Piperidine derivatives useful as CCR5 antagonists

US6602885B2 · kind B2 · 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
• Ruo Steensma · Weehawken, US
• Jayaram R. Tagat · Westfield, US
• Susan F. Vice · Mountainside, US
• Mark Laughlin · Edison, US

Key dates

• Filing date: Nov 8, 2001
• Grant date: Aug 5, 2003
• Expiry date: Nov 8, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D417/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl;R1 is H, alkyl or alkenyl;R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl;R3 is optionally substituted phenyl, heteroaryl or naphthyl;R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2;R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; andR5, R13, R14, R15 and R16 are hydrogen or alkyl 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 in…