Patent SG-11201811515W-A (SG)
Title: Method for producing a polymorphic form of 3-[5-amino-4-(3- cyanobenzoyl)-pyrazol-1-yl]-n-cyclopropyl-4-methylbenzamide
Inventor: SULEIMAN OSAMA
IPC: C07D231/38
Filed: 2017-07-13
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 111111101111 0 1110101011111 011101 0 011111111111111111001111111011111111111 0111111 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\"\" WO 2018/011579 Al 18 January 2018 (18.01.2018) W I P0 I P C T (51) International Patent Classification: MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, A61K 31/415 (2006.01) A61P 29/00 (2006.01) TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, CO7D 231/38 (2006.01) KM, ML, MR, NE, SN, TD, TG). (21) International Application Number: PCT/GB2017/052056 Published: — with international search report (Art. 21(3)) (22) International Filing Date: 13 July 2017 (13.07.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 1612240.0 14 July 2016 (14.07.2016) GB (71) Applicant: MEREO BIOPHARMA 1 LIMITED [ /GB]; 1 Cavendish Place, London, Greater London W1G OQF (GB). (72) Inventors: SULEIMAN, Osama; Johnson Matthey Plc., Fine Chemicals Division (Pharmorphix), 250 Cambridge _ Science Park, Milton Road, Cambridge Cambridgeshire CB4 OWE (GB). PEREZ, Lucia Romero; Johnson — Matthey Plc., Johnson Matthey Chemical Product, Or- = - chard Road, Royston, Hertfordshire SG8 5HE (GB). HAR- _ LACHER, Cornelius Stephan; Zihlackerstrasse 60, 4153 =_ Reinach (CH). JONES, Stewart; Mereo Biopharma Group plc, 4th Floor, 1 Cavendish Place, London, Greater London = W1G OQF (GB). Agent: GILL JENNINGS & EVERY LLP et al.; The (74) Broadgate Tower, 20 Primrose Street, London, Greater Lon- don EC2A 2ES (GB). = (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. Designated States (unless otherwise indicated, for every (84) = kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, — 1-1 01 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, IN 1 1 in ,—, ,-1 (54) Title: METHOD FOR PRODUCING A POLYMORPHIC FORM OF 3-[5-AMINO-4-(3- CYANOBENZOYL)-PYRA- 0 ZOL-1-YL]-N-CYCLOPROPYL-4-METHYLBENZAMIDE --.... , 1 (57) : This invention relates to a process for the preparation of Form A of 3-[5-amino-4-(3- cyanobenzoy1)-pyrazol-1-y1]-N- 0 cyclopropyl-4-methylbenzamide. Also disclosed herein is Form A of 345-amino-4-(3-cyanobenzoy1)-pyrazol-1-y1]-N-cyclopropy1-4- el methylbenzamide, or pharmaceutical compositions thereof, obtainable by the process described herein. C