Myriad Genetics, Inc.

Triad Liquidating Company, LLC

Min Sang Lee

Hiroshi Nakanishi

Jan Urban

Masakatsu Eguchi

Daniel S Sem

Jessymol Mathew

Vincent Huber

Mark Kelly

Qing Dong

Maurizio Pellecchia

Jianqiang Wang

Yong Qin

Hugo Villar

The invention provides a method for identifying a ligand that binds to a macromolecular target. The methods involve (a) attaching an antenna moiety to a first ligand, wherein the ligand binds specifically to a macromolecular target; (b) providing a sample comprising the macromolecular target, the first ligand and a candidate second ligand under conditions wherein the first ligand and the macromolecular target form a bound complex; (c) detecting a subset of magnetization transfer signals between the antenna moiety of the first ligand and the second candidate ligand, wherein the signals are obtained from an isotope edited NOESY spectrum of the sample; thereby determining that the two ligands are proximal in a bound complex, and identifying a second ligand that binds to the macromolecular target.

Nuclear magnetic resonance assembly of chemical entities using advanced antenna probes

The invention provides a method for obtaining a binding compound for a protein family, wherein the members of the protein family bind a common ligand. The method includes the steps of (a) providing a sample containing a protein from the protein family, a first ligand and a second ligand under conditions wherein the first ligand, the second ligand and the protein form a bound complex; (b) detecting magnetization transfer between the first ligand and the second ligand in the bound complex, thereby determining that the two ligands are proximal in the bound complex; and (c) obtaining a candidate binding compound including the first ligand, or a fragment thereof linked to the second ligand, or a homolog thereof, whereby the population contains binding compounds that bind to members of the protein family.

Nuclear magnetic resonance assembly of chemical entities

Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein Y, A, B, Rand Rare as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing the same, are neurokinin (tachykinin) antagonists. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening such libraries to identify biologically active members.

Helix mimetics and composition and methods related thereto

Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed:wherein A, B, X, R, and Rare as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.

Reverse-turn mimetics and methods relating thereto

Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure:including pharmaceutically acceptable salts and stereoisomers thereof, wherein Y, A, B, Rand Rare as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing the same, are neurokinin (tachykinin) antagonists. Libaries contaning the compounds of this invention are also disclosed, as well as methods for screening such libaries identify biologically active members.

Growing community of inventors

Carlsbad, CA, United States of America

Min Sang Lee