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US 8,999,983 B2Granted
Modulators of Hec1 activity and methods therefor
AssigneesTaivex Therapeutics Corporation, Development Center of 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.
Claims13
A compound having a structure according to Formula I
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is ORa or SRa;
- Ra of ORa or SRa is pyrazine, wherein Ra of ORa or SRa is optionally substituted with alkoxy or methoxyalkoxy;
- R2 and R3 are independently hydrogen, C1-C6 alkyl, or halogen;
- R4 is hydrogen or halogen;
- wherein Ra, Rb, Rc, and Rd in R5 are independently hydrogen, halogen, C1-C6 alkyl, or amino.
3 more elements
A method of improving a pharmacokinetic parameter for a compound having a structure selected from the group consisting of
- comprising a step of forming a tosylate salt of the compound;
- wherein the pharmacokinetic parameter comprises an area under the curve (AUC);
- and
- wherein the improvement is increasing AUC in oral administration of the compound.
1 more element
A pharmaceutical composition comprising a carrier and a tosylate salt of a compound having a structure selected from the group consisting of
Dependencies are inferred from the claim text.