Patent · US Expired

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

US6403633B2 · kind B2 · utility

17Cited by
13References
108Claims
0Family size

Assignee

Inventors

Key dates

Filing dateApr 10, 2001
Grant dateJun 11, 2002
Priority date
Expiry dateApr 10, 2021

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.