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US 10,100,005 B1Granted
Mesalazine derivatives
AssigneeEclipse Therapeutics, LLC
InventorDavid Gindelberger
Life of this patent
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Abstract
Provided herein are compounds that are prodrugs for mesalazine. Generally, the compounds described herein correspond to a mesalazine molecule wherein the amino group is replaced by a novel protecting group. For example, in the compounds of Formula I described herein, the compound comprises a glyoxylate derivative moiety. In the compounds of Formula II described herein, the compound comprises a vanillin derivative moiety.
Claims27
A compound of Formula I, or a salt thereof,
- wherein
- R1 is selected from the group consisting of —OR9 and —N(R10R11), wherein R9, R10, and R11 are each independently selected from the group consisting of hydrogen and C1-C6 alkyl;
- R2 is selected from the group consisting of —OR12 and —N(R13R14), wherein R12, R13, and R14 are each independently selected from the group consisting of hydrogen and C1-C6 alkyl;
- R3 and R6 are each independently selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 alkoxy, carboxyl, halogen, and CF3;
- one of R4 and R5 is selected from the group consisting of hydrogen and C1-C6 alkyl, and the other of R4 and R5 is a moiety having the following structure:
- wherein R7 is selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C6 alkoxy, carboxyl, halogen, and CF3;
- and R8 is selected from the group consisting of —OR15 and —N(R16R17), wherein R15, R16, and R17 are each independently selected from the group consisting of hydrogen and C1-C6 alkyl.
4 more elements
Dependencies are inferred from the claim text.