Barbituric acid derivatives, their preparation and use thereof as leukocyte transmigration inhibitors and for treating inflammatory diseases, autoimmune diseases and cancer
AssigneesBar-Ilan University, University of Geneva, Geneva University Hospitals
InventorsArie Lev Gruzman, Paul Bradfield, Tamar Getter, Beat Imhof, Thomas Matthes, Hanoch Senderowitz
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Abstract
Provided herein are novel barbituric acid derivatives, their synthesis and use thereof in blocking leukocyte transmigration. The novel barbituric acid derivatives are useful for the treatment of disorders associated with leukocyte transmigration, such as for example inflammatory diseases and disorders, autoimmune diseases and disorders, and cancers.
Claims28
A compound selected from the compounds of Formula 1, Formula 5, Formula 6, Formula 7 and Formula 9:
- or
- pharmaceutically acceptable salts thereof.
A method of inhibiting leukocyte transmigration in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of general Formula (Ib)
- wherein
- Z is for each phenyl ring independently one or two functional groups;
- each Z is attached to any available carbon atom of the ring in which it is present;
- at least one Z is present, and each Z is independently selected from linear alkyl or branched alkyl, wherein each of the linear alkyl or the branched alkyl may be unsubstituted or substituted with one or more of halo, haloalkyl, cyano, nitro, hydroxyl, alkenyl, aryl, alkoxy, aryloxy, aralkoxy, alkylcarbamido, arylcarbamido, amino, alkylamino, arylamino, dialkylamino, diarylamino, arylalkylamino, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, alkylcarbonyloxy, arylcarbonyloxy, carboxyl, carboxylic ester, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonylamido, alkylsulfonyl, arylsulfonyl, alkylsulfinyl, arylsulfinyl;
- R5 is alkyl, selected from linear alkyl or branched alkyl, wherein the alkyl may be unsubstituted or substituted with one, two, or three substituents selected from the group consisting of halo, nitro, cyano and amino;
- and
- stereoisomers, enantiomers, and tautomers thereof, pharmaceutically acceptable salts thereof and mixtures thereof.
A method of inhibiting leukocyte transmigration in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula 10:
- or pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.