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8119647 |
Fused pyrimidineone compounds as TRPV3 modulators
The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or...
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8063070 |
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. Processes for...
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8022075 |
Diagnostic and remedy for disease caused by amyloid aggregation and/or deposition
To provide a diagnostic drug which binds specifically to an amyloid aggregate and/or an amyloid deposit, to thereby realize imaging and quantification of a disease caused by amyloid aggregation...
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7790750 |
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, R1 and R2 taken...
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RE40793 |
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, R1 and R2 taken...
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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 C1-2 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 crop...
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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 R1 are as defined in the specification, and to pharmaceutical compositions and...
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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 R1 is C1-6alkyloxy,...
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6747032 |
Pyrimidin-4-one compounds
Compound of formula (I): wherein:R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen atom, a halogen atom or a group selected from alkyl, alkoxy, polyhaloalkyl,...
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6740654 |
Squaric acid derivatives
Squaric acid derivatives of formula (1) are described: whereinHet is an optionally substituted bicyclic fused ring heteroaromatic group;L2 is a covalent bond or an atom or group —O—, —S—, —C(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; R1 is selected from the group...
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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, R1 and R2 taken...
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6583146 |
Thiazolopyrimidine compounds, its production and use
Compounds represented by general formula (I): and salts thereof, exhibiting excellent adenosine A3 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, whereinX 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 R1 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, R1 is C1-6...
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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 C1-6 alkanediyl; R1 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 R1 is hydrogen, lower alkyl, phenyl or benzyl, R2 is lower alkyl, lower alkoxy, --O(CH2)n N(R13)(R14), --(CH2)n...
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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; andR1, R2, R3, R4 and R5 are optional substituents have utility in the treatment of...
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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 R4 and R5. The derivatives and...
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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--NR8 --, --NCQ--CHN-- or --NCH-...
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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 --CH2 --CH2 -- (a-1), --CH2 --CH2 --CH2 -- (a-2), or --CH2 --CH2 --CH2 --CH2 -- (a-3),wherein one or two hydrogen atoms...
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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 R1 represents an aliphatic hydrocarbon, aralkyl or aryl group which may be substituted; R2 represents...
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4996208 |
Pesticidal thiazolopyrimidine derivatives
Fungicidal thiazolopyrimidine derivatives of the formula ##STR1## in which R1 stands for hydrogen or alkyl, R2 stands for hydrogen, alkyl or optionally substituted aryl, R3 stands in each case for...
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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 when ...
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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 (--CH2 --) group; R1 and R2 represent hydrogen, C1 -C4 alkyl, c...
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