Patent SG-11201408491S-A (SG)
Title: Analogs of glucagon exhibiting gip receptor activity
Inventor: DIMARCHI RICHARD D
IPC: C07K14/435
Filed: 2013-06-18
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 27 December 2013 (27.12.2013) WIPOIPCT (10) International Publication Number WO 2013/192130 A1 (51) International Patent Classification: C07K14/435 (2006.01) (21) International Application Number: PCT/US2013/046229 (22) International Filing Date: 18 June 2013 (18.06.2013) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 61/662,874 21 June 2012 (21.06.2012) US 61/787,973 15 March 2013 (15.03.2013) US (71) Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION [US/US]; 351 West 10th Street, Indianapolis, Indiana 46202 (US). (71) Applicant (for US only): HOFFMANN-LA ROCHE INC. [US/US]; 340 Kingsland Street, Nutley, New Jersey 07110 (US). (71) Applicant (for all designated States except US): F. HOFF­ MANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124, CH-4070 Basel (CH). (72) Inventors: DIMARCHI, Richard D.; 10890 Wilmington Drive, Carmel, Indiana 46033 (US). SMILEY, David L.; 1013 Sherbrooke Drive, Bloomington, Indiana 47401 (US). BLEICHER, Konrad H.; Reichsgrafensrasse 16, 79102 Freiburg i. Br. (DE). KITAS, Eric A.; Eichbergweg 4, CH-4147 Aesch Baseband (CH). (74) Agents: BREEN, John P. et al.; Barnes & Thornburg LLP, 11 South Meridian Street, Indianapolis, Indiana 46204 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, 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, 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, [Continued on next page] (54) Title: ANALOGS OF GLUCAGON EXHIBITING GIP RECEPTOR ACTIVITY FIGURE 1 Total Change in Body Weight 5-i A -5- — CO -10- < -15- -20- -25- o m i-H CJ o\ i-H cn < CD M m D D 2 O ~r- w m D a T- c n m D D 2 O T W m O T OT m D T- W m O o 2 O (57) Abstract: Provided herein are glu­ cagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treat­ ing diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range. Time (Day 7) o CJ o £ WO 2013/192130 A11 lllll llllllll II llllll III lllll lllll lllll III III III lllll lllll lllll lllll llll lllllll llll llll llll OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, 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. (84) Designated States (unless otherwise indicated, for every kind of regional protection available)'. ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, 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, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: — of inventorship (Rule 4.17 (iv)) Published: — with international search report (Art. 21(3)) — with sequence listing part of description (Rule 5.2(a))