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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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5674883 |
Derivatives of pyridone, their preparation process, the new intermediates obtained, their use as medicaments and the pharmaceutical compositions containing them
Products of formula (I): ##STR1## in which: R 1 , R 2 , R 3 and R 4 represent: --a hydrogen atom, a halogen atom, one of the following radicals: hydroxyl, mercapto, cyano, nitro, sulpho,...
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5670526 |
1,3,4-oxadiazoles
1,3,4-oxadiazole compounds are disclosed. The subject compounds suppress immune function and have hepatoprotection activity.
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5660837 |
Preparing pharmaceutical formulation in form of oil-in-water emulsion
The present invention is related to a pharmaceutical formulation which is an oil-in-water emulsion for parenteral and oral use which comprises (i) an emulsion-stabilizing surface active drug in...
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5658940 |
Succinimide and maleimide cytokine inhibitors
Novel succinimides and maleimides are inhibitors of tumor necrosis factor α and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and...
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5654298 |
Amine derivatives
This invention concerns novel aminopyridinium compounds of the formula I wherein R 1 , R 2 , R 3 , R 5 and R 6 are selected from the following combinations: ##STR1## (a) one of R 2 and R 6 is a...
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5648372 |
Antifungal agents, and compositions
A compound represented by the general formula: ##STR1## wherein R 1 and R 2 denote a halogen atom or hydrogen atom; R 3 means a hydrogen atom or lower alkyl group; l, r and m stand for 0 or 1; A...
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5643906 |
Method of using N-arylheteroarylalkyl imidazol-2-one compounds for treatment of a glaucoma disorder
A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of a glaucoma disorder. Compounds of particular interest are angiotensin II antagonists of the formula...
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5633272 |
Substituted isoxazoles for the treatment of inflammation
A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1##...
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5633271 |
Arthropodicidal oxazolines and thiazolines
Arthropodicidally active compounds, compositions and a method for using them, the compounds having the formula ##STR1## wherein A, Q, Z, (E) q , R 1 and R 2 are as defined in the text.
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5629332 |
Triazole compound and use thereof
A triazole compound or a pharmacologically acceptable salt thereof represented by the following formula (I) ##STR1## wherein R 1 and R 2 are the same or different from each other and each...
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5624916 |
Fungicidal 1,2,4-triazoles
2-Aryl or 2-heterocyclyl-2, 2-disubstituted ethyl-1,2,4-triazoles have been shown to have fungicidal activity.
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5622917 |
Substituted 1H--3-aryl-pyrrolidine-2,4-dione derivatives
The invention relates to new 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, X, Y and G have the meanings given in the description, to a plurality of...
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5622977 |
Tri-substituted (aryl or heteroaryl) derivatives and pharmaceutical compositions containing the same
Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR 1 , where R 1 is a substituted or unsubstituted alkyl; X is --O--, --S-- or --N(R 8 )--, where R 8 is...
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5622976 |
Oxadiazole derivatives having acetylcholinesterase-inhibitory and muscarinic agonist activity
Heterocyclic compounds of the formula: R 1 --Q--Z--X--A--M wherein R 1 is lower alkyl, a heterocyclic group which may have suitable substituent(s), etc; Q is oxadiazolediyl, Z is bond or vinyl,...
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5616587 |
Aqueous risperidone formulations
The present invention is concerned with physicochemically stable aqueous solutions of risperidone for oral and parenteral administration; processes for preparing such formulations.
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5616579 |
Anti-ulcer pyridyloxy derivatives, their preparation and uses
Compounds of formula (I): ##STR1## [wherein: R 1 is a cyclic amino group, or a dialkylamino group; R 2 a group of formula --NHCHR 3 R 4 wherein R 3 and R 4 are each alkyl aryl or aralkyl, or...
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5614537 |
2,4-and 2,5-bistetrazolylpyridines, a process for the preparation thereof and the use thereof as pharmaceuticals
The invention relates 2,4- and 2,5-bistetrazolylpyridines. Said compounds inhibit the enzymes proline hydroxylase and lysine hydroxylase and bring about a selective inhibition of collagen...
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5610170 |
Package form for bicarbonate-containing powdery pharmaceutical compositions and a method of stabilizing the compositions
The invention provides a method and a package form for insuring a stabilized bicarbonate-containing pharmaceutical composition, the method comprises filling the bicarbonate-containing powdery...
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5610171 |
Inhibition of metastasis in patients having cancer with pyridyloxazole-2-ones
This invention is directed to pyridinyloxazole-2-ones which are useful in inhibiting metastasis in patients having cancer. The pyridinyloxazole-2-ones act to inhibit protein kinase C and thereby...
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5607950 |
Muscarinic receptor antagonists
The invetion is a method of treating irritable bowel syndrome with a compound selected from the formula ##STR1## wherein R, R 1 , m, n p are as defined in the specification, or a pharmaceutically...
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5602160 |
Aminoketone derivatives and use thereof
Aminoketone derivative compounds containing a heterocyclic ring bonded to an aminoketone moiety and useful as effective ingredients of centrally acting muscle relaxants and pollakiurea curing...
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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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5602153 |
Method of using 1-arylheteroarylalkyl substituted-1H-1,2,4-triazole compounds for treatment of a giaucoma disorder
A class of 1-arylheteroarylalkyl-substituted-1-H-1,2,4-triazole compounds is described for use in treatment of a glaucoma disorder. Compounds of particular interest are angiotensin II antagonists...
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5599823 |
Substituted biphenylpyridones
Substituted biphenylpyridones can be prepared by alkylating pyridones on the nitrogen. The substituted biphenylpyridones are suitable as active substances in medicaments, in particular in...
