3-AMINO-2-OXO-1-PIPERIDINEACETIC DERIVATIVES AS ENZYME INHIBITORS
申请人:CORVAS INTERNATIONAL, INC.
公开号:EP0802923A1
公开(公告)日:1997-10-29
US4997950A
申请人:——
公开号:US4997950A
公开(公告)日:1991-03-05
[EN] 3-AMINO-2-OXO-1-PIPERIDINEACETIC DERIVATIVES AS ENZYME INHIBITORS<br/>[FR] DERIVES DE L'ACIDE 3-AMINO-2-OXO-1-PIPERIDINEACETIQUE
申请人:——
公开号:WO1995035311A1
公开(公告)日:1995-12-28
[EN] The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis. [FR] La présente invention concerne des aldéhydes de peptides qui sont des inhibiteurs puissants et spécifiques de la thrombine, leurs sels pharmaceutiquement acceptables, et des compositions pharmaceutiquement acceptables de ces derniers. L'invention a également pour objet des procédés pour les utiliser comme agents thérapeutiques pour soigner des maladies chez le mammifère, caractérisées par une thrombose anormale.
Inhibition of Urease Activity by Dipeptidyl Hydroxamic Acids.
dipeptidyl hydroxamic acids (H-X-Gly-NHOH: X = amino acid residues) was synthesized, and the inhibitory activity against Jackbean and Proteus mirabilis ureases [EC3.5.1.5] was examined. A number of H-X-Gly-NHOH inhibited Jackbeanurease with an I50 of the order of 10(-6) M and inhibited Proteus mirabilis urease with an I50 of the order of 10(-5) M. The inhibition against Jackbeanurease was more potent