Selective estrogen receptor-β ligands

A compound having the formula:

• or a pharmaceutically acceptable salt or hydrolyzable ester thereof,
• wherein:
• R1 is H, C1-8alkyl, phenyl, or a 5- or 6-membered ring heterocycle containing 1, 2 or 3 heteroatoms each independently selected from O, N and S and additionally having 0 or 1 oxo groups and 0 or 1 fused benzo rings, wherein the C1-8alkyl, phenyl or heterocycle is substituted by 0, 1, 2 or 3 substituents selected from —Ra, —ORa, —SRa, —NRaRa, —CO2Ra, —OC(═O)Ra, —C(═O)NRaRa, —NRaC(═O)Ra, —NRaS(═O)Ra, NRaS(═O)2Ra, —C(═O)Ra, —S(═O)Ra, —S(═O)2Ra, halogen, cyano, nitro and C1-3haloalkyl;
• R2 is phenyl substituted by 1, 2 or 3 substituents selected from —ORa, —SRa, —NRaRa, —CO2Ra, —OC(═O)Ra, —C(═O)NRaRa, —NRaC(═O)Ra, —NRaS(═O)Ra, —NRaS(═O)2Ra, —C(═O)Ra, —S(═O)Ra, —S(═O)2Ra, halogen, cyano, nitro and C1-3haloalkyl, wherein at least one of the substituents is —OH;
• and wherein the phenyl is additionally substituted by 0, 1 or 2 substituents selected from C1-6alkyl, phenyl and benzyl;
• R3 is hydrogen, C1-6alkyl, —(CH2)mphenyl or —(CH2)mheterocycle, wherein the heterocycle is a 5- or 6-membered ring heterocycle containing 1, 2 or 3 heteroatoms each independently selected from O, N and S and additionally having 0 or 1 oxo groups and 0 or 1 fused benzo rings;
• R4 is H, halogen, C1-6alkyl, C1-6haloalkyl, —(CH2)mphenyl or —(CH2)mheterocycle, wherein the heterocycle is a 5- or 6-membered ring heterocycle containing 1, 2 or 3 heteroatoms each independently selected from O, N and S and additionally having 0 or 1 oxo groups and 0 or 1 fused benzo rings;
• R5 is —Ra, —ORa, —SRa, —NRaRa, —CO2Ra, —OC(═O)Ra, —C(═O)NRaRa, —NRaC(═O)Ra, —NRaS(═O)Ra, —NRaS(═O)2Ra, —C(═O)Ra, —S(═O)Ra, —S(═O)2Ra, halogen, cyano, nitro or C1-3haloalkyl;
• or R5 is C1-3alkyl containing 1 or 2 substituents selected from —ORa, —SRa, —NRaRa, —CO2Ra, —OC(═O)Ra, —C(═O)NRaRa, —NRaC(═O)Ra, —NRaS(═O)Ra, —NRaS(═O)2Ra, —C(═O)Ra, —S(═O)Ra, —S(═O)2Ra, halogen, cyano and nitro;
• R6 is —OH;
• R7 is —Ra, —ORa, —SRa, —NRaRa, —CO2Ra, —OC(═O)Ra, —C(═O)NRaRa, —NRaC(═O)Ra, —NRaS(═O)Ra, —NRaS(═O)2Ra, —C(═O)Ra, —S(═O)Ra, —S(═O)2Ra, halogen, cyano, nitro or C1-3haloalkyl;
• R8 is —Ra, —ORa, —SRa, —NRaRa, —CO2Ra, —OC(═O)Ra, —C(═O)NRaRa, —NRaC(═O)Ra, —NRaS(═O)Ra, —NRaS(═O)2Ra, —C(═O)Ra, —S(═O)Ra, —S(═O)2Ra, halogen, cyano, nitro or C1-3haloalkyl;
• or R8 is C1-3alkyl containing 1 or 2 substituents selected from —ORa, —SRa, —NRaRa, —CO2Ra, —OC(═O)Ra, —C(═O)NRaRa, —NRaC(═O)Ra, —NRaS(═O)Ra, —NRaS(═O)2Ra, —C(═O)Ra, —S(═O)Ra, —S(═O)2Ra, halogen, cyano and nitro;
• R9 is H, C1-5alkyl or C1-3haloalkyl;
• Ra is H, C1-6alkyl, phenyl or benzyl;
• m is 0, 1, 2 or 3;
• n is 1;
• and
• wherein the compound is not 1,2,3,4-tetrahydro-2-(3-hydroxy-4-methoxyphenyl)-7-methoxy-6-isoquinolinol.