US 2022/0125762 A1 · SMALL MOLECULE ANTAGONIST TO PACAP RECEPTOR AND USES THEREOF

Abstract

The invention relates to compounds that demonstrate efficacy in blocking PACAP receptors (e.g. PAC1) and associated methods of treating neurological diseases or disorders using the disclosed compounds. The neurological diseases or disorders include, but are not limited to, stress-related diseases (e.g. chronic stress, post-traumatic stress disorder (PTSD), anxiety, or general anxiety disorder), pain-related diseases (e.g. chronic pain, primary headache disorders, or migraines), or addiction (e.g. addiction to a substance (e.g. addiction to cocaine, amphetamines, methamphetamine, methylphenidate, nicotine, alcohol, prescription medication, marijuana, tobacco, or an opioid selected from heroin, fentanyl, codeine, hydrocodone, morphine, oxycodone, hydromorphone, and methadone)).

Claims88

Dependent claims

A compound of Formula (I):

or a pharmaceutically acceptable salt, solvate, hydrate, polymorph, co-crystal, tautomer, isotopologue, stereoisomer, or prodrug thereof, wherein:
R1 is independently optionally substituted aryl, optionally substituted heteroaryl, halogen, —CN, —NO2, or —C(═O)ORa, wherein each Ra is independently H, or optionally substituted C1-6 alkyl;
R2 is halogen or —NO2;
X1 and X2 are independently C—H or N;
and
n is 1, 2, or 3.

3 more elements

Dependencies are inferred from the claim text.

Facts

Application

17/429,843Filed 13 Feb 2020

Priority

13 Feb 2019

Published

28 Apr 2022

Term ends

Not estimatedThe source records don’t support an estimate.

Classification16 codes

A61K 31/4045
Indoles, e.g. pindolol: indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
A61K 45/06
Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00: mixtures of active ingredients without…
A61K 31/166
Having aromatic rings, e.g. colchicine, atenolol, progabide: having the carbon of a carboxamide group directly attached to the aromatic ring, e.g.…
A61K 31/404
Condensed with carbocyclic rings, e.g. carbazole: indoles, e.g. pindolol

Small molecule antagonist to pacap receptor and uses thereof

Life of this patent

Small molecule antagonist to pacap receptor and uses thereof

Life of this patent

Abstract

Claims88