Patent SG-11201808163W-A (SG)
Title: 6-hydroxy-4-oxo-1,4-dihydropyrimidine-5-carboxamides as apj agonists
Inventor: PI ZULAN
IPC: C07D239/557
Filed: 2017-03-23
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 11M1111101110101011111 HO 1111101110111101111011001110110111110111011# International Bureau ... .... ..)d .... ..... (10) International Publication Number (43) International Publication Date WO 2017/165640 Al 28 September 2017 (28.09.2017) WIP0 I PCT (51) International Patent Classification: Rocky Hill Road, Pennington, New Jersey 08534 (US). CO7D 401/14 (2006.01) CO7D 417/14 (2006.01) LAWRENCE, R. Michael; c/o Bristol-Myers Squibb CO7D 401/06 (2006.01) CO7D 471/04 (2006.01) Company, 311 Pennington Rocky Hill Road, Pennington, CO7D 403/06 (2006.01) A61K 31/505 (2006.01) New Jersey 08534 (US). MENG, Wei; c/o Bristol-Myers C07D 403/14 (2006.01) A61K 31/506 (2006.01) Squibb Company, 311 Pennington Rocky Hill Road, Pen- C07D 239/557 (2006.01) A61P 35/00 (2006.01) nington, New Jersey 08534 (US). MYERS, Michael C.; c/o Bristol-Myers Squibb Company, 311 Pennington (21) International Application Number: Rocky Hill Road, Pennington, New Jersey 08534 (US). PCT/US2017/023801 PHILLIPS, Monique; c/o Bristol-Myers Squibb Com- (22) International Filing Date: pany, Route 206 and Province Line Road, Princeton, New 23 March 2017 (23.03.2017) Jersey 08543 (US). TORA, George 0.; c/o Bristol-Myers Squibb Company, 311 Pennington Rocky Hill Road, Pen- (25) Filing Language: English nington, New Jersey 08534 (US). ZHANG, Xiaojun; c/o (26) Publication Language: English Bristol-Myers Squibb Company, 311 Pennington Rocky Hill Road, Pennington, New Jersey 08534 (US). (30) Priority Data: 62/312,780 24 March 2016 (24.03.2016) US (74) Agents: LIU, Hong et al.; Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, New Jersey (71) Applicant: BRISTOL-MYERS SQUIBB COMPANY 08543 (US). [US/US]; Route 206 and Province Line Road, Princeton, New Jersey 08543 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (72) Inventors: PI, Zulan; c/o Bristol-Myers Squibb Company, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, — 311 Pennington Rocky Hill Road, Pennington, New Jersey BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, _ 08534 (US). BILDER, Donna M; c/o Bristol-Myers DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, Squibb Company, 311 Pennington Rocky Hill Road, Pen- HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, = nington, New Jersey 08534 (US). BRIGANCE, Robert KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, Paul; 28 Lakeside Drive, Levittown, Pennsylvania 19054 MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, = (US). FINLAY, Heather; c/o Bristol-Myers Squibb Com- NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, = pany, 311 Pennington Rocky Hill Road, Pennington, New RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, = Jersey 08534 (US). JIANG, Wen; c/o Bristol-Myers TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, = Squibb Company, 311 Pennington Rocky Hill Road, Pen- ZA, ZM, ZW. nington, New Jersey 08534 (US). JOHNSON, James A.; c/o Bristol-Myers Squibb Company, 311 Pennington (84) Designated States (unless otherwise indicated, for every = kind of regional protection available): ARIPO (BW, GH, = [Continued on next page] = (54) Title: 6-HYDROXY-4-0X0-1,4-DIHYDROPYRIMIDINE-5-CARBOXAMIDES = = = = = — R2 _ ,—, © 7r N A (alk)0.2 0 N I I I OH AS APJ AGONISTS NR 3 R 4 ir) 1— 1 IN 1-1 (57) : The present invention provides 0 and compositions comprising any of such \" ments. i ED compounds novel compounds. (R 1 )1-4 (I) of Formula (I) wherein all variables are as defined in the specification, These compounds are APJ agonists which may be used as medico - O WO 2017/165640 Al MIDEDIMOMOIDEIR010130HinlINIMEMOVOIMIE GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, — as to the applicant's entitlement to claim the priority of 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, — the earlier application (Rule 4.17(iii)) of inventorship (Rule 4.17(iv)) LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, Published: SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). — with international search report (Art. 21(3)) Declarations under Rule 4.17: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii))