Patent SG-11201808625Q-A (SG)
Title: SOLUBLE C5aR ANTAGONISTS
Inventor: FAN PINGCHEN
IPC: C07D211/60
Filed: 2017-04-03
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 11111111011110111010101111101011111011101011111110111010101101111101111011111 International Bureau .. .... ..Yejd (10) International Publication Number .... ..or::,,, (43) International Publication Date WO 2017/176620 A2 12 October 2017(12.10.2017) WIPO I PCT (51) International Patent Classification: (74) Agents: KEZER, William, B. et al.; Mintz Levin Cohn COIF 9/6558 (2006.01) C07D 211/60 (2006.01) Ferris Glovsky And Popeo, P. C., One Financial Center, Boston, MA 02111 (US). (21) International Application Number: PCT/US2017/025704 (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (22) International Filing Date: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, 3 April 2017 (03.04.2017) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, (25) Filing Language: English DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (26) Publication Language: English KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, (30) Priority Data: MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, 62/317,721 4 April 2016 (04.04.2016) US 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, (71) Applicant: CHEMOCENTRYX, INC. [US/US]; 850 TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, Maude Avenue, Mountain View, CA 94043 (US). ZA, ZM, ZW. (72) Inventors: FAN, Pingchen; 2157 Kalenda Commons, Fre- (84) Designated States (unless otherwise indicated, for every mont, CA 94024 (US). KRASINSKI, Antoni; 746 W. kind of regional protection available): ARIPO (BW, GH, Knickerbocker Drive, Sunnyvale, CA 94087 (US). MALI, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, Venkat, Reddy; 20875 Valley Green Drive, Apt. 87, Cu- TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, pertino, CA 95014 (US). MIAO, Shichang; 832 Arcturus TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, — Circle, Foster City, CA 94404 (US). PUNNA, Sreenivas; DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, 938 Fontana Terrace, Sunnyvale, CA 94085 (US). SONG, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, Yang; 750 Polaris Avenue, Foster City, CA 94404 (US). SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, STELLA, Valentino, J.; 1135 West Campus Road, GW, KM, ML, MR, NE, SN, TD, TG). — _ _ Lawrence, KS 66044 (US). ZENG, Yibin; 917 Aruba Published: Lane, Foster City, CA 94404 (US). ZHANG, Penglie; 1036 Jamaica Street, Foster City, CA 94404 (US). — without international search report and to be republished = = = upon receipt of that report (Rule 48.2(g)) = = = = = = = = (54) Title: SOLUBLE C5aR ANTAGONISTS = — Figure 1. Release of active compound 1.543 (from WO 2011/163640) from the compound of Example 22 (0.5 mg/kg mole equiv., AEC=I37 ng.h r/mL) 10000 Ri woo 1 CF 3 (I) © el 100 lo ... .. .._ IN 0 2 4 6 10 11 Tame thrl IN 1-1 (57) : Compounds are provided to modulate the C5a receptor. The compounds have the following Formula (I) including 0 stereoisomers and pharmaceutically acceptable salts thereof, wherein R I , R 2 and R 3 are as defined herein. Methods associated with \" preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.