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1. WO2020198067 - PKM2 MODULATORS AND METHODS FOR THEIR USE

Publication Number WO/2020/198067
Publication Date 01.10.2020
International Application No. PCT/US2020/024035
International Filing Date 20.03.2020
IPC
C07D 231/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
14with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 231/16 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
14with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
16Halogen atoms or nitro radicals
C07D 231/38 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
14with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38Nitrogen atoms
CPC
C07D 231/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
14with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 231/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
14with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
16Halogen atoms or nitro radicals
C07D 231/38
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
14with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38Nitrogen atoms
Applicants
  • SUMITOMO DAINIPPON PHARMA ONCOLOGY, INC. [US]/[US]
Inventors
  • SIDDIQUI-JAIN, Adam
Agents
  • HALLER, Rachel, 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
  • CONLEE, David, C.
  • CARLSON, David, V.
  • CHEN, David, W.
  • STARK, Duncan
  • TARLETON, E., Russell
  • SUN, Eileen, S.
  • HARWOOD, Eric, A.
  • GERTZ, Glenda, A.
  • HAN, Hai
  • TALBERT, Hayley, J.
  • BARRETT, Jared, M.
  • MIXCO, Javier, M.
  • DANLEY, Jeffrey, E.
  • SAKOI, Jeffrey, M.
  • SEO, Jeong, Hee
  • 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.
  • BENDEMIRE, Paul, D.
  • LIN, Qing
  • IANNUCCI, Robert
  • WEBB, Samuel, E.
  • LIU
  • LEEK, Shoko, I.
  • ROSENMAN, Stephen, J.
  • LAWRENZ, Steven, D.
  • ABEDI, Syed
  • SHEWMAKE, Thomas, A.
  • BOLLER, Timothy, L.
  • CANTRELL, Tyler, C.
  • LI, Yiheng
  • SAKOI, Zachary, M.
Priority Data
62/822,70022.03.2019US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PKM2 MODULATORS AND METHODS FOR THEIR USE
(FR) MODULATEURS DE PKM2 ET LEURS PROCÉDÉS D'UTILISATION
Abstract
(EN)
Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I), including pharmaceutically acceptable salts, isotopic forms, tautomers and prodrugs thereof, wherein R1, R2, and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
(FR)
L'invention concerne des composés ayant une activité en tant qu'activateurs de PKM2. L'invention propose des composés de structure suivante (I), ainsi que des sels pharmaceutiquement acceptables, des formes isotopiques, des tautomères et des promédicaments de ceux-ci, R1, R2 et R3 étant tels que définis dans la description. L'invention concerne également des procédés associés à la préparation et à l'utilisation de tels composés, ainsi que des compositions pharmaceutiques comprenant de tels composés.
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