Granted Patent B2

US 12,552,786 · App. 17/967,342 · Granted Feb 17, 2026

Inventors: Bryce A. Harrison (Framingham, MA); James E. Dowling (Lexington, MA); Aleksey I. Gerasyuto (Flemington, NJ); Matthew G. Bursavich (Needham, MA); Dawn M. Troast (Bedford, MA); Blaise S. Lippa (Newton, MA); Bruce N. Rogers (Belmont, MA); Cheng Zhong (Belmont, MA); Qi Qiao (Natick, MA); Fu-Yang Lin (Sudbury, MA); Brian Sosa (Cambridge, MA); Andrea Bortolato (Metuchen, NJ); Mats A. Svensson (New York, NY); Eugene Hickey (Danbury, CT); Kyle D. Konze (Katonah, NY); Tyler Day (New York, NY); Byungchan Kim (West New York, NJ)

Assignee: Morphic Therapeutic, Inc.

C07D471/04A61K9/0053C07D519/00

Abstract

Claims (44)

1 . A compound of formula (I):

A-B—C  (I)

wherein:

A is

B is-alkylene-(O)—;

C is

R is H, alkyl, or aryl;

R 1 is independently selected from the group consisting of H, alkyl, halide, alkoxy, CF 3 , OH, alkylene-OH, NO 2 , —N(H)R, and NH 2 ;

R 2 is substituted or unsubstituted benzoxazolyl, quinolinyl, benzothiophenyl, indazolyl, indolyl, benzotriazolyl, benzisoxazolyl, benzisothiazolyl, or benzthiazolyl;

R 3 is independently selected from the group consisting of H, halide, CF 3 , alkyl, alkylene-alkoxy, aryl, hydroxyl, and alkoxy;

R a is H, (C 1 -C 6 )alkyl, —(C 1 -C 6 )alkylene-O—(C 1 -C 6 )alkyl, or —(C 1 -C 6 )alkylene-O—C(O)O(C 1 -C 6 )alkyl; and

n is 0, 1, 2, 3, or 4;

or a pharmaceutically acceptable salt thereof.

2 . The compound of claim 1 , wherein B is —(CH 2 ) 4 —O—.

3 . The compound of claim 1 , wherein at least one instance of R 1 is alkyl, halide, OMe, OH, alkylene-OH, or NH 2 .

4 . The compound of claim 3 , wherein the at least one instance of R 1 is OMe.

5 . The compound of claim 1 , wherein all instances of R 1 are H.

6 . The compound of claim 1 , wherein R 2 is unsubstituted.

7 . The compound of claim 1 , wherein R 2 is substituted.

8 . The compound of claim 7 , wherein R 2 is substituted with one or more substituents independently selected from the group consisting of alkyl, heterocycloalkyl, alkoxy, —(O)alkyl, -alkylene-O-alkyl, -alkylene-cycloalkyl, -alkylene-O-alkyl, cycloalkyl, aryl, heteroaryl, OH, halide, -alkylene-heteroaryl, -alkylene-O-cycloalkyl, -alkylene-O-heterocyclocycloalkyl, —O-alkylene-cycloalkyl, and —O-alkylene-heterocycloalkyl, wherein each substituent can be further substituted with alkyl, halide, or alkoxyl.

9 . The compound of claim 1 , wherein R 2 is selected from the group consisting of:

wherein R 3 ′ is selected from the group consisting of alkyl, cycloalkyl, alkyl-cycloalkyl, alkoxy, and O-containing heterocycloalkyl.

10 . The compound of claim 1 , wherein R 2 is selected from the group consisting of:

11 . The compound of claim 1 , wherein R 3 is H, halide, Me, OMe, or Ph.

12 . The compound of claim 1 , wherein R a is H.

13 . A pharmaceutical composition, comprising a compound of claim 1 ; and a pharmaceutically acceptable excipient.

14 . The compound of claim 1 ,

wherein:

each R 1 is H;

R a is H; and

n is 0;

or a pharmaceutically acceptable salt thereof.

15 . The compound of claim 14 , wherein B is —(CH 2 ) 4 —O—.

16 . The compound of claim 14 , wherein R 2 is selected from the group consisting of

or the group consisting of

or the group consisting of

or the group consisting of

wherein R 3 ′ is selected from the group consisting of alkyl, cycloalkyl, alkyl-cycloalkl, alkoxy, and O-containing heterocycloalkyl.

17 . The compound of claim 14 , wherein R 2 is selected from the group consisting of

18 . A pharmaceutical composition formulated for oral administration, comprising a compound of claim 14 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient suitable for oral administration.

19 . The compound of claim 1 selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

20 . A compound having the structure:

or a pharmaceutically acceptable salt thereof.

Assignments (4)

Continuity (5)

References Cited (235)