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1. (WO2010080607) YL-BASED INSULIN-LIKE GROWTH FACTORS EXHIBITING HIGH ACTIVITY AT THE INSULIN RECEPTOR
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/080607 International Application No.: PCT/US2009/068713
Publication Date: 15.07.2010 International Filing Date: 18.12.2009
IPC:
A61K 38/00 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
Applicants:
INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION [US/US]; 351 West 10th Street Indianapolis, IN 46202, US (AllExceptUS)
DIMARCHI, Richard, D. [US/US]; US (UsOnly)
CHENG, Shujiang [CN/US]; US (UsOnly)
KOU, Binbin [CN/US]; US (UsOnly)
HAN, Jie [CN/US]; US (UsOnly)
Inventors:
DIMARCHI, Richard, D.; US
CHENG, Shujiang; US
KOU, Binbin; US
HAN, Jie; US
Agent:
BREEN, John, P.; Barnes & Thornburg LLP 11 South Meridian Street Indianapolis, IN 46204, US
Priority Data:
61/139,22319.12.2008US
Title (EN) YL-BASED INSULIN-LIKE GROWTH FACTORS EXHIBITING HIGH ACTIVITY AT THE INSULIN RECEPTOR
(FR) FACTEURS DE CROISSANCE SEMBLABLES À L'INSULINE À BASE D'YL EXPRIMANT UNE HAUTE ACTIVITÉ AU RÉCEPTEUR DE L'INSULINE
Abstract:
(EN) Insulin-like growth factor analogs are disclosed wherein substitution of the IGF native amino acids, at positions corresponding to positions B 16 and B 17 of native insulin, with tyrosine and leucine, respectively, increases potency of the resulting analog at the insulin receptor by tenfold. Also disclosed are prodrug and depot formulations of the IGF analogs, wherein the IGF analog has been modified by the linkage of a dipeptide to the analog through an amide bond linkage. The prodrug and depot formulations disclosed herein have extended half lives of at least 2 hours, 10 hours, and more typically greater than 20 hours, and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.
(FR) L'invention concerne des analogues de facteurs de croissance semblables à l'insuline dans lesquels la substitution des acides aminés natifs de l'IGF, à des positions qui correspondent aux positions B 16 et B 17 de l'insuline native, avec la tyrosine et la leucine, respectivement, augmente par dix la puissance de l'analogue résultant au récepteur de l'insuline. L'invention concerne aussi des formulations de promédicament et retard des analogues de l'IGF, dans lesquelles l'analogue de l'IGF a été modifié par liaison d'un dipeptide à l'analogue grâce à une liaison amide. Les formulations en question ont des demi-vies prolongées d'au moins 2 heures, 10 heures, et plus généralement supérieures à 20 heures, puis sont converties en forme active dans des conditions physiologiques par réaction non enzymatique menée par instabilité chimique.
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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, 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:
EP2376099JP2012512900US20110245164CN102307584CA2747720AU2009335713
IN4434/DELNP/2011