Novel arylalkene derivatives and use thereof as selective estrogen receptor modulators

A pharmaceutical composition, comprising a compound of formula I:

• wherein
• R0 and R1 are independently selected from the group consisting of hydrogen, halogen, alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein the alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are each optionally substituted with one or more groups selected from the group consisting of halogen, —OH, —NH2, —SH, alkyl, halogenated alkyl and alkoxy, and the carbon atoms on the ring of the cycloalkyl, the heterocyclyl and the heteroaryl are optionally oxidized;
• ring A and ring B are each independently selected from aryl, heteroaryl and heterocyclyl, wherein the carbon atoms on the ring of the heterocyclyl and the heteroaryl are optionally oxidized;
• R2 and R3 are independently selected from the group consisting of halogen, —OH, —NH2, —CN, —SH, —COOH, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, alkoxy, alkylsulfanyl, cycloalkyloxy, heterocyclyloxy, monoalkylamino, dialkylamino, —S(O)-alkyl and —S(O)2-alkyl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, alkoxy, alkylsulfanyl, cycloalkyloxy, heterocyclyloxy, monoalkylamino, dialkylamino, —S(O)-alkyl and —S(O)2-alkyl are each optionally substituted with halogen, —OH, heterocyclyl or —NR4R5, wherein R4 and R5 are each independently hydrogen, alkyl or cycloalkyl, or R4 and R5, together with the nitrogen atom to which they attach, form a heterocyclyl which is optionally substituted with alkyl;
• m and n are the number of group R2 on ring A and the number of group R3 on ring B, respectively, and m and n are each independently 0, 1, 2 or 3,
• or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer or prodrug thereof, as well as a pharmaceutically acceptable carrier.

A method for preventing and/or treating estrogen-dependent diseases and conditions in mammals, especially in humans, which method comprises administering to a mammal, especially a human, in need thereof a therapeutically effective amount of a compound of formula I:

• wherein
• R0 and R1 are independently selected from the group consisting of hydrogen, halogen, alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein the alkyl, cycloalkyl heterocyclyl, aryl and heteroaryl are each optionally substituted with one or more groups selected from the group consisting of halogen, —OH, —NH, —SH, alkyl, halogenated alkyl and alkoxy, and the carbon atoms on the ring of the cycloalkyl, the heterocyclyl and the heteroaryl are optionally oxidized;
• ring A and ring B are each independently selected from aryl, heteroaryl and heterocyclyl, wherein the carbon atoms on the ring of the heterocycyl and the heteroaryl are optionally oxidized;
• R2 and R3 are independently selected from the group consisting of halogen, —OH, —NH2, —CN, —SH, —COOH, alkyl, alkenyl, alkynyl, cycloalkyl heterocyclyl, alkoxy, alkylsulfanyl, cycloalkyloxy, heterocyclyloxy, monoalkylamino, dialkylamino, —S(O)-alkyl and —S(O)2-alkyl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, alkoxy, alkylsulfanyl, cycloalkyloxy, heterocyclyloxy, monoalkylamino, dialkylamino, —S(O)-alkyl and —S(O)2-alkyl are each optionally substituted with halogen, —OH, heterocyclyl or —NR4R5, wherein R4 and R5 are each independently hydrogen, alkyl or cycloalkyl, or R4 and R5, together with the nitrogen atom to which they attach, form a heterocyclyl which is optionally substituted with alkyl;
• m and n are the number of group R2 on ring A and the number of group R3 on ring B, respectively, and m and n are each independently 0, 1, 2 or 3,
• or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer or prodrug thereof.