Merck + Co., Inc.

Richard W Ransom

Michael F Sugrue

Pierre J Mallorga

Ian M Bell

Wayne J Thompson

Prasun K Chakravarty

Anthony M Smith

Peter M Munson

John W Hess

Steven M Pitzenberger

Catherine D Strader

Sandor L Varga

Victor J Lotti

Joseph A Borkowski

Keith M Witherup

Wayne J Thomspon

E M Naylor

William J Lumma

The present invention is a cloned human BK-2 bradykinin receptor cloned from a human lung fibroblast cell line. A cDNA clone, also part of the instant invention, encodes a novel 364 amino acid protein (the BK-2 receptor) that has the characteristics of a seven transmembrane domain G-protein coupled receptor. The invention is used to express a BK-2 bradykinin receptor in a host mammalian cell to screen for pharmaceutical antagonists or agonists which bind to or interact with the BK-2 bradykinin receptor protein.

Cloned and expressed human bradykinin BK-2 receptor

This invention is concerned with novel 1,3-dihydro-1-�1-(1-heteroarylpiperidin-4-yl)piperidin-4-yl!-2H-benzimidaz olones, derivatives thereof, their preparation, method of use and pharmaceutical compositions. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).

Muscarine antagonists

This invention is concerned with novel 1-�cycloalkylpioeridin-4-yl!-2H benzimidazolones, their compositions and method of use. The novel compounds are selective muscarinic agonists of the m2 subtype with low activity at the m3 subtype. The compounds are effective for the treatment of glaucoma with fewer side effects than the pilocarpine therapy.

Muscarine agonists

Compounds, 1,3-dihydro-1-{1-�piperidin-4-yl!piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).

Compounds, 1,3-dihydro-1-{1-[piperidin-4-yl]piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).

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

Pyrroloquinoline Bradykinin antagonist

Substituted triazolinone, triazolinethione, and triazolinimine compounds of formula (I) are as neurotensin II antagonists. These compounds have the general formula: ##STR1##

Substituted triazolinones, triazolinethiones, and triazolinimines as

Substituted quinazolinones of the formula are useful as neurotensin antagonists. ##STR1##

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New Britain, PA, United States of America

Richard W Ransom