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4985424 |
Certain substituted 1,7-annelated 1h-indazoles being selective antagonists of 5-ht-receptors
The invention relates to a group of new substituted 1,7-annelated 1H-indazole derivatives being strong and selective antagonists of "neuronal" 5-hydroxytryptamine (5-HT) receptors. The compounds...
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4971966 |
Substituted pyrido(2,3-B) (1,4) benzodiazepin-6-ones, and medicaments containing these compounds
New substituted pyrido[2,3-b][1,4]benzodiazepin-6-ones suitable as vagal pacemakers for the treatment of bradycardias and bradyarrhythmias in human and veterinary medicine are described.
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4960770 |
2-alkyl thieno(triazolo)diazepine compounds and pharmaceutical uses thereof
A thienotriazolodiazepine compound of the formula: ##STR1## wherein Ar is phenyl, pyridyl, substituted phenyl or substituted pyridyl; R 1 and R 3 are the same or different and each is hydrogen,...
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4959361 |
Triazolo(4,3-A)(1,4)benzodiazepines and thieno (3,2-F)(1,2,4)triazolo(4,3-A)(1,4)diazepine compounds which have useful activity as platelet activating factor (PAF) antagonists
The invention relates to compounds of the formula ##STR1## wherein X is --CHCH-- or S; R 1 is lower alkyl, lower alkoxy or trifluoromethyl; R 2 is hydrogen, lower alkyl, lower alkoxy,...
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4939139 |
7-chloro-5,6-di hydro-3-(5-(1,2-dihydroxy-isopropyl)-1,2,4-oxadiazol-3-yl)-5-methyl-6-oxo -4H-imidazo[1,5A][1,4]benzodiazepine
A metabolite of the known anxiolytic agent, 7-chloro-5,6-dihydro-3-(5-isopropyl-1,2,4-oxadiazol-3-yl)-5-
methyl-6-oxo-4 H-i midazo[1,5a][1,4]benzodiazepine is a 1,2-dihydroxy derivative of the...
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4939137 |
Ring-fused thienopyrimidinedione derivatives
The synthesis of ring-fused thienopyrimidinedione derivatives is described. The novel ring-fused thienopyrimidinedione derivatives are generally vasodilating agents and antihypertensive agents and...
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4937240 |
Thienotriazolodiazepine compounds and pharmaceutical uses thereof
A thienotriazolodiazepine compound of the formula: ##STR1## wherein each symbol is as defined in the specification or a pharmaceutically acceptable salt thereof, and pharmaceutical uses thereof....
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4929614 |
Benzodiazepines, process and intermediates for the preparation thereof and their application in therapy
Benzodiazepines of formula ##STR1## in which R 1 is H of halogen, R 2 is H or halogen, Ar is indolyl, phenyl, naphthyl, indolyl monosubstituted with a halogen or with a methoxy or phenyl mono-,...
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4914096 |
6-aryl-substituted-4H-thieno(2,3-e)(1,2,4)triazolo(3,4-c)(1,4)diazepines
The invention discloses certain 6-aryl-substituted-4H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,
4]diazepines useful as PAF inhibitors, pharmaceutical compositions containing said compounds as an...
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4912104 |
Tricyclic fused pryimidine derivatives, and their use as pharmaceuticals
Novel tricyclic fused pyrimidine derivatives represented by the formula (I): ##STR1## wherein R 1 and R 2 are independently C 1 -8 alkyl or C 2 -8 alkenyl; R 3 is hydrogen, C 1 -3 alkyl, C 2...
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4904654 |
7-chloro-5,6-dihydro-3-(5-(2-hydroxy-isoprop yl)-1,2,4-oxadiazol-3-yl)-5-methyl-6-oxo-4H-imidazo[1,5a][1,4]benzodiazep ine
A metabolite of the known anxiolytic agent, 7-chloro-5,6-dihydro-3-(5-isopropyl-1,2,4-oxadiazol-3-yl)-5-
methyl-6-oxo-4 H- imidazo[1,5a][1,4]benzodiazepine is a 2-hydroxy derivative of the...
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4900729 |
Thieno-1,4-diazepines
The invention relates to new thieno-1,4-diazepines of general formula ##STR1## wherein R 1 , R 2 , R 3 , R°, R', Z, X, Y and n have the meanings given in the specification. The new compounds are...
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4886797 |
Heterocyclic compounds and their preparation and use
New heterocyclic derivatives having the general formula: ##STR1## wherein X is ##STR2## or CO 2 R' wherein R' is C 1 -6 -alkyl, C 3 -7 -cycloalkyl, or C 1 -3 -alkoxymethyl, and --A-- is --(CH...
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4873081 |
Percutaneous absorption preparation
A percutaneous absorption preparation which comprises calcium salt of an acidic anti-inflammatory or analgesic drug having carboxyl group as the active ingredient and present in an amount of...
