CRMP2 SUMOylation inhibitors and uses thereof

Patent metadata

Field	Value
Publication number	US-10441586-B2
Application number	US-201615766299-A
Country	US
Kind code	B2
Filing date	Oct 7, 2016
Priority date	Oct 7, 2015
Publication date	Oct 15, 2019
Grant date	Oct 15, 2019

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.

First claim

What is claimed is:

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

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

Assignees

• Univ Arizona

Inventors

• Khanna May
• Khanna Rajesh
• Gokhale Vijay
• Chawla Reena

Classifications

• C07D405/12

  linked by a chain containing hetero atoms as chain links · CPC title

• C07D317/68

  Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen · CPC title

• C07D295/185

  from aliphatic carboxylic acids · CPC title

• C07D295/135

  with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings · CPC title

• A61K31/495

  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}) · CPC title