- THIENOPYRIMIDINE AS CDC7 KINASE INHIBITORS
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The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer
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Page/Page column 154-155
(2010/09/18)
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- Synthesis of the new α- and β-adrenergic antagonist 1-[1-(2-benzodioxanylmethyl)-4-piperidyl]amino-3-(1-naphthoxy)-2- propanol
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The synthesis and in vitro α- and β-adrenergic blocking potency of 1-[1-(2-benzodiaxanylmethyl)-4-piperidyl]amino-3-(1-naphthoxy)-2- propanol (I) are described. Thus, N-benzyl-4piperidone was protected and debenzylated to the carbamate (V), which upon alkaline hydrolysis and acylation gave benzodioxanic amide (IX). Reduction of the amide group, deprotection of the ketone function of (X), and reductive amination gave the 4-aminopiperidine (XIII), which was finally condensed with the appropriate epoxide to yield the aminopropanol (I). Compound (I) is formally derived from a combination of piperoxan (II) and propranolol (III), and was approximately 10 times less potent than each one of these drugs, as an α- and β-adrenergic blocker respectively.
- Mauleon,Antunez,Rosell
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p. 1109 - 1117
(2007/10/02)
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