Composition and methods of use of tetrahydroisoquinoline small molecules to bind and modulate PCSK9 protein activity
US10865185B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Aug 19, 2016 |
| Grant date | Dec 15, 2020 |
| Priority date | — |
| Expiry date | Nov 27, 2036 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K45/06
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound 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 organic compound ligands that can raise LDL levels.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.