http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CA-2147984-C

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filingDate 1993-11-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2006-03-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4f1074b147b81e656c179b92f1343a44
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f0c142c90b4c3d2847d5d073abbc8903
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6c8e566ba50ac89a272de9f1a9c20074
publicationDate 2006-03-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CA-2147984-C
titleOfInvention Butenyl-substituted taxanes and composition
abstract 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.
priorityDate 1992-11-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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