2'-halomethylidene cytidine, uridine and guanosine compounds and

Details 2'-halomethylidene cytidine, uridine and guanosine compounds and 2'-halomethylidene cytidine, uridine and guanosine compounds and

1993-08-27

1995-01-03

Rollins, John W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 49, 514 50, 536 2713, 536 2714, 536 2781, 536 282, 536 255, 536 2853, C07H 19073, C07H 19173

Patent

active

053786939

ABSTRACT:
This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.

REFERENCES:
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Ferrier, "4',5'-Unsaturated, Cyclic Compounds", Adv. Carbohydrate Chem., 24, 250-251 (1969).
Fukukawa et al., "Synthesis of 2'(R)-Substituted Neplanocin A's (Nucleosides and Nucleotides XXXVII)," Chem. Pharm. Bull., 29, 597-600 (1981).
Katritzky et al., Comprehensive Heterocyclic Chemistry, vol. 5, Pergamon Press, New York, 1984, see p. 603.
Takenuki et al., "Design Synthesis, and Antineoplastic Activity of 2'-Deoxy-2'-methylidenecytidine," J. Med. Chem., 31(6), 1063-1064 (1988).
Matsuda et al., "Alkyl Addition Reaction of Pyrimidine 2'-Ketonucleosides:Synthesis of 2'-Branched-Chain Sugar Pyrimidine Nucleosides (Nucleosides and Nucleotides LXXXI)", Chem. Pharm. Bull., 36(3), 945-953 (1988).
Hansske et al., "Nucleic Acid Related Compounds, 43. A Convenient Procedure for the Synthesis of 2' and 3'-Ketonucleosides," Tett. Lett., 24(15), 1589-1592 (1983).
Hansske et al., "2' and 3'-Ketonucleosides and Their Arabino and Xylo Reduction Products," Tetrahedron, 40(1), 125-135 (1984).

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