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1. (WO2010084169) FGF21 DERIVATIVES WITH ALBUMIN BINDER A-B-C-D-E- AND THEIR USE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/084169 International Application No.: PCT/EP2010/050720
Publication Date: 29.07.2010 International Filing Date: 22.01.2010
IPC:
A61K 38/18 (2006.01) ,A61K 47/48 (2006.01) ,A61P 3/04 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
16
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
17
from animals; from humans
18
Growth factors; Growth regulators
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
48
the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
04
Anorexiants; Antiobesity agents
Applicants:
NOVO NORDISK A/S [DK/DK]; Novo Allé DK-2880 Bagsværd, DK (AllExceptUS)
TAGMOSE, Tina Møller [DK/DK]; DK (UsOnly)
GARIBAY, Patrick William [US/DK]; DK (UsOnly)
ANDERSEN, Birgitte [DK/DK]; DK (UsOnly)
WANG, Jishu [CN/CN]; CN (UsOnly)
CONDE FRIEBOES, Kilian Waldemar [DE/DK]; DK (UsOnly)
BAK-JENSEN, Kristian Sass [DK/DK]; DK (UsOnly)
THØGERSEN, Henning [DK/DK]; DK (UsOnly)
WÖLDIKE, Helle [DK/DK]; DK (UsOnly)
NIELSEN, Peter Kresten [DK/DK]; DK (UsOnly)
SLAABY, Rita [DK/DK]; DK (UsOnly)
ZHANG, Xujia [CN/CN]; CN (UsOnly)
WIECZOREK, Birgit [DE/DK]; DK (UsOnly)
Inventors:
TAGMOSE, Tina Møller; DK
GARIBAY, Patrick William; DK
ANDERSEN, Birgitte; DK
WANG, Jishu; CN
CONDE FRIEBOES, Kilian Waldemar; DK
BAK-JENSEN, Kristian Sass; DK
THØGERSEN, Henning; DK
WÖLDIKE, Helle; DK
NIELSEN, Peter Kresten; DK
SLAABY, Rita; DK
ZHANG, Xujia; CN
WIECZOREK, Birgit; DK
Priority Data:
09151227.723.01.2009EP
09152144.305.02.2009EP
09164904.608.07.2009EP
Title (EN) FGF21 DERIVATIVES WITH ALBUMIN BINDER A-B-C-D-E- AND THEIR USE
(FR) DÉRIVÉS DU FGF21 ASSOCIÉS À UN AGGLUTINANT ALBUMINEUX A-B-C-D-E ET LEUR UTILISATION
Abstract:
(EN) The present invention relates to Fibroblast Growth Factor 21 (FGF21), more in particular to derivatives of FGF21 compounds having an albumin binder of the formula A-B- C-D-E- covalently attached. The invention also relates to novel FGF21 analogues, as well as to the pharmaceutical use of these FGF21 derivatives and analogues, in particular for the treatment of diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, and/or Non Alcoholic Fatty Liver Disease (NAFLD). The derivatives of the invention are protracted, e.g. capable of maintaining a low blood glucose level for a longer period of time, capable of increasing the in vivo half-life of FGF21, and/or result in a lower clearance of FGF21. The derivatives of the invention are preferably furthermore of an improved oxidative stability.
(FR) La présente invention concerne le facteur de croissance fibroblastique 21 (FGF21) et, plus précisément, des dérivés de composés de type FGF21 caractérisés par leur association, par liaison covalente, à un agglutinant albumineux de formule A-B-C-D-E. L'invention concerne également des analogues inédits du FGF21, ainsi que l'utilisation pharmaceutique desdits dérivés et analogues du FGF21, en particulier en vue du traitement du diabète, de la dyslipidémie, de l'obésité, des maladies cardiovasculaires, du syndrome métabolique et/ou de la stéatose hépatique non alcoolique (SHNA). Les dérivés de l'invention présentent une action prolongée, c'est-à-dire qu'ils sont capables de maintenir la glycémie sanguine à un niveau bas pendant plus longtemps, ainsi que d'entraîner un allongement de la demi-vie du FGF21 in vivo et/ou une clairance plus faible du FGF21. Les dérivés de l'invention présentent, en outre et de préférence, une résistance à l'oxydation améliorée.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
IL213848MXMX/a/2011/007544EP2389190JP2012515747CN102361647RU2011134454
CA2748593RU0002525393KR1020110117666BRPI1007313AU2010207721IN5267/CHENP/2011
ES2692495