Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Reexamination Certificate
2006-04-18
2006-04-18
Dentz, Bernard (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
C514S553000, C562S106000, C562S126000
Reexamination Certificate
active
07030158
ABSTRACT:
A group of new compounds, N-(all-trans-Retinoyl)-L-cysteic acid, N-(13-cis-Retinoyl)-L-cysteic acid, N-(all-trans-Retinoyl)-L-cysteinesulfinic acid, N-(13-cis-Retinoyl)-L-cysteinesulfinic acid, N-(all-trans-Retinoyl)-L-homocysteic acid, N-(13-cis-Retinoyl)-L-homocysteic acid, and sodium salts of these compounds, including sodium salts of their esters and amides, is shown to exhibit therapeutic effects per se, and which compounds in combination with cytotoxic compounds, such as docetaxel, paclitaxel, doxorubicin and mitoxantrone, exhibit a synergistic effect. These compounds make it possible to manufacture new formulations of poorly soluble pharmaceutical compounds, and the present invention discloses a process of manufacturing water-soluble formulations of such compounds, exemplified by docetaxel, and paclitaxel, exhibiting enhanced pharmacological activity, and formulations of water-soluble pharmaceuticals exemplified by doxorubicin and mitoxantrone, exhibiting improved therapeutic efficacy.
REFERENCES:
patent: 6642271 (2003-11-01), Strelchenok et al.
patent: 40 32 187 (1992-04-01), None
Arsenov, D.V. et al. (2001) “Synthesis of N-(all-trans-retinoyl) doxorubicin and Study of the Antitumor Activity of its Complex with Blood Serum Proteins”Pharmaceutical Chemistry Journal35 (4): 186-189 (Original and English translation).
Aleksov Julian
Strelchenok Oleg
Ardenia Investments Ltd.
Dentz Bernard
Morrison & Foerster / LLP
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