Quinoline derivative for treating rheumatoid arthritis

Patent metadata

Field	Value
Publication number	US-12508258-B2
Application number	US-202117792932-A
Country	US
Kind code	B2
Filing date	Jan 19, 2021
Priority date	Jan 19, 2020
Publication date	Dec 30, 2025
Grant date	Dec 30, 2025

Abstract

A quinoline derivative for treating rheumatoid arthritis and a use thereof in preparing a pharmaceutical composition for treating rheumatoid arthritis. In particular, a use of the quinoline derivative 1-[[[4-(4-Fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinoline-7-yl]oxy]methyl]cyclopropanamine in treating rheumatoid arthritis.

First claim

The invention claimed is:

1 . A method for treating rheumatoid arthritis in a patient, comprising administering to the patient in need of treatment a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof

2 . The method according to claim 1 , wherein the patient has previously received treatment with a disease modifying antirheumatic drug.

3 . The method according to claim 1 , wherein the patient is insufficiently responsive or intolerant to at least one disease modifying antirheumatic drug.

4 . The method according to claim 1 , wherein the patient does not meet target or does not reduce disease activity after having previously received treatment with a traditional disease modifying antirheumatic drug, a targeted disease modifying antirheumatic drug and/or a biological disease modifying antirheumatic drug.

5 . The method according to claim 1 , wherein the compound of formula I or the pharmaceutically acceptable salt thereof is administered as the only active ingredient to a patient.

6 . The method according to claim 1 , further comprising administering other disease modifying antirheumatic drugs, wherein the compound of formula I or the pharmaceutically acceptable salt thereof is administered simultaneously or sequentially with the other disease modifying antirheumatic drugs to a patient with rheumatoid arthritis.

7 . The method according to claim 6 , wherein the other disease modifying antirheumatic drugs are selected from the group consisting of non-biological disease modifying antirheumatic drugs.

8 . The method according to claim 6 , wherein the other disease modifying antirheumatic drugs are selected from the group consisting of one or more of traditional disease modifying antirheumatic drugs, targeted disease modifying antirheumatic drugs and biological disease modifying antirheumatic drugs.

9 . The method according to claim 6 , wherein the other disease modifying antirheumatic drugs are selected from the group consisting of methotrexate.

10 . The method according to claim 6 , wherein the other disease modifying antirheumatic drugs are selected from the group consisting of: methotrexate+sulfasalazine; methotrexate+leflunomide; methotrexate+hydroxychloroquine; sulfasalazine+leflunomide; methotrexate+sulfasalazine+hydroxychloroquine; sulfasalazine+leflunomide+hydroxychloroquine; leflunomide+hydroxychloroquine; sulfasalazine+leflunomide+hydroxychloroquine; and tofacitinib and one or more selected from the group consisting of: methotrexate, sulfasalazine, leflunomide and hydroxychloroquine.

11 . The method according to claim 1 , wherein the pharmaceutically acceptable salt is a salt formed by the compound of formula I and any of the following acids: hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, acetic acid, trifluoroacetic acid, propionic acid, hexanoic acid, heptanoic acid, cyclopentanepropionic acid, glycolic acid, pyruvic acid, lactic acid, malonic acid, succinic acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1,2-ethanedisulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, p-chlorobenzenesulfonic acid, p-toluenesulfonic acid, 3-phenylpropionic acid, trimethylacetic acid, t-butylacetic acid, dodecyl sulfuric acid, gluconic acid, glutamic acid, hydroxyl naphthoic acid, salicylic acid and stearic acid; or the pharmaceutically acceptable salt is a hydrochloride salt; or the pharmaceutically acceptable salt is a dihydrochloride salt.

12 . The method according to claim 1 , wherein the rheumatoid arthritis is active rheumatoid arthritis.

13 . The method according to claim 1 , wherein the rheumatoid arthritis is moderate-to-severe, moderate and/or severe active rheumatoid arthritis.

Assignees

• Chia Tai Tianqing Pharmaceutical Group Co Ltd

Inventors

• Zhang Xiquan
• Yang Ling
• Xu Hongjiang
• Song Wei
• Zou Xiaofang
• Wang Xianju

Classifications

• A61K31/655

  Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds · CPC title

• A61K31/519

  ortho- or peri-condensed with heterocyclic rings · CPC title

• A61K31/4706

  4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine · CPC title

• A61K31/42

  Oxazoles · CPC title

• A61P19/02 Primary

  for joint disorders, e.g. arthritis, arthrosis · CPC title