Patent SG-11201811350Q-A (SG)
Title: Stable hydrolysis-resistant synthetic polyribosylribitolphosphate derivatives as vaccines against haemophilus influenzae type b
Inventor: SEEBERGER PETER H
IPC: A61K31/7032
Filed: 2017-07-28
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1 Ill 11111 0 11101 HOE HI 1 0 011101 010 1110 NOM I 11110 1111 011 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\" WO 2018/020046 Al 01 February 2018 (01.02.2018) WIP0 I PCT (51) International Patent Classification: (74) Agent: ARTH, Hans-Lothar; ABK Patent Attorneys, Jas- C07H 15/04 (2006.01) A61K 31/7042 (2006.01) minweg 9, 14052 Berlin (DE). CO7H 15/26 (2006.01) A61P 11/00 (2006.01) A61K 31/7032 (2006.01) A61K 39/00 (2006.01) (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (21) International Application Number: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, PCT/EP2017/069254 CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, (22) International Filing Date: DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, 28 July 2017 (28.07.2017) 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, (25) Filing Language: English MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, (26) Publication Language: English 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, (30) Priority Data: TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. 16181659.0 28 July 2016 (28.07.2016) EP (84) Designated States (unless otherwise indicated, for every PCT/EP2017/062725 kind of regional protection available): ARIPO (BW, GH, 26 May 2017 (26.05.2017) EP GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, (71) Applicant: MAX-PLANCK-GESELLSCHAFT ZUR UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, FORDERUNG DER WISSENSCHAFTEN E.V. TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, — [DE/DE]; Hofgartenstrasse 8, 80539 Munich (DE). 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, (72) Inventor: SEEBERGER, Peter H.; Rudolf-Bre-TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, itscheid-StraBe 46, 14532 Kleinmachnow (DE). KM, ML, MR, NE, SN, TD, TG). = (54) Title: STABLE HYDROLYSIS-RESISTANT SYNTHETIC POLYRIBOSYLRIBITOLPHOSPHATE DERIVATIVES AS = AGAINST HAEMOPHILUS INFLUENZAE TYPE B VACCINES = (57) : The present invention provides a stable synthetic saccharide = Figure 3 of Hib polyribosylribitol- phosphate (PRP) derivative and conjugate thereof. = = Said saccharide, said conjugate and pharmaceutical compositions thereof are hydrolysis-resistant, long-term stable and useful for the prevention and/or treat- ment of diseases associated with Haemophilus influenzae, and more specifical- = _ = ly of diseases associated with Haemophilus influenzae type b, preferably dis- eases selected from meningitis, pneumonia, and epiglotitis. They have general _ = formula (I): wherein A is formula (II) or formula (III); B is formula (IV); C = [ '' '' i is formula (V); D is formula (VI); E is formula (VII); F is formula (VIII) or 4v formula (IX). n-3 \" d = = = . ! = _ =.. . 5- A '-'. f li-') ? - 1- i. . = 17- T° m 4 nn Il , I.] 7r © © ei © -.... 1-1 © ei C [Continued on next page] WO 2018/020046 Al MIDEDIMOMMIDIREIEHEIDIONINERVOIS Published: — with international search report (Art. 21(3))