2-(取代萘-1-基)-4-喹唑啉酮化合物及其藥用組合物 2-Aryl-4-Quinazolinones And Their Pharmaceutical Compositions

專利類型

發明

專利國別 (專利申請國家)

美國

專利申請案號

13/953,882

專利證號

US 9,045,437 B2

專利獲證名稱

2-(取代萘-1-基)-4-喹唑啉酮化合物及其藥用組合物 2-Aryl-4-Quinazolinones And Their Pharmaceutical Compositions

專利所屬機關 (申請機關)

中國醫藥大學

獲證日期

2015/06/02

技術說明

惡性神經膠質瘤是中樞神經系統最常見的攻擊性成人原發性腫瘤，其治療包括手術、放療和 Temozolomide (TMZ)的輔助化療。然而，對 TMZ 的先天-或後天阻抗性成為目前治療的主要障礙，且 患者的預後情形很差。因此，新藥的開發對於惡性神經膠質瘤的治療是迫切需要的。 從我們的初步研究結果，發現 6-(吡咯啶-1-基)-2-(萘-1-基)喹唑啉-4-酮(MJ-66) 對人類惡性神經膠 質瘤細胞表現優異之抗增殖作用，其 IC50 約為 60 nM。在腦膠質瘤異種移植動物模型中，MJ-66（0.14 mg/kg/生理鹽水）由腹腔內注射給藥，每天一次，持續 10 天，在治療停止後十天發現 MJ-66 能顯著地抑制腫瘤生長，增加小鼠的存活，然而小鼠體重並無降低。 Malignant glioma is the most common aggressive adult primary tumor of the central nervous system. Treatments of malignant gliomas include surgery, radiotherapy and adjuvant temozolomide (TMZ) chemotherapy. However, inherent- and acquired resistance to TMZ present major obstacles to successful treatment, and the prognosis of patients with malignant gliomas remains very poor. Therefore, the development of new drugs for the treatment of malignant gliomas is urgently needed. In our preliminary results, 2-(naphthalene-1-yl)-6-pyrrolidinyl-4-quinazolinone (MJ-66) demonstrated excellent anti-proliferation effect especially on human malignant glioma cells with IC50 of approximately 60 nM. In intracranial glioma xenograft model, MJ-66 (0.14 mg/kg in saline, i.p., q.d., 10 days) significantly inhibited tumor growth and increased the survival of the experimental mice, however, did not decrease the body weight of mice.

備註

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產學合作處生物科技發展育成中心

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