Patent SG-11201906922T-A (SG)
Title: Processes for preparing ag-10, its intermediates, and salts thereof
Inventor: CHAND POORAN
IPC: A61P13/12
Filed: 2018-02-16
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 23 August 2018 (23.08.2018) WIP0 I PCT omit Ill °nolo onm ono oimIE (10) International Publication Number WO 2018/151815 Al (51) International Patent Classification: A61K 31/415 (2006.01) A61P 17/06 (2006.01) A61P 13/12 (2006.01) (21) International Application Number: PCT/US2018/000025 (22) International Filing Date: 16 February 2018 (16.02.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/460,576 17 February 2017 (17.02.2017) US (71) Applicant: EIDOS THERAPEUTICS, INC. [US/US]; 101 Montgomery Street, 25th Floor, San Francisco, CA 94104 (US). (72) Inventors: CHAND, Pooran; 101 Montgomery Street, 25th Floor, San Francisco, CA 94104 (US). GUPTA, Yo- gesh, Kumar; 101 Montgomery Street, 25th Floor, San Francisco, CA 94104 (US). KUMAWAT, Rakesh, Ku- mar; 101 Montgomery Street, 25th Floor, San Francisco, CA 94104 (US). ALHAMADSHEH, Mamoun; 101 Mont- gomery Street, 25th Floor, San Francisco, CA 94104 (US). ZAMBONI, Robert; 101 Montgomery Street, 25th Floor, San Francisco, CA 94104 (US). (74) Agent: KEZER, William B. et al.; Mintz Levin Cohn Fer- ris Glovsky Popeo, P.C., One Financial Center, Boston, MA 02111 (US). (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, (54) Title: PROCESSES FOR PREPARING AG-10, ITS INTERMEDIATES, AND SALTS THEREOF 0 0 K 2 CO 3 +Br'' . \"-\"Br Acetone HO N 2 H. I _H 2 0 HN Ethanol IV— PBr 3 HN OH 0 ' I N— Br+ COOMe OH Vila IN/ Vla 1-1 to 1-1 00 1-1 In 1-1 00 1-1 O DMF K 2 CO 3 COOH COOMe 4 Methanol IX Villa FIG. 1 (57) : Provided herein are improved processes for the preparation of a compound of Formula IX (AG- 10). Also provided herein are pharmaceutically acceptable salts of Formula (I) and Formula (lb) as well as crystalline types of Formula IX (AG- 10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification. [Continued on next page] LiOH WO 2018/151815 Al MIDEDIMOMOIDEIREE3110111HOHOMEEN 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)) before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h))