2'-Cyano pyrimidine nucleoside compounds

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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514 50, 514908, 536 274, 536 281, 536 282, 536 284, 536 285, 536 2852, 536 2853, 536 2854, A61K 3170, C07H 1906, C07H 1909

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056165676

ABSTRACT:
The pyrimidine compounds of the present invention are represented by the following formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein, R.sup.1 represents a hydroxyl or an amino which may be substituted by an acyl group; R.sup.2 represents a hydrogen atom or an alkyl having 1 to 4 carbons; R.sup.3 represents a hydrogen or a hydroxyl; and R.sup.4 and R.sup.5 each represent a hydrogen or together form a group --R.sup.6 R.sup.7 Si--O--SiR.sup.6' R.sup.7' --, wherein R.sup.6, R.sup.7, R.sup.6' and R.sup.7' are the same or different from one another and each represent an alkyl having 1 to 4 carbons. The compounds of the present invention exhibit an excellent antitumor effect.

REFERENCES:
Dieter Habich, et al, "Synthesis of 3'-Cyano-3'-deoxy-.beta.-D-arabino-nucleosides", 1988, pp. 943-947, Synthesis.
Dong Yu et al, "Synthesis of 3'-Cyano-2',3'-dideoyadenosine and 2',3'-Dideoxy-3'-formyladenosine", 1989, pp. 3240-3342, J. Org. Chem.
CA 115(3):29817a (1991) Makuda et al.
J. Med. Chem. vol. 34(9) 2917-2919.
Scientific American (Jan. 1994) vol. 270 No. 1, Beardsley.

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