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1. (WO2017058792) INHIBITORS OF KRAS G12C MUTANT PROTEINS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2017/058792    International Application No.:    PCT/US2016/053957
Publication Date: 06.04.2017 International Filing Date: 27.09.2016
IPC:
C07D 413/14 (2006.01), C07D 403/04 (2006.01), C07D 403/14 (2006.01), C07D 417/14 (2006.01), A61K 31/40 (2006.01)
Applicants: ARAXES PHARMA LLC [US/US]; 3033 Science Park Road, Suite 220 San Diego, California 92121 (US)
Inventors: LI, Liansheng; (US).
FENG, Jun; (US).
LONG, Yun, Oliver; (US).
REN, Pingda; (US).
LIU, Yi; (US)
Agent: HARWOOD, Eric, A.; (US).
OBEIDAT, Baha, A.; (US).
KUMABE, Blake, K.; (US).
SOLTANI, Bobby, B.; (US).
SARGEANT, Brooke; (US).
QUIST, Brooke, W.; (US).
ROTH, Carol, J.; (US).
O'BRIEN, Daniel; (US).
CARLSON, David, V.; (US).
STARK, Duncan; (US).
TARLETON, E., Russell; (US).
SUN, Eileen, S.; (US).
ABRAMONTE, Frank; (US).
HAN, Hai; (US).
TALBERT, Hayley, J.; (US).
WHITE, James, A. D.; (US).
BARRETT, Jared, M.; (US).
PEPE, Jeffrey, C.; (US).
DANLEY, Jeffrey, E.; (US).
SAKOI, Jeffrey, M.; (US).
BAUNACH, Jeremiah, J.; (US).
KARLEN, John, R.; (US).
MORGAN, John, A.; (US).
WAKELEY, John, J.; (US).
COE, Justin, E.; (US).
HENCKEL, Karen, M.; (US).
HEFTER, Karl, A.; (US).
HERMANNS, Karl, R.; (US).
MORGAN, Kevan, L.; (US).
COSTANZA, Kevin, S.; (US).
LINFORD, Lorraine; (US).
COOPER, Michael, P.; (US).
RUSYN, Paul; (US).
LIN, Qing; (US).
HALLER, Rachel, A.; (US).
IANNUCCI, Robert; (US).
KOVELMAN, Robert, L.; (US).
WEBB, Samuel, E.; (US).
LEEK, Shoko, I.; (US).
ROSENMAN, Stephen, J.; (US).
ABEDI, Syed; (US).
SATAGAJ, Thomas, J.; (US).
BOLLER, Timothy, L.; (US).
FERRON, William, O., Jr.; (US)
Priority Data:
62/233,815 28.09.2015 US
Title (EN) INHIBITORS OF KRAS G12C MUTANT PROTEINS
(FR) INHIBITEURS DE PROTÉINES KRAS PORTANT LA MUTATION G12C
Abstract: front page image
(EN)Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein R1, R3a, R3b, R4a, R4b, G1, G2, G3, G4, m1, m2, m3, m4, L1, L2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
(FR)La présente invention concerne des composés ayant une activité d'inhibiteurs de la protéine KRAS portant la mutation G12C. Les composés ont la structure (I) suivante : ou un sel, un tautomère, un stéréoisomère ou un promédicament pharmaceutiquement acceptable de ceux-ci, dans lesquels R1, R3a, R3b, R4a, R4b, G1, G2, G3, G4, m1, m2, m3, m4, L1, L2 et E sont tels que définis dans le présent document. La présente invention concerne en outre des procédés associés à la préparation et à l'utilisation de ces composés, des compositions pharmaceutiques comprenant ces composés, et des procédés de modulation de l'activité de la protéine KRAS portant la mutation G12C pour le traitement de troubles tels que le cancer.
Designated States: 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, JP, KE, KG, 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.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)