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6555546 |
Use of 5HT3 antagonists for promoting intestinal lavage
The present invention is concerned with the use of 5HT 3 antagonists for promoting intestinal lavage, especially in combination with an osmotic agent.
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6555552 |
Azabicyclic amine derivatives and their use as therapeutic agents
The present invention relates compounds of the formula (I): wherein X represents hydrogen or a C 1-4 alkyl group optionally substituted by a hydroxy group; Y represents hydrogen, C 1-6 alkyl or...
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6541520 |
Treatment of addiction and addiction-related behavior
The present invention provides a highly efficient method for treating substance addiction and for changing addiction-related behavior of a mammal suffering from substance addiction. The method...
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6537522 |
Neuroprobes for mapping monoamine reuptake sites
Iodinated neuroprobes for mapping monoamine reuptake sites in the brain, and particularly iodinated neuroprobes that can also serve as radiotracers for use in single-photon emission computed...
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6531484 |
Pyrrolidine modulators of CCR5 chemokine receptor activity
Pyrrolidine compounds of Formula I: (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8a , R 8b , j, k, 1, m, and n are defined herein) are described. The compounds are modulators of CCR5...
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6479509 |
Method of promoting smoking cessation
A method of training a smoker to cease smoking by administering tropane compounds is provided.
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6468998 |
Pyrrolidine compounds and medicinal utilization thereof
The present invention provides a pyrrolidine compound of the formula (I) wherein each symbol is as defined in the specification, an optically active compound thereof and a pharmaceutically...
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6465491 |
6-phenylpyridyl-2-amine derivatives
The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and...
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6432976 |
8-aza-bicyclo&lsqb 3.2.1&rsqb octane NMDA/NR2B antagonists
Novel 3-substituted 8-aza-bicyclo[3.2.1]octanes (commonly known as “tropanes”) substituted in the 8-position are effective as NMDA NR2B antagonists useful for relieving pain.
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6413961 |
Irrigation solution and method for inhibition of pain and inflammation
A method and solution for perioperatively inhibiting a variety of pain, inflammation, spasm and restenosis processes resulting from cardiovascular or general surgical, therapeutic and diagnostic...
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6395748 |
Tropane-derivatives, their preparation and use
Compounds of formula (a), (b), (c), or (d), or any mixture thereof, or a pharmaceutically-acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or...
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6391888 |
Topical anesthetics useful for treating cancer
The invention provides methods which are useful for treating diseases (e.g., cancer) where PKCδ is implicated, and modulation (e.g, inhibition) of its activity is desired.
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6376510 |
Neuromuscular relaxants
Alkoxy and/or acyloxy disubstituted and polysubstituted aralkyl and aralkenyl bis-quaternary ammonium derivatives of cyclic alkanol diesters have neuromuscular relaxant properties.
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6362195 |
Branched alkoxy-substituted 2-aminopyridines as NOS inhibitors
The present invention relates to 6-phenyl-pyridin-2-ylamine derivatives of the formula wherein R 1 , R 2 , R 3 and R 4 are defined as in the specification, that exhibit activity as nitric...
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6350758 |
Tropane derivatives and method for their synthesis
A compound of formula (I) wherein R 1 -R 6 have any of the values defined in the specification are described, as well as pharmaceutical compositions comprising a compound of formula (I), and...
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6323216 |
Basic derivatives of benz[E]isoindol-1-ones and pyrrolo[3,4-c]quinolin-1-ones with 5-HT3-antagonistic activity, their preparation and their therapeutic use
Novel basic derivatives of benz[e]isoindol-1-ones and pyrrolo[3,4-c]quinolin-1-ones which can be represented by the general formula (I) indicated below are described: ##STR1## in which X is CH...
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6306876 |
4-[aryl(8-azabicyclo[3.2.1]octan-3-yl)]aminobenzoic acid derivatives
4-[aryl(8-azabicyclo[3.2.1]octan-3yl)]aminobenzoic acid derivatives are delta-opioid receptor modulators. As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on...
