Patent SG-11201903103V-A (SG)
Title: Dual inhibitors of vista and pd-1 pathways
Inventor: SASIKUMAR POTTAYIL GOVINDAN NAIR
IPC: C07D271/06
Filed: 2017-10-18
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 11111111111 0 1110101011111 011101 0 011111111 0011H11100111111111011110111111 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\" WO 2018/073754 Al 26 April 2018 (26.04.2018) WIP0 I PCT (51) International Patent Classification: C07D 271/06 (2006.01) Declarations under Rule 4.17: — as to applicant's entitlement to apply for and be granted a (21) International Application Number: patent (Rule 4.17(ii)) PCT/IB2017/056463 — of inventorship (Rule 4.17(iv)) (22) International Filing Date: Published: 18 October 2017 (18.10.2017) — with international search report (Art. 21(3)) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 201641035996 20 October 2016 (20.10.2016) IN (71) Applicant: AURIGENE DISCOVERY TECH- NOLOGIES LIMITED [IN/IN]; 39-40, KIADB Industri- al Area, Electronic City Phase II, Hosur Road, Karnataka, Bangalore 560100 (IN). (72) Inventors: SASIKUMAR, Pottayil Govindan Nair; # 5, Deccan Palms, Ananth Nagar Phase, II, Electronic city _ post, Bangalore 560100 (IN). RAMACHANDRA, Mu- ralidhara; V173, Adarsh Palm Retreat, Outer Ring, Road, — Bellandur Post, Bangalore 560103 (IN). NAREMADDE- = - PALLI, Seetharamaiah Setty Sudarshan; 33/A, Shen- _ imahathama temple compound, R., K. Layout, K. G. Nagar, = Bangalore 560019 (IN). — 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. (81) = = = = = — = = Designated States (unless otherwise indicated, for every (84) = 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). = _ 1-1 7r 11 in IN M IN © (54) Title: DUAL INHIBITORS OF VISTA AND PD-1 PATHWAYS --.... ,-1 (57) : The present disclosure relates to 3-substituted 1,2,4-oxadiazole compounds and their derivatives, which are useful as 0 V-domain immunoglobulin suppressor of T-cell activation (VISTA) inhibitors or as dual inhibitors of VISTA and the programmed \" cell death 1 (PD-1) signaling pathway. The disclosure also relates to treatment of disorders by inhibiting an immunosuppressive signal C) induced by VISTA and its ligands, PD-1, PD-L1, and/or PD-L2.