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5254591 |
Pharmaceutical composition for treating gastroesophageal reflux
A pharmaceutical composition useful for treating gastroesophageal reflux comprising oxethazaine and a carrier selected from alginic acid and alginates.
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5248684 |
Certain 2-oxo-quinoline carboxylates or corresponding carboxamides useful as anti-emetics and suppressants of migraine
There is disclosed a heterocyclic compound represented by general formula: ##STR1## wherein R 1 represents hydrogen, lower alkyl or aryl; R 2 represents hydrogen, hydroxyl or lower alkyl; A...
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5244909 |
Methods for the treatment of cognitive disorders
The invention relates to the use of certain compounds which act as antagonists of 5-hydroxytryptamine (5-HT) at 5-HT 3 receptors for the treatment of cognitive disorders such as attentional and...
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5242927 |
Prodrugs for oxadiazole muscarinic agonists
A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring and on the other ring carbon atom with a substituent which is convertible...
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5234931 |
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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5223511 |
Benzimidazoline-2-oxo-1-carboxylic acid compounds useful as 5-HT receptor antagonists
New pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid derivatives which are 5-HT receptor antagonists useful as antiemetic agents and as gastric prokinetic agents of the following...
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5217987 |
Dopamine uptake inhibitors in reducing substance abuse and/or craving
Mazindol and other nonreinforcing dopamine uptake inhibitors are effective to lessen craving for abused substances.
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5200413 |
Indolyl carboxamides useful treating migraine, cluster headache, trigeminal neuralgia or emesis
Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH; X and Y are independently selected from hydrogen or C 1 -4 alkyl, or together are a bond; R 1...
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5185343 |
Nortropyl-1-alkanol derivatives as antiischemic agents
2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH=CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y 1 are taken...
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5126364 |
4-amino-5-chloro-n-(2-pyrrolidinylmethyl)-2,3-dihydrobenzo[b]fura n-7-carboxamide and pharmaceutical compositions containing the same
The compound (R) (-)-4-amino-5-chloro-N-(2-pyrrolidinylmethyl)-2,3-dihydroben
zo[b]furan-7-c arboxamide; the S isomer thereof, and pharmaceutical compositions containing the same.
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5106843 |
Heterocyclic compounds useful as 5-HT.sub.3 antagonists
Aryl ureas and carbamic acid derivatives of formula A--NHCW--Y--B and pharmaceutically acceptable salts thereof wherein A is a specified aromatic radical including 3,5-dichlorophenyl W is O...
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5096901 |
Pharmacologically active amides and esters containing an azabicycloalkane moiety
Compounds of formula ##STR1## wherein R 1 is hydrogen or one or more specified substituents, X is --O-- or --NR 2 -- where R 2 is lower alkyl, lower alkenyl, lower alkynyl, aryl or specified...
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5075314 |
Antimicturition composition and novel method
A wafer, capsule or pill contains an antimuscarinic agent in controlled amounts for oral administration to housebreak domestic animals to effect bladder control.
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5075312 |
Novel anti-micturition composition and method
A wafer, capsule or pill contains an antimuscarinic agent in controlled amounts for oral administration to housebreak domestic animals by preventing nighttime urination.
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5070094 |
N-benzyltropaneamides
N-benzyl tropane amides, which have activity as Class III antiarrhythmic agents, acting by prolonging cardiac action potential repolarization. The invention further provides for compositions...
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5066663 |
Substituted-hetero-cyclopentanones and cyclopentenones and derivatives thereof acting at muscarinic receptors
Substituted-hetero-cyclopentanones and cyclopentenones and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as...
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5066662 |
Substituted oxazolidin-2-ones and 1,2,4-oxadiazolin-5-ones and derivatives thereof acting at muscarinic receptors
Oxazolidin-2-ones and 1,2,4-oxadiazolin-5-ones substituted in the 4-position of the oxazolidin-2-one ring and the 3-position of the 1,2,4-oxadiazolin-5-one ring with a 5- or 6-member...
