9-AMINOMETHYL MINOCYCLINE COMPOUNDS AND USE THEREOF IN TREATING COMMUNITY-ACQUIRED BACTERIAL PNEUMONIA (CABP)

摘要

T _ N T ---------- ------------- Oma dacy c line Concen tra t ion (µ g /m L) T ------ -- _ (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 11 May 2018 (11.05.2018) WIPO I PCT omit Ill °nolo III m Oil IIII iflo oimIE (10) International Publication Number WO 2018/085216 Al (51) International Patent Classification: A61K 31/65 (2006.01) A61P 31/04 (2006.01) CO7C 237/26 (2006.01) (21) International Application Number: PCT/US2017/059165 (22) International Filing Date: 31 October 2017 (31.10.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/416,010 01 November 2016 (01.11.2016) US 62/422,843 16 November 2016 (16.11.2016) US 62/480,516 02 April 2017 (02.04.2017) US 62/500,611 03 May 2017 (03.05.2017) US 62/514,415 02 June 2017 (02.06.2017) US (71) Applicant: PARATEK PHARMACEUTICALS, INC. [US/US]; 75 Park Plaza, 4th Floor, Boston, MA 02116 (US). (72) Inventors: TZANIS, Evangelos L.; 3906 White Stone Road, Newtown Square, PA 19073 (US). MCGOVERN, Paul; 2176 Buttonwood Road, Berwyn, PA 19312 (US). (74) Agent: HANLEY, Elizabeth A. et al.; Mccarter & English, LLP, 265 Franklin Street, Boston, MA 02110 (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). (54) Title: 9-AMINOMETHYL MINOCYCLINE COMPOUNDS AND USE THEREOF IN TREATING COMMUNITY-ACQUIRE BACTERIAL PNEUMONIA (CABP) Mean (± SD Concentrations of Omadacycline during the Bronchoscopy Sampling Times M -- # 1 Alveolar Cells 100 Ak---A Epithelial Lining Fluid *-6 Plasma 0.1 8 10 12 14 16 18 20 22 24 Time (hours FIG. 1-1 © (57) : The invention disclosed herein provides a method for treating Community- Acquired Bacterial Pneumonia (CABP) N using 9-[(2,2-dimethyl-propyl amino)-methyl] -minocycline or a salt thereof, in either oral or IV doses or a combination of both. [Continued on next page] C WO 2018/085216 Al MIDEDIMOMMIDEFIENIIMBEINHERVOIMIE 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))