6-substituted demethyl-estradiol derivatives as selective er-beta agonists

A compound of formula:

• wherein
• R1, R2, R3 and R4 are independently selected from hydrogen, C1-C6 alkyl, halo, a sulfate, a glucuronide, —OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, —N(CH2)n, a phosphate group, and a phosphinate group;
• R11 is selected from H, C1-C6 alkyl, halogen, a sulfate, a glucoronide, —SO2NH2, —COOH, —CN, —CH2CN—, —NHCN—, —CHO, ═CHOCH3, —COO salt, —OSO2alkyl, —NH2, and —NHCO(CH2)n;
• X is selected from C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, halogen, a glucoronide, —NH2, —SO2NH2, —COOH, —CN, —CH2CN, —NHCN, —CHO, —COOsalt, —OSO2alkyl, —SH, —SCH3, —CH[(CH2)nCH3]COOCH3, —(CH2)mCOOCH3, —(CH2)m—O—CH3, —(CH2)m—O—(CH2)nCH3, (CH2)m—S—CH3, —(CH2)m—S—(CH2)nCH3, —(CH2)m—NH—(CH2)nCH3, —C2-C8 alkenyl-O—(CH2)nCH3, —C2-C8 alkenyl-S—(CH2)nCH3, —C2-C8 alkenyl-N—(CH2)nCH3, —C2-C8 alkynyl-O—(CH2)nCH3, —C2-C8 alkynyl-S—(CH2)nCH3, —C2-C8 alkynyl-N—(CH2)nCH3, —(CH2)m—OH, —(CH2)m—O—NH2, —(CH2)m—S—NH2, —NH(CH2)mCH3, —NH(CH2)mOCH3, —NH(CH2)mCHOH—COOH, —N(CH3)2, —(CH2)m(NH)CH2OH, —NHCOOH, —(CH2)mNHCOOH, —NO2, —SCN, —SO2alkyl, —B(OH)2, —(CH2)mN(CH3)—SO2—NH3, —(CH2)m—NH—SO2—NH2, —NHC(═S)CH3, and —NHNH2;
• Y is selected from hydrogen, ═O, —OCO(R6) and —OH;
• m is an integer between 0-20;
• n is an integer between 0-8;
• the symbol represents either a single or a double bond capable of forming a keto group at position 3 or 17;
• and
• the symbol represents any type of bond regardless of the stereochemistry;
• and the respective enantiomers, stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts thereof.