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5837708 |
Sulphonamides
Compounds of the formula ##STR1## wherein the variables are hereinbelow defined. The compounds of formula I are inhibitors for endothelin receptors. They can be used for the treatment of disorders...
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5824677 |
Substituted amino alcohol compounds
Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty....
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5817666 |
Dermatological preparation and method for treating actinic keratoses using 5-FU
A composition for the treatment of actinic keratoses includes 5-fluorouracil and an alpha hydroxy carboxylic acid. The composition may further include ancillary ingredients. A therapeutic method...
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5814639 |
Method for the synthesis, compositions and use of 2'-deoxy-5-fluoro-3'-thiacytidine and related compounds
The present invention relates to a method of preparing the antiviral compounds 2'-deoxy-5-fluoro-3'thiacytidine (FTC) and various prodrug analogues of FTC from inexpensive precursors with the...
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5814640 |
Method of treating gastrointestinal malignancies
The present invention provides a method for the treatment of carcinoma. Those carcinomas include those of visceral origin and in particular gastrointestinal malignancies. The method comprises...
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5811428 |
Pyrimidine carboxamides and related compounds and methods for treating inflammatory conditions
Compounds having utility as antinflammatory agents in general and, more specifically, for the prevention and/or treatment of immunoinflammatory and autoimmune diseases are disclosed. The compounds...
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5807864 |
2-thioxo-tetrahydropyrimidin-4-one derivatives
This invention relates to the use of 2-thioxotetrahydropyrimidin-4-one derivatives to increase HDL cholesterol concentration and as therapeutic compositions for treating atherosclerotic conditions...
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5807863 |
2-(4-pyrazolyloxy-pyrimidin-5-yl) acetic acid derivatives
This invention relates to novel 2-(4-pyrazolyloxy-pyrimidin-5-yl) acetic acid derivatives of formula I ##STR1## wherein R 1 is hydrogen, C 1 -4 alkyl, C 1 -4 alkoxy, C 1 -4 alkylthio, C 3 -6...
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5801181 |
Amino alcohol substituted cyclic compounds
Therapeutic compounds have the formula: (X)j--(core moiety), J being an integer from one to three, the core moiety having at least one, five- to seven-membered ring and X being a racemic mixture,...
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5792773 |
L-β-dioxolane uridine analog administration for treating Epstein-Barr virus infection
The present invention relates to the discovery that certain β-L-dioxolane nucleoside analogs which contain a uracil base, and preferably, a 5-halosubstituted uracil base, exhibit unexpectedly high...
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5789000 |
Sterile aqueous parenteral formulations of cis-diammine dichloro platinum
This invention describes a novel formulation containing both cis-diammine dichloro platinum and a water soluble disulfide, 2,2'-dithio-bis-ethane sulfonate in the same solution, wherein the...
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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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5783576 |
Benzoyl guanidine derivatives, the preparation thereof and their use in pharmaceutical compositions
New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.
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5780506 |
***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
Phenylacetic acid derivatives, and use as fungicides
The present invention relates to phenylacetic acid derivatives of the formula I ##STR1## and their salts. The invention additionally relates to processes and intermediates for preparing these...
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5780473 |
Substituted biphenyl sulfonamide endothelin antagonists
Compounds of the formula ##STR1## inhibit the activity of endothelin.
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5776963 |
3-(heteroaryl)-1- (2,3-dihydro-1h-isoindol-2-yl)alkyl!pyrrolidines and 3-(heteroaryl)-1- (2,3-dihydro-1h-indol-1-yl)alkyl!pyrrolidines and related compounds and their therapeutic untility
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
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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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5773451 |
Substituted arylthioalkylthiopyridines
Described are compounds of formula (I) in which R1,R2,R3,R4,R5,R6,R7, m,n,p, and q are as defined in the description. Such compounds are suitable for use against Helicobacter bacteria. ##STR1##
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5763448 |
Pyrmidine derivatives
A class of substituted pyrimidine derivatives are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment of disorders of the dopamine system, in particular...
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5763447 |
Method of preventing or treating pneumonia in immobilized patients with uridine triphosphates and related compounds
A method of promoting drainage of mucous secretions in the congested airways of a bedridden/immobilized patient or an intubated/mechanically-ventilated patient is disclosed. The method comprises...
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5753715 |
2-disubstituted cyclohexenyl and cyclohexyl antimicrobial agents
The invention relates to cyclohexenyl antibacterial compounds of the formula I: ##STR1## and pharmaceutical compositions containing the compounds, methods for their production and use.
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5750532 |
Pharmaceutically active compounds
The disclosed invention is compounds represented by the formula ##STR1## and pharmacetically acceptable acid salts thereof, wherein each Z is independently tetiary butyl, phenyl, naphthyl or...
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5747500 |
Antiviral 2, 4-pyrimidinedione derivatives
Novel 2,4-pyrimidinedione compounds, and pharmaceutically acceptable salts thereof which possess good antiviral activities, and specifically represented by the following formula(I): ##STR1##...
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5744460 |
Combination for treatment of proliferative diseases
The invention relates to combinations of PKC-targeted (especially PKC-α-targeted) deoxyribo- and ribo-oligonucleotides and derivatives thereof with other chemotherapeutic compounds, as well as to...
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5733920 |
Inhibitors of cyclin dependent kinases
The invention provides novel inhibitors of cyclin-dependent kinases, in particular inhibitors of the CDK/cyclin complexes such as CDK4/cyclin D1. The novel compounds are analogs of chromones. These...
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5728687 |
Antitumour compositions containing taxane derivatives
Pharmaceutical compositions having therapeutic synergy comprising taxol or Taxotere or analogues thereof combined with at least one therapeutically useful substance for treating neoplastic diseases.
