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5622934 |
Peptides with an insulin-like action
Peptides with an insulin-like action, of formula I: ##STR1## in which G is a hydrogen atom, an amino add residue, or a monosubstituted or polysubstituted amino acid; D is an amino acid residue, a...
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5618793 |
Nikkomycin analogs
Compounds of the formula ##STR1## wherein R 3 , R 4 , J, K, Z, and Het are as set forth herein are described. The compounds of formula I are useful as agents in the treatment of fungal infections.
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5616612 |
Urethanes and ureas that enhance the growth of bone marrow progenitor cells
The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or...
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5616606 |
Oligopeptide antiretroviral agents
Oligopeptide antiretroviral agents are represented by formula (I), wherein A is a moiety bearing a positive charge and of a size which avoids steric inhibition of binding of said compound to...
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5614498 |
Endothelin antagonistic substance
Peptides having the formula: ##STR1## inhibit the binding of endothelin to its ET B receptor and are useful in treating diseases associated with excess production or secretion of endothelin.
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5614535 |
Adhesion receptor antagonists
Compounds of the formula I ##STR1## in which R 1 and X have the meanings herein defined, their physiologically unobjectionable salts and/or solvates inhibit the binding of fibrinogen to the...
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5614499 |
Peptide derivatives as thrombin inhibitors
The invention relates to new competitive inhibitors of thrombin, pharmaceutical compositions containing the compounds as active ingredients, and the use of the compounds as anticoagulants for...
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5610144 |
Pyrrolidine and thiazolidine derivatives, their preparation and medicaments containing them
This invention relates to compositions of formula: ##STR1## and their salts, their preparation and the medicaments containing them.
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5610146 |
2,3-disubstituted isoxazolidines, a process for their preparation, agents containing them, and their use
The invention relates to compounds of the formula ##STR1## in which A denotes an optionally substituted radical from the series comprising alkyl, acyl, cycloalkyl, aryl and heteroaryl; A 1 ...
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5602102 |
Dipeptidyl peptidase-I inhibitors and uses thereof
Therapeutic agents and methods for the treatment of immunologically mediated diseases and malignancies of myeloid cell or lymphoid cell origin. These particular methods utilize the characterization...
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5601801 |
Radiolabelled angiotensin converting enzyme inhibitors
Angiotensin convening enzyme (ACE) inhibitors can be labelled with Iodine-123, Iodine-125, Iodine-127 or Iodine-131, useful to image the kidneys and lungs for diagnosis and treatment of diseases...
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5599793 |
Antithromobotic agents
This invention relates to L-arginine aldehyde derivatives, having the Formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing...
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5597805 |
Peritoneal dialysis solutions
Peritoneal dialysis solutions are specially formulated for use during and immediately after an episode of peritonitis. The solutions include one or more additives to minimize the injury and...
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5593976 |
New ureido derivatives of poly-4-amino-2-carboxy-1-methyl compounds
The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur; each of the B...
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5591758 |
Organic nitrates, processes for their preparation and their use in the treatment of cardiovascular diseases
Organic nitrates, processes for their preparation and their use in the treatment of vascular diseases and in particular in the treatment of angina. The said nitrates correspond to the following...
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5585360 |
Peptide compounds derived from boronic acid
The invention relates to the compounds of formula (I): ##STR1## in which: R 1 denotes hydrogen, acyl, alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl or linear or branched C 1 -C 6 alkyl,...
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5585359 |
Inhibitors of farnesyl-protein transferase
The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX...
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5585357 |
Heteroaryloxymethyl ketones as interleukin-1βconverting enzyme inhibitors
Compounds which inhibit interleukin-1β protease activity, pharmaceutical compositions containing the compounds and methods using the compounds are provided. The compounds have the formula ##STR1##...
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5585358 |
Derivatives of valproic acid amides and 2-valproenoic acid amides, method of making and use thereof as anticonvulsant agents
A compound having the structure: ##STR1## wherein R 1 , R 2 , and R 3 are independently the same or different and are hydrogen, a C 1 -C 6 alkyl group, an aralkyl group, or an aryl group, and n...
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5583101 |
Use of nitrogen oxide species and adducts to inhibit skeletal muscle contraction
A method for inhibiting or relaxing skeletal muscle contractions which comprises contacting said skeletal muscle with a skeletal muscle relaxing amount, and a method for the treatment of disease...
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5580896 |
Treatment of pain and colorectal cancer with dipeptoids of α-substituted Trp-Phe derivatives
This invention relates to the treatment of pain and inhibiting the growth of colorectal cancer with dipeptoids of α-substituted Trp-Phe derivatives.
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5578574 |
Antithrombotic agents
This invention relates to L-arginine aldehyde derivatives, having the formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing...
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5578593 |
Spiro piperidines and homologs promote release of growth hormone
There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote...
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5574016 |
Peptide compound and a process for the preparation thereof
The present invention concerns glycoprotein IIa/IIIb antagonists and platelet aggregation inhibitors of the formula (I): ##STR1## wherein R 1 is aryl which may have one or more suitable...
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5574017 |
Antibacterial agents
The present invention provides methods and pharmaceutical preparations for inhibiting the growth of bacterial microorganisms.
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5571793 |
Endoparasiticidal compositions based on open-chain tetradepsipeptides
The present invention relates to the use of open-chain tetradepsipepties of the formula ##STR1## in a method for combatting endoparasites in humans and animals.
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5571792 |
Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase
Novel inhibitors of protein farnesyltransferase enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in controlling tissue...
