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1. (WO2019027366) ANTIMICROBIAL PEPTIDOMIMETICS
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THE CLAIMS DEFINING THE INVENTION:

1. A compound of formula


or a pharmaceutically acceptable salt or solvate thereof;

wherein Li is -(CH2)m-, C2-C5 alkenylene, C2-C5 alkynylene, C3-C6 cycloalkylene, phenylene or benzylene, wherein m is selected from 1 to 5;

wherein Ri and R2 are independently selected from H or CH3, or

Ri is selected from H or CH3 and R2 is


wherein L2 is -(CH2)n-, C2-C5 alkenylene, C2-C5 alkynylene, C3-C6 cycloalkylene, phenylene or benzylene, wherein n is selected from 1 to5;

wherein R3-R8 are independently H, CI, I, Br or F;

wherein at least one of R3-R8 is CI, I, Br or F;

wherein L3 is -(CH2)0-, C2-C5 alkenylene, C2-C5 alkynylene, C3-C6 cycloalkylene, phenylene or benzylene, wherein o is selected from 1 to 5;

wherein L4 is -(CH2)P-, C2-C5 alkenylene, C2-C5 alkynylene, C3-C6 cycloalkylene, phenylene or benzylene, wherein p is selected from 1 to 5;

wherein Rio, Rn and R12 are independently H or -CH3.

A process of making compounds of formula (I)


or a pharmaceutically acceptable salt or solvate thereof;

wherein Li is -(CH2)m-, C2-C5 alkenylene, C2-C5 alkynylene, C3-C6 cycloalkylene, phenylene or benzylene, wherein m is selected from 1 to 5;

wherein Ri and R2 are independently selected from H or CH3, or

Ri is selected from H or CH3 and R2 is


wherein L2 is -(CH2)n-, C2-Cs alkenylene, C2-Cs alkynylene, C3-C6 cycloalkylene, phenylene or benzylene, wherein n is selected from 1 to5;

wherein R3-R8 are independently H, CI, I, Br or F;

wherein at least one of R3-R8 is CI, I, Br or F;

wherein R9 is

wherein L3 is -(CH2)0-, C2-Cs alkenylene, C2-Cs alkynylene, C3-C6 cycloalkylene, phenylene or benzylene, wherein o is selected from 1 to 5;

wherein L4 is -(CH2)P-, C2-Cs alkenylene, C2-Cs alkynylene, C3-C6 cycloalkylene, phenylene or benzylene, wherein p is selected from 1 to5;

wherein Rio, Rn and Ri2 are independently H or -CH3,

by reacting following compounds of formula (II):


wherein R6, R7, Rg, Rio, Rn,Ri2, Li, L3 and L4 have the meaning given above; wherein PGi, PG2 and PG3 can be any protecting group such as t-Boc or Pbf;

in the presence of an amide/peptide cou ling reagent with compounds of the formula (III)


wherein R2-R5 are defined as mentioned above,

wherein * denotes an stereogenic carbon;

and deprotection with an acid.

3. A compound of formula (I) according to claim 1 or a pharmaceutically acceptable salt or solvate therefore for use as a medicament.

4. A compound of formula (I) according to claim 1 or a pharmaceutically acceptable salt or solvate thereof for use in the treatment of diseases, disorders and conditions which are a bacteria infection.

5. The compound of claim 4 wherein the bacterial infection is caused by a Gram- positive bacteria strain.

6. The compound of claim 4 wherein the bacterial infection is caused by Staphylococcus aureus, Methicillin-resistant Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae or Propionibacterium acnes.

7. The compound of claim 4 wherein the bacterial infection is caused by bacteria that have gained a resistance against the penicillin-type antibiotics, Vancomycin, Linezolid, Retapamulin, Tigecycline or Mupirocin.

8. The compound of claim 4 wherein the bacterial infection is treated by topical use of the compound.

9. Use of a compound of formula (I) according to claim 1 or a pharmaceutically acceptable salt or solvate thereof in the manufacture of a medicament for the treatment of a disease, disorder or condition selected from any bacterial infection.

10. The compound of claim 9 wherein the bacterial infection is caused by a Gram- positive bacteria strain.

11. The use according to claim 9 wherein the bacterial infection is caused by Staphylococcus aureus, Meticillin-resistant Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae or Propionibacterium acnes.

12. The use according to claim 9 wherein the bacterial infection is caused by bacteria that have gained a resistance against the penicillin-type antibiotics, Vancomycin, Linezolid, Retapamulin, Tigecycline or Mupirocin.

13. The use according to claim 9 wherein the bacterial infection is treated by topical application of a compound of formula (I).

14. A method of treating a bacterial infection caused disease, disorder or condition in a subject in need of such treatment, comprising administered to said subject a compound of formula (I) according to claim 1 or a pharmaceutically acceptable salt or solvate thereof.

15. The method according to claim 14 wherein the bacterial infection is treated by topical application of a compound of formula (I).

16. A method of treating or preventing an acne condition in a subject in need of such treatment, comprising administering to said subject a compound of the formula (I) or a pharmaceutically acceptable salt or solvate thereof.

17. A method of disinfecting a surface against bacterial contamination, comprising applying to said surface a compound of the formula (I) or an acceptable salt or solvates thereof.

18. A pharmaceutical composition comprising a compound of formula (I) according to claim 1 or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable excipient.

19. A pharmaceutical composition comprising a compound of formula (I) according to claim 1 or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable excipient for use in the treatment of a bacterial infection.