# US 12,180,206 B2 · Aceclidine derivatives, compositions thereof and methods of use thereof

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- Number: US 12,180,206 B2
- Document ID: US12180206B2
- Status: Granted
- Kind: B2
- Application number: 17/988,366
- Filed: 2022-11-16
- Published: 2023-05-18
- Granted: 2024-12-31
- Earliest claimed: 2021-11-17
- Assignees: Lenz Therapeutics Operations, Inc.
- Applicants: LENZ Therapeutics Operations, Inc.
- Inventors: Gerald Horn
- Web page: https://patentgrep.com/patent/US12180206B2

## CPC

- C07D 471/00: Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 31/4748: forming part of bridged ring systems (strychnine A61K31/475; morphinan derivatives A61K31/485)
- A61K 47/40: Cyclodextrins; Derivatives thereof
- A61P 27/10: for accommodation disorders, e.g. myopia
- C07D 453/02: containing not further condensed quinuclidine ring systems
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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

## Abstract

The present invention is directed to derivatives of aceclidine. The present invention is further directed to ophthalmological compositions comprising a therapeutically effective amount of a compound of the present invention and one or more pharmaceutically acceptable excipients. The present invention is further directed to a methods of treating presbyopia or glaucoma or reducing hyperemia comprising administering to a patient in need thereof a therapeutically effective amount of a compound of the present invention.

## Claims

### Claim 1

A pharmaceutically acceptable salt of a compound comprising a cation of formula (I),
wherein R1 is an alkyl, and
wherein R2 is an amine or tert-butyl.

### Claim 2

An ophthalmological composition comprising a therapeutically effective amount of (i) a pharmaceutically acceptable salt of a compound comprising a cation of formula (I):
wherein R1 is an alkyl, and
wherein R2 is an amine or tert-butyl, or
(ii) a compound of formula (III)
or a pharmaceutically acceptable salt thereof,
wherein the pH of the composition is at least 3 log units less than the pKa of the compound.

### Claim 3 (depends on 2)

The composition of claim 2, further comprising a cyclodextrin.

### Claim 4 (depends on 3)

The composition of claim 3, wherein the cyclodextrin is selected from an alpha-cyclodextrin, a beta-cyclodextrin and a gamma-cyclodextrin.

### Claim 5

A method of treating presbyopia or glaucoma comprising administering to a patient in need thereof a therapeutically effective amount of (i) a pharmaceutically acceptable salt of a compound comprising a cation of formula (I):
wherein R1 is an alkyl, and
wherein R2 is an amine or tert-butyl, or
(ii) a compound of formula (III)
or a pharmaceutically acceptable salt thereof.

### Claim 6

A method of reducing hyperemia comprising administering to a patient in need thereof a therapeutically effective amount of (i) a pharmaceutically acceptable salt of a compound comprising a cation of formula (I):
wherein R1 is an alkyl, and
wherein R2 is an amine or tert-butyl, or
(ii) a compound of formula (III)
or a pharmaceutically acceptable salt thereof.