7-氯-5-甲基-1H-吡唑并[4,3-b]吡啶-3-胺 | 113140-14-0

• 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: 7-氯-5-甲基-1H-吡唑并[4,3-b]吡啶-3-胺
• 英文名称: 3-amino-7-chloro-5-methyl-1H-pyrazolo[4,3-b]pyridine
• 英文别名: 7-Chloro-5-methyl-1H-pyrazolo[4,3-b]pyridin-3-amine
• CAS: 113140-14-0
• 化学式: C₇H₇ClN₄
• 分子量: 182.612
• InChiKey: SDUXEFIOARHCOA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  67.6
• 氢给体数：
  2
• 氢受体数：
  3

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  7-氯-5-甲基-1H-吡唑并[4,3-b]吡啶-3-胺 、 硫酸 在 sodium nitrite 作用下， 以 水 为溶剂， 生成 7-Chloro-3-diazo-5-methyl-pyrazolo[4,3-b]pyridine
  参考文献：
  名称：

  Pharmaceutically useful pyrazolo[4,3-b]pyridines

  摘要：

  化合物的公式（I）或其盐或溶剂化物：## STR1 ##其中：R.sub.0是氢或C.sub.1-6烷基；或与R.sub.3一起是C.sub.4-6聚亚甲基；R.sub.1和R.sub.2都是氢；或R.sub.1是氢，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烷基或C.sub.2-4烷酰基，以及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，或一起是C.sub.4-6聚亚甲基；或COR.sub.10，其中R.sub.10是OH或C.sub.1-4烷基，或COR.sub.10是药学上可接受的酯或酰胺，或R.sub.2是氢，C.sub.1-6烷基或苯，可选择地被卤素，CF.sub.3，C.sub.1-4烷氧基或C.sub.1-4烷基置换，而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，可选择地被C.sub.1-C.sub.4烷基置换；R.sub.3是氢；或C.sub.1-10烷基或C.sub.3-10环烷基，任选地被羟基，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烷酰基，或一起是C.sub.3-6聚亚甲基；C.sub.2-10烯基；或苯，可选择地被卤素，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烷基或C.sub.2-7烷酰基；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R.sub.3是具有芳香环中最多十个原子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，除了含有碱性氮的基团，可选择地被一或两个取代基取代，所述取代基选择自卤素，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.23R.sub.24，其中R.sub.23和R.sub.24独立选择自氢，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.25，其中R.sub.25是羟基，C.sub.1-6烷氧基或NR.sub.26R.sub.27，其中R.sub.26和R.sub.27独立选择自氢或C.sub.1-6烷基；R.sub.4是氢，或C.sub.1-4烷基，苯基或苄基，其中每个在苯环中选择自卤素，CF.sub.3，C.sub.1-4烷氧基或C.sub.1-4烷基并附加在氮原子1或2处；而R.sub.x是C.sub.1-6烷基，卤素，硝基，NR.sub.18R.sub.19，其中R.sub.18和R.sub.19独立选择自氢，C.sub.1-6烷基或C.sub.2-7烷酰基，腈，COOH，CONH.sub.2；苯或苄，可选择地被一或两个卤素，硝基，C.sub.1-6烷氧基，羟基，C.sub.2-7烷酰氧基，NR.sub.18R.sub.19，C.sub.1-6烷基，CF.sub.3，CN取代；噻吩基，呋喃基或吡咯基，可选地N-取代C.sub.1-6烷基，但R.sub.1为氢且R.sub.2和R.sub.x为甲基时，R.sub.0和R.sub.3不能同时为氢，该化合物对于治疗炎症或过敏症状是有用的。

  公开号：

  US04833136A1
• 作为产物：
  描述：

  ammonium sulfate 、 7-Chloro-5-methyl-3-nitro-1H-pyrazolo[4,3-b]pyridine 、 铁粉 、 iron(II) sulfate 在 sodium hydroxide 、 硫酸 作用下， 以 甲醇 、 乙醇 、 水 为溶剂， 生成 7-氯-5-甲基-1H-吡唑并[4,3-b]吡啶-3-胺
  参考文献：
  名称：

