7R7′, nitro, R1OCH2, R1O, NH2, C═OSR1, SO2R1 or NR4R5;
• Q2 is H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycloalkyl or substituted heterocycloalkyl, arylalkyl or substituted arylalkyl, alkynyl or substituted alkynyl, aryl or substituted aryl, heterocyclo (e.g., heteroaryl) or substituted heterocyclo (e.g., substituted heteroaryl), halo, CN, R1OC═O, R4C═O, R5R6NC═O, HOCR7R7′, nitro, R1OCH2, R1O, NH2, C═OSR1, SO2R1 or NR4R5;
• L is a bond, (CR7R7′)n, NH, NR5, NH(CR7R7′)n, or NR5(CR7R7′)n, where n=0-3;
• R1 and R1′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkyalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl;
• R2 is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl;
• R3 and R3′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, halo, CN, hydroxylamine, hydroxamide, alkoxy or substituted alkoxy, amino, NR1R2, thiol, alkylthio or substituted alkylthio;
• R4 is H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, R1C═O, R1NHC═O, R1OC═O, SO2OR1, or SO2NR1R1′;
• R5 is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, R1C═O, R1NHC═O, SO2R1, SO2OR1, or SO2NR1R1′;
• R6 is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, CN, OH, OR1, R1C═O, R1NHC═O, SO2R1, SO2OR1, or SO2NR1R1′;
• R7 and R7′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, halo, N3, CN, OR1, O(C═O)R1, O(C═O)NHR1, O(C═O)OR1, nitro, hydroxylamine, hydroxylamide, amino, SR1, SeR1, NHR4, NR2R5, NOR1, thiol, alkylthio or substituted alkylthio, R1C═O, R1OC═O, R1NHC═O, SO2R1, SOR1, PO3R1R1′, R1R1′NC═O, C═OSR1, SO2R1, SO20R1,
• SO2NR1R1′, OSO2-aryl, OSO2— (substituted aryl), OSO2-heterocyclo, OSO2— (substituted heterocyclo), or COCl;
• R5 and R8′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkyalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, nitro, halo, CN, OR1, amino, NHR4, NR2R5, NOR1, alkylthio or substituted alkylthio, C═OSR1, R1OC═O, R1C═O, R1NHC═O, R1R1′NC═O, SO20R1, S═OR1, SO2R1, PO3R1R1′, or SO2NR1R1′;
• R9 and R9′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, CN, OH, OR1, R1C═O, R1OC═O, R1NHC═O, SO2OR1, or SO2NR1R1′;
• and
• R10 and R10′ are each independently H, R1, COOR1, CONR1R2, halo, CN, OR1, R1C═O, SO2R1 or SO2NR1R1′.

A method for treating a condition or disorder comprising administering to a mammalian species a therapeutically effective amount of a compound of the following formula:

• wherein the symbols have the following meanings, and are, for each occurrence, independently selected:
• G is an aryl or heterocyclo group, where said group is mono- or polycyclic, and which is optionally substituted at one or more positions;
• Z is O, S, NH, or NR6;
• E and M are selected such that
• (i) E is CR7R7′ and M is C-Q2;
• or
• (ii) E is C═CR10R10′ and M is N or C-Q2;
• A1 is CR7 or N;
• A2 is CR7 or N;
• Y is J-J′-J″ where J is (CR7R7′)n and n=0-3, J′ is a bond or O, S, S═O, SO2, NH, NR7, C═O, OC═O, NR1C═O, CR7R7′, C═CR8R8′, R2P═O, R2P═S, R2OP═O, R2NHP═O, OP═OOR2, OP═ONHR2, OP═OR2, OSO2, C═NR7, NHNH, NHNR6, NR6NH, N═N, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo or aryl or substituted aryl, and J″ is (CR7R7′)n and n=0-3, where Y is not a bond;
• W is CR7R7′—CR7R7′, CR8═CR8′CR7R7′—C═O, NR9—CR7R7′, N═CR8, N═N, NR9—NR9′, S—CR7R7′, SO—CR7R7′, SO2—CR7R7′, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, or aryl or substituted aryl;
• Q1 is H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycloalkyl or substituted heterocycloalkyl, arylalkyl or substituted arylalkyl, alkynyl or substituted alkynyl, aryl or substituted aryl, heterocyclo (e.g., heteroaryl) or substituted heterocyclo (e.g., substituted heteroaryl), halo, CN, R1OC═O, R4C═O, R5R6NC═O, HOCR7R7′, nitro, R1OCH2, R1O, NH2, C═OSR1, SO2R1 or NR4R5;
