Patent SG-11201907956U-A (SG)
Title: Biodegradable drug-polymer conjugate
Inventor: BIRKETT STEPHEN
IPC: A61P27/02
Filed: 2018-03-14
Abstract: 20 30 Time (Days] 50 50 —M— Example 170 —0—.Example 197 —A— Example 191 Example 233 Mess o f p o ly mer 1%1 SO 70 60 50 40 30 20 10 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 20 September 2018 (20.09.2018) WIP0 I PCT omit IIl °nolo Oil woo °mum oimIE (10) International Publication Number WO 2018/165711 Al (51) International Patent Classification: A61K 47/50 (2017.01) A61K 31/47 (2006.01) A61K 31/5575 (2006.01) A61K 31/433 (2006.01) A61K 31/085 (2006.01) A61P 27/02 (2006.01) A61K 31/21 (2006.01) (21) International Application Number: PCT/AU2018/050234 (22) International Filing Date: 14 March 2018 (14.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 2017900888 14 March 2017 (14.03.2017) AU 15/458,546 14 March 2017 (14.03.2017) US (71) Applicant: POLYACTIVA PTY LTD [AU/AU]; Level 9, 278 Collins Street, Melbourne, Victoria 3000 (AU). (72) Inventors: BIRKETT, Stephen, Lonsdale; 11 Langewan Road, Langwarrin, Victoria 3910 (AU). DONOHUE, An- drew, Craig; 15 Birdwood Street, Bentleigh East, Victoria 3165 (AU). D' SOUZA, Asha, Marina; 53 Shepparson Av- enue, Carnegie, Victoria 3163 (AU). NG, Sara Man Yee; 124 Wurundjeri Boulevard, Berwick, Victoria 3806 (AU). SULISTIO, Adrian; 1/17-19 Peate Avenue, Glen Iris, Vic- toria 3146 (AU). TAIT, Russell, John; 33 Campbell Road, Balwyn, Victoria 3103 (AU). VALADE, David; 1A Stel- la Street, Glenroy, Victoria 3046 (AU). NAYLOR, Alan; 1 Limekiln Close, Royston Hertfordshire SG8 9XP (GB). WATLING, Jason; 6 Seville Court, Cheltenham, Victoria 3192 (AU). SCULLINO, Carmen, Vittoria; 11 Elizabeth Street, Moonee Ponds, Victoria 3039 (AU). (54) Title: BIODEGRADABLE DRUG-POLYMER CONJUGATE Figure 10 X —Q—R—Q—X D ( I) J-( Y — A), III (57) : A drug-polymer conjugate, which is a copolymer of at least one monomer of formula (I): (I) where: X may be the same or different at each occurrence and represents a terminal functional group comprising an alkyne or an azide; Q is independently selected at each occurrence and may be present or absent and when present, represents a linking group; R is selected from the group consisting of linear or branched hydrocarbon, optionally substituted aryl and optionally substituted heteroaryl; D is a releasable drug selected from prostaglandins, [3-blockers and mixtures thereof; L is a linker group group; and at least one co-monomer of Formula III III J represents a linking functional group, n is 2 to 8, preferably 3 to 8; Y comprises a polyether of formula (ORa)m wherein Ra is independently ethylene, propylene and butylene and m is from 1 to 300 (preferably 2 to 300) and the polyether is in chain with one or more groups which are preferably selected from one or more of optionally substituted straight or branched Ci to do alkylene, amino, [Continued on next page] WO 2018/165711 Al 11111101MOMOIDEIREEMOMMIDIEMMOVOIS (74) Agent: PHILLIPS ORMONDE FITZPATRICK; Level 16, 333 Collins Street, Melbourne, Victoria 3000 (AU). (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). Published: — with international search report (Art. 21(3)) ether, ester, amide, carbonate and carbamate; A may be the same or different at each occurrence and represents a group comprising a terminal functional group comprising an alkyne or an azide functionality, wherein said terminal functional group is complementary to the terminal functional group X of formula (I) providing triazole moieties from reaction of X and A.