Title:
METHODS FOR IMPROVING THE ANTAGONISTIC/AGONISTIC PROPERTIES OF PEPTIDIC ANTAGONISTS/AGONISTS OF THE CORTICOTROPIN-RELEASING FACTOR RECEPTOR (CRFR)
Document Type and Number:
WIPO Patent Application WO2002024732
Kind Code:
A3
Abstract:
The present invention relates to a method for improving the antagonistic/agonistic properties of peptidic antagonists/agonists of the corticotropin-releasing factor receptor (CRFR). Further, the present invention relates to an antagonist of the ligand of the corticotropin-releasing factor receptor (CRFR) comprising or alternatively consisting of the amino acid sequence of astressin wherein at least Ala at position 11 is replaced by another amino acid. Further, the present invention relates to an antibody directed against the agonist or antagonist of the present invention. Also described is an anti-idiotypic antibody which is directed against the antibody(ies) of the invention. The present invention also relates to a pharmaceutical or diagnostic composition comprising the antagonist, the agonist, the antibody(ies) and/or the anti-idiotypic antibody of the invention. Furthermore, the present invention relates to a kit comprising the agonist, the antagonist, the antibody(ies) and/or the anti-idiotypic antibody of the present invention. Also described is the use of the agonist, the antagonists, the antibody(ies) and/or the anti-idiotypic antibody of the invention for the preparation of a pharmaceutical composition for the treatment, diagnosis and/or prevention of corticotropin-releasing factor receptor-associated diseases. The present invention also relates to a method of refining the agonist and/or the antagonists of the present invention by means of peptidomimetics and synthesizing the refined compound. Furthermore, the present invention relates to a method of formulating the agonist/antagonist of the invention into a pharmaceutical composition.
Inventors:
ECKART KLAUS (DE)
SPIESS JOACHIM (DE)
JAHN OLAF (DE)
SPIESS JOACHIM (DE)
JAHN OLAF (DE)
Application Number:
PCT/EP2001/011031
Publication Date:
January 23, 2003
Filing Date:
September 24, 2001
Export Citation:
Assignee:
MAX PLANCK GESELLSCHAFT (DE)
ECKART KLAUS (DE)
SPIESS JOACHIM (DE)
JAHN OLAF (DE)
ECKART KLAUS (DE)
SPIESS JOACHIM (DE)
JAHN OLAF (DE)
International Classes:
A61K38/22; C07K14/575; G01N33/68; A61K38/00; (IPC1-7): C07K14/575; A61K38/22; G01N33/68
Domestic Patent References:
| WO1996019499A2 | 1996-06-27 |
Other References:
A RÜHMANN ET AL.: "Structural requirements for peptidic antagonists of the corticotropin-releasing factor receptor (CRFR): development of CRFR-2beta selective antisauvagine-30", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF USA., vol. 95, December 1998 (1998-12-01), NATIONAL ACADEMY OF SCIENCE. WASHINGTON., US, pages 15264 - 15269, XP002211901, ISSN: 0027-8424
J E RIVIER ET AL.: "Constrained corticotropin releasing factor antagonists (astressin analogues) with long duration of action in the rat.", JOURNAL OF MEDICINAL CHEMISTRY., vol. 42, no. 16, 1999, AMERICAN CHEMICAL SOCIETY. WASHINGTON., US, pages 3175 - 3182, XP002211902, ISSN: 0022-2623
J RIVIER ET AL.: "Astressin analogues (corticotropin-releasing factor antagonists) with extended duration of action in the rat", JOURNAL OF MEDICINAL CHEMISTRY., vol. 41, no. 25, 1998, AMERICAN CHEMICAL SOCIETY. WASHINGTON., US, pages 5012 - 5019, XP002211903, ISSN: 0022-2623
O JAHN ET AL.: "Pharmacological characterization of recombinant rat corticotropin releasing factor binding protein using different sauvagine analogs", PEPTIDES, vol. 22, no. 1, 2001, ELMSFORD, US, pages 47 - 56, XP002211904, ISSN: 0196-9781
J E RIVIER ET AL.: "Constrained corticotropin releasing factor antagonists (astressin analogues) with long duration of action in the rat.", JOURNAL OF MEDICINAL CHEMISTRY., vol. 42, no. 16, 1999, AMERICAN CHEMICAL SOCIETY. WASHINGTON., US, pages 3175 - 3182, XP002211902, ISSN: 0022-2623
J RIVIER ET AL.: "Astressin analogues (corticotropin-releasing factor antagonists) with extended duration of action in the rat", JOURNAL OF MEDICINAL CHEMISTRY., vol. 41, no. 25, 1998, AMERICAN CHEMICAL SOCIETY. WASHINGTON., US, pages 5012 - 5019, XP002211903, ISSN: 0022-2623
O JAHN ET AL.: "Pharmacological characterization of recombinant rat corticotropin releasing factor binding protein using different sauvagine analogs", PEPTIDES, vol. 22, no. 1, 2001, ELMSFORD, US, pages 47 - 56, XP002211904, ISSN: 0196-9781
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