发明名称 |
N-OXIDE-CONTAINING PHARMACEUTICAL COMPOUNDS |
摘要 |
<p>The invention provides a method of preparing a therapeutically active compound having reduced hERG activity, which method comprises: (a) selecting a non-N-oxide drug compound containing a basic tertiary amino group, wherein said non-N-oxide compound is known to have or is suspected of having a therapeutically unacceptable level of hERG inhibitory activity; (b) testing the non-N-oxide drug compound for hERG inhibitory activity; (c) reacting the non-N-oxide drug compound with an oxidising agent to form an N- oxide drug compound having an N-oxide at the basic tertiary amino group; (d) testing the N-oxide drug compound for hERG inhibitory activity; (e) testing the N-oxide drug compound for therapeutically useful activity; (f) comparing the hERG inhibitory activity of the N-oxide drug compound and non- N-oxide drug compound; and (g) when the N-oxide drug compound has therapeutically useful activity and has hERG activity which is at least ten fold less than the hERG inhibitory activity of the non-N-oxide drug compound, formulating the N-oxide drug compound for use in medicine. Also provided by the invention are novel compounds prepared by the aforementioned method and the use of the novel compounds in medicine.</p> |
申请公布号 |
WO2008139152(A1) |
申请公布日期 |
2008.11.20 |
申请号 |
WO2008GB01595 |
申请日期 |
2008.05.09 |
申请人 |
SENTINEL ONCOLOGY LIMITED;BOYLE, ROBERT, GEORGE;TRAVERS, STUART |
发明人 |
BOYLE, ROBERT, GEORGE;TRAVERS, STUART |
分类号 |
C07C291/04;A61K31/13;A61P35/00;C07C311/32;C07D401/12;C07D403/14;C07D413/14;C07D417/12;C07D417/14 |
主分类号 |
C07C291/04 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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