SIEBER STEPHAN (DE)
KUNOLD ELENA (DE)
| AMENDED CLAIMS received by the International Bureau on 07 February 2018 (07.02.2018) 1 . A compound for use in the treatment of a bacterial disease, said compound having a structure according to Formula I wherein R1 , R2, R7, R8, R9 are each independently selected from the group consisting of hydrogen, halogen, cyano, (CrC6)alkyl and (CrC6)haloalkyl, preferably wherein R7, R8, R9 are hydrogen and R1 is selected from the group consisting of hydrogen, cyano and halogen, preferably hydrogen and halogen, and R2 is (CrC6)alkyl or (d-CeJhaloalkyl; R3 is -NHR4 or -NR5R6; R4 is selected from the group consisting and substituted or unsubstituted naphthyl; R5 and R6 are each independently selected from the group consisting of substituted or unsubstituted (C1-C6)alkyl, substituted or unsubstituted (d-CeJheteroalkyl, substituted or unsubstituted (C2-C6)alkenyl and substituted or unsubstituted (C6-C10)aryl(Ci-C6)alkyl; wherein R5 and R6 join together with the nitrogen atom to which they are attached to form a ring, which is optionally substituted with one or more independently selected R51, preferably wherein the formed ring is a five, six or seven-membered ring, which is optionally substituted with one or more independently selected R51; Y1 and Y2 are each independently selected from the group consisting of O, S, SO, S02 and CH2; Y3 is CR11R12; R 1 and R12 are each independently selected from the group consisting of hydrogen and halogen; R13 is selected from the group consisting of hydrogen, (C C6)alkyl, (d-C6)haloalkyl and halogen, preferably hydrogen; R14 is selected from -0-(d-C6)alkyl, -0-(C C6)haloalkyl, -NH-CH3 and substituted or unsubstituted (C6-C14)aryl; R15 is selected from the group consisting of (CrC6)alkyl, (d-C6)haloalkyl and unsubstituted (C6- C14)aryl, preferably (d-CeJalkyl and (d-C6)haloalkyl; R3 , R32, R33, R34 and R35 are each independently selected from the group consisting of hydrogen, substituted or unsubstituted (C1-C6)alkyl, -C(0)R14, substituted or unsubstituted (C6- C14)aryl(C C6)alkyl, -OR15 and -NH-C(0)-NH-B; R51 is selected from the group consisting of hydrogen, substituted or unsubstituted (C C6)alkyl, (Ci-C6)heteroalkyI, (C C6)haloalkyl; substituted or unsubstituted (C2-C6)alkenyl, substituted or unsubstituted (C2-C6)alkynyl, substituted or unsubstituted (C3-C8)cycloalkyl, substituted or unsubstituted (C6-C10)aryl, substituted or unsubstituted (d-Cio)aryl(d-C6)alkyl, substituted or unsubstituted (C3-C10)heteroaryl, substituted or unsubstituted (d-d0)heteroaryl(d-d)alkyl, halogen, -CN, -N02, -OR61, -N(R62)(R63), -N(R61)(OR61), -S(O)0-2R61, -S(0)1-2OR61, -OS(0)1-2R61, - OS(0)1-2OR61, -S(0)1-2N(R62)(R63), -OS(0)1-2N(R62)(R63), -N(R61)S(0)1-2R61, -NR61S(0)1-2OR61, -N R61S(0)1-2N(R62)(R63), -C(=W)R61, -C(=W)WR61, -WC(=W)R61, and -WC(=W)WR61; R6 is, in each case, selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl; R62 and R63 are, in each case, independently selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl; R is independently selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, and -OR61; W is independently selected from O, S, and N(R64); B is phenyl, optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, (Ci-C6)alkyl, (CrCeJhaloalkyl, halogen, cyano, nitro, -0-(C1-C6)alkyl and -CMCrCeJhaloalkyl, preferably hydrogen, (C C6)alkyl, (CrC6)haloalkyl and halogen; X is selected from O or S; or a pharmaceutically acceptable salt, solvate or hydrate thereof. 2. A pharmaceutical composition for use in the treatment of a bacterial disease, wherein said composition comprises a compound having a structure according to Formula I wherein R1, R2, R7, R8, R9 are each independently selected from the group consisting of hydrogen, halogen, cyano, (d-C6)alkyl and (CrC6)haloalkyl, preferably wherein R7, R8, R9 are hydrogen and R is selected from the group consisting of hydrogen, cyano and halogen, preferably hydrogen and halogen, and R2 is or (Ci-Cejhaloalkyl; R3 is -NHR4 or-NR5R6; R is selected from the group consisting of , and substituted or unsubstituted naphthyl; R5 and R6 are each independently selected from the group consisting of substituted or unsubstituted (d-d)alkyl, substituted or unsubstituted (d-C6)heteroalkyl, substituted or unsubstituted (C2-C6)alkenyl and substituted or unsubstituted (C6-C10)aryl(Ci-C6)alkyl; wherein R5 and R6 join together with the nitrogen atom to which they are attached to form a ring, which is optionally substituted with one or more independently selected R51, preferably wherein the formed ring is five, six or seven-membered ring, which is optionally substituted with one or more independently selected R5 ; Y1 and Y2 are each independently selected from the group consisting of O, S, SO, S02 and CH2; Y3 is CR11R12; R11 and R12 are each independently selected from the group consisting of hydrogen and halogen; R13 is selected from the group consisting of hydrogen, (Ci-C6)alkyl, (d-d)haloalkyl and halogen, preferably hydrogen; R14 is selected from -0-(d-C6)alkyl, -0-(d-C6)haloalkyl, -NH-CH3 and substituted or unsubstituted (C6-C14)aryl; R15 is selected from the group consisting of (d-C6)alkyl, (d-C6)haloalkyl and unsubstituted (C6- C14)aryl, preferably (d-d)alkyl and (d-d)haloalkyl; R31, R32, R33, R34 and R35 are each independently selected from the group consisting of hydrogen, substituted or unsubstituted (d-C6)alkyl, -C(0)R14, substituted or unsubstituted (C6- C14)aryl(Ci-Ce)alkyl. -OR15 and -NH-C(0)-NH-B; R5 is selected from the group consisting of hydrogen, substituted or unsubstituted (d-C6)alkyl, (d-d)heteroalkyl, (d-C6)haloalkyl; substituted or unsubstituted (C2-C6)alkenyl, substituted or unsubstituted (C2-C6)alkynyl, substituted or unsubstituted (C3-C8)cycloalkyl, substituted or unsubstituted (C6-C10)aryl, substituted or unsubstituted (C6-do)aryl(d-C6)alkyl, substituted or unsubstituted (C3-C10)heteroaryl, substituted or unsubstituted (C3-dp)heteroaryl(d-C6)al.kyl, halogen, -CN, -N02, -OR61, -N(R62)(R63), -N(R61)(OR61), -S(O)0-2R61, -S(0)1-2OR61, -OS(0)1-2R61, - OS(0)1-2OR61, -S(0)1-2N(R62)(R63), -OS(0)1-2N(R62)(R63), -N(R61)S(0)1-2R61, -NR61S(0)i-2OR61, -N R61S(0)1-2N(R62)(R63), -C(=W)R61, -C(=W)WR61, -WC(=W)R61, and -WC(=W)WR61; R6 is, in each case, selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl; R62 and R63 are, in each case, independently selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, and heterocyclyl; -R64 is independently selected from the group consisting of -H, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, and -OR61; W is independently selected from O, S, and N(R64); B is phenyl, optionally substituted with 1-3 substituents independently selected from the group consisting of hydrogen, (d-C6)alkyl, (C C6)haloalkyl, halogen, cyano, nitro, -0-(CrC6)alkyl and -0-(C C6)haloalkyl, preferably hydrogen, (d-C6)alkyl, (d-d)haloalkyl and halogen; X is selected from O or S; or a pharmaceutically acceptable salt, solvate or hydrate thereof. 3. The compound for use according to claim 1 or the pharmaceutical composition for use according to claim 2, wherein the compound having a structure according to Formula (I) is characterized in that R3 is -NR4. 4. The compound for use or the pharmaceutical composition for use according to any one of claims 1-3, wherein the compound having a structure according to Formula (I) is characterized in that R31 R33 R34 R35 g_e hyd rogen ; R32 is hydrogen or -NH-C(0)-NH-B; R14 is selected from the group consisting of -O-iC Ceihaloalkyl and substituted or unsubstituted phenyl; and R15 is (d-CeJalkyl or (C C6)haloalkyl. 5. The compound for use or the pharmaceutical composition for use according to any one of claims 1-4, wherein the compound having a structure according to Formula (I) is characterized in that R , R , R and R are hydrogen; R33 is selected from the group consisting of hydrogen, (Ci-Cejalkyl, -CH2-R16 -C(0)-R14 and - OR15, preferably hydrogen, (d-C^alkyl and -OR15; R 4 is substituted or unsubstituted phenyl, preferably unsubstituted phenyl; R15 is (Ci-C6)alkyl or (d-CeJhaloalkyl, preferably (d-CeJalkyl; and R16 is substituted or unsubstituted phenyl, preferably unsubstituted phenyl. 