公开(公告)号：EP1732570A2

公开(公告)日：2006-12-20

申请号：EP05700503.5

申请日：2005-01-27

申请人： Vysoká skola chemicko-technologická v Praze ,  Ustav organické chemie a biochemie av cz ,  Ustav anorganické chemie ac cz ,  Department of virology, University of Heidelberg

发明人： KRÁL, Vladimir ,  CIGLER, Petr ,  KONVALINKA, Jan ,  KOZÍSEK, Milan ,  PREJDOVÁ, Jana ,  GRÜNER, Bohumir ,  PLESEK, Jaromir ,  LEPSÍK, Martin ,  POKORNÁ, Jana ,  KRÄUSSLICH, Hans-Georg ,  BODEM, Jochen

IPC分类号： A61K31/69 ,  C07F5/05 ,  A61P31/18

CPC分类号： C07F15/065 ,  A61K31/69

摘要： The present invention provides novel HIV protease inhibitors containing substituted borane, carborane or metallacarborane clusters with 6 to 12 boron atoms in each cluster, wherein the charge of each borane, carborane or metallacarborane cluster is 0, -1 or -2; the number of borane, carborane or metallacarborane clusters in the inhibitor molecule is 1 to 9, and the carborane clusters in metallacarborane inhibitors are coordinated to transition metal atom, selected from the group containing cobalt, iron, nickel and ruthenium. In the cluster can be present heteroatoms as nitrogen, phosphorus, silicon, germanium, tin and sulphur. Pharmaceutical compositions containing these inhibitors and their use, both in vitro and in vivo. They are characterized by high effectivity and stability.