Patent SG-11201906223T-A (SG)
Title: Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer
Inventor: LANMAN BRIAN ALAN
IPC: A61K31/437
Filed: 2017-12-21
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 28 June 2018 (28.06.2018) WIPO I PCT omit VIII °nolo HE VIII ono X11 ois (10) International Publication Number WO 2018/119183 A2 (51) International Patent Classification: CO7D 275/04 (2006.01) CO7D 403/04 (2006.01) CO7D 417/04 (2006.01) A61K 31/428 (2006.01) CO7D 471/08 (2006.01) A61K 31/429 (2006.01) CO7D 513/04 (2006.01) A61K 31/437 (2006.01) CO7D 487/10 (2006.01) A61K 31/517 (2006.01) CO7D 487/04 (2006.01) A61K 31/519 (2006.01) CO7D 239/80 (2006.01) A61K 31/498 (2006.01) CO7D 471/04 (2006.01) A61K 31/4985 (2006.01) CO7D 401/04 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/US2017/067801 (22) International Filing Date: 21 December 2017 (21.12.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/438,334 22 December 2016 (22.12.2016) US (71) Applicant: AMGEN INC. [US/US]; One Amgen Center Drive, Thousand Oaks, California 91320-1799 (US). (72) Inventors: LANMAN, Brian Alan; 6000 De Soto Avenue #305, Woodland Hills, California 91367 (US). CEE, Victor J.; 2881 Capella Way, Thousand Oaks, California 91362 (US). PICKRELL, Alexander J.; 30948 Minute Man Way, Westlake Village, California 91361 (US). REED, An- thony B.; 3031 Charlotte Street, Newbury Park, Califor- nia 91320 (US). YANG, Kevin C.; 8871 Camino Real Av- enue, San Gabriel, California 91775 (US). KOPECKY, David John; 2420 14th Street, NW, Apt. 533, Washing- ton, District of Columbia 20009 (US). WANG, Hui-Ling; 822 Lynnmere Drive, Thousand Oaks, California 91360 (US). LOPEZ, Patricia; 5614 Le Sage Avenue, Wood- land Hills, California 91367 (US). ASHTON, Kate; 30948 Minute Man Way, Westlake Village, California 91361 (US). BOOKER, Shon; 15243 Camarillo Street, Sherman Oaks, California 91403 (US). TEGLEY, Christopher M.; 478 Thunderhead Street, Thousand Oaks, California 91360 (US). (74) Agent: REIDY, Joseph F.; M/S 35-1-B, Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320-1799 (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). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: without international search report and to be republished upon receipt of that report (Rule 48.2(g)) 1-1 O \" (57) : Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors 0 are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers. (54) Title: KRAS G12C INHIBITORS AND METHODS OF USING THE SAME