Phosphonooxymethyl ethers of taxane derivatives
First Claim
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1. A compound having the formula ##STR113## wherein R1 is hydroxy, --OCH2 (OCH2)m OP(O)(OH)2, --OC(O)Rx or --OC(O)ORx ;
- R2'"'"' is hydrogen, and R2 is hydrogen, hydroxy, --OCH2 (OCH2)m OP(O)(OH)2, --OC(O)Rx or --OC(O)ORx ;
R3 is hydrogen, hydroxy, C1-6 alkyloxy, --OC(O)Rx, --OCH2 (OCH2)m OP(O)(OH)2 or --OC(O)ORx ;
one of R6 or R7 is hydrogen and the other is hydroxy, C1-6 alkanoyloxy, or --OCH2 (OCH2)m OP(O)(OH2);
or R6 and R7 together form an oxo group;
with the proviso that at least one of R1, R2, R3, R6 or R7 is --OCH2 (OCH2)m OP(O)(OH)2 ;
m is zero or an integer one to six inclusive;
R4 and R5 are independently C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or --Z--R6 ;
Z is a direct bond, C1-6 alkyl or C2-6 alkenyl;
R6 is aryl, substituted aryl, C3-6 cycloalkyl, or heteroaryl;
p is 0 or 1; and
Rx is C1-6 alkyl optionally substituted with one to six same or different halogen atoms, C3-6 cycloalkyl, C2-6 alkenyl or hydroxy;
or Rx is a radical of the formula ##STR114## wherein D is a bond or C1-6 alkyl; and
Ra, Rb and Rc are independently hydrogen, amino, C1-6 alkylamino, di-C1-6 alkylamino, halogen, C1-6 alkyl, or C1-6 alkoxy.
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Abstract
The present invention concerns antitumor compounds. More particularly, the invention provides novel taxane derivatives, pharmaceutical compositions thereof, and their use as antitumor agents.
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Citations
43 Claims
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1. A compound having the formula ##STR113## wherein R1 is hydroxy, --OCH2 (OCH2)m OP(O)(OH)2, --OC(O)Rx or --OC(O)ORx ;
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R2'"'"' is hydrogen, and R2 is hydrogen, hydroxy, --OCH2 (OCH2)m OP(O)(OH)2, --OC(O)Rx or --OC(O)ORx ; R3 is hydrogen, hydroxy, C1-6 alkyloxy, --OC(O)Rx, --OCH2 (OCH2)m OP(O)(OH)2 or --OC(O)ORx ; one of R6 or R7 is hydrogen and the other is hydroxy, C1-6 alkanoyloxy, or --OCH2 (OCH2)m OP(O)(OH2);
or R6 and R7 together form an oxo group;
with the proviso that at least one of R1, R2, R3, R6 or R7 is --OCH2 (OCH2)m OP(O)(OH)2 ;m is zero or an integer one to six inclusive; R4 and R5 are independently C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or --Z--R6 ; Z is a direct bond, C1-6 alkyl or C2-6 alkenyl; R6 is aryl, substituted aryl, C3-6 cycloalkyl, or heteroaryl; p is 0 or 1; and Rx is C1-6 alkyl optionally substituted with one to six same or different halogen atoms, C3-6 cycloalkyl, C2-6 alkenyl or hydroxy;
or Rx is a radical of the formula ##STR114## wherein D is a bond or C1-6 alkyl; and
Ra, Rb and Rc are independently hydrogen, amino, C1-6 alkylamino, di-C1-6 alkylamino, halogen, C1-6 alkyl, or C1-6 alkoxy. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43)
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Specification