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5594010 |
Substituted monopyridylmethyl derivatives
The substituted monopyridyl and bipyridyl derivatives are prepared by reacting substituted pyridine halides with phenylboronic acids. They are suitable for use as active compounds in medicaments...
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5591755 |
Pyridinyl thiadiazolyl compounds for treating glaucoma
The present invention relates to therapeutically active azacyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are...
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5580889 |
Insecticidal nitromethyl or niteoimino-heteromethyl-heterocyclics
Novel insecticides of the formula ##STR1## in which n is 0 or 1, X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R 9 variously...
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5580871 |
4-Heteroaryl- 1,4-dihydropyridine compounds with calcium agonist and alpha.sub.1 -antagonist activity
There are provided novel 1,4-dihydropyridine compounds, compositions containing them and methods of using them to treat congestive heart failure.
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5578550 |
Herbicidal oxadiazole carbonamide compounds
The invention pertains to a compound of the general formula ##STR1## wherein A represents an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or aralkyl group, or a...
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5574051 |
Certain-[3-aryl-prop-2-ynyl]-5-(arylsulfonyl) thiazolidine -2,4-dione derivatives
This invention relates to novel 5-[3-aryl-prop-2-ynyl]-5-(arylsulfonyl)- thiazolidine-2,4-diones and 5-[3-aryl-prop-2-ynyl]-5-(arylsulfanyl)thiazolidine-2,4-dion
es characterized by the general...
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5571821 |
Sulfonamides and derivatives thereof that modulate the activity of endothelin
Sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods...
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5567735 |
Therapeutic amides
Amides having formula I: ##STR1## wherein E, X, R 2 and R 3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo...
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5565474 |
1-heteroarylazetidines and -pyrrolidines process for their preparation and pharmaceutical compositions containing them
The present invention relates to new 1-heteroarylazetidines and new 1-heteroarylpyrrolidines endowed with 5-HT 3 agonist activity of formula (I): ##STR1## in which A is --CH=CH--; R is hydrogen,...
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5563158 |
Aromatic compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using...
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5561142 |
Substituted sulfonamides as selective β.sub.3 agonists for the treatment of diabetes and obesity
Substituted sulfonamides are selective β 3 adrenergic receptor agonists with very little β 1 and β 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis...
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5559138 |
Method of Treating Glaucoma Using Oxadiazolyl or Thiadiazolyl Tetrahydropyridines
This invention relates to the treatment of glaucoma by topically administering a compound selected among ##STR1## wherein Z, R, and R 1 are defined in the specification, and a pharmaceutically...
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5556867 |
Oxazoline derivative, its production and its use
An oxazoline derivative having the formula: ##STR1## which is useful for control of insects, mites and/or ticks.
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5534528 |
Thiadiazolyl tetrhydrpyridines for treating glaucoma
The present invention relates to therapeutically active azacyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are...
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5532259 |
Isoxazole-4-carboxamides and hydroxyalkylidenecyanoacetamides, pharmaceuticals containing these compounds and their use
Isoxazole-4-carboxamides and hydroxyalkylidenecyanoacetamides, pharmaceuticals containing these compounds and their use Isoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide...
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5527818 |
Sulfamoyltriazole derivatives of fungicidal composition containing same as effective component thereof
The present invention relates to a sulfamoyl triazole derivative and a fungicide containing same as an effective component, the sulfamoyl triazole derivative being expressed by general formula (I):...
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5523312 |
Antipicornaviral agents
Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1##...
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5514694 |
Peptidyl ketoamides
A novel class of peptide α-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally...
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5500427 |
Cyclic compounds and their use
The present invention relates to a compounds represented by the following formula or salts thereof. ##STR1## The above compounds have strong angiotensin II antagonistic action, antihypertensive...
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5498619 |
Aminoketone derivative and use thereof
Aminoketone derivative compounds containing a heterocyclic ring bonded to an aminoketone moiety and useful as effective ingredients of centrally acting muscle relaxants and pollakiurea curing...
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5496853 |
Benzoxa condensed ring compounds, process for producing the same and pharmaceutical composition comprising the same
Pharmaceutical compositions containing a benzoxazole compound and a 2,3-dihydrobenzofuran compound represented by the following formula (I) and its pharmaceutically acceptable salt: ##STR1## In the...
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5492908 |
Diaminotrifluoromethylpyridine derivatives, process for their production and phospholipase A.sub.2 inhibitor containing them
A method of treating rheumatoid arthritis using a diaminotrifluoromethylpyridine derivative of the formula (I) or its salt: ##STR1## wherein X is --CW 1 R 1 , --COCOR 2 , --CW 1 NHCOR 2 ,...
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5486531 |
Hydroxymethylfurazancarboxylic acid derivatives
The present invention relates to hydroxymethylfurazancarboxylic acid derivatives of the general formula I ##STR1## in which one of the radicals R 1 and R 2 represents hydroxymethyl and the other...
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5482951 |
Triazole derivatives as well as insecticide and acaricide
A novel triazole derivative for use in an insecticide or an acaricide has a general formula [I]: ##STR1## (wherein R 1 is an alkyl group, X is a hydrogen atom, a halogen atom or the like, n is an...
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5482953 |
2,4-and 2,5-bistetrazolylpyridines and the use thereof as pharmaceuticals
The invention relates to 2,4- and 2,5-bistetrazolylpyridines. Said compounds inhibit the enzymes proline hydroxylase and lysine hydroxylase and bring about a selective inhibition of collagen...
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