Patent · US Expired

Heteroaryl amidines, methylamidines and guanidines, and the use thereof as protease inhibitors

US6562840B1 · kind B1 · utility

9Cited by
18References
36Claims
0Family size

Assignee

Inventors

Key dates

Filing dateFeb 26, 2002
Grant dateMay 13, 2003
Priority date
Expiry dateFeb 26, 2022

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D417/14
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The present invention is directed to compounds of Formula I: wherein X is O, S or NR7 and R1—R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.

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