Siemens Medical Solutions Usa, Inc.

Kyorin Pharmaceutical Co., Ltd.

Eli Lilly and Company

Glaxo Group Limited

Smithkline Beecham Corporation

Activx Biosciences, Inc.

Anna Katrin Szardenings

Kai Chen

Joseph C Walsh

Umesh B Gangadharmath

Dhanalakshmi Kasi

Anjana Sinha

Gang Chen

Eric Wang

Chul Yu

Changhui Liu

Hartmuth C Kolb

Vani P Mocharla

Tieming Zhao

Bei Li

Alan D Borthwick

John Liddle

Paul Graham Wyatt

Deirdre Mary Bernadette Hickey

Masahiro Nomura

Andrew McMurtrie Mason

Yasumichi Fukuda

Shigeki Seto

Neil Derek Miller

Steven Leslie Sollis

David George Hubert Livermore

Kyoko Okada

Oana Cociorva

Richard Jonathan Hatley

Fabrizio Nerozzi

Wei Zhang

Yasushi Kohno

David Alan Campbell

Min Wu

Ayako Nakamura

Kazuhiro Yumoto

Peter J H Scott

Michael Schaefers

Andreas Faust

Sven Hermann

Guenter Haufe

Marek Liyanage

Hans-Joerg Breyholz

Daniel Kurt Cashion

Vani P Mocharia

Stefan Wagner

Verena Hugenberg

Klaus Kopka

Harmuth C Kolb

Peter Jh Scott

Peter JH Scott

Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.

PSMA imaging agents

Compounds for targeting and agents for imaging, Prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.

Novel compounds and pharmaceutical compositions having MMP inhibitory activity are disclosed, which have been found to be particularly useful in the prevention, treatment and diagnostic imaging of diseases associated with an unpaired activity of MMP, amongst others MMP-2, MMP-8, MMP-9 and/or MMP-13 to name a few. The compounds of the present invention are useful for the prevention, the treatment and the in vivo diagnostic imaging of a range of disease states (inflammatory, malignant and degenerative diseases) where specific matrix metalloproteinases are known to be involved.

Compounds with matrix-metalloproteinase inhibitory activity and imaging agents thereof

Provided herein are spirocyclic aminoquinolones of formula I and compositions containing the compounds. The compounds and compositions provided herein are useful in the prevention, amelioration or treatment of GSK-3 inhibitors mediated diseases.

Spirocyclic aminoquinolones as GSK-3 inhibitors

Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and &#x3b2;-amyloid peptides are presented herein. The invention also relates to methods of imaging A&#x3b2; and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.

Imaging agents for detecting neurological disorders

A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof.

Substituted diketopiperazines as oxytocin antagonists

Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering ti a patient in need compounds of formula (I) capable of binding to tau proteins and &#x3b2;-amyloid peptides are presented herein. The invention also relates to methods of imaging A&#x3b2; and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.

Provided herein are spirocyclic aminoquinolones of formula I and compositions containing the compounds. The compounds and compositions provided herein are useful in the prevention, amelioration or treatment of GSK-3 inhibitors mediated diseases. In Formula (I): Xis O or NR; A is bond or substituted or unsubstituted C-Calkylene, wherein the substituents when present are selected from one to four Qgroups; where Qis alkyl or haloalkyl; p is 0 or 1; and q is an integer of 0 to 2. 

Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases. 

Cyanoaminoquinolones and tetrazoloaminoquinolones as GSK-3 inhibitors

A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.

Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.

Aminoquinolones as GSK-3 inhibitors

A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of the formula (I) and/or a physiologically acceptable derivative thereof, wherein the substituents have the meaning given in the description. Disclosed are also novel compounds of formula (I) and processes for their preparation.

The present invention provides tagged acyl phosphate probes ('TAPPs'), and methods of their preparation and use. The subject methods and compositions can provide enhanced simplicity and accuracy in identifying changes in the presence, amount, or activity of target proteins in a complex protein mixture, preferably nucleotide binding proteins using nucleotide binding protein-directed TAPPs. The profiling methods described herein can have a number of steps leading to the identification of target nucleotide binding protein(s) in a complex protein mixture.

Acyl-nucleotide probes and methods of their synthesis and use in proteomic analysis

Growing community of inventors

Torrance, CA, United States of America

Anna Katrin Szardenings