公开(公告)号：EP0817787A4

公开(公告)日：2000-09-13

申请号：EP96910605

申请日：1996-03-27

申请人： ISIS PHARMACEUTICALS INC

发明人： COOK PHILLIP DAN ,  AN HAOYUN ,  GUINOSSO CHARLES J ,  KUNG PEI-PEI ,  FRASER ALLISTER S

IPC分类号： G01N33/15 ,  A61K31/33 ,  A61K31/395 ,  A61K31/435 ,  A61K31/53 ,  A61P29/00 ,  A61P31/04 ,  A61P43/00 ,  C07B61/00 ,  C07D255/02 ,  C07D273/00 ,  C07D471/08 ,  C07D471/18 ,  C07D498/08 ,  C07D515/08 ,  C07D521/00 ,  C07D519/00 ,  G01N33/531

CPC分类号： C07D471/08 ,  B01J2219/0072 ,  C07D515/08

摘要： Novel macrocyclic compounds are constructed to include large cyclic structures that are interrupted by at least one ring sytem. Each interrupting ring system includes two bridgehead atoms. Bridgehead atoms are bonded to one or more bridges that interconnect one or more ring systems thereby forming a large cyclic structure. Located in each bridge are two or more nitrogenous moieties that are derivatized with chemical functional groups. The ring systems can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring. These can also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the macrocyclic compounds. In accordance with certain embodiments of the invention, libraries of such macrocyclic compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the library.