PHARMACEUTICAL COMPOSITIONS COMPRISING SELECTIVE AGONISTS OF MELANOCORTIN 1 RECEPTOR AND THEIR USE IN THERAPEUTIC METHODS

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EP 2 925 340 B8

(12)	CORRECTED EUROPEAN PATENT SPECIFICATION
	Note: Bibliography reflects the latest situation

(15)	Correction information:
	Corrected version no 1 (W1 B1)

(48)	Corrigendum issued on:
	24.07.2019 Bulletin 2019/30

(45)	Mention of the grant of the patent:
	08.05.2019 Bulletin 2019/19

(21)	Application number: 13857618.6

(22)	Date of filing: 20.11.2013

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International Patent Classification (IPC):

A61K 38/34^(2006.01)
A61K 38/07^(2006.01)
A61Q 17/04^(2006.01)
C07K 5/097^(2006.01)
A61Q 19/04^(2006.01)
A61K 38/00^(2006.01)
A61P 35/00^(2006.01)

A61K 38/06^(2006.01)
A61K 8/64^(2006.01)
A61Q 19/00^(2006.01)
C07K 5/117^(2006.01)
A61Q 19/08^(2006.01)
A61P 17/00^(2006.01)

(86)	International application number:
	PCT/US2013/071033

(87)	International publication number:
	WO 2014/081846 (30.05.2014 Gazette 2014/22)

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PHARMACEUTICAL COMPOSITIONS COMPRISING SELECTIVE AGONISTS OF MELANOCORTIN 1 RECEPTOR AND THEIR USE IN THERAPEUTIC METHODS

PHARMAZEUTISCHE ZUSAMMENSETZUNGEN ENTHALTEND SELEKTIVE AGONISTEN DES MELANOCORTIN-1-REZEPTORS ZUR VERWENDUNG IN THERAPIEVERFAHREN

COMPOSITIONS PHARMACEUTIQUES COMPRENANT DES AGONISTES SÉLECTIFS DU RÉCEPTEUR DE LA MÉLANOCORTINE 1, ET LEUR UTILISATION DANS UNE MÉTHODE THÉRAPEUTIQUE

(84)	Designated Contracting States:
	AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

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Priority:

21.11.2012 US 201261729018 P

(43)	Date of publication of application:
	07.10.2015 Bulletin 2015/41

(73)	Proprietor: University Of Cincinnati
	Cincinnati, OH 45221-0829 (US)

(72)	Inventors:
	ABDEL-MALEK, Zalfa, A. Cincinnati, OH 45209 (US) KOIKOV, Leonid Cincinnati, OH 45233 (US) KNITTEL, James, J. Belchertown, MA 01007 (US)

(74)	Representative: Moore, Michael Richard et al
	Keltie LLP No.1 London Bridge London SE1 9BA London SE1 9BA (GB)

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References cited: :

WO-A1-2011/063366
US-A1- 2010 216 655

US-A1- 2006 003 386

HOLDER JERRY RYAN ET AL: "STRUCTURE-ACTIVITY RELATIONSHIPS OF THE MELANOCORTIN TETRAPEPTIDE AC-HIS-DPHE-ARG-TRP-NH2 AT THE MOUSE MELANOCORTIN RECEPTORS: PART 2 MODIFICATIONS AT THE PHE POSITION", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 45, no. 14, 1 July 2002 (2002-07-01), pages 3073-3081, XP009077300, ISSN: 0022-2623, DOI: 10.1021/JM010524P
YANG Y ET AL: "Novel binding motif of ACTH analogues at the melanocortin receptors", BIOCHEMISTRY 20091020 AMERICAN CHEMICAL SOCIETY USA, vol. 48, no. 41, 20 October 2009 (2009-10-20), pages 9775-9784, XP055270052, DOI: 10.1021/BI900634E
CHEN M ET AL: "Functional characterization of the modified melanocortin peptides responsible for ligand selectivity at the human melanocortin receptors", PEPTIDES, ELSEVIER, AMSTERDAM, NL, vol. 27, no. 11, 1 November 2006 (2006-11-01), pages 2836-2845, XP027957587, ISSN: 0196-9781 [retrieved on 2006-11-01]
KOIKOV L N ET AL: "Sub-Nanomolar hMC1R Agonists by End-Capping of the Melanocortin Tetrapeptide His-D-Phe-Arg-Trp-NH2", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, vol. 13, 1 January 2003 (2003-01-01), pages 2647-2650, XP002342336, ISSN: 0960-894X, DOI: 10.1016/S0960-894X(03)00552-3
ABDEL-MALEK ZALFA A ET AL: "alpha-MSH tripeptide analogs activate the melanocortin 1 receptor and reduce UV-induced DNA damage in human melanocytes", PIGMENT CELL & MELANOMA RESEARCH, vol. 22, no. 5, October 2009 (2009-10), pages 635-644, XP009189878,
RUWE A R ET AL: "Semi-rigid tripeptide agonists of melanocortin receptors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, vol. 19, no. 17, 1 September 2009 (2009-09-01), pages 5176-5181, XP026458585, ISSN: 0960-894X [retrieved on 2009-07-09]
KOIKOV ET AL.: 'Analogs of sub-nanomolar hMC1 R agonist LK-184 [Ph( CH 2) 3CO-His-D-Phe-Arg-Trp-NH2). An additional binding site within the human melanocortin receptor 1?' BIOORGANIC & MEDICINAL CHEMISTRY LETTERS., [Online] vol. 14, 09 June 2004, pages 3997 - 4000, XP055213969 Retrieved from the Internet: <URL:http://www.sciencedirect.com/ science /article/pii/S0960894X04006900>
CATANIA, A.: 'Melanocortins: Multiple Actions and Therapeutic Potential' ADVANCES IN EXPERIMENTAL MEDICINE AND BIOLOGY vol. 681, 2010, XP055263088 ISBN: 978-1-4419-6353-6 Retrieved from the Internet: <URL:http://f3.tiera.ru/llgenesis/575-579/5 76000/103eeea76e1380c962de22f451fb36c24.>
SINGH ET AL.: 'Incorporation of a Bioactive Reverse-Turn Heterocycle into a Peptide Template Using Solid-Phase Synthesis To Probe Melanocortin Receptor Selectivity and Ligand Conformations by 2D 1 H NMR' J. MED. CHEM., [Online] vol. 54, 09 February 2011, pages 1379 - 1390, XP055213971 Retrieved from the Internet: <URL:http://pubs.acs.org/doi/abs/10.1021/jm 101425m.>


	Remarks:
	The file contains technical information submitted after the application was filed and not included in this specification

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