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5288743 |
Indole carboxylate derivatives which inhibit leukotriene biosynthesis
Compounds of the structure ##STR1## where A is straight or branched divalent alkylene or divalent cycloalkylene, R 1 is selected from hydrogen; alkylthio; optionally substituted phenylthio;...
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5286739 |
Parenteral formulations for the inhibition of systemic hypotension associated with nitric oxide production or endothelial derived relaxing factor
An anti-hypotensive formulation comprising an essentially arginine-free or low arginine (less than about 0.1%, most preferably, about 0.01%) containing mixture of amino acids is provided. The...
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5284862 |
Derivatives of 2-carboxyindoles having pharmaceutical activity
The present invention relates to novel 3-substituted-2-carboxyindoles; including as 3-substituents amides of hydroxamic acids and derivatives thereof or urea and carbonyl, carboxyl or phosphonic...
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5270326 |
Treatment for tissue ulceration
Compounds of the formulas ##STR1## wherein R 1 is H and R 2 is alkyl (3-8C) or wherein R 1 and R 2 taken together are --(CH 2 ) n -- wherein n=3-5; R 3 is H or alkyl (1-4C); R 4 is a...
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5268385 |
Method for treating schizophrenia
This invention provides a method for treating the symptoms of schizophrenia by interacting selectively with presynaptic dopaminergic D 2 receptors without appreciably activating postsynaptic...
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5266572 |
Antipsychotic 1-cycloalkylpiperidines
There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma...
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5258398 |
Antithrombotic diaminoalkanoic acid derivatives
This invention relates to novel diaminoalkanoic acid derivatives that inhibit platelet aggregation and thrombus formation in mammalian blood thereby being useful in the prevention and treatment of...
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5256687 |
Pharmaceutical composition for the treatment of high blood pressure
The invention relates to a pharmaceutical composition comprising an angiotensin converting enzyme inhibitor (trandolpril or pamipril) and a loop diuretic (Furosemide or piretanide), and to their...
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5256657 |
Succinamide derivative matrix-metalloprotease inhibitors
Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH 2 R 1 has the R-configuration, the carbon atom bearing CH 2 R 2 has...
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5250565 |
Indole-,benzofuran-,and benzothiophene-containing lipoxygenase-inhibiting compounds
Pro-drugs of potent 5-lipoxygenase inhibiting compounds comprise compounds of the formula ##STR1## in which A is an alkylene or alkenylene group, X is oxygen, sulfur, sulfoxyl, or substituted...
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5248688 |
Method and substrate composition for treating atherosclerosis
A method and substrate composition for treating atherosclerosis are provided. The method involves parenterally administering the substrate composition as an aqueous solution to substantially lower...
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5244915 |
Amico acid derivatives cyclized at the C-terminal
Novel α-substituted Trp dipeptoid derivatives cyclized at the C-terminal useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, or as...
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5229413 |
Compositions containing indole-2-carboxylate compounds for treatment of CNS disorders
Compositions containing certain indole-2-carboxylate compounds and derivatives are described as being therapeutically effective in treatment of CNS disorders resulting from neurotoxic damage or...
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5227397 |
Polyamines and polypeptides useful as antagonists of excitatory amino acid neuro-transmitters and/or as blockers of calcium channels
This invention relates to certain polyamines and polypeptides found to be present in the venom of the Agelenopsis aperta spider. The polyamines of this invention and the salts thereof antagonize...
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5223529 |
N-phenylamides and medicinal products containing them
Compounds of formula: ##STR1## in which R 1 is (a) a phenyl radical or a substituted phenyl radical, (b) a chain --CH(R 8 )--COOR 4 , (c) a chain --CH 2 --CO--NR 5 R 6 or (d) a phenylalkyl...
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5217988 |
Indolyl indolylakyl-N-terminal cycloalkoxy-C-terminal amino hydroxyβ-amino acid derivatives
Non-peptidyl compounds characterized generally as indolyl/indolylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy β-amino acid derivatives are useful as renin inhibitors for treatment of...
