# US 10,441,586 B2 · CRMP2 SUMOylation inhibitors and uses thereof

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

- Number: US 10,441,586 B2
- Document ID: US10441586B2
- Status: Granted
- Kind: B2
- Application number: 15/766,299
- Filed: 2016-10-07
- Published: 2018-10-11
- Granted: 2019-10-15
- Earliest claimed: 2015-10-07
- Assignees: Arizona Board of Regents on Behalf of the University of Arizona
- Applicants: Arizona Board of Regents On Behalf of the University of Arizona
- Inventors: May Khanna; Rajesh Khanna; Vijay Gokhale; Reena Chawla
- Web page: https://patentgrep.com/patent/US10441586B2

## CPC

- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/452: Piperidinium derivatives (pancuronium A61K31/58)
- A61K 31/4525: containing a five-membered ring with oxygen as a ring hetero atom
- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61P 25/02: for peripheral neuropathies
- C07D 295/135: with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
- C07D 295/185: from aliphatic carboxylic acids
- C07D 317/68: Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention provides compounds that can modulate the amount of Nav 1.7 protein, a key protein in pain signaling, that is present in the cellular surface and methods for using such compounds. In particular, compounds of the invention modulate the amount of Nav 1.7 protein on the cellular surface by modulating SUMOylation of CRMP2. Thus, compounds of the invention can be used to treat various clinical conditions associated with the presence and/or activation of Nav 1.7 protein on the cellular surface and/or SUMOylation of CRMP2.

## Claims

### Claim 1

A compound encompassed within the following formula:
wherein X is either NH or O;
wherein R1 is selected from the group consisting of
selected from the group consisting of:
wherein R2 is selected from the group consisting of hydrogen, OCH3, and Flourine;
wherein R3 is selected from the group consisting of

### Claim 2 (depends on 1)

The compound of claim 1, wherein the compound is selected from