Patent SG-11201407591P-A (SG)
Title: Process of making hydroxylated cyclopentapyrimidine compounds and salts thereof
Inventor: BABU SRINIVASAN
IPC: C12P17/16
Filed: 2013-05-17
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 21 November 2013 (21.11.2013) WIPOIPCT (10) International Publication Number WO 2013/173784 A1 (51) International Patent Classification: C12P17/16 (2006.01) C07D 403/04 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2013/041695 17 May 2013 (17.05.2013) English English (30) Priority Data: 61/648,535 17 May 2012 (17.05.2012) US (71) Applicant: GENENTECH, INC. [US/US]; 1 DNA Way, South San Francisco, California 94080-4990 (US). (72) Inventors: BABU, Srinivasan; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080-4990 (US). GOSSELIN, Francis; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080-4990 (US). RAN, Yingqing; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080-4990 (US). RE- MARCHUK, Travis; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080-4990 (US). SAV­ AGE, Scott J.; c/o Genentech, Inc., 1 DNA Way, South San Francisco, California 94080-4990 (US). STULTS, Jeffrey; c/o Genentech, Inc., DNA Way, 1 South San Fran­ cisco, California 94080-4990 (US). YAJIMA, Herbert; c/o Genentech, Inc., 1 DNA Way, South San Francisco, — California 94080-4990 (US). (74) Agents: MALEN, Peter L. et al.; Viksnins Harris & Padys PLLP, 7900 International Drive, Suite 670, Bloomington, Minnesota 55425 (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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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, 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, 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, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: — of inventorship (Rule 4.17(iv)) 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)) •t 00 l> m i> i-H o CJ (54) Title: PROCESS OF MAKING HYDROXYLATED CYCLOPENTAPYRIMIDINE COMPOUNDS AND SALTS THEREOF (57) Abstract: The invention provides new processes for making and purifying salts of hydroxylated cyclopentapyrimidine com­ pounds, which are useful as AKT inhibitors used in the treatment of diseases such as cancer, including the monohydrochloride salt of (S)-2-(4-chlorophenyl)-1 -(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1 -yl)-3-(isop- ropylamino)propan-1 -one.