# US 12,760,020 B2 · Solid state forms of vericiguat and process for preparation thereof

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- Number: US 12,760,020 B2
- Document ID: US12760020B2
- Status: Granted
- Kind: B2
- Application number: 18/683,859
- Filed: 2022-08-31
- Published: 2024-10-24
- Granted: 2026-10-13
- Earliest claimed: 2021-08-31
- Assignees: Assia Chemical Industries Ltd.
- Applicants: Assia Chemical Industries Ltd.
- Inventors: Luna Ben-Sahel Katsav; Jenny Goldshtein; Limor Adani; Abed Masarwa; Anantha Rajmohan Muthusamy; Meenakshi Sundaram Somasundaram; Siva Rama Krishna Muppalla; Anand Kumar Pandey; Jitendra Kamalakar Sonar; Sumit Kumar
- Web page: https://patentgrep.com/patent/US12760020B2

## CPC

- C07D 471/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present disclosure encompasses solid state forms of Vericiguat, in embodiments crystalline polymorphs of Vericiguat, processes for preparation thereof, and pharmaceutical compositions thereof.

## Claims

### Claim 1

A crystalline Form VT1 of Vericiguat characterized by one or more of the following data:
a) an XRPD pattern having peaks at 6.0, 10.3, 15.6, 18.4 and 20.1 degrees 2-theta±0.2 degrees 2-theta;
b) a solid state 13C NMR spectrum having peaks at 45.0, 51.3, 114.7, 120.2, 125.9, 139.8 and 160.5 ppm±0.2 ppm; or
c) a solid state 13C NMR spectrum having the following chemical shift absolute differences from a reference peak at 146.9 ppm±2 ppm of 101.9, 95.6, 32.2, 26.7, 21.0, 7.1 and 13.7 ppm±0.1 ppm.

### Claim 2 (depends on 1)

The crystalline Form VT1 of Vericiguat according to claim 1, which is characterized by an XRPD pattern having peaks at 6.0, 10.3, 15.6, 18.4 and 20.1 degrees 2-theta±0.2 degrees 2-theta, and also having one, two, or three additional peaks selected from 12.4, 17.0 and 31.1 degrees two theta±0.2 degrees two theta.

### Claim 3 (depends on 1)

The crystalline Form VT1 of Vericiguat according to claim 1, which is characterized by an XRPD pattern having peaks at 6.0, 10.3, 12.4, 15.6, 17.0 18.4, 20.1 and 31.1 degrees 2-theta±0.2 degrees 2-theta.

### Claim 4 (depends on 1)

The crystalline Form VT1 of Vericiguat according to claim 1, which is further characterized by an XRPD pattern having an additional peak at 2.3±0.2 degrees 2-theta.

### Claim 5 (depends on 1)

The crystalline Form VT1 of Vericiguat according to claim 1, which is further characterized by an XRPD pattern having an absence of a peak at 3.2±0.2 degrees 2-theta, or 5.1±0.2 degrees 2-theta, or 5.4±0.2 degrees 2-theta, or 6.4±0.2 degrees 2-theta, or 6.6±0.2 degrees 2-theta.

### Claim 6 (depends on 1)

The crystalline Form VT1 of Vericiguat according to claim 1, wherein said crystalline form is an anhydrous form.

### Claim 7 (depends on 1)

The crystalline Form VT1 of Vericiguat according to claim 1, which contains no more than about 20% of any other crystalline forms of Vericiguat.

### Claim 8 (depends on 1)

The crystalline Form VT1 of Vericiguat according to claim 1, which contains no more than about 20% of amorphous Vericiguat.

### Claim 9 (depends on 1)

A pharmaceutical composition comprising the crystalline form VT1 of Vericiguat according to claim 1.

### Claim 10 (depends on 1)

A pharmaceutical formulation comprising the crystalline Form VT1 Vericiguat according to claim 1, with at least one pharmaceutically acceptable excipient.

### Claim 11 (depends on 1)

A process for preparing a pharmaceutical formulation comprising combining the crystalline Form VT1 of Vericiguat according to claim 1 with at least one pharmaceutically acceptable excipient.

### Claim 12 (depends on 1)

A medicament comprising the crystalline Form VT1 of Vericiguat according to claim 1.

### Claim 13 (depends on 1)

A method of treating chronic heart failure, comprising administering a therapeutically effective amount of the crystalline Form VT1 of Vericiguat according to claim 1 to a subject in need of the treatment.