SG11201805092WA - Cortistatin analogs and uses thereof - Google Patents

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization IIIMIOH0110101011111 HO 11111011101110111 011111111011110111111011011# International Bureau .. .... ..Yejd (10) International Publication Number (43) International Publication Date ..... ...r .....1 WO 2017/112815 Al 29 June 2017(29.06.2017) WIPO I PCT (51) International Patent Classification: C07D 519/00 (2006.01) C07K 16/26 C07D 493/08 (2006.01) (21) International Application Number: (22) International Filing Date: 21 December (25) Filing Language: (26) Publication Language: (30) Priority Data: 62/387,246 23 December 2015 (23.12.2015) 62/297,494 19 February 2016 (19.02.2016) (71) Applicant: PRESIDENT AND FELLOWS VARD COLLEGE [US/US]; 17 MA 02138 (US). (72) Inventors: SHAIR, Matthew, D.; lows of Harvard College, 17 Quincy MA (US). PELISH, Henry, Efrem; AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (2006.01) 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, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, PCT/US2016/068125 MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, 2016 (21.12.2016) 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, English ZA, ZM, ZW. English (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, US GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, US TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, OF HAR- DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, Quincy St, Cambridge, 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). c/o President and Fel- Street, Cambridge, Declarations under Rule 4.17: c/o President and Fel- - as to applicant's entitlement to apply for and be granted a Street, Cambridge, patent (Rule 4.17(ii)) — as to the applicant's entitlement to claim the priority of the al.; Knowles Intellectu- earlier application (Rule 4.17(iii)) Center Terrace Published: indicated, for every — with international search report (Art. 21(3)) AE, AG, AL, AM, — lows of Harvard College, 17 Quincy — MA (US). = (74) Agents: BELLOWS, Brent, R. et Property LLC, 400 Perimeter al Strategies, NE, Suite 200, Atlanta, GA 30346 (US). (81) (unless otherwise Designated States = kind of national available): protection = USES THEREOF .4. vehicle .0.. F 1 mpk PO CA 0.16 mpk IP -4- B It) mpk PO = (54) Title: CORTISTATIN ANALOGS AND = = = = GI 0 = .61 32768 .. = .0 16384 . _ c 8192 . = 4096 2048 0 0 go 1024 _ c„) 512 _ 0 eD 256 .9 128 C 5 mpk PO -is. D 3nips; IV 1-1 & ir) 1 3 6 9 1.2 15 ,-1 Treatment days GC ei 11 FIG. 31 11 IN 1-1 (57) : Specific Cortistatin derivatives with advantageous properties for in vivo administration to a host, including a human, N in need thereof are provided. These novel species have advantageous pharmacokinetics, low toxicity, low to moderate hERG activ - ity, and/or other pharmacological properties which make them stand out among the class of Cortistatins as superior candidates for 0 human administration.