# US 12,109,198 B2 · Macrocyclic azolopyridine derivatives as EED and PRC2 modulators

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- Number: US 12,109,198 B2
- Document ID: US12109198B2
- Status: Granted
- Kind: B2
- Application number: 18/085,134
- Filed: 2022-12-20
- Published: 2024-05-02
- Granted: 2024-10-08
- Earliest claimed: 2019-03-15
- Assignees: Fulcrum Therapeutics, Inc.
- Applicants: Fulcrum Therapeutics, Inc.
- Inventors: Ivan Viktorovich Efremov; Steven Kazmirski; Qingyi Li; Lorin A. Thompson, III; Owen Brendan Wallace; Shawn Donald Johnstone; Feng Zhou; Peter Rahl
- Web page: https://patentgrep.com/patent/US12109198B2

## CPC

- A61P 35/00: Antineoplastic agents
- F41G 1/30: Reflecting-sights specially adapted for smallarms or ordnance (reflecting-sights in general G02B)
- C07D 491/18: Bridged systems
- C07D 491/22: in which the condensed system contains four or more hetero rings
- F21V 9/08: for producing coloured light, e.g. monochromatic; for reducing intensity of light (with provision for controlling the colour F21V9/40)
- F41G 1/345: {for illuminating the sights}
- G02B 23/00: Telescopes, e.g. binoculars; Periscopes; Instruments for viewing the inside of hollow bodies; Viewfinders; Optical aiming or sighting devices
- G02B 23/06: having a focussing action, e.g. parabolic mirror
- F21Y 2115/10: Light-emitting diodes [LED]
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- F41G: WEAPON SIGHTS; AIMING (optical aspects thereof G02B)
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- F21V: FUNCTIONAL FEATURES OR DETAILS OF LIGHTING DEVICES OR SYSTEMS THEREOF; STRUCTURAL COMBINATIONS OF LIGHTING DEVICES WITH OTHER ARTICLES, NOT OTHERWISE PROVIDED FOR
- G02B: OPTICAL ELEMENTS, SYSTEMS OR APPARATUS
- F21Y: INDEXING SCHEME ASSOCIATED WITH SUBCLASSES F21K, F21L, F21S and F21V, RELATING TO THE FORM OR THE KIND OF THE LIGHT SOURCES OR OF THE COLOUR OF THE LIGHT EMITTED

## 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.

## Claims

### Claim 1

A method of treating B-thalassemia in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound represented by 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:

### Claim 2 (depends on 1)

The method of claim 1, wherein R1 is

### Claim 3 (depends on 1)

The method of claim 1, wherein R2 is selected from the group consisting of H, C1 alkyl, and halogen.

### Claim 4 (depends on 1)

The method of claim 1, wherein the compound is represented by:

### Claim 5 (depends on 1)

The method of claim 1, wherein the compound is represented by: