Patent SG-11201909615Y-A (SG)
Title: Salt of an aminopyridine derivative compound, a crystalline form thereof, and a process for preparing the same
Inventor: OH SANG HO
IPC: C07D413/14
Filed: 2018-04-18
Abstract: O O (12) 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 oimitia °nolo Oil mum iflo oimIE (10) International Publication Number WO 2018/194356 Al (51) International Patent Classification: CO7D 413/14 (2006.01) A61K 31/5377 (2006.01) (21) International Application Number: PCT/KR2018/004473 (22) International Filing Date: 18 April 2018 (18.04.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 10-2017-0051687 21 April 2017 (21.04.2017) KR (71) Applicant: YUHAN CORPORATION [KR/KR]; 74, No- ryangjin-ro, Dongjak-gu, Seoul 06927 (KR). (72) Inventors: OH, Sang Ho; 967-2004, 6, Gosan-ro 539beon- gil, Gunpo-si, Gyeonggi-do 15821 (KR). KIM, Jong Gyun; 102-1302, 44, Podowon-ro 27beon-gil, Don- gan-gu, Anyang-si, Gyeonggi-do 14128 (KR). OH, Se- Woong; 120-1201, 85, Hwasan-ro, Jangan-gu, Suwon-si, Gyeonggi-do 16420 (KR). HAN, Tae Dong; 103-1601, 1842, Yonggu-daero, Giheung-gu, Yongin-si, Gyeonggi-do 17080 (KR). CHUNG, Soo Yong; 1401-1003, 19, Dong- tandaerosibeom-gil, Hwaseong-si, Gyeonggi-do 18477 (KR). LEE, Seong Ran; 326-902, 132, Cheongmyeong- ro, Yeongtong-gu, Suwon-si, Gyeonggi-do 16707 (KR). KIM, Kyeong Bae; 410-404, 45, Jagok-ro 3-gil, Gang- nam-gu, Seoul 06374 (KR). LEE, Young Sung; 103-603, 107, Seoun-ro, Seocho-gu, Seoul 06624 (KR). SHIN, Woo Seob; 542-802, 12, Maeyeong-ro 310beon-gil, Yeong- tong-gu, Suwon-si, Gyeonggi-do 16697 (KR). JU, Hyun; 403-802, 55, Dongtansunhwan-daero 26-gil, Hwaseong-si, Gyeonggi-do 18466 (KR). KANG, Jeong Ki; 8409-202, 46-23, Wellbeing town-ro 36beon-gil, Yeongtong-gu, Su- won-si, Gyeonggi-do 16223 (KR). PARK, Su Min; 108-401, 64, Gagyeong-ro, Heungdeok-gu, Cheongju-si, Chungcheongbuk-do 28408 (KR). KIM, Dong Kyun; 402-ho, 51-16, Sangbong-gil, Bongdam-eup, Hwaseong-si, Gyeonggi-do 18316 (KR). (74) Agent: FIRSTLAW P.C.; 60 Mabang-Ro, Seocho-Ku, Seoul 06775 (KR). (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, 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, (54) Title: SALT OF AN AMINOPYRIDINE DERIVATIVE COMPOUND, A CRYSTALLINE FORM THEREOF, AND A PRO- CESS FOR PREPARING THE SAME O 9000 8000 7000 6000 5000 4000 :3000 2000 1000 - c7.1 II 2-Theta-Scale (57) : The present invention relates to novel mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyra- zol-1-yppyrimidine-2-ylamino)-4-methoxy-2-morpholinophenypacrylamide, a novel crystalline form thereof, and a process for preparing the same. More specifically, the present invention relates to mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phe ny1-1H-pyrazol-1-y1)pyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, which is excellent in stability, solubility, and bioavailability when it is administered not only alone but also in combination with other drugs and which has a high purity, a crystalline form thereof, and a process for preparing the same. [Continued on next page] WO 2018/194356 Al MIDEDIMOMOIDEIREEMOMOHMOIMIOMMOIMMIS 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). Published: — with international search report (Art. 21(3))