# US 9,751,903 B2 · Pharmaceutical compounds for use in the therapy of clostridium difficile infection

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- Number: US 9,751,903 B2
- Document ID: US9751903B2
- Status: Granted
- Kind: B2
- Application number: 15/172,171
- Filed: 2016-06-03
- Published: 2016-09-29
- Granted: 2017-09-05
- Earliest claimed: 2011-09-29
- Assignees: ETH Zurich
- Applicants: ETH Zurich
- Inventors: Bastien Castagner; Jean-Christophe Leroux; Mattias Ivarsson; Gisbert Schneider; Anna Pratsinis
- Web page: https://patentgrep.com/patent/US9751903B2

## CPC

- C07F 9/117: with cycloaliphatic alcohols
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)

## Abstract

The invention relates to a compound described by a general formula (1), wherein each X independently from other X can be OPO32−, OPSO22− or OSO3−; R1 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.

## Claims

### Claim 1

A compound described by a general formula (1)
wherein R1 is a solubility function R2 selected from the group consisting of
a polyethylene glycol and
a polyglycerol,
and each X independently of any other X is selected from OPO32−, OPSO22−,or OSO3−.

### Claim 2 (depends on 1)

The compound according to claim 1, wherein R1 is a polyethylene glycol.

### Claim 3 (depends on 2)

The compound according to claim 2, wherein said polyethylene glycol is described by a formula (R3—(O—CH2—CH2)n—) with R3 being hydrogen, methyl or ethyl, and n having a value from 3 to 200.

### Claim 4 (depends on 2)

The compound according to claim 2, wherein said polyethylene glycol is described by a formula (R3—(O—CH2—CH2)n—) with R3 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.

### Claim 5 (depends on 2)

The compound according to claim 2, wherein said polyethylene glycol is described by a formula (R3—(O—CH2—CH2)n—) with R3 being hydrogen, methyl or ethyl, and n having a value of 7, 9, 11 or 45.

### Claim 6 (depends on 2)

The compound according to claim 2 described by a general formula (2a), or (3a)
wherein X and R1 have the meaning outlined above.

### Claim 7 (depends on 2)

The compound according to claim 2 described by a general formula (2b) or (3b)
wherein X and R1 have the meaning outlined above.

### Claim 8 (depends on 2)

The compound according to claim 2 described by a general formula (4a) or (4b)
wherein R1 has the meaning outlined above.

### Claim 9 (depends on 2)

The compound according to claim 2 described by a general formula (5a) or (5b)
wherein R1 has the meaning outlined above.

### Claim 10 (depends on 2)

The compound according to claim 2 described by a general formula (6a) or (6b)
wherein R1 has the meaning outlined above.

### Claim 11 (depends on 2)

The compound according to claim 2, wherein said polyethylene glycol is CH3(OCH2—CH2)9—O— or CH3(OCH2—CH2)45—O—.

### Claim 12 (depends on 2)

The compound according to claim 2, wherein said polyethylene glycol is CH3(OCH2—CH2)7—O— or CH3(OCH2—CH2)11—O—.

### Claim 13 (depends on 2)

The compound according to claim 2 described by formula (7)

### Claim 14

A compound described by a general formula (1)
wherein R1 is a polyethylene glycol, each X independently of any other X is selected from OPO32−, OPSO22−, or OSO3−, and wherein said polyethylene glycol is described by a formula (R3—(O—CH2—CH2)2—) with R3 being hydrogen, methyl or ethyl.

### Claim 15 (depends on 14)

The compound according to claim 14 described by a general formula (2a), or (3a)
wherein X and R1 have the meaning outlined above.

### Claim 16 (depends on 14)

The compound according to claim 14 described by a general formula (2b) or (3b)
wherein X and R1 have the meaning outlined above.

### Claim 17 (depends on 14)

The compound according to claim 14 described by a general formula (4a) or (4b)
wherein R1 has the meaning outlined above.

### Claim 18 (depends on 14)

The compound according to claim 14 described by a general formula (5a) or (5b)
wherein R1 has the meaning outlined above.

### Claim 19 (depends on 14)

The compound according to claim 14 described by a general formula (6a) or (6b)
wherein R1 has the meaning outlined above.
