Patent Number: 7,825,121

Title: Piperazine derivatives useful as CCR5 antagonists

Abstract: The use of CCR5 antagonists of the formula ##STR00001## or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R.sup.1 is hydrogen or alkyl; R.sup.2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R.sup.3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R.sup.4, R.sup.5 and R.sup.7 are hydrogen or alkyl; R.sup.6 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.

Inventors: Ramanathan; Ragulan (Kendall Park, NJ), Ghosal; Anima (Edison, NJ), Miller; Michael W. (Scotch Plains, NJ), Chowdhury; Swapan K. (Warren, NJ), Alton; Kevin B. (Cedar Knolls, NJ)

Assignee: Schering Corporation

International Classification: A61K 31/497 (20060101); A01N 43/54 (20060101); C07D 403/00 (20060101); C07D 239/00 (20060101)

Expiration Date: 2019-11-02 0:00:00