Patent · US Expired

Aminobenzenedicarboxylic acid-based combinatorial libraries

US6127191A · kind A · utility

4Cited by
3References
6Claims
0Family size

Assignee

Inventors

Key dates

Filing dateNov 26, 1997
Grant dateOct 3, 2000
Priority date
Expiry dateNov 26, 2017

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07C2603/74
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The present invention provides a library of compounds, each comprised of a common aminobenzenedicarboxylic acid core structure (scaffold) that serves as a template for synthesizing approximately 10.sup.1 -10.sup.6 compounds which are analogs of the scaffold. The library is employed to study ligand binding by biological receptors, such as enzymes, G-protein coupled receptors and membrane channels. For example, certain individual compounds within the library selectively bind and inhibit the action of trypsin-like serine proteases. The present invention also relates to combinatorial synthetic methods for making such libraries of compounds. Additionally, the present invention relates to novel scaffold-modified solid supports, particularly scaffold-modified polymer resins and methods for preparing said resins. Further, the present invention is directed to methods for screening a compound or plurality of compounds made according to the synthetic methods disclosed herein, which comprise using the compounds in suitable assays developed for detecting the compounds' utility as pharmaceutical agents.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.