6. The compound for use or the pharmaceutical composition for use according to any one of claims 1-5, wherein the compound having a structure according to Formula (I) is characterized in that 7. The compound for use or the pharmaceutical composition for use according to any one of claims 1-6, wherein the compound having a structure according to Formula (I) is characterized in that are selected from the group consisting of , preferably preferably R13 is hydrogen or halogen, preferably hydrogen. 8. The compound for use or the pharmaceutical composition for use according to any one of claims 1-7, wherein the compound having a structure according to Formula (I) is characterized in that R1 is halogen, preferably chlorine; R2 is -CH3 or -CF3, preferably -CF3. 9. The compound for use or the pharmaceutical composition for use according to any one of claims 1-8, wherein the bacterial disease is caused by at least one bacteria selected from the group consisting of Listeria monocytogenes, Listeria welshimeri, Staphylococcus aureus, MRSA and clinical isolates thereof; Vancomycin-intermediate Staphylococcus aureus, Vancomycin- resistant Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus epidermidis, Staphylococcus saprophytics, Staphylococcus lugdunensis, Staphylococcus schleiferi, Staphylococcus caprae, Streptococcus pneumoniae, Streptococcus viridans, Streptococcus pyogenes, Streptococcus agalactiae, Enterococcus faecalis, Enterococcus faecium, Bacillus licheniformis, Bacillus subtilis, Bacillus anthracis, Bacillus cereus, Bacillus thuhngiensis, Bacillus larvae, Mycobacterium tuberculosis, Mycobactenum bovis, Mycobacterium leprae, Mycobacterium ulcerans, Mycobacterium kanasasii, Mycobacterium avium, Mycobactenum paratuberculosis, Mycobacterium scrofulaceam, Mycobacterium microti, Mycobacterium africanum, Mycobacterium canettii, Mycobacterium intracellular, Mycobacterium simiae, Mycobacterium szulgai, Mycobacterium xenopi, Mycobacterium fortuitum, Mycobacterium chelonei, Mycobacterium marinum, Nocardia asteroids, Rhodococcus equi and Burkholderia thailandensis, preferably wherein the bacterial disease is caused by gram positive bacteria. 10. A compound having a structure according to Formula II wherein R1 is cyano or halogen, preferably halogen, more preferably chlorine; R2 is (CrC6)alkyl or (Ci-Cf haloalkyl, preferably (d-C6)haloalkyl, more preferably -CF3; Y1 and Y2 are each independently selected from the group consisting of O, S, SO and S02, preferably O or S, more preferably O; Y3 is CR11R12; R 1 and R 2 are each independently selected from the group consisting of hydrogen and halogen, preferably halogen, more preferably fluorine; R13 is selected from the group consisting of hydrogen, (d-C6)alkyl, (C^CeJhaloalkyl and halogen, preferably hydrogen; X is O or S, preferably O; or a pharmaceutically acceptable salt, solvate or hydrate thereof. 11. The compound according to claim 10, wherein said compound is selected from the group consisting of 1-(4-chloro-3-methylphenyl)-3-(2,2-difluorobenzo[d][1 ,3]dioxol-5-yl)urea, 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2,2-difluorobenzo[d][1 ,3]dioxol-5-yl)urea, 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2,2-difluorobenzo[d][1 ,3]dioxol-5-yl)thiourea, 1-(benzo[d][1 ,3]dioxol-5-yl)-3-(4-chloro-3-(trifluoromethyl)phenyl)urea, and 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2,2-difluorobenzo[d][1 ,3]dioxol-4-yl)urea. 12. The compound according to any one of claims 10 and 11 for use in medicine. 13. The compound according to any one of claims 10 and 1 1 for use in the treatment of a bacterial disease, preferably wherein the bacterial disease is caused by gram positive bacteria, more preferably by a methicillin-resistant Staphylococcus aureus strain(MRSA). 14. A kit comprising a compound according to any one of claim 10 and 11 and at least one pharmaceutically acceptable carrier. 15. Use of a compound having a structure according to any one of claims 10 and 11 as a disinfectant. |