Symbol of the Government of Canada

Canadian Patents Database

Patent Summary

(12) Patent: (11) CA 2210924
(54) English Title: PACLITAXEL ANALOGS, PREPARATION AND USE AS ANTITUMOR AGENTS
(54) French Title: ANALOGUES DU PACLITAXEL, LEUR PREPARATION ET LEUR UTILISATION EN TANT QU'AGENTS CONTRE LES TUMEURS

Abstract



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.


Patent Details

(51) International Patent Classification (IPC):
  • C07D 305/14 (2006.01)
  • A61K 31/335 (2006.01)
(72) Inventors (Country):
  • PANDEY, RAMESH C. (United States)
  • YANKOV, LUBEN K. (United States)
  • NAIR, RAGHU (United States)
  • POULEV, ALEX (United States)
(73) Owners (Country):
  • XECHEM, INC. (United States)
(71) Applicants (Country):
  • XECHEM, INC. (United States)
(74) Agent: BERESKIN & PARR
(45) Issued: 2004-03-02
(86) PCT Filing Date: 1996-12-13
(87) PCT Publication Date: 1997-08-14
Examination requested: 1999-12-22
(30) Availability of licence: N/A
(30) Language of filing: English

(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

View or Download Images

Click on a link under View Patent Image to view a section of the image or click on a link under Download Patent Image in PDF format to download a section of the image in PDF format. PDF files can be viewed, saved, and printed using Adobe Acrobat Reader . Adobe Acrobat Reader is available for free download from Adobe's Web site.

If you have any difficulty accessing content, you can call the Client Service Centre at (819) 997-2985 or send them an e-mail at CIPO Client Service Centre.

View Patent Image Download Patent Image in PDF Format Size of Image (KB) Number of Pages
Cover Page Cover Page 42 1
Abstract Abstract 30 3
Claims Claims 324 16
Description Description 2,577 89
Drawings Drawings 686 46
Representative Drawing Representative Drawing 6 1