乙基 7-氯-1H-吡唑并[4,3-b]吡啶-6-羧酸 | 100478-04-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡唑并吡啶类
• 中文名称: 乙基 7-氯-1H-吡唑并[4,3-b]吡啶-6-羧酸
• 中文别名: 乙基7-氯-1H-吡唑并[4,3-b]吡啶-6-羧酸
• 英文名称: Ethyl 7-chloro-1H-pyrazolo[4,3-B]pyridine-6-carboxylate
• CAS: 100478-04-4
• 化学式: C₉H₈ClN₃O₂
• 分子量: 225.634
• InChiKey: XIHDSBGJZZFOSZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  67.9
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  乙基 7-氯-1H-吡唑并[4,3-b]吡啶-6-羧酸 在 正丁胺 、 水 、 乙酸乙酯 作用下， 以 正丁胺 为溶剂， 反应 3.0h， 以to give ethyl 7-n-butylamino-1H-pyrazolo [4,3-b]pyridine-6-carboxylate (2.75 g, 67%), m.p. 164°-170° C.的产率得到ethyl 7-n-butylamino-1H-pyrazolo[4,3-b]-pyridine-6-carboxylate
  参考文献：
  名称：

  Pharmacologically useful pyrazolopyridines

  摘要：

  式(I)的化合物：##STR1## 其中：X是NR，其中R是氢，C.sub.1-6烷基; 氧; 硫; SO; 或SO.sub.2; 或R和R.sub.3一起取C.sub.4-6聚亚甲基; R.sub.1是氢或C.sub.1-6烷基; R.sub.2是CN，CR.sub.5R.sub.6Y，其中R.sub.5和R.sub.6独立选择自氢和C.sub.1-4烷基，Y选择自氢，OR.sub.7或SR.sub.7，其中R.sub.7是氢，C.sub.1-4烷基，C.sub.2-4烷酰基和NR.sub.8R.sub.9，其中R.sub.8和R.sub.9独立选择自氢，C.sub.1-4烷基，C.sub.2-4烯基或C.sub.2-4烷酰基，或R.sub.8和R.sub.9一起取C.sub.4-6聚亚甲基，或COR.sub.10，其中R.sub.10是C.sub.1-4烷基，前提是当R.sub.1是氢时，Y不是氢；或R.sub.2是氢C.sub.1-6烷基或苯基，可选地被卤素，CF.sub.3，C.sub.1-4烷氧基或C.sub.1-4烷基取代；R.sub.1是CN，CR.sub.5R.sub.6Y或COR.sub.10，如上所定义的R.sub.2；或R.sub.1和R.sub.2一起形成C.sub.3-C.sub.6聚亚甲基，可选地被C.sub.1-C.sub.4烷基取代；R.sub.3是C.sub.1-10烷基或C.sub.3-10环烷基，可选地被羟基，C.sub.1-4烷氧基，硫醇，C.sub.1-4烷基硫醇或NR.sub.11R.sub.12取代，其中R.sub.11和R.sub.12独立选择自氢，C.sub.1-6烷基或C.sub.2-7酰基，或者一起是C.sub.3-6聚亚甲基；C.sub.2-10烯基；或苯基，可选地被卤素，CF.sub.3，C.sub.1-4烷氧基，C.sub.1-4烷基，羟基，硝基，氰基，C.sub.2-10酰氧基，NR.sub.13R.sub.14，其中R.sub.13和R.sub.14独立选择自氢，C.sub.1-6烷基，C.sub.2-7酰基，C.sub.1-6烷基磺酰基或COR.sub.15，其中R.sub.15是羟基，C.sub.1-6烷氧基或NR.sub.16R.sub.17，其中R.sub.16和R.sub.17独立选择自氢或C.sub.1-6烷基；或与R一起为C.sub.4-6聚亚甲基；R.sub.4是氢；或C.sub.1-4烷基或苯甲基，可选地在苯环上被一或两个卤素，CF.sub.3，C.sub.1-4烷氧基或C.sub.1-4烷基取代，并连接在氮原子1或2上，被用于治疗炎症和过敏性疾病。

  公开号：

  US04837238A1
• 作为产物：
  描述：

  Ethyl 7-oxo-4,7-dihydro-1H-pyrazolo[4,3-b]pyridine-6-carboxylate 在 N,N-二甲基甲酰胺 草酰氯 作用下， 以 氯仿 为溶剂， 反应 3.0h， 生成 乙基 7-氯-1H-吡唑并[4,3-b]吡啶-6-羧酸
  参考文献：
  名称：

