- PYRAZINE COMPOUND
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PROBLEM TO BE SOLVED: To provide a compound showing improved control activity on various pests or its salt. SOLUTION: The present invention provides a pyrazine compound having a 4-pyridyl group represented by formula (1) or its salt. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
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Paragraph 0247
(2019/07/11)
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- SYNTHESIS OF META-SUBSTITUTED [18F]-3-FLUORO-4-AMINOPYRIDINES BY DIRECT RADIOFLUORINATION OF PYRIDINE N-OXIDES
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Disclosed herein are methods for the fluorination aromatic N-heterocyclic N-oxides that comprise at least one leaving group. The N-oxides may be reduced to the fluorinated aromatic N-heterocyclic amine analogs. This novel fluorination approach may be successfully applied for synthesizing aromatic N-heterocyclic compounds labeled with 18F.
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Paragraph 0054
(2018/01/19)
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- Synthesis of: Meta -substituted [18F]3-fluoro-4-aminopyridine via direct radiofluorination of pyridine N -oxides
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Due to their electron-rich aromatic structure, nucleophilic (radio)fluorination of pyridines is challenging, especially at the meta position. In this paper, we describe the first example of direct fluorination of a pyridine N-oxide to produce a meta fluorinated pyridine. Specifically, fluorination of 3-bromo-4-nitropyridine N-oxide produced in several minutes 3-fluoro-4-nitropyridine N-oxide in moderate yield at room temperature. This intermediate compound was later converted to 3-fluoro-4-aminopyridine easily by catalytic hydrogenation. Furthermore, this approach was successfully applied for labeling with fluorine-18. The use of pyridine N-oxides for the preparation of fluoropyridines is unprecedented in the chemical literature and has the potential to offer a new way for the synthesis of these important structures in pharmaceuticals and radiopharmaceuticals.
- Brugarolas,Freifelder,Cheng,Dejesus
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supporting information
p. 7150 - 7152
(2016/06/09)
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- COMPOUNDS AND COMPOSITIONS FOR MODULATING EGFR ACTIVITY
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The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating EGFR activity, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated EGFR activity.
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Page/Page column 85; 86
(2014/01/08)
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- Chemical compounds
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Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
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Page/Page column 42
(2008/06/13)
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- Tropane derivatives useful in therapy
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The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.
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- Novel non-convalent thrombin inhibitors
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The present invention provides compounds which have a pyrazinone or pyridinone ring at P3 and an optionally substituted heteroaryl group at P1. These compounds have biological activity as active and potent inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds and pharmaceutical compositions comprising these compounds as therapeutic agents for treatment of disease states in mammals which are characterized by abnormal thrombosis are also described.
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- Potential anxiolytic agents. 2. Improvement of oral efficacy for the pyrido[1,2-a]benzimidazole (PBI) class of GABA-A receptor modulators
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We have further explored the structure-activity relationships of pyrido[1,2-α]benzimidazole (PBI) derivatives (viz. prototype 1), a novel series of central GABA-A receptor modulators, with the intent of enhancing oral efficacy. A study involving the introduction of acidic or basic groups led to the identification of RWJ-38293 (3a) as a potential anxiolytic agent.
- Maryanoff,McComsey,Ho,Shank,Dubinsky
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p. 333 - 338
(2007/10/03)
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