  Pharmaceutically useful pyrazolo[4,3-b]pyridines

  摘要：

  化合物的公式（I）或其盐或溶剂化物：## STR1 ##其中：R.sub.0是氢或C.sub.1-6烷基；或与R.sub.3一起是C.sub.4-6聚亚甲基；R.sub.1和R.sub.2都是氢；或R.sub.1是氢，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烷基或C.sub.2-4烷酰基，以及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，或一起是C.sub.4-6聚亚甲基；或COR.sub.10，其中R.sub.10是OH或C.sub.1-4烷基，或COR.sub.10是药学上可接受的酯或酰胺，或R.sub.2是氢，C.sub.1-6烷基或苯，可选择地被卤素，CF.sub.3，C.sub.1-4烷氧基或C.sub.1-4烷基置换，而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，可选择地被C.sub.1-C.sub.4烷基置换；R.sub.3是氢；或C.sub.1-10烷基或C.sub.3-10环烷基，任选地被羟基，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烷酰基，或一起是C.sub.3-6聚亚甲基；C.sub.2-10烯基；或苯，可选择地被卤素，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烷基或C.sub.2-7烷酰基；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R.sub.3是具有芳香环中最多十个原子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，除了含有碱性氮的基团，可选择地被一或两个取代基取代，所述取代基选择自卤素，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.23R.sub.24，其中R.sub.23和R.sub.24独立选择自氢，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.25，其中R.sub.25是羟基，C.sub.1-6烷氧基或NR.sub.26R.sub.27，其中R.sub.26和R.sub.27独立选择自氢或C.sub.1-6烷基；R.sub.4是氢，或C.sub.1-4烷基，苯基或苄基，其中每个在苯环中选择自卤素，CF.sub.3，C.sub.1-4烷氧基或C.sub.1-4烷基并附加在氮原子1或2处；而R.sub.x是C.sub.1-6烷基，卤素，硝基，NR.sub.18R.sub.19，其中R.sub.18和R.sub.19独立选择自氢，C.sub.1-6烷基或C.sub.2-7烷酰基，腈，COOH，CONH.sub.2；苯或苄，可选择地被一或两个卤素，硝基，C.sub.1-6烷氧基，羟基，C.sub.2-7烷酰氧基，NR.sub.18R.sub.19，C.sub.1-6烷基，CF.sub.3，CN取代；噻吩基，呋喃基或吡咯基，可选地N-取代C.sub.1-6烷基，但R.sub.1为氢且R.sub.2和R.sub.x为甲基时，R.sub.0和R.sub.3不能同时为氢，该化合物对于治疗炎症或过敏症状是有用的。

  公开号：

  US04833136A1

文献信息

• Pyrazolo[4,3-b]pyridine derivatives, process for their preparation and pharmaceutical compositions containing them
  申请人：BEECHAM GROUP PLC

