University of Colorado

Other

Pennwalt Corporation

University Patents, Inc.

Cortech, Inc.

Nova Technology Limited Partnership

University Technology Corporation

John M Stewart

Lajos Gera

Raymond J Vavrek

Daniel C F Chan

Eric T Whalley

Paul A Bunn, Jr

Paul Bunn

Eunice York

Dan H Morris

Daniel C Chan

Karl W Hahn

Richard E Chipkin

Wieslaw A Klis

Gary R Matsueda

The invention provides bradykinin antagonists and pharmaceutically acceptable salts thereof having anti-cancer activity. These anti-cancer compounds are particularly useful for inhibiting the growth of lung and prostate cancers.

Anti-cancer compounds

The present invention provides compounds useful to inhibit tumor growth and to induce apoptosis. In general, the anti-cancer agents (ACA) are described by the formula:[ACA]-X[Formula I]wherein X is a linker group having 2&#x2013;5 functional groups or is absent, n=1, and ACA is selected from the group consisting of Formula II, Formula III, Formula IV, Formula V, and Formula VI, as described herein. Other compounds described herein are defined by the Formula VII, as described herein.

Anti-cancer compounds and methods related thereto

The present invention provides bradykin antagonists containing pentafluorophenylalanine which are therapeutically useful. Moreover, the present invention provides methods to antagonize bradykinin receptors in a mammal in need of such antagonism, comprising administering a bradykinin antagonist containing pentafluorophenylalanine. Also provided are methods to treat inflammation in a mammal in need of such inhibition, comprising administering a bradykinin antagonist containing pentafluorophenylalanine. Lastly, a method to treat cancer in a mammal in need of such inhibition, comprising administering a bradykinin antagonist containing pentafluorophenylalanine.

Bradykinin antagonists containing pentafluorophenylalanine

The present invention provides bradykinin antagonists effective to inhibit cancer cell growth. Also provided are methods of inhibiting lung cancer cell growth by administering a therapeutically effective amount of a dimerized bradykinin antagonist.

Cytolytic bradykinin antagonists

The present invention provides des-Arg.sup.9 bradykinin analogs which are selective B1 receptor antagonists.

Des-Arg.sup.9 -BK antagonists

The present invention pertains to modified bradykinin antagonist peptides of the formula X-A.sup.0 -B.sup.1 -C.sup.2 -D.sup.3 -E.sup.4 -F.sup.5 -G.sup.6 -H.sup.7 -J.sup.8 -K.sup.9, where at least one of F.sup.5, H.sup.7 and J.sup.8 is an indane substituted amino acids.

Bradykinin antagonist peptides containing indane-substituted amino acids

A multi-dimensional ball-striking paddle consisting of a frame, handles on the frame, a primary ball-striking surface affixed to the frame, and a plurality of secondary balls striking surfaces extending transversely to the primary ball-striking surface.

Multi-dimensional ball-striking paddle

The design, and synthesis of peptide-based molecules termed helizymes which possess catalytic activity are described herein The catalytic molecules of the invention comprise a number of amphiphilic helical peptides, which interact via hydrophobic interactions and which are bonded at their carboxyl ends to a multifunctional base. Active site residues functional for catalysis are positioned within or at the N-termini of the helical peptides. The helizyme molecule adopts a conformation in aqueous medium such that a substrate binding pocket is formed and such that functional active site geometry results from the association of the helical peptides Specifically exemplified helizymes possess specificities and at least one catalytic activity of chymotrypsin, trypsin and acetylcholine esterase.

Synthetic helizyme enzymes

The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with an aliphatic, cyclic or aromatic amino acid of the D-configuration converts bradykinin agonists into a bradykinin antagonist. The invention further includes additional modifications at other positions within the novel 7-position modified bradykinin antagonists including C-terminal and N-terminal extensions and replacement of arginine in the one and nine positions which increase enzyme resistance, antagonist potency and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of the mannal and human body in which an excess of bradykinin or related kinins are produced or injected as by bites into the body.

Bradykinin antagonist peptides

The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with an aromatic amino acid or the D-configuration converts bradykinin agonists into a bradykinin antagonist. The invention further includes additional modifications at other positions within the novel 7-position modified bradykinin antagonists which increase enzyme resistance, antagonist potency and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of the mammal and human body in which an excess of bradykinin or related kinins are produced or injected as by bites into the body.

A class of dipeptide derivatives having opiate activity having the formula

Dipeptide derivatives having opiate activity

A method for preparing novel peptide alcohols exemplified by the reduction of enkephalins and particularly the met-enkephalin to produce pentapeptides and tetrapeptides of the following formula

Growing community of inventors

Denver, CO, United States of America

John M Stewart