# US 11,897,873 B2 · Kappa opioid receptor antagonists and products and methods related thereto

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- Number: US 11,897,873 B2
- Document ID: US11897873B2
- Status: Granted
- Kind: B2
- Application number: 17/390,531
- Filed: 2021-07-30
- Published: 2022-05-26
- Granted: 2024-02-13
- Earliest claimed: 2017-03-17
- Assignees: Blackthorn Therapeutics, Inc.; The Scripps Research Institute
- Applicants: The Scripps Research Institute; BlackThorn Therapeutics, Inc.
- Inventors: Edward Roberts; Miguel A. Guerrero; Mariangela Urbano; Hugh Rosen; Robert M. Jones; Candace Mae Laxamana; Xianrui Zhao; Eric Douglas Turtle
- Web page: https://patentgrep.com/patent/US11897873B2

## CPC

- C07D 413/14: containing three or more hetero rings
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/06: Antimigraine agents
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: wherein X, Y, R1, R2, R4, R5, R6, R7, R8 and R11 are as defined herein.

## Claims

### Claim 1

A pharmaceutical composition comprising a compound having the following structure, or a pharmaceutically acceptable hydrate, solvate, isotope or salt thereof, together with at least one pharmaceutically acceptable carrier, diluent or excipient:

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1 formulated for oral administration.

### Claim 3 (depends on 2)

The pharmaceutical composition of claim 2 wherein the oral formulation is a tablet, capsule, troche, lozenge, syrup or emulsion.

### Claim 4 (depends on 2)

The pharmaceutical composition of claim 2 wherein the oral formulation is a tablet or capsule.

### Claim 5 (depends on 3)

The pharmaceutical composition of claim 3 wherein the tablet or capsule is in a dosage form for administration once a day.

### Claim 6 (depends on 3)

The pharmaceutical composition of claim 3 wherein the tablet or capsule is in a dosage form for administration two or three times a day.