申请人:——
公开号:US20030069252A1
公开(公告)日:2003-04-10
The use of CCR5 antagonists of the formula
1
or a pharmaceutically acceptable salt thereof, wherein
R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl;
R
1
is hydrogen or alkyl;
R
2
is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl;
R
3
is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl;
R
4
, R
5
and R
7
are hydrogen or alkyl;
R
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.
本发明涉及CCR5拮抗剂的使用,其
化学式为1或其药学上可接受的盐,其中R是可选取的取代苯基、
吡啶基、
噻吩基或
萘基;R1是氢或烷基;R2是取代苯基、取代杂环芳基、
萘基、
芴基、二苯甲基或可选取代的苯基或杂环芳基烷基;R3是氢、烷基、烷氧基烷基、环烷基、环烷基烷基或可选取代的苯基、苯基烷基、
萘基、
萘基烷基、杂环芳基或杂环芳基烷基;R4、R5和R7是氢或烷基;R6是氢、烷基或烯烃基;用于治疗HIV、固体器官移植排斥、移植物抗宿主病、关节炎、类风湿性关节炎、炎症性肠病、特应性皮炎、
银屑病、哮喘、过敏或多发性硬化症,还公开了新型化合物、包含它们的药物组合物以及本发明CCR5拮抗剂与抗HIV药物或治疗炎症性疾病的药物组合的组合物。