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1. (WO2018140598) FUSED N-HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF
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Pub. No.: WO/2018/140598 International Application No.: PCT/US2018/015227
Publication Date: 02.08.2018 International Filing Date: 25.01.2018
IPC:
C07D 401/14 (2006.01) ,C07D 401/04 (2006.01) ,C07D 403/04 (2006.01) ,C07D 205/04 (2006.01) ,A61P 35/00 (2006.01) ,A61K 31/495 (2006.01) ,A61K 31/4035 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
205
Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
02
not condensed with other rings
04
having no double bonds between ring members or between ring members and non-ring members
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403
condensed with carbocyclic rings, e.g. carbazole
4035
Isoindoles, e.g. phthalimide
Applicants:
ARAXES PHARMA LLC [US/US]; 3033 Science Park Road, Suite 220 San Diego, California 92121, US
Inventors:
LI, Liansheng; US
FENG, Jun; US
LIU, Yuan; 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
EIDT, Chandra, E.; 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
CARTER, James, 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
LIGON, Toby, J.; US
FERRON, William, O., Jr.; US
Priority Data:
62/450,95326.01.2017US
Title (EN) FUSED N-HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF
(FR) COMPOSÉS N-HÉTÉROCYCLIQUES FUSIONNÉS ET LEURS PROCÉDÉS D'UTILISATION
Abstract:
(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, stereoisomer or prodrug thereof, wherein A, B, E, L1, Ra. Rb, Rc and ○ 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 en tant qu'inhibiteurs de la protéine KRAS portant la mutation G12C. Les composés de l'invention ont la structure suivante (I) ou un sel, stéréoisomère ou promédicament pharmaceutiquement acceptable de ceux-ci, dans laquelle A, B, E, L1, Ra, Rb, Rc et ○ sont tels que définis dans la description. L’invention concerne en outre des procédés associés à la préparation et à l'utilisation desdits 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.
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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, 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
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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)