Patent SG-11201906539Y-A (SG)
Title: Hyperstabilized liposomes increase targeting of mitotic cells
Inventor: NG CHANG ZHI ADRIAN
IPC: A61K9/127
Filed: 2018-01-17
Abstract: WO 18/ 13600 2 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 26 July 2018 (26.07.2018) WIPO I PCT omit °nolo oimIE (10) International Publication Number WO 2018/136002 Al (51) International Patent Classification: A61K 9/127 (2006.01) A61K 31/519 (2006.01) A61K 31/00 (2006.01) A61P 35/00 (2006.01) A61K 47/00 (2006.01) (21) International Application Number: PCT/SG2018/050026 (22) International Filing Date: 17 January 2018 (17.01.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/447,498 18 January 2017 (18.01.2017) US (71) Applicant: TEMASEK LIFE SCIENCES LABORATO- RY LIMITED [SG/SG]; National University of Singapore, 1 Research Link, Singapoore 117604 (SG). (72) Inventors: NG, Chang Zhi Adrian; c/o Temasek Life Sciences Laboratory Limited, National University of Singa- pore, 1 Research Link, Singapore 117604 (SG). CHEONG, Shen-Yi Ian; c/o Temasek Life Sciences Laboratory Limit- ed, National University of Singapore, 1 Research Link, Sin- gapore 117604 (SG). (74) Agent: MATTEUCCI, Gianfranco; Marks & Clerk Sin- gapore LLP, Tanjong Pagar, P 0 Box 636, Singapore 910816 (SG). (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, 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)) — in black and white; the international application as filed contained color or greyscale and is available for download from PATENTSCOPE (54) Title: HYPERSTABILIZED LIPOSOMES INCREASE TARGETING OF MITOTIC CELLS (57) : Hyperstable liposome comprising an anti-mitotic agent, one or more anions and one or more cations entrapped in the inner milieu, 81921 wherein the entrapped anti-mitotic drug is released at a slow rate that is less than 0.6% in 12 hours or less than 5% in 8 hours when the liposomes a 4096, are suspended in 600mM sucrose. These liposomes are useful in the treat- ment of cancer. In particular, HEPC:Chol:DSPE-PEG2000 (50:45:5) li- posomes comprising BI 2536 and citrate:phosphate in a ratio of 1 :3. pp 2048 , LL CC 1024, - A - H 512 1.0 0.8 0.6 0.4 0.2 Concentration (M) Fig. 2