52177-40-9

Upstream product

• 53267-93-9 O-methyl-N-tert-butoxycarbonyl-L-tyrosine 
• 70601-63-7 (D)-4-methoxyphenylalanine hydrochloride 
• 75-36-5 acetyl chloride 
• 100-51-6 benzyl alcohol 
• 137992-25-7 N-t-butoxycarbonyl-O-methyl-L-tyrosine benzyl ester 
• 100-39-0 benzyl bromide 
• 3978-80-1 Boc-Tyr-OH 

Downstream Products

• 122225-86-9 N-<(1-methylpiperidin-4-yl)carbonyl>-O-methyltyrosine benzyl ester 
• 122224-96-8 N-<(1-methylpiperidin-4-yl)carbonyl>-O-methyltyrosine 
• 215455-05-3 N-Ethoxycarbonylmethyl-2-(R)-amino-3-(4-methoxyphenyl)-propionic acid benzyl ester 

Relevant academic research and scientific papers

Total synthesis of proposed structure of coibamide A, a highly N- and O-methylated cytotoxic marine cyclodepsipeptide

Total synthesis of the originally proposed structure of coibamide A, a highly N- and O-methylated cytotoxic marine cyclodepsipeptide, has been accomplished by using a [(4+1)+3+3]-peptide fragment-coupling strategy and careful examination and optimization

Heterocyclic derivatives and their use as antithrombotic agents

The present invention relates to antithrombotic compounds comprising the group Q, Q having formula (I), wherein the substructure (i) is a structure selected from (a, b and c), wherein X is O or S; X′ being independently CH or N; and m is 0, 1, 2 or 3; wherein the group Q is bound through an oxygen atom or an optionally substituted nitrogen or carbon atom, or a pharmaceutically acceptable salt thereof or a prodrug thereof. The compounds of the invention are therapeutically active and in particular are antithrombotic agents.

ORALLY ACTIVE RENIN INHIBITORS

This invention relates to compounds of the formula STR1 wherein Q, Z, D, E, R 3, R 4, R 5 and R 6 are defined as below, and the pharmaceutically acceptable salts thereof are disclosed. The compounds are useful as antihypertensive agents.

Studies directed toward the design of orally active renin inhibitors. 1. Some factors influencing the absorption of small peptides

A systematic evaluation of structure-absorption relationships using a high throughput intraduodenal rat screening model has led to the delineation of a set of structural parameters that appear to govern bioavailability in a series of peptide-based renin inhibitors. Optimum structures, exemplified by 25 and 41, incorporated a single, solubilizing substituent at the C- or N- terminus combined with a lipophilic P2-site residue. Both inhibitors gave unprecedented plasma drug levels upon intraduodenal administration to monkeys, and the calculated bioavailability for 41 (14 ± 4%) is the highest reported for any peptidic renin inhibitor.

Orally active renin inhibitors

This invention relates to compounds of the formula wherein Q, Z, D, E, R3, R?, R? and R? are defined as below, and the pharmaceutically acceptable salts thereof are disclosed. The compounds are useful as antihypertensive agents.