Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-09-30
1998-06-02
Trinh, Ba K.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549414, 549510, 549511, A61K 31335, C07D30514
Patent
active
057600724
ABSTRACT:
A paclitaxel prodrug has a paclitaxel portion coupled to a cleavable N-(aliphatic or aromatic)-O-glycosyl carbamate spacer group, and can be administered orally, topically or by injection to provide an anti-tumor effect, the prodrug being activated by a hydrolizing enzyme, an endogeneous enzyme or an exogeneous enzyme.
REFERENCES:
R.G.G. Leenders et al, "beta-Glucuronyl Carbamate Based Pro-moieties Designed for Prodrugs in ADEPT", Tetrahedron Letters, vol. 36, No. 10, pp. 1701-1704, Mar. 1995, Oxford GB.
K.C. Nicolaou et al, "Design, Synthesis and Biological Activity of Protaxols", Nature, vol. 364, No. 6436, Jul. 29, 1993, p. 464-466.
Y. Ueda et al, Synthesis and Antitumour Evaluation of 2'-Oxycarbonylpaclitaxels (Paclitaxel-2'-Carbonates), Bioorganic and Medicinal Chemistry Letters, vol. 4, No. 15, 1994, pp. 1861-1864.
M.L. Rodrigues et al, "Synthesis and beta-lactamase-mediated Activation of a Cephalosporin-taxol Prodrug", Chemistry and Biology, vol. 2, April 1995, pp. 223-227.
de Bont Hendricus B. A.
de Vos Dick
Haisma Hidde J.
Leenders Ruben G. G.
Scheeren Johan W.
Pharmachemie B.V.
Trinh Ba K.
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