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5786378 |
Heterocyclic thioesters
This invention relates to neurotrophic low molecular weight, small molecule heterocyclic thioesters and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the...
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5783587 |
Benzoyl Piperidines/pyrrolidines for enhancing synaptic response
Benzoyl piperidines and pyrrolidines and compounds of related structure are disclosed for use in enhancing synaptic responses mediated by AMPA receptors. The compounds are effective in the...
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5776503 |
Amino acid solutions for treatment of peritoneal dialysis patients
The present invention provides a dialysis solution that contains amino acids for treating and/or preventing malnutrition in a peritoneal dialysis patient. The amino acid composition is optimized to...
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5776927 |
Methionine sulfone and S-substituted cysteine sulfone derivatives as enzyme inhibitors
This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The...
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5773263 |
Production aflastatin A from streptomyces sp., a pharmaceutical composition and methods of use
The antibiotic aflastatin A or its salt and its production by Streptomyces sp. MRI 142, FERM BP-5841 is presented. Aflastatin A is incorporated into a pharmaceutical composition and is employed as...
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5773434 |
Facilitation of AMPA receptor-mediated synaptic transmission in brain as a treatment for schizophrenia
Psychotic symptoms are treated by the administration of drugs which amplify the ability of natural stimulators of AMPA receptors to enhance the mediation of excitatory synaptic response. What is...
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5753691 |
Agents for inhibiting the production of IL-1β and the release of TNFα
The pharmaceutical use of 1-cinnamoyl-2-pyrrolidinone derivatives having the activities to inhibit the production of IL-1β and the release of TNFα. Those derivatives are useful in the treatment...
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5747522 |
Amino acid derivatives
N-Acyl-α-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R"' and Q have the significance given in the description, can be used for the treatment or prophylaxis of...
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5744487 |
Prolineamide derivatives
A prolineamide derivative represented by the formula (I): ##STR1## or a salt or hydrate thereof or a pharmaceutically acceptable salt thereof, which has a protease inhibition activity and is useful...
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5741799 |
Heterocyclic thrombin inhibitors
Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R 1 , R 2 , R 3 , G, G x , R 6 ', Ra, Xa, R 6 , Rb, R 3 , p, Q, A and R 4 are as defined herein.
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5739155 |
Haloalkylthio,-sulfinyl and -sulfonyl arylpyrrole insecticidal and acaricidal agents
Haloalkylthio, -sulfinyl and -sulfonyl arylpyrrole compounds which are effective for the control of insects and acarids are described. A method for the insecticidal and acaricidal use of said...
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5736565 |
Therapeutic compounds suitable for the treatment of diseases connected with glutathione deficiency, process for their preparation, and pharmaceutical compositions containing same
The present invention is referred to sulphur-acylated derivatives of L-pyroglutamyl-L-cysteine of formula (I) ##STR1## where R is a linear or branched alkyl containing 1 to 6 carbon atoms, their...
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5733539 |
Bait for fishes and shellfishes
The invention discloses a bait for fishes and shellfishes characterized in that the bait comprises a matrix material containing a microorganically fermented product of a plant residue obtained by...
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5731335 |
(1-Heteroazolyl-1-heterocycane derivatives and their use as neuroprotective agents
This invention provides heterocyclic compounds of formula (I) that are potentially useful in the treatment of neuropsychiatric disorders associated with progressive processes leading to neuronal...
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5728402 |
Controlled release formulation of captopril or a prodrug of captopril
The invention provides a controlled release pharmaceutical unit dose composition for oral administration which comprises: (a) an internal phase which comprises captopril or a prodrug of captopril...
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5716926 |
Composition of pyruvate and protein and method for increasing protein concentration in a mammal
The present invention is based in part upon the discovery that the use of pyruvate in enteral formulations, in combination with an anabolic protein composition, produces a synergistic effect in...
