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PDEdelta INHIBITOR FOR THE TREATMENT OF CANCER
专利权人:
Macau University of Science and Technology
发明人:
YAO, Xiao Jun,LEUNG, Lai Han,LUO, Lian Xiang,LIU, Liang
申请号:
AU2015101666
公开号:
AU2015101666A4
申请日:
2015.11.13
申请国别(地区):
AU
年份:
2016
代理人:
摘要:
#$%^&*AU2015101666A420160218.pdf#####ABSTRACT The present invention relates to the administration of a novel compound advantageously efficacious as PDE6 inhibitor and its effects on subjects with cancer. More specifically, the present invention is directed to a method for administering a compound having favorable geometric properties for interacting with the PDE6 prenyl-binding pocket, namely has certain structural components such as a three-cyclic backbone and at least one benzoyl-moiety in a side chain having at least two substituents containing highly electronegative atoms and being linked to the backbone via an aliphatic chain, for treating a subject suffering from a disease such as cancer, in particular non-small-cell lung cancer. The presence of said structural components particularly contributes to an advantageous interaction with PDE6, in particular with amino acids deep in the binding pocket. The present invention further provides a method to target tumor cells harboring an RAS gene mutation as well as pharmaceutical compositions comprising said compound. 32
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