97441-39-9

Upstream product

• 78775-63-0 diethyl α-(1-methyl-1-phenylethyl)malonate 

Downstream Products

• 114359-58-9 Ethyl 2(R,S)-[[(4-morpholinyl)carbonyl]amino]-3, 3-dimethyl-3-phenylpropionate 
• 116183-35-8 Morpholine-4-carboxylic acid {(R)-1-[(S)-1-((1S,2R,3S)-1-cyclohexylmethyl-2,3-dihydroxy-5-methyl-hexylcarbamoyl)-2-(1H-imidazol-4-yl)-ethylcarbamoyl]-2-methyl-2-phenyl-propyl}-amide 
• 116183-34-7 (2S,3R,4S)-2-{[(4-morpholinylcarbonyl)-L-β,β-dimethylphenylalanyl-L-histidyl]amino}-1-cyclohexyl-3,4-dihydroxy-6-methylheptane 
• 114359-59-0 2(R,S)-[[(4-Morpholinyl)carbonyl]amino]-3,3-dimethyl-3-phenylpropionic acid 
• 64287-40-7 <α,α-Dimethyl-benzyl>-carbaethoxy-keten 

Relevant academic research and scientific papers

Peptidylaminodiols

A renin inhibiting compound of the formula: STR1 wherein A is a substituent; W is C=O or CHOH; U is CH2 or NR2, provided that when W is CHOH then U is CH2 ; R1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, (alpha,alpha)-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R2 is hydrogen or loweralkyl; R3 is loweralkenyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R4 is loweralkyl, cycloalkylmethyl or benzyl; R5 is vinyl, formyl, hydroxymethyl or hydrogen; R7 is hydrogen or loweralkyl; R8 and R9 are independently selected from OH and NH2 ; and R6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R5 and R7 are both hydrogen and R8 and R9 are OH, the carbon bearing R5 is of the "R" configuration and the carbon bearing R6 is of the "S" configuration, or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.

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.

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.

Renin-inhibiting functionalized peptidyl aminodiols and - triols

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

Renin-inhibiting peptidyl heterocycles

A renin inhibiting compound of the formula:*(formula 01)* wherein A is a substituent; W is C=O, CHOH or NR2 wherein R2 is hydrogen or loweralkyl; U is C=O, CH2 or NR2 wherein R2 is hydrogen or loweralkyl, with the proviso that when W is CHOH then U is CH2 and with the proviso that U is C=O or CH2 when W is NR2; V is CH, C(OH) or C(halogen) with the proviso that V is CH when U is NR2; R1 is loweralkyl, cycloalkylalkyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, 4-hydroxybenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (unsubstituted heterocyclic)methyl, (substituted heterocyclic)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino, provided that B is CH2 or CHOH or A is hydrogen when R1 is phenoxy, thiophenoxy or anilino; R3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, azidoalkyl, aminoalkyl, (alkyl)aminoalkyl, dialkylaminoalkyl,(alkoxy)(alkyl)aminoalkyl, (alkoxy)aminoalkyl, benzyl or heterocyclic ring substituted methyl; R4 is loweralkyl, cycloalkylmethyl or benzyl; R5 is OH or NH2; and Z is a substituent. Also disclosed are compositions for and a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.

Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a structurally modified phenylalanine residue to impart proteolytic stability

A series of renin inhibitors have been prepared and evaluated for their susceptibility to cleavage by the serine protease chymotrypsin. The compounds were designed by consideration of the structural requirements in the active-site region of renin and chymotrypsin. By systematic alteration of the P3 phenylalanine residue, compounds with varying degrees of renin inhibitory potency and chymotrypsin susceptibility were obtained. Selected analogues from this group were examined in vivo for both their hypotensive effects and metabolic patterns.