TAXANE DERIVATIVE PHOSPHONOOXYMETHYL ESTERS, INTERMEDIATE COMPOUNDS, ANTITUMOR PHARMACEUTICAL COMPOSITION, METHOD OF TUMOR GROWTH SUPPRESSION IN MAMMALS Russian patent published in 1999 - IPC

Abstract RU 2136673 C1

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to taxane derivative phosphonooxymethyl esters of the formula (I) where R1 - hydroxy-group, -OCH2(OCH2)mOP(O)(OH)2 or OC(O)ORx; R2′ - hydrogen atom; R2 - hydroxy-group, -OCH2(OCH2)mO-P(O)(OH)2′-OC(O)ORx; or R2′ - fluorine atom and R2 - hydrogen atom; R3 - H, hydroxy-, acetoxy-group; R4,R5 is C1-6-alkyl or Z-R6 where Z - a direct bond; R6′ - aryl or heteroaryl; Rx is C1-6-alkyl; p = 0 or 1; R6,R7 in common form oxo-group at condition that at least one of R1,R2 is OCH2(OCH2)mOP(O)(OH)2; m = 0 or 1, or their pharmaceutically acceptable salts that show antitumor activity. EFFECT: improved method of synthesis, antitumor activity of compounds. 54 cl, 5 tbl, 11 ex

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RU 2 136 673 C1

Authors

Erzhi Golik

Dolatraj Vias

Dzhon Dzh. Rajt

Genri Vong

Dzhon F.Kadou

Dzhon K.Totatil

Ven-Sen Li

Murrej A.Kaplan

Robert K.Perron

Dates

1999-09-10Published

1993-12-23Filed