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US 10,369,130 B2Granted
Antibacterial compounds
AssigneeAZIEN DE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.
InventorsRosella Ombrato, Barbara Garofalo, Giorgina Mangano, Alessandra Capezzone De Joannon, Gaia Corso, Gabriele Magaro′, Guido Furlotti, Tommaso Iacoangeli
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Abstract
The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials.
Claims13
A compound of formula (I)
- A-L1-B-L2-Y-L3-C (I)
- wherein
- A is a group of the following formula:
- wherein
- R1 is H or halogen atom,
- R2 is H, halogen atom, OH, (C1-3)alkyl or (C1-3)alkoxy, and
- R3 is H, (C1-3)alkyl or (C1-3)alkoxy;
- L1 is σ bond, —O— or —N(R′)—, wherein R′ is H or (C1-3)alkyl;
- B is a divalent residue of a piperazine or piperidine ring;
- L2 is σ bond, —CH2—, —O—, or —N(R′)—, wherein R′ is H or (C1-3)alkyl;
- Y is a (C1-6)alkylenyl, (C2-6)alkenylenyl, (C2-6)alkynylenyl, or (C3-6)cycloalkylenyl group, said group being optionally substituted with one or more groups selected from —OH, (C1-3)alkyl, (C3-6)cycloalkyl, 3- to 5-membered oxacycloalkyl, —COOR′, —NR′R″ wherein R′ and R″, identical or different each other, are hydrogen atom or (C1-3)alkyl;
- L3 is —O—, —(CH2)2—, —N(R′)—, —N(R′)—C(═O)—, —N(R′)—C(═S)—, —N(R′)—(C1-6)alkylenyl-, —C(═O)—N(R′)—, —C(═O)—N(R′)—(C1-6)alkylenyl-, —SO2—N(R′)—, —N(R′)—SO2—, wherein R′ is hydrogen atom or (C1-3)alkyl;
- C is a group of formula (V), (VI), or (VIII):
- wherein
- n is an integer from 0 to 3
- P1 and P2, equal or different each other, are CH or N
- P3 is O, S or NH;
- R6 and R7 together form a 5- or 6-membered aliphatic or aromatic ring, optionally comprising at least one heteroatom selected from N and O,
- R8 and R9, equal or different each other, are a hydrogen atom or an aryl group, or together form a 5- or 6-membered aliphatic or aromatic ring, optionally comprising at least one heteroatom selected from N and O,
- R10 and R11 together form a 5- or 6-membered aliphatic or aromatic ring,
- and wherein each hydrogen atom linked to a carbon or nitrogen atom forming the ring of formulae (V), (VI), or (VIII) is optionally substituted with at least one substituent selected from the group consisting of halogen atom, (C1-3)alkyl or (C1-3)alkoxy;
- or an addition salt with a pharmaceutically acceptable organic or inorganic acid or base, an enantiomer, N-oxide, or quaternary ammonium salt of said compound of formula (I).
19 more elements
A method for treating a bacterial infection, comprising administering, to a subject in need thereof, an effective amount of compound of formula (I)
- A-L1-B-L2-Y-L3-C (I)
- wherein
- A is a group of the following formula:
- wherein
- R1 is H or halogen atom,
- R2 is H, halogen atom, OH, (C1-3)alkyl or (C1-3)alkoxy, and
- R3 is H, (C1-3)alkyl or (C1-3)alkoxy;
- L1 is σ bond, —O— or —N(R′)—, wherein R′ is H or (C1-3)alkyl;
- B is a divalent residue of a piperazine or piperidine ring;
- L2 is σ bond, —CH2—, —O—, or —N(R′)—, wherein R′ is H or (C1-3)alkyl;
- Y is a (C1-6)alkylenyl, (C2-6)alkenylenyl, (C2-6)alkynylenyl, or (C3-6)cycloalkylenyl group, said group being optionally substituted with one or more groups selected from —OH, (C1-3)alkyl, (C3-6)cycloalkyl, 3- to 5-membered oxacycloalkyl, —COOR′, —NR′R″ wherein R′ and R″, identical or different each other, are hydrogen atom or (C1-3)alkyl;
- L3 is —O—, —(CH2)2—, —N(R′)—, —N(R′)—C(═O)—, —N(R′)—C(═S)—, —N(R′)—(C1-6)alkylenyl-, —C(═O)—N(R′)—(C1-6)alkylenyl-, —SO2—N(R′)—, —N(R′)—SO2—, wherein R′ is hydrogen atom or (C1-3)alkyl;
- C is a group having a 5- or 6-membered saturated or unsaturated ring, or a 9- or 10-membered fused bicyclic ring;
- or an addition salt with a pharmaceutically acceptable organic or inorganic acid or base, an enantiomer, N-oxide, or quaternary ammonium salt of said compound of formula (I).
11 more elements
Dependencies are inferred from the claim text.