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US 2009/0156472 A1Published application
Cyclic Depsipeptides
AssigneeNovartis AG
InventorsPhilipp Krastel, Brigitta-Maria Liechty, Joseph Gottfried Meingassner, Esther Shmitt, Erwin Paul Schreiner
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Abstract
The present application relates to cyclic depsipeptides, or derivatives thereof, having the structure of formula (I), and uses thereof, e.g. as inhibitors of kallikrein 7 and human neutrophil elastase.
Claims23
A cyclic depsipeptide, or a derivative thereof, having the structure of formula (I):
- wherein an ester bond is formed between the carboxy group of A7 and the hydroxy group of A2,
- wherein X and A1 are each independently optional,
- and wherein
- X is H or an amino group modifying moiety and may be typically selected from an aryl carbonyl residue or from an acyl residue,
- A1 is glutamine, ornithine, glutamic acid or a derivative thereof,
- A2 is threonine or serine,
- A3 is leucine,
- X is Ahp, 3-amino-piperidine-2-one, dehydro-AHP, Ahp-I, Ahp-II, proline, 5-hydroxy-proline or a derivative thereof, wherein the point of fusion (with A3 and A5) are at the nitrogen atom and the carboxyl oxygen (by virtue of the replacement of a hydrogen atom by a bond) of the proline, and 5-hydroxyproline,
- wherein Ahp, 3-amino-piperidine-2-one, dehydro-AUP, Ahp-I, and Ahp-II, are as defined below, and wherein the point of fusion (with A3 and A5) are at the nitrogen atoms of the said compounds (by virtue of the replacement of a hydrogen atom by a bond):
- wherein X is O or a bond, and R is an organic moiety or is a radical as defined in claim 3,
- A5 is isoleucine, phenylalanine or valine,
- A6 is tyrosine, N-Me-tyrosine or a derivative thereof,
- A7 is leucine, isoleucine or valine,
- or a pharmaceutically acceptable salt thereof.
11 more elements
A cyclic depsipeptide, or a derivative thereof, or a pharmaceutically acceptable salt thereof, in particular and essentially as described in the description and/or the working examples.
Dependencies are inferred from the claim text.