- HETEROCYCLIC PEPTIDE RENIN INHIBITORS
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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.
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- Psoriasis treatment
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The present invention relates to the use of renin inhibitors and to renin inhibitor compositions for treatment of psoriasis.
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- Glaucoma treatment
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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.
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- Glaucoma treatment
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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
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- Potent, Low Molecular Weight Renin Inhibitors Containing a C-Terminal Heterocycle: Hydrogen Bonding at the Active Site
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A series of low-nanomolar renin inhibitors containing novel C-terminal heterocycles has been designed by formally cyclizing the C-terminus of a glycol-based inhibitor to the second hydroxyl.Molecular modeling suggests that the heterocyclic oxygen hydrogen
- Rosenberg, Saul H.,Dellaria, Joseph F.,Kempf, Dale J.,Hutchins, Charles W.,Woods, Keith W.,et al.
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p. 1582 - 1590
(2007/10/02)
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- Renin-inhibiting peptidyl heterocycles
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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.
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