C - Chemistry – Metallurgy – 07 – D
Patent
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) C07C 227/22 (2006.01) C07C 231/12 (2006.01) C07C 233/87 (2006.01) C07D 205/08 (2006.01) C07D 205/085 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01) C07F 7/08 (2006.01) C07F 7/18 (2006.01)
Patent
CA 2147854
Taxane derivatives having an alkyl substituted C13 side-chain, having the following formula: Image wherein X1 is -OX6, -SX7, or -NX8X9; X2 is hydrogen, alkyl, alkenyl, alkynyl, aryl; or heteroaryl; X3 is optionally substituted alkyl; X4 is hydrogen; X5 is -COX10 or -SO2X11; X6 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, or a hydroxy protecting group; X5 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, monocyclic aryl or monocyclic heteroaryl; and R31 is hydrogen, alkyl, alkenyl, phenyl or monocyclic heteroaryl. The taxane derivatives of the present invention are useful as antileukemia and antitumor agents.
xane derivatives having an alkyl substituted C13 side-chain.
Chai Ki-Byung
Holton Robert A.
Idmoumaz Hamid
Nadizadeh Hossain
Suzuki Yukio
Florida State University
Smart & Biggar
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