Patent number: 6387930
Abstract: The use of CCR5 antagonists of the formula
or a pharmaceutically acceptable salt thereof, wherein
X is —C(R13)2—, —C(R13)(R19)—, —C(O)—, —O—, —NH—, —N(alkyl)—,
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; and
R5, R13, R14, R15 and R16 are hydrogen or alkyl for the treatment of HIV, solid organ transplant rejection, graft v.
Type:
Grant
Filed:
May 1, 2000
Date of Patent:
May 14, 2002
Assignee:
Schering Corporation
Inventors:
Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin
