C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 405/00 (2006.01) A61K 31/44 (2006.01) A61K 31/695 (2006.01) C07D 205/08 (2006.01) C07D 305/14 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01) C07D 409/14 (2006.01) C07F 7/10 (2006.01) C07F 7/18 (2006.01)
Patent
CA 2158863
Taxane derivatives having a pyridyl substituted C13 side- chain. The derivatives are of the formula: Image wherein X1 is -OX6, -SX7, or -NX8X9; X2 is hydrogen, C1-15 alkyl, C1-15 alkenyl, C1-15 alkynyl, C6-15 aryl, or C6-15 heteroaryl; X3 is hydrogen; X4 is pyridyl; X5 is -COX10, or -SO2X11; X6 is hydrogen, C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-is aryl, C6-15 heteroaryl, or a hydroxy protecting group; X7 is C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-15 aryl, C6-15 heteroaryl, or sulfhydryl protecting group; X8 is hydrogen, C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-15 aryl, C6-15 heteroaryl, or heterosubstituted C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-15 aryl or C6-15 heteroaryl; X9 is an amino protecting group; X10 is C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-15 aryl, C6-15 heteroaryl, t-butoxy, or heterosubstituted C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-15 aryl or C6-15 heteroaryl; X11 is C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-15 aryl, C6-15 heteroaryl, -OX10 or -NX8X14: X14 is hydrogen, C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-is aryl, or C6-15 heteroaryl; 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 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, C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-15 aryl, C6-15 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, C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-15 aryl, or C6-15 heteroaryl, hydroxy, protected hydroxy or together with R6a forms an oxo; R6a is hydrogen, C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-is aryl, or C6-is 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; R10 is hydrogen: R10a is -OCOR29, hydroxy, or protected hydroxy; R14 is hydrogen, C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-is aryl, Cg-15 heteroaryl, hydroxy, protected hydroxy or together with R1 forms a carbonate: R14a is hydrogen, C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, C6-15 aryl, or C6-15 heteroaryl; R29 and R30, are independently hydrogen, C1-15 alkyl, C1-15 alkenyl, C1-15 alkynyl, monocyclic C6-15 aryl or monocyclic C6-is heteroaryl; and R31 is hydrogen, C1-15 alkyl, C2-15 alkenyl, C2-15 alkynyl, phenyl or monocyclic C6-15 heteroaryl. The derivates are useful as antitumor and antileukemia agents.
xane derivatives having a pyridyl substituted C13 side-chain.
Holton Robert A.
Rengan Kasthuri
Florida State University
Smart & Biggar
LandOfFree
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