Thromboxane receptor antagonists
AssigneeUniversity College Dublin, National University of Ireland, Dublin
InventorsB. Therese Kinsella, Helen Reid
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Abstract
The invention relates to novel chemical entities that act as thromboxane (TX) A2 receptor, or T prostanoid receptor (TP), antagonists and to their use in the treatment of human diseases in which thromboxane (TX) A and of all other agents that act as incidental ligands of TP, including the endoperoxide prostaglandin (PG)G2/PGH2, 20-hydroxyeicosatetraenoic acid (20-HETE) and the free-radical derived isoprostanes (e.g., 8-iso-prostaglandin (PG)F2α), play a role. Compounds of the invention preferably include a benzenesulfonyl urea in which the benzene is substituted by a substituted biphenylyloxy group (e.g., at the 2 position) and by a nitrile group (e.g., at the 5 position), which compounds show promising results as TP-isoform selective TP antagonists.
Claims15
A compound comprising a benzenesulfonyl urea wherein the benzene is substituted at the 2 position by a substituted biphenylyloxy group and at the 5 position by a nitrile group,
- wherein the biphenylyloxy group is substituted by one selected from the group consisting of a halogenated alkyl group, a halogenated methoxy group, a primary amide, a secondary amide, a tertiary amide, and a nitrile group, and
- wherein the urea is substituted by one selected from the group consisting of a halogen, an alkyl group, a halogenated alkyl group, an aryl group, and a halogenated aryl group, or a pharmaceutically acceptable salt thereof.
A compound represented by formula (I):
- wherein:
- R1 is selected from the group consisting of:
- a halogen, an alkyl group, a cycloalkyl group, an aryl group, a heterocycloalkyl group, a halogenated alkyl group, a halogenated cycloalkyl group, a halogenated aryl group, a halogenated heterocycloalkyl group, a halogenated methoxy group, an ethoxy group, an isopropoxy group, a tert-butoxy group, a halogenated ethoxy group, a halogenated isopropoxy group, a halogenated tert-butoxy group, a primary amide, a secondary amide, a tertiary amide, OH, a halogen, CO2H, methyl ketone, a nitrile group, a methyl ester group, an ethyl ester group, an isopropyl ester group, a tert-butyl ester group, a halogenated methyl ester group, a halogenated ethyl ester group, a halogenated isopropyl ester group, and a halogenated tert-butyl ester group;
- and
- R2 is selected from the group consisting of a halogen, an alkyl group, a halogenated alkyl group, an aryl group, and a halogenated aryl group,
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.