Patent SG-11202000098R-A (SG)
Title: Polymorphic forms of dasatinib
Inventor: BHAT RAMAKRISHNA
IPC: C07D417/12
Filed: 2018-07-07
Abstract: 21heta - Scale Figure 3 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) oviolo Ina oimIE (19) World Intellectual Property Organization International Bureau (10) International Publication Number WO 2019/008555 Al (43) International Publication Date 10 January 2019 (10.01.2019) WIPO I PCT Uttara Kannada 581327 (IN). RAGHUNADHACHET- TY, Jithendrababu; No .7-138/D/10, Aragonda, Tha- vanam Palli Mandal, Andhra Pradesh, Chittoor District 517129 (IN). KALIAPPAN, Mariappan; Sri Sangili Matha Stores, Keelakuyilkudi Villakku, Theni Main Road, Nagamalai, Tamilnadu, Madurai 625019 (IN). PALLE, Venkata, Raghavendracharyulu; 194/A, Mythri Nagar, Madinaguda, Miyapur, Telangana, Hyderabad 500049 (IN). REGALLA, VijayBhaskar, Reddy; H.No: 1-102-1, Cha- trai (mandal & Post), Burugugudem Road, Andhra Pradesh, Krishna District 521214 (IN). (74) Agent: MAJUMDAR, Subhatosh et al.; S. Majumdar & Co., 5, Harish Mukherjee Road, West Bengal, Kolkata 700 025 (IN). (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, (51) International Patent Classification: CO7D 417/12 (2006.01) (21) International Application Number: PCT/IB2018/055022 07 July 2018 (07.07.2018) English English (22) International Filing Date: (25) Filing Language: (26) Publication Language: (30) Priority Data: 201741024067 07 July 2017 (07.07.2017) IN 201741029965 24 August 2017 (24.08.2017) IN 201841001249 11 January 2018 (11.01.2018) IN 201841007613 28 February 2018 (28.02.2018) IN (71) Applicant: BIOCON LIMITED [IN/IN]; 20th KM, Hosur Road, Electronic City, Karnataka, Bangalore 560 100 (IN). (72) Inventors: BHAT, Ramakrishna, Parameshwar; Kadekodi, Po: Dhareshwar, Ta: Kumta, Karnataka, Dist: (54) Title: POLYMORPHIC FORMS OF DASATINIB 15<x.2' n.f)f) 11 C 9000 anon r•-• .• W O 20 19/008555 Al (57) : The present invention provides for the dasatinib- thymine co-crystal and dasatinib-adenine co-crystal. The present invention further provides dasatinib-butanediol solvate. The present invention further provides for crystalline dasatinib-(f) — 1, 2-Butane diol, crystalline dasatinib (R)-1, 2-Butanediol, crystalline dasatinib (S)-1, 2-Butanediol and crystalline dasatinib (±)-2, 3-Butanediol and processes for preparation thereof. The present invention also provides for a process for preparation of amorphous dasatinib using dasatinib- butanediol solvate. The present invention further provides for the preparation of anhydrous dasatinib. The present invention also provides for a process for preparation of dasatinib monohydrate from anhydrous dasatinib [Continued on next page] WO 2019/008555 Al MIDEDIMOMOIDEIROMOIDOVIIMHEMMODEVOIMIE 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)) Published: — with international search report (Art. 21(3))