121533-55-9

Upstream product

• 116-11-0 2-Methoxypropene 
• 104856-06-6 tert-butyl [(1S,2S)-1-(cyclohexylmethyl)-2-hydroxy-3-butenyl]carbamate 
• 124577-56-6 (4S,5S)-3-(tert-butoxycarbonyl)-4-(cyclohexylmethyl)-5-<2-(mesyloxy)ethyl>-2,2-dimethyloxazolidine 
• 124577-55-5 (4S,5S)-3-(tert-butoxycarbonyl)-4-(cyclohexylmethyl)-2,2-dimethyloxazolidine-5-ethanol 
• 104856-05-5 (3RS,4S)-4-<(tert-butyloxy)carbonyl>-5-(cyclohexylmethyl)-3-hydroxy-1-pentene 
• 77-76-9 2,2-dimethoxy-propane 
• 104882-44-2 (2S,3S)-2-(tert-butoxycarboxamido)-1-cyclohexyl-5-hexen-3-ol 
• 143122-11-6 (4S,5S)-5-allyl-3-(tert-butoxycarbonyl)-4-(cyclohexylmethyl)-2,2-dimethyloxazolidine 
• 145341-80-6 (4S,5S)-3-(tert-butoxycarbonyl)-4-cyclohexylmethyl-5-formylmethyl-2,2-dimethyl-1,3-oxazolidine 

Downstream Products

• 143122-12-7 (4S,5R)-3-(tert-butoxycarbonyl)-4-(cyclohexylmethyl)-2,2-dimethyloxazolidine-5-methanol 
• 143122-13-8 (4S,5R)-3-(tert-butoxycarbonyl)-4-(cyclohexylmethyl)-5-<(mesyloxy)methyl>-2,2-dimethyloxazolidine 
• 143122-30-9 (4S,5S)-3-(tert-butoxycarbonyl)-4-(cyclohexylmethyl)-5-<(1,2-dihydro-2-oxo-1-pyridyl)methyl>-2,2-dimethyloxazolidine 
• 143122-31-0 (4S,5S)-3-(tert-butoxycarbonyl)-4-(cyclohexylmethyl)-2,2-dimethyl-5-<(4-pyridyloxy)methyl>oxazolidine 
• 143122-29-6 (4S,5S)-3-(tert-butoxycarbonyl)-4-(cyclohexylmethyl)-2,2-dimethyl-5-<(2-pyridyloxy)methyl>oxazolidine 
• 143122-33-2 (4S,5S)-3-(tert-butoxycarbonyl)-4-(cyclohexylmethyl)-2,2-dimethyl-5-<(2-pyridylthio)methyl>oxazolidine 
• 143122-32-1 (4S,5S)-3-(tert-butoxycarbonyl)-4-(cyclohexylmethyl)-2,2-dimethyl-5-<(1,4-dihydro-4-oxo-1-pyridyl)methyl>oxazolidine 
• 143142-37-4 (4S,5S)-3-(tert-butoxycarbonyl)-4-(cyclohexylmethyl)-2,2-dimethyl-5-<(1H-1,2,4-triazol-3-ylthio)methyl>oxazolidine 
• 1053694-85-1 {(R)-1-[(1S,2S)-1-Cyclohexylmethyl-2-hydroxy-3-(2-oxo-2H-pyridin-1-yl)-propylcarbamoyl]-2-methylsulfanyl-ethyl}-carbamic acid tert-butyl ester 
• 1054649-92-1 {(R)-1-[(1S,2S)-1-Cyclohexylmethyl-2-hydroxy-3-(4-oxo-4H-pyridin-1-yl)-propylcarbamoyl]-2-methylsulfanyl-ethyl}-carbamic acid tert-butyl ester 
• 139470-42-1 {(R)-1-[(1S,2R)-1-Cyclohexylmethyl-2-hydroxy-3-(pyridin-2-yloxy)-propylcarbamoyl]-2-methylsulfanyl-ethyl}-carbamic acid tert-butyl ester 
• 1054641-61-0 {(R)-1-[(1S,2R)-1-Cyclohexylmethyl-2-hydroxy-3-(pyridin-2-ylsulfanyl)-propylcarbamoyl]-2-methylsulfanyl-ethyl}-carbamic acid tert-butyl ester 
• 1055036-50-4 {(R)-1-[(1S,2R)-1-Cyclohexylmethyl-2-hydroxy-3-(pyridin-4-yloxy)-propylcarbamoyl]-2-methylsulfanyl-ethyl}-carbamic acid tert-butyl ester 
• 1054662-93-9 {(R)-1-[(1S,2R)-1-Cyclohexylmethyl-2-hydroxy-3-(1H-[1,2,4]triazol-3-ylsulfanyl)-propylcarbamoyl]-2-methylsulfanyl-ethyl}-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

CYCLIC RENIN INHIBITORS CONTAINING 3(S)-AMINO-4-CYCLOHEXYL-2(R)-HYDROXY-BUTANOIC ACID OR 4-CYCLO-HEXYL-(2R,3S)-DIHYDROXYBUTANOIC ACID OR RELATED ANALOGS

Compounds of the formula: STR1 are disclosed. These compounds inhibit the angiotensinogen-cleaving action of the natural proteolytic enzyme, renin, and are useful in treating, preventing or managing renin-associated hypertension, hyperaldosteronism, congestive heart failure, and glaucoma.

Renin inhibitors containing a pyridyl amino diol derived C-terminus

Based on the concept of transition-state analogs, a series of nonpeptide renin inhibitors with the new (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy- 6-(2-pyridyl)hexane moiety at the C-terminal functionality were synthesized and evaluated for inhibition

Cyclic renin inhibitors

Compounds of the formula: are disclosed. These compounds inhibit the angiotensinogen-cleaving action of the natural proteolytic enzyme, renin, and are useful in treating, preventing or managing renin-associated hypertension, hyperaldosteronism, congestive

Renin inhibitors containing new P1-P1' dipeptide mimetics with heterocycles in P1'

A series of renin inhibitors containing new P1-P1' dipeptide mimetics are presented. The P1-P1' mimetics were obtained from (4S,5S)-3-(tert- butoxycarbonyl)-4-(cyclohexylmethyl)-5-[(ω-mesyloxy)alkyl]-2,2- dimeth

Macrocyclic lactones having renin inhibiting properties

Compounds of the formula:

Design and synthesis of P2-P1'-linked macrocyclic human renin inhibitors

Using a computer model of the active site of human renin developed at Merck, we designed a series of novel P2-P1'-linked, macrocyclic renin inhibitors 3-10. These unique inhibitors incorporate a transition-state isostere within a 13- or 14-membered ring. The three most active compounds in this family were 13-membered-ring glutamine-derived inhibitor 3, 14-membered-ring diaminopropionic acid derived inhibitor 6, and 13-membered-ring diol 9 (IC50 0.61, 0.59, 0.65 μM, respectively). Modification of inhibitor 3 at P4 led to 56 nM macrocyclic renin inhibitor 39. This study shows the viability of renin inhibitor designs which incorporate a scissile-bond replacement within a macrocycle.