THERAPEUTIC COMBINATIONS CONTAINING RAF INHIBITOR AND ERK INHIBITOR Russian patent published in 2022 - IPC A61K31/505 A61K31/4965 A61K31/5377 A61K45/06 A61P35/00 

Abstract RU 2774612 C2

FIELD: medicine; pharmaceutics.

SUBSTANCE: group of inventions relates to the field of medicine and pharmaceutics, in particular for the treatment of KRAS-mutant non-small cell lung cancer (hereinafter – NSCLC), BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (hereinafter – CRC) and KRAS-mutant ovarian cancer. For this purpose, a pharmaceutical combination is developed, containing CRAF inhibitor, which is a compound A of N-(3-(2-(2- hydroxyethoxy)-6-morpholinopyridine-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide or its pharmaceutically acceptable salt, and ERK inhibitor, which is a compound B of 4-(3-amino-6-((1S,3S,4S)-3-fluoro-4-hydroxycyclohexyl)pyrazin-2-yl)-N-((S)-1-(3-bromo-5- fluorophenyl)-2-(methylamino)ethyl)-2-fluorobenzamide or its pharmaceutically acceptable salt. A pharmaceutical composition, the use of a pharmaceutical combination, and a treatment method are also disclosed.

EFFECT: group of inventions provides the creation of a combination of a compound A and a compound B, the combination of which will optimize the suppression of signal transmission by means of MAPK in KRAS- and BRAF-mutant NSCLC; this combination may also contribute to the prevention of occurrence of the resistance to a combination of BRAF and MEK (mitogen-activated protein kinase) inhibitors in BRAFV600E-mutant NSCLC.

12 cl, 3 dwg, 6 tbl, 6 ex

Similar patents RU2774612C2

Title Year Author Number
COMBINATION THERAPY 2018
  • Cooke, Vesselina
RU2815400C2
COMPOSITIONS BASED ON SHP2 INHIBITOR AND METHODS OF CANCER TREATMENT 2018
  • Nichols, Robert J.
  • Goldsmith, Mark A.
  • Schulze, Christopher
  • Smith, Jacqueline
  • Wildes, David E.
  • Kelsey, Stephen
  • Singh, Mallika
RU2805355C2
PHARMACEUTICAL COMBINATIONS 2017
  • Caponigro, Giordano
  • Cao, Zhu Alexander
RU2759669C2
PHARMACEUTICAL COMBINATIONS OF CDK4/6 INHIBITOR AND B-Raf INHIBITOR 2013
  • Kaponigro Dzhordano
  • Styuart Darrin
  • Kim Sunkiu
  • Loo Elis
  • Delech Skott
RU2685250C2
COMBINATIONS OF PI3K INHIBITOR AND MEK INHIBITOR 2010
  • Marshija Belvin
  • Ajris T. Chan'
  • Lori Fridman
  • Klaus P. Kheflikh
  • Dzhon Preskott
  • Dzheffri Uollin
RU2563193C2
DETERMINATION OF CELL SENSITIVITY TO TREATMENT WITH B-Raf INHIBITOR BY DETECTION OF K-ras MUTATION AND LEVELS OF RTK EXPRESSION 2010
  • Khatzivassiliu Dzhordzhija
  • Malek Shiva
RU2553379C2
NEW METHYLQUINAZOLINONE DERIVATIVES 2020
  • Dolente, Kozimo
  • Khyuings, Devid Stiven
  • Khuntsiker, Daniel
  • Krummenakher, Daniela
  • Pettatstsoni, Perdzhordzho Franchesko Tommazo
  • Vikhmann, Yurgen
RU2802968C1
MDM2 INHIBITORS AND COMBINATIONS THEREOF 2016
  • Halilovic, Ensar
  • Caponigro, Giordano
  • Horn-Spirohn, Thomas
  • Lehar, Joseph
RU2740091C2
COMBINATION OF (A) PHOSPHOINOSITIDE-3-KINASE INHIBITOR AND (B) Ras/Raf/Mek PATHAWAY MODULATOR 2009
  • Garsija-Ehcheverrija Karlos
  • Mera Sove-Mishel'
  • St'Juart Darrin
  • Vi S'Jusan
  • Frich Kristine
  • Nejdzhel Tobi
RU2508110C2
SYNERGISTIC COMBINATIONS OF PI3K- AND MEK-INHIBITORS 2012
  • Fritch Kristin
  • Khuan Sichzhun
  • Bem Markus
  • Di Tomazo Emmanyuell
  • Kosart Yan Gse
RU2607944C2

RU 2 774 612 C2

Authors

Caponigro, Giordano

Meyer, Matthew John

Cooke, Vesselina

Stuart, Darrin

Dates

2022-06-21Published

2017-09-18Filed