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THERAPEUTIC BORON-CONTAINING COMPOUNDS
专利权人:
发明人:
申请号:
EP13700587.2
公开号:
EP2802593A1
申请日:
2013.01.08
申请国别(地区):
EP
年份:
2014
代理人:
摘要:
The present invention relates to compounds of Formula (I) wherein R1 and R3 are hydrogen R2 and R4, which may be the same or different, are hydrogen, a C1-6 alkyl group optionally substituted by an aryl group which may itself be substituted, the substituent group including an alkyl group or an -OR group in which R is a C1-3 alkyl group, with one or more hydrogen atoms optionally replaced with a halogen atom or an aryl group which may be substituted, the substituent group including an alkyl group or an -OR group in which R is a C1-3 alkyl group, with one or more hydrogen atoms optionally replaced with a halogen atom with the proviso that R2 and R4 are not both hydrogen the atom of R4 which is attached to Cβ is either a saturated carbon atom or an atom which is part of a 1 substituted aromatic ring (AA)0-5 is an amino acid, amino acid derivative, peptide of up to 5 amino acids or a peptidomimetic thereof which optionally incorporates an N-terminal capping group, when the group is (AA)0 an N-terminal capping group is present, covalently attached to the nitrogen atom shown in Formula (I) and the capping group comprises at least 5 non-hydrogen atoms R5 is hydrogen or a C1-3 20 alkyl group, when AA=0, R5 may form a cyclic group with the N-terminal capping group R6 and R7 independently of one another denote hydrogen or a C1-6 alkyl group or together with the boron atom and the oxygen atoms, form a mono-, bi- or tricyclic, saturated or partly unsaturated, mono-, di-, tri- or tetra- C1-6 alkylated or phenylated ring system having 5-18 ring members and salt forms and stereoisomers thereof. The invention further relates to pharmaceutical formulations containing these compounds and the use of these compounds in therapy, particularly as antimicrobial agents, more particularly as an agent effective in treating a Mycobacterium tuberculosis infection or a Candida albicans infection. (I)La présente invention se rapporte aux composés de formule (I) dans laquelle R1 et R3 représentent
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