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US 2013/0172267 A1Published application
Use of cyclic depsipeptides to inhibit kallikrein 7
AssigneeNovartis AG
InventorsPhilipp KRASTEL, Brigitta-Maria Liechty, Esther Schmitt, Erwin Paul Schreiner
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Abstract
The present application relate to cyclic depsipeptides, or derivatives thereof, having the formula (I), and uses thereof, e.g. as inhibitors of kallikrein 7.
Claims10
Method of treating a subject suffering from a kallikrein 7-dependent disease, comprising:
- administering to said subject a therapeutically effective amount of a cyclic depsipeptide, or a derivative thereof, having the structure of formula (I):
- wherein the ester bond is found between the carboxy group of A7 and the hydroxy group of A2,
- wherein X and A1 are each independently optional,
- and wherein
- X is any chemical residue
- A1 is a standard amino acid,
- A2 is threonine or serine or 5-methylhydroxyproline,
- A3 is a non-basic standard amino acid or a non-basic non-standard amino acid, or a non-basic derivative thereof,
- A4 is Ahp, dehydro-AHP, proline or a derivative thereof,
- A5 is isoleucine, leucine, phenylalanin, prolin, threonine, or valine,
- A6 is alanine, phenylalanine, tryptophan, tyrosine or a derivative thereof
- A7 is leucine, isoleucine or valine,
- wherein the nitrogen atom of the amid bond between A5 and A6 can be substituted with a methyl
- or a pharmaceutically acceptable salt of cyclic depsipeptide or a derivative thereof.
11 more elements
5-7. (canceled)
Dependencies are inferred from the claim text.