  THERAPEUTIC 5,6,5-TRICYCLIC ANALOGS

  摘要：

  这项发明提供了一种新颖的化学系列，其化学式为I，以及利用该化合物结合到GABA A 受体的苯二氮卓位点并负性调节GABA A 的α5亚型的方法，以及利用化合物I的制备药物治疗GABA A 受体相关疾病的方法。该发明还提供了一种在动物体内调节一个或多个GABA A 亚型的方法，包括向动物体内施用化合物I的有效量。

  公开号：

  US20120095016A1

文献信息

• Certain 7-amino-pyrazolo[4,3-b]pyridines useful in treating inflammatory
  申请人：Beecham Group p.l.c.

  公开号：US04716160A1

  公开（公告）日：1987-12-29

  Compounds of formula (I) ##STR1## wherein: R is hydrogen or C.sub.1-6 alkyl; R.sub.1 and R.sub.2 are both hydrogen; or R.sub.1 is hydrogen, C.sub.1-6 alkyl; and R.sub.2 is CN; CR.sub.5 R.sub.6 Y where R.sub.5 and R.sub.6 are independently selected from hydrogen and C.sub.1-4 alkyl and Y is selected from hydrogen, OR.sub.7 or SR.sub.7 where R.sub.7 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, and NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl or together are C.sub.4-6 polymethylene, or COR.sub.10 where R.sub.10 is OH or C.sub.1-4 alkyl, or COR.sub.10 is a pharmaceutically acceptable ester or amide; or R.sub.2 is hydrogen, C.sub.1-6 alkyl, or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; and R.sub.1 is CN, CR.sub.5 R.sub.6 Y or COR.sub.10 as defined for R.sub.2 above; or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.6 polymethylene optionally substituted by C.sub.1 -C.sub.4 alkyl; R.sub.3 a mono- or fused bi-cyclic heteroaryl group having up to ten atoms in the aromatic ring(s), not more than two of which are selected from nitrogen, oxygen or sulphur, other than those containing basic nitrogen, optionally substituted by one or two substituents selected from halogen, CF.sub.3, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, hydroxy, nitro, cyano, C.sub.2-10 acyloxy, NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkanoyl or C.sub.1-6 alkylsulphonyl; or COR.sub.13 wherein R.sub.13 is hydroxy, C.sub.1-6 alkoxy or NR.sub.14 R.sub.15 wherein R.sub.15 and R.sub.14 are independently selected from hydrogen or C.sub.1-6 alkyl; and R.sub.4 is hydrogen, or C.sub.1-4 alkyl, or benzyl optionally substituted in the phenyl ring by one or more of halogen, CF.sub.3, C.sub.1-4 alkyl, and is attached at nitrogen atom 1 or 2; show anti-inflammatory and anti-allergy activity.

  化合物的式子(I) ##STR1## 其中：R为氢或C.sub.1-6烷基；R.sub.1和R.sub.2都是氢；或者R.sub.1为氢、C.sub.1-6烷基；R.sub.2为CN；CR.sub.5R.sub.6Y，其中R.sub.5和R.sub.6分别独立地选择自氢和C.sub.1-4烷基，而Y选择自氢、OR.sub.7或SR.sub.7，其中R.sub.7为氢、C.sub.1-4烷基或C.sub.2-4酰基，以及NR.sub.8R.sub.9，其中R.sub.8和R.sub.9独立地选择自氢、C.sub.1-4烷基、C.sub.2-4烯基或C.sub.2-4酰基，或者一起为C.sub.4-6聚亚甲基，或者为COR.sub.10，其中R.sub.10为OH或C.sub.1-4烷基，或者COR.sub.10为药学可接受的酯或酰胺；或者R.sub.2为氢、C.sub.1-6烷基或苯基，可选择通过卤素、CF.sub.3、C.sub.1-4烷氧基或C.sub.1-4烷基中的一个或多个取代，而R.sub.1为CN、CR.sub.5R.sub.6Y或COR.sub.10，如上所定义；或者R.sub.1和R.sub.2一起形成C.sub.3-C.sub.6聚亚甲基，可选择通过C.sub.1-C.sub.4烷基取代；R.sub.3为具有多达十个原子的芳环中的单环或融合双环杂环基团，其中不超过两个选择自氮、氧或硫，不包括含有碱性氮的基团，可选择通过卤素、CF.sub.3、C.sub.1-4烷氧基、C.sub.1-4烷基、羟基、硝基、氰基、C.sub.2-10酰氧基、NR.sub.11R.sub.12（其中R.sub.11和R.sub.12独立地选择自氢、C.sub.1-6烷基、C.sub.2-7酰基或C.sub.1-6烷基磺酰基）或COR.sub.13（其中R.sub.13为羟基、C.sub.1-6烷氧基或NR.sub.14R.sub.15，其中R.sub.14和R.sub.15独立地选择自氢或C.sub.1-6烷基）取代；R.sub.4为氢或C.sub.1-4烷基或苄基，可选择在氮原子1或2上附着；表现出抗炎和抗过敏活性。
• Pharmacologically useful pyrazolopyridines
  申请人：Beecham Group p.l.c.