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5728706 |
Benzenesulfonamide derivative and process for preparing thereof
A benzenesulfonamide derivative of the formula I!: ##STR1## wherein Ring A and Ring B are the same or different and each substituted or unsubstituted benzene ring, Q is a single bond or a group of...
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5728684 |
Determination of prodrugs metabolizable by the liver and therapeutic use thereof
A method of ascertaining if a prodrug is useful for treating a disease is disclosed. The prodrug is acceptable if it is metabolized in liver cells by aldehyde oxidase to produce an active drug or...
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5728707 |
Treatment and prevention of primary and metastatic neoplasms with salts of aminoimidazole carboxamide
Methods and compositions for the prevention and/or inhibition of primary and secondary metastatic neoplasms are described. Individuals at a high risk of developing neoplasia and/or cancer patients...
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5723471 |
Pyrimidine fungicides
A fungicidal compound of formula (I) or a stereoisomer thereof, wherein R is H or CH 3 , A is CH or N, and B is OCH 3 or NHCH 3 . ##STR1##
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5723469 |
Amino-acid amide derivatives, agricultural or horticultural fungicides, and method for producing the same
The present invention provides an agricultural or horticultural fungicide including an effective amount of an amino-acid derivative represented by the formula: ##STR1## wherein R 1 represents a...
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5719132 |
Compositions and methods of treating HIV with d4T, 5-fluorouracil/tegafur, and uracil
The present invention is directed to the use of pharmaceutical compositions containing anti-retroviral effective amounts of (a) d4T and (b) 5-fluorouracil or a prodrug, or salt thereof.
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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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5712285 |
Pyrrolo-pyridine derivatives
A class of pyrrolo 2,3 -b!pyridine derivatives, linked via the 3-position thereof by a methylene group to a tetrahydropyridinyl moiety, the latter moiety being substituted in turn by an aryl- or...
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5707995 |
Pesticidal pyrimidine compounds
Compounds of formula (I) in which X 1 and X 2 each represents oxygen; S(O) n , n being 0, 1 or 2; or CO, CH 2 or NR, R being hydrogen or alkyl; R 1 and R 10 are each hydrogen or halogen; R 2 ...
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5708000 |
N4-substituted cytosinyl 1,3-oxathiolane nucleoside analogues, and their antiviral activity
The present invention pertains to the field of organic chemistry, and particularly therapeutic chemistry. The invention provides cis-form 5-(cytosinyl-1) 1,3-oxathiolanes of general formula (I),...
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5700805 |
Substituted 1-amino-3-phenyluracils
Substituted 1-amino-3-phenyluracils I ##STR1## where the variables have the following meanings: R 1 =H, F, Cl; Y=O, S; Z=--CH=N--OH, --CH=N--O--(alkyl), --CH=N--O--(alkylene)--O--(alkyl),...
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5691338 |
1,2-dithiole-3 thiones for the treatment of reverse transcriptase-dependent viral infections
This invention provides a method of inhibiting the replication of a reverse transcriptase-dependent virus in cells which comprises contacting infected cells with an effective amount of a...
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5684011 |
Pyrimidine derivatives useful as nematicides
The invention provides novel compounds of formula (I) having nematicidal, insecticidal, acaricidal and fungicidal properties, compositions comprising them and processes and intermediates for their...
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5679684 |
Hydroxyalkylammonium-pyrimidines and nucleoside derivatives, useful as inhibitors of inflammatory cytokines
Novel hydroxyalkylammonium-pyrimidine of the formula ##STR1## and nucleoside derivatives have been found to be useful as inhibitors of inflammatory cytokines. They can be used, inter alia, in the...
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5677324 |
Benzopyranes as potassium channel openers
The present invention relates to compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein the dashed line represents an optional covalent bond; X is O, NH, S or a direct...
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5674894 |
Amidine derivatives useful as platelet aggregation inhibitors and vasodilators
The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.
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5670507 |
Method for reversing multiple drug resistant phenotype
There is disclosed a method for reversing the multiple drug resistant (MDR) phenotype in tumors insensitive to hydrophobic chemotherapeutic drugs due to over expression of mdr-1, comprising...
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5661153 |
1-arylpyrimidine derivatives and pharmaceutical use thereof
The present invention relates to 1-arylpyrimidine derivatives represented by general formula (I): ##STR1## wherein R 1 is H, alkyl or aralkyl; Ar is 1-naphthyl, or a substituted or...
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5654319 |
N-[(4-heteroaryl-1-piperidinyl)alkyl]-2,3-naphthalimides and related compounds and their therapeutic utility
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a...
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5646135 |
Method for controlling coccidiosis
The present invention relates to an improved method for controlling coccidiosis in poultry which comprises administering to poultry on shuttle medication an additional medication prior to switching...
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5643913 |
Pharmaceutical compositions of 5-substituted uracil compounds
Pharmaceutical compositions containing 5-substituted uracil compounds are disclosed. The compositions are preferably in the form of a tablet or capsule.
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5639764 |
2-[(4-heteroaryl)-1-piperidinyl)alkyl]-1,3-indandiones and related compound and their therapeutic utility
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a...
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5637593 |
Tryptamine analogues as 5-ht1-like agonists
A compound of structure (I), in which A 1 is O, S(O) n in which n is 0, 1 or 2, NR, CH 2 , or CH(OH); A 2 is a bond or CH 2 ; or A 1 A 2 is CHCH; R is hydrogen or C 1 -4 alkyl; R 1 is an...
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5635509 |
Piperidine derivatives useful as neurokinin antagonists
Compounds of formula I ##STR1## wherein Q 1 , Q 2 , Q 3 , and Q 4 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide...
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