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5714142 |
Method and compositions for increasing the serum half-life of pharmacologically active agents by binding to transthyretin-selective ligands
Compositions and methods are provided for increasing the serum half-life of a pharmacologically active agent. The novel compositions are covalent conjugates of the selected pharmacologically active...
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5714518 |
HIV protease inhibitors and methods of making the same
HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well...
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5714510 |
Topical proxyl composition and method
A composition and method for ameliorating a cellular dysfunction of a tissue such as the cosmetic treatment of hair loss and stimulation of hair growth is disclosed. The method comprises...
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5714482 |
Topical spin labels and method
A composition and method for ameliorating a cellular dysfunction of a tissue such as the cosmetic treatment of hair loss and stimulation of hair growth are disclosed. The method comprises...
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5712269 |
M.sub.2 receptor ligand for the treatment of neurological disorders
Muscarinic M 2 receptor ligands are described which are suitable for the treatment of neurological disorders, and which may be administered with minimal side-effects. A method of synthesis of...
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5712273 |
Amino acid derivatives, processes for the manufacture thereof and pharmaceutical compositions (II) containing these compounds
The invention relates to new amino acid derivatives of general formula I R 1 -R 11 --A 1 --B (I) and the pharmaceutically acceptable salts thereof, wherein group B...
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5705522 |
Compounds having anti-inflammatory and anti-viral activity, compositions of these, alone and in combination with reverse transcriptase inhibitors
A new family of compounds having anti-inflammatory, anti-viral, and brocho-dilating activity having the following linear and cyclic formulas: ##STR1## and compositions of these, which alone, and in...
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5703104 |
Cyclic amides and derivatives thereof
Compounds, topical compositions and methods useful for preventing the penetration of toxic chemicals through the skin of a mammal are disclosed. The compounds of the invention provide an enhanced...
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5693630 |
Phenylethyl and phenylpropylamines
Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain, m is 2 or 3, R 1 is a hydrogen atom, or a...
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5691356 |
Disubstituted heterocyclic thrombin inhibitors
Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q...
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5686469 |
Aminomethylene derivaties as immunosuppressants
Compounds which suppress human T-lymphocyte proliferation are disclosed. The active compounds essentially contain at least the following structure: ##STR1##
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5686451 |
Combination of an ace inhibitor and a diuretic
Pharmaceutical formulations comprising as active ingredients an angiotensin converting enzyme (ACE) inhibitor at a dose level normally found effective as an antihypertensive and a diuretic at a...
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5674906 |
Stilbene compounds and pharmaceutical compositions containing them
Stilbene compounds of the following formula (I) or their pharmaceutically acceptable salts are effective as carcinostatics and of low toxicity: ##STR1## wherein X represents a hydrogen atom or a...
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5674864 |
N-substituted derivatives of α-mercapto alkylamines, their preparation process and the intermediates obtained, their use as medicaments and the compositions containing them
Novel α-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein the substituents are as defined in the specification.
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5672621 |
Carbonarin antiinsectan metabolites
Carbonarins A, B, C, D, E, F, G, and H have been isolated from the sclerotia of the fungus Aspergillus carbonarius. The carbonarius are effective for controlling Coleopteran and Lepidopteran...
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5667792 |
Derivatives of 2,5-dihydroxyphenylcarboxylic acids, and their utilization in cosmetic or dermatological compositions with a depigmenting action
A cosmetic or dermatological composition with a depigmenting action comprises derivatives of 2,5-dihydroxyphenylcarboxylic acids, their homologs, and their salts, with the derivatives having the...
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5665754 |
Substituted pyrrolidines
Novel pyrrolidine compounds which are useful for inhibiting the function of Type IV phosphodiesterase (PDE-IV) as well as methods for making the same are disclosed. Applications in treating...
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5665756 |
Aminoalkyloximes useful in the treatment of depression and obsessive compulsive disorders
Novel aminoalkyloximes of the formula ##STR1## wherein: a. X is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, or a group of the formula ##STR2## wherein Y is hydrogen or loweralkyl,...
