Patent SG-11201901355S-A (SG)
Title: Methods of treating severe insulin resistance by interfering with glucagon receptor signaling
Inventor: GROMADA JESPER
IPC: C07K16/28
Filed: 2017-08-29
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property MD 1101111 0 DOI HIM 011101 0 0111111111111110111111 01111111011110111111 Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/044903 Al 08 March 2018 (08.03.2018) WI P0 I P C T (51) International Patent Classification: Road, Tarrytown, New York 10591 (US). HARP, Joyce; c/ A61K 39/395 (2006.01) C07K 16/28 (2006.01) o Regeneron Pharmaceuticals Inc., 777 Old Saw Mill River A61K 45/06 (2006.01) A61P 3/10 (2006.01) Road, Tarrytown, New York 10591 (US). C07K 16/26 (2006.01) (74) Agent: CROWLEY-WEBER, Cara L. et al.; Brownstein (21) International Application Number: Hyatt Farber Schreck, LLP, 410 Seventeenth Street, Suite PCT/US2017/049137 2200, Denver, Colorado 80202 (US). (22) International Filing Date: (81) Designated States (unless otherwise indicated, for every 29 August 2017 (29.08.2017) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, (25) Filing Language: English CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, (26) Publication Language: English DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, (30) Priority Data: HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, 62/381,263 30 August 2016 (30.08.2016) US KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, 62/411,032 21 October 2016 (21.10.2016) US MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, (71) Applicant: REGENERON PHARMACEUTICALS, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, INC. [US/US]; 777 Old Saw Mill River Road, Tarrytown, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. New York 10591-6707 (US). (84) Designated States (unless otherwise indicated, for every (72) Inventors: GROMADA, Jesper; c/o Regeneron Pharma- kind of regional protection available): ARIPO (BW, GH, ceuticals, Inc., 777 Old Saw Mill River Road, Tarrytown, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, New York 10591 (US). OKAMOTO, Haruka; c/o Regen- UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, eron Pharmaceuticals, Inc., 777 Old Saw Mill River Road, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, = Tarrytown, New York 10591 (US). JASPERS, Stephen; c/ EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, = — o Regeneron Pharmaceuticals Inc., 777 Old Saw Mill River MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, = (54) Title: METHODS OF TREATING SEVERE INSULIN RESISTANCE BY INTERFERING WITH GLUCAGON RECEPTOR SIGNALING = = IR Antagonist = Infusion .\"- Isotype control + PBS # = 4 ..0- H41-(1327P + PBS Isotype control + S961 = .1€0 H41-11327P ÷ S961 = , = t V = Ttille 0100 FIG. 1A ,-, 0 en (57) : Provided herein are methods of treating a patient with severe insulin resistance. The methods comprise administering to O N a patient in need thereof a therapeutic amount of a GCG/GCGR signaling pathway inhibitor, such that blood glucose or beta-hydroxy- 1 butyrate levels are lowered or that the severe insulin resistance is mediated, or a condition or disease characterized by severe insulin 0 7 r resistance is mediated, or at least one symptom or complication associated with the condition or disease is alleviated or reduced in —. severity. The GCG/GCGR signaling pathway inhibitor can be a small molecule inhibitor of the signaling pathway, an antisense inhibitor GC of 1-1 the signaling pathway, a GCG neutralizing monoclonal antibody, a GCGR antagonist, a peptide inhibitor of the signaling pathway, © a DARPin, a Spiegelmer, an aptamer, engineered Fn type-III domains, etc. The therapeutic methods are useful for treating a human el suffering from severe insulin resistance. o [Continued on next page] WO 2018/044903 Al O II 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))