Pyrimidine nucleoside compound or its salt

Details Pyrimidine nucleoside compound or its salt Pyrimidine nucleoside compound or its salt

2006-01-30

2010-11-02

Crane, Lawrence E (Department: 1623)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

C536S028500

Reexamination Certificate

active

07825103

ABSTRACT:
Provided is a pyrimidine nucleoside compound represented by the following formula (1):or a pharmaceutically acceptable salt thereof, wherein one of X and Y represents a cyano group, and the other represents a hydrogen atom; one of R1and R2represents a hydrogen atom, a carbonyl group having a C1-C6 alkyl group which has been mono-substituted by an amino group, or a group represented by (R3)(R4)(R5)Si—, and the other represents a group represented by (R6)(R7)(R8)Si—, or R1and R2together form a 6-membered cyclic group represented by —Si(R9)(R10)—; R3, R4, R5, R6, R7, and R8each represent a C1-C10 linear or branched alkyl group which may have a substituent, a C3-C6 cycloalkyl group which may have a substituent, a C6-C14 aryl group which may have a substituent, or a C1-C6 alkyl group which has been substituted by one or two C6-C14 aryl groups and which may have a substituent; and R9and R10each represent a C1-C6 linear or branched alkyl group which may have a substituent. The pyrimidine nucleoside compound of formula (1) or a pharmaceutically acceptable salt thereof exhibits a potent antitumor effect and is therefore useful as a therapeutic agent for preventing or treating a tumor.

REFERENCES:
patent: 5061793 (1991-10-01), Grindey et al.
patent: 5691319 (1997-11-01), Kaneko et al.
patent: 61-148193 (1986-07-01), None
patent: 4 235182 (1992-08-01), None
patent: 5 194497 (1993-08-01), None
patent: 7-179491 (1995-07-01), None
patent: 2003 113197 (2003-04-01), None
John S. Evans, et al.; “Antitumor Activity of 1-β-D-Arabinofuranosylcytosine Hydrochloride”; Pro. Soc. Exp. Bio. Med.; 1961; pp. 350-353.
Akio Hoshi, et al.; “Antitumor Activity of 1-Hexylcarbamoyl-5-Fluorouracil in a Variety of Experimental Tumors”; Oct. 1976; Gann, 67; pp. 725-731.
Kenjiro Kodama, et al.; “Antitumor Activity and Pharmacology of 1-β-D-Arabinofuranosylcytosine-5′-stearylphosphate: An Orally Active Derivative of 1-β-D-Arabinofuranosylcytosine”; Jpn. J. Cancer Res. 80, Jul. 1989; pp. 679-685.
Akira Matsuda, et al.; “Antitumor activity of sugar-modified cytosine nucleosides”; Cancer Sci; Feb. 2004; vol. 95; No. 2; pp. 105-111.
Akira Matsuda, et al.; “Protein, Nucleic Acid, and Enzyme”; 43; 1998; pp. 1981-1989 (with partial English Translation).
Matthew H. Katz, et al.; “Survival Efficacy of Adjuvant Cytosine-Analogue CS-682 in a Fluorescent Orthotopic Model of Human Pancreatic Cancer”; Cancer Research; Mar. 1, 2004; 64; pp. 1828-1833.
Akira Matsuda, et al., “Nucleosides and Nucleotides. 100. 2′-C-Cyano-2′ -Deoxy-1-Beta-D-Arabinofuranosylcytosine (CNDAC): Design of a Potential Mechanism-Based DNA-Strand-Breaking Antineoplastic Nucleoside”, Journal of Medicinal Chemistry, vol. 34, No. 9, pp. 2917-2919, 1991.
Atsushi Azuma, et al.,“Nucleosides and Nucleotides. 122. 2′ -C-Cyano-2′ -Deoxy-1-Beta-D-Arabinofuranosylcytosine and Its Derivatives. A New Class of Nucleoside With a Broad Antitumor Spectrum”, Journal of Medicinal Chemistry, vol. 36, No. 26, pp. 4183-4189, 1991.

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