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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...
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.
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,...
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 --CHCH-- or S; R 1 is lower alkyl, lower alkoxy or trifluoromethyl; R 2 is hydrogen, lower alkyl, lower alkoxy,...
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...
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...
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....
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-,...
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...
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...
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...
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...
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...
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...
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...
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 ...
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:...
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...
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...
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...
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,...
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...
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...
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...
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...
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...
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,...
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...
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...
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...
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...
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,...
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.
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; ...
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...
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...
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.
4663321 Triazolobenzodiazepines and pharmaceutical use  
Triazolobenzodiazepines of the formula: ##STR1## are disclosed which are antagonists of cholecystokinin (CCK).
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...
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...
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...
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...
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...
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...
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...
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...
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...
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...
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,...
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...