EP1699495A2 — Conjugates of angiotensin ii and an imaging moiety

USPTO Abstract

The invention comprises pharmaceuticals of formula (I) Z-(L)n-V, wherein V denotes a peptide, L denotes an optional linker, Z denotes a group that optionally can carry an imaging moiety M, n denotes 0 or 1. The pharmaceuticals are active as therapeutic agents for the treatment of heart failure, cardiac arrhythmias and diseases were fibrosis is prominent such as COPD, liver fibrosis and atherosclerosis and are also useful as diagnostic agents for the diagnosis of heart failure and diseases were fibrosis is prominent such as COPD, liver fibrosis and atherosclerosis. The novel pharmaceuticals comprise a targeting moiety that binds to a receptor that may or may not be up-regulated and/or over-expressed in the diseased area. The targeting moiety comprises a group which for imaging agents carry a diagnostically imageable moiety, an optional linker group and a peptide moiety. The novel pharmaceutical compounds have high affinity for the Angiotensin Receptors, in particularly for the Angiotensin II (Ang II) type 1 (AT1) receptor.