Abstract: Aromatic 1,4-benxodiazepines 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: Novel 2-substituted-aminomethyl-1,4-benzodiazepines which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals, especially of humans.

Abstract: Triazolobenzodiazepines of the formula: ##STR1## are disclosed which are antagonists of cholecystokinin (CCK).

Abstract: Novel peptides of the formula: ##STR1## where R.sup.1 through R.sup.8 are various radicals derived from L- and D- amino acids; having LHRH antagonist activity; useful in reducing fertility.Pharmaceutical compositions and methods for use in reducing fertility.

Abstract: A non-fermentation process for preparing a benzodiazepinedione of the formula: ##STR1## and intermediates is disclosed.

Abstract: Novel quinazolino-1,4-benzodiazepin-5,13-diones, which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds from compounds prepared by aerobic fermentation of certain Aspergillus alliaceus strains, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.

Abstract: Novel indol-3-yl-quinazolino-1,4-benzodiazepin-5,13-diones, which are antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds from compounds prepared by aerobic fermentation of certain Aspergillus alliaceus strains, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.

Abstract: Novel quinazolino-1,4-benzodiazepin-5,13-dione derivatives, which are soluble in aqueous media and which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds from compounds prepared by aerobic fermentation of certain Aspergillus alliaceus strains, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.

Abstract: Tetracyclic compounds of the formula: ##STR1## and a process for their preparation are disclosed. The compounds have cholecystokinin inhibiting activity.

Abstract: Chiral N-protected, N-substituted .alpha.-amino acids are described. These compounds are prepared by condensation of an N-protected .alpha.-amino acid with an aldehyde followed by the selective reductive cleavage of an oxazolidinone intermediate.

Abstract: Novel peptides of the formula: ##STR1## where A through G, X and Y are various amino acids and substituents; having long lasting LHRH agonist and antagonist activity; useful in promoting fertility, reducing fertility, respectively.

Abstract: Novel peptides of the formula: ##STR1## where A through G, X and Y are various amino acids and substituents; having long lasting LHRH agonist and antagonist activity; useful in promoting fertility, reducing fertility, respectively.

Abstract: Highly active and long lasting cyclic hexapeptide analogs of somatostatin are prepared. A single amino acid of D-configuration, functioning as a spacer for the remaining amino acids, replaces seven of the ring amino acids of somatostatin. The amino acid adjacent to this spacer amino acid is methylated on the nitrogen and is of the D-configuration. The two amino acids on either side of this dipeptide are also of D-configuration. The remaining two amino acids, Trp and Lys are either D- or L-. The order of the amino acids is reversed relative to the sequence found in somatostatin. The structures therefore represent a modified form of D-retro peptide analogs. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions.

Abstract: Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.

Abstract: Novel peptides of the formula: ##STR1## wherein X is S or (CH.sub.2).sub.n and n is 0, 1 or 2, and R.sub.1 through R.sub.6 are various amino acid and other substituents; having long-lasting enkephalin agonist activity; useful in treating pain and in treating schizophrenia.

Abstract: Novel peptides of the formula: ##STR1## wherein X is S or (CH.sub.2).sub.n and n is 0, 1 or 2, and R.sub.1 through R.sub.6 are various amino acid and other substituents; having long-lasting enkephalin agonist activity; useful in treating pain and in treating schizophrenia.

Abstract: Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synethesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.

Abstract: Synthetic novel cyclic hexapeptide having the structure: ##STR1## and the dipeptide ##STR2## are prepared. Oral administration of these peptides improves the digestive efficiency of certain herbivorous animals.

Abstract: Nitroarginyl peptides are selectively reduced to the corresponding arginyl peptides by titanium (III). The nitro protecting group which is labile toward nucleophilic reagents is retained through part of a synthesis and selectively removed prior to treatment with nucleophiles such as hydrazine and ammonia. The selectivity of titanium (III) for removal of the nitro functionality increases the flexibility of this protecting group in the synthesis of arginyl peptides. The present novel process is useful in the synthesis of medicinal peptides such as molluscan cardiac stimulant H-Phe-Met-Arg-Phe-NH.sub.2.

Abstract: Polyenes are synthesized from unsaturated materials having allylic hydroxyl groups, which react with imidosulfides to produce sulfones. Removal of the sulfone group, e.g. by reaction with alkyllithium and iodine, results in compounds in which the allylic carbons are joined by a double bond. The reactions take place easily over wide temperature ranges. The method is particularly advantageous in the synthesis of carotenoids from polyene alcohols, being much simpler and easier to use than previous carotenoid syntheses.