# US 12,760,045 B2 · 3-pyrrolidine-indole derivatives as serotonergic psychedelic agents for the treatment of CNS disorders

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- Number: US 12,760,045 B2
- Document ID: US12760045B2
- Status: Granted
- Kind: B2
- Application number: 18/747,540
- Filed: 2024-06-19
- Published: 2024-10-10
- Granted: 2026-10-13
- Earliest claimed: 2020-02-04
- Assignees: Mindset Pharma Inc.
- Applicants: Mindset Pharma Inc.
- Inventors: Abdelmalik Slassi; Joseph Araujo
- Web page: https://patentgrep.com/patent/US12760045B2

## CPC

- C07F 9/5728: {condensed with carbocyclic rings or carbocyclic ring systems}
- A61P 25/24: Antidepressants
- C07D 403/06: linked by a carbon chain containing only aliphatic carbon atoms
- A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
- C07B 2200/05: Isotopically modified compounds, e.g. labelled
- A61K 31/404: Indoles, e.g. pindolol
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- A61K 31/454: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

The present application relates to 3-cyclic amine-indole derivatives of general Formula (I), to processes for their preparation, to compositions comprising them and to their use in activation of a serotonin receptor in a cell, as well as to treating diseases, disorders or conditions by activation of a serotonin receptor in a cell. The diseases, disorders or conditions include, for example, psychosis, mental illnesses, and other neurological diseases, disorders and conditions.

## Claims

### Claim 1

A method for treating a mental illness selected from: depression, depression in Alzheimer's disease, treatment resistant depression, depression in terminally ill cancer patients, major depressive disorder, post-traumatic stress disorder (PTSD), mood disorders and major depressive disorder, comprising administering a therapeutically effective amount of one or more compounds or a pharmaceutically acceptable salt thereof, selected from:
Com-
pound
ID #
Chemical Structure
I-1
I-2
I-3
I-4
I-5
I-6
I-7
I-8
I-9
I-10
I-11
I-12
I-13
I-14
I-15
I-16
I-17
I-18
I-19
I-20
I-21
I-22
I-23
I-24
I-25
I-26
1-27
I-28
1-29
1-30
1-31
1-32
1-33
1-34
1-35
1-36
I-37
I-38
I-39
I-40
I-41
I-42
I-43
I-44
I-45
I-46
I-48
I-49
I-50
I-51
I-52
I-53
I-54
to a patient in need thereof.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the disease, disorder or condition is selected from depression, depression in Alzheimer's disease, treatment resistant depression, major depressive disorder, and post-traumatic stress disorder (PTSD).

### Claim 3 (depends on 2)

The method according to claim 2, wherein the one or more compounds or a pharmaceutically acceptable salt thereof, is/are selected from:
Compound ID #
Chemical Structure
I-1
I-2
I-7
I-37
I-38
I-40
I-44
and
I-54

### Claim 4 (depends on 3)

The method according to claim 3, wherein the disease, disorder or condition is depression.

### Claim 5 (depends on 3)

The method according to claim 3, wherein the disease, disorder or condition is depression in Alzheimer's disease.

### Claim 6 (depends on 3)

The method according to claim 3, wherein the disease, disorder or condition is treatment resistant depression.

### Claim 7 (depends on 3)

The method according to claim 3, wherein the disease, disorder or condition is major depressive disorder.

### Claim 8 (depends on 3)

The method according to claim 3, wherein the disease, disorder or condition is post-traumatic stress disorder (PTSD).

### Claim 9 (depends on 4)

The method according to claim 4, wherein the one or more compounds or a pharmaceutically acceptable salt thereof, is/are selected from:
Compound ID #
Chemical Structure
I-1
I-37
I-40
I-44
and
I-54

### Claim 10 (depends on 5)

The method according to claim 5, wherein the one or more compounds or a pharmaceutically acceptable salt thereof, is/are selected from:
Compound ID #
Chemical Structure
I-1
I-37
I-40
I-44
and
I-54

### Claim 11 (depends on 6)

The method according to claim 6, wherein the one or more compounds or a pharmaceutically acceptable salt thereof, is/are selected from:
Compound ID #
Chemical Structure
I-1
I-37
I-40
I-44
and
I-54

### Claim 12 (depends on 7)

The method according to claim 7, wherein the one or more compounds or a pharmaceutically acceptable salt thereof, is/are selected from:
Compound ID #
Chemical Structure
I-1
I-37
I-40
I-44
and
I-54

### Claim 13 (depends on 8)

The method according to claim 8, wherein the one or more compounds or a pharmaceutically acceptable salt thereof, is/are selected from:
Compound
ID #
Chemical Structure
I-1
I-37
I-40
I-44
and
I-54

### Claim 14 (depends on 4)

The method according to claim 4, wherein the one or more compounds or a pharmaceutically acceptable salt thereof, is/are selected from:
Compound ID #
Chemical Structure
I-1
I-44
and
I-54

### Claim 15 (depends on 5)

The method according to claim 5, wherein the one or more compounds or a pharmaceutically acceptable salt thereof, is/are selected from:
Compound
ID #
Chemical Structure
I-1
I-44
and
I-54

### Claim 16 (depends on 6)

The method according to claim 6, wherein the one or more compounds or a pharmaceutically acceptable salt thereof, is/are selected from:
Compound ID #
Chemical Structure
I-1
I-44
and
I-54

### Claim 17 (depends on 7)

The method according to claim 7, wherein the one or more compounds or a pharmaceutically acceptable salt thereof, is/are selected from:
Compound ID #
Chemical Structure
I-1
I-44
and
I-54

### Claim 18 (depends on 8)

The method according to claim 8, wherein the one or more compounds or a pharmaceutically acceptable salt thereof, is/are selected from:
Compound ID #
Chemical Structure
I-1
I-44
and
I-54