Patent SG-11201901999X-A (SG)
Title: Crystalline forms of a lysyl oxidase-like 2 inhibitor and methods of making
Inventor: LONERGAN DAVID
IPC: C07D401/12
Filed: 2017-09-06
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1#11101111 0 11101 HOE 3E1 0 011101111H 1110 11111 00 11110 1111 MI Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/048943 Al 15 March 2018 (15.03.2018) WIP0 I PCT (51) International Patent Classification: (74) Agent: ZUNIC, Valentin B.; Wilson Sonsini Goodrich & C07D 401/12 (2006.01) A61K 31/4439 (2006.01) Rosati, 650 Page Mill Road, Palo Alto, California 94304 (21) International Application Number: (US). PCT/US2017/050332 (81) Designated States (unless otherwise indicated, for every (22) International Filing Date: kind of national protection available): AE, AG, AL, AM, 06 September 2017 (06.09.2017) 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, (25) Filing Language: English DZ, EC, EE, EG, ES, F1, GB, GD, GE, GH, GM, GT, HN, (26) Publication Language: English 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, (30) Priority Data: MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, 62/384,596 07 September 2016 (07.09.2016) US 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, (71) Applicant: PHARMAKEA, INC. [US/US]; 3030 Bunker TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. Hill Street, Suite 300, San Diego, California 92109 (US). (84) Designated States (unless otherwise indicated, for every (72) Inventors: LONERGAN, David; 307 N Rios Ave., Solana kind of regional protection available): ARIPO (BW, GH, Beach, California 92075 (US). HOLME, Kevin Ross; GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, 13644 Landfair Road, San Diego, California 92130 (US). UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, ROWBOTTOM, Martin W.; 8389 Reagan Glen, San TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, Diego, California 92127 (US). — EE, ES, F1, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, = (54) Title: CRYSTALLINE FORMS OF A LYSYL = = = = = = = = _ _ = 1-1 OXIDASE-LIKE 2 INHIBITOR XRPD ./ of Ii FIGURE Compound , 1 2, Form AND 1 METHODS OF MAKING Lk) ‘, 1 c 7 9 9 10 „ 12 13 10 1„6 1„0 19 „ 21 22 23 24 25 2C 27 20 e9 en 2-Theta Scale 11' ER/M-1749-63-14 C:7 GC 7r c: : :: , (57) : Described herein are crystalline forms of pharmaceutically acceptable salts of the 1ysy1 oxidase-like 2 (LOXL2) in- -- --- GC hibitor (3-(4-(aminomethyl)-6-(trifluoromethyppyridin-2-yloxy)phenyl)((3R,4R)-3-fluoro-4-hydroxypyrrolidin-1-y1)methanone. Also ,—I described are methods of making the LOXL2 inhibitor, pharmaceutical compositions and medicaments comprising the LOXL2 in- CZ hibitor, and methods of using the LOXL2 inhibitor in the treatment of conditions, diseases, or disorders associated with LOXL2 activity. ei C [Continued on next page] WO 2018/048943 Al MIDEDIMOMOIDEIREEMOOVIVEIMOIMIDOMEHOIS 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(11)) — 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))