- AMINO-DIHYDROTHIAZINE AND AMINO-DIOXIDO DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE
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The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.
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- Fully automated continuous flow synthesis of highly functionalized imidazo[1,2-a] heterocycles
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[Chemical equation presented] The first continuous flow synthesis of imidazo[1,2-a]pyridine-2-carboxylic acids directly from 2-aminopyridines and bromopyruvic acid has been developed, representing a significant advance over the corresponding in-flask method. The process was applied to the multistep synthesis of imidazo[1,2-a]pyridine-2-carboxamides, including a Mur ligase inhibitor, using a two microreactor, multistep continuous flow process without isolation of intermediates.
- Herath, Ananda,Dahl, Russell,Cosford, Nicholas D.P.
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supporting information; experimental part
p. 412 - 415
(2010/04/26)
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- IMIDAZO[1,2-A]PYRIDINES FOR THE TREATMENT OF CNS AND CARDIAC DISEASES
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The present invention relates to imidazo[1,2-a]pyridine compounds of formula (1) STR1 which are dopamine D-4 antagonists and useful as anti-psychotic agents.
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