Aryl-benzimidazole compounds having antiinfective activity
AssigneeGenesoft, Inc.
InventorsDustin L. McMinn, Roland W. Burli, Jacob Kaizerman, Eldon E. Baird, Matthew J. Taylor
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Abstract
Aryl-benzimidazole compounds according to the formula 1 where Ar1, R1, R2, Y, W, and N are as defined herein, bind to DNA and have antibacterial activity.
Drawings
Claims43
A compound having the formula
- 53
- and pharmaceutically acceptable salts thereof,
- wherein
- Ar1 is a substituted or unsubstituted phenyl, naphthyl, 5-member heteroaromatic, 6-member heteroaromatic, or fused ring heteroaromatic group;
- subscript m is 0 or 1 and subscript n is an integer from 1 to 25, inclusive, with the provisos that if m is 0, then at least one moiety Y is a moiety M4 and n is at least 2;
- each moiety Y is independently selected from the group consisting of
- (a) moieties M1 having the formula
- 54
- wherein
- one of X1, X2, and X3 is a ring vertex selected from the group consisting of —O—, —S—, and —NR2—, and the other two of X1, X2, and X3 are ring vertices selected from the group consisting of ═N— and ═CR1—;
- (b) moieties M2 having the formula
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- wherein
- x is 0 or 1 and each R15 is independently H, OH, NH2, or F;
- (c) moieties M3 having the formula
- 56
- wherein each L is independently a divalent moiety separating —NH— and —(C═O)— by 3 or 4 atoms;
- and
- (d) moieties M4 having the formula
- 57
- wherein each Ar2 is independently selected from the group consisting of
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- W is N(R2)2 or OR2;
- wherein in the preceding formulae
- each R1 is independently H, F, Cl, Br, I, CN, OH, NO2, NH2, a substituted or unsubstituted (C1-C12)alkyl group, or a substituted or unsubstituted (C1-C12)heteroalkyl group;
- and
- each R2 is independently H, a substituted or unsubstituted (C1-C12)alkyl group, or a substituted or unsubstituted (C1-C12)heteroalkyl group.
Dependencies are inferred from the claim text.