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1. 发明申请

US20080124407A1 INHIBITING CYP3A4 INDUCTION 审中-公开
标题翻译：抑制CYP3A4诱导
公开(公告)号：US20080124407A1
公开(公告)日：2008-05-29
申请号：US11867299
申请日：2007-10-04
申请人： David L. Eaton , Kenneth Thummel , Changcheng Zhou , Theo Bammler
发明人： David L. Eaton , Kenneth Thummel , Changcheng Zhou , Theo Bammler
IPC分类号： A61K36/38 , A61K31/26 , A61P9/12 , A61K31/5517 , A61K31/497
CPC分类号： A61K31/26 , A61K31/497 , A61K31/5517
摘要： The present invention is directed to a method of inhibiting CYP3A4 induction. The method involves administering a compound of the following formula: R1—X—(CH2)n—N═C═S with R1, X, and n defined herein, binds to a Pregnane X Receptor or Steroid and Xenobiotic Receptor (SXR or NR1I2) under conditions effective to inhibit CYP3A4 gene induction. The present invention also include a method of administering a compound, described herein, together with the CYP3A4 inducer to prevent a loss of efficacy in the subject to whom the CYP3A4 inducer is repeatedly administered. In addition, such compounds can be administered to block the interaction between a CYP3A4 inducer and another drug being administered that is a substrate of CYP3A4.
摘要翻译：本发明涉及抑制CYP3A4诱导的方法。该方法包括给予下式化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> R 1 -X-（CH）＆lt; N＆gt; -NCS＆lt;？in-line-formula description =“In-line Formulas”end =“tail”？> R＆lt; 1＆lt; 和n定义在有效抑制CYP3A4基因诱导的条件下与妊娠X受体或类固醇和异生素受体（SXR或NR1I2）结合。本发明还包括与CYP3A4诱导剂一起施用本文所述的化合物以防止在重复施用CYP3A4诱导物的受试者中的功效丧失的方法。此外，可以施用这样的化合物以阻断CYP3A4诱导剂与作为CYP3A4的底物的另一种正在给药的药物之间的相互作用。

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