Halogenated somatostatin analogs with multiple somatostatin receptor subtype selectivity
AssigneeGrafton Therapeutics SàRl
InventorsAlan HARRIS, Adrian DALY
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Abstract
The present invention relates to halogenated somatostatin analogs with selectivity for multiple somatostatin receptor subtypes and pharmaceutical compositions comprising the same. Moreover, the present invention relates to said halogenated somatostatin analogs and pharmaceutical compositions for use in therapy and/or diagnosis, for example in the treatment and/or diagnosis of diseases (e.g., cancer such as a neuroendocrine cancer) that are characterized by a high expression (e.g., overexpression) of one or more somatostatin receptor subtypes (e.g., somatostatin receptor 2 (SST2) and/or somatostatin receptor 5 (SST5)).
Claims15
A compound of the Formula I, or a pharmaceutically acceptable salt or solvate thereof:
- wherein:
- X1 is selected from the group consisting of —F, —Cl, —Br, and —I;
- X2 is selected from the group consisting of —F, —Cl, —Br, and —I;
- and
- Y1 is selected from the group consisting of —H, a chelator, L1-H, -L1-chelator, an amino protecting group, and a solid support;
- wherein L1 is a linker;
- provided that X1 and X2 are not both —I.
Dependencies are inferred from the claim text.