Abstract: The present invention provides a process for the synthesis of compounds of formula (II) or pharmaceutically acceptable salts thereof.

Abstract: The invention is concerned with hydroxymethyl-imidazodiazepines and their esters of general formula I. These compounds can be used as anxiolytic and/or anticonvulsant and/or muscle relaxant and/or sedative-hypnotic active substances.

Abstract: There are provided novel compounds of formula (I) ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined in the specification and optical isomers and racemates thereof and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy.

Abstract: Vitronectin receptor antagonists having the formula: ##STR1## which are useful for the treatment of inflammation, cancer and cardiovascular disorders, such as atherosclerosis and restenosis, and diseases wherein bone resorption is a factor, such as osteoporsis.

Abstract: Tricyclic diazepines of the formula: wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.

Abstract: The present invention discloses new processes in the preparation of midazolam (VII), ##STR1## a commercially important pharmaceutical, as well a new intermediates in those processes from a known benzophenone (I) starting material.

Abstract: Compounds of the formula (1) ##STR1## wherein X and Y are each N or NH, Z is O or OH, (1) when X=N and Y=NH, Z=O, and *1 and *3 are double bonds, (2) when X=NH and Y=N, Z=O, and *2 and *3 are double bonds, (3) when X=N and Y=N, Z=OH, and *2 and *4 are double bonds, and R is a side chain derived from an amino acid; for example, the amino acid is glycine with R=H, alanine with R=CH.sub.3, glutamic acid with R=CH.sub.2 CH.sub.2 COOH, lysine with R=CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, or leucine with R=CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3, and/or an analogues thereof are useful for imparting a "thick, sour" taste to foods.

Abstract: The present invention discloses new processes in the preparation of midazolam (VII), ##STR1## a commercially important pharmaceutical, as well a new intermediates in those processes from a known benzophenone (I) starting material.

Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.

Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.

Abstract: Imidazolinobenzodiazepines are cholecystokinin B (CCK-B) antagonists useful as anxiolytic agents.

Abstract: The present invention discloses new processes in the preparation of midazolam (VII), ##STR1## a commercially important pharmaceutical, as well a new intermediates in those processes from a known benzophenone (I) starting material.

Abstract: Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.C<, --CO--N< or --CS--N< as the partial structure --X . . . Y<; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Ring C is optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.

Abstract: A therapeutic agent for osteoporosis, comprising an azepine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof as an active ingredient, a method for treating osteoporosis comprising administering said compound and a use of said compound for the production of a therapeutic agent for osteoporosis. The compounds of the formula (I) have superior bone resorption-inhibitory activity and act to reduce the increased amount of calcium in blood serum, which is caused by bone resorption.

Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.

Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.

Abstract: A process for the manufacture of 4H-imidazo?1,5-a!?1,4!benzodiazepine derivatives of formula I ##STR1## wherein R.sup.1 is phenyl or mono- or disubstituted phenyl;R.sup.2 is hydrogen, halogen, nitro, cyano, trifluoromethyl or lower alkyl;R.sup.3 is hydrogen or lower alkyl; andR.sup.4 is hydrogen or lower alkyland of pharmaceutically usable salts of these compounds by decarboxylating a 4H-imidazo?1,5-a!?1,4!benzodiazepinecarboxylic acid of formula II ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the above significances, at elevated temperature and under elevated pressure in the presence of an organic solvent. The compounds of formula I and their pharmaceutically usable acid addition salts are known muscle relaxants, sedatives and anticonvulsants.

Abstract: Compounds of structures (I) and (Ia) are Class III antiarrhythmic agents ##STR1##

Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.

Abstract: Tricyclic diazepines of the Formula I: ##STR1## wherein A, B, D, E, F, Y, and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.

Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.

