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5756508 |
Muscarine antagonists
This invention is concerned with novel 1,3-dihydro-1- 1-(1-heteroarylpiperidin-4-yl)piperidin-4-yl!-2H-benzimidaz olones, derivatives thereof, their preparation, method of use and pharmaceutical...
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5753673 |
Quinolinecarboxylic acid derivatives
Quinolinecarboxylic acid derivatives represented by the following formula: ##STR1## wherein C is hydroxymethyl, methoxy, ethoxy or morpholinyl, or pharmaceutically acceptable salts thereof exhibit...
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5750537 |
Use of 5HT.sub.3 antagonist to treat impotence
An impotence remedy containing a 5HT 3 antagonist as the active ingredient.
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5736556 |
Tropane-2-aldoxime derivatives as nevro transmitter reuptake inhibitors
The present invention discloses compounds of the formula, ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R 3 , and R 4 each have the meanings set forth in...
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5733917 |
Heterocyclic compound
Endo-(8-methyl-8-azabicyclo 3.2.1!oct-3-yl) 1-isopropyl-2(1H)-quinolone-3-carboxylate represented by Formula (I): ##STR1## or an acid addition salt thereof acts on a serotonin 4 receptor thereby to...
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5712287 |
Method of treating urinary bladder dysfunctions
The present invention relates to a novel method for treating a mammal suffering from urinary bladder dysfunctions.
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5712284 |
Azalicyclooctane derivatives as anti-arrhythmic agents
A compound of formula (I) or a salt thereof, or a solvate thereof: ##STR1## wherein B represents a C 1 -4 n-alkylene group wherein each carbon is optionally substituted by a C 1 -6 alkyl group; Z...
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5710168 |
2-piperidino-1-alkanol derivatives as neuroprotective agents
A method of blocking N-methyl-D-aspartic acid (NMDA) receptor sites in a mammal in need thereof with an effective NMDA blocking (neuroprotective and antiischemic) amount of 2-piperidino-1-alkanol...
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5703108 |
Bone deposition by certain prostaglandin agonists
Methods for the treatment of bone disorders utilizing certain prostaglandin agonists/antagonists.
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5698179 |
Iodinated neuroprobe for mapping monoamine reuptake sites
An iodinated neuroprobe is provided for mapping monoamine reuptake sites. The iodinated neuroprobe is of the formula: ##STR1## wherein: R=aryl, substituted aryl, heterocyclic, CO(CH 2 ) n Y, (CH 2...
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5686463 |
Oxadiazoles useful in the treatment of senile dementia
A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring, and substituted on the other ring carbon atom with a substituent of low...
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RE35593 |
Azabicylo oxime compounds
A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R 1 represents ##STR2## in which each of p and q independently represents an integer of 2 to 4, r...
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5637596 |
Azabicycloalkyl derivatives of imidazo[1,5-a]indol-3-one and process for their preparation
Novel 5-HT 3 receptor antagonist compounds having the general formula (I) ##STR1## wherein each of R, R 1 and R 2 , which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C 1 ...
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5629307 |
Use of ibogaine in reducing excitotoxic brain damage
This invention discloses that ibogaine, a plant derivative, can be used as a safe NMDA antagonist at relatively high dosages (including dosages high enough to cause hallucinations), to reduce or...
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5610164 |
(Thiophen-2-yl)-piperidin or tetrahydropyridin azabicyclocarboxamides
This invention provides compounds having the structure ##STR1## wherein R is hydrogen, alkyl, alkenyl, alkynyl, --COR 2 , phenyl, or phenylalkyl; the dotted line represents an optional double bond;...
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5583142 |
Analgesic and nootropic drugs
Compounds of general formula: ##STR1## where: Ar=phenyl or beta-naphtyl, or aromatic heterocyclic 6-membered ring containing one or two nitrogen atoms; R 1 =one or more substituents of the Ar...
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5580883 |
Aminobenzene compounds to prevent nerve cell degradation
A compound useful for central antioxidant having inhibitory activity of degeneration and necrocytosis of cerebral cells of the formula (I): ##STR1## wherein A and B are independently (1) a group of...
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5574043 |
Certain [1,2,5-thiadiazol-4-yl]-1-azabicyclo [3.2.1]octane derivatives and their pharmaceutical uses
The present invention relates to therapeutically active azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are...
