公开(公告)号：WO2005073240A3

公开(公告)日：2005-11-17

申请号：PCT/CZ2005000006

申请日：2005-01-27

Applicant: VS CHEMICKO TECHNOLOGICKA V PR ,  USTAV ORGANICKE CHEMIE A BIOCH ,  USTAV ANORGANICKE CHEMIE AV CZ ,  DEPT OF VIROLOGY UNIVERSITY OF ,  KRAL VLADIMIR ,  CIGLER PETR ,  KONVALINKA JAN ,  KOZISEK MILAN ,  PREJDOVA JANA ,  GRUENER BOHUMIR ,  PLESEK JAROMIR ,  LEPSIK MARTIN ,  POKORNA JANA ,  KRAEUSSLICH HANS-GEORG ,  BODEM JOCHEN

Inventor： KRAL VLADIMIR ,  CIGLER PETR ,  KONVALINKA JAN ,  KOZISEK MILAN ,  PREJDOVA JANA ,  GRUENER BOHUMIR ,  PLESEK JAROMIR ,  LEPSIK MARTIN ,  POKORNA JANA ,  KRAEUSSLICH HANS-GEORG ,  BODEM JOCHEN

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

CPC classification number: C07F15/065 ,  A61K31/69

Abstract: 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.

Abstract translation: 本发明提供了新颖的HIV蛋白酶抑制剂，其含有在每个簇中具有6至12个硼原子的取代的硼烷，碳硼烷或金刚砂硼烷簇，其中每个硼烷，碳硼烷或金刚砂簇的电荷为0，-1或-2; 抑制剂分子中的硼烷，碳硼烷或金刚砂簇的数目为1至9，并且金属硼烷抑制剂中的碳硼烷簇与选自钴，铁，镍和钌的过渡金属原子配位。 在簇中可以存在氮，磷，硅，锗，锡和硫的杂原子。 含有这些抑制剂的药物组合物及其在体外和体内的用途。 它们的特点是高效和稳定。