Abstract: The novel imidazodiazepine derivatives of the formula: ##STR1## wherein the substituents are as described in the specification, can be used for the control or prevention of epileptic seizures, anxiety, tension and excitation states, sleep disorders, schizophrenic symptoms, hepatic encephalopathy and senile dementia, as well as, in the partial or complete antagonization of undesired side-effects of substances acting on benzodiazepine receptors after over-dosage or after their use in intensive medicine and in anesthesia.

Abstract: The present invention is directed to imidazo[1,5-a][1,4]benzodiazepine-3-carboxamide compounds of the formula: ##STR1## wherein R is hydrogen, C.sub.3 CH.sub.2 --, CH.sub.2 .dbd.CHCH.sub.2 --, (CH.sub.3).sub.2 CH--, CH.sub.3 CH.sub.2 CH.sub.2 --, or ##STR2## or a pharmaceutically acceptable salt thereof. These compounds and their pharmaceutically acceptable salts possess anti-anxiety and anti-epileptic activity.

Abstract: Novel tricyclic fused pyrimidine derivatives of the formula (I): ##STR1## wherein either one of R.sup.1 and R.sup.2 is hydrogen or an optionally substituted aralkyl group and the other is hydrogen, an optionally substituted aralkyl group or an aliphatic hydrocarbon group; R.sup.3 is hydrogen, an aliphatic hydrocarbon group or acyl group; and A is an optionally substituted divalent hydrocarbon chain having 2 to 4 carbon atoms and salts thereof are strong adenosine antagonists and activate cerebral functions and metabolisms, thus being useful as therapeutic or prophylactic agents for neurological or psychic changes caused by cerebral apoplexy, brain injury or cerebral atrophy.

Abstract: Platelet activating factor antagonists of formula (I), (II) or (III): ##STR1## where A is optionally substituted benzene, pyridine, naphthalene, quinoline, thiophene, benzothiophene, pyrazole or isothiazole,X is O, S or NHY is 1,4 phenylene or a group of formula ##STR2## R.sup.1 is H or optionally substituted C.sub.1 -C.sub.4 alkyl, R.sup.2 and R.sup.3 are H or C.sub.1 -C.sub.4 alkyl,B is an optionally fused 5- or 6-membered ring containing nitrogen atoms,Het is an optionally substituted 5-membered heterocyclic ring containing nitrogen or a pyridine ring, the ring optionally being fused to benzene or nitrogen-containing heterocyclic ring.

Abstract: New heterocyclic derivatives having the general formula: ##STR1## wherein X is ##STR2## or CO.sub.2 R' wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, or C.sub.1-3 -alkoxymethyl, and--A-- is --(CH.sub.2).sub.n --Y--(CH.sub.2).sub.m --,wherein n and m are 0 or 1 and --Y-- is --O--, --S--, --CH.sub.2 --, or --NR"--, wherein R" is hydrogen or C.sub.1-6 -alkyl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics and in human and animal health as anthelmintics, ecto- and endoparasiticides, insecticides and acaricides.

Abstract: New heterocyclic derivatives having the general formula: ##STR1## wherein X is ##STR2## or CO.sub.2 R' whereinR' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, or C.sub.1-3 -alkoxymethyl, andA-- is --(CH.sub.2).sub.n --Y--(CH.sub.2).sub.m --,wherein n and m are 0 or 1 and --Y-- is --O--, --S--, --CH.sub.2 --, or --NR''--, wherein R'' is hydrogen or C.sub.1-6 -alkyl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics and in human and animal health as anthelmintics, etco- and endoparasiticides, insecticides and acaricides.

Abstract: 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 and/or gastrin-related disorders of the gastrointestinal, central nervous and appetite regulatory systems; compositions comprising these compounds; and methods of treatment employing these compounds.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, trifluoromethyl, hydroxyl, nitro, amino, cyano, methylsulfonamido, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 3 carbon atoms, (alkyl of 1 to 3 carbon atoms)thio or (alkanoyl of 2 to 4 carbon atoms)amino;R.sub.3 is hydrogen, fluorine, chlorine, bromine or alkyl of 1 to 3 carbon atoms;R.sub.

Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.