Title:
【発明の名称】新規なペプチダーゼ阻害剤類
Document Type and Number:
Japanese Patent JP3203579
Kind Code:
B2
Abstract:
This invention relates to analogs of peptidase substrates in which the nitrogen atom of the scissile amide group of the substrate peptide has been replaced by a substituted malonyl moiety. The contemplated peptidase inhibitors of the foregoing enzymes are selected from the generic formula the hydrates, isosteres or the pharmaceutically acceptable salts thereof wherein X is R1 is hydrogen, an amino protecting group selected from Group K, an alpha -amino acid or a peptide comprised of a number of alpha -amino acid building blocks, said alpha -amino acid or peptide optionally bearing on its terminal nitrogen atom an amino protecting group selected from Group K, R2 is the "R group" residue of the alpha -amino acid responsible for directing the inhibitor to the active site of the enzyme or is -A-SiR7R8R9, C1-10 alkyl, aralkyl or aryl with R7, R8 and R9, each being selected from C1-10, alkyl, aralkyl or aryl and A is a C1-6 alkylene, R4 is the specific R-group residue of the alpha -amino acid for that peptidase substrate analog, R5 is an alpha -amino acid or peptide comprised of alpha -amino acids or is deleted, Y is NHR3 or OR3 with R3 being H, C1-7 alkyl, benzyl or phenethyl. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
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Inventors:
Philip Bay
Michael angelastro
Syujatta Medi
Michael angelastro
Syujatta Medi
Application Number:
JP26036089A
Publication Date:
August 27, 2001
Filing Date:
October 06, 1989
Export Citation:
Assignee:
Merrell Pharmaceuticals, Inc.
International Classes:
A61K38/55; A61P3/00; A61P7/02; A61P7/06; A61P13/02; A61P15/00; A61P29/00; A61P37/00; A61P37/08; C07C215/04; C07C223/02; C07C225/02; C07C229/08; C07C229/26; C07C229/36; C07C231/12; C07C237/06; C07C237/08; C07C237/12; C12N9/99; C07C237/22; C07C257/16; C07C271/22; C07C271/54; C07C279/18; C07C279/24; C07C311/36; C07C311/37; C07F7/10; C07K1/02; C07K1/06; C07K1/113; C07K5/02; C07K5/06; C07K5/062; C07K5/065; C07K5/072; C07K5/08; C07K5/083; C07K5/10; C07K7/02; C07K14/81; A61K38/00; (IPC1-7): C07C229/08; C07C223/02; C07C225/02; C07C229/26; C07C229/36; C07C237/06; C07C237/08; C07C237/12; C07C237/22; C07C279/24; C07C311/36; C07C311/37; C07K1/02; C07K5/06; C07K5/08; C12N9/99
Domestic Patent References:
| JP50111005A | ||||
| JP4920118A | ||||
| JP50142505A | ||||
| JP58198296A | ||||
| JP55138389A |
Attorney, Agent or Firm:
Katsuro Sasai