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6121292 |
Methods for reversing multidrug resistance
The present invention provides methods for reversing multidrug resistance in a resistant neoplasm by treating a mammal in need of said treatment with a substituted indole, benzofuran,...
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6114327 |
Anti-viral compounds
The present application provides a series of benzimidazole compounds of formula I: ##STR1## which inhibit the growth of picornaviruses, such as rhinoviruses (bovine and human), enteroviruses such...
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6107329 |
Substituted n-(indole-2-carbonyl)-glycinamides and derivatives as glycogen phosphorylase inhibitors
Compounds of Formula (1) wherein R 6 is carboxy, (C 1 -C 8 )alkoxycarbonyl, benzyloxycarbonyl, C(O)NR 8 R 9 or C(O)R 12 as glucogen phosphorylase inhibitors, pharmaceutical compositions...
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6083944 |
Quinoline-containing α-ketoamide cysteine and serine protease inhibitors
The present invention is directed to quinoline-containing α-ketoamide inhibitors of cysteine and serine proteases are disclosed. Methods for making these compounds, and methods for using the same...
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6083959 |
Quinoline derivatives, processes for their preparation and their use as medicaments
A compound of the formula: ##STR1## wherein R 1 is lower alkyl, R 2 is hydrogen, lower alkyl or a heterocyclic group, R 3 is hydrogen, lower alkyl or halogen, R 4 is lower alkyl or...
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6080859 |
Pyrroloindole derivatives and intermediates in producing the same
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6051572 |
Azetidine, pyrrolidine and piperidine derivatives
A class of azetidine, pyrrolidine and piperidine derivatives, substituted by inter alia a phenylmorpholinyl, phenylpiperidinyl or benzimidazolone moiety, are selective agonists of 5-HT 1 -like...
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6046191 |
Combination
The invention relates to the co-administration of an inhibitor of induced nitric oxide synthase and an inhibitor of cyclooxygenase-2 for the treatment of inflammation and inflammatory disorders.
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6022880 |
Substituted pyridylamino indoles
There are disclosed various compounds of the formula below, ##STR1## where R, R 1 , W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions...
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6013648 |
CB.sub.2 Receptor agonist compounds
The use of human CB 2 receptor-specific agonists of formula (I) or (I') for preparing immunomodulating drugs is disclosed. In formulae (I) and (I'), R 1 is a group selected from --CH 2 CHR 10 ...
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5972937 |
Heterocyclic compounds possessing 5HT.sub.2C receptor antagonist activity
The invention relates to heterocyclic families of compounds having pharmacological activity, in particular possessing 5HT 2C receptor antagonist activity processes for their preparation, to...
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5948791 |
Quinoline derivatives for treating malaria
The invention relates to novel quinoline derivatives and their therapeutic use against malaria.
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5939413 |
Piperazine derivatives
This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation...
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5935954 |
Compounds with improved multi-drug resistance activity
The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical...
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5935953 |
Methods for controlling invertebrate pests using cocaine receptor binding ligands
The invention relates to a method of controlling an invertebrate pest, comprising contacting the pest with a pest-controlling amount of an agent having substantial inhibitory activity toward a...
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5891902 |
Indole derivatives
The present invention relates to indole derivatives represented by formula (I): ##STR1## wherein R 1 and R 2 independently represent hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen,...
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5891875 |
Morpholinyl tachykinin receptor antagonists
This invention provides methods of treating a physiological disorder associated with an excess of tachykinins in a mammal which comprises administering to a mammal in need of said treatment a...
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5869499 |
Benzyloxyquinuclidines as substance P antagonists
A compound of chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein X and Y are each hydrogen, halogen, C 1 -C 6 alkyl, halosubstituted C 1 -C 6 alkyl, C 1 -C 6 ...
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5861412 |
Dihydro-isoquinoline compounds and their use as pharmaceuticals
Compound of general formula I ##STR1## wherein A is a benzo or thieno group; R 1 is (C 4 -6)cycloalkyl, (C 4 -6)cycloalkyl-(C 1 -5)alkyl or ##STR2## R 2 , m, R 3 , R 4 , R and u are defined as...
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5807883 |
2-oxoindoline derivative
Disclosed is a 2-oxoindoline derivative represented by the formula (I): ##STR1## wherein Ring A represents a benzene ring which is substituted in the 5-position or 6-position by a lower alkyl group...
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5789404 |
3-substituted 1-arylindole compounds
3-Substituted 1-arylindole compounds are provided having general formula (I) ##STR1## wherein Ar is an optionally substituted aryl group; X represents a divalent hydrocarbon group, methyleneoxy or...
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5780467 |
Morpholine compounds are prodrugs useful as tachykinin receptor antagonists
Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma, and emesis.
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5776932 |
1,3,5-tribsubstituted indazole derivatives, processes for preparing, and for pharmacological treatment therewith
1,3,5-trisubstituted indazole derivatives of the formula ##STR1## wherein R1 is H, (b) a C 1 -6 straight or branched, substituted or unsubstituted alkyl residue, (c) a C 3 -7 cycloalkyl residue,...
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5753673 |
Quinolinecarboxylic acid derivatives
Quinolinecarboxylic acid derivatives represented by the following formula: ##STR1## wherein C is hydroxymethyl, methoxy, ethoxy or morpholinyl, or pharmaceutically acceptable salts thereof exhibit...