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6294545 |
Bicyclic amines and their use as insecticides
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6288079 |
Tropane-derivatives, their preparation and use
Compounds of formula (a), (b), (c), or (d), or any mixture thereof, or a pharmaceutically-acceptable salt thereof; ##STR1## wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl,...
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6284770 |
Medicaments for the treatment of non-constipated female irritable bowel syndrome
This invention relates to the use of 5-HT3 receptor antagonists in the treatment of nonconstipated female IBS patients.
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6255319 |
5-aryl-3-(8-azabicyclo[3.2.1]oct-3-yl)-1,3,4-oxadiazol-2(3H)-one derivatives as 5-ht4 receptor ligands
Compound of general formula (I) ##STR1## in which R 1 represents an alkyl or cycloalkylmethyl group, X 1 represents a hydrogen or halogen atom or an alkoxy group, or alternatively OR 1 and X 1 ...
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6235747 |
6-phenyl-pyridin-2-ylamine derivatives
The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and...
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6221879 |
8-azabicyclo[3.2.1] octane-3-methanamine derivatives as ligands of D2 and D3 dopamine and 5HT1A and 5HT2 serotonin receptors
Compounds of general formula (I) ##STR1## in which U represents a group of general formula (A) or (B) ##STR2## in which formulae V represents a hydrogen or halogen atom, a (C 1 -C 3 )alkyl group...
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6221878 |
Method for treatment of depression
The invention relates to the use of compounds which act as antagonists of 5-hydroxytryptamine (5-HT) at 5-HT 3 receptors for the treatment of depression.
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6207677 |
Piperidine derivatives having anxiolytic effect
Piperidine compounds having the general formula (I), ##STR1## wherein R 1 is (a) a group consisting of alkyl, alkenyl, cycloalkyl, cycloalkenyl, phenyl, cycloalkylalkyl, cycloalkenylalkyl,...
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6200991 |
Imidazole derivatives, preparation and therapeutic application thereof
A compound of formula (I) ##STR1## the process of preparing compounds of formula (I), their pharmaceutical compositions, and the method of treating diseases associated with M 3 muscarinic and/or...
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6177442 |
Bicyclic amine derivatives
The invention provides a compound of formula (I): ##STR1## wherein A represents a bidentate group of formula --CH 2 --X--CH 2 -- (wherein X is methylene, sulfur or oxygen), X'CCY or X'WC--CYZ...
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6177451 |
Epibatidine and derivatives thereof as nicotine cholinergic receptor agonists
The present invention provides methods of treatment utilizing pharmaceutical compositions comprising an effective nicotine agonist amount of epibatidine (1) or a synthetic...
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6166032 |
Method for controlling tobacco use and alleviating withdrawal symptoms due to cessation of tobacco use
A method for controlling tobacco use and alleviating withdrawal symptoms due to the cessation of tobacco use comprising administering to a human desiring to control tobacco use and/or suffering...
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6140338 |
Chemokine receptor antagonists
The present invention relates to a compound of the general formula: ##STR1## wherein each of R 1 and R 2 which may be the same or different, is e.g. a hydrogen atom, a halogen atom or a lower...
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6117882 |
5-HT.sub.4 agonists and antagonists
Compounds of formula I: ##STR1## are used as antagonists and partial agonists for the serotonin receptor 5-HT 4 and provide therapeutic methods for treatment of disorders caused by or affected by...
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6114347 |
Pharmaceutical formulation for the prophylaxis and pretreatment of a poisoning caused by organophosphorus cholinesterase inhibitors
A pharmaceutical formulation for the prophylaxis and preliminary treatment of a poisoning caused by organophosphorus cholinesterase inhibitors is characterized in that it consists of an active...