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5066665 |
Substituted isoxazolidin-3-ones and derivatives thereof acting at muscarinic receptors
Substituted isoxazolidin-3-ones and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting...
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5063230 |
Substituted saturated and unsaturated indole quinoline and benzazepine carboxamides and their use as pharmacological agents
This invention relates to a series of bicyclic benzomonoazacyclic carboxamide compounds of the general formula: ##STR1## Where Z is tertiary amine, which are useful for the method of treating...
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5045546 |
8-azabicyclo[3.2.1]octylalkylthiazolidines
Novel 8-azabicyclo[3.2.1]octylalkylthiazolidinones of the formula ##STR1## where R 1 , R 2 , R 3 , R 4 , m, x and y are defined herein, process for the preparation thereof, and methods of treating...
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5039528 |
EAA antagonists as anti-emetic drugs
This invention relates to a method and a class of pharmaceutical agents for suppressing vomiting, nausea, and other emetic symptoms. The method involves administering to a susceptible mammal a...
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5036057 |
Method of treating gastroesophageal reflux
A pharmaceutical composition comprising a local anaesthetic adapted to inhibit relaxation of the lower oesophageal sphincter and a carrier therefor comprising a material adapted to float on...
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5030637 |
Anisodamine to prevent and treat eye disease
A method is disclosed for the prevention and alleviation of pathologic changes in the eye such as diabetic retinopathy or senile macular degeneration. The claimed method involves the parenteral...
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5006533 |
Certain 3-bromo-2,6-dimethoxybenzamides and pharmaceutical use thereof
3-Bromo-2,6-dimethoxybenzamides useful as neuroleptic agents are described.
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5001133 |
Benzoic acid derivatives
The substituted benzoic acid heterocyclic amides and esters are serotonin M antagonists. Included are compounds of the formula Iq ##STR1## wherein R 1 , R 2 , R 3 , Z' and R 8 ' have various...
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4997839 |
2-quinolyl ethers
Novel ethers of formula ##STR1## their heteroaromatic N-oxides, and the pharmaceutically acceptable acid additions of the compounds of formula (I) and their N-oxides possess 5-HT 3 -antagonistic...
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4988691 |
Isoxazole containing compounds exhibiting anti-serotonin activity
Compounds of formula ##STR1## (wherein R, R 1 , R 2 and Y have the meanings indicated in the description), a process for the preparation thereof and pharmaceutical compositions containing them as...
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4973588 |
Imidazole derivatives having anti-hypoxia properties
A novel N-substituted imidazole or thioimidazole derivative and a pharmacologically acceptable acid addition salt thereof, which have a brain function-improving action, are disclosed. The...
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4952586 |
Edrophonium-atropine composition and therapeutic uses thereof
A composition is provided which includes a balanced combination of an edrophonium component and an atropine component. A preferred embodiment has 0.5 mg of edrophonium chloride and 8 micrograms of...
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4952587 |
Physiologically active 1,2,4,-oxa- and thiadiazoles
The present invention provides a compound of formula I or a salt or prodrug thereof: ##STR1## wherein the dotted circle represents one or two double bonds in any position in the 5-membered ring; ...
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4937247 |
1-acyl indazoles
Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CH or N; Y is NH or O; R 1 is hydrogen or halogen; R 2 is a group of formula (a), (b) or (c)...
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4937236 |
Anxiolytic N-substituted benzamides
A method of treating anxiety including administering to a person to be treated an effective amount of compounds of the general formula: ##STR1## wherein the various substituents are defined...
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4935413 |
Carbamate physical property-improving reagent
A physical property-improving reagent which comprises an alkenoylcarbamate compound of the formula: ##STR1## wherein R is a hydrogen atom or a lower alkyl group, X is an oxygen atom (--O--), a...
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4929625 |
Ethers
Novel ethers of formula ##STR1## their heteroaromatic N-oxides, and the pharmaceutically acceptable acid additions of the compounds of formula (I) and their N-oxides possess 5-HT 3 -antagonistic...
