- HETERO-HALO 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 or any of Compounds 100-128 or any of those in Tables 2 or 3) 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 207
(2017/01/26)
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- A Michael Equilibration Model to Control Site Selectivity in the Condensation toward Aminopyrazoles
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A Michael equilibration model is presented to provide for site-selective pyrazole condensations between alkoxyacrylonitriles and hydrazines. Both pyrazole isomers were accessed with high selectivity by employment of kinetically or thermodynamically controlled conditions. Substrate scope and identification of Michael intermediates, as well as competitive pathways, support the presented mechanistic proposal. Sandmeyer derivatization provided site-selective access to fully substituted pyrazoles.
- Fandrick, Daniel R.,Sanyal, Sanjit,Kaloko, Joseph,Mulder, Jason A.,Wang, Yuwen,Wu, Ling,Lee, Heewon,Roschangar, Frank,Hoffmann, Matthias,Senanayake, Chris H.
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supporting information
p. 2964 - 2967
(2015/06/30)
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- Application of Ullmann and Ullmann-Finkelstein reactions for the synthesis of N-aryl-N-(1H-pyrazol-3-yl) acetamide or N-(1-aryl-1H-pyrazol-3-yl) acetamide derivatives and pharmacological evaluation
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Ullmann-type reactions are becoming a major tool in medicinal chemistry. In this article, we describe the use of these Copper-catalyzed reactions with various precursors, acyl-heteroarylamines or pyrazoles of interest for pharmacomodulation. To the medicinal chemist they offer new, usually untapped disconnection approaches to compounds of interest. They thus open the way to new original analogues of bioactive compounds possibly not patented, from common building-blocks. They also allow C to N bioisosteric replacements, which sometimes are synthetically challenging. We report for the first time the critical effect of acetylamino substituents on the regioselective arylation of unsymmetrical pyrazoles that are useful for medicinal chemists. Finally, we have applied this strategy to the design of novel AT1 receptor antagonists. Though this family has been extensively investigated in the past 30 years, N-arylation and C to N replacement made possible by Ullmann chemistry, can produce original antagonists.
- Deprez-Poulain, Rebecca,Cousaert, Nicolas,Toto, Patrick,Willand, Nicolas,Deprez, Benoit
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scheme or table
p. 3867 - 3876
(2011/11/12)
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- 4-CARBOX PYRAZOLE DERIVATES USEFUL AS ANTI-VIRAL AGENTS
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Novel antiviral compounds of Formula (I) : wherein: A represents hydroxy; R1 represents aryl, heteroaryl bonded through a ring carbon atom, or heterocyclyl bonded through a ring carbon atom, C1-6alkyl or -C5-9cycloalkyl, each of which may be optionally su
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Page/Page column 32-33
(2010/02/14)
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