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    • 2. 发明申请
    • CONJUGATES OF ANGIOTENSIN II AND AN IMAGING MOIETY
    • 血管紧张素II和成像环境的关系
    • WO2005044313A3
    • 2006-05-11
    • PCT/NO2004000335
    • 2004-11-05
    • AMERSHAM HEALTH ASCUTHBERTSON ALANINDREVOLL BAARDERIKSEN MORTEN
    • CUTHBERTSON ALANINDREVOLL BAARDERIKSEN MORTEN
    • A61K51/08A61K38/08A61K49/00A61P1/16A61P9/00A61P9/06A61P9/10A61P11/00C07K7/14
    • A61K51/08A61K38/085A61K49/0043A61K49/0056A61K51/088C07K7/14
    • 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 (AT 1 ) receptor.
    • 本发明包括式(I)Z-(L)-N-V的药物,其中V表示肽,L表示任选的接头,Z表示任选地可携带成像部分M的基团, n表示0或1.药物作为治疗心力衰竭的治疗剂是有活性的,心律不齐,纤维化突出如COPD,肝纤维化和动脉粥样硬化等疾病,也可用作诊断心力衰竭的诊断剂, 纤维化疾病如COPD,肝纤维化和动脉粥样硬化等疾病突出。 新型药物包含结合受体的靶向部分,所述受体在患病区域中可能或可能不被上调和/或过度表达。 靶向部分包含用于成像剂携带诊断可成像部分,任选的连接基团和肽部分的基团。 新型药物化合物对血管紧张素受体具有高亲和力,特别是对于血管紧张素II(Ang II)1型(AT 1 H 1)受体。