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    • 20. 发明申请
    • 4-ANILIDO SUBSTITUTED QUINAZOLINES AND USE THEREOF AS INHIBITORS OF EPIDERMAL GROWTH FACTOR RECEPTOR KINASES
    • 4-ANILIDO取代喹啉腈及其作为抗生殖因子受体激动剂的抑制剂
    • WO2004013091A2
    • 2004-02-12
    • PCT/IL2003/000632
    • 2003-07-31
    • YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEMGAZIT, AvivLEVITZKI, Alexander
    • GAZIT, AvivLEVITZKI, Alexander
    • C07D
    • C07D401/12A61K31/517C07D239/86C07D239/88C07D239/94C07D239/95C07D403/04C07D403/12C07D417/12C07D417/14
    • The present invention provides 4-anilido substituted quinazoline compounds which are potent inhibitors of protein tyrosine (PTK) kinase activity, particularly epidermal growth factor receptor (EGFR) kinase activity, and pharmaceutical compositions comprising these compounds. The present invention further provides methods of inhibiting the activity of a protein tyrosine kinase (PTK), for example an EGFR kinase, comprising the step of contacting the PTK with an effective inhibitory amount of any of the quinazoline compounds defined herein. The present invention further provides a method of inhibiting the activity of a protein tyrosine kinase (PTK) in a subject, for example an EGFR kinase, comprising the step of administering to the subject a therapeutically effective amount of any of the quinazoline compounds defined herein. The present invention further provides a method of treating or preventing a protein tyrosine kinase (PTK) related disorder in a subject, for example an EGFR related disorder, comprising the step of administering to the subject a therapeutically effective amount of any of the quinazoline compounds defined herein. The quinazoline compounds are useful in treating a variety of PTK related disorders such as cell proliferative disorders, fibrotic disorders, metabolic disorders and cancer.
    • 本发明提供了作为蛋白酪氨酸(PTK)激酶活性,特别是表皮生长因子受体(EGFR)激酶活性的有效抑制剂的4-苯胺基取代的喹唑啉化合物,以及包含这些化合物的药物组合物。 本发明进一步提供了抑制蛋白酪氨酸激酶(PTK),例如EGFR激酶的活性的方法,其包括使PTK与有效抑制量的本文定义的任何喹唑啉化合物接触的步骤。 本发明进一步提供了抑制受试者例如EGFR激酶中蛋白质酪氨酸激酶(PTK)的活性的方法,包括向受试者施用治疗有效量的本文定义的任何喹唑啉化合物的步骤。 本发明还提供了治疗或预防受试者中的蛋白酪氨酸激酶(PTK)相关病症的方法,例如EGFR相关病症,其包括向受试者施用治疗有效量的任何定义的喹唑啉化合物 于此。 喹唑啉化合物可用于治疗各种PTK相关疾病,例如细胞增殖性疾病,纤维化病症,代谢紊乱和癌症。