114359-43-2

Upstream product

• 40137-22-2 3-methylamino-propane-1,2-diol 
• 52177-38-5 α-isocyanato-L-O-methyltyrosine methyl ester 

Downstream Products

• 114359-44-3 (2RS)-<<(2,3-dihydroxypropyl)methylamino>carbonyl>-O-methyltyrosine 
• 127944-50-7 (S)-N-[(S)-1-[(1S,2R)-1-Cyclohexylmethyl-2-((S)-3-ethyl-2-oxo-oxazolidin-5-yl)-2-hydroxy-ethylcarbamoyl]-2-(3H-imidazol-4-yl)-ethyl]-2-[3-(2,3-dihydroxy-propyl)-3-methyl-ureido]-3-(4-methoxy-phenyl)-propionamide 

Relevant academic research and scientific papers

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.

Water-Soluble Renin Inhibitors: Design of a Subnanomolar Inhibitor with a Prolonged Duration of Action

Incorporation of nonreactive polar functionalities at the C- and N-termini of renin inhibitors led to the development of a subnanomolar compound (21) with millimolar solubility.This inhibitor demonstrated excellent efficacy and a long duration of action upon intravenous administration to monkeys.While activity was also observed intraduodenally, a comparison of the blood pressure responses indicated low bioavailability.Subsequent experiments in rats showed that, although the compound was absorbed from the gastrointrestinal tract, extensive liver extraction severely limited bioavailability.

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.

Angiotensinogen analogs

The invention relates to renin inhibiting compounds of the formula STR1 wherein A is hydrogen; loweralkyl; arylalkyl; OR10 or SR10 wherein R10 is hydrogen, loweralkyl or aminoalkyl; NR11 R12 wherein R11 and R12 are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl; STR2 wherein B is NH, alkylamino, S, O, CH2 or CHOH and R13 is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, aminoalkyl, alkoxycarbonylalkyl, carboxyalkyl, N-protected aminoalkyl, alkylaminoalkyl, (N-protected)(alkyl)aminoalkyl, dialkylaminoalkyl, (heterocyclic) alkyl or a substituted or unsubstituted heterocyclic; W is CO or CHOH and U is CH2 or NR2 with the proviso that when W is CHOH then U is CH2 ; R1 is loweralkyl, cycloaklylmethyl, benzyl, α,α-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)-methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R1 is phenoxy, thiophenoxy or anilino, B is CH2 or CHOH or A is hydrogen, R3 is loweralkyl, vinylloweralkyl, benzyl or heterocyclic ring substituted methyl, R5 is loweralkyl, cycloalkylmethyl or benzyl; R2 and R4 are independently selected from hydrogen and loweralkyl; R6 is CHOH or CO; R7 is CH2, CF2 or CF with the proviso that when R6 is CO, R7 is CF2 ; R8 is CH2, CHR14 wherein R14 is lower-alkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, or R7 and R8 taken together can be STR3 with the proviso that when R7 is CF2, R8 is CH2 ; E is O, S, SO, SO2, NR15 wherein R15 is hydrogen or loweralkyl or NR16 CO wherein R16 is hydrogen or loweralkyl; R9 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protected group, or E and R9 taken together can be N3, with the proviso that when E is NH, R9 is an N-protecting group; and pharmaceutically acceptable salts thereof.