Abstract: This invention relates to novel benzodiazepine derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof, ##STR1## (wherein R.sup.1 is an aryl group, or an aromatic heterocyclic radical of 5-membered monocyclic, 6-membered monocyclic or 5- and 6-membered bicyclic structure, which may optionally be substituted; and R.sup.2 is an aryl group which may optionally be substituted), to medicinal compositions comprising the same, and to a process for producing the same. The compounds of formula (I) shown above exhibit antagonism for the CCK-B receptor and the action of depressing the gastric acid secretion caused by the stimulus of pentagastrin, and are therefore useful as a drug for the relief of diseases related to the CCK-B receptor and the gastrin receptor.

Abstract: Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated.

Abstract: Compounds of Formula (I), and salts and prodrugs thereof, wherein R.sup.1 represents C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 optionally substituted phenyl or R.sup.2 represents a group (A) where W is CH.sub.2 or NR.sup.10, and W.sup.1 is CH.sub.2, or W and W.sup.1 each represent 0; R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.13 R.sup.14 ; R.sup.4 is H, C.sub.1-4 alkyl, optionally substituted phenyl or optionally substituted benzyl; R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are H or C.sub.1-4 alkyl; or any two of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 together form a chain (CH.sub.2).sub.t, and any other two of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 optionally form a chain (CH.sub.2).sub.s where s and t are independently 1, 2 or 3; m is 2, 3, 4, 5, 6, 7, 8 or 9; n is 0, 1, 2, 3 or 4; and x is 0, 1, 2 or 3; are CCK and/or gastrin antagonists useful in therapy.

Abstract: Disclosed are new benzodiazepine compounds which are useful as cholecystokinin and gastrin receptor antagonists and are useful in the treatment of anxiety, panic and pain.

Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein: R.sup.1 is H, certain optionally substituted C.sub.1.6 alkyl, or C.sub.3-7 cycloalkyl;R.sup.2 is (CH.sub.2).sub.q -tetrazolyl optionally substituted in the tetrazole ring by C.sub.1-4 alkyl, (CH.sub.2).sub.q -imidazolyl (where q is 0, 1, 2 or 3), CONHSO.sub.2 R.sup.9, SO.sub.2 NHCOR.sup.9 (where R.sup.9 is C.sub.1-6 alkyl, optionally substituted aryl or trifluoromethyl). SO.sub.2 NHR.sup.10 (where R.sup.10 is a nitrogen containing heterocycle), cyclopropyl or (CH.sub.2), CO.sub.2 H, where n is 1 or 2;R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ;R.sup.4 is C.sub.1-7 straight or branched chain alkyl; andx is 0, 1, 2 or 3;are CCK and/or gastrin receptor antagonists. They and compositions thereof are useful in therapy.

Abstract: 3-Acylamino-5-Aminobenzo[1,5]diazepines are useful in the treatment of arrhythmia.

Abstract: Benzo-(1,5)-diazepine derivatives with an amide or urea function in the 3-position are useful in the treatment of arrhythmia.

Abstract: Intermediates of the formula: ##STR1## wherein R.sup.1 is tetrazolyl or imidazolyl, each of which may have an imino protective group,R.sup.2 is phenyl which may have a halogen atom,R.sup.3 is hydrogen or halogen, andA is lower alkylene, or a salt thereof.They are useful in the preparation of benzodiazepine derivatives and pharmaceutically acceptable salts thereof which are cholecystokinin (CCK) antagonists and therefore can be used as therapeutical agents for emesis, pancreatitis, satiety and appetite control, pain control, insulinoma, gastroparesis, acute obstructive cholecystitis, irritable bowel disease and carcinoma of pancreas.

Abstract: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).

Abstract: This invention relates to benzodiazepine compounds which are useful as antagonists of cholecystokinin and gastrin.

Abstract: Benzodiazepine analogs of the formula: ##STR1## wherein: R.sup.3 is ##STR2## --NH(CH.sub.2).sub.2 --.sub.3 NHCOR.sup.7, ##STR3## or --X.sup.11 NR.sup.18 SO.sub.2 (CH.sub.2).sub.q R.sup.7 ; R.sup.7 is O,S,HH, or NR.sup.15 with the proviso that X.sup.7 can be NR.sup.15 only when R.sup.1 is not H.are disclosed which are antagonists of gastrin and cholecystokinin (CCK) with enhanced aqueous solubility and have properties useful in the treatment of disorders of gastric secretion, appetite regulation, gastrointestinal motility, pancreatic secretion, and dopaminergic function, as well as in treatment producing potentiation of morphine and other opiate analgesics.

Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## R.sup.1 is H, certain optionally substituted alkyl or C.sub.3-7 cycloalkyl;R.sup.2 represents (CH.sub.2).sub.m -tetrazolyl, (CH.sub.2).sub.m -imidazolyl, CONR.sup.6 R.sup.7, CONHSO.sub.2 R.sup.9, SO.sub.2 NHCOR.sup.9, SOC.sub.1-4 alkyl, SO.sub.2 NHR.sup.10, 5-hydroxy-4-pyrone, (CH.sub.2).sub.n CO.sub.2 H, ##STR2## or a group ##STR3## wherein X is O, S or NR.sup.11 ; one of Z and Y is C.dbd.O and the other is O, S or NR.sup.12 ;R.sup.3 represents H or C.sub.1-6 alkyl;R.sup.4 represents 2-, 3- or 4-pyridyl;R.sup.5 represents C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; andx is 0, 1, 2 or 3;are CCK and/or gastrin receptor antagonists useful in therapy.

Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams ##STR1## which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

Abstract: A compound of the formula ##STR1## the process for its preparation and intermediate thereof. The compound is useful as a cholecystokinin antagonist.

Abstract: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).

Abstract: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).

Abstract: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).

Abstract: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).

Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

Abstract: Compounds of Formula I are antagonists of oxytocin and are useful in the treatment of preterm labor and dysmenorrhea, and for stoppage of labor prepatory to Caesarean delivery.

Abstract: Compounds corresponding to the formula I ##STR1## in which R.sup.1 represents hydrogen, lower alkyl or cycloalkylalkyl with 4-7 carbon atoms,R.sup.2 represents hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl, andR.sup.3 represents hydrogen, halogen, lower alkyl or lower alkoxy, orR.sup.2 and R.sup.3 together denote an alkylenedioxy group,R.sup.4 represents cycloalkyl with 5 to 6 carbon atoms, thiophene or optionally substituted phenyl,R.sup.5 represents hydrogen or halogen,R.sup.6 represents hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl, andZ represents an alkylene chain with 2-4 carbon atoms, which can optionally be mono- or disubstituted by lower alkyl or onto which a 5-6-membered carbocyclic ring can optionally be fused, or represents an --X--CH.sub.2 --CH.sub.2 -- chain,which have pharmacologically valuable properties, are described, together with a method for their preparation.

Abstract: Novel radiolabeled cholecystokinin-A (CCK-A) antagonists have been developed which, after intravenous injection, localize in the pancreas as a result of specific binding to CCK-A receptors. These tracers, when labeled with appropriate radiohalogens, are useful as commercial diagnostic imaging radiopharmaceuticals and radiotherapeutic drugs.

Abstract: This invention relates to new benzodiazepine derivatives and pharmaceutically acceptable salts thereof. More particularly, it relates to new benzodiazepine derivatives and pharmaceutically acceptable salts thereof which are cholecystokinin (CCK) antagonists and therefore can be used as therapeutical agents for emesis, pancreatitis, satiety and appetite control, pain control, insulinoma, gastroparesis, acute obstructive cholecystitis, irritable bowel disease, carcinoma of pancreas, etc.

Abstract: BZDs of the general formula 1: ##STR1## where: R represents H, alkyl, alkenyl, cycloalkyl or cycloalkenyl each with up to 8 carbon atoms, phenylalkyl with an alkylene chain of 1 to 3 carbon atoms and optionally substituted on the phenyl radical with one or two substituents selected from the group consisting of Cl, Br, F, CN, CF.sub.3, NO.sub.2, lower alkyl, and OCH.sub.3, or represents a phenyl radical which is optionally substituted with one or two substituents selected from the group consisting of Cl, F, Br, CN, I, CF.sub.3 NO.sub.2, lower alkyl and OCH.sub.3, or represents a 5-membered or 6-membered heterocyclic radical with 1 or 2 heteroatoms from the group consisting of O, N and S; R.sub.1 represents H or, together with R.sub.2, forms a bond; R.sub.2 and R.sub.

Abstract: An economical, one-pot process for resolution-racemization of primary amines with .alpha.-hydrogens via selective crystallization of diastereomeric chiral sulfonic acid salts and the subsequent in situ racemization of the other enantiomer by the catalytic addition of aromatic aldehydes, and a key process intermediate thereof.

Abstract: Benzodiazepine analogs of the formula: ##STR1## are disclosed which are antagonists of gastrin and cholecystokinin (CCK).

Abstract: The present invention provides an improved process for producing 3-acylamino benzodiazepines of the formula: ##STR1## wherein: R is loweralkyl of from 1-6 carbon atoms, aryl such as phenyl and halophenyl, aralkyl, alkyloxy, aralkyloxy, indolyl or substituted indolyl;R' is hydrogen, loweralkyl of from 1-6 carbon atoms, carboxymethyl or carbalkoxymethyl wherein the alkoxy groups contain from 1-4 carbon atoms;X is hydrogen or halogen;Y is hydrogen or halogen.These compounds are useful because of their activity as cholecystokinin (CCK) inhibitors.