Literature DB >> 24387030

Aminothienopyridazines as imaging probes of tau pathology: a patent evaluation of WO2013090497.

Carlo Ballatore1, Amos B Smith, Virginia M-Y Lee, John Q Trojanowski, Kurt R Brunden.   

Abstract

Small-molecule ligands, amenable to positron emission tomography (PET) imaging of different types of neurodegenerative disease-associated amyloid deposits in the CNS of living patients, hold considerable promise for diagnostic purposes, as well as for monitoring disease progression and the effectiveness of treatments. The patent entitled 'Heterocyclic Compounds as Imaging Probes of Tau Pathology' (WO2013090497) discloses the identification of a novel class of tau imaging agents, the aminothienopyridazines. Selected compounds from this class are described that can stain selectively tau pathology in brain tissue sections. Moreover, examples of this class of compounds exhibit absorption, distribution, metabolism, excretion and pharmacokinetics (ADME-PK) properties that are appropriate for CNS PET ligands.

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Year:  2014        PMID： 24387030      PMCID： PMC4399384          DOI： 10.1517/13543776.2014.871526

Source DB:  PubMed          Journal:  Expert Opin Ther Pat        ISSN： 1354-3776            Impact factor:   6.674


  20 in total

Review 1.  Neurodegenerative tauopathies.

Authors:  V M Lee; M Goedert; J Q Trojanowski
Journal:  Annu Rev Neurosci       Date:  2001       Impact factor: 12.449

2.  [(18)F]T807, a novel tau positron emission tomography imaging agent for Alzheimer's disease.

Authors:  Chun-Fang Xia; Janna Arteaga; Gang Chen; Umesh Gangadharmath; Luis F Gomez; Dhanalakshmi Kasi; Chung Lam; Qianwa Liang; Changhui Liu; Vani P Mocharla; Fanrong Mu; Anjana Sinha; Helen Su; A Katrin Szardenings; Joseph C Walsh; Eric Wang; Chul Yu; Wei Zhang; Tieming Zhao; Hartmuth C Kolb
Journal:  Alzheimers Dement       Date:  2013-02-12       Impact factor: 21.566

3.  Imaging of tau pathology in a tauopathy mouse model and in Alzheimer patients compared to normal controls.

Authors:  Masahiro Maruyama; Hitoshi Shimada; Tetsuya Suhara; Hitoshi Shinotoh; Bin Ji; Jun Maeda; Ming-Rong Zhang; John Q Trojanowski; Virginia M-Y Lee; Maiko Ono; Kazuto Masamoto; Harumasa Takano; Naruhiko Sahara; Nobuhisa Iwata; Nobuyuki Okamura; Shozo Furumoto; Yukitsuka Kudo; Qing Chang; Takaomi C Saido; Akihiko Takashima; Jada Lewis; Ming-Kuei Jang; Ichio Aoki; Hiroshi Ito; Makoto Higuchi
Journal:  Neuron       Date:  2013-09-18       Impact factor: 17.173

4.  Uncharged thioflavin-T derivatives bind to amyloid-beta protein with high affinity and readily enter the brain.

Authors:  W E Klunk; Y Wang; G F Huang; M L Debnath; D P Holt; C A Mathis
Journal:  Life Sci       Date:  2001-08-17       Impact factor: 5.037

5.  Inhibition of tau aggregation in a novel Caenorhabditis elegans model of tauopathy mitigates proteotoxicity.

Authors:  Chronis Fatouros; Ghulam Jeelani Pir; Jacek Biernat; Sandhya Padmanabhan Koushika; Eckhard Mandelkow; Eva-Maria Mandelkow; Enrico Schmidt; Ralf Baumeister
Journal:  Hum Mol Genet       Date:  2012-05-18       Impact factor: 6.150

6.  Novel 18F-labeled arylquinoline derivatives for noninvasive imaging of tau pathology in Alzheimer disease.

Authors:  Nobuyuki Okamura; Shozo Furumoto; Ryuichi Harada; Tetsuro Tago; Takeo Yoshikawa; Michelle Fodero-Tavoletti; Rachel S Mulligan; Victor L Villemagne; Hiroyasu Akatsu; Takayuki Yamamoto; Hiroyuki Arai; Ren Iwata; Kazuhiko Yanai; Yukitsuka Kudo
Journal:  J Nucl Med       Date:  2013-07-15       Impact factor: 10.057

7.  A lipophilic thioflavin-T derivative for positron emission tomography (PET) imaging of amyloid in brain.

Authors:  Chester A Mathis; Brian J Bacskai; Stephen T Kajdasz; Megan E McLellan; Matthew P Frosch; Bradley T Hyman; Daniel P Holt; Yanming Wang; Guo-Feng Huang; Manik L Debnath; William E Klunk
Journal:  Bioorg Med Chem Lett       Date:  2002-02-11       Impact factor: 2.823

8.  Aminothienopyridazines and methylene blue affect Tau fibrillization via cysteine oxidation.

Authors:  Alex Crowe; Michael J James; Virginia M-Y Lee; Amos B Smith; John Q Trojanowski; Carlo Ballatore; Kurt R Brunden
Journal:  J Biol Chem       Date:  2013-02-26       Impact factor: 5.157

9.  Imaging brain amyloid in Alzheimer's disease with Pittsburgh Compound-B.

Authors:  William E Klunk; Henry Engler; Agneta Nordberg; Yanming Wang; Gunnar Blomqvist; Daniel P Holt; Mats Bergström; Irina Savitcheva; Guo-feng Huang; Sergio Estrada; Birgitta Ausén; Manik L Debnath; Julien Barletta; Julie C Price; Johan Sandell; Brian J Lopresti; Anders Wall; Pernilla Koivisto; Gunnar Antoni; Chester A Mathis; Bengt Långström
Journal:  Ann Neurol       Date:  2004-03       Impact factor: 10.422

10.  Early clinical PET imaging results with the novel PHF-tau radioligand [F18]-T808.

Authors:  David T Chien; A Katrin Szardenings; Shadfar Bahri; Joseph C Walsh; Fanrong Mu; Chunfang Xia; William R Shankle; Alan J Lerner; Min-Ying Su; Arkadij Elizarov; Hartmuth C Kolb
Journal:  J Alzheimers Dis       Date:  2014       Impact factor: 4.472
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