# US 11,077,094 B2 · Spiro-lactam NMDA receptor modulators and uses thereof

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- Number: US 11,077,094 B2
- Document ID: US11077094B2
- Status: Granted
- Kind: B2
- Application number: 16/536,582
- Filed: 2019-08-09
- Published: 2020-07-02
- Granted: 2021-08-03
- Earliest claimed: 2013-01-29
- Assignees: Aptinyx Inc.
- Applicants: Aptinyx Inc.
- Inventors: John A. Lowe, III; M. Amin Khan
- Web page: https://patentgrep.com/patent/US11077094B2

## CPC

- A61K 31/397: having four-membered rings, e.g. azetidine
- A61K 31/407: condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- 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 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 487/10: Spiro-condensed systems
- Y02P 20/55: Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- Y02P: CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS

## Abstract

Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

## Claims

### Claim 1

A compound represented by:
or a pharmaceutically acceptable salt thereof.

### Claim 2

A pharmaceutical composition, the pharmaceutical composition comprising:
a compound represented by:
or a pharmaceutically acceptable salt thereof; and
a pharmaceutically acceptable excipient.