Macrocyclic azolopyridine derivatives as EED and PRC2 modulators
AssigneeFulcrum Therapeutics, Inc.
InventorsIvan Viktorovich Efremov, Steven Kazmirski, Qingyi Li, Lorin A. Thompson, III, Owen Brendan Wallace, Shawn Donald Johnstone, Feng Zhou, Peter Rahl
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Abstract
The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula I: or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X1, X2, X3, A1, A2, Y, R1, R2, R3, and R4 are as described herein.
Claims10
A compound having the formula Ih-a:
- or a pharmaceutically acceptable salt thereof,
- wherein
- A1 is —O—;
- A2 is —CH2—;
- R2 and R3 are each independently selected, for each occurrence, from the group consisting of:
- H, halogen, —OH, and C1 alkyl, wherein the C1 alkyl is optionally substituted with one or more halogens;
- and
- R1 is selected from the group consisting of:
A compound represented by:
- or a pharmaceutically acceptable salt thereof.
A compound represented by:
- or a pharmaceutically acceptable salt thereof.
A method of treating sickle cell disease in a subject in need thereof, comprising administering to the subject an effective amount of a compound according to the formula:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.