NEW CYTOTOXIC MACROLIDES COMPRISING TRIS(OXAZOL), METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHODS FOR TREATMENT Russian patent published in 2003 - IPC

Abstract RU 2217433 C2

FIELD: organic chemistry, chemical technology, medicine, pharmacy. SUBSTANCE: invention relates to new cytotoxic macrolide compound of the formula (I) wherein X represents lower alkyl; R1 and R2 represent hydrogen atom or lower alkyl; R3a represents hydrogen atom; R3b represents compounds of the formula (II) or (III) or R3a and R3b in common represent oxygen atom; R4 represents hydrogen atom, hydroxy-group, lower alkoxy-group and so on; R5 represents hydrogen atom, carbamoyl and so on; R6a represents hydrogen atom; R6b represents hydroxy-group either R6a and R6b in common represent oxygen atom; R7 represents hydrogen atom and so on; R8 represents lower alkoxy- group and so on; Y1 represents hydrogen atom or methyl; Y2 represents hydrogen atom or Y1 and Y2 in common represent double bond being in definitions of groups of the formula (I) lower alkyl and lower alkyl fragment of lower alkanoyl or lower alkoxy-group means linear or branched alkyl group comprising 1-6 carbon atoms, such as methyl, ethyl and so on. Invention relates to method for treatment of mammals damaged with malignant tumor sensitive to compound of the formula (I) and involving administration to the damaged individual therapeutically effective dose of indicated compound or its pharmaceutical composition. Invention relates to pharmaceutical preparation eliciting antitumor effect containing compound of the formula (I) as an active component and a carrier. Invention relates to method for preparing compound of the formula (I) that involves treatment of the known Kabiramides taken among Kabiramide B or C with acid, respectively, in suitable solvent. Invention provides preparing new compound eliciting an antitumor effect. EFFECT: improved preparing method, valuable medicinal properties of macrolides. 10 cl, 1 tbl

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RU 2 217 433 C2

Authors

Khiga Tatsuo

Garsia Gravalos Dolores

Fernandes-Puehntes Khose Luis

Dates

2003-11-27Published

1999-01-27Filed