BACKBONE CYCLIZED RADIOLABELLED SOMATOSTATIN ANALOGS

Title:

BACKBONE CYCLIZED RADIOLABELLED SOMATOSTATIN ANALOGS

Document Type and Number:

WIPO Patent Application WO2002062819

Kind Code:

A3

Abstract:

Novel radiodiagnostic and radiotherapeutic peptides which are conformationally constrained backbone cyclized somatostatin analogs, having improved somatostatin receptor subtype affinity and selectivity are disclosed. The backbone cyclized peptide analogs disclosed posses unique and superior properties over other analogs, such as chemical and metabolic stability, selectivity, increased biovailability and improved pharmacokinetics. Furthermore, the unique patterns of receptor subtype selectivity provide compounds having improved diagnostic and therapeutic utilities. Pharmaceutical compositions comprising the backbone cyclized somatostatin analogs and radiolabelled analogs, reagents for synthesizing same, and methods of using such compositions for radiodiagnostic and radiotherapeutic purposes are also disclosed.

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Inventors:

BONASERA THOMAS A (IL)
LIVNAH NURIT (IL)
YECHEZKEL TAMAR (IL)
SALITRA YOSEPH (IL)

Application Number:

PCT/IL2002/000091

Publication Date:

September 25, 2003

Filing Date:

February 04, 2002

Export Citation:

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Assignee:

PEPTOR LTD (IL)
BONASERA THOMAS A (IL)
LIVNAH NURIT (IL)
YECHEZKEL TAMAR (IL)
SALITRA YOSEPH (IL)

International Classes:

A61K51/08; C07K14/655; A61K38/00; (IPC1-7): A61K38/12

Foreign References:

US5871711A	1999-02-16
US5932189A	1999-08-03

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