Novel 2'-methylidenenucleotide compounds, methods for...

C - Chemistry – Metallurgy – 12 – P

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C12P 19/30 (2006.01) A61K 31/70 (2006.01) C07H 19/10 (2006.01)

Patent

CA 2158462

Novel 2'-methylidenenucleotide compounds of the formula (I) Image ( I ) wherein R is a hydrogen or a halogen, R1 and R2 are the same or different and each is a fatty acid residue or a hydrocarbon residue, and R3 and R4 are the same or different and each is a hydrogen, a halogen or an alkyl; salts thereof; methods for production thereof; and pharmaceutical use thereof. The compounds and salts thereof show an excellent antitumor effect in mammals. More specifically, they show a remarkable activity of inhibiting growth of mouse tumors, cultured human tumor cells, and human tumors transplanted to nude mice, and are useful for the treatment and prevention of recurrence of lung cancer, gastrointestinal cancer, breast cancer, cervical cancer, gynecological cancer, urinological cancer, leukemia, melanoma, lymphogenous metastatic tumor and the like in mammals. They are also useful as antitumor agents since they have an increased bioavailability and low toxicity. In addition, they have the effects of maintaining and enhancing their activities.

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