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5565430 |
Azaaspartic acid analogs as interleukin-1β converting enzyme inhibitors
Disclosed are compounds, compositions and methods for inhibiting interleukinprotease activity. The compounds, α-substituted acetamides a ##STR1## wherein: R 2 =H or alkyl; R 3 =halo, O(CO) 0...
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5562921 |
Stable solid pharmaceutical compositions containing enalapril maleate
Enalapril maleate is unstable when associated with many excipients commonly used in the manufacture of pharmaceutical compositions. Stable solid compositions are provided by mixing enalapril...
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5561112 |
Pseudopeptide isosteres of gly-asp and their use as antithrombic agents
Pseudopeptides of formula I in free or salt form ##STR1## wherein A, B, R 1 , X, Y and m are defined as in claim 1, and their use in the prophylactic and acute treatment of thrombosis.
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5561133 |
Thymidylate synthase inhibiting quinazolinones
Quinazolines of the formula ##STR1## wherein R 1 is typically methyl, hydrogen or amino; R 2 is typically methyl or propargyl; Ar is typically phenylene or 2'-fluorophenylene; R 3 is the residue...
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5561111 |
Stable glutamine derivatives for oral and intravenous rehydration and nutrition therapy
A method for the treatment of dehydration or nitrogen deficiency-based malnutrition is provided which involves administering to a patient in need thereof an effective amount of a compound selected...
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5561113 |
New pseudopeptide compounds of neurokinins
A compound of formula (I): ##STR1## in which: R represents naphthyl, 5,6,7,8-tetrahydronaphthyl, 1,2,3,4-tetrahydronaphthyl, thienyl, optionally substituted phenyl or (C 3 -C 7 )cycloalkyl, n...
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5561146 |
Modified guanidino and amidino thrombin inhibitors
Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; and R 1 is cyano, hydroxyl,...
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5559092 |
Cosmetic composition
A composition suitable for topical application to mammalian skin and hair for inducing, maintaining or increasing hair growth comprises a hair growth promoter chosen from glutamine derivatives and...
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5554594 |
Imidazolidine derivatives
The present invention relates to compounds of the general formula I ##STR1## in which R, R 1 to R 4 , r, Y, Z and W are defined as indicated in the description, a process for their preparation and...
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5550110 |
Endothelin Antagonists II
Novel antagonists of endothelin are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute...
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5543396 |
Proline phosphonate derivatives
Peptidyl derivatives of diesters of α-aminoalkylphosphonic acids, particularly those with proline or related structures, their use in inhibiting serine proteases with chymotrypsin-like,...
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5543397 |
New N-acyl dipeptides and their use
Novel N-acyl depeptides of the formula: R 2 --NH--CHR 1 --CO--AS in which AS, R 1 and R 2 have certain, more precisely defined meanings. These N-acyl dipeptides are more stable under...
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5541163 |
Renin inhibiting N-(2-amino-2-oxoethyl)butanediamide derivatives
Disclosed herein are compounds of the formula: A--N(R 1 )C(O)CH 2 CHR 2 C(O)--B wherein A is R 3 R 4 NC(O)CH 2 wherein, for example, R 3 is hydrogen or alkyl and R 4 is hydrogen, alkyl or...
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5538950 |
Endothelin antagonists and their preparation
A compound of the formula: ##STR1## in which R 3 is hydrogen or lower alkyl, R 4 is pyridyl (lower) alkyl; and R 1 , R 2 , R 5 and A are defined in the description; or a pharmaceutically...
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5536724 |
Antiinflammatory and antineoplastic 5-deazaaminopterins and 5,10-dideazaaminopterins
Antiinflammatory and antineoplastic 5-deazaaminopterins and 5,10-dideazaaminopterins and their 5 and 10 alkyl analogs. A method for the treatment and prevention of inflammatory disease, such as...
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5534538 |
N-acyl dipeptides and their compositions
Novel a-acyl dipeptides of the formula: R 2 --NH--CHR 1 --O--AS in which AS, R 1 and R 2 have certain, more precisely defined meanings. These N-acyl dipeptides are more stable under...
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5534492 |
Muramyl peptide for the treatment of toxicity
Muramyl peptide compounds are useful in the treatment of toxicity, particularly when this condition results from alcohol, hypnotics or sedatives, anaesthetics, opioids or drug abuse generally. The...
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5534496 |
Methods and compositions to enhance epithelial drug transport
Methods and compositions provided for enhancing the transport of drugs (including peptides, oligonucleotides, proteins and conventional drugs) across epithelial cells at mucosal sites. The methods...
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5523313 |
Indole-containing peptide and process for preparing the same
There is disclosed an indole-containing peptide represented by the formula (I): ##STR1## wherein R represents hydrogen atom, a lower alkyl group or formyl group; and X represents oxygen atom or...
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5523289 |
Pharmaceutical composition
A pharmaceutical tablet composition comprising a compound of the formula (II): ##STR1## wherein R 1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-1-oxo-4-piperazinyl, 2-oxo-4-piperazinyl,...
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5519005 |
Method of inhibition of cellular and molecular level biological interactions utilizing non-peptidic surrogates of the Arg-Gly-Asp sequence
A method of inhibition of cellular and molecular level biological interactions which are dependent on RGD interactions is disclosed. The method comprises administering a compound of the formula I ...
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5518735 |
Meta-substituted phenylalanine derivatives
D,L-, L- and D-phenyl alanine derivatives of formula (I) defined in claim 1 in which R 1 is an amidino-, guanidino-, oxamidino-, aminomethyl- or amino group have been discovered which effectively...
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5514670 |
Submicron emulsions for delivery of peptides
The present invention provides emulsions comprising a plurality of submicron particles, a bioactive peptide, and an aqueous continuous phase or that effect enhanced oral bioavailability of the...
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