Merck + Co., Inc.

Sandor L Varga

Daniel F Veber

John J Baldwin

Gerald S Ponticello

Kenneth L Shepard

Marcia E Christy

Robert G Strachan

Ruth F Nutt

Wayne J Thompson

Stephen F Brady

Terry A Lyle

Jacob M Hoffman, Jr

Steven M Pitzenberger

Susan F Britcher

Richard W Ransom

Victor J Lotti

Frederick W Holly

Anthony G Zacchei

Keith M Witherup

Ling L Lee

William J Lumma

Frederick W Holly, Deceased

A pyrroloquinoline compound of the following formula is disclosed: ##STR1## wherein H,

Pyrroloquinoline Bradykinin antagonist

4-(2-Methyl-2-hydroxypropylamino)-5,6-dihydrothieno[2,3-b]thiopyran-2-sulfo namide-7,7-dioxide is a major mammalian metabolite of 4-(2-methylpropylamino)-5,6-dihydrothieno[2,3-b]thiopyran-2-sulfonamide-7, 7-dioxide and is itself an active carbonic anhydrase inhibitor useful in the treatment of ocular hypertension by topical administration.

4-(2-methyl-2-hydroxypropylamino)-5,6-dihydrot

Fluoro-and hydroxy-derivatives of 5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines wherein the substituents are on non-benzenoid carbons are active anticonvulsants and antagonists of N-methyl-D-aspartate.

Derivatives of

1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as anti-hypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.

1-aryloxy-3-(substituted aminoalkylamino)-2-propanols, pharmaceutical

1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as antihypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.

1-aryloxy-3-(substituted aminoalkylamino)-2-propanols

There are disclosed cyclic octapeptide analogs of the tridecapeptide, neurotensin.

Cyclic octapeptide analogs of neurotensin

There are disclosed metabolically protected linear analogs of the carboxy terminal pentapeptide fragment of the tridecapeptide, neurotensin.

Metabolically protected analogs of neurotensin

Synthetic novel cyclic hexapeptides having the structure:

Cyclic hexapeptides

Novel tripeptides are disclosed. These tripeptides have anti-depressant activity and thyrotropin releasing hormone activity. Processes for preparing these tripeptides are also disclosed.

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Harleysville, PA, United States of America

Sandor L Varga