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7388005 |
Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo [1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C 1-2 alkyl group and a...
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7192948 |
Bicyclic heterocycles as HIV integrase inhibitors
The invention encompasses a series cyclic bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the...
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7141564 |
Nitrogen-containing bicyclic heterocycles for use as antibacterials
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
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6900216 |
Dihydroimidazo[2,1-b]thiazole and dihydro-5h-thiazolo[3,2-A]pyrimidines as antidepressant agents
The present invention relates to certain novel substituted dihydroimidazo[2,1-b]thiazole and dihydro-5H-thiazolo[3,2-a]pyrimidine compounds including pharmaceutically acceptable salts thereof which...
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6838462 |
Insecticidal azoles
The present invention relates to novel heterocyclic compounds of formula (I)
where A, R1, R2, Y, Z, and n are defined in the disclosure, to processes for their preparation, and to their use as...
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6833371 |
Pyrazolopyrimidines
Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More...
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6828326 |
Pyrimidinone fused bicyclic metalloproteinase inhibitors
The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R 1 are as defined in the specification, and to pharmaceutical compositions...
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6800628 |
N-substituted 4-((-4′-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties
This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R 1 is C 1-6...
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6747032 |
Pyrimidin-4-one compounds
Compound of formula (I): wherein: R 1 , R 2 , R 3 and R 4 , which may be the same or different, each represent a hydrogen atom, a halogen atom or a group selected from alkyl, alkoxy,...
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6740654 |
Squaric acid derivatives
Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L 2 is a covalent bond or an atom or group —O—,...
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6670365 |
Substituted imidazo 1,2a&rcub azines as selective inhibitors of cox-2
The invention refers to new compounds of formula (I), wherein A and B are selected from the group consisting of N and CH, with the condition that when A is N, B is N; R 1 is selected from the...
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6635643 |
Bicyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivatives
The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R 1 and R 2 ...
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6583146 |
Thiazolopyrimidine compounds, its production and use
Compounds represented by general formula (I): and salts thereof, exhibiting excellent adenosine A 3 receptor antagonism: wherein A is an optionally substituted benzene ring; B may be further...
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6525056 |
Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (CRH) antagonists, useful for treating cns and stress-related disorders
Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress...
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6348457 |
4-&lsqb 3-benzofuranyl&rsqb piperidinyl and 4-&lsqb 3-benzothienyl&rsqb piperidinyl derivatives
The invention is concerned with novel compounds of the formula the pharmaceutically acceptable acid addition salts thereof and the stereochemically isomeric forms thereof, wherein X is oxygen or...
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6303614 |
Tetrahydro gamma-carbolines
The present invention concerns the compounds of formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R 1 is...
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6187802 |
Substituted 4-arylmethylene-2-imino-2,3-dihydrothiazoles and derivatives and their pharmaceutical use
Compounds of Formula I ##STR1## including pharmaceutically acceptable salts thereof in the form of individual enantiomers, racemates, or other mixtures of enantiomers, in which Ar is phenyl,...
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6096761 |
Esters of 3-hydroxy-piperidinemethanol derivatives
The present invention of compounds of formula (I), ##STR1## a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R 1 is C...
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6057325 |
Hexahydro-pyrido(4,3-b)indole derivatives as antipsychotic drugs
This invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C 1 -6 alkanediyl; R 1 is...
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5958931 |
Phenyl-substituted 5H-thiazolo 3,2-A!pyrimidine derivative glutamate receptor antagonists
The invention is concerned with compounds of the general formula ##STR1## wherein R 1 is hydrogen, lower alkyl, phenyl or benzyl, R 2 is lower alkyl, lower alkoxy, --O(CH 2 ) n N(R 13 )(R 14...
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5929114 |
Arylthio compounds
Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O,...
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5919788 |
4-(1H-indol-1-yl)-1-piperidinyl derivatives
The present invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dashed line designates...
