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US 2008/0306040 A1Published application
Antibacterial amide macrocycles VII
OwnerRainer Endermann, Kerstin Ehlert +3inventors
InventorsRainer Endermann, Kerstin Ehlert, Martin Michels, Stefan Weigand, Guido Schiffer
Life of this patent
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Abstract
The invention relates to antibacterial amide macrocycles and methods for their preparation, their use for the treatment and/or prophylaxis of diseases as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially bacterial infections.
Claims14
A compound of formula
- in which
- R26 represents hydrogen, halogen, hydroxy or methyl,
- R7 represents a group of formula
- whereby
- R1 represents hydrogen or hydroxy,
- * is the linkage site to the carbon atom,
- R2 represents hydrogen or methyl,
- R3 represents a group of formula
- whereby
- * is the linkage site to the nitrogen atom,
- A represents a bond or phenyl,
- R4 represents hydrogen, amino or hydroxy,
- R5 represents a group of formula
- wherein
- * is the linkage site to the carbon atom,
- R23 represents hydrogen or a group of formula *-(CH2)n—OH or *-(CH2)o—NH2,
- wherein
- * is the linkage site to the carbon atom,
- n and o independently of one another are a number 1, 2, 3 or 4,
- m is a number 0 or 1,
- R8 and R12 independently of one another represent a group of formula *-CONHR14 or *-CH2CONHR15
- wherein
- * is the linkage site to the carbon atom,
- R14 and R15 independently of one another represent a group of formula
- wherein
- * is the linkage site to the nitrogen atom,
- R4a represents hydrogen, amino or hydroxy,
- R5a represents hydrogen, methyl or aminoethyl,
- R6a represents hydrogen or aminoethyl,
- or
- R5a and R6a together with the nitrogen atom to which they are bonded form a piperazine ring,
- R8a and R12a independently of one another represent *-(CH2)Z1a—OH, *-(CH2)Z2a—NHR13a, *-CONHR14a or *-CH2CONHR15a,
- wherein
- * is the linkage site to the carbon atom,
- Z1a and Z2a independently of one another are a number 1, 2 or 3,
- R13a represents hydrogen or methyl,
- and
- R14a and R15a independently of one another represent a group of formula
- wherein
- * is the linkage site to the nitrogen atom,
- R4c represents hydrogen, amino or hydroxy,
- R5c represents hydrogen, methyl or aminoethyl,
- R6c represents hydrogen or aminoethyl,
- kc is a number 0 or 1,
- and
- lC is a number 1, 2, 3 or 4,
- R9a and R11a independently of one another represent hydrogen or methyl,
- R10a represents amino or hydroxy,
- R16a represents a group of formula
- wherein
- * is the linkage site to the nitrogen atom,
- R4d represents hydrogen, amino or hydroxy,
- R5d represents hydrogen, methyl or aminoethyl,
- R6d represents hydrogen or aminoethyl,
- kd is a number 0 or 1,
- and
- ld is a number 1, 2, 3 or 4,
- ka is a number 0 or 1,
- and
- la, wa, xa and ya independently of one another are a number 1, 2, 3 or 4,
- R9 represents hydrogen, methyl, *-C(NH2)═NH or a group of formula
- wherein
- * is the linkage site to the nitrogen atom,
- R20 represents hydrogen or *-(CH2)i—NHR22,
- wherein
- R22 represents hydrogen or methyl,
- and
- i is a number 1, 2 or 3,
- R21 represents hydrogen or methyl,
- f is a number 0, 1, 2 or 3,
- g is a number 1, 2 or 3,
- and
- h is a number 1, 2, 3 or 4,
- R16 and R17 independently of one another represent a group of formula
- wherein
- * is the linkage site to the nitrogen atom,
- R4b represents hydrogen, amino or hydroxy,
- R5b represents hydrogen, methyl or aminoethyl,
- R6b represents hydrogen or aminoethyl,
- or
- R5b and R6b together with the nitrogen atom to which they are bonded form a piperazine ring,
- R8b and R12b independently of one another represent *-(CH2)Z1b—OH, *-(CH2)z2b—NHR13b, *-CONHR4b or *-CH2CONHR15b,
- wherein
- * is the linkage site to the carbon atom,
- R3b represents hydrogen or methyl,
- and
- Z1b and Z2b independently of one another are a number 1, 2 or 3,
- and
- R4b and R1b independently of one another represent a group of formula
- wherein
- * is the linkage site to the nitrogen atom,
- R4g represents hydrogen, amino or hydroxy,
- R5g represents hydrogen, methyl or aminoethyl,
- R6g represents hydrogen or aminoethyl,
- kg is a number 0 or 1,
- and
- lg is a number 1, 2, 3 or 4,
- R9b and R11b independently of one another represent hydrogen or methyl,
- R10b represents amino or hydroxy,
- kb is a number 0 or 1,
- lb, wb, xb and yb independently of one another are a number 1, 2, 3 or 4,
- R18 represents hydrogen, amino or hydroxy,
- R19 represents hydrogen, methyl or a group of formula
- wherein
- * is the linkage site to the nitrogen atom,
- R25 represents hydrogen or *-(CH2)u—NHR
- wherein
- R29 represents hydrogen or methyl,
- and
- u is a number 1, 2 or 3,
- R28 represents hydrogen or methyl,
- s is a number 0, 1, 2 or 3,
- and
- t is a number 1, 2 or 3,
- R24 represents hydrogen or aminoethyl,
- d is a number 1, 2 or 3,
- k and q independently of one another are a number 0 or 1,
- l, r, w and y independently of one another are a number 1, 2, 3 or 4,
- independently of one another may when w, r or y equals 3 carry a hydroxy group, or one of its salts, its solvates or the solvates of its salts.
116 more elements
Dependencies are inferred from the claim text.