  公开号：EP0239191A2

  公开（公告）日：1987-09-30

  A compound of the formula (I) or a salt or solvate thereof: in which: R₀ is hydrogen or C1-6 alkyl; or together with R₃ is C4-6 polymethylene; R₁ and R₂ are both hydrogen; or R₁ is hydrogen, C1-6 alkyl; and R₂ is CN; CR₅R₆Y where R₅ and R₆ are independently selected from hydrogen and C1-4 alkyl and Y is selected from hydrogen, OR₇ or SR₇ where R₇ is hydrogen, C1-4 alkyl or C2-4 alkanoyl, and NR₈R₉ where R₈ and R₉ are independently hydrogen, C1-4 alkyl, C2-4 alkenyl or C2-4 alkanoyl or together are C4-6 polymethylene; or COR₁₀ where R₁₀ is OH or C1-4 alkyl, or COR₁₀ is a pharmaceutically acceptable ester or amide, or R₂ is hydrogen, C1-6 alkyl, or phenyl optionally substituted by halogen, CF₃, C1-4 alkoxy or C1-4 alkyl, and R₁ 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 hydrogen; or C1-10 alkyl or C3-10 cycloalkyl, either optionally substituted by hydroxy, C1-4 alkoxy, thiol, C1-4 alkylthio or NR₁₁R₁₂ wherein R₁₁ and R₁₂ are independently hydrogen, C1-6 alkyl or C2-7 alkanoyl or together are C3-6 polymethylene; 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, NR₁₃R₁₄ wherein R₁₃ and R₁₄ are independently selected from hydrogen, C1-6 alkyl, or C2-7 alkanoyl; or COR₁₅ wherein R₁₅ is hydroxy, C1-6 alkoxy or NR₁₆R₁₇ wherein R₁₆ and R₁₇ are independently selected from hydrogen or C1-6 alkyl; or R₃ is 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, CF₃, C1-4 alkoxy, C1-4 alkyl, hydroxy, nitro, cyano, C2-10 acyloxy, NR₂₃R₂₄ wherein R₂₃ and R₂₄ are independently selected from hydrogen, C1-6 alkyl, C2-7 alkanoyl or C1-6 alkylsulphonyl; or COR₂₅ wherein R₂₅ is hydroxy, C1-6 alkoxy or NR₂₆ R₂₇ wherein R₂₆ and R₂₇ are independently selected from hydrogen or C1-6 alkyl; R₄ is hydrogen, or C1-4 alkyl, phenyl or benzyl, each of which is 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 l or 2; and Rx is C1-6 alkyl, halogen, nitro, NR₁₈R₁₉ where R₁₈ and R₁₉ are independently hydrogen, C1-6 alkyl or C2-7 alkanoyl, nitrile, COOH, CONH₂; phenyl or benzyl optionally substituted by one or two of halogen, nitro, C1-6 alkoxy, hydroxy, C2-7 alkanoyloxy, NR₁₈R₁₉, C1-6 alkyl, CF₃, CN; thienyl, furyl or pyrryl optionally N-substituted by C1-6 alkyl, with the proviso that R₀ and R₃ are not both hydrogen when R₁ is hydrogen and R₂ and Rx are methyl, is useful for treating inflammatory or allergic conditions.

  式 (I) 的化合物或其盐或溶液： 其中 R₀ 是氢或 C1-6 烷基；或与 R₃ 一起是 C4-6 聚亚甲基； R₁ 和 R₂ 都是氢； 或 R₁ 是氢、C1-6 烷基；R₂ 是 CN；CR₅R₆Y 其中 R₅ 和 R₆ 独立选自氢和 C1-4 烷基，Y 选自氢、OR₇ 或 SR₇ 其中 R₇ 是氢、C1-4烷基或C2-4烷酰基，以及 NR₈R₉，其中 R₈ 和 R𠢙 独立地为氢、C1-4烷基、C2-4烯基或C2-4烷酰基，或共同为 C4-6 聚亚甲基；或 COR₁₀，其中 R₁₀ 是 OH 或 C1-4 烷基，或 COR₁₀ 是药学上可接受的酯或酰胺、 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 R₁ 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是氢；或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R₁₁和R₁₂独立地是氢、C1-6烷基或C2-7烷酰基，或共同形成C3-6聚亚甲基；C2-10烯基；或任选被卤素、CF₃、C1-4 烷氧基、C1-4 烷基、羟基、硝基、氰基、C2-10 乙酰氧基、NR₁₃R₁₄ 中的一个或两个取代的苯基，其中 R₁₃ 和 R₁₄ 独立选自氢、C1-6 烷基或 C2-7 烷酰基；或 COR₁₅，其中 R₁₅ 是羟基、C1-6 烷氧基或 NR₁₆R₁₇，其中 R₁₆ 和 R₁₇ 独立选自氢或 C1-6 烷基； 或 R₃是单环或融合双环杂芳基，在芳香环中最多有十个原子，其中不超过两个原子选自氮、氧或硫，但含碱基氮的杂芳基除外、可任选被一个或两个取代基取代，这些取代基选自卤素、CF₃、C1-4 烷氧基、C1-4 烷基、羟基、硝基、氰基、C2-10 乙酰氧基、NR₂₃R₂₄，其中 R₂₃ 和 R₂₄ 独立选自氢、C1-6 烷基、C2-7 烷酰基或 C1-6 烷基磺酰基；或 COR₂₅ 其中 R₂₅ 是羟基、C1-6 烷氧基或 NR₂₆ R₂₇ 其中 R₂₆ 和 R₂₇ 独立选自氢或 C1-6 烷基； R₄是氢、或C1-4烷基、苯基或苄基，其中每个苯基环可选择被卤素、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l或2上；和 Rx 是 C1-6 烷基、卤素、硝基、NR₁₈R₁₉，其中 R₁₈ 和 R₁₉ 独立地是氢、C1-6 烷基或 C2-7 烷酰基、腈、COOH、CONH₂；任选被卤素、硝基、C1-6 烷氧基、羟基、C2-7 烷酰氧基、NR₁₈R₁₉、C1-6 烷基、CF₃、CN 中的一个或两个取代的苯基或苄基；任选被 C1-6 烷基 N-取代的噻吩基、呋喃基或吡喃基、 当 R₁ 为氢、R₂ 和 Rx 为甲基时，R₀ 和 R₃ 不能都是氢。
• US4833136A
  申请人：——

