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5739129 |
CCK or gastrin modulating 5-heterocyclic-1, 5 benzodiazepines
Compounds of general formula (I) and physiologically salts thereof, processes for their preparation and their use as modulators of the effects of gastrin and CCK.
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5733867 |
1, 5-benzodiazepine derivatives
Compounds of general formula (I) ##STR1## wherein R 1 represents a phenyl, C 3 -7 cycloalkyl, C 7 -11 bridgedcycloalkyl or C 1 -6 alkyl group which alkyl group may be substituted by a hydroxy,...
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5726171 |
N-(1-alkyl-5-phenyl-2,3,4,5-tetrahydro-1H-benzo B! 1,4!diazepi n-3yl)-acetamides
This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.
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5719141 |
2,9-diamino- and 2-amino-8-carbamoyl-4-hydroxy-alkanoic acid amide derivatives
Compounds of the formula I ##STR1## in which R 1 is arylamino, N-aryl-N-(lower alkoxy-lower alkyl)-amino, N-aryl-N-aryl-lower alkyl-amino or heterocyclyl bonded via a ring carbon atom, X is a...
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5719143 |
Polysubstituted 3-acylamino-5-phenyl-1, 4-benzodiazepin-2-one derivatives, process for their preparation and the pharmaceutical compositions containing them
The invention relates to the compounds of formula (I) ##STR1## in which R I , R II , X 1 , X 2 , X 3 and X 4 are as defined in claim 1.
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5716953 |
1,5-benzodiazepine derivatives
Compounds of formula (I) ##STR1## wherein the substituents are defined in the specification are antagonists of gastrin and CCK.
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5700797 |
N-(2,4-dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3-yl)-3-amides
This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.
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5696110 |
Benzodiazepine derivatives and their use as antagonists of cholecystokinin and/or gastrin receptors
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5696116 |
Pharmaceutical composition which contains a renin angiotensin system inhibitor and an endothelin antagonist
A pharmaceutical composition suitable for the treatment of cardiovascular disorders is described which comprises an inhibitor of the Renin Angiotensin System and an endothelin antagonist.
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5693637 |
Bicycle derivatives, their preparation and use
The description relates to bicyclene derivatives of formula (I) in which A, B, D, E, G, K, L, R 1 , R 2 , Z 1 and Z 2 have the meanings given in the description, and their production. These...
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5691331 |
N-(2,4-Dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3yl) -3- amides
This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.
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5686449 |
1,5-benzodiazepines useful as gastrinor CCK-antagonists
The invention relates to compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof having gastrin and/or CCK-B antagonist activity.
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5679671 |
Amino acid derivative
The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase...
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5679650 |
Pharmaceutical compositions including mixtures of an adenosine compound and a catecholamine
A purine compound, which has a desired and an undesired effect when a dosage sufficient to induce the desired effect is administered to a mammal, is combined with a counteracting agent, wherein the...
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5679673 |
Aralkyl bridged diazabicycloalkane derivatives for CNS disorders
Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula:...
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5674865 |
Nonpeptidyl integrin inhibitors having specificity for the GPII.sub.b III.sub.a
A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII b III a receptor and is...
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5658901 |
2,3-dihydro-1-(2,2,2,-trifluoroethyl)-2-oxo-5-phenyl-1H-1,4-benzo diazepines
This invention is concerned with novel compounds represented by structural formula I ##STR1## where X and Y are independently hydrogen, chloro, fluoro, bromo, iodo, or trifluoromethyl and n is 0, 1...
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5654294 |
Spiro lactam dual action inhibitors
Compounds of the formula ##STR1## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular...
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5654298 |
Amine derivatives
This invention concerns novel aminopyridinium compounds of the formula I wherein R 1 , R 2 , R 3 , R 5 and R 6 are selected from the following combinations: ##STR1## (a) one of R 2 and R 6 is a...
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5646140 |
1,5-benzodiazepine derivatives having CCK antagonistic or agonistic activity
This invention pertains to novel benzodiazepine compounds of formula (I) ##STR1## which exhibit agonistic activity for CCK-A receptors, enabling them to modulate the hormones gastrin and...
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5641775 |
3-phenylureido-1,5-benzodiazepine-diones useful as gastrin or antagonists
The invention relates to 3-phenylureido-1,5-benzodiazepine-diones of formula (I) ##STR1## and pharmaceutically acceptable salts and solvates thereof, and to their use as gastrin/CCK-B antagonists.
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5641773 |
Methods for treating viral infections
The present invention includes, inter alia, methods of treating cells infected with a virus capable of causing an immunodeficiency disease and related pharmaceutical compositions.
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5639751 |
N-acyl-2,3-benzodiazepine derivatives for treating acute and chronic neurodegenerative disorders
The invention relates to novel N-acyl-2,3-benzodiezapine derivatives of the general formula (I), their stereoisomers and acid-addition salts, pharmaceutical compositions containing them and a...
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5639745 |
Fused-bicyclic lactams as interleukin-1β converting enzyme inhibitors
Disclosed are compounds, compositions and methods for inhibiting interleukin-1β protease activity. The compounds, bicyclic derivatives of aldehydes and α-substituted methyl ketones, have the...
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5637585 |
Crystal form of benzodiazepine derivatives
This invention provides the form B crystal of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo-5-phenyl-1H-1
,4-benzodiazep in-3-yl]-3-(3-tolyl)urea which is produced by recrystallizing the compound...
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5635504 |
Diazepine containing dual action inhibitors
Compounds of the formula ##STR1## wherein: ##STR2## A is are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors.
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5633251 |
N-2,3-dihydro-1-(2-propyl)-2-oxo-5-phenyl-1h-1,4-benzodiazepines
This invention is concerned with novel compounds represented by structural formula I ##STR1## where R 1 is ##STR2## X and Y are independently hydrogen, fluoro, chloro, bromo, iodo, or...
