SELECTIVE EGFR MUTANT INHIBITOR WITH INSERTION IN EXON 20 Russian patent published in 2022 - IPC A61K31/519 A61P35/00 

Abstract RU 2774629 C2

FIELD: medicine.

SUBSTANCE: invention relates to a method for the treatment of a patient with malignant tumor expressing EGFR having a mutation with an insertion in exon 20, with a compound selected from a group consisting of: (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dighydropyrimido[5,4-b]indolysin-8-yl)acrylamide; (S)-N-(4-amino-6-methylene-5-(quinolin-3-yl)-7,8-dighydro-6H-pyrimido[5,4-b]pyrrolizin-7-yl)acrylamide; and (S,E)-N-(4-amino-6-methylene-5-(quinolin-3-yl)-7,8-dihydro-6H-pyrimido[5,4-b]pyrrolizin-7-yl)-3-chloracrylamide; and (R)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dighydropyrimido[5,4-b]indolysin-8-yl)-N-methylacrylamide or its salt. The use of the specified compound for the production of an antitumor agent for the treatment of a patient with malignant tumor expressing EGFR having a mutation with an insertion in exon 20 is also proposed.

EFFECT: obtaining a compound for the treatment of malignant tumor.

9 cl, 15 dwg, 8 tbl, 10 ex

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RU 2 774 629 C2

Authors

Miyadera, Kazutaka

Aoyagi, Yoshimi

Hasako, Shinichi

Dates

2022-06-21Published

2017-10-13Filed