Patent SG-11201908619T-A (SG)
Title: Pd-1/pd-l1 inhibitors
Inventor: AKTOUDIANAKIS EVANGELOS
IPC: C07D241/20
Filed: 2018-04-19
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 IIl °nolo oimIE (10) International Publication Number WO 2018/195321 Al (51) International Patent Classification: C07D 405/14 (2006.01) CO7D 519/00 (2006.01) A61K 31/497 (2006.01) A61P 35/00 (2006.01) CO7D 403/14 (2006.01) CO7D 401/14 (2006.01) CO7D 241/18 (2006.01) CO7D 401/04 (2006.01) CO7D 241/20 (2006.01) CO7D 498/04 (2006.01) CO7D 487/08 (2006.01) CO7D 213/61 (2006.01) CO7D 487/10 (2006.01) CO7D 213/64 (2006.01) CO7D 491/107 (2006.01) (21) International Application Number: PCT/US2018/028382 (22) International Filing Date: 19 April 2018 (19.04.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/488,017 20 April 2017 (20.04.2017) US 62/507,678 17 May 2017 (17.05.2017) US (71) Applicant: GILEAD SCIENCES, INC. [US/US]; 333 Lakeside Drive, Foster City, California 94404 (US). (72) Inventors: AKTOUDIANAKIS, Evangelos; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). APPLEBY, Todd; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). CHO, Aesop; c/o Gilead Sciences, Inc., 333 Lakeside Dri- ve, Foster City, California 94404 (US). DU, Zhimin; c/ o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). GRAUPE, Michael; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). GUERRERO, Juan A.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). JABRI, Salman Y.; 870 Harrison St., Unit 404, San Francisco, California 94107 (US). LAD, Lateshku- mar Thakorlal; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). MACHICAO TELLO, Paulo A.; c/o Gilead Sciences, Inc., 333 Lake- side Drive, Foster City, California 94404 (US). MEDLEY, Jonathan William; c/o Gilead Sciences, Inc., 333 Lake- side Drive, Foster City, California 94404 (US). METO- BO, Samuel E.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). MUKHERJEE, Declarations under Rule 4.17: Prasenjit Kumar; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). NADUTHAM- 1-1 BI, Devan; c/o Gilead Sciences, Inc., 333 Lakeside Dri- ve, Foster City, California 94404 (US). NOTTE, Grego- ry; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). PARKHILL, Eric Q.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, Cal- (54) Title: PD-1/PD-L1 INHIBITORS ifornia 94404 (US). PHILLIPS, Barton W.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). SIMONOVICH, Scott Preston; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, Califor- nia 94404 (US). SQUIRES, Neil H.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). VENKATARAMANI, Chandrasekar; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). WANG, Peiyuan; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). WATKINS, William J.; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). XU, Jie; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, California 94404 (US). YANG, Kin Shing; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, Califor- nia 94404 (US). ZIEBENHAUS, Christopher Allen; c/o Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, Cal- ifornia 94404 (US). (74) Agent: TANNER, Lorna L. et al.; SHEPPARD MULLIN RICHTER & HAMPTON, 379 Lytton Avenue, Palo Alto, California 94301-1479 (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). as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) 1-1 © (57) : Compounds according to formula (I), methods of using said compounds singly or in combination with additional agents N and compositions of said compounds for the treatment of cancer are disclosed. O [Continued on next page] WO 2018/195321 Al IIMEDIMOM0101011EFIEDERIMEIIIMOVOIllii0VOIMIE 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))