• Q2 is H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocycloalkyl or substituted heterocycloalkyl, arylalkyl or substituted arylalkyl, alkynyl or substituted alkynyl, aryl or substituted aryl, heterocyclo (e.g., heteroaryl) or substituted heterocyclo (e.g., substituted heteroaryl), halo, CN, R1OC═O, R4C═O, R5R6NC═O, HOCR7R7′, nitro, R1OCH2, R1O, NH2, C═OSR1, SO2R1 or NR4R5;
• L is a bond, (CR7R7′)n, NH, NR5, NH(CR7R7′)n, or NR5(CR7R7′)n, where n=0-3;
• R1 and R1′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkyalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl;
• R2 is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl;
• R3 and R3 are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, halo, CN, hydroxylamine, hydroxamide, alkoxy or substituted alkoxy, amino, NR1R2, thiol, alkylthio or substituted alkylthio;
• R4 is H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, R1C═O, R1NHC═O, R1OC═O, SO2OR1, or SO2NR1R1′;
• R5 is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, R1C═O, R1NHC═O, SO2R1, SO2OR1, or SO2NR1R1′;
• R6 is alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, CN, OH, OR1, R1C═O, R1NHC═O, SO2R1, SO2OR1, or SO2NR1R1′.
• R7 and R7′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, halo, N3, CN, OR1, O(C═O)R1, O(C═O)NHR1, O(C═O)OR1, nitro, hydroxylamine, hydroxylamide, amino, SR1, SeR1, NHR4, NR2R5, NOR1, thiol, alkylthio or substituted alkylthio, R1C═O, R1OC═O, R1NHC═O, SO2R1, SOR1, PO3R1R1′, R1R1′NC═O, C═OSR1, SO2R1, SO2OR1, SO2NR1R1, OSO2-aryl, OSO2— (substituted aryl), OSO2-heterocyclo, OSO2— (substituted heterocyclo), or COCl;
• R8 and R8′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkyalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, nitro, halo, CN, OR1, amino, NHR4, NR2R5, NOR1, alkylthio or substituted alkylthio, C═OSR1, R1OC═O, R1C═O, R1NHC═O, R1R1′NC═O, SO2OR1, S═OR1, SO2R1, PO3R1R1′, or SO2NR1R1′;
• R9 and R9′ are each independently H, alkyl or substituted alkyl, alkenyl or substituted alkenyl, alkynyl or substituted alkynyl, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, cycloalkylalkyl or substituted cycloalkylalkyl, cycloalkenylalkyl or substituted cycloalkenylalkyl, heterocycloalkyl or substituted heterocycloalkyl, aryl or substituted aryl, arylalkyl or substituted arylalkyl, CN, OH, OR1, R1C═O, R1OC═O, R1NHC═O, SO2OR1, or SO2NR1R1′;
• and
• R10 and R10′ are each independently H, R1, COOR1, CONR1R2, halo, CN, OR1, R1C═O, SO2OR1 or SO2NR1R1′;
• wherein said condition or disorder is selected from the group consisting of benign prostate hypertrophia, adenomas and neoplasies of the prostate, malignant tumor cells containing the androgen receptor, heart disease, hirsutism, acne, hyperpilosity, seborrhea, endometriosis, polycystic ovary syndrome, androgenic alopecia, hypogonadism, osteoporosis, suppressing spermatogenisis, libido, cachexia, anorexia, inhibition of muscular atrophy in ambulatory patients, androgen supplementation for age related decreased testosterone levels in men, prostate cancer, breast cancer, endometrial cancer, hot flashes, vaginal dryness, menopause, amennoreahea, dysmennoreahea, contraception, pregnancy termination, cancers containing the progesterone receptor, endometriosis, cachexia, menopause, cyclesynchrony, meniginoma, fibroids, labor induction, psychotic disorders, drug dependence, non-insulin dependent Diabetes Mellitus, dopamine receptor mediated disorders, congestive heart failure, disregulation of cholesterol homeostasis, and attenuating the metabolism of a pharmaceutical agent.