09-11-2000 дата публикации
Номер: WO2000066559A1
Автор:
Anandan Palani,
Bahige M. Baroudy,
Bernard R. Neustadt,
Brian A. Mckittrick,
Hubert B. Josien,
Jayaram R. Tagat,
John W. Clader,
Mark A. Laughlin,
Michael W. Miller,
Ruo Steensma,
Stuart W. Mccombie,
Susan F. Vice
The use of CCR5 antagonists of formula (I) or a pharmaceutically acceptable salt thereof, wherein X is -C(R13)2-, -C(R13)(R19)-, -C(O)-, -O-, -NH-, -N(alkyl)-, (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l), (m) or (n); 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, -CH¿2?CH2OH, -CH2CH2-O-alkyl, -CH2C(O)-O-alkyl, -CH2C(O)NH2, -CH2C(O)-NHalkyl or -CH2C(O)-N(alkyl)2; R?19¿ is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R?5, 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 inflammatory diseases.
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