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US 7,351,709 B2Granted
Estrogen receptor ligands
AssigneeWyeth
InventorsPaige Erin Mahaney, Michael Byron Webb, Fei Ye, Joseph Peter Sabatucci
Life of this patent
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Abstract
The present invention relates to estrogen receptor ligands, and compounds and methods for treating diseases associated with excessive estrogen receptor activity. Compound of the formula I are disclosed: wherein W is O or (CR8)2, and R1 to R8, Y, and m are defined as defined herein.
Claims25
A compound of the structure I:
- or a pharmaceutically acceptable salt thereof;
- wherein:
- m is 1, 2, 3, 4, or 5;
- n is, independently, 0, 1, 2, 3, 4, or 5;
- W is O or C(R8)2;
- Y is (C(R8)2)n—X—(C(R8)2)n, wherein X is a bond, O, OC(═O), C(═O), or S(O)2;
- R1 is H, C1-C6 alkyl, C2-C7 alkenyl, cycloalkyl, cycloalkenyl, or arylalkyl;
- R2 and R3 are each, independently, H, C1-C6 alkyl, or C2-C7 alkenyl, provided that both are not H;
- R4, R5, R6, and R7 are each, independently, H, C1-C6 alkyl, C2-C7 alkenyl, hydroxyl, alkoxy, aryloxy, halogen, trifluoromethyl, CN, NO2, C(═O)R8, or C(═O)OR8;
- and
- R8 is, independently, H, C1-C6 alkyl, or phenyl,
- wherein each of said C1-C6 alkyl, said C2-C7 alkenyl, said cycloalkyl, said cycloalkenyl, said alkoxy, said arylalkyl, said aryloxy, and said phenyl is optionally substituted with 1-3 moieties independently selected from the group consisting of halogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, NR4R5, N[(CH2)2]2O, N[(CH2)2]2NR4, NHSO2R4, NR4C(═O)R5, NHC(—O)OR4, NO2, SO2NR4R5, SO2R4, OR4, C(═O)R4, COOR4, CONR4R5, and CN.
9 more elements
A compound of the structure II:
- or pharmaceutically acceptable salt thereof
- wherein:
- m is 1, 2, or 3;
- X is C(═O) or S(O)2;
- R1 is H, C1-C6 alkyl, C2-C7 alkenyl, cycloalkyl, cycloalkenyl, or arylalkyl;
- R2 and R3 are each, independently, H, C1-C6 alkyl, C2-C7 alkenyl, provided that both are not H;
- R4, R5, R6, and R7 are each, independently, H, C1-C6 alkyl, C2-C7 alkenyl, hydroxyl, alkoxy, aryloxy, halogen, trifluoromethyl, CN, NO2, C(═O)R8, or C(═O)OR8;
- and
- R8 is H, C1-C6 alkyl, or phenyl,
- wherein each of said C1-C6 alkyl, said C2-C7 alkenyl said cycloalkyl, said cyoloalkenyl, said alkoxy, said arylalkyl, said aryloxy, and said phenyl is optionally substituted with 1-3 moieties independently selected from the group consisting of halogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, NR4R5, N[(CH2)2]2O, N[(CH2)2]2NR4, NHSO2R4, NRC(—O)R5, NH4C(═O)OR4, NO2, SO2NR4R5, SO2R4;
- OR4, C(—O)R4, COOR4, CONR4R5, and CN.
8 more elements
Dependencies are inferred from the claim text.