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5869492 |
Condensed thiazole derivatives, having 5-HT receptor affinity
Compounds of formula I ##STR1## in which A is S(O) p or O; p is 0, 1 or 2; g is 0, 1, 2, 3, or 4; n is 2 or 3; and R 1 , R 2 , R 3 , R 4 and R 5 are optional substituents have utility in the...
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5798361 |
5H-thiazolo 3,2-a!pyrimidin-5-one derivatives
The present invention relates to new 5H-thiazolo 3,2-a!pyrimidin -5-one derivatives having the formula (I): ##STR1## wherein Ar is phenyl optionally substituted by one or two groups selected from...
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5688801 |
Method of inhibiting neurotransmitter activity using microencapsulated 3-piperidiny2-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
A pharmaceutical composition comprising a biodegradable and biocompatible composition comprising a 1,2 benzazole within a polymeric matrix. The 1,2 benzazole composition, pharmaceutically...
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5610157 |
N-(3-hydroxy-4-piperidinyl) (dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzo-dioxin) carboxamide derivatives
N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal...
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5599813 |
Thiazolopyrimidine derivatives
Thiazolopyrimidine derivatives represented by the formula ##STR1## and salts thereof are provided, which are characterized by a carboxamide residue substituted with R 4 and R 5 . The derivatives...
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5532243 |
Antipsychotic nitrogen-containing bicyclic compounds
There are provided nitrogen-containing bicyclic compounds, pharmaceutical compositions containing these compounds and methods of using these compounds to treat physiological or drug-induced...
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5397782 |
Method of treating addiction to alcohol
Method of treating addiction to alcohol and symptoms related to withdrawal of said alcohol comprising the administration of certain 4-[bis(halophenyl)methylene]-1-piperidinyl derivatives.
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5321028 |
Antihypertensive 3-piperidinyl-indazole derivatives
3-Piperidinyl-indazole derivatives and their pharmaceutically acceptable acid addition salts being useful antagonists of neurotransmitters; pharmaceutical compositions containing the same and a...
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5300509 |
2-furyl-oxazolo[5,4-d]-pyrimidines
Compounds of formula I, and pharmaceutically acceptable salts thereof, ##STR1## in which R1 is hydrogen (1-6C)alkyl or (1-4C)alkanoyl; A is --NCQ--O--, NCQ--NR 8 --, --NCQ--CHN-- ...
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5272150 |
Hydroxyalkylfuranyl derivatives
Hydroxyalkylfuranyl derivatives, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof having antiallergic properties, compositions containing the same and...
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5262418 |
N-(4-piperidinyl) (dihydroxybenzofuran or dihydro-2H-benzopyran)carboxamide derivatives
Piperidine derivatives of formula ##STR1## wherein A is a radical of formula --CH 2 --CH 2 -- (a-1), --CH 2 --CH 2 --CH 2 -- (a-2),...
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5082838 |
Sulfur-containing fused pyrimidine derivatives, their production and use
Disclosed is a compound represented by the formula (I) or a salt thereof: ##STR1## wherein R 1 represents an aliphatic hydrocarbon, aralkyl or aryl group which may be substituted; R 2 represents...
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4996208 |
Pesticidal thiazolopyrimidine derivatives
Fungicidal thiazolopyrimidine derivatives of the formula ##STR1## in which R 1 stands for hydrogen or alkyl, R 2 stands for hydrogen, alkyl or optionally substituted aryl, R 3 stands in...
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4985432 |
5H-1,3,4-thiadiazolo(3,2-A)pyrimidin-5-one derivatives and agricultural-horticultural fungicide composition containing the same
A new class of 5H-1,3,4-thiadiazolo[3,2-a]pyrimidin-5-one derivatives were synthesized. They are useful as agricultural-horticultural fungicides.
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4971971 |
5H-1,3,4-thiadiazolo(3,2-A)pyrimidin-5-one derivatives and functional compositions containing the same
A class of novel 5H-1,3,4-thiadiazolo[3,2-a]-pyrimidin-5-one derivatives are disclosed. These compounds exhibit remarkable fungicidal activities for pathogenic fungi of cucumber gray mold, cucumber...
