Patent SG-11201901795Q-A (SG)
Title: Biosynthetic heparin
Inventor: DOUAISI MARC
IPC: C12P19/64
Filed: 2017-09-07
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1111111011110111010101111101101001111111111111111111111111111111111111111111 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\" WO 2018/048973 Al 15 March 2018 (15.03.2018) WI P0 I P C T (51) (21) (22) (25) Filing Language: (26) (30) (71) (72) Inventors: DOUAISI, Marc; c/o Rensselaer Polytechnic — International Patent Classification: o Rensselaer C12N 9/10 (2006.01) C12P 19/64 (2006.01) New C12P 19/04 (2006.01) o Rensselaer International Application Number: New PCT/US2017/050385 o Rensselaer New International Filing Date: selaer 07 September 2017 (07.09.2017) York selaer English Publication Language: English tute, Kevin; Priority Data: Troy, 62/384,341 07 September 2016 (07.09.2016) US J.; c/o Applicant: RENSSELAER POLYTECHNIC INSTI- Troy, TUTE [US/US]; 110 8th Street, Troy, New York c/o 12180-3590 (US). New laer 12180-3590 Institute, 110 8th Street, Troy, New York 12180-3590 (US). GROVER, Navdeep; c/o Rensselaer Polytechnic Institute, (74) Agent: 110 8th Street, Troy, New York 12180-3590 (US). DAT- 3000 TA, Payel; c/o Rensselaer Polytechnic Institute, 110 8th lumbia Street, Troy, New York 12180-3590 (US). PASKALE- (81) Designated VA, Elena; c/o Rensselaer Polytechnic Institute, 110 8th kind Street, Troy, New York 12180-3590 (US). LIN, Lei; c/ AO, Polytechnic Institute, 110 8th Street, Troy, York 12180-3590 (US). BRODFUEHRER, Paul; c/ Polytechnic Institute, 110 8th Street, Troy, York 12180-3590 (US). SIMMONS, Trevor J.; c/ Polytechnic Institute, 110 8th Street, Troy, York 12180-3590 (US). ONISHI, Akihiro; c/o Rens- 12180-3590 Polytechnic Institute, 110 8th Street, Troy, New 12180-3590 (US). HIRAKANE, Makoto; c/o Rens- Polytechnic Institute, 110 8th Street, Troy, New York (US). FU, Li; c/o Rensselaer Polytechnic Insti- 110 8th Street, Troy, New York 12180-3590 (US). LI, c/o Rensselaer Polytechnic Institute, 110 8th Street, New York 12180-3590 (US). LINHARDT, Robert Rensselaer Polytechnic Institute, 110 8th Street, New York 12180-3590 (US). DORDICK, Jonathan; Rensselaer Polytechnic Institute, 110 8th Street, Troy, York 12180-3590 (US). MORI, Daisuke; c/o Rensse- Polytechnic Institute, 110 8th Street, Troy, New York (US). MAEBIUS, Stephen et al.; Foley & Lardner LLP, K Street NW, Suite 600, Washington, District of Co- 20007-5109 (US). States (unless otherwise indicated, for every of national protection available): AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, _ = Title: BIOSYNTHETIC HEPARIN Legend 'tt• Glucuronic acid 4 iduranic add N.acetyl giucosamine S Suifo group First intermediate Second Intermediate Third Intermediate Biosynthetic : The present disclosure relates synthesis may involve three intermediates starting from heparosan. Heparosan NSO N52S NS2S6S heparin to synthesis Figure 1 * s Chemical N-de-acetylation and N-suffatia n *so .4k tots N SNS NS C.5-epi & 205T is • ass NS 2S NS 2S N S SOST'1&3 S S . a \ 2S NS 30ST- * PAPS PAPS Mill PAPS (54) = = _ — = — = = = = — = — 1-1 en IN CT GC 71- 0 --.... 00 1-1 N (57) ... The (BSIO . 3$N525 /- 6S S 6S 6S 6S • * 4 • • NS 2 N of heparin, which may be bioequivalent to porcine USP Heparin Sodium. [Continued on next page] WO 2018/048973 Al MIDEDIMOMOIDEIREEMOOVIVEIMOHIIMOVOIS 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: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(11)) — as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: — with international search report (Art. 21(3))