- Radiosynthesis of SPECT tracers: Via a copper mediated 123I iodination of (hetero)aryl boron reagents
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A general method for the copper mediated nucleophilic 123I-iodination of (hetero)aryl boronic esters and acids has been developed. The broad substrate scope of this radiosynthetic approach allows access to [123I]DPA-713, [123I]IMPY, [123I]MIBG and [123I]IPEB that are four commonly used SPECT radiotracers. Our results infer that aryl boronic reagents can now be employed as common precursors for both fluorine-18 and iodine-123 radiolabelling.
- Wilson, Thomas C.,McSweeney, Greg,Preshlock, Sean,Verhoog, Stefan,Tredwell, Matthew,Cailly, Thomas,Gouverneur, Véronique
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supporting information
p. 13277 - 13280
(2016/11/17)
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- INHIBITORS OF HISTONE DEACETYLASE
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This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula (I), (II), (IIa), (III), (IV), (V), or (VI)) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.
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Paragraph 0271
(2016/04/26)
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- RADIOACTIVE FLUORINE-LABELED QUINOXALINE COMPOUND
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Provided is a compound effective as a diagnostic imaging probe targeting amyloid and an agent for Alzheimer's disease diagnosis including the compound.
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Paragraph 0048-0049
(2014/04/03)
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- Structure-activity relationships and in vivo evaluation of quinoxaline derivatives for PET imaging of β-amyloid plaques
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This letter describes the synthesis, structure-activity relationships, and in vivo evaluation of a new series of 2-phenylquinoxaline (PQ) derivatives for imaging β-amyloid (Aβ) plaques in Alzheimer's disease (AD). In experiments in vitro, the affinity of
- Yoshimura, Masashi,Ono, Masahiro,Matsumura, Kenji,Watanabe, Hiroyuki,Kimura, Hiroyuki,Cui, Mengchao,Nakamoto, Yuji,Togashi, Kaori,Okamoto, Yoko,Ihara, Masafumi,Takahashi, Ryosuke,Saji, Hideo
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supporting information
p. 596 - 600
(2013/07/26)
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- COMPOSITIONS AND METHODS FOR THE TREATMENT AND ANALYSIS OF NEUROLOGICAL DISORDERS
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Provided herein are compositions and methods for the treatment and analysis of neurological disorders. In particular, provided herein are small molecules targeted to amyloid-β (Aβ ) or metal-Aβ species for the treatment, diagnosis, or study of neurological conditions such as Alzheimer's disease (AD) and other diseases and conditions.
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- 2-Arylimidazo[2,1-b]benzothiazoles: A new family of amyloid binding agents with potential for PET and SPECT imaging of Alzheimer's brain
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We designed and synthesized a small series of 2-aryl-imidazo[2,1-b] benzothiazole, representing a combination of motifs from the two most potent amyloid imaging agents, PIB and IMPY. The binding affinity of the new compounds ranged from 6 to 133 nM. Among the best compounds, 3b (Ki = 6 nM) can be labeled with 11CH3 for PET imaging whereas 3j (K i = 10.9 nM) can be labeled with 123I for SPECT imaging.
- Alagille, David,Dacosta, Herve,Baldwin, Ronald M.,Tamagnan, Gilles D.
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scheme or table
p. 2966 - 2968
(2011/06/24)
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- Small molecule modulators of copper-induced Aβ aggregation
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(Chemical Equation Presented) Our design of bifunctional metal chelators as chemical probes and potential therapeutics for Alzheimer's disease (AD) is based on the incorporation of a metal binding moiety into structural frameworks of Aβ aggregate-imaging
- Hindo, Sarmad S.,Mancino, Allana M.,Braymer, Joseph J.,Liu, Yihong,Vivekanandan, Subramanian,Ramamoorthy, Ayyalusamy,Lim, Mi Hee
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supporting information; experimental part
p. 16663 - 16665
(2010/02/15)
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- Compounds and amyloid probes thereof for therapeutic and imaging uses
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The present invention provides compounds and amyloid probes thereof that allow for an antemortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the
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Page/Page column 28; 39
(2008/06/13)
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- Intramolecular sensitisation of lanthanide(III) luminescence by acetophenone-containing ligands: The critical effect of para-substituents and solvent
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Tetraazamacrocyclic ligands have been prepared in which three of the four nitrogen atoms are functionalised with carboxylate donors and the fourth is alkylated with apara-substituted acetophenone group {-CH2C(O)C6H4-X, whe
- Beeby, Andrew,Bushby, Lisa M.,Maffeo, Davide,Gareth Williams
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- A facile protocol for the convenient preparation of amino-substituted α-bromo- and α,α-dibromo arylmethylketones
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Amino-substituted arylmethylketones are selectively brominated in sulfuric acid to afford the corresponding dibromomethylarylketones that are then debrominated with diethylphosphite to give the desired bromomethylarylketones in excellent yield.
- Diwu, Zhenjun,Beachdel, Christopher,Klaubert, Dieter H.
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p. 4987 - 4990
(2007/10/03)
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