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4921860 |
Quinuclidyl- and tropanyl-pyridyl ethers as 5-HT.sub.3 receptor antagonists
Pyridyl ethers of formula ##STR1## [where R is hydrogen, or 1 to 4 hydroxy, alkyl, alkoxy, amino, alkylamino, dialkylamino, halogen, trifluoromethyl, phenyl, halophenyl, alkyphenyl, alkoxyphenyl,...
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4920127 |
Substituted indoles and their use as 5-HT.sub.3 receptor antagonists
Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O; R 1 is hydrogen, fluoro or chloro; R 2 and R 5 are independently hydrogen or C 1 -6...
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4898860 |
Anticonvulsant composition and method
An anticonvulsant composition comprising as an active ingredient an amount effective for controlling seizures in mammals of a compound selected from the group consisting of dextromethorphan and...
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4891378 |
Nortropanyl containing pyrrolidinones, pharmaceutical compositions and use
The invention relates to new substituted pyrrolidinones of general formula ##STR1## wherein R 1 represents a phenyl group which may be mono- or di-substituted by methyl, methoxy, fluorine,...
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4889849 |
Spasmolytically active tertiary amine derivatives
The invention relates to new spasmolytically active tertiary amine derivatives and the salts thereof, of the formula (1) ##STR1## wherein the symbols have the following meanings: .circle.A is...
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4888353 |
Carboxamides useful as antiemetic or antipsychotic agents
Carboxamides represented by the formula (I): ##STR1## wherein Z represents the carbon atoms necessary to complete a 5- to 7-membered ring, R 1 , R 2 , and R 3 may be the same or different and...
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4886808 |
Indazolyl carboxylic acid amides useful for treating migraine clusters headache, trigeminal neuralgia or emesis
Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CO and Y is NH; Z is NR 3 wherein R 3 is hydrogen, C 1 -6 alkyl, C 3 -7 alkenyl-methyl, phenyl or...
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4882327 |
Certain heterocyclic N-substituted carboxamides
Compounds of formula (I), or a pharmaceutically acceptable salt thereof: Y-CO-L-Z (I) wherein L is NH or O; Y is a group of formula (a), (b)...
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4877780 |
Antiemetic N-substituted benzamides
Compounds of the general formula: ##STR1## wherein the various substituents are defined hereinbelow have pharmacological properties rendering them useful as antiemetic agents with reduced...
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4871744 |
Certain 2,3-dihydro-indole-1-carboxamido-N-[8-azabicyclo(3.2.1)octan-3-yl]d e
Compounds of formula (I) and pharmaceutically acceptable salts thereof; ##STR1## wherein L is NH or O; X and Y are independently selected from hydrogen or C 1 -4 alkyl, or together are a bond; ...
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4851407 |
Novel treatment
A method of treatment of emesis, anxiety and/or IBS in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or (II) or a pharmaceutically...
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4826838 |
Analgesic carbocyclic and heterocyclic carbonylmethylene-and carbonylmethypipidines and-pyrrolidines
Carbocyclic and heterocyclic carbonylmethylene- and carbonylmethylpiperidines and -pyrrolidines are serotonin antagonists.
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4822795 |
Pharmaceutically useful esters and amides
Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O; X is N or CR 3 wherein R 3 is hydrogen or C 1 -6 alkoxy; Y is N or CR 4 wherein R 4 ...
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4808588 |
Heterocyclic ureas and carbonates useful as pharmaceuticals
Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein: Het is monocyclic heteroaryl having two adjacent carbon atoms, a and b, depicted in formula (I); p1 R 1 ...
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4808582 |
New cinnamoic compounds, the process for preparing same and the use thereof in therapeutics
Compounds of formula: ##STR1## wherein: Ar is an aromatic group; R and R 1 are H or CH 3 ; A represents a nitrogenized heterocyclic radical; B is OH or forms with the adjacent CO group, either an...
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4803199 |
Pharmaceutically useful heterocyclic and carbocyclic acid esters and amides of alkylene bridged piperidines
The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.
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