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7384917 |
Chimeric natriuretic peptides
Peptides of Dendroaspis, including chimeric peptides thereof, are provided, as well as methods of using the peptides as natriuretics, diuretics, and/or vasodilators.
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7361637 |
Hypotensors
There are provided a method for selection of a substance which is capable of controlling activation of prorenin where an adjusting ability of the activation of prorenin by protein-protein...
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7071169 |
Pyrane derivatives as both ACE-and NEP-inhibitors
Compounds of the formula (I), wherein R1, R1–R7 and alk have meaning as defined, pharmaceutical compositions thereof, and use thereof for the treatment and/or prevention of cardiovascular d...
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6998137 |
Proteins deposited onto sparingly soluble biocompatible particles for controlled protein release into a biological environment from a polymer matrix
The present invention relates to compositions and methods for the modulated release of one or more proteins or peptides. The composition is comprised of a biocompatible polymeric matrix, a protein...
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6551578 |
Modulated release particles for aerosol delivery
A modulated release aerosol formulation is disclosed. The formulation comprises a polysaccharide polymer having a selected medicament associated therewith, a fluid carrier for carrying and...
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6495338 |
Drug screening and diagnosis based on paracrine tubular renin-angiotensin system
The present invention relates to a method for screening drugs for use in treating hypertension using the tubular renin-angiotensinogen system identified by the present invention. The invention...
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6468507 |
Non-aqueous aerosol formulation comprising rosiglitazone maleate, a non-aqueous carrier, and an amino acid stabilizer
A non-aqueous medicinal aerosol formulation comprising rosiglitazone maleate, a fluid carrier, and an amino acid stabilizer. The aerosol formulation may also include drug combination formulations...
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6464959 |
Non-aqueous aerosol suspension comprising troglitazone, a fluid propellant, and an amino acid stabilizer
A non-aqueous medicament aerosol formulation comprising troglitazone, or a derivative thereof, a fluid carrier, and an amino acid stabilizer. The aerosol formulation may also include drug...
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6201072 |
Biodegradable low molecular weight triblock poly(lactide-co- glycolide) polyethylene glycol copolymers having reverse thermal gelation properties
A water soluble, biodegradable ABA- or BAB-type tri-block polymer is disclosed that is made up of a major amount of a hydrophobic A polymer block made of a biodegradable polyester and a minor...
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6191156 |
Compositions and methods for treating bladder dysfunction
A method for treating patients having bladder dysfunction is described. The method involves the step of treating a patient with a renin-angiotensin system inhibitor. Preferably the inhibitor is an...
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6034175 |
Salts of peptides with carboxy-terminated polyesters
This invention relates to novel salts composed of a cation derived from a peptide containing at least one basic group and an anion derived from a carboxy-terminated polyester, processes for the...
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5981470 |
Uterine fibroid treatment
The use of a) an angiotensin-converting enzyme (ACE) inhibitor such as Captopril or Enalapril, b) an angiotensin II-receptor antagonist such as Saralasin or Losartan, or c) a renin inhibitor, such...
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5932462 |
Multiarmed, monofunctional, polymer for coupling to molecules and surfaces
Multi-armed, monofunctional, and hydrolytically stable polymers are described having the structure ##STR1## wherein Z is a moiety that can be activated for attachment to biologically active...
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5776885 |
Sustained and controlled release of water insoluble polypeptides
A pharmaceutical composition for the sustained release of a peptide wherein the composition includes a polylactide polymer, a polymer of lactic acid and glycolic acid, or a mixture of such polymers...
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5688770 |
Antiglaucoma compositions and methods
The present invention relates to ophthalmo-logical pharmaceutical compositions comprising a renin inhibitor and to methods for using said composition in the treatment of glaucoma.
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5672584 |
Cyclic prodrugs of peptides and peptide nucleic acids having improved metabolic stability and cell membrane permeability
Provided are cyclic prodrugs of biologically active peptides and peptide nucleic acids exhibiting improved cell membrane permeability and enzymatic stability, containing...
