Nova Patents
EP0804465B1

Novel elastase inhibitors

Abstract

This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase. The inhibitors are short, synthetic peptides in which the P2 moiety is substituted with various nitrogen-containing heterocyclic groups. As inhibitors of human neutrophil elastase, the compounds are useful in the treatment of a patient afflicted with a neutrophil associated inflammatory disease.

EP0804465B1, drawing sheet 1
Sheet 1 of 95

Term

Term ended

Expired 5 May 2015, 11.4 years ago.

  1. Priority
  2. Filed
  3. Granted
  4. Expired
  5. Today

15 claims: 4 independent, 11 dependent

  1. 1
    A compound of the formula or a hydrate or pharmaceutically acceptable salt thereof wherein P 4    is Ala, bAla, Leu, Ile, Val, Nva, bval, Nle or a bond;P 3    is Ala, bAla, Leu, lie, Val, Nva, bVal, Nle, or Lys substituted on its epsilon amino group with a morpholino-B-group;P 2    is Pro(4-OBzl);R 1    is a side chain of Ala, Leu, Ile, Val, Nva or bVal;K   is or wherein Z   is N or CH, and B   is a group of the formulae and wherein R' is hydrogen or a C 1-6 alkyl group.
  2. 13
    Use of a compound as in one of claims 1-10, optionally in combination with a pharmaceutically acceptable carrier, for the preparation of a human neutrophil elastase inhibitor.
  3. 14
    Use of a compound as in one of claims 1-10, optionally in combination with a pharmaceutically acceptable carrier, for the preparation of a pharmaceutical composition for the treatment of a neutrophil associated inflammatory disease.
  4. 15
    Use of a compound as in one of claims 1-10, optionally in combination with a pharmaceutically acceptable carrier, for the preparation of a pharmaceutical composition for the treatment of emphysema.
Independent claims4