Patent SG-11201903327P-A (SG)
Title: Crystalline forms of eravacycline
Inventor: LAFRANCE DANNY
IPC: A61P31/00
Filed: 2017-10-19
Abstract: WO 18/0757 67 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 26 April 2018 (26.04.2018) WIPO I PCT omit VIII °nolo III o IID 100 1111010 Imo oimIE (10) International Publication Number WO 2018/075767 Al (51) International Patent Classification: C07D 295/15 (2006.01) A61P 35/00 (2006.01) A61K 31/65 (2006.01) A61P 1/00 (2006.01) A61P 31/00 (2006.01) (21) International Application Number: PCT/US2017/057385 (22) International Filing Date: 19 October 2017 (19.10.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/410,230 19 October 2016 (19.10.2016) US (71) Applicant: TETRAPHASE PHARMACEUTICALS, INC. [US/US]; 480 Arsenal Street, Suite 110, Watertown, MA 02472 (US). (72) Inventors; and (71) Applicants: LAFRANCE, Danny [US/US]; 22A Welles- ley Ave., Natick, MA 01760 (US). HOGAN, Philip, C. [US/US]; 437 Washington St., Apt. 1, Brighton, MA 02135 (US). LIU, Yansheng [CN/US]; 8 Ginn Road, Winches- ter, MA 01890 (US). HE, Minsheng [US/US]; 34 Mar- land Street, Andover, MA 01810 (US). CHEN, Chi-Li [CN/US]; 11 Waban Street, Newton, MA 02458 (US). NIU, John [US/US]; 20 Reeves Road, Bedford, MA 01730 (US). (74) Agent: ABELLEIRA, Susan, M. et al.; Foley Hoag LLP, 155 Seapiort Boulevard, Boston, MA 02210-2600 (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, 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: — of inventorship (Rule 4.17(iv)) Published: — with international search report (Art. 2 I (3)) (54) Title: CRYSTALLINE FORMS OF ERAVACYCLINE S i'. ee_ H 3 C, N ,CH 3 OH sitions comprising crystalline forms of the bis-HCL salt of a compound repre- NH 2 sented by Structural Formula 1 described herein. The crystalline forms of the (57) : The invention relates to crystalline forms of the bis-HCI salt of a compound represented by Structural Formula 1, and pharmaceutical compo- bis-HCI salt of a compound of Structural Formula 1 and compositions com- OH 0 HO O 0 (1), prising the crystalline forms of the compound of Structural Formula 1 provid- ed herein, in particular, crystalline Form I, crystalline Form J, crystalline Form A, and crystalline Form B, or mixtures thereof, can be incorporated into phar- maceutical compositions, which can be used to treat various disorders. Also described herein are methods for preparing the crystalline forms (e.g., Forms I, J, B and A) of the bis-HCI salt of a compound represented by Structural Formula 1.