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1. WO2020002487 - COMPOUNDS

Publication Number WO/2020/002487
Publication Date 02.01.2020
International Application No. PCT/EP2019/067111
International Filing Date 27.06.2019
IPC
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
12
in which the condensed system contains three hetero rings
14
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
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
541
Non-condensed thiazines containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C07D 471/14 (2006.01)
A61K 31/541 (2006.01)
A61P 35/00 (2006.01)
CPC
A61K 9/00
C07D 471/14
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 4070 Basel, CH (AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BE, BF, BG, BH, BJ, BN, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CL, CM, CN, CO, CR, CU, CY, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IR, IS, IT, JO, JP, KE, KG, KH, KM, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, ME, MG, MK, ML, MN, MR, MT, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SI, SK, SL, SM, SN, ST, SV, SY, SZ, TD, TG, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, ZA, ZM, ZW)
  • HOFFMANN-LA ROCHE INC. [US/US]; Overlook at Great Notch, 150 Clove Road 8th Floor, Suite 8 - Legal Department Little Falls, New Jersey 07424, US (US)
Inventors
  • DUPLESSIS, Martin; US
  • GOERGLER, Annick; CH
  • JAESCHKE, Georg; CH
  • KOCER, Buelent; CH
  • KUHN, Bernd; CH
  • LAZARSKI, Kiel; US
  • LIANG, Yanke; US
  • NAGEL, Yvonne Alice; CH
  • OBST SANDER, Ulrike; CH
  • RICCI, Antonio; CH
  • RUEHER, Daniel; CH
  • STEINER, Sandra; CH
Agents
  • BERNARD, Guillaume; CH
Priority Data
18180758.729.06.2018EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) COMPOUNDS
(FR) COMPOSÉS
Abstract
(EN)
The present invention provides compounds which are selective allosteric inhibitors of T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.
(FR)
La présente invention concerne des composés qui sont des inhibiteurs allostériques sélectifs De T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S contenant des mutants EGFR, leur fabrication, des compositions pharmaceutiques les contenant et leur utilisation en tant que substances thérapeutiquement actives.
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