C-2′ methylated derivatives of paclitaxel for use as...

Details C-2′ methylated derivatives of paclitaxel for use as... C-2′ methylated derivatives of paclitaxel for use as...

2006-12-26

2006-12-26

Solola, Taofiq (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S449000, C549S060000, C549S472000, C549S510000

Reexamination Certificate

active

07153884

ABSTRACT:
Taxane derivatives of formula (I) in which: R is trifluoromethyl, phenyl, 2-furyl, 2-thienyl; R1is t-butoxycarbonyl or benzoyl; R2is hydroxy; R3is hydrogen or, together with R2, it forms the residue of a cyclic carbonate of formula: II with the proviso that when R3 is hydrogen, R is different from phenyl. Compounds of formula (I) have antitumor activity

REFERENCES:
Kant et al., “Diastereoselective addition of Grignard reagents to azetidine-2-,3-dione: synthesis of novel Taxol analogues” Tetrahedron Letters, vol. 37, No. 36, 1996, pp. 6495-6498 XP002216532.
Chen et al., “Novel C-4 Paclitaxel (Taxel) Analogs: Potent Antitumor Agents” Bioorganic & Medicinal Chemistry Letters, Oxford, GB, vol. 5, No. 22, 1995, pp. 2741-2746, XP001025908 ISSN: 0960-894X.
Chen et al., “Paclitaxel (Taxol) Chemistry and Structure—Activity Relationship” Chemistry and Pharmacology of Taxol and its Derivatives, XX, XX, NR. 22, pp. 165-253 XP008005396 (1995).

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