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US 2024/0308986 A1Published application
Estrogen receptor-modulating compounds
AssigneeRadius Pharmaceuticals, Inc.
InventorChris MILLER
Life of this patent
Estimating the term…
Abstract
Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
Claims12
1-4. (canceled)
A compound of formula II′
- wherein:
- each Ra is independently selected from H, C1-C3 alkyl, phenyl (optionally substituted with 1-3 groups selected from fluorine, chlorine, C1-C3 alkyl, CN, OC1-C3 alkyl, OH), OH, OC1-3alkyl, CN, fluorine, chlorine, O(CO)R, O(CO)NR1R2, OPO3, OSO3, O(SO2)NR1R2, or two adjacent Ra together form:
- R is C1-C6 alkyl or aryl;
- R1 and R2 are each independently hydrogen or C1-C6 alkyl;
- each R3 is independently hydrogen;
- C1-C12 acyl or C1-C12 acyloxy;
- each R4 is independently hydrogen, C1-C3 alkyl, fluorine or chlorine;
- each Re is independently selected from hydrogen, halogen, OH, O(CO)R, O(CO)NR1R2, OPO3, OSO3, O(SO2)NR1R2, or wherein two adjacent Re together form:
- each Rf is independently H, C1-C3 alkyl, OC1-C3 alkyl, fluorine or chlorine;
- Rg is hydrogen, C1-C3 alkyl, C1-C3 fluoroalkyl, CN, fluorine, chlorine or bromine;
- X is CH2 or a bond;
- Y is N, and Z is selected from CRf or N;
- U and V are each independently selected from CRa or N;
- and
- W is —CHR′—CHR′—NH—C1-C4alkyl, —CHR′—CHR′—NH—C1-C4fluoroalkyl, —CHR′—CHR′—NH—C3-C6cycloalkyl, —CHR′—CHR′—NH—C1-C4alkyl-C3-C6cycloalkyl,
- wherein each R′ is independently H or C1-C3alkyl;
- or a pharmaceutically acceptable salt thereof.
14 more elements
8-27. (canceled)
A compound selected from:
- 1-(4-(2-((Cyclopropylmethyl)amino)ethyl)benzyl)-2-(4-methoxyphenyl)-3-methyl-1H-indol-5-ol;
- 1-(4-(2-((Cyclopropylmethyl)amino)ethyl)benzyl)-3-fluoro-2-(o-tolyl)-1H-indol-5-ol;
- and
- 2-Fluoro-N-(4-((8-fluoro-7-(o-tolyl)pyrrolo[3,2-e]indazol-6(3H)yl)methyl)phenethyl)ethan-1-amine.
1 more element
Dependencies are inferred from the claim text.