Organic compounds
A compound of formula (I) wherein Y is oxygen or sulfur, and X 1 , X 2 and X 3 are independently of each other hydrogen, halogen, hydroxy or linear or branched (C 1-6 )-alkoxy, or hydroxy-(C 1-6 )alkyl or (C 1-6 )alkoxy-(C 1-6 )alkyl, mono- or dihalogenated (C 1-6 )-alkyl, amino(C 1-6 )-alkyl, hydroxy(C 1-6 )-alkyl, with one of the two provisos that: (1) at least of X 1 , X 2 and X 3 is other than hydrogen, and (2) X 2 is other than hydroxy, when X 1 and X 3 are hydrogen.
1. A compound of formula (I) comprising:
optionally in the form of a salt,
wherein
Y is oxygen or sulfur, and
X 1 ,X 2 and X 3 are independently of each other hydrogen, halogen, or (C 1-6 )-alkoxy, with the proviso that at least one of X 1 , X 2 and X 3 is other than hydrogen.
2. The compound of claim 1 , which is selected from the group consisting of:
14-O-[(3-Fluoro-phenylsulfanyl)-acetyl]-mutilin,
14-O-[(4-Fluoro-phenylsulfanyl)-acetyl]-mutilin,
14-O-[(3,5-Difluoro-phenylsulfanyl)-acetyl]-mutilin,
14-O-[(3,4-Difluoro-phenylsulfanyl)-acetyl]-mutilin,
14-O-[(3-Methoxy-phenylsulfanyl)-acetyl]-mutilin,
14-O-[(4-Methoxy-phenylsulfanyl)-acetyl]-mutilin, and
14-O-[(3,4-Dimethoxy-phenylsulfanyl)-acetyl]-mutilin.
3. The compound of claim 1 , in the form of a salt.
4. The compound of claim 1 , wherein the compound is in a pharmaceutical composition.
5. A pharmaceutical composition comprising:
a compound of claim 1 in association with at least one pharmaceutical excipient.
6. The pharmaceutical composition of claim 5 , further comprising another pharmaceutically active agent.
7. The compound of claim 2 , in the form of a salt.
8. A pharmaceutical composition comprising:
a compound of claim 2 in association with at least one pharmaceutical excipient.
9. A pharmaceutical composition comprising:
a compound of claim 3 in association with at least one pharmaceutical excipient.
10. A compound of formula (I) comprising:
optionally in the form of a salt,
wherein
Y is oxygen or sulfur, and
X i , X 2 and X 3 are independently of each other hydrogen or halogen, with the proviso that at least one of X 1 , X 2 and X 3 is other than hydrogen.
11. The compound of claim 10 , which is selected from the group consisting of:
14-O-[(3-Fluoro-phenylsulfanyl)-acetyl]-mutilin,
14-O-[(4-Fluoro-phenylsulfanyl)-acetyl]-mutilin,
14-O-[(3,5-Difluoro-phenylsulfanyl)-acetyl]-mutilin, and
14-O-[(3,4-Difluoro-phenylsulfanyl)-acetyl]-mutilin.
12. The compound of claim 10 , in the form of a salt.
13. The compound of claim 11 , in the form of a salt.
14. A pharmaceutical composition comprising:
a compound of claim 10 in association with at least one pharmaceutical excipient.
15. A pharmaceutical composition comprising:
a compound of claim 11 in association with at least one pharmaceutical excipient.
16. The compound of claim 2 , which is selected from the group consisting of:
14-O-[(3-Methoxy-phenylsulfanyl)-acetyl]-mutilin,
14-O-[(4-Methoxy-phenylsulfanyl)-acetyl]-mutilin, and
14-O-[(3,4-Dimethoxy-phenylsulfanyl)-acetyl]-mutilin, optionally in the form of a salt.
17. A method of treating bacterial infections caused by Staphylococcus aureus, Enterococcus faecalis, Streptococcus pneumonia, Moraxelly catarrhalis and Escherichia coli , comprising administering to a subject in need of such treatment an effective amount of a compound of claim 1 , optionally in the form of a pharmaceutically acceptable salt.
18. A method of treating bacterial infections caused by Staphylococcus aureus, Enterococcus faecalis, Streptococcus pneumonia, Moraxelly catarrhalis and Escherichia coli , comprising administering to a subject in need of such treatment an effective amount of a compound of claim 2 , optionally in the form of a pharmaceutically acceptable salt.
19. A method of treating bacterial infections caused by Staphylococcus aureus, Enterococcus faecalis, Streptococcus pneumonia, Moraxelly catarrhalis and Escherichia coli , comprising administering to a subject in need of such treatment an effective amount of a compound of claim 10 , optionally in the form of a pharmaceutically acceptable salt.
20. A method of manufacturing a composition for treatment of diseases mediated by microbes, the method comprising:
obtaining a compound according to claim 1 ; and
including the compound in a medicament for the treatment of diseases mediated by microbes.