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US 2017/0304235 A1Published application
Linear guanidine derivatives, methods of preparation and uses thereof
AssigneeLead Discovery Siena S.R.L.
InventorsMaurizio BOTTA, Giorgio MACCARI, Stefania SANFILIPPO, Filomena DE LUCA, Jean-Denis DOCQUIER, Davide DEODATO
Life of this patent
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Abstract
The present invention relates to linear guanidine derivatives, methods of preparation, uses and pharmaceutical compositions thereof. The compounds of Formulas 1 or 2 exhibit high antimicrobial activity against Gram positive and Gram negative bacteria.
Claims21
A compound of general formula 1:
- or a pharmaceutical acceptable salt, hydrate or solvate thereof;
- wherein:
- R1, R3, R5, R7, R9 and R11 are the same or different groups, selected between H, methyl, ethyl, propyl, prop-2-ynyl, but-2-enyl, 2-methylprop-2-enyl, 3-methylbut-2-enyl, phenyl, benzyl, dimethylphenyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, acetyl, propanoyl, N-alkyl-carbamoyl, N-alkyl-thiocarbamoyl, N-alkyl-carbamimidoyl or saturated linear or branched C1-10 alkyl;
- R2, R4, R6, R8, R10 and R12 are the same or different groups, selected between H, methyl, ethyl, or saturated linear or branched C1-5 alkyl;
- X is O or S;
- L is a number from 0 to 2;
- n1, n2 and n3 can be the same or different and are numbers from 2 to 10;
- and
- m1, m2 and m3 can be the same or different and are numbers from 2 to 10.
6 more elements
A compound having the general formula 2:
- or a pharmaceutical acceptable salt, hydrate or solvate thereof;
- wherein:
- R1, R3, R5, and R7, are the same or different groups, selected between H, methyl, ethyl, propyl, prop-2-ynyl, but-2-enyl, 2-methylprop-2-enyl, 3-methylbut-2-enyl, phenyl, benzyl, dimethylphenyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, acetyl, propanoyl, N-alkyl-carbamoyl, N-alkyl-thiocarbamoyl, N-alkyl-carbamimidoyl or saturated linear or branched C1-10 alkyl;
- R2, R4, R6, and R8, are the same or different groups, selected between H, methyl, ethyl, or saturated linear or branched C1-5 alkyl
- L is a number from 1 to 3;
- n1 and n2 can be the same or different and are numbers from 2 to 10;
- and
- m1 and m2 can be the same or different and are numbers from 2 to 10.
5 more elements
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A process for the preparation of an intermediate of formula 7a or 7b comprising:
Dependencies are inferred from the claim text.