Patent SG-11201907448R-A (SG)
Title: Macrocyclic broad spectrum antibiotics
Inventor: SMITH PETER
IPC: C07D245/04
Filed: 2018-02-22
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 0111111010 0111 °nolo Holum° mumionio oimIE (10) International Publication Number WO 2018/149419 Al (51) International Patent Classification: CO7D 245/04 (2006.01) A61P 31/04 (2006.01) A61K 31/395 (2006.01) (21) International Application Number: PCT/CN2018/076957 (22) International Filing Date: 22 February 2018 (22.02.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: PCT/CN2017/073575 15 February 2017 (15.02.2017) CN PCT/CN2017/085075 19 May 2017 (19.05.2017) CN (71) Applicants: RQX PHARMACEUTICALS, INC. [US/US]; 11099 N. Torrey Pines Road, Suite 290, La Jolla, CA 92037 (US). GENENTECH, INC. [US/US]; 1 DNA Way, South San Francisco, CA 94080 (US). (72) Inventors: SMITH, Peter, Andrew; 260 King Street Unit 909, San Francisco, CA 94107 (US). ROBERTS, Tuck- er, Curran; 536 Maple Street, Apt. 301, San Diego, CA 92103 (US). HIGUCHI, Robert, I.; 434 Marview Dri- ve, Solana Beach, CA 92075 (US). PARASELLI, Pra- suna; 6323 Oleander Way, San Diego, CA 92130 (US). KOEHLER, Michael, F., T.; 516 Georgia Avenue, Pa- lo Alto, CA 94306 (US). SCHWARZ, Jacob, Bradley; 7211 Balmoral Way, San Ramon, CA 94582 (US). CRAW- FORD, James, John; 1501 Church St #102, San Fran- cisco, CA 94131 (US). LY, Cuong Q.; 801 Maple Av- enue, Burlingame, CA 94010 (US). HANAN, Emily, J.; 1904 Woodside Road, Redwood City, CA 94061 (US). HU, Huiyong; 34121 Susa Terrace, Fremont, CA 94555 (US). CHEN, Yongsheng; 288 Fute Zhong Road, Waigao- qiao Free Trade Zone, Shanghai 200131 (CN). YU, Zhiy- ong; 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131 (CN). (74) Agent: AFD CHINA INTELLECTUAL PROPERTY LAW OFFICE; Suite B 1601A, 8 Xue Qing Road, Haidi- an, Beijing 100192 (CN). (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). 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)) (54) Title: MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS (57) : Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.