C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 305/14 (2006.01) A61K 31/33 (2006.01) A61K 31/695 (2006.01) C07D 205/08 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01) C07F 7/10 (2006.01)
Patent
CA 2158862
Taxane derivatives having an alkoxy, alkenoxy or aryloxy substituted C13 side chain. The taxane derivative, in a broad sense, is a taxane derivative having the formula (see formula 3) wherein X1 is -OX6, -SX7, or -NX8X9; X2 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl; X3 and X4 are independently hydrogen, alkyl, alkenyl, alkynyl, or heteroaryl; X5 is -COOX10; 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 or aryl, provided that X10 is other than t-butyl; R1 is hydrogen, hydroxy, protected hydroxy or together with R14 forms a carbonate; R2 is hydrogen, hydroxy, -OCOR31 or together with R2a forms an oxo; R2a is hydrogen or taken together with R2 forms an oxo; 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, or together with R6a forms an oxo; R6a is hydrogen, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, or together with R6 forms an oxo; R7 is hydrogen or together with R7a forms an oxo; R7a is hydrogen, halogen, protected hydroxy, -OR28, or together with R7 forms an oxo; R9 together with R9a forms an oxo; R10 is hydrogen or together with R10a forms an oxo; R10a is hydrogen, -OCOR29, hydroxy, or protected hydroxy, or together with R10 forms an oxo; 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; R2a is hydrogen, acyl, or a hydroxy protecting group; and R29, R30, and R31 are independently hydrogen, alkyl, alkenyl, alkynyl, monocyclic aryl or monocyclic heteroaryl, provided, however, that when X10 is methyl or ethyl, at least one of said other X1 - X9, R1 - R6a, R7, R7a, R9, R9a, R10, R10a, R14, R14a, and R28 to R31 has a value such that the structure of the taxane is different from that of taxotere.TM.. The taxane derivatives are antileukemia and antitumor agents.
Chai Ki-Byung
Holton Robert A.
Idmoumaz Hamid
Nadizadeh Hossain
Rengan Kasthuri
Florida State University
Smart & Biggar
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