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5563148 |
Specific 5-HT3 antagonists
This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia,...
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5554626 |
Substituted heterocyclic compounds as dopamine-reuptake inhibitors
The present invention discloses compounds of the formula ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R 3 , and R 4 each have the meanings set forth in...
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5552407 |
Anhydroecgonine 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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5552408 |
Benzimidazoline-2-oxo-1-carboxylic acid derivatives useful as 5-ht receptor antagonists
A method for treating a human host suffering from psychosis, which method comprises administering to such host a therapeutically effective amount of a compound of the formula I ##STR1## wherein the...
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5530008 |
Use of 5-HT.sub.3 receptor antagonists in treating panic disorders or obsessive compulsive disorders
5-HT 3 Receptor antagonists are useful in treating panic disorders or obsessive compulsive disorders.
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5525613 |
Covalently coupled benzoylecgonine ecgonine and ecgonidine
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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5523299 |
5-(2-oxyphenyl)-pyrrole derivatives as dopamine D.sub.3 receptor antagonists
Compounds of formula (I), ##STR1## wherein R 1 represents C 1 -4 alkyl; and R 2 , R 3 , R 4 and R 5 each independently represent hydrogen, halogen, C 1 -4 alkyl, C 1 -4 alkoxy, C 1 -4 alkoxyC 1...
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5521183 |
Use of 5-HT ligands as anti-pruritic agents
The present invention is based on the finding that 5-HT receptor ligands are useful in treating experimental models of clinically encountered pruritus (itch). A 5-HT ligand as used in this...
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5480651 |
Composition and method for treating nicotine craving in smoking cessation
A method for relieving craving in a nicotine-habituated patient and a composition for treating the patient is provided. The composition administered has a non-specific acetylcholine agonist and a...
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5468758 |
Crystalline forms of endo-2,3-dihydro-N-(8-methyl)-8-azabicyclo[3.2.1]oct-3-yl)-2-oxo-1H-benz imidazole-1-carboxamides
Crystalline and pharmacologically active monohydrates of endo-2,3-dihydro-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2-
oxo-1H-benzimi dazole-1-carboxamide hydrochloride and of...
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5444070 |
Phenyl substituted heterocyclic compounds
The present invention discloses compounds of the formula ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R 3 , and R 4 each have the meanings set forth in...
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5436255 |
Method of treating diseases susceptable to treatment by blocking NMDA-receptors
3-Piperidino-1-chromanol derivatives and analogs having the formula ##STR1## wherein A and B are taken together and are --CH 2 CH 2 -- or A and B are taken separately and are each H; X is CH 2...
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5436251 |
Treatment of anxiety and gastrointestinal disorders with azabicyclo carbonyl-2-(cyclopropylmethyloxy)benzamide
(Endo)-N-[[[8-azabicyclo[3.2.1]octan-3-yl]amino]carbonyl]-2-
(cyclopropylmet hyloxy)benzamide and pharmaceutically acceptable salts thereof possess 5-HT 3 antagonistic activity and are useful in...
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5416092 |
3-azabicyclo[3.2.1]-oct-8-yl-terminated non-peptidyl α-succinamidoacyl aminodiols as anti-hypertensive agents
Non-peptidyl compounds characterized generally as α-succinamidoacyl aminodiols having a 3-azabicyclo[3.2.1]-oct-8-yl-type group at the N-terminus are useful as renin inhibitors for the treatment...
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5411968 |
Treatment of anxiety
The invention relates to the use of compounds which act as 5-hydroxytryptamine (5-HT) antagonists at 5-HT "M" receptors in the treatment of anxiety.
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5401750 |
Derivatives of substituted imidazol-2-one and process for their preparation
Derivatives of 1-phenyl-3-azabicycloalkylimidazolidin-2-ones are provided of general formula (I) ##STR1## in which inter alia R 3 represents a group ##STR2## wherein n is an integer of 1 or 2 and...
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5399562 |
Indolones useful as serotonergic agents
This invention relates to compounds of the formula: ##STR1## which are useful as 5-HT 4 agonists or antagonists and 5-HT 3 antagonists.
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5395832 |
Benzamide derivatives
A benzamide derivative represented by the following formula: ##STR1## wherein R 1 represents a hydrogen atom or a lower alkanoyl group; R 2 represents a hydrogen atom or a halogen atom; R 3 ...
