Apoptosis signal-regulating kinase inhibitors

Patent metadata

Field	Value
Publication number	US-9586932-B2
Application number	US-201514716526-A
Country	US
Kind code	B2
Filing date	May 19, 2015
Priority date	Jul 13, 2009
Publication date	Mar 7, 2017
Grant date	Mar 7, 2017

Abstract

The present invention relates to compounds of Formula (I):

wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 , R 1 , R 2 , R 3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).

First claim

What is claimed is:

1. A method of treating COPD in a mammal, comprising administering to a mammal in need thereof a therapeutically effective dose of a compound of Formula

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 wherein the compound is administered with an additional therapeutic agent.

3. The method of claim 2 wherein the additional therapeutic agent is selected from the group consisting of: epinephrine, terbutaline, albuterol 25, salmeterol, theophylline, ipratropium bromide, tiotropium, methylprednisolone (Solu-Medrol, Medrol).

4. The method of claim 3 wherein the additional therapeutic agent is administered in combination with the compound of formula (I) as a unit dosage form.

Assignees

• Gilead Sciences Inc

Inventors

• Graupe Michael
• Koch Keith
• Corkey Britton K
• Notte Gregory
• Melvin Jr Lawrence S

Classifications

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• C07D471/04

  Ortho-condensed systems · CPC title