Butenyl-substituted taxanes and composition

Details Butenyl-substituted taxanes and composition Butenyl-substituted taxanes and composition

C - Chemistry, Metallurgy

07

D

C07D 305/14 (2006.01) A61K 31/335 (2006.01) A61K 31/337 (2006.01) A61K 31/34 (2006.01) A61P 35/00 (2006.01) A61P 35/02 (2006.01) C07C 229/38 (2006.01) C07C 311/00 (2006.01) C07C 323/26 (2006.01) C07D 205/08 (2006.01) C07D 205/085 (2006.01) C07D 305/10 (2006.01) C07D 307/68 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01) C07F 7/10 (2006.01) G01N 27/447 (2006.01)

Patent

CA 2147984

Taxane derivatives having a 3' butenyl substituted C13 side chain, having the following formula are disclosed: (see formula I) wherein X1 is -OX6, -SX7, or -NX8X9; X2 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; X3 is hydrogen; X4 is isobutenyl; X5 is -COX10, or -SO2X11; X6 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxy protecting group; X7 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or sulfhydryl protecting group; X8 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, or heterosubstituted alkyl, alkenyl, alkynyl, aryl or heteroaryl; X9 is an amino protecting group; X10 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, t-butoxy or heterosubstituted alkyl, alkenyl, alkynyl, aryl or heteroaryl; X11 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, -OX10, or -NX8X14; X14 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; R1 is hydrogen, hydroxy, protected hydroxy or together with R14 forms a carbonate; R2 is hydrogen, hydroxy, -OCOR31 together with R2a forms an oxo; R2a is hydrogen or taken together with R2 forms an oxo or; R4 is hydrogen, together with R4a forms an oxo, oxirane or methylene, or together with R5a and the carbon atoms to which they are attached form an oxetane ring; R4a is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyano, hydroxy, -OCOR30, or together with R4 forms an oxo, oxirane or methylene; R5 is hydrogen or together with R5a forms an oxo; R5a is hydrogen, hydroxy, protected hydroxy, acyloxy, together with R5 forms an oxo, or together with R4 and the carbon atoms to which they are attached form an oxetane ring; R6 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, hydroxy, protected hydroxy or together with R6a forms an oxo; R6a is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, hydroxy, protected hydroxy or together with R6 forms an oxo; R7 is hydrogen or together with R7a forms an oxo; R7a is halogen, hydroxy, or together with R7 forms an oxo; R9 together with R9a forms an oxo; R9a together with R9 forms an oxo; R10 is hydrogen; R10a is -OCOR29, hydroxy, or protected hydroxy; R14 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, hydroxy, protected hydroxy or together with R1 forms a carbonate; R14a is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; R29 and R30 are independently hydrogen, alkyl, alkenyl, alkynyl, monocylcic aryl or monocyclic heteroaryl; and R31 is hydrogen, alkyl, alkenyl, alkynyl, phenyl or monocyclic heteroaryl. The taxane derivatives of the present invention are useful as antileukemia and antitumor agents.

xane derivatives having a 3' butenyl substituted C13 side chain.

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