Substituted quinazolines
AssigneeShire LLC
InventorsRichard Franklin, Bernard T. Golding
Life of this patent
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Abstract
This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence 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 at the position of substitution;
- or wherein R1 and R2, and/or R3 and R4 together with the carbon to which they are attached form a blocking group which functions to directly or indirectly 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;
- 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, C1-6 alkyl, or a Group I metal ion;
- provided always that R1, R2, R3 and R4 are not all hydrogen, or that when one of R1 and R2 is methyl and R3 and R4 are hydrogen then other of R1 and R2 is not hydrogen.
Dependencies are inferred from the claim text.