  公开号：US04837238A1

  公开（公告）日：1989-06-06

  Compounds of the formula (I): ##STR1## wherein: X is NR wherein R is hydrogen, C.sub.1-6 alkyl; oxygen; sulphur; SO; or SO.sub.2 ; or R and R.sub.3 taken together are C.sub.4-6 polymethylene; R.sub.1 is hydrogen or C.sub.1-6 alkyl; and R.sub.2 is CN, CR.sub.5 R.sub.6 Y where R.sub.5 and R.sub.6 are independently selected from hydrogen and C.sub.1-4 alkyl and Y is selected from hydrogen, OR.sub.7 or SR.sub.7 where R.sub.7 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkanoyl, and NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl or R.sub.8 and R.sub.9 together are C.sub.4-6 polymethylene, or COR.sub.10 where R.sub.10 is C.sub.1-4 alkyl, provided that Y is other than hydrogen when R.sub.1 is hydrogen; or R.sub.2 is hydrogen C.sub.1-6 alkyl or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; and R.sub.1 is CN, CR.sub.5 R.sub.6 Y or COR.sub.10 as defined for R.sub.2 above; or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.6 polymethylene optionally substituted by C.sub.1 -C.sub.4 alkyl; R.sub.3 is C.sub.1-10 alkyl or C.sub.3-10 cycloalkyl, either optionally substituted by hydroxy, C.sub.1-4 alkoxy, thiol, C.sub.1-4 alkylthio or NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently hydrogen, C.sub.1-6 alkyl or C.sub.2-7 alkanoyl or together are C.sub.3-6 polymethylene; C.sub.2-10 alkenyl; or phenyl optionally substituted by one or two of halogen, CF.sub.3, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, hydroxy, nitro, cyano, C.sub.2-10 acyloxy, NR.sub.13 R.sub.14 wherein R.sub.13 and R.sub.14 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkanoyl, C.sub.1-6 alkylsulphonyl or COR.sub.15 wherein R.sub.15 is hydroxy, C.sub.1-6 alkoxy or NR.sub.16 R.sub.17 wherein R.sub.16 and R.sub.17 are independently selected from hydrogen or C.sub.1-6 alkyl; or together with R is C.sub.4-6 polymethylene; and R.sub.4 is hydrogen; or C.sub.1-4 alkyl or benzyl optionally substituted in the phenyl ring by one or two of halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl and is attached at nitrogen atom 1 or 2, are disclosed as having utility in the treatment of inflammatory and allergic disorders.

