Patent SG-11201909418W-A (SG)
Title: Small molecule inhibitors of bcl-2-associated death promoter (bad) phosphorylation
Inventor: LOBIE PETER EDWARD
IPC: C07D241/04
Filed: 2018-04-18
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 25 October 2018 (25.10.2018) WIPO I PCT omit VIII °nolo VIII VIII 11011111° oimIE (10) International Publication Number WO 2018/194520 Al (51) International Patent Classification: CO7D 211/06 (2006.01) A61K 31/496 (2006.01) CO7D 241/04 (2006.01) A61P 35/00 (2006.01) A61K 31/445 (2006.01) (21) International Application Number: PCT/SG2018/050194 (22) International Filing Date: Central College Campus, Palace Road, Bangalore 560001 (IN). (74) Agent: AMICA LAW LLC; 30 Raffles Place, #14-01 Chevron House, Singapore 048622 (SG). (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). Declarations under Rule 4.17: — of inventorship (Rule 4.17(iv)) Published: — with international search report (Art. 21(3)) — in black and white; the international application as filed contained color or greyscale and is available for download from PATENTSCOPE 18 April 2018 (18.04.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 1706162.3 19 April 2017 (19.04.2017) GB (71) Applicants: NATIONAL UNIVERSITY OF SINGA- PORE [SG/SG]; 21 Lower Kent Ridge Road, Singa- pore 119077 (SG). UNIVERSITY OF MYSORE [IN/IN]; Manasagangotri, Mysore 570006 (IN). BANGALORE UNIVERSITY [IN/IN]; Central College Campus, Palace Road, Bangalore 560001 (IN). = (72) Inventors: LOBIE, Peter Edward; c/o National Uni- versity of Singapore, Cancer Science Institute of Sin- gapore, 21 Lower Kent Ridge Road, Singapore 119077 (SG). PANDEY, Vijay Kumar; c/o National Universi- ty of Singapore, Cancer Science Institute of Singapore, 21 Lower Kent Ridge Road, Singapore 119077 (SG). KANCHUGARAKOPPAL SUBBEGOWDA, Rangap- pa; c/o University of Mysore, Department of Stud- ies in Chemistry, Manasagangotri, Mysore 570006 (IN). SALUNDI, Bassappa; c/o Bangalore University, Depart- ment of Chemistry, Central College Campus, Palace Road, Bangalore 560001 (IN). CHAKRABHAVI DHANAN- JAYA, Mohan; c/o University of Mysore, Department of Studies in Chemistry, Manasagangotri, Mysore 570006 (IN). RANGAPPA, Shobith; c/o University of Mysore, Department of Studies in Chemistry, Manasagangotri, Mysore 570006 (IN). VENKATACHALAIAH, Srini- vasa; c/o Bangalore University, Department of Chemistry, W O 20 18/ 19 45 20 Al (54) Title: SMALL MOLECULE INHIBITORS OF BCL-2-ASSOCIATED DEATH PROMOTER (BAD) PHOSPHORYLATION Rza R2b (R 1 ) n (57) : The invention relates to compounds of general formula (I): wherein R 1 , n, R 2a , R 2b , and R 3 are as defined herein. The compounds are inhibitors of Bc1-2-associated death promoter (BAD) phosphorylation and have anti-apoptotic activity and are useful in the treatment of cancer, particularly breast cancer, endometrial cancer, ovarian cancer, liver cancer, colon cancer, prostate cancer or pancreatic cancer.