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The present invention provides novel paclitaxel
analogs, specifically 2", 3" side-chain halogenated
cephalomannine of the formula
Image
wherein,
I. (2"R,3"S)-dihalocephalomannine
Image
II. (2"S,3"R)-dihalocephalomannine
Image
III. (2"R,3"S)-dihalo-7-epi-cephalomannine
Image
IV. (2"S,3"R)-dihalo-7-epi-cephalomannine
Image
(2"y 3"S)-dihalocephalomannine
Image R1=H R2=OH
(2" R~3"R)-dihalocepha~omannine
R ' Image Rt=OH Ri=H
(2"'S~3"S)-dihalo-7-epi-cephalomannine
Rl-H RZnOH
Image
(2"R,3"R)-dihalo-7-epi-cephalomannine
R _ R~=H Ri=OH
Image
and X = halogen, which show strong in vitro and in vivo
paclitaxel-like efficacy in a variety of tumors.
Note: Data on abstracts and claims is shown in the official language in which it was submitted.
|
(30) Application Priority Data:
|
| Application No. |
Country |
Date |
| 08/571,427 |
United States |
1995-12-13 |
| 08/672,397 |
United States |
1996-05-29 |
| 08/654,424 |
United States |
1996-05-29 |
|
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