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The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Patent No.:

US 10688114 B1

PDFFull Text
Date of Patent:
Jun. 23, 2020

Filed:

Apr. 10, 2019

Composition and methods of use of small molecules as binding ligands for the modulation of proprotein convertase subtilisin/kexin type 9(pcsk9) protein activity

Applicant:

Srx Cardio, Llc, Pittsford, NY (US);

Inventors:

Thomas E Barta, Carrboro, NC (US);

Jonathan W Bourne, Fairport, NY (US);

Kyle D Monroe, Pittsford, NY (US);

Michael M Muehlemann, Liverpool, NY (US);

Assignee:

SXR Cardio, LLC, Pittsford, NY (US);

Attorney:

Medlen & Carroll, LLP

Primary Examiner:

Taofiq A Solola

Int. Cl.
CPC ...
A61K 31/675 (2006.01); C07F 9/59 (2006.01); C07F 9/6518 (2006.01); A61K 45/06 (2006.01); A61K 31/41 (2006.01); A61K 31/454 (2006.01); A61K 31/4245 (2006.01); A61K 31/683 (2006.01); A61K 38/00 (2006.01); A61K 38/05 (2006.01); C07D 401/12 (2006.01); C07D 403/12 (2006.01); C07D 413/14 (2006.01); C07F 9/653 (2006.01); C07K 5/065 (2006.01);
U.S. Cl.
CPC ...
A61K 31/675 (2013.01); A61K 31/41 (2013.01); A61K 31/4245 (2013.01); A61K 31/454 (2013.01); A61K 31/683 (2013.01); A61K 38/005 (2013.01); A61K 38/05 (2013.01); A61K 45/06 (2013.01); C07D 401/12 (2013.01); C07D 403/12 (2013.01); C07D 413/14 (2013.01); C07F 9/59 (2013.01); C07F 9/6518 (2013.01); C07F 9/65312 (2013.01); C07K 5/06078 (2013.01);
Abstract

This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.

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