  式(I)的化合物：##STR1## 其中：X是NR，其中R是氢，C.sub.1-6烷基; 氧; 硫; SO; 或SO.sub.2; 或R和R.sub.3一起取C.sub.4-6聚亚甲基; R.sub.1是氢或C.sub.1-6烷基; R.sub.2是CN，CR.sub.5R.sub.6Y，其中R.sub.5和R.sub.6独立选择自氢和C.sub.1-4烷基，Y选择自氢，OR.sub.7或SR.sub.7，其中R.sub.7是氢，C.sub.1-4烷基，C.sub.2-4烷酰基和NR.sub.8R.sub.9，其中R.sub.8和R.sub.9独立选择自氢，C.sub.1-4烷基，C.sub.2-4烯基或C.sub.2-4烷酰基，或R.sub.8和R.sub.9一起取C.sub.4-6聚亚甲基，或COR.sub.10，其中R.sub.10是C.sub.1-4烷基，前提是当R.sub.1是氢时，Y不是氢；或R.sub.2是氢C.sub.1-6烷基或苯基，可选地被卤素，CF.sub.3，C.sub.1-4烷氧基或C.sub.1-4烷基取代；R.sub.1是CN，CR.sub.5R.sub.6Y或COR.sub.10，如上所定义的R.sub.2；或R.sub.1和R.sub.2一起形成C.sub.3-C.sub.6聚亚甲基，可选地被C.sub.1-C.sub.4烷基取代；R.sub.3是C.sub.1-10烷基或C.sub.3-10环烷基，可选地被羟基，C.sub.1-4烷氧基，硫醇，C.sub.1-4烷基硫醇或NR.sub.11R.sub.12取代，其中R.sub.11和R.sub.12独立选择自氢，C.sub.1-6烷基或C.sub.2-7酰基，或者一起是C.sub.3-6聚亚甲基；C.sub.2-10烯基；或苯基，可选地被卤素，CF.sub.3，C.sub.1-4烷氧基，C.sub.1-4烷基，羟基，硝基，氰基，C.sub.2-10酰氧基，NR.sub.13R.sub.14，其中R.sub.13和R.sub.14独立选择自氢，C.sub.1-6烷基，C.sub.2-7酰基，C.sub.1-6烷基磺酰基或COR.sub.15，其中R.sub.15是羟基，C.sub.1-6烷氧基或NR.sub.16R.sub.17，其中R.sub.16和R.sub.17独立选择自氢或C.sub.1-6烷基；或与R一起为C.sub.4-6聚亚甲基；R.sub.4是氢；或C.sub.1-4烷基或苯甲基，可选地在苯环上被一或两个卤素，CF.sub.3，C.sub.1-4烷氧基或C.sub.1-4烷基取代，并连接在氮原子1或2上，被用于治疗炎症和过敏性疾病。
• Pyrazolopyridine derivatives and their use in treating inflammation and
  申请人：Beecham Group p.l.c.

  公开号：US04621089A1

  公开（公告）日：1986-11-04

  Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: X is NR wherein R is hydrogen or C.sub.1-6 alkyl, oxygen, sulphur, SO or SO.sub.2 ; R.sub.1 is COR.sub.5 wherein R.sub.5 is hydroxy, or COR.sub.5 is a pharmaceutically acceptable ester or amide group; or CF.sub.3 ; and R.sub.2 is hydrogen, C.sub.1-6 alkyl or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; or R.sub.2 is COR.sub.5 as defined or CF.sub.3 and R.sub.1 is hydrogen; R.sub.3 is C.sub.1-10 alkyl, optionally substituted by hydroxy, C.sub.1-4 alkoxy, thiol, C.sub.1-4 alkylthio or NR.sub.6 R.sub.7 wherein R.sub.6 and R.sub.7 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.3-6 polymethylene; C.sub.2-10 alkenyl or phenyl optionally substituted by one or two of halogen, CF.sub.3, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, hydroxy, nitro, cyano, C.sub.2-10 acyloxy, NR.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkanoyl or C.sub.1-6 alkylsulphonyl or COR.sub.10 wherein R.sub.10 is hydroxy, C.sub.1-6 alkoxy or NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are independently selected from hydrogen or C.sub.1-6 alkyl; and R.sub.4 is hydrogen; or C.sub.1-4 alkyl or benzyl attached at nitrogen atom 1 or 2 having anti-inflammatory and/or anti-allergy activity, a process for their preparation and their use as pharmaceuticals.

