Antibacterial basic biaromatic derivatives with aminoalkoxy substitution
AssigneeIdorsia Pharmaceuticals Ltd
InventorsSylvaine Cren, Astrid Friedli, Georg Rueedi, Cornelia Zumbrunn
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Abstract
The invention relates to antibacterial compounds of formula I wherein R1a, R2a, R2b, R3a, R3b, R4, R5, U1, U2, U3, U4, V1, V2, V3, V4, X and Q and n are as defined in the specification. It further relates pharmaceutical compositions containing these compounds and the uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections. These compounds are useful antimicrobial agents effective against a variety of human and veterinary pathogens including among others Gram-positive and Gram-negative aerobic and anaerobic bacteria.
Claims15
A compound of formula I
- wherein
- n represents 0, 1, 2 or 3;
- R1a represents H or (C1-C3)alkyl;
- R2a and R2b each independently represents H or (C1-C3)alkyl;
- R3a and R3b each independently represents H or (C1-C3)alkyl;
- R4 represents H, (C1-C3)alkyl, or (C2-C3)alkyl-NR4aR4b, wherein R4a and R4b are independently from each other H or (C1-C3)alkyl;
- R5 represents H, (C1-C3)alkyl, or (C2-C3)alkyl-NR5aR5b, wherein R5a and R5b are independently from each other H or (C1-C3)alkyl;
- or
- R2a and R2b together with the carbon atom which bears them, form a 3 to 6-membered cycloalkyl ring;
- or
- R4 and R5 together with the nitrogen atom which bears them, form a 4 to 6-membered heterocycloalkyl ring;
- or
- R4 and R5 together with the nitrogen atom which bears them, form a 6 to 8-membered bicyclic heterocycloalkyl ring, which bicyclic heterocycloalkyl ring may optionally be substituted by a group NR6R7, wherein R6 and R7 are independently from each other H or (C1-C3)alkyl;
- or
- R4 and R5 together with the nitrogen atom which bears them and the adjacent CR2aR2b or CR3aR3b together form an amidine group;
- or
- R1a and R3a, together with the carbon atoms which bear them and the carbon atom which connects these latter two atoms, form a 4 to 6-membered cycloalkyl ring, whereby R2a, R2b and R3b each represent H, and n represents 1;
- or
- R1a and R4, together with the carbon and nitrogen atoms which bear them and the carbon atom(s) which connect(s) the latter two atoms, form a 4 to 6-membered heterocycloalkyl ring, whereby R2a, R2b, optional R3a and optional R3b each represent H, n represents 0 or 1, and said 4 to 6-membered heterocycloalkyl ring optionally comprises a substituent selected from OCH3 or CH3;
- or
- R2a and R4 together with the carbon and nitrogen atoms which bear them and the optional carbon atom(s) which connect the latter two atoms, form a 4 to 6-membered heterocycloalkyl ring, whereby R1a, optional R3a and optional R3b each represent H, R2b represents H, NH2 or OH, and n represents 0, 1 or 2;
- U1 represents N or CH, U2 represents N, CH, C—O(C1-C3)alkyl, or C—CN, U3 represents N or CH and U4 represents N or CH, it being understood that at most three of U1, U2, U3 and U4 can represent N at the same time;
- V1 represents N or CH, V2 represents N or CH, V3 represents N or CH and V4 represents N or CH, it being understood that at most three of V1, V2, V3 and V4 can represent N at the same time;
- X represents CH or N;
- Q represents O or S;
- or a salt of this compound.
Dependencies are inferred from the claim text.