112190-41-7

Downstream Products

• 147895-52-1 (4S,5R,1'S,2'R)-3-(tert-Butyloxycarbonyl)-4-(cyclohexylmethyl)-2,2-(dimethyl)-5-[1'-hydroxy-2'-methoxycarbonyl-3'-(methyl)butyl]oxazolidine 
• 142688-71-9 (4S,5R,1'R)-3-(tert-Butyloxycarbonyl)-4-(cyclohexylmethyl)-5-(2',2'-difluoro-2'-ethoxycarbonyl-1'-(hydroxy)ethyl)-2,2-(dimethyl)oxazolidine 
• 138588-20-2 (4R,5S)-5-[(1R,2S)-2-tert-Butylsulfanylcarbonyl-1-(imidazole-1-carbothioyloxy)-3-methyl-butyl]-4-cyclohexylmethyl-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester 
• 129921-97-7 (4R,5S)-5-((1R,2S)-2-Butylcarbamoyl-1-hydroxy-3-methyl-butyl)-4-cyclohexylmethyl-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester 
• 138588-21-3 (4R,5R)-5-((R)-2-tert-Butylsulfanylcarbonyl-3-methyl-butyl)-4-cyclohexylmethyl-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester 
• 138588-19-9 (4S,5R)-4-Cyclohexylmethyl-5-((2S,3R)-3-isopropyl-4-oxo-oxetan-2-yl)-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester 
• 125816-10-6 (3R,5R)-5-((R)-1-Amino-2-cyclohexyl-ethyl)-3-isopropyl-dihydro-furan-2-one 
• 138588-18-8 (4S,5R)-5-((1S,2S)-2-tert-Butylsulfanylcarbonyl-1-hydroxy-3-methyl-butyl)-4-cyclohexylmethyl-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester 
• 138588-18-8 (4S,5S)-5-((1S,2S)-2-tert-Butylsulfanylcarbonyl-1-hydroxy-3-methyl-butyl)-4-cyclohexylmethyl-2,2-dimethyl-oxazolidine-3-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

Psoriasis treatment

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

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.

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.

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 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.