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QUINOXALINE DERIVATIVES WHICH ARE SELECTIVE AGAINST TRYPANOSOMA CRUZI AND DO NOT CAUSE MUTAGENIC EFFECTS

机译：选择性抗锥RY克鲁斯（QRYPANOSOMA CRUZI）的喹诺酮衍生物，不会引起诱变效应

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摘要

The present invention relates to derivatives of 3- trifluoromethylquinoxaline 1,4-dioxide (QDO) with ester or amide functionality in the 2 position, with excellent selectivity for Trypanosoma cruzi, and which present a selective mechanism of action that is different to the drugs used in therapy and do not cause mutagenicity. These compounds have a lipophilicity that is suitable for use in any pharmaceutical formulation. The invention comprises the QDO compounds of Formula I and II (Figure 6), the derivatives thereof, the methods for preparing said compounds by reacting a benzofuroxan and a trifluoromethyl. The invention also relates to pharmaceutical formulations for treating patients with Chagas disease and to the use of the claimed compounds.

机译：本发明涉及3-三氟甲基喹喔啉1，4-二氧化物（QDO）的酯或酰胺官能度在2位的衍生物，其对克鲁维氏锥虫的选择性优异，并具有选择性的作用机理。与治疗中使用的药物不同，不会引起诱变。这些化合物具有适用于任何药物制剂的亲脂性。本发明包括式I和II的QDO化合物（图6），其衍生物，通过使苯并呋喃和三氟甲基反应制备所述化合物的方法。本发明还涉及用于治疗患有恰加斯病的患者的药物制剂以及所要求保护的化合物的用途。

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公开/公告号WO2012096556A1

专利类型
公开/公告日2012-07-19

原文格式PDF
申请/专利权人 MONGE ANTONIO;PEREZ SILVIA;ALDANA IGNACIO;MORENO ELSA;TORRES ENRIQUE;CERECETTO MEYER HUGO;GONZALEZ HORMAIZTEGUY MARIA MERCEDES;PANIAGUA SOLIS JORGE FERNANDO;
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申请/专利号WO2011MX00006
发明设计人 MONGE ANTONIO;PEREZ SILVIA;ALDANA IGNACIO;MORENO ELSA;TORRES ENRIQUE;CERECETTO MEYER HUGO;GONZALEZ HORMAIZTEGUY MARIA MERCEDES;PANIAGUA SOLIS JORGE FERNANDO;
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申请日2011-01-11
分类号C07D241/52;A61K31/498;
国家 WO
入库时间 2022-08-21 17:14:43

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