  公式（I）的化合物及其药学上可接受的盐：##STR1## 其中：X是NR，其中R是氢或C.sub.1-6烷基，氧，硫，SO或SO.sub.2; R.sub.1是COR.sub.5，其中R.sub.5是羟基，或COR.sub.5是药学上可接受的酯或酰胺基团;或CF.sub.3; R.sub.2是氢，C.sub.1-6烷基或苯基，可选地被卤素，CF.sub.3，C.sub.1-4烷氧基或C.sub.1-4烷基取代;或R.sub.2是定义的COR.sub.5或CF.sub.3，而R.sub.1是氢; R.sub.3是C.sub.1-10烷基，可选地被羟基，C.sub.1-4烷氧基，硫醇，C.sub.1-4烷基硫基或NR.sub.6R.sub.7取代，其中R.sub.6和R.sub.7独立地是氢或C.sub.1-6烷基，或一起是C.sub.3-6聚亚甲基; C.sub.2-10烯基或苯基，可选地被卤素，CF.sub.3，C.sub.1-4烷氧基，C.sub.1-4烷基，羟基，硝基，氰基，C.sub.2-10酰氧基，NR.sub.8R.sub.9，其中R.sub.8和R.sub.9独立地选自氢，C.sub.1-6烷基，C.sub.2-7烷酰基或C.sub.1-6烷基磺酰基或COR.sub.10，其中R.sub.10是羟基，C.sub.1-6烷氧基或NR.sub.11R.sub.12，其中R.sub.11和R.sub.12独立地选自氢或C.sub.1-6烷基;以及R.sub.4是氢;或C.sub.1-4烷基或苄基附在氮原子1或2上，具有抗炎和/或抗过敏活性，其制备过程及其作为药物的用途。
• Pyrazolopyridine derivatives
  申请人：BEECHAM GROUP PLC

  公开号：EP0154220A2

  公开（公告）日：1985-09-11

  Compounds of formula (I) and pharmaceutically accept- bie salts thereof: wherein: X is NR wherein R is hydrogen or C1-6 alkyl, oxygen, sulphur, SO or SO2: R, is COR5 wherein R6 is hydroxy, or COR5 is a pharmaceutically acceptable ester or amide group; or CF3; and R2 is hydrogen, C1-6 alkyl or phenyl optionally substituted by halogen, CF3, C1-4 alkoxy or C1-4 alkyl; or R2 is COR6 as defined or CF3 and R1 is hydrogen; R3 is C1-10 alkyl, optionally substituted by hydroxy, C1-4 alkoxy, thiol, C1-4 alkylthio or NR6R7 herein R6 and R7 are Independently hydrogen or C1-6 alkyl or together are C3-6 polymethlene; C2-10 alkenyl or phenyl optionally substituted by one or two of halogen, CF3, C1-4 alkoxy, C1-4 alkyl, hydroxy, nitro, cyano, C2-10 acyloxy, NR8R9 wherein R8 and R9 are independently selected from hydrogen, C1-6 alkyl, C2-7 alkanoyl or C1-6 alkylsulphonyl or COR10 wherein R10 is hydroxy, C1-6 alkoxy or NR11R12 wherein R11 and R12 are independently selected from hydrogen or C1-6 alkyl; and R4 is hydrogen: or C1-4 alkyl or benzyl attached at nitrogen atom 1 or 2 having anti-inflammatory and/or anti-allergy activity, a process for their preparation and their use as pharmaceuticals.

  式 (I) 化合物及其药用盐： 其中 X 是 NR，其中 R 是氢或 C1-6 烷基、氧、硫、SO 或 SO2： R，是 COR5，其中 R6 是羟基，或 COR5 是药学上可接受的酯基或酰胺基；或 CF3；R2 是氢、C1-6 烷基或任选被卤素、CF3、C1-4 烷氧基或 C1-4 烷基取代的苯基；或 R2 是所定义的 COR6 或 CF3，R1 是氢； R3 是 C1-10 烷基，可选择被羟基、C1-4 烷氧基、硫醇、C1-4 烷硫基或 NR6R7 取代，其中 R6 和 R7 分别是氢或 C1-6 烷基，或一起是 C3-6 聚亚甲基；C2-10烯基或苯基，可选择被卤素、CF3、C1-4烷氧基、C1-4烷基、羟基、硝基、氰基、C2-10酰氧基、NR8R9（其中R8和R9独立地选自氢、C1-6烷基、C2-7烷酰基或C1-6烷基磺酰基）或COR10（其中R10是羟基、C1-6烷氧基或NR11R12（其中R11和R12独立地选自氢或C1-6烷基）中的一个或两个取代；和 R4 是氢：或连接在氮原子 1 或 2 上的 C1-4 烷基或苄基，具有抗炎和/或抗过敏活性，其制备方法和药物用途。
• Pyrazolopyridines, their preparation and pharmaceutical compositions containing them
  申请人：BEECHAM GROUP PLC

