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US 2017/0362210 A1Published application
Anti-estrogenic compounds
AssigneePfizer Inc.
InventorsPeter J. KUSHNER, David C. MYLES, Cyrus L. HARMON, Leslie Carol HODGES GALLAGHER
Life of this patent
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Abstract
The present disclosure provides a compound of Formula I: or a pharmaceutically acceptable salt wherein X, R1-R8, Y1-Y5, m, n, p, and q are defined herein. The novel 2H-chromene compounds are useful for the modulation of disorders mediated by estrogen, and other disorders, as described herein. The present invention also relates to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions.
Claims26
A compound of Formula I
- or a pharmaceutically acceptable salt thereof,
- wherein
- X is CH2, O, S, NH, or N—(C1-C4 alkyl);
- R1 is —(C(Y1)(Y2))m—C((Y3)(Y4)(Y5)), wherein Y1, Y2, Y3, Y4 and Y5 are independently hydrogen or fluorine;
- m is 0 or 1;
- R2 is hydrogen, halogen, cyano, or hydroxy;
- R3 is hydrogen, halogen, C1-C4 alkyl, —CH2F, —CHF2, or —CF3;
- R4 and R5 are each independently hydrogen, halogen, or hydroxy, provided that R4 and R5 are not both hydroxy;
- R6 and R7 are each independently hydrogen or halogen;
- R8 is hydrogen, halogen, cyano, hydroxy, or C1-4 alkyl;
- n is 1 or 2;
- p is 1 or 2;
- and
- q is 1.
11 more elements
A compound of Formula II
- or a pharmaceutically acceptable salt thereof,
- wherein
- X is CH2, O, S, NH, or N—(C1-C4 alkyl);
- R1 is —(C(Y1)(2))m—C((Y3)(Y4)(Y5)), wherein Y1, Y2, Y3, Y4, and Y5 are independently hydrogen or fluorine;
- m is 0 or 1;
- R2 is hydrogen, halogen, cyano, or hydroxy;
- R3 is hydrogen, halogen, C1-C4 alkyl, —CH2F, —CHF2, or —CF3;
- R4 and R5 are each independently hydrogen, halogen, or hydroxy, provided that R4 and
- R5 are not both hydroxy;
- and
- R6 and R7 are each independently hydrogen or halogen.
8 more elements
A compound, which is
- or a pharmaceutically acceptable salt thereof.
A compound, which is
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.