University of California

Syntex (u.s.a.) Inc.

Roberto P Rosenkranz

Joseph M Muchowski

Murray Edmond Goodman

Lawrence Emerson Fisher

Michael S Verlander

Kenneth L Melmon

Deborah L McClelland

Edvige Galeazzi

Debra Marr-Leisy

Joan Marie Caroon

Neal Castagnoli

Kenneth Jacobson

Compounds of Formula I ##STR1## in which: R.sub.1 is hydrogen, lower alkyl, --C(O)R.sub.3, or --C(O)NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 are independently lower alkyl, phenyl, or phenyl lower alkyl;

Bis(benzylpyrrolidine) derivatives useful for treating congestive heart

Compound of Formula I ##STR1## in which: R.sub.1 is hydrogen, lower alkyl, --C(O)R.sub.3, or --C(O)NR.sub.3 R.sub.4, where R.sub.3 and R.sub.4 are independently lower alkyl, phenyl, or phenyl lower alkyl;

Bis(benzylpyrrolidine) derivatives as dopamine agonists

Dopamine agonist compounds disclosed are useful in treating hypertension and congestive heart failure in mammals. The compounds have the following general formula (I) ##STR1## wherein: X is nitrogen or CH;

Benzylpyrrolidine derivatives as dopamine agonists

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

Biologically active drugs, e.g. catecholamine hormones, are coupled to carrier molecules, e.g. monodisperse peptides to produce conjugate molecules. The conjugate molecules retain biological activity, but the pharmacokinetic, pharmacodynamic and/or potency properties of the drug is modified. The drug is coupled to the carrier via a spacer moiety which not only serves to covalently link the drug to the carrier, but also insulates the biologically active portion of the drug, i.e., the pharmacophore, from degradation during the coupling process. The carrier preferably consists of a monodisperse peptide in which the sequence of amino acid residues is carefully preselected and controlled.

Growing community of inventors

Menlo Park, CA, United States of America

Roberto P Rosenkranz