Granted Patent
B2
US 12,473,377 · App. 18/146,269 · Granted Nov 18, 2025
Antibody-ALK5 inhibitor conjugates and their uses
Assignee:
Synthis Therapeutics, Inc.
C07K16/4283A61K47/6803A61K47/6851C07D231/04C07K16/2881C07K16/30C07K2317/21C07K2317/24C07K2317/54C07K2317/55C07K2317/56
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Abstract
The present disclosure relates to antibody-drug conjugates comprising ALK5 inhibitors and their uses.
Claims (15)
1 . A process for making an antibody drug conjugate (ADC), comprising conjugating an ALK5 inhibitor having the structure
or
to one or more reduced cysteine residues of an antibody or antigen binding fragment thereof.
2 . The process of claim 1 , wherein the ALK5 inhibitor is conjugated to the one or more reduced cysteine residues of the antibody or antigen binding fragment thereof via a protease-sensitive linker.
3 . The process of claim 2 , wherein the protease-sensitive linker comprises a dipeptide, a tripeptide, a tetrapeptide, or a pentapeptide.
4 . The process of claim 2 , wherein the protease-sensitive linker comprises a valine-citrulline dipeptide.
5 . The process of claim 1 , wherein the ALK5 inhibitor has the structure
6 . The process of claim 1 , wherein the ALK5 inhibitor has the structure
7 . The process of claim 1 , which comprises conjugating a compound having the structure
to one or more reduced cysteine residues of the antibody or antigen binding fragment thereof.
8 . The process of claim 1 , further comprising, prior to conjugating the ALK5 inhibitor to one or more reduced cysteine residues of the antibody or antigen binding fragment thereof, contacting the antibody or antigen binding fragment thereof with dithiothreitol (DTT) or tricarbonylethylphosphine (TCEP) to provide one or more reduced cysteine residues on the antibody or antigen binding fragment thereof.
9 . A process for making an antibody drug conjugate (ADC), comprising:
(a) contacting an antibody or antigen binding fragment thereof with dithiothreitol (DTT) or tricarbonylethylphosphine (TCEP); and
(b) conjugating a compound having the structure
to one or more reduced cysteine residues on the antibody or antigen binding fragment thereof.
Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Oct 20, 2025
From: THOMAS-KARYAT, DORI A.
To: SYNTHIS, LLC
Reel/Frame 072601/0669 →
MERGER AND CHANGE OF NAME
Recorded Oct 20, 2025
From: SYNTHIS THERAPEUTICS, INC.; SYNT, INC.
To: SYNTHIS THERAPEUTICS, INC.
Reel/Frame 072601/0965 →
CHANGE OF NAME
Recorded Oct 20, 2025
From: SYNTHIS, LLC
To: SYNTHIS THERAPEUTICS, INC.
Reel/Frame 073161/0921 →
Continuity (6)
Continuation
16286122
· Feb 26, 2019
Continuation
16029351
· Jul 6, 2018
Continuation
15404233
· Jan 12, 2017
Provisional Application
62278928
· Jan 14, 2016
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