# US 11,026,923 B2 · 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors

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- Number: US 11,026,923 B2
- Document ID: US11026923B2
- Status: Granted
- Kind: B2
- Application number: 17/060,742
- Filed: 2020-10-01
- Published: 2021-01-28
- Granted: 2021-06-08
- Earliest claimed: 2016-07-04
- Assignees: H. Lundbeck A/S
- Applicants: H. Lundbeck A/S
- Inventors: Jan Kehler; Karsten Juhl; Mauro Marigo; Paulo Jorge Vieira Vital; Mikkel Jessing; Morten Langgård; Lars Kyhn Rasmussen; Carl Martin Sebastian Clementson
- Web page: https://patentgrep.com/patent/US11026923B2

## CPC

- A61K 31/4162: condensed with heterocyclic ring systems
- A61K 31/4745: condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48)
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- 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 413/04: directly linked by a ring-member-to-ring-member bond
- C07D 471/04: Ortho-condensed systems
- C07D 305/06: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring atoms
- C07D 401/04: directly linked by a ring-member-to-ring-member bond
- 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)

## Abstract

The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

## Claims

### Claim 1

A compound of formula (I):
or a pharmaceutically acceptable salt thereof, wherein:
L is NH;
R1 is H or C1-C5 alkyl;
R2 is C1-C4 alkyl;
R3 is methyl substituted with a 5-membered heteroaryl which is substituted with methyl, or is methyl substituted with a pyridinyl which is substituted with C1-C3 fluoroalkyl or C1-C3 alkoxy; and
R4 is pyridinyl which is substituted with C1-C3 alkoxy.

### Claim 2 (depends on 1)

The compound of claim 1:
or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 2)

The compound of claim 2:

### Claim 4 (depends on 2)

A pharmaceutically acceptable salt of the compound of claim 2.

### Claim 5 (depends on 2)

A pharmaceutical composition comprising the compound of claim 2, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

### Claim 6 (depends on 1)

The compound of claim 1:
or a pharmaceutically acceptable salt thereof.

### Claim 7 (depends on 6)

The compound of claim 6:

### Claim 8 (depends on 6)

A pharmaceutically acceptable salt of the compound of claim 6.

### Claim 9 (depends on 6)

A pharmaceutical composition comprising the compound of claim 6, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

### Claim 10 (depends on 1)

The compound of claim 1:
or a pharmaceutically acceptable salt thereof.

### Claim 11 (depends on 10)

The compound of claim 10:

### Claim 12 (depends on 10)

A pharmaceutically acceptable salt of the compound of claim 10.

### Claim 13 (depends on 10)

A pharmaceutical composition comprising the compound of claim 10, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.

### Claim 14 (depends on 1)

The compound of claim 1:
or a pharmaceutically acceptable salt thereof.

### Claim 15 (depends on 14)

The compound of claim 14:

### Claim 16 (depends on 14)

A pharmaceutically acceptable salt of the compound of claim 14.

### Claim 17 (depends on 14)

A pharmaceutical composition comprising the compound of claim 14, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient.