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US 2013/0095057 A1Published application
Compounds for the treatment of clostridium difficile-associated disease
AssigneeSummit Corporation PLC
InventorsPeter David Johnson, Richard John Vickers, Francis Xavier Wilson, Colin Richard Dorgan, Lauren Jayne Sudlow, Stephen Paul Wren, Renate Van Well
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Abstract
Disclosed are compounds of formula (I): or a pharmaceutically acceptable N-oxide, salt, hydrate, solvate, complex, bioisostere, metabolite or prodrug thereof, which are of use in the treatment of infection with, and diseases caused by, Clostridium difficile.
Claims25
A compound of formula (I):
- R1 is selected from an optionally substituted aryl, heteroaryl, carbocyclyl and heterocyclyl group, the optional substitution being with one or more substituents selected from halo, CN, NO2, R3, OR3, N(R3)2, COR3, CO2R3, C(═O)SR3, SR3, S(═O)3R , SO2R3, NR4C(═O)R3, NR4CO2R3, OC(═O)NR3R4, NR4SO2R3, C(═NR)NR3R4, C(═S)NR3R4, NR4C(═NR)NR3R4, NR4C(═S)NR3R4, NR4C(═O)NR3R4, CONR3R4 and SO2NR3R4;
- R2 is an optionally substituted aromatic 8-14 membered fused bicyclic or tricyclic ring system in which one or more of the carbon atoms may be replaced by N, O, S, SO or SO2 and the optional substitution being with one or more substituents selected from halo, CN, NO2, R3, OR3, N(R3)2, COR3, CO2R3, C(═O)SR3, SR3, S(═O)R3, SO2R3, NR4C(═O)R3, NR4CO2R3, OC(═O)NR3R4, NR4SO2R3, C(═NR4)NR3R4, C(═S)NR3R4, NR4C(═NR4)NR3R4, NR4C(═S)NR3R4, NR4C(═O)NR3R4, CONR3R4 and SO2NR3R4;
- R3 is selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 carbocyclyl, C4-C7 heterocyclyl and 5- or 6- membered aryl or heteroaryl, any of which may be optionally substituted with one or more substituents selected from halo, CN, NO2, R4, OR4, N(R4)2, COR4, CO2R4, C(═O)SR4, SR4, S(═O)R4, SO2R4, NR4C(═O)R5, NR4CO2R4, OC(═O)NR4)2, NR4SO2R4, C(═NR)N(R4)2, C(═S)N(R4)2, NR4C(═NR4)N(R4)2, NR4C(═S)N(R)2, NR4C(═O)N(R4)2, CON(R4)2 and SO2N(R4)2;
- R4 is selected from hydrogen, C1-C6 alkyl and C3-C7 carbocyclyl, optionally substituted with one or more halo atoms;
- or a pharmaceutically acceptable N-oxide, salt, hydrate, solvate, complex, bioisostere, metabolite or prodrug thereof for use in a method for the treatment of Clostridium difficile-associated disease (CDAD).
2 more elements
A compound of formula (I):
- R1 is selected from an optionally substituted aryl, heteroaryl, carbocyclyl and heterocyclyl group, the optional substitution being with one or more substituents selected from halo, CN, NO2, R3, OR3, N(R3)2, COR3, CO2R3, C(═O)SR3, SR3, S(═O)R3, SO2R3, NR4C(═O)R3, NR4CO2R3, OC(═O)NR3R4, NR4SO2R3, C(═NR4)NR3R4, C(═S)NR3R4, NR4C(═NR4)NR3R4, NR4C(═S)NR3R4, NR4C(═O)NR3R4, CONR3R4 and SO2NR3R4;
- R2 is an optionally substituted aromatic 8-14 membered fused bicyclic or tricyclic ring system in which one or more of the carbon atoms may be replaced by N, O, S, SO or SO2 and the optional substitution being with one or more substituents selected from halo, CN, NO2, R3, OR3, N(R3)2, COR3, CO2R3, C(═O)SR3, SR3, S(═O)R3, SO2R3, NR4C(═O)R3, NR4CO2R3, OC(═O)NR3R4, NR4SO2R3, C(═NR)NR3R4, C(═S)NR3R4, NR4C(═NR)NR3R4, NR4C(═S)NR3R4, NR4C(═O)NR3R4, CONR3R4 and SO2NR3R4;
- R3 is selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 carbocyclyl, C4-C7 heterocyclyl and 5- or 6- membered aryl or heteroaryl, any of which may be optionally substituted with one or more substituents selected from halo, CN, NO2, R4, OR4, N(R4)2, COR4, CO2R4, C(═O)SR4, SR4, S(═O)R4, SO2R4, NR4C(═O)R4, NR4CO2R4, OC(═O)NR4)2, NR4SO2R4, C(═NR4)N(R4)2, C(═S)N(R4)2, NR4C(═NR4)N(R4)2, NR4C(═S)N(R4)2, NR4C(═O)N(R4)2, CON(R4)2 and SO2N(R4)2;
- R4 is selected from hydrogen, C1-C6 alkyl and C3-C7 carbocyclyl, optionally substituted with one or more halo atoms;
- or a pharmaceutically acceptable N-oxide, salt, hydrate, solvate, complex, bioisostere, metabolite or prodrug thereof, optionally for use in therapy or prophylaxis, for example in a method for the treatment of a bacterial infection or disease.
2 more elements
Dependencies are inferred from the claim text.