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1. WO2020113071 - COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF CANCER

Publication Number WO/2020/113071
Publication Date 04.06.2020
International Application No. PCT/US2019/063702
International Filing Date 27.11.2019
IPC
C07D 471/10 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic 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
02in which the condensed system contains two hetero rings
10Spiro-condensed systems
C07D 487/10 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
10Spiro-condensed systems
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 471/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic 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 C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
10Spiro-condensed systems
C07D 487/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
10Spiro-condensed systems
Applicants
  • ARAXES PHARMA LLC [US]/[US]
Inventors
  • LIANSHENG, Li
  • LIU, Yuan
  • WU, Tao
  • REN, Pingda
  • LIU, Yi
Agents
  • HARWOOD, Eric, A.
  • OBEIDAT, Baha, A.
  • KUMABE, Blake, K.
  • SOLTANI, Bobby, B.
  • ZENTZ, Bradley, J.
  • SARGEANT, Brooke
  • QUIST, Brooke, W.
  • ROTH, Carol, J.
  • EIDT, Chandra, E.
  • WITTKOPP, Cristina, J.
  • O'BRIEN, Daniel
  • CARLSON, David, V.
  • STARK, Duncan
  • SUN, Eileen, S.
  • GERTZ, Glenda, A.
  • HAN, Hai
  • TALBERT, Hayley, J.
  • BARRETT, Jared, M.
  • MIXCO, Javier, M.
  • SAKOI, Jeffrey, M.
  • BAUNACH, Jeremiah, J.
  • ZHANG, Jianping
  • MORGAN, John, A.
  • WAKELEY, John, J.
  • COE, Justin, E.
  • HENCKEL, Karen, M.
  • HEFTER, Karl, A.
  • HERMANNS, Karl, R.
  • CLAYTON, Kenneth W.
  • MORGAN, Kevan, L.
  • COSTANZA, Kevin, S.
  • COOPER, Michael, P.
  • RUSYN, Paul
  • LIN, Qing
  • HALLER, Rachel, A.
  • IANNUCCI, Robert
  • TARLETON, E., Russell
  • WEBB, Samuel, E.
  • LIU, Shi
  • LEEK, Shoko, I.
  • ROSENMAN, Stephen, J.
  • LAWRENZ, Steven, D.
  • ABEDI, Syed
  • SHEWMAKE, Thomas, A.
  • BOLLER, Timothy, L.
  • LIGON, Toby, J.
  • CANTRELL, Tyler, C.
  • SAKOI, Zachary M.
Priority Data
62/773,08429.11.2018US
62/773,10429.11.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF CANCER
(FR) COMPOSÉS ET PROCÉDÉS D'UTILISATION ASSOCIÉS POUR LE TRAITEMENT DU CANCER
Abstract
(EN)
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (I) or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein A, B, R1, R3, L1, L2, L3, E, A1, A2, A3, A4, G1, G2,W, X, Y, Z, m1, m2, n1, and n2 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 présentant une activité en tant qu'inhibiteurs de la protéine KRAS portant la mutation G12C. Les composés ont la structure suivante (I) : (I) ou un sel pharmaceutiquement acceptable, un stéréoisomère, une forme isotopique ou un promédicament de ceux-ci, A, B, R1, R3, L1, L2, L3, E, A1, A2, A3, A4, G1, G2,W, X, Y, Z, m1, m2, n1 et n2 étant 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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