University of California

Leland Stanford Junior University

Debra Marr-Leisy

Murray Edmond Goodman

Kenneth L Melmon

Michael S Verlander

Roberto P Rosenkranz

Michael Verlander

Manzoor M Khan

Histamine derivatives are disclosed which find use as effect and tissue-specific immune modulators. Specifically, the primary terminal nitrogen in histamine is derivatized to introduce a variable length side chain having 0 to 1 branch of from 1 to 3 carbons; 0 to 2 non-oxo-carbonyl groups; 0 to 4 heteroatoms, other than the non-oxo carbonyl oxygen; 0 to 1 aryl or alkyl-aryl group; and 0 to 1 functionally bound amino acid, polypeptide, or protein or derivative thereof.

Histamine derivatives as immune modulators

Molecular structures of .beta.-adrenergic antagonists are modified to produce biologically active compounds. The .beta.-antagonists are modified to form molecules of the general structure: ##STR1## wherein R is most generally R'--OCH.sub.2 --, and in some instances is R'--, and R'=an aryl or substituted aryl moiety; R'=--H, --CH.sub.3, or a short chain alkyl moiety; and Y=--OH, or more usually, --OAX or --NHAX, where A=an alkyl, aryl, or aralkyl moiety, and X=a terminal grouping, such as --CH.sub.3, --CF.sub.3 or --(CH.sub.2).sub.n COOH; or AX may be a carrier moiety consisting of a defined peptide or protein.

Derivatives of .beta.-adrenergic antagonists

Growing community of inventors

La Jolla, CA, United States of America

Debra Marr-Leisy