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5643879 |
Amino-substituted heterocycles as renin inhibitors
The invention concerns novel renin-inhibitory compounds which contain an amino-substituted heterocycle at the P2 position. These are useful for treating renin-associated hypertension, congestive...
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5523289 |
Pharmaceutical composition
A pharmaceutical tablet composition comprising a compound of the formula (II): ##STR1## wherein R1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-1-oxo-4-piperazinyl, 2-oxo-4-piperazinyl,...
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5468732 |
Phosphorus containing renin inhibitors
Phosphorus containing polypeptides as renin inhibitors, useful as antihypertensive agents.
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5459131 |
Renin inhibitors
Renin inhibiting compounds of the formula: ##STR1## wherein A is a moiety selected from those of the formula: ##STR2## where Z is O, S, SO, or SO2, P is 1 or 2 and X is --O-- or --S--; and analogs...
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5445832 |
Process for the preparation of microspheres made of a biodegradable polymeric material
The process is aimed at providing a composition designed for the sustained and controlled release of medicamentous peptide substances, obtained in the form of microspheres of a biodegradable...
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5401722 |
Peptide analogues
New peptide analogues of the formula I R1 --Z--NR2 --CHR3 --CR4 --(CH2)o --(CR5)t --(CH2)v --CE--Cw H2w --R6 Iin which R1 to R6 Z, E, o, t and w have the meanings described herein, and the salts...
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5389616 |
Amino acid derivatives
The compounds of the formula ##STR1## wherein A, R1, R2, R3, R4, R5 and R6 are as set forth above, are described.The compounds of formula I have an inhibitory activity on the natural enzyme renin...
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5378690 |
New renin-inhibitory oligopeptides, their preparation and their use
Oligopeptides of formula (I): ##STR1## where R1 -R5 are various organic groups, and A represents a group of formula --NH-- or --(CH2)n --, in which n represents an integer of from 1 to 3, have...
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5378689 |
Peptides having renin inhibitory activity, their preparation and use
Compounds of formula (I): ##STR1## [in which: R1 is heterocyclic group having 5 or 6 ring atoms, or --NR7 R8, where R7 is alkyl and R8 is optionally substituted phenyl, optionally substituted...
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5378691 |
Amino acid derivatives
New amino acid derivatives of the formula I R1 --Cp H2p --(NH)y --CO--NH--CHR2 --CO--Z--Cm H2m --CO--NH--CHR3 --CR4 --(CHR5)n --CO--E--Q--Y Iin which R1 to R5, p, y, Z, m, n, E, Q and Y have the...
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5376638 |
Methods for treating renin-related disorders with amylin antagonists
Methods for treating conditions associated with elevated, inappropriate or undesired renin activity are disclosed which comprise administration of an effective amount of any amylin antagonist alone...
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5360791 |
Renin-inhibiting aminodiol derivatives
The invention relates to compounds of the formula I ##STR1## in which A denotes a radical of the formula II ##STR2## in which E denotes a CH2 group or an NR9 radical, G denotes a radical from the...
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5350741 |
Enteric formulations of physiologically active peptides and proteins
An enteric formulation for a proteinous drug which protects it from enzymatic degradation and promotes its uptake by the intestinal tract when administered orally, comprises either a solid mass of...
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5346887 |
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##...
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5332742 |
Renin inhibitors
A renin inhibiting compound of the formula: ##STR1## wherein R1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-l-oxo-4-piperazinyl, 2-oxo-4-piperazinyl, 4-morpholinyl, 4-thiomorpholinyl or...
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5328916 |
Heterocyclic compounds useful for inhibition of renin
New heterocyclic compounds of the formula X--W--CR1 R2 --CO--Y--NR3 --CHR4 --CR5 --CH2 --(CR6 R7)r --Z--Het Iin which R1 to R7, W, X, Y, Z, r and Het have the meanings defined herein, and the salts...
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5283250 |
Quinolinyl/quinolinylalkyl-N-terminal amino hydroxy
Non-peptidyl compounds characterized generally as quinolinyl/quinolinylalkyl-N-terminal amino hydroxy β-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. ...
