108868-89-9

Upstream product

• 107202-61-9 (2R,3S)-3-(t-butoxycarbonylamino)-4-cyclohexyl-1,2-epoxybutane 

Downstream Products

• 108868-91-3 (2S,3S)-1-amino-2-hydroxy-3-<(tert-butyloxycarbonyl)amino>-4-cyclohexylbutane acetic acid salt 
• 108868-66-2 {(S)-1-[(S)-1-[(1S,2S)-1-Cyclohexylmethyl-2-hydroxy-3-(4-methyl-pentanoylamino)-propylcarbamoyl]-2-(1H-imidazol-4-yl)-ethylcarbamoyl]-2-phenyl-ethyl}-carbamic acid tert-butyl ester 
• 108868-58-2 (2S,3S)-1-<<(3-methylbutyl)carbonyl>amino>-2-hydroxy-3-<(tert-butyloxycarbonyl)amino>-4-cyclohexylbutane 

Relevant academic research and scientific papers

Novel Renin Inhibitors Containing Analogues of Statine Retro-Inverted at the C-Termini: Specificity at the P2 Histidine Site

Substituted 1,3- and 1,4-diamines were prepared from epoxides derived from Boc-leucine or Boc-cyclohexylalanine. These diamines were incorporated into renin inhibitors (IC50 = 4-1500 nM) replacing the Leu-Val scissile bond in small peptide analogues of angiotensinogen. Replacement of the P2 histidine imidazole with other heterocycles maintained or enhanced binding while changing the overall basicity of the inhibitor. Finally, substitution of O-methyltyrosine for the P3 phenylalanine suppressed chymotrypsin cleavage of the P3-P2 bond.

RENIN INHIBITING COMPOUNDS

The invention relates to renin inhibiting compounds of the formula STR1 wherein A is hydrogen; loweralkyl; arylalkyl; Or 10 wherein R 10 is hydrogen or loweralkyl; NR 11 R 12 wherein R. sub.11 and R 12 are independently selected from hydrogen and loweralkyl; or R 13--CO--B wherein B is NH, O, CH 2, HNCH 2 and R 13 is loweralkyl, alkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, aminoalkyl, N-protected aminoalkyl, hydroxylated dialkylamino, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic, carboxyalkyl, or lower alkyl carboxyalkyl esters; W is N or CH: U,V may be the following combinations H,OH; OH,H; H, H; or when taken together as O represents a carbonyl with the provisos that if U,V=H, OH, then W=CH, and if U,V=O then W=N; R 1 , R 3 and R 5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R 2, R 4, R 7, R 8 and R 9 are hydrogen or loweralkyl and may be the same or different; X is NH, O, S, SO, SO 2, or CH 2 ; and R 6 is loweralkyl cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protecting group, with the proviso that R 6 may be an N-protecting group when X is NH.