104882-02-2Relevant academic research and scientific papers
New approaches to the asymmetric synthesis of dipeptide isosteres via β-Lactam Synthon Method
Ojima, Iwao,Wang, Hong,Wang, Tao,Ng, Edward W.
, p. 923 - 926 (2007/10/03)
New and efficient synthetic routes to dipeptide isosteres with high enantiomeric purity, e.g., hydroxyethylene, dihydroxyethylene and hydroxyethylamine isosteres, have been developed via oxiranes 6 and formyloxazolines 13 derived from N-t-Boc-β-lactams 4.
Glaucoma treatment
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, (2008/06/13)
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.
Peptidylaminodiols
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, (2008/06/13)
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.
ALPHA-AMINOACYL BETA-AMINOACYL AMINODIOLS AS ANTI-HYPERTENSIVE AGENTS
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, (2008/06/13)
Compounds characterized generally as α-aminoacyl β-aminoactyl aminodiols are useful as renin inhibitors for the treatment of hypertension.
PEPTIDYL ALPHA-AMINOACYL AMINODIOL CARBAMATES AS ANTI-HYPERTENSIVE AGENTS
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, (2008/06/13)
Non-peptidyl compounds characterized generally as aminoacyl aminodiol carbamates are useful as renin inhibitors for the treatment of hypertension.
Glaucoma treatment
-
, (2008/06/13)
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
