PYRIMIDINE COMPOUND AND MEDICINAL COMPOSITION THEREOF

• Main Authors: ASANO, OSAMU, HARADA, HITOSHI, MIYAZAWA, SHUHEI, NAKAGAWA, MAKOTO, HIROTA, KAZUO, KOTAKE, YOSHIHIKO, YASUDA, NOBUYUKI, NAGAKAWA, JUNICHI, KABASAWA, YASUHIRO, UEDA, MASATO, YASUDA, MASAHIRO, IIDA, DAISUKE
• Format: Patent
• Language: English; French; Japanese
• Published: 01.05.2003
• Edition: 7
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

A novel pyrimidine compound having an excellent antagonistic activity against adenosine receptors (A1, A2A, and A2B receptors). Specifically, it is a compound represented by the following formula, a salt of the compound, or a solvate of either. (I) In the formula, R1 and R2 are the same or different and each represents hydrogen, optionally substituted C1−6 alkyl, etc.; R3 represents hydrogen, halogeno, etc.; R4 represents an optionally substituted C6−14 aromatic hydrocarbon ring group, optionally substituted 5− to 14−membered nonaromatic heterocyclic group having at least one unsaturated bond, etc.; and R5 represents an optionally substituted C6−14 aromatic hydrocarbon ring group or optionally substituted 5− to 14−membered aromatic heterocyclic group. A novel pyrimidine compound having an excellent antagonistic activity against adenosine receptors A1, A2A, and A2B receptors. Specifically, it is a compound represented by the following formula, a salt of the compound, or a solvate of either. I In the formula, R1 and R2 are the same or different and each represents hydrogen, optionally substituted C1-6 alkyl, etc. R3 represents hydrogen, halogeno, etc. R4 represents an optionally substituted C6-14 aromatic hydrocarbon ring group, optionally substituted 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond, etc. and R5 represents an optionally substituted C6-14 aromatic hydrocarbon ring group or optionally substituted 5- to 14-membered aromatic heterocyclic group. L'invention concerne un nouveau composé de pyrimide ayant une excellente activité antagoniste contre les récepteurs d'adénosine (récepteurs A1, A2A et A2B). Plus particulièrement, l'invention concerne un composé représenté par la formule suivante, son sel ou son solvate. Dans la formule (I), R1 et R2 sont identiques ou différents et chacun représente hydrogène, alkyle C1-6 éventuellement substitué, etc. ; R3 représente hydrogène, halogéno, etc. ; R4 représente un groupe cyclique hydrocarbure aromatique C6-14 éventuellement substitué, groupe hétérocyclique non aromatique à 5-14 chaînons éventuellement substitués ayant au moins une liaison insaturée, etc. ; et R5 représente groupe cyclique hydrocarbure aromatique C6-14 éventuellement substitué ou groupe hétérocyclique aromatique à 5-14 chaînons éventuellement substitué.