  公开号：EP0193329A2

  公开（公告）日：1986-09-03

  Compounds of the formula (I): wherein: X is NR wherein R is hydrogen, C1-6 alkyl or as defined hereinafter with R3; oxygen; sulphur; SO; or SO2; R, is hydrogen or C1-6alkyl; and R2 is CN, CR5R6Y where Rs and R6 are independently selected from hydrogen and C1-4 alkyl and Y is selected from hydrogen, OR, or SR, where R7 is hydrogen, C1-4 alkyl or C2-4 alkanoyl, and NR8R9 where R8 and R9 are independently hydrogen, C1-4 alkyl, C 2.4 alkenyl or C2-4 alkanoyl or together are C 4-6 polymethylene, or COR10 where R,o is C1-4 alkyl, provided that Y is other than hydrogen when R, is hydrogen; or R2 is hydrogen, C1-6 alkyl or phenyl optionally substituted by halogen, CF3, C1-4 alkoxy or C1-4 alkyl; and R, is CN, CR5R6Y or COR10 as defined for R2 above; or R1 and R2 together form C3-C6 polymethylene optionally substituted by C1-C4 alkyl; R3 is C1-10 alkyl or C3-10 cycloalkyl, eitheroptionally substituted by hydroxy, C1-4 alkoxy, thiol, C1-4alkylthio or NR11R12 wherein R,, and R12 are independently hydrogen, C1-6 alkyl or C 2-7 alkanoyl or together are C3.6 polymethylene; C2-10 alkenyl; or phenyl optionally substituted by one or two of halogen, CF,, C1-4 alkoxy, C1-4 alkyl, hydroxy, nitro, cyano, C2-10 acyloxy, NR13R14 wherein R13 and R14 are independently selected from hydrogen, C1-6 alkyl, C2-7alkanoyl or C1-6 alkylsulphonyl or COR15 wherein R15 is hydroxy, C1-6 alkoxy or NR16R17 wherein R16 and R,7 are independently selected from hydrogen or C1-6 alkyl; or together with R is C 4-6 polymethylene; and R4 is hydrogen; or C1-4 alkyl or benzyl optionally substituted in the phenyl ring by one or two of halogen, CF3, C1-4 alkoxy or C1-4 alkyl and is attached at nitrogen atom 1 or 2, are disclosed as having utility in the treatment of inflammatory and allergic disorders.

  式 (I) 的化合物： 其中 X 是 NR，其中 R 是氢、C1-6 烷基或下文定义的 R3、氧、硫、SO 或 SO2； R，是氢或 C1-6 烷基；和 R2 是 CN、CR5R6Y（其中 Rs 和 R6 独立选自氢和 C1-4 烷基）和 Y（选自氢、OR 或 SR），其中 R7 是氢、C1-4 烷基或 C2-4 烷酰基，和 NR8R9（其中 R8 和 R9 独立是氢、C1-4 烷基、C 2.4 烯基或 C2-4 烷酰基）或一起是 C 4-6 聚亚甲基，或 COR10（其中 R，o 是 C1-4 烷基），条件是当 R，是氢时，Y 不是氢； 或 R2 是氢、C1-6 烷基或任选被卤素、CF3、C1-4 烷氧基或 C1-4 烷基取代的苯基；且 R 是 CN、CR5R6Y 或 COR10，如上文对 R2 所定义； 或 R1 和 R2 共同形成任选被 C1-C4 烷基取代的 C3-C6 聚亚甲基； R3是C1-10烷基或C3-10环烷基，任选被羟基、C1-4烷氧基、硫醇、C1-4烷硫基或NR11R12取代，其中R,,和R12独立地是氢、C1-6烷基或C 2-7烷酰基，或一起是C3.6聚亚甲基；C2-10烯基；或可选被卤素、CF、C1-4烷氧基、C1-4烷基、羟基、硝基、氰基、C2-10酰氧基、NR13R14（其中R13和R14独立地选自氢、C1-6烷基、C2-7烷酰基或C1-6烷基磺酰基）或COR15（其中R15是羟基、C1-6烷氧基或NR16R17（其中R16和R,7独立地选自氢或C1-6烷基）或与R一起是C 4-6聚亚甲基中的一个或两个取代的苯基）取代的苯基。 R4 是氢；或 C1-4 烷基或苄基，可选择在苯环上被卤素、CF3、C1-4 烷氧基或 C1-4 烷基中的一个或两个取代，并连接在氮原子 1 或 2 上。