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5747486 |
Thienopyridine or thienopyrimidine derivatives and their use
This invention provides an anti-inflammatory agent, particularly an agent for treating arthritis, and a bone resorption inhibiting agent, containing a thienopyridine or thienopyrimidine derivative...
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5731340 |
Glycinamide derivatives, processes for their preparation and medicines containing them
The present invention relates to compounds of formula: ##STR1## which are agonists of cholecystokinin receptors and pharmaceutical compositions containing them.
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5703075 |
Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones
This invention relates to compounds of Formula I ##STR1## which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of Formula I...
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5696145 |
1-benzyl-1,3-dihydroindol-2-one derivatives, their preparation and the pharmaceutical compositions in which they are present
The present invention relates to 1-benzyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## to their preparation and to the pharmaceutical compositions in which they are present. These...
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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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5691334 |
Pyrrolydenemethyl-derivatives and process for their preparation
New and known 5- (2H-pyrrol-2-ylidene)methyl!-2,2'-bi-1H-pyrrole derivatives, having immunomodulating activity and, represented by the general formula (I) and the pharmaceutically acceptable salts...
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5663167 |
Antipsychotic composition and method of treatment
A method for treating a serious psychotic mental illness includes the step of administering to a patient in need of such treatment a combination of (i) an α 2 -adrenergic receptor antagonist and...
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5658926 |
Carbostyril derivative and platelets aggregation inhibitory agent
The present invention provides a carbostyril derivative represented by the following general formula ##STR1## (wherein A, R and W have the same definitions as given above; and the carbon-to-carbon...
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5654296 |
Condensed heterocyclic compounds, their production and use
The compound ##STR1## wherein ring A represents a benzene ring; Ar represents an aromatic group; R 1 and R 2 independently represent hydrogen, acyl or hydrocarbon group or R 1 and R 2 ...
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5652247 |
Carbostyril derivatives
Novel carbostyril derivatives of the formula: ##STR1## wherein R 1 is H, NO 2 , alkoxy, alkoxycarbonyl, alkyl, halogen, optionally substituted amino, OH, CN, COOH, alkanoyloxy, hydrazinocarbonyl;...
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5631281 |
N-substituted cycloalkyl and polycycloalkyl α-substituted Trp-Phe- and phenethylamine derivatives
Novel unnatural dipeptoids of α-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, colorectal...
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5614518 |
Morpholine derivatives as dopamine receptor subtype ligands
A class of substituted morpholine derivatives of formula ##STR1## wherein Y represents an optionally substituted bicyclic heteroaromatic ring system containing one or two nitrogen atoms, the ring...
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5612362 |
Imidazolinone derivatives as tachykinin receptor antagonists
Compounds of formula (I) and salts and prodrugs wherein Q 1 is a specified aryl group, the dotted line is an optional double bond, Z is O or NR 3 , R 1 and R 3 are H or specified optionally...
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5612336 |
Heterocyclic amide derivatives as tachykinin antagonists
Compounds of formula (I), and salts and prodrugs thereof, wherein Q 1 is phenyl substituted by one or more halo; optionally substituted naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or...
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5610177 |
Acylated amino acids as endothelin antagonists
Novel acylated amino acids which are antagonists of endothelin are described. Methods for their preparation and pharmaceutical compositions containing them are also included. The compounds are...
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5610176 |
Tachykinin (NK1) receptor antagonists
The invention concerns tachykinin antagonists. The compounds are alcohols, amines and prodrugs of nonpeptides which have utility in treating disorders mediated by tachykinins. Such disorders are...
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5607943 |
Annelated dihydropyridines and the use thereof for preparing pharmaceutical preparations
A compound of formula I ##STR1## wherein A denotes a benzo, indolo or thieno group; R 1 denotes thienyl or the group ##STR2## wherein R 7 , R 8 and R 9 independently of one another may...
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5593991 |
Imidazole compounds, use and process of making
Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.
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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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5578604 |
5-vinyl- and 5-ethinyl-quinolone- carboxylic acids
The invention relates to new 5-vinyl- and 5-ethinyl-quinolone- and -naphthyridonecarboxylic acids, to processes for their preparation, and to antibacterial compositions and feed additives...
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5565447 |
Indole derivatives
A compound of formula (I) ##STR1## wherein R 1 and R 2 each represents a hydrogen atom or an alkyl group, Z represents a ring selected from: ##STR2## in which n represents 4, 5 or 6; ##STR3## in...
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5563142 |
Diaromatic substituted compounds as anti-HIV-1 agents
The present invention includes diaromatic substituted heterocyclic compounds (III) ##STR1## which are useful in treating individuals infected with the HIV virus.
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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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5559125 |
Hydroxyquinolone derivatives
A class of 4-hydroxy-2-(1H)-quinolone derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or...
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5536745 |
(Hetero)-aryl ketones derivatives with antibacterial properties
Conformationally restricted aryl and heteroaryl ketones derived from monic acid have useful antibacterial properties.
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5532237 |
Indole derivatives with affinity for the cannabinoid receptor
Disclosed are indole derivatives having activity on the cannabinoid receptors and the methods of their preparation. The compounds are useful for lowering ocular intra ocular pressure and treating...
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