Patent SG-11201908603P-A (SG)
Title: Macrocyclic compound and uses thereof
Inventor: KISHI YOSHITO
IPC: A61P35/00
Filed: 2018-04-03
Abstract: 30 10 20 Days 0 -4 , -control -411FHali-B 0.05 mg/kg -•<. Compound (1) 0.2 mg/kg Re la t ive tumor volum e 4 • 3 - 2 GO N Go O C (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) CORRECTED VERSION (19) World Intellectual Property Organization International Bureau (43) International Publication Date 1111111111110110101011111011010 I 1011111101110110141011110# (10) International Publication Number WO 2018/187331 A8 11 October 2018 (11.10.2018) WIPO I PCT (51) International Patent Classification: CO7D 493/22 (2006.01) A61K 31/357 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/US2018/025887 (22) International Filing Date: 03 April 2018 (03.04.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/482,030 05 April 2017 (05.04.2017) US 62/526,677 29 June 2017 (29.06.2017) US 15/814,105 15 November 2017 (15.11.2017) US 62/586,416 15 November 2017 (15.11.2017) US (71) Applicants: PRESIDENT AND FELLOWS OF HAR- VARD COLLEGE [US/US]; 17 Quincy Street, Cam- bridge, MA 02138 (US). EISAI R&D MANAGEMENT CO., LTD. [JP/JP]; 4-6-10 Koishikawa, Bunkyo-ku, Tokyo, 112-8088 (JP). (72) Inventors: KISHI, Yoshito; 75 Cambridge Parkway, Unit E902, Cambridge, MA 02142-1233 (US). KIRA, Kazunobu; C/o Eisai Co., Ltd., Tsukuba Research Labora- tories, 5-1-3 Tokodai, Ibaraki, Tsukuba-shi, 300-2635 (JP). ITO, Ken; C/o Eisai Co., Ltd., Tsukuba Research Labora- tories, 5-1-3 Tokodai, Ibaraki, Tsukuba-shi, 300-2635 (JP). (74) Agent: BAKER, C., Hunter; Wolf, Greenfield & Sacks, P.C., 600 Atlantic Avenue, Boston, MA 02210-2206 (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, (54) Title: MACROCYCLIC COMPOUND AND USES THEREOF Figure 1 Compound (1) (57) : The present invention provides novel Compound (1) having tumor vascular remodeling effect and/or anti-CAF (Cancer Associated Fibroblasts) activity, or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable and medical uses thereof. Compound (1) [Continued on next page] WO 2018/187331 A8 MIDEDIM01101 DIONER131111111111111111111111111111110#10# 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, 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). Published: — with international search report (Art. 21(3)) (48) Date of publication of this corrected version: 06 December 2018 (06.12.2018) (15) Information about Correction: see Notice of 06 December 2018 (06.12.2018)