Lexicon Pharmaceuticals, Inc.

Janssen Pharmaceutica Nv

Lexicon Genetics Corporation

Coelacanth Corporation

Hartmuth C Kolb

Zhi-Cai Shi

Ramanaiah C Kanamarlapudi

Paul F Richardson

Wei Zhang

José Ignacio Andrés-Gil

Joseph Elisabeth Leenaerts

Frederik Jan Rita Rombouts

Guy Maurits R Bormans

Gerard M McGeehan

Katleen Fierens

Gallen Triana-Baltzer

Zhi-Min Wang

John Randall Slemmon

Cullen Cavallaro

Lieven Denis Herwig Declercq

Diederik Willem Elisabeth Moechars

Spencer David Kimball

Cynthia Anne Fink

Joseph Barbosa

Ashok R Tunoori

Haihong Jin

Heidi Theis

Gaznabi Khan

Laxma Reddy Kolla

Alexander Gontcharov

Qun Sun

The present invention relates to novel, selective radiolabelled tau ligands which are useful for imaging and quantifying tau aggregates, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue or a subject, in vitro or in vivo, and to precursors of said compounds.

Tau PET imaging ligands

Methods of measuring the amount of singly- or multiply-phosphorylated p217+ tau protein in a sample are provided. Methods of detecting or diagnosing tauopathies, methods of determining the effectiveness of a treatment of a tauopathy, and methods of determining whether a subject is suitable for anti-p217+ tau antibody therapy are also provided. Also described are antibodies for use in the methods and kits comprising the antibodies.

Assays to detect neurodegeneration

This invention concerns novel thiazolopyrazole compounds and compositions comprising them. Methods of using these compounds for the treatment, prevention and management of various diseases and disorders are also encompassed by the invention.

Thiazolopyrazoles and methods of their use

This invention concerns novel thiazole compounds. Methods of using these compounds for the treatment, prevention and management of various diseases or disorders, as well as pharmaceutical compositions of these compounds, are also disclosed.

Thiazoles and methods of their use

Disclosed are efficient and scalable processes for preparing 1,2,4- and 1,3,4-oxadiazole carboxylates from readily available starting materials.

Large scale synthesis of 1,2,4- and 1,3,4-oxadiazole carboxylates

Disclosed is a one step method for preparing a &#x3b2;-substituted sulfide by treating a &#x3b2;-halosulfide with a nucleophile in water.

Water as promoter in the nucleophilic substitution of chloride

Disclosed is a safe, efficient and environmentally friendly method for preparing imidoesters.

Modified safe and efficient process for the environmentally friendly synthesis of imidoesters

PPAR-&ggr; agonists as agents for the treatment of type II diabetes

Disclosed is a one step method for preparing a 1,2,3-triazole carboxylic acid by treating an azide with a &bgr;-ketoester in the presence of a base.

One step synthesis of 1,2,3-triazole carboxylic acids

Disclosed is an improved method for preparing an activated carboxylic acid in the form of a pentafluorophenyl ester, an improved method for making a carboxamide from a pentaflourophenyl ester, and a carboxamide and carboxamide library prepared using both of these methods.

Amide library formation using a &ldquo;by-product-free&rdquo; activation/coupling sequence

Disclosed are novel compounds of which function as a sulfonyl linker between a target molecule and a polymer solid support, novel sulfonyl aziridine scaffold intermediates to optimize the regioselectivity associated with the nucleophilic substitution of these aziridines, a method for making derivatized aziridine, and a method for making derivatized amines.

Sulfonyl linker for the creation of libraries via immobilization of amines

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East Windsor, NJ, United States of America

Hartmuth C Kolb