# US 12,594,276 B2 · Inhibitors of human immunodeficiency virus replication

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- Number: US 12,594,276 B2
- Document ID: US12594276B2
- Status: Granted
- Kind: B2
- Application number: 19/043,910
- Filed: 2025-02-03
- Published: 2025-08-07
- Granted: 2026-04-07
- Earliest claimed: 2024-02-05
- Assignees: ViiV HEALTHCARE UK (NO. 5) LIMITED
- Applicants: ViiV Healthcare UK (No.5) Limited
- Inventors: Manoj Patel; Kyle E. Parcella; Eric P. Gillis; B Narasimhulu Naidu
- Web page: https://patentgrep.com/patent/US12594276B2

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/439: the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46)
- A61K 31/4402: only substituted in position 2, e.g. pheniramine, bisacodyl
- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61K 31/4985: Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
- A61K 31/505: Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K 31/513: having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
- A61K 31/5365: ortho- or peri-condensed with heterocyclic ring systems
- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61K 31/635: having a heterocyclic ring, e.g. sulfadiazine
- A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
- A61P 31/18: for HIV
- C07D 471/04: Ortho-condensed systems
- 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

A compound of Formula (I), including pharmaceutically acceptable salts thereof, and compositions and methods for treatment or prevention of human immunodeficiency virus (HIV) infection are set forth. Novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection are described. Formula (I) is as follows:

## Claims

### Claim 1

A compound which is
or a pharmaceutically acceptable salt thereof.

### Claim 2

A compound which is:

### Claim 3 (depends on 1)

The compound or pharmaceutically acceptable salt according to claim 1, as a pharmaceutically acceptable salt.

### Claim 4 (depends on 2)

The compound according to claim 2, wherein the compound is a crystalline compound
and is characterized by having at least nine diffraction angles, when measured using Cu Kα radiation, selected from a group consisting of about 5.1, 5.6, 6.9, 7.6, 8.2, 8.7, 9.1, 9.8, 11.1, 11.3, 11.9, 13.2, 13.9, 14.4, 14.7, 15.2, 15.4, 16.0, 16.6, 16.8, 17.2, 17.5, 18.4, 18.7, 19.1, 19.4, 19.9, 20.3, 20.5, 21.0, 21.4, 22.0, 22.6, 23.8, 24.0, 24.4, 24.7, 25.1, 25.8, 26.2, 26.8, 27.0, 27.6, 27.9, 28.5, 28.8, 29.2, 29.8, 30.1, 31.1, 31.3, 31.9, 32.5, 32.7, 33.2, 34.1, 34.8, 35.4, 36.1, 37.7, 38.7, 39.0, 39.5, and 39.7 degrees±0.2° 2θ.

### Claim 5 (depends on 1)

A pharmaceutical composition comprising a) the compound or pharmaceutically acceptable salt thereof as defined in claim 1, and b) a pharmaceutically acceptable excipient.

### Claim 6 (depends on 1)

A combination of
a) a compound or pharmaceutically acceptable salt thereof as defined in claim 1; and
b) an agent used for treatment of AIDS or HIV infection selected from the group consisting of Dolutegravir, lamivudine, Fostemsavir, Cabotegravir, maraviroc, rilpivirine, atazanavir, Tenofovir, Alafenamide, EFdA, Doravirine, and darunavir.

### Claim 7 (depends on 2)

The compound according to claim 2, wherein the compound is a crystalline compound and is characterized by a DSC thermogram having a melting onset of about 216° C.