128117-25-9

Upstream product

• 128117-24-8 methyl 2-benzyl-3-<<1-(benzyloxycarbonyl)azetidin-3-yl>thio>propionate 
• 128117-23-7 3-(acetylthio)-1-(benzyloxycarbonyl)azetidine 
• 128117-22-6 1-Benzyloxycarbonyl-3-hydroxyazetidine 
• 3070-71-1 methyl 2-benzylacrylate 
• 5669-19-2 2-Benzyl-2-propenoic acid 

Downstream Products

• 128117-26-0 methyl 2-Benzyl-3-(1-methylazetidin-3-ylsulfonyl)propionate 

Relevant academic research and scientific papers

Studies directed toward the design of orally active renin inhibitors. 2. Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl- 3-[[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-L-alanine amide of (2S,3R,4S)-2-amino-1-cyc

Employing a set of empirical guidelines for the design of well-absorbed renin inhibitors, we have followed two strategies to improve potency while maintaining bioavailability. One process involved incorporation of an extended N-terminal residue bearing a

Peptidyl difluorodiol renin inhibitors

A renin inhibiting compound of the formula: wherein A is a functional group; W is (1)-C(O)-,(2)-CH(OH)-or(3)-N(R?)-wherein R? is hydrogen or loweralkyl; U is (1)-C(O)-,(2)-CH?-or(3)-N(R?)-wherein R? is hydrogen or lower alkyl, with the proviso that when W is-CH(OH)-then U is-CH?-and with the proviso that U is-C(O)-or-CH?-when W is-N(R?)-; V is (1)-CH-,(2)-C(OH)-or(3)-C(halogen)-with the proviso that v is-CH--when U is-N(R?)-; Q is-CH(R?)-or-C(=CHR1a)-wherein R? is (1) loweralkyl,(2) cycloalkylalkyl,(3) arylalkyl,(4) (heterocyclic) alkyl,(5) 1-benzyloxyethyl,(6) phenoxy,(7) thiophenoxy or(8) anilino, provided that B is-CH?-or-CH(OH)-or A is hydrogen when R? is phenoxy, thiophenoxy or anilino and R1a is aryl or heterocyclic; R? is a functional group; R? is (1) loweralkyl,(2) cycloalkylmethyl or(3) benzyl; R? is-CH(OH)-or-C(O)-; R? is-CH(OH)-or-C(O)-; and Z is (1) lower alkyl,(2) aryl,(3) arylalkyl,(4) cycloalkyl,(5) cycloalkylalkyl,(6) heterocyclic or(7) (heterocyclic)alkyl; or a pharmaceutically acceptable salt, ester or prodrug thereof.

PEPTIDYL AMINODIOL RENIN INHIBITORS

A renin inhibiting compound having an aminodiol functional group is useful for treating hypertension, congestive heart failure and glaucoma and inhibits retroviral protease.

Renin-inhibiting functionalized peptidyl aminodiols and - triols

A renin inhibiting compound of the formula: or a pharmaceutically acceptable salt, ester or prodrug thereof.