NEW DERIVATIVES OF PEG Russian patent published in 2019 - IPC C08G65/333 A61K47/50 A61K47/60 A61K31/337 A61K31/407 A61K31/496 A61K31/513 A61K31/7068 A61P35/00 

Abstract RU 2697551 C2

FIELD: chemistry.

SUBSTANCE: present invention refers to a compound of formula (1) or its pharmaceutically acceptable salt

,

where R1 is a single bond, -N(R3)(CH2)n1CO- or -N(R4)(CH2)n2N (R5)CO(CH2)n3CO- (where R3 is a hydrogen atom or an alkyl group having 1–6 carbon atoms; R4 and R5 are bonded together and represent an alkylene group having 1–4 carbon atoms; and n1, n2 and n3 are identical or different from each other, each being integer from 1 to 3); R2 is (2'-cyano-2'-deoxy-β-D-arabinofuranosyl) cytosine or a group of formulas (b), (d), (e) or (f)

, ,

(e), (f ),

where R15 is an alkyl group having 1–6 carbon atoms; and R16 represents a hydrogen atom or an alkanoyl group having 2–6 carbon atoms; m is equal to number from 10 to 1000; and arrow denotes binding point. Also disclosed are embodiments of using said compound, a drug and a pharmaceutical composition for treating a malignant tumour containing it, and a method of treating a malignant tumour with using it.

EFFECT: technical result is development of new therapeutic agent for malignant tumour, which is very safe, enables to reduce negative side effects, such as severe gastrointestinal toxicity or bone toxicity, has a stable anti-tumour effect and enables improving administration and administration frequency.

8 cl, 16 dwg, 7 tbl, 10 ex

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RU 2 697 551 C2

Authors

Fukushima, Masakazu

Eshima, Kiyoshi

Dates

2019-08-15Published

2015-12-03Filed