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6107307 |
Inhibition of serotonin reuptake
This invention provides 3-(bicyclic heteroaryl)-8-azabicyclo[3.2.1]oct-2-enes and 3-(bicyclic heteroaryl)-8-azabicyclo[3.2.1]octanes which are useful for the inhibition of serotonin reuptake in...
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6100275 |
8-azabicyclo[3.2.1.]oct-2-ene derivatives, their preparation and use
A compound having the formula, ##STR1## or any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl,...
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6087379 |
Cyclic amine derivatives
A cyclic amine derivative represented by the following formula: ##STR1## wherein R 1 represents a substituted or unsubstituted phenyl group, R 2 represents a substituted of unsubstituted C 1 -C...
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6077848 |
Benzoylecgonine, ecgonine and ecgonidine derivatives
The present invention relates to a novel class of covalently coupled benzoylecgonine, ecgonine and ecgonidine derivatives that are useful for alleviating the symptoms of immunoregulatory disorders,...
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6030966 |
Heterocyclic compound and their use
The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel...
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H001838 |
Insecticidal N-(arylalkyl)-4-[Bis(substituted aryl)hydroxymethyl]azabicyclo[3.3.1.]nonanes and [3.2.1.]octanes
Compounds for control of insects and arcarids are disclosed and exemplified which are N-(arylalkyl)-4-[bis(substituted aryl)hydroxymethyl]azabicyclo[3.3. 1 .]nonanes and [3.2.1.]octanes, including...
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6013242 |
Tropane derivatives with selective binding to the serotonin reuptake transporters for treatment of mental illness and as intermediates in the formation of imaging diagnostic agents for depression
Biologically active derivatives of the tropane ring system are provided which selectively bind either to the 5-HT or DA reuptake site, leading to compounds which have use for the treatment of...
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6008227 |
Process for blocking 5-HT and dopamine uptake with biologically active tropane derivatives
Selective blockade of DA and 5-HT uptake sites with 3-aryltropane derivatives.
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5968926 |
Antipsychotic method
The present invention relates to a novel method for treating a mammal suffering from or susceptible to schizophrenia and schizophreniform diseases.
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5958945 |
Naphthamide derivatives of 3-beta-amino azabicyclo octane or nonane as neuroleptic agents
The invention pertains to novel azabicyclo-naphthalene-carboxamide derivatives, a method for preparing same and the use thereof as a medicament. The compounds of the invention are of formula (I)....
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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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5900418 |
Method for treatment of obesity
A method is provided for the control of obesity comprising administering to a mammal including humans suffering from obesity an acetylcholine esterase reactivator or prodrug derivative thereof...
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5880121 |
4,5-dihydronaphth (1,2-c) isoxazoles and derivatives thereof
4,5-Dihydronaphth 1,2-c!isoxazole derivatives of the general formula: ##STR1## where A, X and n are defined herein are disclosed. Such compounds are useful as serotonin 5-HT 3 antagonists. These...
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5834484 |
Cocaine analogs
Cocaine analogs are disclosed. The analogs, certain 6-alkyl substituted tropane derivatives, bind to the cocaine binding site on dopamine transporter, without interfering with the dopamine...
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5821249 |
Anhydroecogonine compounds and their use as anticholinergic agents
Methylecgonidine (MEG; anhydroecgonine methylester), is produced when cocaine base ("crack") is heated. MEG alone and in combination with cocaine was tested for action on isolated tracheal rings...
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5817621 |
External remedy possessing trophoprotective effect
A dermatological composition for external use comprising a lipid ointment base, vitamin A, a salicylic acid or a derivative thereof, D-camphor, a biogenic GABAergic substance, a biogenic...
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5798363 |
Use for tachykinin antagonists to treat emesis
The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel...
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5770738 |
Esters of bi- and tricyclic amino alcohols, their preparation and their use in pharmaceutical compositions
The new compounds of formula A--O--CO--Z (I) (wherein A and Z are defined as explained in the specification) can be prepared by conventional...
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