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Polyalkylene glycol derivatives of inhibitors of epidermal growth factor receptor tyrosine kinase
专利权人:
Eyal Mishani
发明人:
Eyal Mishani,Samar Dissoki,Galith Abourbeh,Alexander Levitzki
申请号:
US11714760
公开号:
US08461166B2
申请日:
2007.03.07
申请国别(地区):
US
年份:
2013
代理人:
摘要:
Novel epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors, pharmaceutical compositions including same and their use in the treatment of EGFR-TK related diseases or disorders are disclosed. Novel radiolabeled EGFR-TK inhibitors as their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are further disclosed. The disclosed EGFR-TK inhibitors comprise a polyalkylene glycol moiety and/or a hydroxy-containing moiety and are characterized by improved solubility, biostability and bioavailability. Processes of preparing the disclosed EGFR-TK inhibitors and of radiolabeling same, via, for example, one-step radiosyntheses, are also disclosed.
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