Patent CA-3092357-A1 (CA)
Title: Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
Inventor: LUENGO JUAN
IPC: A61P35/00
Filed: 2019-03-14
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 111111 10111111 11111 0111 111110111 111110111 0101111111111 0111 11111110 1111101111011 1111 Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2019/178368 Al 19 September 2019 (19.09.2019) WIPO I PCT (51) International Patent Classification: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CO7D 487/04 (2006.01) A 61P 35/00 (2006.01) CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, CO7D 519/00 (2006.01) A 611(31/519 (2006.01) 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, (21) International Application Number: KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, PCT/US2019/022288 MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, (22) International Filing Date: OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, 14 March 2019 (14.03.2019) 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. (25) Filing Language: English (84) Designated States (unless otherwise indicated, for every (26) Publication Language: English kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, 62/642,727 14 March 2018 (14.03.2018) US UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, 62/666,726 04 May 2018 (04.05.2018) US TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, 62/742,048 05 October 2018 (05.10.2018) US 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, (71) Applicant: PRELUDE THERAPEUTICS, INCORPO- TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, RATED [US/LJS]; 200 Powder Mill Road, Experimental KM, ML, MR, NE, SN, TD, TG). Station E440/3213, Wilmington, DE 19803 (US). (72) Inventors: LUENGO, Juan; 50 Amherst Ct., Phoenixville, Published: PA 19460 (US). LIN, Hong; 11 Fairwind Lane, Exton, PA ¨ with international search report (Art. 21(3)) 19341 (US). HAWKINS, Michael; 318 Heckler St., Am-bler, PA 19002 (US). SHETTY, Rupa; 712 Amberley Dri-= ve, Blue Bell, PA 19422 (US). PITIS, Philip; 108 Sunrise Drive, NorthWales, PA 19454 (US). SABORIT VILLAR-= ROYA, Gisela; 13 Passatge Manent, 08330 Premia De Mar (US). ______________________________________ (74) Agent: LODISE, Stephanie, A. et al.; Baker & Hostetler LLP, 2929 Arch Street, Cira Centre, 12th Floor, Philadel-phia, PA 19104-2891 (US). ______________________________________ (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (54) Title: SELECTIVE INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASE 5 (PRMT5) (57) Abstract: The disclosure is directed to compounds of Formula I, which R1 are inhibitors of protein methyltransferase 5 (PRMT5). Pharmaceutical compo-sitions comprising compounds of Formula I, as well as methods of their use and preparation, are also described. N ) R2N HO 5 R R4111.- .,,to X HO 00 MIF CA 3092357 2020-08-25