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4873076 |
Method of safely providing anesthesia or conscious sedation
A method of inducing anesthesia or conscious sedation while avoiding serious hypotensive episodes comprising the administration of a parenterally active benzodiazpine in conjunction with an opiate...
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4868176 |
Novel imidazobenzodiazepines
A compound selected from the group consisting a compound of the formula ##STR1## wherein R 1 is selected from the group consisting of phenyl, cycloalkyl of 4 to 6 carbon atoms and ##STR2## R 4 ...
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4863920 |
Imidazodiazepine derivatives for treatment of disorders of the central nervous system
A compound for treating disorders of the central nervous system, which is of the formula wherein A taken together with the two carbon atoms denoted by α and β is one of the following groups:...
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4847248 |
1,4-Benzodiazepines with 5- and 6-membered heterocyclic rings and their use as cholecystokinins and gastrin antagonists
Aromatic 1,4-benzodiazepines with fused 5- or 6-membered heterocyclic rings which are antagonists of cholecystokinins and/or gastrin, and are useful in the treatment or prevention of CCK-related...
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4835152 |
1-(4-Aminophenyl)-4-methyl-7,8-methylenedioxy-3,4-dihydro-5H-2,3-b enzodiazepine and acid addition salts thereof same
The invention relates to new 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-3,4-dihydro-5H
-2,3-benzodiaz epi ne of formula (1), optically active isomers and acid addition salts thereof as well as...
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4820703 |
PAF-antagonistic thienotriazolodiazepine compounds and pharmaceutical uses thereof
A thienotriazolodiazepine compound of the formula: ##STR1## wherein A is alkylene or substituted alkylene and each other symbol is as defined in the specification and a pharmaceutically acceptable...
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4808605 |
Tetrahydronaphthalene derivatives as calcium antagonists
Compounds of the formula ##STR1## wherein R is lower-alkyl, R 1 is halogen, R 2 is C 1 -C 12 -alkyl, R 3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy,...
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4783455 |
Substituted pyrimidoindoles and diazepinoindoles useful as hypoglycaemics
Compounds of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R represents lower alkyl or a mono- or bicyclic aryl or heteroaryl radical, R 1 and R 2 which...
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4775671 |
Imidazodiazepines
There is presented compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by α and β signifies one of the groups ##STR2## and the dotted line signifies the double...
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4772599 |
Benzodiazepine derivatives and their preparation and use
New benzodiazepine derivatives of the general formula ##STR1## wherein X 1 and X 2 independently are ##STR2## wherein R 1 is C 1 -3 -alkyl, C 3 -5 -cycloalkyl, C 1 -3 -alkoxymethyl, C 1 -3...
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4761411 |
Dihydrobenzopyrrolobenzodiazepines useful for treating pyschoses
The invention relates to dihydrobenzopyrrolobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF 3 , lower alkyl, lower alkoxy, lower...
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4745112 |
Oxadiazolylimidazobenzodiazepine, compositions, and method III
The application discloses novel benzodiazepine agonist compounds, namely, compounds having the formula ##STR1## wherein X is F, CF 3 , CH 3 , or CN, pharmaceutical compositions thereof, and a...
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4734411 |
Pyrrolizidine compounds, salts thereof, process for the preparation of same and pharmaceutical agents comprising same
Novel pyrrolizidine compounds represented by the formula ##STR1## wherein R is a radical of ##STR2## R 1 is hydrogen, halogen, alkyl group, alkoxy group, alkanoyl group, trifluoromethyl radical,...
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4725596 |
Pyrimidine derivatives having anti-allergy, anti-inflammatory and immuno suppressant activity
Certain pyrimidine derivatives are useful in treating allergic, inflammatory and hyperproliferative skin diseases and in suppressing the immune response. Methods for preparing the compounds and...
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4701325 |
Injectable aqueous solution containing hydrogensulfite and/or sulfite and anticancerous benzodiazepine compound
An alkali metal hydrogensulfite or sulfite is effective for controlling a local injury such as inflammation and vein injury occurring on the injection of an antitumor benzodiazepine compound of the...
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4694003 |
Method of treating depression with 5-(aminoalkyl)-11-phenyl-5H-dibenzo(b,e)(1,4) diazepines
A method of treating depression with 5-(aminoalkyl)-11-phenyl-5H-dibenzo[b,e][1,4]diazepines having the formula: ##STR1## wherein R 1 and R 2 are selected from hydrogen or methyl and X is...
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4687762 |
Water soluble drug complex and method for production of same
The invention provides a method of producing a water-soluble complex comprising a water-insoluble drug and a phospholipid, comprising the steps of (1) dissolving a water-insoluble drug and a...
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4686219 |
11-(Piperazin- or homopiperazin-1-yl)-5H-imidazo-(2,1-C)(1,4)benzodiazepines useful as anti-allergics
Compounds of the formula ##STR1## wherein R 1 and R 2 , which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, trifluoromethyl, hydroxyl, nitro,...