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5393767 |
Insect control with substituted triazole and tetrazole compounds
Insects, especially sucking insects, such as brown planthoppers, and phytophageous mites, such as two-spotted spider mites, are controlled by applying an triazole or tetrazole compound substituted...
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5389643 |
Aminobenzoic acid derivatives useful for treating gastro-intestinal conditions
An aminobenzoic acid derivative represented by the following general formulas (I), (I-2) or (I-3), or a pharmacologically acceptable salt thereof, which exhibits a serotonin antagonism and an...
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5380738 |
2-substituted oxazoles further substituted by 4-fluorophenyl and 4-methylsulfonylphenyl as antiinflammatory agents
2-Substituted-4-(4-fluorophenyl)-5-(4-(methylsulfonyl)phenyl
)oxazoles or 2-substituted-5-(4-fluorophenyl)-4-(4-(methylsulfonyl)phenyl
)oxazoles and derivatives thereof are found to posses...
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5376667 |
Derivatives of benzoylecgonine, ecgonine and their multiple pharmacological properties
The present invention relates to a novel class of benzoylecgonine, ecgonine and ecgonidine derivatives which are useful for preventing and treating immunoregulatory disorders, neuromuscular...
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5374636 |
2,3-trans-disubstituted tropane compounds which have useful pharmaceutical utility
The present invention discloses compounds of the formula ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R 3 , and R 4 each have the meanings set forth in...
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5369113 |
Certain 2,3-diphenyl-2-(1,2,4-oxadiazol-5-yl)tropanes useful as dopamide reuptake inhibitors
The present invention discloses compounds of the formula ##STR1## any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein R, R 3 , and R 4 each have the meanings set forth in...
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5364863 |
Specific 5-HT.sub.3 antagonists
This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia,...
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5356905 |
Neuroprotective 3-piperidino-4-hydroxychroman derivatives and analogs
3-Piperidino-1-chromanol derivatives and analogs having the formula ##STR1## wherein A and B are taken together and are --CH 2 CH 2 -- or A and B are taken separately and are each H; X is CH 2...
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5334599 |
Heteroaryl-8-azabicyclo[3,2,1]octanes as antipsychotic agents, 5-HT.sub.3 receptor antagonists and inhibitors of the reuptake of serotonin
This invention relates to compounds of the formula ##STR1## where X is --O--, --S-- or --NH--; Y is hydrogen, halogen and loweralkoxy; p is 1 or 2; n is 2, 3 or 4; R is hydrogen,...
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5330990 |
Substituted urea compounds and their preparation and use
New substituted urea compounds of formula I, or a pharmaceutically acceptable salt thereof: ##STR1## wherein R 1 is a group of formula II, III or IV ##STR2## where n is 2 or 3, p is 1 or 2, q is 1...
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5324723 |
Oxazoles and thiazoles for the treatment of senile dementia
1,3-Oxazole and 1,3-thiazole compounds of formula I, and their pharmaceutically acceptable salts and prodrugs: ##STR1## wherein X represents oxygen or sulphur; R 1 represents a non-aromatic...
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5288731 |
2,6-methano-2H-1-benzoxocincarboxylic acids, esters and amides
Novel compounds which are 2,6-methano-2H-1-benzoxocincarboxamides having 5-HT 3 -antagonist properties including unique CNS, antiemetic and gastric prokinetic activities and which are void of any...
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5262427 |
3-substituted and optionally 1-substituted azacyclic or azabicyclic compounds, pharmaceutical compositions, thereof and their use as stimulants of cognitive functions
Azacyclic compounds selected from the group consisting of ##STR1## wherein R 1 is H or C 1 -6 -alkyl R 3 is ##STR2## wherein R' is C 3 -8 -alkyl, cyclopropyl, C 4 -8 -cycloalkyl, benzyl which...
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5256670 |
N-aryl-3-aryl-4-substituted- 2,3,4,5-tetrahydro-1H-pyrazole-1-carboxamides, insecticidal compositions containing such compounds and methods of controlling insects such compounds
This invention relates to N-aryl-3-aryl-4-substituted-2,3,4,5-tetrahydro-1H-pyrazole-1
-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of...
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