104856-05-5

Upstream product

• 1826-67-1 vinyl magnesium bromide 

Downstream Products

• 122226-05-5 (4S,5R,2'S,4'S)-3-<(tert-butyloxy)carbonyl>-4-(cyclohexylmethyl)-2,2-dimethyl-5-(4'-methyltetrahydrofuran-2'-yl)oxazolidine 
• 127230-36-8 (3S,5S,1'R,2'S)-5-<2'-<(tert-butyloxy)carbonyl>-3'-cyclohexyl-1'hydroxypropyl>-3-methyldihydrofuran-2(3H)-one 
• 122226-04-4 (4S,5R,1'S,3'S)-3-<(tert-butyloxy)carbonyl>-4-(cyclohexylmethyl)-5-(1'4'-dihydroxy-3'-methylbutyl)-2',2'-dimethyloxazolidine 
• 122226-02-2 (5S,4'S,5'R)-5-<3'-<(tert-butyloxy)carbonyl>-4'-(cyclohexylmethyl)-2',2'-dimethyloxazolidin-5'-yl>-3-methylenedihydrofuran-2(4H)-one 
• 122226-03-3 (3S,5S,4'S,5'R)-5-<3'-<(tert-butyloxy)carbonyl>-4'-(cyclohexylmethyl)-2',2'-dimethyloxazolidin-5'-yl>-3-methyldihydrofuran-2(3H)-one 
• 127230-19-7 (4S,5R)-4-Cyclohexylmethyl-5-((1S,3S)-1-hydroxy-4-methanesulfonyloxy-3-methyl-butyl)-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester 
• 127230-21-1 Toluene-4-sulfonic acid (2S,4S,5R,6S)-7-cyclohexyl-4,5-dihydroxy-2-methyl-6-(toluene-4-sulfonylamino)-heptyl ester 
• 127306-04-1 (4S,5S)-3-[(tert-butyloxy)carbonyl]-4-(cyclohexylmethyl)-2,2-dimethyloxazolidine-5-carboxaldehyde 
• 117997-58-7 tert-butyl (4S,5R)-4-(cyclohexylmethyl)-5-formyl-2,2-dimethyl-3-oxazolidinecarboxylate 
• 121533-55-9 (4S,5S)-3-tert-butoxycarbonyl-4-cyclohexylmethyl-2,2-dimethyl-5-vinyloxazolidine 
• 122226-01-1 3-<(tert-butyloxy)carbonyl>-4-(cyclohexylmethyl)-2,2-dimethyl-5-vinyloxazolidine 

Relevant academic research and scientific papers

HETEROCYCLIC PEPTIDE RENIN INHIBITORS

A renin inhibiting compound of the formula STR1 wherein X is N, O or CH; R 1 is absent or a functional group; A and L are independently selected from absent, C=O, SO 2 and CH 2 ; D is C=O, SO. sub.2 or CH 2 ; Y is N or CH; R 2 is hydrogen, loweralkyl or substituted alkyl; Z is a functional group; R 3 is loweralkyl or substituted alkyl; n is 0 or 1; and T is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.

Psoriasis treatment

The present invention relates to the use of renin inhibitors and to renin inhibitor compositions for treatment of psoriasis.

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.

HETEROCYCLIC RENIN INHIBITORS

A renin inhibiting compound of the formula: STR1 wherein A is a substituent; R 1 is loweralkyl, loweralkenyl, alkoxyalkyl, [(alkoxy) alkoxy]alkyl, alkoxycarbonylalkyl, carboxyalkyl, (thioalkoxy) alkyl, benzyl or heterocyclic ring substituted methyl; R 2 i

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.

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 wherein A is a substituent; W is CO or CHOH and U is CH2/sub

Renin-inhibiting functionalized peptidyl aminodiols and - triols

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

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 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.