Merck + Co., Inc.

William J Paleveda, Jr

Kenneth L Shepard

Daniel F Veber

Robert G Strachan

Frederick W Holly

Ruth F Nutt

Ralph F Hirschmann

Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt; ester and amide or derivatives; and methods of treatment comprising administering such compounds and compositions.

Tricyclicdicarboximides

Somatostatin analogs having the structural formula: Cyclo[(X).sub.j -(A).sub.k -(B).sub.1 -Phe-Phe-(D- or L-)Trp-Lys-Thr-Phe-Thr-(C).sub.m ] Wherein

Somatostatin analogs

Somatostatin analogs having the structural formula: ##STR1## are prepared by controlled stepwise procedures starting with individual amino acid components. These peptides have the property of lowering blood glucose, inhibiting gastric secretion, inhibiting growth hormone release and inhibiting glucagon release in humans and animals.

Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt, ester and amide derivatives; and methods of treatment comprising administering such compounds and compositions.

N-(Benzoxazolinyl-2-one)-tricyclic dicarboximides

Somatostatin analog, hereinafter designated des(Ala.sup.1 -Gly.sup.2)desaminocys.sup.3 -somatostatin, having the structure: ##STR1## is prepared by controlled stepwise procedures starting with individual amino acid components. This peptide has the property of lowering blood glucose, inhibiting gastric secretion and inhibiting growth hormone release in humans and animals.

Process for preparing somatostatin analog

Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt, ester and amide derivatives, and methods of treatment comprising administering such compounds and compositions.

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Lansdale, PA, United States of America

William J Paleveda, Jr