Condensed pyrimidine derivative

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 487/04 (2006.01) A61K 31/495 (2006.01) A61K 31/505 (2006.01) A61K 31/517 (2006.01) A61P 35/00 (2006.01) C07D 239/70 (2006.01) C07D 239/86 (2006.01) C07D 239/90 (2006.01) C07D 401/06 (2006.01) C07D 401/08 (2006.01) C07D 401/12 (2006.01) C07D 405/06 (2006.01) C07D 405/08 (2006.01) C07D 405/12 (2006.01) C07D 409/06 (2006.01) C07D 409/08 (2006.01) C07D 409/12 (2006.01) C07D 417/06 (2006.01) C07D 417/08 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2076431

ABSTRACT OF THE DISCLOSURE Novel pyrimidine derivatives and pharmacologically acceptable salts thereof are disclosed which exhibit excellent antitumor activity, and are represented by the following general formula: Image (I) wherein R1 represents a hydroxyl or amino group; R2 represents a phenylene, pyridinediyl, thiendiyl, furandiyl or thiazoldiyl group, -CO2R5 and -CO2R6 may be the same or different from each other and each represents a carboxyl group or a carboxylic acid ester, the part X-Y-Z represents Image , Image or Image , A represents an oxygen atom, a group represented by the formula: Image (wherein R3 and R4 may be the same or different from each other and each represents a hydrogen or halogen atom or a hydro-carbon group which may be substituted, or alternatively R3 and R4 may be united to form an alkylidene group which may be substituted) or a group represented by the formula: Image (wherein R70 represents a hydrogen atom or a hydrocarbon group), and n is an integer of 1 to 3, provided that the compound in which R1 represents oxygen, and hydrogen is attached to nitrogen at 3-position is included in the above shown definition. Processes for preparation of the derivatives (I) and their salts are also disclosed, as well as antitumor drugs containing the same.

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