Substituted 1-methyl-1,2,3,4-tetrahydroisoquinoline molecules as PCSK9 allosteric binders
US11008313B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Sep 15, 2017 |
| Grant date | May 18, 2021 |
| Priority date | — |
| Expiry date | May 12, 2038 |
Classification
- Technology area (CPC G)Physics
- CPC primaryG01N2333/96433
- WIPO fieldMeasurement
- WIPO sectorInstruments
Abstract
The present invention relates to PCSK9 allosteric binding compounds of Formula I: (Formula (I)) and pharmaceutically acceptable salts thereof, wherein X1, X2, Y, R1, R2, RA, RB and n are as defined herein. The present invention also relates to compositions which comprise an allosteric binding compound of the invention or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. The invention further relates, inter alia, to methods for inducing PCSK9 protein degradation in a subject, and methods for treating atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions, comprising administering to a subject an effective amount of a compound or a pharmaceutically acceptable salt of the invention. The invention also provides a means for the in vitro labeling, detection and/or quantification of PCSK9 in biological samples.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.