Compounds for the treatment of clostridium difficile-associated disease

• Main Authors: COLIN RICHARD DORGAN, RICHARD VICKERS, STEPHEN PAUL WREN, FRANCIS XAVIER WILSON
• Format: Patent
• Language: English
• Published: 07.12.2011
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Compounds for the treatment of clostridium difficile-associated diseaseCompounds of formula (I) or a pharmaceutically acceptable N-oxide, salt, hydrate, solvate, complex, bioisostere, metabolite or prodrug thereof wherein X and A1-A5are independently selected from N and CR5, with the proviso that A4and/or A5is N; R1and R2are independently selected from an optionally substituted aryl, heteroaryl, carbocyclyl and heterocyclyl group and R5is independently selected from hydrogen, halogen, CN, NO2R4, OR4, N(R4)2, COR4, CO2R4, C(=O)SR4, SR4, S(=O)R4, SO2R4, NR4C(=O)R4, NR4CO,R4, OC(=O)N(R4)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)2and SO2N(R4)2, where R4is selected from hydrogen, C1-C6alkyl and C3-C7carbocyclyl optionally substituted with one or more halo atoms. Compounds of formula (I) for use in the treatment of a clostridium difficile-associated disease (CDAD), preferably colitis, pseudomembranous colitis, diarrhoea and antibiotic associated diseases is also outlined. The preparation and use of 2-(pyridin-4-yl)-5-(2-(pyridin-4-yl)-1H-benzo[d]imidazol-5-yl)-2H-benzo[d][1,2,3]triazole and 2-(pyridin-4-yl)-6- (2-(pyridin-4-yl)-1H-benzo[d]imidazol-5-yl)-2H-indazole in the treatment of a clostridium difficile-associated disease (CDAD) is outlined.