# US 11,299,496 B2 · Ligands for alpha-7 nicotinic acetylcholine receptors and methods of treating neurological and inflammatory conditions

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- Number: US 11,299,496 B2
- Document ID: US11299496B2
- Status: Granted
- Kind: B2
- Application number: 15/328,112
- Filed: 2015-07-23
- Published: 2017-08-03
- Granted: 2022-04-12
- Earliest claimed: 2014-07-23
- Assignees: Northeastern University; University of Florida Research Foundation, Inc.
- Applicants: Northeastern University; University of Florida Research Foundation, Inc.
- Inventors: Ganeshsingh A. Thakur; Abhijit R. Kulkarni; Roger Lee Papke
- Web page: https://patentgrep.com/patent/US11299496B2

## CPC

- C07D 495/04: Ortho-condensed systems
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- C07D 221/16: containing carbocyclic rings other than six-membered
- C07D 401/04: directly linked by a ring-member-to-ring-member bond
- C07D 401/10: linked by a carbon chain containing aromatic rings
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 405/04: directly linked by a ring-member-to-ring-member bond
- C07D 409/04: directly linked by a ring-member-to-ring-member bond
- C07D 409/10: linked by a carbon chain containing aromatic rings
- C07D 409/14: containing three or more hetero rings
- C07D 417/04: directly linked by a ring-member-to-ring-member bond
- C07D 491/048: the oxygen-containing ring being five-membered
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Compounds are provided which bind to an allosteric site on the mammalian alpha-7 nicotinic acetylcholine receptor (alpha-7 nAChR) and act as positive allosteric modulators with or without allosteric agonist activity. The compounds are useful in diagnosing, preventing, or treating a variety of disorders involving cognition, learning, memory, neurodegeneration, drug addiction, inflammation, chronic pain, and neuropathic pain. The compounds also can be used to enhance memory and learning in normal individuals.

## Claims

### Claim 1

A compound having one of the following formulas:
wherein the compound binds to an alpha-7 nicotinic acetylcholine receptor.

### Claim 2 (depends on 1)

The compound of claim 1 which is substantially enantiomerically pure.

### Claim 3 (depends on 1)

The compound of claim 1, wherein the compound comprises one or more of 18F, 19F, 75Br, 76Br, 123I, 124I, 125I, 131I, 11C, 13C, 13N, 15O, or 3H.

### Claim 4 (depends on 3)

A radiolabeled compound of claim 3, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and an excipient.

### Claim 5 (depends on 1)

The compound of claim 1, wherein the compound is a positive allosteric modulator of the alpha-7 nicotinic acetylcholine receptor.

### Claim 6 (depends on 1)

The compound of claim 1, wherein the compound is an allosteric agonist of the alpha-7 nicotinic acetylcholine receptor.

### Claim 7 (depends on 1)

The compound of claim 1, wherein the compound is capable of improving cognitive function, learning, and/or memory deficit.

### Claim 8 (depends on 1)

The compound of claim 1, wherein the compound is capable of reducing inflammation.

### Claim 9 (depends on 1)

The compound of claim 1, wherein the compound is capable of reducing neuropathic pain or pain related to a cognitive disorder.

### Claim 10 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and an excipient.