Small Molecule Inhibitors of Dusp6 and Uses Therefor
AssigneeUniversity of Pittsburgh—Of the Commonwealth System of Higher Education
InventorsBilly W. Day, Waikok Michael Tsang, Vasiliy N. Korotchenko
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Abstract
Compounds that stimulate fibroblast growth factor production, and thus cell growth are provided. Also provided are compositions comprising the compounds and methods of using the compounds. The compounds can be used to treat wounds, to expand cell populations, such as hematopoietic cells, or to grow tissue in vitro, among other uses.
Claims20
A compound having the formula:
- in which R1 represents one or more independently of H, halo, C1-3 alkyl, C1-3 alkoxyl or —CN;
- R2 is a a secondary or tertiary amine group;
- R3 is one or more independently of H, halo, C1-3 alkyl, C1-3 alkoxyl or —CN;
- and R4 is ═O or —OH, wherein
- when both R1 and R3 are H,
- R4 is —OH, or
- R3 is one or more independently of halo, C1-3 alkyl, C1-3 alkoxyl or —CN, and
- when R1 is H and R4 is ═O, R3 is one or more independently of halo, C1-3 alkyl, C1-3 alkoxyl or —CN,
- or a pharmaceutically-acceptable salt thereof.
A method of inhibiting dual specificity phosphatase 6 (Dusp6)-induced dephosphorylation of extracellular signal-related kinase (ERK), comprising contacting a cell with a compound having the formula:
- in which R1 represents one or more independently of H, halo, C1-3 alkyl, C1-3 alkoxyl or —CN;
- R2 is a secondary or tertiary amine group;
- R3 is one or more independently of H, halo, C1-3 alkyl, C1-3 alkoxyl or —CN;
- and R4 is ═O or —OH, wherein
- when both R1 and R3 are H,
- R4 is —OH, or
- R3 is one or more independently of halo, C1-3 alkyl, C1-3 alkoxyl or —CN, and
- when R1 is H and R4 is ═O, R3 is one or more independently of halo, C1-3 alkyl, C1-3 alkoxyl or —CN,
- or a pharmaceutically-acceptable salt thereof, in an amount effective to inhibit dephosphorylation of ERK by Dusp6.
Dependencies are inferred from the claim text.