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US 11,028,086 B2Granted
Pyrido-imidazo rifamycins
AssigneeBiofer S.p.A.
InventorsEgidio Marchi, Alessandro Lapini Sacchetti, Claudia Ori, Lisa Preti
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Abstract
The present invention relates to novel pyrido-imidazo rifamycins, characterized by a highly selective antibacterial activity and low absorption by oral route.
Claims28
A compound of Formula (I) or pharmaceutically acceptable salts thereof
- wherein
- R and R1 may be H,
- with the proviso that:
- when
- then R1═H and R2═CH3CO— or H;
- when
- then R═H and R2═CH3CO— or H;
- when
- then R1═H and R2═CH3CO— or H;
- and
- when
- then R═H and R2═CH3CO— or H;
- wherein R3 and R4 are the same or different and selected from the group comprising hydrogen, linear or branched C1-C10 alkyl, optionally substituted with one or more substituents selected from aminoalkyl, alkoxy, phenoxy, or sulfo, and aryl, optionally mono- or disubstituted with C1-C4 alkyl or alkoxy groups, halogen, amino, nitro;
- or
- R3 and R4 taken together with two consecutive carbon atoms of the pyridine core may form a phenyl ring, optionally substituted with C1-C4 alkyl, or a 5- or 6-membered heterocyclic ring, optionally substituted with C1-C4 alkyl,
- R5 is selected from the group comprising hydrogen, hydroxy, linear or branched C1-C10 alkyl, optionally substituted with one or more substituents selected from aminoalkyl, alkoxy, phenoxy, or sulfo, and aryl optionally mono- or disubstituted with C1-C4 alkyl or alkoxy groups, halogen, amino, nitro.
13 more elements
A compound selected from the group consisting of 4′-[(alkyloxy-iminomethyl]-4-desoxypyrido[1′,2′-1,2]imidazo[5,4-c]rifamycin and 4′-[N-alkyliminomethyl]-4-desoxypyrido[1′,2′-1,2]imidazo[5,4-c]rifamycin SV.
The compound:
- 4′-hydroxymethyl-4-desoxypyrido[1′,2′-1,2]imidazo[5,4-c]rifamycin S or SV, or pharmaceutically acceptable salts thereof.
The compound:
- 4′-formyl-4-desoxypyrido[1′,2′-1,2]imidazo[5,4-c]rifamycin S or SV, e or pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.