# US 10,370,363 B2 · Inhibitors of CXCR2

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 10,370,363 B2
- Document ID: US10370363B2
- Status: Granted
- Kind: B2
- Application number: 15/722,785
- Filed: 2017-10-02
- Published: 2018-06-21
- Granted: 2019-08-06
- Earliest claimed: 2015-11-19
- Assignees: ChemoCentryx, Inc.
- Applicants: Chemocentryx, Inc.
- Inventors: Xi Chen; Dean R. Dragoli; Junfa Fan; Jaroslaw Kalisiak; Manmohan Reddy Leleti; Viengkham Malathong; Jeffrey McMahon; Hiroko Tanaka; Ju Yang; Chao Yu; Penglie Zhang; Venkat Mali
- Web page: https://patentgrep.com/patent/US10370363B2

## CPC

- C07D 405/12: linked by a chain containing hetero atoms as chain links
- A61K 31/4035: Isoindoles, e.g. phthalimide
- A61K 31/422: not condensed and containing further heterocyclic rings
- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 17/06: Antipsoriatics
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- C07B 59/002: {Heterocyclic compounds}
- C07D 405/14: containing three or more hetero rings
- C07D 413/12: linked by a chain containing hetero atoms as chain links
- C07B 2200/05: Isotopically modified compounds, e.g. labelled
- 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
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

Compounds are provided as inhibitors of CXCR2, having the structure:

## Claims

### Claim 1

A compound having formula
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1.

### Claim 3 (depends on 2)

The pharmaceutical composition of claim 2, further comprising one or more additional therapeutic agents.

### Claim 4 (depends on 3)

The pharmaceutical composition of claim 3 wherein the one or more additional therapeutic agents are selected from the group consisting of a cytotoxic chemotherapeutic agent, an anti-cancer or anti-tumor vaccine, chimeric antigen receptor (CAR) T cell immunotherapeutic agent, and checkpoint inhibitors.

### Claim 5 (depends on 3)

The pharmaceutical composition of claim 3 wherein the one or more additional therapeutic agents are selected from the group consisting of:
drugs that block the activity of CTLA-4 (CD152), PD-1 (CD279), PDL-1 (CD274), TIM-3, LAG-3 (CD223), VISTA, KIR, NKG2A, BTLA, PD-1H, TIGIT, CD96, 4-1BB (CD137), 4-1BBL (CD137L), GARP, CSF-1R, A2AR, CD73, CD47, tryptophan 2,3-dioxygenase (TDO) or indoleamine 2,3 dioxygenase (IDO), and agonists of OX40, GITR, 4-1BB, ICOS, STING or CD40.

### Claim 6 (depends on 1)

A method of treating a disease or disorder selected from the group consisting of psoriasis, rheumatoid arthritis, radiation induced fibrotic lung disease, autoimmune bullous dermatosis (AIBD), chronic obstructive pulmonary disease, and ozone-induced airway inflammation in a subject in need thereof, said method comprising administering an effective amount of a compound or a pharmaceutically acceptable salt of claim 1 to said subject.

### Claim 7 (depends on 1)

A method of treating a cancer selected from the group consisting of rhabdomyocarcoma, Lewis lung carcinoma (LLC), non-small cell lung cancer, esophageal squamous cell carcinoma, esophageal adenocarcinoma, renal cell carcinoma (RCC), colorectal cancer (CRC), acute myeloid leukemia (AML), breast cancer, gastric cancer, prostatic small cell neuroendocrine carcinoma (SCNC), liver cancer, glioblastoma, liver cancer, oral squamous cell carcinoma, head and neck squamous cell carcinoma, pancreatic cancer, thyroid papillary cancer, intrahepatic cholangiocellular carcinoma, hepatocellular carcinoma, bone cancer, and nasopharyngeal carcinoma in a subject in need thereof, said method comprising administering an effective amount of a compound or a pharmaceutically acceptable salt of claim 1 to said subject.

### Claim 8 (depends on 7)

A method of claim 7, wherein the compound or a pharmaceutically acceptable salt thereof, is used to treat cancer alone or in combination with one or more other anti-cancer therapies.

### Claim 9 (depends on 8)

A method of claim 8, wherein the compound or a pharmaceutically acceptable salt thereof, is used to treat cancer in combination with one or more of a cytotoxic chemotherapeutic agent, an anti-cancer vaccine, an anti-tumor vaccine, and a chimeric antigen receptor (CAR) T cell immunotherapeutic agent, and gene transfer therapy.

### Claim 10 (depends on 8)

A method of claim 8, wherein the compound or a pharmaceutically acceptable salt thereof, is used to treat cancer in combination with one or more checkpoint inhibitors.

### Claim 11 (depends on 8)

The method of claim 8 wherein the one or more other anti-cancer therapy is selected from the group consisting of: drugs that block the activity of CTLA-4(CD152), PD-1 (CD279), PDL-1 (CD274), TIM-3, LAG-3 (CD223), VISTA, KIR, NKG2A, BTLA, PD-1H, TIGIT, CD96, 4-1BB (CD137), 4-1BBL (CD137), GARP, CSF-1R, A2AR, CD73, CD47, tryptophan 2,3-dioxygenase (TDO) or indoleamine 2,3 dioxygenase (IDO), and agonists of OX40, GITR, 4-1BB, ICOS, STING or CD40.

### Claim 12 (depends on 1)

The compound of claim 1 having the formula

### Claim 13 (depends on 1)

The compound of claim 1 having the formula