# US 12,180,193 B2 · Accelerating fibrosarcoma protein degrading compounds and associated methods of use

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 12,180,193 B2
- Document ID: US12180193B2
- Status: Granted
- Kind: B2
- Application number: 17/459,179
- Filed: 2021-08-27
- Published: 2023-03-16
- Granted: 2024-12-31
- Earliest claimed: 2020-08-28
- Assignees: Arvinas Operations, Inc.
- Applicants: Arvinas Operations, Inc.
- Inventors: Keith R. Hornberger; Jing Wang
- Web page: https://patentgrep.com/patent/US12180193B2

## CPC

- C07D 403/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- A61P 35/00: Antineoplastic agents
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (Raf, such as c-Raf, A-Raf, and/or B-Raf), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds Raf, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

## Claims

### Claim 1

A compound, wherein the compound is selected from the group consisting of:

### Claim 2 (depends on 1)

A composition comprising a compound of claim 1, and a pharmaceutically acceptable carrier.

### Claim 3 (depends on 2)

The composition of claim 2, wherein the composition further comprises at least one additional bioactive agent.

### Claim 4 (depends on 3)

The composition of claim 3, wherein the additional bioactive agent is an anti-cancer agent.