Lantibiotic NAI-802, Pharmaceutically Acceptable Salts, Compositions and Uses Thereof

A compound of formula (I):

• wherein X represents NH2 or Ala;
• Y represents —S—, —S(O)—, —S(O)2;
• Z represents OH or NR1R2 wherein R1 and R2 independently represent:
• hydrogen or
• an alkyl of 1 to 20 carbon atoms;
• an alkenyl of 2 to 20 carbon atoms;
• an alkynyl of 2 to 20 carbon atoms;
• a cycloalkyl of 3 to 8 carbon atom optionally substituted by one or two substituents independently selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms, phenyl, phenyl-(C1-C4)alkyl, phenoxy, phenoxy-(C1-C4)alkyl wherein the phenyl and the phenyl portion of the phenyl lower-alkyl, phenoxy and phenoxy-(C1-C4)alkyl group is optionally substituted by one or two substituents selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, and (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms;
• a phenyl radical optionally substituted by one or two substituents independently selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms, phenyl, phenyl-(C1-C4)alkyl, phenoxy, phenoxy-(C1-C4)alkyl wherein the phenyl and the phenyl portion of the phenyl lower-alkyl, phenoxy and phenoxy-(C1-C4)alkyl group is optionally substituted by one or two substituents selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, and (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms
• a benzyl radical optionally substituted on the phenyl ring by one or two substituents independently selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms, phenyl, phenyl-(C1-C4)alkyl, phenoxy, phenoxy-(C1-C4)alkyl wherein the phenyl and the phenyl portion of the phenyl lower-alkyl, phenoxy and phenoxy-(C1-C4)alkyl group is optionally substituted by one or two substituents selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, and (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms
• a naphthyl radical optionally substituted by one or two substituents selected from halo, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, and (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms
• a group of formula
• —(CH2)nOR3
• in which n represents an integer from 2 to 8 and R3 represent
• hydrogen or
• (C1-C4) alkyl or
• a cycloalkyl of 3 to 8 carbon atom optionally substituted by one or two substituents independently selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms, phenyl, phenyl-(C1-C4)alkyl, phenoxy, phenoxy-(C1-C4)alkyl wherein the phenyl and the phenyl portion of the phenyl lower-alkyl, phenoxy and phenoxy-(C1-C4)alkyl group is optionally substituted by one or two substituents selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, and (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms.
• a phenyl radical optionally substituted by one or two substituents independently selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms, phenyl, phenyl-(C1-C4)alkyl, phenoxy, phenoxy-(C1-C4)alkyl wherein the phenyl and the phenyl portion of the phenyl lower-alkyl, phenoxy and phenoxy-(C1-C4)alkyl group is optionally substituted by one or two substituents selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, and (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms
• a group of formula
• —(CH2)nNR4R5
• in which n represents an integer from 2 to 8 and R4 and R5 independently represent
• hydrogen or
• (C1-C4) alkyl or
• a cycloalkyl of 3 to 8 carbon atom optionally substituted by one or two substituents independently selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms, phenyl, phenyl-(C1-C4)alkyl, phenoxy, phenoxy-(C1-C4)alkyl wherein the phenyl and the phenyl portion of the phenyl lower-alkyl, phenoxy and phenoxy-(C1-C4)alkyl group is optionally substituted by one or two substituents selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, and (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms.
• phenyl radical optionally substituted by one or two substituents independently selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms, phenyl, phenyl-(C1-C4)alkyl, phenoxy, phenoxy-(C1-C4)alkyl wherein the phenyl and the phenyl portion of the phenyl lower-alkyl, phenoxy and phenoxy-(C1-C4)alkyl group is optionally substituted by one or two substituents selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, and (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms
• a benzyl radical optionally substituted on the phenyl ring by one or two substituents independently selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms, phenyl, phenyl-(C1-C4)alkyl, phenoxy, phenoxy-(C1-C4)alkyl wherein the phenyl and the phenyl portion of the phenyl lower-alkyl, phenoxy and phenoxy-(C1-C4)alkyl group is optionally substituted by one or two substituents selected from halo, cyano, (C1-C4)alkyl optionally substituted by 1 to 3 halogen atoms, and (C1-C4) alkoxy optionally substituted by 1 to 3 halogen atoms
• R4 and R5 taken together represent a —(CH2)3, —(CH2)4—, —(CH2)2—O—(CH2)2, —(CH2)2—S—(CH2)2 or
• R4 and R5 taken together with the adjacent nitrogen atom represent:
• a piperazine moiety which may be substituted in position 4 with a substituent selected from (C1-C4) alkyl, (C3-C8) cycloalkyl, pyridyl, benzyl and substituted benzyl wherein the phenyl moiety bears 1 or 2 substituents selected from chloro, bromo, nitro, (C1-C4) alkyl and (C1-C4) alkoxy.