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US 2020/0206299 A1Published application
Inhibitors of beta-arrestin-neurokinin 1 receptor interactions for the treatment of pain
AssigneeTakeda Pharmaceutical Company Limited
InventorNigel Bunnett
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Abstract
The present invention relates to compounds and their uses. In particular, to compounds that inhibit the interaction between β-arrestin and the intracellular C-terminus of the activated NK1R and their use in the treatment of pain.
Claims21
A method for the treatment of a disease or disorder mediated by endosomal substance P (SP) or neurokinin 1 receptor (NK1R) signaling comprising administering to a subject in need thereof a compound that inhibits interaction between β-arrestin and the intracellular C-terminus of the activated NK1R.
A β-arrestin inhibitor of the formula:
- A-D
- wherein
- A is a membrane permeant residue that facilitates transport of the β-arrestin inhibitor across a cellular membrane, and
- D represents a fragment of one or more phosphorylation sites on the intracellular C-terminus of NK1R, or
- a pharmaceutically acceptable salt thereof.
2 more elements
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Dependencies are inferred from the claim text.