C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 405/14 (2006.01) A61K 31/506 (2006.01) C07D 401/04 (2006.01) C07D 409/14 (2006.01)
Patent
CA 2463284
The present invention provides a novel pyrimidine compound having an excellent adenosine receptor (A1, A2A, A2B receptor) antagonistic action. More specifically, it provides a compound represented by the following formula, a salt thereof or a solvate of them. (see formula I) In the formula, R1 and R2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, a cycloalkyl group having three to eight carbon atoms which maybe substituted, a cycloalkenyl group having three to eight carbon atoms which maybe substituted, a 5 to 14-membered non-aromatic heterocyclic group which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, an acyl group having one to six carbon atoms which may be substituted or an alkylsulfonyl group having one to six carbon atoms which may be substituted; R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, a nitrogen atom which may be substituted, an oxygen atom which may be substituted or a sulfur atom which may be substituted; R4 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted or a 5 to 14-membered non-aromatic heterocyclic group having at least one or more unsaturated bonds which may be substituted; and R5 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted or a 5 to 14-membered aromatic heterocyclic group which may be substituted. 236
L'invention concerne un nouveau composé de pyrimide ayant une excellente activité antagoniste contre les récepteurs d'adénosine (récepteurs A¿1?, A¿2A? et A¿2B?). Plus particulièrement, l'invention concerne un composé représenté par la formule suivante, son sel ou son solvate. Dans la formule (I), R?1¿ et R?2¿ sont identiques ou différents et chacun représente hydrogène, alkyle C¿1-6?éventuellement substitué, etc. ; R?3¿ représente hydrogène, halogéno, etc. ; R?4¿ représente un groupe cyclique hydrocarbure aromatique C¿6-14 ?éventuellement substitué, groupe hétérocyclique non aromatique à 5-14 chaînons éventuellement substitués ayant au moins une liaison insaturée, etc. ; et R?5¿ représente groupe cyclique hydrocarbure aromatique C¿6-14 ?éventuellement substitué ou groupe hétérocyclique aromatique à 5-14 chaînons éventuellement substitué.
Asano Osamu
Harada Hitoshi
Hirota Kazuo
Iida Daisuke
Kabasawa Yasuhiro
Eisai Co. Ltd.
Eisai R&d Management Co. Ltd.
Smart & Biggar
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