Triazolo [4,5-d] pyrimidine derivatives and their use as purinergic receptor antagonists

• Main Authors: J. LERPINIERE, S. GAUR, R.J. GILLESPIE
• Format: Patent
• Language: Chinese; English
• Published: 12.05.2004
• 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

式(I)化合物或其可药用盐或其前药在治疗或预防其中阻断嘌呤受体，特别是腺苷受体，更特别是A#-[2A]受体可对其有益的病症中的应用，其中R#-[1]选自H、烷基、芳基、烷氧基、芳氧基、烷硫基、芳硫基、卤素、CN、NR#-[5]R#-[6]、NR#-[4]COR#-[5]、NR#-[4]CONR#-[5]R#-[6]、NR#-[4]CO#-[2]R#-[7]和NR#-[4]SO#-[2]R#-[7]；R#-[2]选自经由不饱和碳连接的芳基；R#-[3]选自H、烷基、COR#-[5]、CO#-[2]R#-[7]、CONR#-[5]R#-[6]、CONR#-[4]NR#-[5]R#-[6]和SO#-[2]R#-[7]；R#-[4]、R#-[5]和R#-[6]独立地选自H、烷基和芳基，或者当R#-[5]和R#-[6]在NR#-[5]R#-[6]基团中时，R#-[5]和R#-[6]可连接以形成杂环基，或者当R#-[4]、R#-[5]和R#-[6]在(CONR#-[4]NR#-[5]R#-[6])基团中时，R#-[4]和R#-[5]可连接以形成杂环基；且R#-[7]选自烷基和芳基，特别是其中所述病症是运动病症例如帕金森氏病，或者所述病症是抑郁症、认知或记忆减损、急性或慢性疼痛、ADHD或嗜眠症，或所述化合物用于个体中的神经保护；用于治疗的式(I)化合物；和新的式(I)化合物自身。 The use of a compound of formula (I): wherein R1 is selected from H, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, halogen, CN, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from aryl attached via an unsaturated carbon; R3 is selected from H, alkyl, COR5, CO2R7, CONR5R6, CONR4NR5R6 and SO2R7; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an NR5R6 group, R5 and R6 may be linked to form a heterocyclic group, or where R4, R5 and R6 are in a (CONR4NR5R6) group, R4 and R5 may be linked to form a heterocyclic group; and R7 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chronic pain, ADHD or narcolepsy, or for neuroprotection in a subject; compounds of formula (I) for use in therapy; and novel compounds of formula (I) per se.