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1. (WO2018068017) HETEROCYCLIC COMPOUNDS AS INHIBITORS OF RAS AND METHODS OF USE THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/068017 International Application No.: PCT/US2017/055656
Publication Date: 12.04.2018 International Filing Date: 06.10.2017
IPC:
C07D 401/04 (2006.01) ,C07D 403/04 (2006.01) ,C07D 403/14 (2006.01) ,C07D 471/04 (2006.01) ,C07D 487/04 (2006.01) ,A61K 31/4035 (2006.01) ,A61K 31/437 (2006.01) ,A61P 35/00 (2006.01) ,C07D 513/04 (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
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
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
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
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
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
435
having six-membered rings with one nitrogen as the only ring hetero atom
4353
ortho- or peri-condensed with heterocyclic ring systems
437
the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
513
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/, C07D477/232
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
Applicants: ARAXES PHARMA LLC[US/US]; 3033 Science Park Road, Suite 220 San Diego, California 92121, US
Inventors: WU, Tao; US
WANG, Yi; US
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:
62/405,70107.10.2016US
62/450,96626.01.2017US
Title (EN) HETEROCYCLIC COMPOUNDS AS INHIBITORS OF RAS AND METHODS OF USE THEREOF
(FR) COMPOSÉS HÉTÉROCYCLIQUES EN TANT QU'INHIBITEURS DE RAS 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, R", Q, W, X, Y, Z, n1, n2and '--" 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 disclosed.
(FR) La présente invention concerne des composés ayant une activité en tant qu'inhibiteurs de la protéine KRAS mutante G12C. Les composés ont la structure suivante (I) : ou un sel, stéréoisomère ou promédicament pharmaceutiquement acceptable de ceux-ci, dans laquelle A, B, R", Q, W, X, Y, Z, n 1 , n 2 et '--" sont tels que définis dans la description. L’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 mutante 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)