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5278148 |
Amino acid derivatives useful for treating high blood pressure
Compounds of the formula ##STR1## wherein R1 is hydrogen or methyl, R2 is ethyl, propyl, isopropyl, imidazol-2-yl, imidazol-4-yl, pyrazol-3-yl, thiazol-4-yl, thien-2-yl, ethoxycarbonyl,...
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5260278 |
Diol-containing renin inhibitors
The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, and diseases caused by retroviruses...
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5258362 |
Renin inhibiting compounds
A renin inhibiting compound of the formula: ##STR1## wherein R0 is a mimic of the Phe-His dipeptide sequence of angiotensinogen which preceeds the renin cleavage site; R4 is loweralkyl,...
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5246959 |
Poly(aminoalkyl)aminocarbonyl aminoacyl aminodiol amino acid derivatives as anti-hypertensive agents
Non-peptidyl compounds characterized generally as poly(aminoalkyl)aminocarbonyl aminoacyl aminodiol derivatives of amino acids are useful as renin inhibitors for the treatment of hypertension....
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5229369 |
Aminoalkylaminocarbonyl aminodiol amino acid derivatives as anti-hypertensive agents
Non-peptidyl compounds characterized generally as aminoalkylaminocarbonyl aminodiol derivatives of amino acids are useful as renin inhibitors for the treatment of hypertension. Compounds of...
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5221667 |
Renin inhibiting peptides having an α-heteroatom amino acid at the P3 position
The invention concerns novel renin-inhibitory compounds which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, glaucoma, and diseases caused by...
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5219851 |
Tetrahydroisoquinoline-type renin inhibiting peptides
The invention concerns novel renin-inhibitory compounds which contain a tetrahydroisoquinoline or similar heterocycle at the P3 position. These are useful for treating hypertension, congestive...
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5217958 |
1,2-hydroxy phosphonates and derivatives thereof
Compounds of the formula ##STR1## are disclosed. These compounds are inhibitors of renin and therefore useful as cardiovascular agents.
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5215966 |
Peptide and renin inhibitors
Novel amino acid derivatives of the formula I X--Z--NH--CHR1 --CO--NR2 --CHR3 --CR4 --(CHR5)n --CO--E--W'--Ywherein X, Z, R1, R2, R3, R4, R5, E, W', Y and n have the meanings defined herein and...
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5215967 |
Aminoacid derivatives inhibiting renin
New amino acid derivatives of the formula R1 --Z--NR2 --CHR3 --CR4 --(CHR5)a --CO--E--Q--Ywherein R1 to R5, a, Z, E, Q and Y have the meanings defined herein, and salts thereof inhibit the activity...
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5198426 |
Renin inhibitors containing C-terminal dihydroxy amides
The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, glaucoma and diseases caused by...
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5180744 |
Aralkyl-N-terminal amino hydroxy
Non-peptidyl compounds characterized generally as aralkyl-N-terminal amino hydroxy β-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular ...
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5180725 |
Quinoxalinyl/quinoxaliy; alkyl-N-terminal amino hydroxy
Non-peptidyl compounds characterized generally as quinoxalinyl/qunioxalinylalkyl-N-terminal amino hydroxy β-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. ...
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5179102 |
Naphthyridinyl/naphthyridinylalkyl-n-terminal anino hydroxy β-amino acid derivatives
Non-peptidyl compounds characterized generally as naphthyridinyl/naphthyridinylalkyl-N-terminal amino hydroxy β-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. ...
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5178877 |
Encapsulated renin inhibitor composition
A pharmaceutical composition comprising a solution of a tenin inhibitor of the formula: ##STR1## wherein R1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-1-oxo-4-piperazinyl,...
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5175181 |
Imidazolyl/imidazolylalkyl-N-terminal amino hydroxy
Non-peptidyl compounds characterized generally as imidazolyl/imidazolylalkyl-N-terminal amino hydroxy β-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. ...
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5175170 |
β-amino acid derivatives
Non-peptidyl compounds characterized generally as cycloalkyl/cycloalkylkyl-N-terminal amino hydroxy β-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds ...
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