Patent SG-11201811737S-A (SG)
Title: Novel fatty acid modified urocortin-2 analogs for the treatment of diabetes and chronic kidney disease
Inventor: ALSINA-FERNANDEZ JORGE
IPC: A61K38/00
Filed: 2017-07-13
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property MD 1101111 0 DOI HIM 011101 0 0111111 01110111110111111111111111111111111111 Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/013803 Al 18 January 2018 (18.01.2018) W I P0 I P C T (51) International Patent Classification: TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, A61K 38/00 (2006.01) CO7K 14/47 (2006.01) EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, A61K 38/22 (2006.01) CO7K 14/575 (2006.01) MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (21) International Application Number: TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, PCT/US2017/041922 KM, ML, MR, NE, SN, TD, TG). (22) International Filing Date: Declarations under Rule 4.17: 13 July 2017 (13.07.2017) — as to applicant's entitlement to apply for and be granted a (25) Filing Language: English patent (Rule 4.17(ii)) — as to the applicant's entitlement to claim the priority of the (26) Publication Language: English earlier application (Rule 4.17(iii)) (30) Priority Data: Published: 62/362,711 15 July 2016 (15.07.2016) US — with international search report (Art. 21(3)) 62/431,682 08 December 2016 (08.12.2016) US — with sequence listing part of description (Rule 5.2(a)) 62/491,385 28 April 2017 (28.04.2017) US (71) Applicant: ELI LILLY AND COMPANY [US/US]; Lilly Corporate Center, Indianapolis, Indiana 46285 (US). (72) Inventors: ALSINA-FERNANDEZ, Jorge; c/o ELI LIL- LY AND COMPANY, P.O. Box 6288, Indianapolis, In- diana 46206-6288 (US). GUO, Lili; c/o ELI LILLY AND COMPANY, P.O. Box 6288, Indianapolis, Indiana 46206-6288 (US). LEE, John; c/o ELI LILLY AND COM- PANY, P.O. Box 6288, Indianapolis, Indiana 46206-6288 (US). (74) Agent: GRIMSHAW, Kyle W. et al.; ELI LILLY AND COMPANY, P.O. Box 6288, Indianapolis, Indiana 46206-6288 (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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, 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, 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, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, 1-1 ..! (54) Title: NOVEL FATTY ACID MODIFIED UROCORTIN-2 ANALOGS FOR THE TREATMENT OF DIABETES AND M CHRONIC KIDNEY DISEASE of (57) : The present invention provides a compound or a pharmaceutically acceptable salt of the Formula : X1 I V X2 SLDV M PIGLLQIL X 3 EQEKQEKEKQQA K* T N A X 4 ILAQ V-NH2 wherein the Xi denotes that the I residue is modified by either acetylation or methylation at the N-terminus; wherein X2 is L or T; wherein X3 is L or I; wherein X4 is Q or E; and wherein C 1-1 0 .-- f - 5 a modified K residue (\"K*\") at position 29 is modified through conjugation to the epsilon-amino group of the K-side chain with a group of the formula -X- 5 X 6 , wherein X5 is selected from the group consisting of one to four amino acids; one to four ([2-(2-Amino- N ethoxy)-ethoxy]-acetyl) moieties; and combinations of one to four amino acids and one to four ([2-(2-Amino-ethoxy)- ethoxy]-acetyl) moieties; and X6 is a C14 - C24 fatty acid. In some embodiments, the group of the formula -X 5 -X 6 is ([2-(2-Amino-ethoxy)-ethox3]- C acety1)2-(yE)2-00-(CH2) x -0O2H where xis 16 or 18.