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Publication Number
US-11987558-B1
Publication Date
2024-05-21
Expiration Date
Abstract
The present disclosure relates to ALK5 inhibitors and their uses.
Core Innovation
The patent describes ALK5 inhibitor-antibody conjugates (ADCs) having an ADC linker architecture that includes an antibody component, a linker moiety connected to a drug moiety, and a drug loading parameter p. The disclosure represents the ADC by Ab-(-[Aa-Ww-Yy]-D)p and describes parameters for drug loading, including embodiments with about 2-8 drugs/antibody, often about 2-4 or 5-7, and preferred embodiments such as about 1-8.
The ALK5 inhibitors are described as small-molecule drug moieties in ADCs and as ATP-competitive reversible ALK5 inhibitors that prevent R-Smad phosphorylation. The anti-T cell surface antibody is described in terms of internalizing antibodies and multiple antibody formats, and target molecules on T cells include CD3, CD4, CD8, CD25, and PD1.
The disclosure further describes linker architectures for attaching ALK5 inhibitors to antibodies in ADCs. The linkers are characterized as cleavable or non-cleavable, including acid-labile linkers, protease-sensitive linkers, and disulfide/reducing linkers, with direct linkage also described.
Claims Coverage
The provided claim text identifies one independent claim directed to a compound having a specified structure, with a dependent refinement specifying the hydrochloride salt form. The inventive coverage in the input is therefore limited to a structurally defined compound and its HCl salt form.
Specified compound structure
A compound having the structure.
Hydrochloride salt form
The HCl (hydrochloride) salt of the compound having the structure.
Claim coverage centers on a structurally defined compound, with a refinement that specifies the compound as an HCl salt.
Stated Advantages
Reduce on-target toxicity associated with TGF-β pathway inhibition.
Avoid tumor-promoting effects of broad TGF-β pathway blockade.
Documented Applications
Use of ALK5 inhibitor small-molecule structures as drug moieties in antibody-drug conjugates (ADCs), including linker attachment architectures and ADC formation context.
Targeting T cells with ALK5 inhibition through anti–T cell surface antibody conjugates.
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