University of California

The University of Texas System

The United States of America, As Represented by the Secretary, Department of Health and Human Services

University of Connecticut

Saint Louis University

The Henry M. Jackson Foundation for the Advancement of Military Medicine Inc.

Astrocyte Pharmaceuticals, Inc.

Fm Therapeutics Co., Ltd.

Kenneth A Jacobson

Murray Edmond Goodman

Daniela Salvemini

Michael S Verlander

James D Lechleiter

Bhalchandra V Joshi

Theodore E Liston

Lak Shin Jeong

William S Korinek

Kenneth L Melmon

Dilip K Tosh

Hea Ok Kim

Artem Melman

Neal Castagnoli

Seung Ah Choe

Evgeny Kiselev

Albert M Van Rhee

Anna Junker

Thatikonda Santhosh Kumar

Elisa Uliassi

Ben Bih-Ren Wang

Harvey Pollard

Bruce Liang

Thatikonda Santosh Kumar

Ji-Long Jiang

Biologically active derivatives of norepinephrine are disclosed. Such derivatives are catecholamines wherein isoproterenol is modified by extending the isopropyl functional grouping to an alkyl, aryl, or alkyl-aryl chain of variable length where said chain terminates in a carboxylic acid functional group, or in a substituted amide functional group. Such derivatives are .beta.-adrenergic and a number of such derivatives e.g., 6-(.beta.-3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid p-toluide, 6-(.beta.-3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid para-n-butyl anilide; 6-(.beta.,3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid para-methoxy anilide; 6-(.beta.-3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid paratrifluoromethyl anilide; and 6-(.beta.-3,4-dihydroxyphenyl-.beta.-hydroxy)-ethylamino heptanoic acid N-methyl para-toluide display a .beta.-adrenergic activity at least several orders of magnitude greater than isoproterenol itself. Several methods of producing such active derivatives are also disclosed.

Biologically active catecholamine derivatives

Growing community of inventors

La Jolla, CA, United States of America

Kenneth A Jacobson