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2 238 278

(13)

(51)

IPC

(21) (22)

Application

98110369/04, 1998-06-01

(24)

Start date

1998-06-01

(22)

Actual filing date

1998-06-01

(45)

Published

2004-10-20

(72)

Inventor

Khattori KatsuoIshikava ToruIshitsuka KhideoKochi JasunoriOikava NobukhiroShimma NobuoSuda Khitomi

(73)

Holder

F.Khoffmann-Lja Rosh Ag

DERIVATIVES OF 5'-DEOXYCYTIDINE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF Russian patent published in 2004 - IPC

Abstract RU 2238278 C2

FIELD: organic chemistry, biochemistry, nucleosides, medicine.

SUBSTANCE: invention relates to derivatives of 5'-deoxycytidine of the general formula (I):

wherein R¹ means hydrogen atom or group that is hydrolyzed easily in physiological fluids; R² means hydrogen atom or group -CO-OR⁴ wherein R⁴ means saturated hydrocarbon group with direct or branched chain comprising from 1 to 15 carbon atoms, or group of the formula -(CH₂)_n-Y wherein Y means cyclohexyl or phenyl; n is a whole number from 0 to 4; R³ means hydrogen, bromine, iodine atom, cyano-group, (C₁-C₄)-alkyl group that can be substituted with halogen atom(s), vinyl or ethynyl group that can be substituted with halogen atom(s), (C₁-C₄)-alkyl under condition that R² and R³ can't mean hydrogen atom simultaneously. Compounds elicit an antitumor activity. Also, invention relates to pharmaceutical compositions used for treatment of tumor and containing a derivative of 5'-deoxycytidine as an active component being separately or in combination with 5-fluorouracil or its derivative.

EFFECT: valuable medicinal properties of compound and compositions.

7 cl, 3 tbl, 51 ex

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RU 2 238 278 C2

Authors

Khattori Katsuo

Ishikava Toru

Ishitsuka Khideo

Kochi Jasunori

Oikava Nobukhiro

Shimma Nobuo

Suda Khitomi

Dates

2004-10-20—Published

1998-06-01—Filed