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5663188 |
Synergistic therapeutic compositions of angiotensin I converting enzyme inhibitors and angiotensin II antagonists and methods
This invention relates to compositions and methods for achieving a therapeutic effect such as lowering blood pressure and treating congestive heart failure in a mammal. More specifically, this...
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5663174 |
Aromatic sulfonamide derivatives, their use as enzyme inhibitors and pharmaceutical compositions containing them
Aromatic sulfonamide derivatives, particularly benzenesulfonamide, 4-fluorobenzenesulfonamide, 5-chloro-1-naphthalenesulfonamide and 5-isoquinolinesulfonamide derivatives are provided that inhibit...
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5661122 |
Treatment of congestive heart failure
Methods of enhancing myocardial contractility and cardiac performance in a mammal with congestive heart failure are disclosed. In a first method a mammal with congestive heart failure is treated by...
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5661166 |
Saishin N compounds, process for preparing same and antiulcer agents containing same
A Saishin N derivative represented by the following general formula: ##STR1## wherein X represents a carbonyl group or a >CH--ORx group, or X bonds to a carbon atom in Y or Z to represent a...
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5658936 |
Enhancement of erectile function with renin-angiotensin system inhibitors
A method for treating patients having erectile dysfunction is described. The method involves treating patients with a renin-angiotensin system inhibitor. A method for treating a subject to improve...
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5648393 |
Treatment of male impotence with s-nitrosylated compounds
Methods of relaxing corpus cavernosum smooth muscle, treating disease states responsive to prevention or relaxation of undesirable contractions of corpus cavernosum smooth muscle and of treating...
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5643960 |
Method of delaying onset of alzheimer's disease symptoms
The present invention relates, in general, to a method of preventing or delaying the onset of Alzheimer's disease and related neurodegenerative disorders. The method involves the administration to...
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5639768 |
Substituted amidino compounds, their manufacture and methods of treatment
The invention relates to the compounds of formula (I) wherein the C(NH)--NHR 3 group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which: R 1 is...
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5637600 |
Phenylpyrrole derivatives and their use as dopamine D.sub.3 antagonists
The present invention relates to pyrrole compounds, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, in particular as anti-psychotic agents.
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5633277 |
Sulfonamide aminomethylene derivatives as immunosuppressants
Compounds which suppress human T-lymphocyte proliferation are disclosed. The active compounds essentially contain at least the following structure: ##STR1##
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5624939 |
N-acyl pyrrolidines and drugs for the treatment or prevention of cholecystokinin and gastrin-related disorders
Compounds of formula I ##STR1## wherein the substituents are as defined herein, are disclosed as treatments for disorders linked to CCK and gastrin. Processes for preparing the compounds are also...
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5622985 |
Method for preventing a second heart attack employing an HMG CoA reductase inhibitor
A method is provided for preventing or reducing the risk of a second heart attack in a patient having a substantially normal serum cholesterol level by administering an HMG CoA reductase inhibitor...
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5622984 |
Amidinophenol derivatives
Amidinophenol derivatives of the formula (I): ##STR1## wherein R 1 and R 2 are (i) H, (ii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO 2 , (vii) benzoyl, (viii) COOR 4 (in which R 4 is...
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5621005 |
Aqueous pharmaceutical suspension for substantially water insoluble pharmaceutical actives
The present invention relates to an aqueous pharmaceutical suspension composition comprising: from about 0.2% to 20% of a substantially water insoluble pharmaceutical active, e.g. ibuprofen; a...
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5621000 |
Nitric esters having a pharmacological activity and process for their preparation
Nitric esters with pharmacological activity having general formula (I), their pharmaceutical utilisation and process for their preparation. ##STR1##
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5612061 |
Composition and method for the treatment of premenstrual syndrome
A composition for the treatment of premenstrual syndrome comprising an effective amount of calcium, magnesium, an analgesic and a diuretic sufficient to reduce the symptoms of premenstrual syndrome.
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