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5218123 |
Didehydrotryptophan derivatives and pharmaceutical use thereof
Novel didehydrotryptophan derivatives useful as agents in the reduction of gastric acid secretion and in the treatment of anxiety, psychoses, and the symptoms of cognitive decline are disclosed....
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5216019 |
Pain killer
The invention relates to the use of L-tryptophane and a peripheral degradation inhibitor for L-tryptophan for the preparation of an analgesic drug for humans, the ratio by weight of L-tryptophan to...
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5214063 |
4-aminobutyric acid compounds, compositions and methods of use for treating disorders related to a dysfunction of GABA.sub.B receptors
A compound of formula (I): ##STR1## in which R, R 1 and R 2 are as defined in the description. Medicinal product, which is useful in treating disorders related to a dysfunction of GABA B receptors.
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5196435 |
Melatonin derivatives and combinations with antiestrogen compounds for treating mammalian breast carcinoma
Derivatives of melatonin and the pharmaceutically acceptable salts thereof are useful for therapeutically treating hormonally dependent mammalian breast carcinoma. Combination treatments of...
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5192798 |
Lipophilic polyamines useful for treating hypercholesterolemia
This invention relates to novel lipophilic polyamines of formula I, the method of using these compounds to treat hypercholesterolemia, and intermediates thereto. Z 1 --(CH 2 ) n --Y 1 --X 1 ...
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5192753 |
Anti-rheumatoid arthritic drugs in the treatment of dementia
This invention pertains to the novel use of anti-rheumatoid arthritic drugs in the treatment of dementia. A method of treating dementia in human beings which comprises administering to the human...
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5190968 |
(Polycyclic-arylmethoxy) indoles as inhibitors of leukotriene biosynthesis
Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They...
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5189054 |
3-amidoindolyl derivatives and pharmaceutical compositions thereof
The present invention is directed to a new class of 3-amido and 3-sulfamido-indolyl NMDA antagonists and their use in the treatment of a number of disease states.
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5189025 |
Methods for the treatment of malignant disease in patients using citrulline containing amino acid solutions
Disclosed are total parenteral nutrition formulations which include essential amino acids in combination with either arginine or ornithine, for use in the detection of recurrent malignant disease...
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5187187 |
Irreversible ligands for nonsteroidal antiinflammatory drug and prostaglandin binding sites
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5185157 |
Treatment of refractory Eosinophilia-Myalgia Syndrome with L-tryptophan composition
A method of treating a human patient with refractory Eosinophilia Myalgia Syndrome via oral administration of an effective dosage range of from 1000 mg. to 3000 mg. of a pharmaceutical composition,...
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5180729 |
Use of sigma receptor antagonists for treatment of cocaine abuse
The invention relates to a method of treating cocaine abuse or addiction in a mammal which comprises administering to the mammal an effective amount of a sigma receptor antagonist lacking or having...
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5162341 |
Use of sigma receptor antagonists for treatment of amphetamine abuse
The invention relates to a method of treating drug abuse or addiction involving amphetamine or amphetamine-related drugs with pharmacological effects similar to amphetamine in a mammal which...
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5162362 |
Octahydroindole-2-carboxylic acids
What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds;...
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5158969 |
Indole derivatives as potassium channel blockers
A method of treating a disease in a mammal, including a human, responsive to blockade of potassium channels, which comprises administering to a mammal in need thereof an effective amount of a...
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5153226 |
Acat inhibitors for treating hypocholesterolemia
The present invention are novel amino acid amide compounds of the following general formula which inhibit the enzyme acylcoenzyme A:cholesterol acyltransferase: ##STR1## wherein R is phenyl or 1-...
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5151433 |
Stabilized medicinal substances, a process for the preparation thereof, and stable medicinal formulations
Stabilized compounds of the formula I ##STR1## in which R, R 1 , R 2 , R 3 , R 4 and R 5 have the stated meanings, and a process for the preparation thereof, are described. The stabilized...
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5147888 |
N-terminal indolyy indolylalkylaminodiol β-amino acid derivatives
Non-peptidyl compounds characterized generally as heterocyclic acyl aminodiol β-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular...