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4673674 |
Diazepinoindoles useful for treating depression, schizophrenia, social withdrawal or anxiety and pharmaceutical compositions containing them
Diazepinoindoles or pharmaceutically acceptable acid addition salts thereof are useful as antidepressant, conflict reducing or neuroleptic agents.
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4670433 |
Oxadiazolyl imidazobenzodiazepine derivatives pharmaceutical compositions thereof, and method of treating therewith
New oxadiazolyl imidazobenzodiazepine derivatives having the formula ##STR1## wherein R 3 has the formula ##STR2## wherein R" is hydrogen, C 1 -6 alkyl C 1 -6 alkoxymethyl or C 3 -6 - cycloalkyl; ...
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4668674 |
(+)-6-chloro-5,10-dihy dro-5-[(1-methyl-4-piperidinyl)-acetyl]-11H-dibenzo[b,][1,4]diazepin-11-o ne, the isolation thereof and its use as a pharmaceutical material
There are described (+)-6-chloro-5,10-dihydro-5-[(1-methyl-4-piperidinyl)-acetyl
]-11H-dibenzo [b,e][1,4]diazepin-11-one, the isolation thereof from a mixture of enantiomers and its use as a...
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4666903 |
Novel use of benzodiazepine antagonist
Benzodiazepine antagonists are used to regenerate the sensitivity response to and prevent tolerance of benzodiazepine which otherwise develops during chronic benzodiazepine exposure. The...
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4666913 |
Hydroxy and aminothiazolyl-benzodiazinone compounds, cardiotonic compositions including the same, and their uses
A method for increasing cardiotonic contractility in humans or other animals using a class of hydroxy and aminothiazolyl-benzodiazinone compounds and pharmaceutical compositions including the same.
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4663321 |
Triazolobenzodiazepines and pharmaceutical use
Triazolobenzodiazepines of the formula: ##STR1## are disclosed which are antagonists of cholecystokinin (CCK).
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4647560 |
New benzodiazepines and their use
The present invention relates to novel benzodiazepines, acid addition salts thereof, processes for their preparation and their use in combating diseases, in particular for the treatment of cerebral...
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4623646 |
PAF-antagonistic diazepines, methods of use
The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I. ##STR1## wherein A is an...
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4622319 |
Methods of using PAF-antagonistic diazepines
The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I or II ##STR1## wherein A...
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4622321 |
Oxadiazolylimidazobenzodiazepine, compositions, and method
The application discloses a novel benzodiazepine agonist compound, namely, 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5,6-dihydro-5-methyl-
6-oxo-4H-imida zo [1,5-a][1,4]benzodiazepine, pharmaceutical...
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4621083 |
PAF-antagonistic diazepines
The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I or II: ##STR1## wherein A...
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4603131 |
Method and composition for treating and preventing irritation of the mucous membranes of the nose
A method and composition for preventing and treating irritation of the mucous membranes of the nose wherein a tricyclic anti-depressant topically applied to the nose is effective prophylactically...
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4595535 |
Diazacycloalkyl-1,2,4-triazolo[2,3-c][1,3]benzodiazepines useful as neuroleptic and/or antihistaminic agents
Described are 5-diazacycloalkyltriazolo[2,3-c][1,3]benzodiazepines, for example compounds of the formula ##STR1## wherein R 1 represents hydrogen, halogen, trifluoromethyl, lower alkylthio, lower...
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4594436 |
Isomeric 2-chloromethyl-1,4-benzodiazepine or 3-chloro-1,5-benzodiazocine compound
[1,2]-fused 1,4-benzodiazepine compounds are disclosed corresponding to the general formula I ##STR1## wherein X is an oxygen or sulfur atom or an optionally substituted imino group, R 1 is a...
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4594190 |
Quaternary salts of dibenzo[1,4]diazepinones, pyrido-[1,4]benzodiazepinones, pyrido[1,5]benzodiazepinones with antiulcer, antisecretory, spasmolytic and antimusarinic activities
Quaternary salts of 11-acyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one, 6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-5-one and...
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4588721 |
Treatment of negative symptoms of schizophrenia
Therapeutic process for treating the negative symptoms of schizophrenia in humans comprising the systematic administration of a compound of the formula ##STR1## X is a member selected from the...
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4585771 |
Antiinflammatory imidazole derivatives
Imidazole derivatives of Formula I ##STR1## wherein AR 1 and AR 2 each independently represent phenyl optionally substituted by halogen atoms, alkyl groups, or alkoxy groups, R 1 is pyrrolyl,...
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4556653 |
Pyrido[1,5]benzodiazepinone derivatives and pharmacological activities thereof
11-Acyl derivatives of 5,11-dihydro-6H-pyrido-[2,3-b][1,4]benzodiazepin-6-one, 6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-5-one and 5,11-dihydro-6H-benzo[2,3-b][1,4]benzodiazepin-6-one, their...
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