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4921854 |
Condensed thiazolopyrimidine, pyrimido-thiazine or thiazepine pyrimidine compounds
The compounds of the general formula I ##STR1## and pharmaceutically acceptable acid addition salts and hydrates thereof possess useful immunostimulant properties and can be used in therapy. In the...
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4908379 |
Nitrogen-containing heterocyclic compounds and compositions for controlling and/or preventing pests and blights (diseases)
A nitrogen-containing heterocyclic compound of the following formula: ##STR1## wherein D represents --N or ##STR2## E represents N--, ##STR3## G represents --N, ##STR4## with proviso that...
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4874766 |
Method of promoting wound-healing
Method of promoting wound-healing by topically applying a serotonin-antagonistic compound.
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4866064 |
5H-1,3,4-thiadiazolo(3,2-A)pyrimidin-5-one derivatives and fungicidal compositions containing the same
A class of novel 5H-1,3,4-thiadizaolo[3,2-a]pyrimidin-5-one derivatives are disclosed. These compounds exhibit remarkable fungicidal activities for pathogenic fungi of cucumber gray mold, cucumber...
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4839374 |
4-((Bicyclic heterocyclyl)-methyl and -hetero)-piperidines
4-[Bicyclic heterocyclyl)methyl and -hetero]-piperidines having antihistaminic and serotonin-antagonistic properties which compounds are useful agents in the treatment of allergic diseases.
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4804663 |
3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
3-Piperdinyl-1,2-benzisothiazoles and 3-piperidinyl-1,2-benzisoxazoles and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties and being useful in the...
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4609660 |
Substituted carboxy-thiazolo[3,2-a]pyrimidine derivatives
Carboxy-thiazolo[3,2-a]pyrimidine derivatives, and pharmaceutical compositions containing them. The compounds and compositions possess anti-allergic activity.
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4551457 |
Substituted thiazolo[3,2-a]pyrimidines and process for their preparation
Pharmacologically active thiazolo[3,2-a]pyrimidines of the formula ##STR1## wherein A is a bond between the α- and β-carbon atoms or (--CH 2 --) group; R 1 and R 2 represent hydrogen, C 1 -C...
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4548938 |
5-H-1,3,4-thiadiazolo[3,2-a]pyrimidin-5-one compounds
Novel 5H-thiazolo- and 5H-1,3,4-thiadiazolo[3,2-a]pyrimidin-5-one and 3,4-dihydro-2H,6H-pyrimido[2,1-b] [1,3]-thiazin-6-one derivatives, which compounds are useful psychotropic agents.
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4535081 |
Antiallergic and antiulcer 1-oxo-1H-thiazolo[3,2-a]pyrimidine-2-carboxamides and intermediates therefor
Antiallergy and antiulcer agents having the formula (I), ##STR1## and their pharmaceutically acceptable salts, wherein R 1 and R 2 taken separately are each hydrogen or lower alkyl; and R 1 and...
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4525357 |
Derivatives of bicyclic 2-iminothiazolidine oximes
Novel derivatives of bicyclic 2-iminothiazolidine oximes and methods of preparing same. This invention is also directed to an insecticidal composition comprising an acceptable carrier and an...
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4522944 |
Carboxamido-derivatives of 5H-1,3,4-thiadiazolo[3,2-a]pyrimidines, compositions and use
The present invention relates to new carboxamido-derivatives of 5H-1,3,4-thiadiazolo[3,2-a]pyrimidines, to a process for their preparation and to pharmaceutical (i.e. anti-inflammatory and...
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4476127 |
7-Diethylamino-5-methyl-thiazolo[5,4-d]pyrimidine and pharmaceutical composition containing same
The compound related to this invention is 7-diethylamino-5-methyl-thiazolo[5,4-d]pyrimidine. The compound related to this invention possesses vasodilating action, hypotensive action, inhibitory...
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