Taxanes having furyl or thienyl substituted side-chain

Details Taxanes having furyl or thienyl substituted side-chain Taxanes having furyl or thienyl substituted side-chain

C - Chemistry, Metallurgy

07

D

C07D 305/14 (2006.01) A61K 31/337 (2006.01) A61K 31/341 (2006.01) A61K 31/381 (2006.01) C07D 205/08 (2006.01) C07D 405/12 (2006.01) C07D 407/00 (2006.01) C07D 407/12 (2006.01) C07D 409/00 (2006.01) C07D 409/12 (2006.01) C07D 413/14 (2006.01) C07F 7/08 (2006.01)

Patent

CA 2158454

Taxane derivatives having a C13 side chain which includes a furyl or thienyl substituent of the formula: (see above formula) wherein X1 is -OX6, -SX-7, or -NX8X9; X2 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; X3 is furyl or thienyl; X4 is hydrogen; X5 is -COX10, or -SO2X11; X6 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, or a 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; R14 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, hydroxy, protected hydroxy or together with R1 forms a carbonate; R14a is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; R10 is hydrogen; R10a is -OCOR29, hydroxy, or protected hydroxy; R9 together with R9a forms an oxo; R9a together with R9 forms an oxo; R7a is hydrogen or together with R7 forms an oxo; R7 is hydroxy, or together with R7a forms an oxo; R6 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, or together with R6a forms an oxo; R6a is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, or together with R6 forms an oxo; 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; R4 is hydrogen, together with R4a forms an oxo, 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; R2 is hydrogen, hydroxy, or -OCOR31; R2a is hydrogen or taken together with R2 forms an oxo; R1 is hydrogen, hydroxy, protected hydroxy; R29 and R30 are independently hydrogen, alkyl, alkenyl, alkynyl, monocyclic aryl or monocyclic heteroaryl; and R31 is hydrogen, alkyl, alkenyl, alkynyl, phenyl or monocyclic heteroaryl; provided, however, R7 together with R7a forms an oxo; R4a is hydrogen, alkyl, alkenyl alkynyl, aryl, heteroaryl, cyano, hydroxy, -OCOR30 wherein R30 is other than methyl, or together with R4 forms an oxo, oxirane or methylene; R2 is hydrogen, hydroxy, or -OCOR31 wherein R31 is other than phenyl; R1 is other than hydroxy or R14 is other than hydrogen. The taxane derivatives may be used as antileukemia and antitumor agents.

xane derivatives having a C13 side chain which includes a furyl or thienyl substituent.

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