Piperazine derivatives useful as CCR5 antagonists

US6391865B1 · kind B1 · utility

Assignee

• SCHERING CORPORATION · US

Inventors

• Bahige M. Baroudy · Westfield, US
• John W. Clader · Cranford, US
• Hubert Josien · Hoboken, US
• Stuart W. McCombie · Caldwell, US
• Brian McKittrick · New Vernon, US
• Michael Miller · Scotch Plains, US
• Bernard R. Neustadt · West Orange, US
• Anandan Palani · Bound Brook, US
• Elizabeth M. Smith · Verona, US
• Ruo Steensma · Weehawken, US
• Jayaram R. Tagat · Westfield, US
• Susan F. Vice · Mountainside, US
• Eric J. Gilbert · Scotch Plains, US
• Marc A. Labroli · West Point, US

Key dates

• Filing date: May 1, 2000
• Grant date: May 21, 2002
• Expiry date: May 1, 2020

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D413/06
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, whereinR is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl;R1 is hydrogen or alkyl;R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl;R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl;R4, R5 and R7 are hydrogen or alkyl;R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.