Patent SG-11201811140U-A (SG)
Title: Purified cenicriviroc and purified intermediates for making cenicriviroc
Inventor: MORRA NICHOLAS
IPC: A61K31/395
Filed: 2017-06-21
Abstract: FIGo r- 0.1 ,— 0, NON , E CO , C, 0 CO 0 CO CO CO .3 , CV , NCO CO 0 .0 0 0 CV CV 0 0 CO Li, CO CV 0, 0. 0 0 0 CO CO C, 0 0, 0, c 0 co oci r- r- r- cri 0 0 0 1 \/ CV CO CV LO CO CV 0 0 CO 0 CV 0, , LO LO , 0 P-- 0 0 0 0, O. 0 ,-- LI , 0 0 0 CO 0 CO 0 0, 0 CD , CD 0 0 0 0 CO CO 0 0 0 , 0 0 CV CV CO CO Lo co co cr, o -cr r- co CID 0 CV Lo •cr o co co o 0 , 1 0 00 CO r- Lo co co co Lo Lo Lo Lo Lo Lo o coo Lo Lo -cr -cr -cr co o o or or 7L i 0 0 0 0 0 0 0 0 0 0 or or (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 28 December 2017 (28.12.2017) WI P0 I PC T oimitia Holm o Hum! omonunom ois (10) International Publication Number WO 2017/223155 Al (51) International Patent Classification: A61K 31/395 (2006.01) A61K 31/403 (2006.01) (21) International Application Number: PCT/US2017/038460 (22) International Filing Date: 21 June 2017 (21.06.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/352,885 21 June 2016 (21.06.2016) US (71) Applicant: TOBIRA THERAPEUTICS, INC. [US/US]; 400 Interpace Parkway, Parsippany, New Jersey 07054 (US). (72) Inventors: MORRA, Nicholas; c/o Tobira Therapeutics, INC., 400 Interpace Parkway, Parsippany, New Jersey 07054 (US). PHIASIVONGSA, Pasit; c/o Tobira Thera- peutics, INC., 400 Interpace Parkway, Parsippany, New Jer- sey 07054 (US). (74) Agent: BLINKA, Thomas, A. et al.; 1299 Pennsylvania Avenue, N.W., Suite 700, Washington, District of Columbia 20004-2400 (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: PURIFIED CENICRIVIROC AND PURIFIED INTERMEDIATES FOR MAKING CENICRIVIROC Current Data Parameters NAME 1301.114-J28 EXPND 1 PRDCND 1 F2 - Acquisition Parameters Date 20120720 The 14.54 INSTNR aped PRDSND 5 NR ONP IN PULPRDO z930 TO 32768 SOLVENT CEDE NS DS 2 SNH 8278148 Hz FIDRES 0.252829 Hz AQ 1.9792372 sec RC 1024 DN 60 6.0 .400 use uses DE 0 s 1E 300.0 K D1 1.00000000 sec CHANNEL 11' NUC1 1H P1 820 uses PL1 -8.00 BO SF01 400.1324710 MHz F2 - Processing parameters SI 32768 SF 400.130000O MHz M/DM CN SSB LB 0.30 Hz SB 0 PC 1.00 10 NMA plot parameters CX 20.00 a RP 0.500 ppm F1 340110 Hz F2P 0.500 ppm F2 200.07 Hz PPMCK 0.4000 ppmics H2CK 150.05200 Hzics ) co Lc, 03 0 , 1 CD O -cr oci rs- CO Lf, CV 00 CC; -cr N ppm 8 7 6 5 0 (57) : The disclosure includes high purity compounds having CCR5 and/or CCR2 antagonism, or salts thereof, high purity \" intermediates thereto and processes for synthesizing the same. [Continued on next page] C WO 2017/223155 Al IMEDIMOMMIDIRMEMEEHOIIIIHMODEVOIS Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) 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))