Judit Erchegyi

US Patent:

7238775, Jul 3, 2007

Filed:

Jan 24, 2005

Appl. No.:

11/041676

Inventors:

Jean E. F. Rivier - La Jolla CA, US
Jean Claude Reubi - Berne, CH
Judit Erchegyi - San Diego CA, US
Roland Riek - La Jolla CA, US

Assignee:

The Salk Institute for Biological Studies - San Diego CA

International Classification:

A61K 38/00

US Classification:

530311, 530300

Abstract:

Analogs of SRIF which are selective for SSTR4 in contrast to the other cloned SRIF receptors are useful in determining tissue and cellular expression of the receptor SSTR4 and its biological role in regulating tumor growth. SRIF analog peptides, such as des-AA[Ala]-SRIF; des-AA[Aph]-SRIF, des-AA[Aph]Cbm-SRIF; des-AA[Tyr,Ala]-Cbm-SRIF, and des-AA[Tyr,CMe-L-2Nal]-SRIF, and counterparts incorporating D-Cysand/or D-Trpand/or Ala, bind with high affinity to the cloned human receptor SSTR4 and activate the receptor, but they do not bind with significant affinity to human SSTR1, SSTR2, SSTR3 or SSTR5. By incorporating an iodinated tyrosine in position-2 in these SSTR4-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, cytotoxins or highly radioactive elements can be N-terminally coupled or complexed thereto.

US Patent:

7960342, Jun 14, 2011

Filed:

Oct 15, 2007

Appl. No.:

11/872367

Inventors:

Jean E. F. Rivier - La Jolla CA, US
Judit Erchegyi - San Diego CA, US
Jean Claude Reubi - Berne, CH
Helmut R. Maecke - Basel, CH

Assignee:

The Salk Institute for Biological Studies - La Jolla CA
Universitat Bern - Bern
University Hospital Basel - Basel

International Classification:

A61K 38/18
A61K 38/31

US Classification:

514 97, 514 111

Abstract:

SRIF peptide antagonists, which are selective for SSTR2 in contrast to the other cloned SRIF receptors and which bind with high affinity to the cloned human receptor SSTR2 but do not activate the receptor, have many useful functions. Because they do not bind with significant affinity to SSTR1, SSTR3, SSTR4 or SSTR5, their administration avoids potential undesirable side effects. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, highly radioactive moieties can be N-terminally coupled, complexed or chelated thereto.

US Patent:

8501687, Aug 6, 2013

Filed:

Jun 13, 2011

Appl. No.:

13/159020

Inventors:

Jean E. F. Rivier - La Jolla CA, US
Judit Erchegyi - San Diego CA, US
Jean Claude Reubi - Berne, CH
Helmut R. Maecke - Basel, CH

International Classification:

A61K 38/31
A61K 3/10
A61K 7/12

US Classification:

514 71

Abstract:

SRIF peptide antagonists, which are selective for SSTR2 in contrast to the other cloned SRIF receptors and which bind with high affinity to the cloned human receptor SSTR2 but do not activate the receptor, have many useful functions. Because they do not bind with significant affinity to SSTR1, SSTR3, SSTR4 or SSTR5, their administration avoids potential undesirable side effects. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, highly radioactive moieties can be N-terminally coupled, complexed or chelated thereto. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates.

US Patent:

20080299040, Dec 4, 2008

Filed:

Apr 16, 2008

Appl. No.:

12/104318

Inventors:

Jean E. F. RIVIER - La Jolla CA, US
Judit Erchegyi - San Diego CA, US
Jean Claude Reubi - Berne, CH
Helmut R. Maecke - Basel, CH

International Classification:

A61K 51/08
C07K 7/64
A61P 35/00
A61K 38/12

US Classification:

424 169, 530321, 514 11, 424 111

Abstract:

The invention is directed to somatostatin analogs which are receptor antagonists of the somatostatin receptor, including receptor-selective antagonists, especially sst2-selective antagonists. Related compounds and compositions are included, including antagonists complexed with or conjugated to radioactive nuclides. The antagonists of the invention are useful in diagnosing and treating neoplastic and non-neoplastic mammalian diseases; such methods, and kits, are encompassed.