PCSK9 inhibitors and methods of use thereof
AssigneeAstraZeneca AB
InventorsMichael H. Serrano-Wu, Brian K. Hubbard, Virendar Kaushik, Doug Daniels
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Abstract
The invention relates to a novel inhibitor pharmacophore of PCSK9 and heteroaryl compounds that bind the PCSK9 protein.
Claims20
A compound or pharmaceutically acceptable salt thereof, wherein the compound contacts PCSK9 and binds to a binding pocket defined by amino acid residues Val589 and Ser636 of human PCSK9,
- wherein the compound or pharmaceutically acceptable salt thereof comprises an H-bond acceptor/donor group having two H-bond acceptor moieties and one H-bond donor moiety to form two H-bonds with residue Val589, and form one H-bond with Ser636 of human PCSK9.
The compound or pharmaceutically acceptable salt thereof according to 1, wherein the compound or pharmaceutically acceptable salt thereof comprises an H-bond acceptor/donor group having two H-bond donor moieties and one H-bond acceptor moiety disposed to donate an H-bond to and accept an H-bond from the backbone amide functionality of residue Val589, and donate an H-bond to the hydroxymethyl sidechain of Ser636 of human PCSK9.
Dependencies are inferred from the claim text.