Substituted quinazolines
AssigneeShire LLC
InventorsRichard Franklin, Bernard T. Golding, Peter A. Cicala
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Abstract
This invention relates to the discovery of prodrugs of 3- or 5-substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets.
Claims20
A compound of Formula (I) or a pharmaceutically acceptable salt or solvate thereof
- wherein:
- R1, R2, R3 and R4 independently represent hydrogen or a blocking group which functions to prevent metabolic reaction either directly or indirectly at the 3-position;
- or R1 and R2, and/or R3 and R4 together with the carbon to which they are attached form a blocking group which functions to prevent metabolic reaction at the 3-position, the remainder of groups R1 to R4 being hydrogen;
- R5 is selected from the group comprising:
- fluoro, chloro, bromo and iodo;
- R6 is selected from the group comprising:
- fluoro, chloro, bromo and iodo;
- and
- R7 and R8 are independently selected from the group comprising:
- H;
- halo;
- cyano;
- C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, and C1-6 haloalkoxy;
- and
- R9 is H or C1-6 alkyl,
- R10 is selected from the group comprising:
- hydrogen;
- C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and C3-8 cycloalkyl wherein each of the foregoing groups may be optionally substituted by 1 to 5 groups chosen independently from the group comprising:
- halo, hydroxyl, cyano, nitro, C1-4 alkylsulphonyl and COOH;
- or R10 is a pharmaceutically acceptable cation, and
- X is O or S,
- provided always that R1, R2, R3 and R4 are not all hydrogen.
Dependencies are inferred from the claim text.