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5145845 |
Substituted 2-carboxylindoles having pharmaceutical activity
The present invention relates to novel compounds, which are derivatives of ureas, thioureas, carbamates, sulfonylureas, sulfonamides, amides, and thioamides of 2-carboxyindoles as illustrated by...
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5132113 |
Nutritional composition containing essential amino acids
A nutritional composition is disclosed which is based on essential amino acids.
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5128346 |
Derivatives of D-glutamic acid and D-aspartic acid
A compound of the formula: ##STR1## wherein R 1 and R 2 are substituents; R 6 is hydrogen, loweralkyl, cycloalkyl, loweralkenyl, arylalkyl, (substituted aryl)alkyl, or (heterocyclic)alkyl; B is...
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5124324 |
Indole derivatives
Disclosed are compounds of formula I ##STR1## wherein R 1 is a hydrogen atom, a C 1 -C 6 alkyl group, benzyl or an indolyl carbonyl group, R 2 is a saturated or unsaturated 5- or 8-membered...
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5124322 |
Dipeptide collagenase inhibitors
Novel compounds of formula (I), salts, solvates and hydrates thereof: ##STR1## in which: R 1 and R 2 are independently hydrogen; alkyl; alkoxy; halogen; or CF 3 ; R 3 is hydrogen; acyl, such...
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5122537 |
Arylvinylamide derivatives and pharmaceutical use
The invention relates to new arylvinylamide derivatives of formula ##STR1## wherein Y is a bicyclic ring system chosen from (A), (B), (C), (D), and (E); ##STR2## in which m is zero, 1 or 2; R is...
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5118683 |
Esters of 4-hydroxy-1,3-benzenedimethanol and compositions and methods employing such compounds
Compounds of the formula I ##STR1## wherein R 5 represents C 1 to C 6 -alkyl or the group --(CH 2 ) n --Z--(CH 2 ) m --Ar; Z represents O, S or --CH 2 --; n represents an integer of 1...
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5118695 |
1-hydroxyindole fungicides
1-Hydroxyindoles of the following formula are useful in controlling fungi: ##STR1## wherein: R 1 is hydrogen or an electron withdrawing group; R 2 is selected from the group consisting of...
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5116861 |
Nitrosothiol derivatives and their use
Novel nitrosothiol derivatives of the formula: ##STR1## wherein R 1 and R 2 are independently a hydrogen atom or a hydrocarbon residue which may be substituted; R 3 is a hydrogen atom, an acyl...
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5110797 |
Peptide compound and a pharmaceutically acceptable salt thereof
Peptide compounds of formula (I): ##STR1## wherein A is hydrogen or an amino-protecting group; X is a member selected from the group consisting of Gly, Glu, Tyr, Asp, Phe, Ile, Ala, Pro, Leu, Hyp,...
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5109000 |
Thiol carboxylic acid derivatives and their use as collagenase inhibitor
Novel compounds of the formula (I), processes for their preparation and their use as collagenase inhibitors are described: ##STR1## in which R 1 is hydroxy; alkoxy; aryloxy; aralkyloxy; --NR 6 R...
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5106847 |
Excitatory amino acid antagonists, compositions and use
The present invention is directed a new group of indole derivatives that are NMDA antagonists.
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5104639 |
Method for biological testing and/or developing pharmaceuticals for treatment of disorders using electrochromatography
A method for establishing a treatment protocol for correcting an abnormal condition or disease in a living organism is described. The method comprises the steps of analyzing body fluids from normal...
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5096700 |
Halogenated aminohexanoates and aminobutyrates antimicrobial agents
The subject invention involves halogenated amino acid derivatives useful as antimicrobial agents having the structure: ##STR1## wherein --R is hydrogen or 2-aminoethyl; --R' is hydroxy, alkoxy,...
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5093352 |
Antidepressant agents
2-aryl substituted N-acetyl tryptamines are utilized as antidepressant agents.
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5086070 |
4-benzyl-1H-indoles and anti-arrthymic use thereof
Novel 4-benzyl-1H-indoles of the formula ##STR1## in all diastereoisomeric forms and mixtures thereof having antiarhythmic activity.
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