Synthesis and Evaluation of Novel (4-Hydroxyphenyl) Substituted Carbocycles as Potent and Selective Estrogen Receptor Beta Agonists
AssigneesMarquette University, Concordia University
InventorsWilliam A. Donaldson, Daniel S. Sem, Edward A. Wetzel
Life of this patent
Estimating the term…
Abstract
Disclosed are 4-hydroxylphenyl substituted carbocycles and there use as selective agonists of the estrogen receptor beta isoform (ERβ). The disclosed compounds may be formulated as pharmaceutical compositions and administered to treat diseases associated with ER activity, such as proliferative diseases and disorders and/or psychiatric diseases or disorders.
Claims36
A compound having a Formula I:
- wherein X1, X2, Y1, and Y2 are independently selected from the group consisting of hydrogen, halogen, and hydroxyl;
- optionally with the proviso that when X1 and X2 are halogen then Y1 and Y2 are hydrogen and optionally with the proviso that when Y1 and Y2 are halogen then X1 and X2 are hydrogen;
- W is selected from the group consisting of hydrogen, hydroxyl, and oxo;
- R2, R3, R5, and R6 are independently selected from hydrogen, deuterium, and halogen;
- and
- R4 is hydrogen or a hydroxyl protecting group.
-3. (canceled)
-7. (canceled)
-11. (canceled)
-14. (canceled)
-19. (canceled)
A compound having a Formula II:
- wherein:
- R1a and R1b are independently selected from hydrogen, hydroxyl, carboxy alkyl ester, and hydroxy alkyl, optionally with the proviso that R1a and R1b are not the same;
- R1c is selected from hydrogen and hydroxyl;
- R2, R3, R5, and R6 are independently selected from hydrogen, deuterium, and halogen;
- and
- R4 is hydrogen or a hydroxyl protecting group.
-23. (canceled)
-28. (canceled)
-31. (canceled)
-34. (canceled)
-39. (canceled)
A compound having a Formula III:
- wherein R1 is selected from hydrogen, hydroxyl, alkyl, hydroxyalkyl, and haloalkyl;
- R2, R3, R5, and R6 are independently selected from hydrogen, deuterium, and halogen, with the proviso that if R3, R5, and R6 are hydrogen, then R1 is haloalkyl;
- and
- R4 is hydrogen or hydroxyl protecting group.
-49. (canceled)
-54. (canceled)
A compound having a Formula IV:
- wherein R2, R3, R5, and R6 are independently selected from hydrogen, deuterium, and halogen;
- R7 is hydrogen or alkyl;
- R8 and R9 are independently selected from the group consisting of hydrogen, hydroxyl, and hydroxyalkyl;
- a is 0 or 1;
- b is 0 or 1;
- and
- n is 0 or 1.
-58. (canceled)
(canceled)
-66. (canceled)
Dependencies are inferred from the claim text.