Title:
C-2' METHYLATED DERIVATIVES OF PACLITAXEL FOR USE AS ANTITUMOUR AGENTS
Document Type and Number:
WIPO Patent Application WO/2003/013503
Kind Code:
A1
Abstract:
Taxane derivatives of formula (I) in which: R is trifluoromethyl, phenyl, 2-furyl, 2-thienyl; R?1¿ is t-butoxycarbonyl or benzoyl; R¿2? is hydroxy; R¿3? is hydrogen or, together with R¿2?, it forms the residue of a cyclic carbonate of formula: I I with the proviso that when R3 is hydrogen, R is different from phenyl.Compounds of formula (I) have antitumor activity.
Inventors:
BOMBARDELLI EZIO (IT)
FONTANA GABRIELE (IT)
BATTAGLIA ARTURO (IT)
CIMITAN SAMANTA (IT)
FONTANA GABRIELE (IT)
BATTAGLIA ARTURO (IT)
CIMITAN SAMANTA (IT)
Application Number:
PCT/EP2002/008185
Publication Date:
February 20, 2003
Filing Date:
July 23, 2002
Export Citation:
Assignee:
INDENA SPA (IT)
BOMBARDELLI EZIO (IT)
FONTANA GABRIELE (IT)
BATTAGLIA ARTURO (IT)
CIMITAN SAMANTA (IT)
BOMBARDELLI EZIO (IT)
FONTANA GABRIELE (IT)
BATTAGLIA ARTURO (IT)
CIMITAN SAMANTA (IT)
International Classes:
A61P35/00; C07D305/14; C07D407/12; A61K31/337; (IPC1-7): A61K31/337; A61P35/00; C07D305/14; C07D407/12; C07D409/12
Other References:
KANT, J. ET AL.: "Diastereoselective addition of Grignard reagents to azetidine-2,3-dione: synthesis of novel Taxol analogues", TETRAHEDRON LETTERS, vol. 37, no. 36, 1996, pages 6495 - 6498, XP002216532
CHEN S-H ET AL: "NOVEL C-4 PACLITAXEL (TAXEL) ANALOGS: POTENT ANTITUMOR AGENTS", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 5, no. 22, 1995, pages 2741 - 2746, XP001025908, ISSN: 0960-894X
CHEN S-H ET AL: "PACLITAXEL (TAXOL) CHEMISTRY AND STRUCTURE - ACTIVITY RELATIONSHIP", CHEMISTRY AND PHARMACOLOGY OF TAXOL AND ITS DERIVATIVES, XX, XX, NR. 22, PAGE(S) 165-253, XP008005396
CHEN S-H ET AL: "NOVEL C-4 PACLITAXEL (TAXEL) ANALOGS: POTENT ANTITUMOR AGENTS", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 5, no. 22, 1995, pages 2741 - 2746, XP001025908, ISSN: 0960-894X
CHEN S-H ET AL: "PACLITAXEL (TAXOL) CHEMISTRY AND STRUCTURE - ACTIVITY RELATIONSHIP", CHEMISTRY AND PHARMACOLOGY OF TAXOL AND ITS DERIVATIVES, XX, XX, NR. 22, PAGE(S) 165-253, XP008005396
Attorney, Agent or Firm:
Bianchetti, Giuseppe (Via Rossini 8, Milano, IT)
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