110613-89-3

Upstream product

• 110613-67-7 (4S,5S)-N-isopentyl-5-<<(tert-butyloxy)carbonyl>amino>-6-cyclohexyl-4-hydroxyhex-1-ene-2-carboxamide 
• 110613-29-1 N-isopentylmethacrylamide 
• 98105-42-1 (S)-2-(t-butoxycarbonylamino)-3-cyclohexyl-1-propanal 

Downstream Products

• 110613-42-8 {(S)-1-[(S)-1-[(1S,2S)-1-Cyclohexylmethyl-2-hydroxy-4-(3-methyl-butylcarbamoyl)-pent-4-enylcarbamoyl]-2-(1H-imidazol-4-yl)-ethylcarbamoyl]-2-phenyl-ethyl}-carbamic acid tert-butyl ester 
• 110613-44-0 N--5(S)-amino-6-cyclohexyl-4(S)-hydroxy-2-(N-isopentylcarbamoyl)hex-1-ene 
• 110613-52-0 {(S)-1-[(S)-1-[(1S,2S)-1-Cyclohexylmethyl-2-hydroxy-4-(3-methyl-butylcarbamoyl)-pent-4-enylcarbamoyl]-2-(1H-imidazol-4-yl)-ethylcarbamoyl]-2-hydroxy-ethyl}-carbamic acid tert-butyl ester 
• 110613-51-9 (4S,5S)-5-[(S)-2-((S)-2-Acetylamino-3-phenyl-propionylamino)-3-(1H-imidazol-4-yl)-propionylamino]-6-cyclohexyl-4-hydroxy-2-methylene-hexanoic acid (3-methyl-butyl)-amide 
• 110613-54-2 N--L-phenylalanyl-L-alanyl>-5(S)-amino-6-cyclohexyl-4(S)-hydroxy-2-(N-isopentylcarbamoyl)hex-1-ene 1,2-oxide 
• 110613-53-1 (4S,5S)-6-Cyclohexyl-4-hydroxy-5-[(S)-2-(2-hydroxy-3-phenyl-propionylamino)-3-(1H-imidazol-4-yl)-propionylamino]-2-methylene-hexanoic acid (3-methyl-butyl)-amide 
• 110613-90-6 N--L-histidyl>-5(S)-amino-6-cyclohexyl-4(S)-hydroxy-2-(N-isopentylcarbamoyl)hex-1-ene 

Relevant academic research and scientific papers

Glaucoma treatment

A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: STR1 where A is a substituent; W is CO or CHOH and U is CH2 or NR2 wherein R2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is Ch2 ; R1 is loweralkyl, cycloalkyl methyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, 1-bezyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)loweralkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R4 is substituted hydroxyalkyamino.

Renin Inhibitors Based on Novel Dipeptide Analogues. Incorporation of the Dehydrohydroxyethylene Isostere at the Scissile Bond

The design and synthesis of renin inhibitors that incorporate the novel dipeptide isostere (4S,5S)-5-amino-6-cyclohexyl-4-hydroxyhex-1-ene-2-carboxylic acid as a transition-state analogue are described.Titanium-promoted condensation of dilithiated N-alkylmethacrylamides with protected amino aldehydes results in efficient preparation of protected dipeptide analogues 7 and 8.Incorporation of 7 into the partial sequence of angiotensinogen affords potent in vitro inhibitors of human renin.Further chemical manipulation of the unsaturated amide moiety allows the study of structure-activity relationships in both the P1' and P2' sites.Details of the syntheses, stereochemical determinations, and in vitro renin inhibition are presented.