Taxoid anti-tumor agents and pharmaceutical compositions thereof

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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549511, 514449, C07D30514, A61K 31337

Patent

active

060969091

ABSTRACT:
This invention relates to a taxoid of the formula (I) ##STR1## wherein R.sup.1 is 1-propenyl radical;

REFERENCES:
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patent: 5294737 (1994-03-01), Ojima
patent: 5739362 (1998-04-01), Holton et al.
Greene et al, "Protective Group in Organic Synthesis", 2nd ed., 1991, pp. 10-12.
Ojima et al. "Synthesis and Biological Activity of 3'-Alkyl-and 3'-Alkyl-and 3'-Alkenyl-3'-Dephenyldocetaxels", Bioorganic & Medicinal Chemistry Letters, vol. 4, No. 21, pp. 2631-2634 (1994).
Ojima et al., "N-Acyl-3-Hydroxy-.beta.-lactams as Key Intermediates for Taxotere and its Analogs" Bioorganic & Medicinal Chemistry Letters, vol. 3, No. 11, pp.2479-2482, Apr. 1993.
Ojima et al., "A Highly Efficient Route to Taxotere by the .beta.-Lactam Synthon Method"; Tetrahedron Letters, vol. 34, No. 26, pp. 4149-4152, 1993.
Ojima et al., "New and Efficient Routes to Norstatine and its Analogs with High Enantiomeric Purity by .beta.-Lactam Synthon Method"; Tetrahedron Letters, vol. 33, No. 39, pp. 5737-5740, 1992.
Ojima et al., "New and Efficient Approaches to the Semisynthesis of Taxol and its C-13 Side Chain Analogs by Means of .beta.-Lactam Synthon Method"; Tetrahedron vol. 48, No. 34, pp. 6985-7012, 1992.
Iwao Ojima, "In Vitro Evaluation," Department of Experimental Therapeutics, Roswell Park Cancer Institute, Sheet A, Aug. 26, 1994.
Iwao Ojima, "In Vitro Evaluation," Department of Experimental Therapeutics, Roswell Park Cancer Institute, Sheet B, May 24, 1994.
Iwao Ojima, Olivier Duclos, Scott D. Kuduk, Chung-Ming Sun, John C. Slater, Fran.cedilla.ois Lavelle, Jean M. Veith, and Ralph J. Bernacki, "Synthesis and Biological Activity of 3'-Alkyl-and 3'-Alkenyl-3'-Dephenyldocetaxels", Bioorganic & Medicinal Chemistry Letters, vol. 4, No. 21, pp. 2631-2634, Sep. 7, 1994.

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