Pharmaceutical compounds for use in the therapy of clostridium difficile infection
The invention relates to a compound described by a general formula (1), wherein each X independently from other X can be OPO 3 2− , OPSO 2 2− or OSO 3 − ; R 1 is a solubility function such as a polyethylene glycol moiety. The invention further relates to the use of the compounds according to the invention in the therapy of infection by Clostridium difficile.
1. A compound described by a general formula (1)
wherein R 1 is a solubility function R 2 selected from the group consisting of
a polyethylene glycol and
a polyglycerol,
and each X independently of any other X is selected from OPO 3 2− , OPSO 2 2− ,or OSO 3 − .
2. The compound according to claim 1 , wherein R 1 is a polyethylene glycol.
3. The compound according to claim 2 , wherein said polyethylene glycol is described by a formula (R 3 —(O—CH 2 —CH 2 ) n —) with R 3 being hydrogen, methyl or ethyl, and n having a value from 3 to 200.
4. The compound according to claim 2 , wherein said polyethylene glycol is described by a formula (R 3 —(O—CH 2 —CH 2 ) n —) with R 3 being hydrogen, methyl or ethyl, and n having a value selected from 3 to 200, 3 to 20, 10 to 30 and 9 to 45.
5. The compound according to claim 2 , wherein said polyethylene glycol is described by a formula (R 3 —(O—CH 2 —CH 2 ) n —) with R 3 being hydrogen, methyl or ethyl, and n having a value of 7, 9, 11 or 45.
6. The compound according to claim 2 described by a general formula (2a), or (3a)
wherein X and R 1 have the meaning outlined above.
7. The compound according to claim 2 described by a general formula (2b) or (3b)
wherein X and R1 have the meaning outlined above.
8. The compound according to claim 2 described by a general formula (4a) or (4b)
wherein R 1 has the meaning outlined above.
9. The compound according to claim 2 described by a general formula (5a) or (5b)
wherein R 1 has the meaning outlined above.
10. The compound according to claim 2 described by a general formula (6a) or (6b)
wherein R 1 has the meaning outlined above.
11. The compound according to claim 2 , wherein said polyethylene glycol is CH 3 (OCH 2 —CH 2 ) 9 —O— or CH 3 (OCH 2 —CH 2 ) 45 —O—.
12. The compound according to claim 2 , wherein said polyethylene glycol is CH 3 (OCH 2 —CH 2 ) 7 —O— or CH 3 (OCH 2 —CH 2 ) 11 —O—.
13. The compound according to claim 2 described by formula (7)
14. A compound described by a general formula (1)
wherein R 1 is a polyethylene glycol, each X independently of any other X is selected from OPO 3 2− , OPSO 2 2− , or OSO 3 − , and wherein said polyethylene glycol is described by a formula (R 3 —(O—CH 2 —CH 2 ) 2 —) with R 3 being hydrogen, methyl or ethyl.
15. The compound according to claim 14 described by a general formula (2a), or (3a)
wherein X and R 1 have the meaning outlined above.
16. The compound according to claim 14 described by a general formula (2b) or (3b)
wherein X and R1 have the meaning outlined above.
17. The compound according to claim 14 described by a general formula (4a) or (4b)
wherein R 1 has the meaning outlined above.
18. The compound according to claim 14 described by a general formula (5a) or (5b)
wherein R 1 has the meaning outlined above.
19. The compound according to claim 14 described by a general formula (6a) or (6b)
wherein R 1 has the meaning outlined above.