Patent SG-11201909189Q-A (SG)
Title: 6-pyrimidin-isoindole derivative as erk1/2 inhibitor
Inventor: READER MICHAEL
IPC: A61P35/00
Filed: 2018-04-20
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 25 October 2018 (25.10.2018) WIP0 I PCT omit °nolo Him um Hollow° ow (10) International Publication Number WO 2018/193410 Al (51) International Patent Classification: CO7D 405/14 (2006.01) A61P 35/00 (2006.01) A61K 31/506 (2006.01) (21) International Application Number: PCT/IB2018/052745 (22) International Filing Date: 20 April 2018 (20.04.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 1706327.2 20 April 2017 (20.04.2017) GB (71) Applicant: OTSUKA PHARMACEUTICAL CO., LTD. [JP/JP]; 2-9, Kanda Tsukasa-machi, Chiyoda-Ku, Tokyo 1018535 (JP). (72) Inventors: READER, Michael; 436 Cambridge Science Park, Milton Road, Cambridge CB4 OQA (GB). WILSHER, Nicola Elizabeth; 436 Cambridge Science Park, Milton Road, Cambridge CB4 OQA (GB). SAUN- DERS, Mark Henry; 111 Innovation Drive, Milton Park, Abingdon Oxfordshire OX14 4RZ (GB). BAGULEY, Paul Anthony; 111 Innovation Drive, Milton Park, Abingdon Oxfordshire OX14 4RZ (GB). LINDLEY, Colin Thomas; 111 Innovation Drive, Milton Park, Abingdon Oxfordshire OX14 4RZ (GB). MELLING, Robert Craig; 111 Innova- tion Drive, Milton Park, Abingdon Oxfordshire OX14 4RZ (GB). ADAMCZYK, Bozena Ewa; Via Alessandro Flem- ing, 4, CAP 37135 Verona (IT). SCARATI, Mirka; Via Alessandro Fleming, 4, CAP 37135 Verona (IT). (74) Agent: NAKAMICHI, Yoshihiro; SOJU Partners, 5th Floor, Okina Bldg., 2-9, Nishitenma 3-chome, Kita-ku, Os- aka-shi, Osaka 5300047 (JP). (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: - as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) of inventorship (Rule 4.17(iv)) Published: — with international search report (Art. 21(3)) (54) Title: 6-PYRIMIDIN-ISOINDOLE DERIVATIVE AS ERK1/2 INHIBITOR (57) : This invention relates to the compound (2R)-2-(6-{5-chloro-2-[(oxan-4-yDamino]pyrimidin-4-yll -1 -oxo-2,3-dihydro-1 H-isoindo1-2-y1)-N-[(1 S)-1-(3-fluoro-5-methoxypheny1)-2-hydroxyethyl]propanamide, and in particular to novel physical forms of the compound, a process for preparing the compound and synthetic intermediates for use in the process, and novel formulations containing the compound, as well as therapeutic uses of the compound.