Patent ID: 6545125
Filing Date: 2003-04-08
Classification: A61K,A61P,C07K

Abstract:
A compound which exhibits antitumor activity represented by the following formula (1) or a tautomer or a stereoisomer thereof:Xâ€”Lâ€”Yâ€ƒâ€ƒ(1) whereinX represents (i) paclitaxel or (ii) a derivative thereof selected from the group consisting of taxol derivatives having antitumor activity; L represents a linker having at least one functional group; and Y represents the formula wherein R represents â€”(CH2)4NH2, â€”(CH2)3NHCONH2, â€”(CH2)3NH (C&boxH;NH)NH2 or â€”(CH2)3NH2; or the formula wherein Z1 represents C(&boxH;O)NH or (E) CH&boxH;CH; Z2 represents C(&boxH;O)NH or (E) CH&boxH;CH; R1 represents H or a methyl group; R2 represents an isobutyl group or an isopropyl group; R3 represents H, an isobutyl group or a benzyl group; and R4 represents H or an isobutyl group; and * represents a bond to L.