Siemens Medical Solutions Usa, Inc.

Eli Lilly and Company

University of Michigan

Peter J H Scott

Joseph C Walsh

Gang Chen

Hartmuth C Kolb

Dhanalakshmi Kasi

Kai Chen

Umesh B Gangadharmath

Vani P Mocharla

Qianwa Liang

Eric Wang

Tieming Zhao

Anjana Sinha

Henry Clifton Padgett

Zhiyong Gao

Chunfang Xia

Bing Wang

Farhad Karimi

Brian A Duclos

Thomas Lee Collier

Anna Katrin Szardenings

Melanie S Sanford

Chul Yu

Changhui Liu

Allen F Brooks

Melissa Rodnick

Joseph J Topczewski

Naoko Ichiishi

Vani P Mocharia

Daniel Kurt Cashion

The present application is directed to radiolabeled imaging agents comprising a radiolabel, and a substrate, pharmaceutical compositions comprising radiolabeled imaging agents, and methods of using the radiolabeled imaging agents. The present application is further directed to methods of preparing the radiolabeled imaging agent. Such imaging agents can used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT).

Substrate based PET imaging agents

Copper-catalyzed radiofluorination of iodonium salts, iodonium salts, and compounds obtained by copper-catalyzed radiofluorination of iodonium salts are disclosed. Diagnostic and therapeutic methods involving such compounds also are disclosed.

Copper catalyzed [18F]fluorination of iodonium salts

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.

Imaging agents for detecting neurological disorders

Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.

Imaging agents useful for identifying AD pathology

The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.

Development of molecular imaging probes for carbonic anhydrase-IX using click chemistry

Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.

Imaging agents for detecting neurological dysfunction

The present disclosure provides methods for treating cancer in a patient in need of such treatment, the method includes prequalifying a patient's therapeutic treatment by performing a molecular imaging procedure to the patient using a labeled biomarker specific for a cancer target at the tumor site; and administering a therapeutic effective amount of a compound comprising a targeting agent linked to a chemotherapeutic or a targeting agent linked to an antibody. Embodiments of the present invention also include compounds and compositions for using such methods.

Achievement of a high therapeutic index through molecular imaging guided targeted drug treatment

Growing community of inventors

Ypsilanti, MI, United States of America

Peter J H Scott