C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
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.
Haneda Toru
Kitoh Kyosuke
Kotake Yoshihiko
Nomura Hiroaki
Ueda Norihiro
Eisai Co. Ltd.
G. Ronald Bell & Associates
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