136630-82-5

Upstream product

• 136630-95-0 (4S,5S)-4-Benzyl-5-(2-methanesulfonyloxy-ethyl)-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester 
• 133333-22-9 (4S,5S)-4-benzyl-3-(tert-butoxycarbonyl)-2,2-dimethyloxazolidine-5-acetic acid methyl ester 
• 136630-94-9 (4S,5S)-4-Benzyl-5-(2-hydroxy-ethyl)-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester 
• 101669-80-1 methyl (3S,4S)-N-tert-butoxycarbonyl-4-amino-3-hydroxy-5-phenylpentanoate 
• 203806-66-0 (4S,5S)-4-Benzyl-5-but-3-enyl-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester 
• 136630-80-3 (S)-4-benzyl-5-(2-cyanoethyl)-2,2-dimethyloxazolidine-3-carboxylic acid tert-butyl ester 

Downstream Products

• 120451-87-8 BOC-PheΨ<(S)-CHOHCH2>Gly-ACHPA-Ile N-<(4-amino-2-methyl-5-pyrimidinyl)methyl>amide 
• 136658-79-2 N_α-propanoyl>ACHPA>Ile N-<(4-amino-2-methyl-5-pyrimidinyl)methyl>amide 

Relevant academic research and scientific papers

HYDROXY-ETHYLENE DERIVATIVES FOR THE TREATMENT OF ARTHROSIS

The present invention relates to compounds of the formula I and in particular medicaments comprising at least one compound of the formula I for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering

New approaches to the asymmetric synthesis of dipeptide isosteres via β-Lactam Synthon Method

New and efficient synthetic routes to dipeptide isosteres with high enantiomeric purity, e.g., hydroxyethylene, dihydroxyethylene and hydroxyethylamine isosteres, have been developed via oxiranes 6 and formyloxazolines 13 derived from N-t-Boc-β-lactams 4.

Substrate Analogue Renin Inhibitors Containing Replacements of Histidine in P2 or Isosteres of the Amide Bond between P3 and P2 Sites

Incorporation of β-alanine or γ-aminobutyric acid in position P2 of ACHPA or LeuΨVal-based tetrapeptides gave highly active renin inhibitors (compounds V,VI, and XVII) with high specificity for renin and a remarkable stability against chymotrypsin.Replacement of the amide bond between P2 and P3 by isosteres (ketomethylenes, hydroxyethylenes, and the corresponding thio-insertion analogues) led to compounds (VIII-XIII, XVIII, and XIX) with renin inhibitory activity in the nanomolar range.Oral activity was achieved by incorporation of polar functionalities at the N-terminus of β-alanine-containing tetrapeptides.One of these compounds (XXVIII) was chosen for further studies.This inhibitor demonstrated excellent efficacy and a long duration of action after intravenous and oral administration to cynomolgus monkeys.