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5631251 |
5-cyclopropyl-1,4 benzodiazepine-2-ones
This invention is concerned with novel compounds represented by structural formula I ##STR1## Z is C 0 -6 alkyl; and R 1 is phenyl or mono or disubstituted phenyl, where the substitutents are Cl,...
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5629310 |
Low dose temazepam
This invention relates to a hard gelatin capsule containing no more than 5 to 10 milligrams of crystalline temazepam and its use in the treatment of transient insomnia.
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5624922 |
Aryl-fused and hetaryl-fused-2,4-diazepine and 2,4-diazocine antiarrhythmic agents
Aryl-fused- and hetaryl-fused-2,4-diazepines of formula XXXVI, benzodiazocines of formula XXX, benzodiazepines of formula II ##STR1## δ-aminoamides of formula III and aryldimethanamines of formula...
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5624921 |
Hypotriglyceridemic aminoacetylmercapto derivatives
The present invention relates to the use of certain aminoacetylmercapto derivatives in treating patients suffering from hypertriglyceridemia, atherosclerosis and hypercholesterolemia.
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5620975 |
Pharmaceutical composition and method for the control of hypertension
Pharmaceutical composition comprising a tetrahydronaphthalene derivative of the formula ##STR1## wherein R 1 is halogen, R 2 is lower-alkoxy-lower-alkylcarbonyloxy, X is C 2 -C 8 -alkylene and...
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5618811 |
Tetrahydro-1H-benzazepinones and hexahydroazepinones as selective cholecystokinin-B receptor antagonists
This invention relates to compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 and X are as defined in the application. These compounds are CCK-B receptor antagonists and are useful in the...
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5614509 |
Pharmaceutical agents for preventing the development of tolerance during the treatment with benzodiazepine-receptor-binding active ingredients
The use of NMDA receptor antagonists or their physiologically compatible salts for preventing the development of tolerance during the long-term treatment with benzodiazepine-receptor-binding active...
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5612335 |
Cyclic compounds and pharmaceutical compositions containing them
The invention relates to cyclic derivatives of general formula ##STR1## wherein R a , R b , X and Y are as defined in claim 1, the tautomers, the stereoisomers including the mixtures thereof and...
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5602125 |
Thienodiazepine derivatives as cholecystokinin and gastrin antagonists
Thienodiazepine compounds of formula (1) wherein: R 1 represents H, optionally substituted C 1 -6 alkyl or C 3 -7 cycloalkyl; R 2 represents optionally substituted phenyl; or R 2 represents a...
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5602122 |
Method for lowering total serum cholesterol and treating hypercholesterolemia with aminoacetylmercapto derivatives
The present invention relates to the use of certain aminoacetylmercapto derivatives in treating patients suffering from hypercholesterolemia.
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5599813 |
Thiazolopyrimidine derivatives
Thiazolopyrimidine derivatives represented by the formula ##STR1## and salts thereof are provided, which are characterized by a carboxamide residue substituted with R 4 and R 5 . The derivatives...
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5597818 |
Methods of treating cardiac arrhythmia
Benzodiazepine analogs have been found to be useful in treating cardiac abnormalities.
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5595990 |
Antiarrhythmic benzodiazepines
Benzo-(1,5)-diazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia. The compounds have structural formulae: ##STR1##
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5585376 |
1,5-benzodiazepine derivatives having CCK and/or gastrin antagonistic activity
The present invention relates to compounds of general formula (I) ##STR1## and physiologically acceptable salts thereof wherein the group NR 1 R 2 represents a 5-7 membered saturated heterocyclic...
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5580895 |
1,5-benzodiazepine derivatives
The present invention relates to compounds of formula (I) which are antagonists of gastrin and CCK-B receptors. The compounds of formula (I) are 1,5-benzodiazepine derivatives. ##STR1##
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5569654 |
Benzodiazepinones
Compounds of general formula (I) ##STR1## and physiologically acceptable salts thereof; wherein R 1 represents CH 2 CONR 5 R 6 or CH 2 COR 7 ; R 2 represents a phenyl group optionally...
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5563144 |
Antiserotonins, their preparation and pharmaceutical compositions containing them
This invention relates to compounds having the formula R 1 -(CH 2 ) n -Het wherein R 1 is a residue having the formula (B), (C), (D); Het represents a radical phenyl-4 tetrahydro-1,2,3,6...
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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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5563136 |
3-Ureidobenzodiazepinones useful as antagonists of CCK or of gastrin
This invention relates to compounds having formula (I), ##STR1## wherein R 1 is a hydrogen or halogen atom or an alkyl, alkoxy, alkylthio, nitro, hydroxy or cyano radical; R 2 is an alkyl radical...
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5554600 |
Methods for inhibiting endometriosis
The present invention provides a method for inhibiting endometriosis comprising administering to a woman in need of treatment an effective amount of a compound of formula I ##STR1## wherein R is...
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5550124 |
Use of peripheral-type benzodiazpine sites for treatment of CNS trauma or disease
It is a purpose of this invention to provide a means of treating various central nervous system (CNS) injuries to prevent or minimize damage to the CNS. A novel use has been found for some...
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5550126 |
Central cholecystokinin antagonists having pharmaceutical activity
Pharmaceutical compositions and methods of using CCK-ligands D,L-glutamic acid and D,L-aspartic acid as antipsychotic, antianxiety, and agents useful in treatment or prevention of withdrawal...
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5541182 |
Benzodiazepine aryl urea derivatives
This invention relates to novel benzodiazepine derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof, ##STR1## (wherein R 1 is an aryl group, or...
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