Agouron Pharmaceuticals, Inc.

Triad Therapeutics, Inc.

Traid Therapeutics, Inc.

Pfizer Healthcare Ireland

Anna Maria Tempczyk-Russell

Steven Lee Bender

Allen Borchardt

Robert Steven Kania

Cynthia Louise Palmer

Michael D Varney

Maurizio Pellecchia

Michael Raymond Collins

Daniel S Sem

Stephan James Cripps

Michael Brennan Wallace

Min Teng

Siegfried Heinz Reich

Theodore Otto Johnson, Jr

Hiep The Luu

Ye Hua

Michael David Johnson

Christine Thomas

Sepehr Sarshar

Mitchell David Nambu

Dilip Ramakant Bhumralkar

Abhijit Suresh Bhat

Shao Song Chu

Suzanne Pritchett Benedict

Alice Lee

Olivier Alexandre Laurent

Wei Hong Yu

Richard Ryan Preston

Larry Andrew Alegria

Zhengwei Peng

Michelle Yang

Robert Steve Kania

The present invention relates to a polypeptide comprising 7 &#x3b2;-strands A, B, C, D, E, F, and G sequentially connected together by connecting chains of amino acids, and a first &#x3b1;-helix sequentially located on the EF chain between &#x3b2;-strands E and F, wherein the &#x3b2;-strands are arranged so as to form a first &#x3b2;-sheet comprising &#x3b2;-strands A, B, D, and E, and a second &#x3b2;-sheet comprising &#x3b2;-strands C, F and G, said first and second &#x3b2;-sheets being covalently bonded together so as to form a first Ig domain; wherein the EF chain between &#x3b2;-strands E and F comprises the sequence X-X-X-X-KH(SEQ ID NO:98), and X, Xand Xare each independently any amino acid residue, characterized in that Xis selected from the group consisting of A, G, I, V, L, R, S, T, Q, P, N, M, H, W, and pharmaceutically acceptable salts, stereoisomers, tautomers, solvates, and prodrugs thereof.

Mutant antibodies and conjugation thereof

Methods for rapidly identifying drug candidates that can bind to an enzyme at both a common ligand site and a specificity ligand site, resulting in high affinity binding. The bi-ligand drug candidates are screened from a focused combinatorial library where the specific points of variation on a core structure are optimized. The optimal points of variation are identified by which atoms of a ligand bound to the common ligand site are identified to be proximal to the specificity ligand site. As a result, the atoms proximal to the specificity ligand site can then be used as a point for variation to generate a focused combinatorial library of high affinity drug candidates that can bind to both the common ligand site and the specificity ligand site. Different candidates in the library can then have high affinity for many related enzymes sharing a similar common ligand site.

NMR-solve method for rapid identification of bi-ligand drug candidates

Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use

Indazole compounds and pharmaceutical compositions for Inhibiting protein kinases, and methods for their use

Methods for rapidly identifying drug candidates that can bind to an enzyme at both a common ligand site and a specificity ligand site, resulting in high affinity binding. The bi-ligand drug candidates are screened from a focused combinatorial library where the specific points of variation on a core structure are optimized. The optimal points of variation are identified by which atoms of a ligand bound to the common ligand site are identified to be proximal to the specificity ligand site. As a result the atoms proximal to the specificity ligand site can then be us ed as a point for variation to generate a focused combinatorial library of high affinity drug candidates that can bind to both the common ligand site and the specificity ligand site. Different candidates in the library can then have high affinity for many related enzymes sharing a similar common ligand site.

NMR-solve method for rapid identification of Bi-ligand drug candidates

Diaminothiazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

Thiazole compounds and pharmaceutical compositions for inhibiting protein kinases and methods for their use

Growing community of inventors

Ramona, CA, United States of America

Anna Maria Tempczyk-Russell