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    • 14. 发明授权
    • Pyrazolo�1,5-A!pyrimidine derivatives and anti-inflammatory agent
containing the same
    • 吡唑并[1,5-A]嘧啶衍生物和含有它们的抗炎剂
    • US5688949A
    • 1997-11-18
    • US133086
    • 1993-10-07
    • Makoto InoueKinji HashimotoToshiko KuwaharaYukio SugimotoTakuji UesakoToshiaki Funato
    • Makoto InoueKinji HashimotoToshiko KuwaharaYukio SugimotoTakuji UesakoToshiaki Funato
    • A61K31/505A61P29/00C07D487/04
    • C07D487/04
    • Pyrazolo�1,5-a!pyrimidine derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, carboxyl, lower alkoxy-carbonyl, phenyl, lower alkyl optionally having a substituent selected from OH, carboxyl and lower alkoxy-carbonyl, or cycloalkyl, or R.sub.1 and R.sub.2 may combine each other to form lower alkylene; R.sub.5 is group of --SR.sub.6 or group of --NR.sub.7 R.sub.8 in which R.sub.6 is pyridyl or phenyl optionally having 1 to 3 substituents selected from OH and lower alkyl; and R.sub.7 and R.sub.8 are H, phenyl optionally having 1 to 3 substituents selected from OH, lower alkyl, lower alkoxycarbonyl and carboxyl, or R.sub.7 and R.sub.8 may combine each other to form with a nitrogen atom with which they bond 1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, or 1-piperazinyl group substituted by a phenyl group optionally being substituted by halogen or trihalomethyl, hydroxy-lower alkyl or diphenyl-lower alkyl, or a salt thereof, and anti-inflammatory agent containing as active ingredient compound of the above formula, wherein R.sub.1, R.sub.3 and R.sub.4 are H, R.sub.2 is lower alkyl or cycloalkyl, R.sub.5 is group of --NR.sub.7 R.sub.8 (R.sub.7 is H, R.sub.8 is phenyl substituted by OH and two lower alkyl).
    • PCT No.PCT / JP91 / 01043 Sec。 371日期:1993年10月7日 102(e)日期1993年10月7日PCT 1991年8月6日PCT PCT。 出版物WO92 / 18504 日期:1992年10月29日具有下式的吡唑并[1,5-a]嘧啶衍生物:其中R1,R2,R3和R4是H,羧基,低级烷氧基 - 羰基,苯基,任选具有选自 OH,羧基和低级烷氧基 - 羰基或环烷基,或者R 1和R 2可以相互结合形成低级亚烷基; R5是-SR6或-NR7R8基团的基团,其中R6是吡啶基或任选具有1至3个选自OH和低级烷基的取代基的苯基; 并且R 7和R 8是H,任选具有1至3个选自OH,低级烷基,低级烷氧基羰基和羧基的取代基的苯基,或者R 7和R 8可以彼此结合形成氮原子,与它们键合1-吡咯烷基, 被卤素或三卤代甲基,羟基 - 低级烷基或二苯基 - 低级烷基或其盐任选取代的苯基取代的1-氧代-1-吡咯烷基或1-哌嗪基,以及含有作为活性成分的化合物的抗炎剂 其中R1,R3和R4是H,R2是低级烷基或环烷基,R5是-NR7R8基团(R7是H,R8是被OH取代的苯基和两个低级烷基)。