# US 10,246,458 B2 · Ergoline compounds and uses thereof

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- Number: US 10,246,458 B2
- Document ID: US10246458B2
- Status: Granted
- Kind: B2
- Application number: 15/943,714
- Filed: 2018-04-03
- Published: 2018-11-15
- Granted: 2019-04-02
- Earliest claimed: 2015-01-20
- Assignees: Xoc Pharmaceuticals, Inc.
- Applicants: Xoc Pharmaceuticals, Inc.
- Inventors: Thomas Armer; Geoff McKinley; Scott Borland; Miguel Guzman; Ármin Szabolcs; János Gerencser
- Web page: https://patentgrep.com/patent/US10246458B2

## CPC

- C07D 471/06: Peri-condensed systems
- A61P 1/08: for nausea, cinetosis or vertigo; Antiemetics
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/06: Antimigraine agents
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/20: Hypnotics; Sedatives
- A61P 25/22: Anxiolytics
- A61P 25/24: Antidepressants
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 25/30: for treating abuse or dependence
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 495/06: Peri-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Provided herein are ergoline compounds and pharmaceutical compositions thereof. In some embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1A, 5-HT1B and 5-HT1D receptors without agonizing the 5-HT2B receptor using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the 5-HT2B adrenergic alpha2A and/or the alpha2B receptors using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the D2 and D3 receptor using the compounds and pharmaceutical compositions disclosed herein.

## Claims

### Claim 1

A compound represented by structural Formula (VIII):
or a salt thereof, wherein:
R1 is cycloalkyl;
R3 is hydrogen or alkyl;
R4 and R5 are independently hydrogen, halo, —OR120, —OC(O)NR121R122, —OC(O)R123 or together with the atoms to which they are attached form a double bond;
R6 and R7 are independently hydrogen, alkyl or substituted alkyl;
R8 is alkyl;
R120 is hydrogen or alkyl;
R121, R122 are independently hydrogen or alkyl; and
R123 is alkyl.

### Claim 2 (depends on 1)

The compound or salt of claim 1, wherein R6 is hydrogen.

### Claim 3 (depends on 1)

The compound or salt of claim 1, wherein R1 is cyclopropyl.

### Claim 4 (depends on 1)

The compound or salt of claim 1, wherein R3 is methyl.

### Claim 5 (depends on 1)

The compound or salt of claim 1, wherein R4 and R5 are independently hydrogen or halo.

### Claim 6 (depends on 5)

The compound or salt of claim 5, wherein R4 is hydrogen.

### Claim 7 (depends on 5)

The compound or salt of claim 5, wherein R5 is hydrogen.

### Claim 8 (depends on 1)

The compound or salt of claim 1, wherein R7 is a substituted alkyl.

### Claim 9 (depends on 8)

The compound or salt of claim 8, wherein R7 is alkyl substituted by hydroxyl or methoxy.

### Claim 10 (depends on 1)

The compound or salt of claim 1, wherein R8 is methyl.

### Claim 11 (depends on 1)

The compound of claim 1, represented by the structure:
or a salt thereof.

### Claim 12 (depends on 1)

The compound of claim 1, represented by the structure:
or a salt thereof.

### Claim 13 (depends on 1)

The compound of claim 1, represented by the structure:
or a salt thereof.

### Claim 14 (depends on 1)

The compound of claim 1, represented by the structure:
or a salt thereof.

### Claim 15 (depends on 1)

The compound of claim 1, represented by the structure:
or a salt thereof.

### Claim 16 (depends on 1)

A pharmaceutical composition comprising a compound or salt of claim 1 and a pharmaceutically acceptable excipient.