# US 9,750,730 B2 · Apoptosis signal-regulating kinase inhibitor

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- Number: US 9,750,730 B2
- Document ID: US9750730B2
- Status: Granted
- Kind: B2
- Application number: 15/140,204
- Filed: 2016-04-27
- Published: 2016-08-18
- Granted: 2017-09-05
- Earliest claimed: 2012-01-27
- Assignees: Gilead Sciences, Inc.
- Applicants: Gilead Sciences, Inc.
- Inventors: Gregory Notte
- Web page: https://patentgrep.com/patent/US9750730B2

## CPC

- C07D 401/14: containing three or more hetero rings
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)}
- 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 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 13/12: of the kidneys
- A61P 19/04: for non-specific disorders of the connective tissue
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/12: Antivirals
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 213/56: Amides
- C07D 233/56: with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
- C07D 401/04: directly linked by a ring-member-to-ring-member bond
- 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

## Abstract

The present invention relates to a compound of formula (I): The compound has apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and is thus useful in the treatment of diseases such as kidney disease, diabetic nephropathy and kidney fibrosis.

## Claims

### Claim 1

A method of treating liver fibrosis comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula (I)
or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the liver fibrosis is selected from the group consisting of, chronic liver fibrosis and acute liver fibrosis.

### Claim 3 (depends on 1)

The method of claim 1, wherein the pharmaceutically acceptable salt is the hydrochloride salt.

### Claim 4 (depends on 1)

The method of claim 1, wherein the therapeutic amount ranges from 1 mg to 250 mg.

### Claim 5 (depends on 1)

The method of claim 1, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered orally.

### Claim 6 (depends on 1)

The method of claim 1, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered in a single or multiple doses.

### Claim 7 (depends on 1)

The method of claim 1, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered in combination with other therapeutic agents.

### Claim 8 (depends on 7)

The method of claim 7, wherein the one or more therapeutic agents is selected from the group consisting of angiotensin converting enzyme inhibitors, angiotensin II receptor blockers, antihypertensive agents, antibiotic agents, analgesic agents, antidepressant agents, or antianxiety agents.

### Claim 9 (depends on 7)

The method of claim 7, wherein the pharmaceutical composition and the one or more therapeutic agents are administered simultaneously.

### Claim 10 (depends on 7)

The method of claim 7, wherein the pharmaceutical composition and the one or more therapeutic agents are administered one after the other within intervals.