Abstract: This invention relates to novel compounds, their synthesis and use as selective .alpha..sub.1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the .alpha..sub.1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Abstract: A method of antagonizing the function of cholecystokinins in a disease state in mammals, especially in humans, which comprises administering a pharmaceutically-effective amount of certain 2-acylaminomethyl-1,4-benzodiazepine derivatives or their salts, alone or with a pharmaceutical carrier, with or without an adjuvant.

Abstract: Benzofused lactams and their use as antagonists of cholecystokinin are disclosed.

Abstract: The compound having Formula I and several minor related compounds are produced by the aerobic fermentation of Aspergillus alliaceus Thom and Church, ATCC No. 20655 or ATCC No. 20656. ##STR1## The compound of Formula I and the several minor related compounds are antagonists of cholecystokinin (CCK). CCK antagonists are useful in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems of animals, especially humans.