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US 10,588,909 B2Granted
Modulators of HEC1 activity and methods therefor
AssigneesTaivex Therapeutics Corporation, Development Center for Biotechnology
InventorsJiann-Jyh Huang, Shih-Hsien Chuang, Ying-Shuan Eda Lee, Yu-Ling Huang, Johnson Lau
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Abstract
Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Such compounds disrupt Nek2/Hec1 binding and may be useful as chemotherapeutic agents for neoplastic diseases.
Claims12
A method for inhibiting a xenograft tumor outgrowth, comprising:
- administering to a mammal in need thereof a compound according to Formula I in an amount effective to inhibit the xenograft tumor outgrowth;
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is ORa or SRa;
- Ra and R1 is pyrazine, optionally substituted with alkoxy or methoxyalkoxy;
- R2 and R3 are independently hydrogen, C1-C6 alkyl, or halogen;
- R4 is hydrogen or halogen;
- R5 is
- and
- wherein Ra, Rb, Rc, and Rd in R5 are independently hydrogen, halogen, C1-C6 alkyl, or amino.
6 more elements
A method for inhibiting a xenograft tumor outgrowth, comprising:
- administering to a mammal in need thereof a compound in an amount effective to inhibit the xenograft tumor outgrowth or a pharmaceutically acceptable salt thereof, wherein the compound has a structure selected from the group consisting of
A method of disrupting Hec1/Nek2 interaction, comprising contacting a Hec1/Nek2 complex with a compound according to Formula I in an amount effective to disrupt Hec1/Nek2 binding,
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is ORa or SRa;
- Ra in R1 is pyrazine, optionally substituted with alkoxy or methoxyalkoxy;
- R2 and R3 are independently hydrogen, C1-C6 alkyl, or halogen;
- R4 is hydrogen or halogen;
- R5 is
- and
- wherein Ra, Rb, Rc, and Rd in R5 are independently hydrogen, halogen, C1-C6 alkyl, or amino.
5 more elements
Dependencies are inferred from the claim text.