IP Library Granted Patent US 12,528,803
Granted Patent B2
US 12,528,803 · App. 17/967,346 · Granted Jan 20, 2026

Inhibitors of αvβ6 integrin

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); 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
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Quick Facts
Patent No.
US 12,528,803
App. No.
17/967,346
Granted
Jan 20, 2026
Kind
B2
Abstract

Disclosed are small molecule inhibitors of αvβ6 integrin, and methods of using them to treat a number of diseases and conditions. The small molecule inhibitors of αvβ6 integrin have a tetrahydroquinoline moiety linked by a -alkylene-CH(F)—, -alkylene-C(F) 2 —, -alkylene-CH(F)CH 2 —, -alkylene-C(F)2CH 2 —, -alkylene-O-alkylene-CH(F)—, or -alkylene-O-alkylene-C(F) 2 — to a pyrrolidine moiety.

Claims (36)

1 . A compound of formula (I):

A-B—C  (I)

wherein:

A is

B is -alkylene-C*H(F)—, -alkylene-C*(F) 2 —, -alkylene-CH(F)C*H 2 —, or -alkylene-C(F) 2 C*H 2 —;

C is

R 1 , in each instance, is independently H, alkyl, or alkoxy;

R 2 is substituted or unsubstituted aryl;

R 3 is H,

R a is H or (C 1 -C 6 )alkyl;

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

* denotes the point of attachment of B to C; and

the absolute configuration at any stereocenter is R, S, or a mixture thereof;

or a pharmaceutically acceptable salt thereof.

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

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

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

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

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

7 . The compound of claim 6 , wherein R 2 is substituted with one or more substituents independently selected from alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, alkoxy, OH, halide, —(O)alkyl, -alkylene-heteroaryl, -alkylene-O-alkyl; -alkylene-O-cycloalkyl, alkylene-O-heterocyclocycloalkyl, —O-alkylene-cycloalkyl, —O-alkylene-heterocycloalkyl, and each of which can be further substituted with alkyl, halogen, and alkoxyl.

8 . The compound of claim 1 , wherein B is —(CH 2 ) 4 C*H(F)— or —(CH 2 ) 4 C*(F) 2 —.

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

or a pharmaceutically acceptable salt thereof.

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

or a pharmaceutically acceptable salt thereof.

11 . The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

12 . The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

13 . The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

14 . The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

15 . The compound of claim 1 , wherein the compound is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

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

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 2, 2022
From: HARRISON, BRYCE A.; DOWLING, JAMES E.; BURSAVICH, MATTHEW G.; TROAST, DAWN M.; LIPPA, BLAISE S.; ROGERS, BRUCE N.; ZHONG, CHENG; LIN, FU-YANG; SOSA, BRIAN S.
To: MORPHIC THERAPEUTIC, INC.
Reel/Frame 061633/0542 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 2, 2022
From: GERASYUTO, ALEKSEY I.; BORTOLATO, ANDREA; SVENSSON, MATS A.; HICKEY, EUGENE; KONZE, KYLE D.; DAY, TYLER; KIM, BYUNGCHAN
To: SCHRÖDINGER, INC.
Reel/Frame 061633/0562 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 2, 2022
From: SCHRÖDINGER, INC.
To: SCHRÖDINGER, LLC
Reel/Frame 061633/0583 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 2, 2022
From: SCHRÖDINGER, LLC
To: MORPHIC THERAPEUTIC, INC.
Reel/Frame 061875/0480 →
Continuity (5)
Continuation 17717672 · Apr 11, 2022
Continuation 17513449 · Oct 28, 2021
Continuation 17271985
Provisional Application 62724397 · Aug 29, 2018
Related Publication 20230242524A1 · Aug 3, 2023
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