ANTITUMOUR AGENT INTENSIFIER Russian patent published in 2015 - IPC C07D239/54 C07D405/12 A61K31/513 A61P35/00 A61P35/02 A61P43/00 

Abstract RU 2548913 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a new intensifier of the antitumour effect, which is a uracil derivative of the general formula (I) or its pharmaceutically acceptable salt. In the general formula (I) X represents a C1-5-alkylene group, and wherein one of methylene groups making an alkylene group is optionally substituted by an oxygen atom; R1 represents a hydrogen atom or a C1-6-alkyl group; R2 represents a hydrogen atom or a halogen atom; and R3 represents a C1-6-alkyl group, C2-6-alkenyl group, C3-6-cycloalkyl group, (C3-6-cycloalkyl)-C1-6-alkyl group, halogen-C1-6-alkyl group or a 5-6-merous saturated heterocyclic group with an oxygen atom as a heteroatom, a uracil derivative presented by the following formula (I). The invention also refers to a method for potentiating the antitumour action or a method of treating tumours, involving administering an effective amount of a combination of the above uracil derivative or its pharmaceutically acceptable salt and an antimetabolite in an effective amount. The antimetabolite represents an agent specified in 5-fluoruracil (5-FU), potassium tegafur/gimeracil/oteracil (TS-1), tegafur/uracil (UFT), capecitabin, 5-fluor-2'-deoxyuridine (FdUrd) and Pemetrexed.

EFFECT: preparing the intensifier of the antitumour effect.

18 cl, 10 dwg, 10 tbl, 67 ex

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RU 2 548 913 C2

Authors

Fukuoka Masaesi

Jokogava Tatsusi

Mijakhara Seidzi

Mijakosi Khitosi

Jano Vakako

Taguti Dzunko

Takao Jajoi

Dates

2015-04-20Published

2010-11-29Filed