  公开号：US4833136A

  公开（公告）日：1989-05-23
• Pharmaceutically useful pyrazolo[4,3-b]pyridines
  申请人：Beecham Group p.l.c.

  公开号：US04833136A1

  公开（公告）日：1989-05-23

  A compound of the formula (I) or a salt or solvate thereof: ##STR1## in which: R.sub.0 is hydrogen or C.sub.1-6 alkyl; or together with R.sub.3 is C.sub.4-6 polymethylene; 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 is hydrogen; or 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, or C.sub.2-7 alkanoyl; 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 R.sub.3 is 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.23 R.sub.24 wherein R.sub.23 and R.sub.24 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkanoyl or C.sub.1-6 alkylsulphonyl; or COR.sub.25 wherein R.sub.25 is hydroxy, C.sub.1-6 alkoxy or NR.sub.26 R.sub.27 wherein R.sub.26 and R.sub.27 are independently selected from hydrogen or C.sub.1-6 alkyl; R.sub.4 is hydrogen, or C.sub.1-4 alkyl, phenyl or benzyl, each of which is 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; and R.sub.x is C.sub.1-6 alkyl, halogen, nitro, NR.sub.18 R.sub.19 where R.sub.18 and R.sub.19 are independently hydrogen, C.sub.1-6 alkyl or C.sub.2-7 alkanoyl, nitrile, COOH, CONH.sub.2 ; phenyl or benzyl optionally substituted by one or two of halogen, nitro, C.sub.1-6 alkoxy, hydroxy, C.sub.2-7 alkanoyloxy, NR.sub.18 R.sub.19, C.sub.1-6 alkyl, CF.sub.3, CN; thienyl, furyl or pyrryl optinoally N-substituted by C.sub.1-6 alkyl, with the proviso that R.sub.0 and R.sub.3 are not both hydrogen when R.sub.1 is hydrogen and R.sub.2 and R.sub.x are methyl, is useful for treating inflammatory or allergic conditions.

  化合物的公式（I）或其盐或溶剂化物：## STR1 ##其中：R.sub.0是氢或C.sub.1-6烷基；或与R.sub.3一起是C.sub.4-6聚亚甲基；R.sub.1和R.sub.2都是氢；或R.sub.1是氢，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烷基或C.sub.2-4烷酰基，以及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，或一起是C.sub.4-6聚亚甲基；或COR.sub.10，其中R.sub.10是OH或C.sub.1-4烷基，或COR.sub.10是药学上可接受的酯或酰胺，或R.sub.2是氢，C.sub.1-6烷基或苯，可选择地被卤素，CF.sub.3，C.sub.1-4烷氧基或C.sub.1-4烷基置换，而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，可选择地被C.sub.1-C.sub.4烷基置换；R.sub.3是氢；或C.sub.1-10烷基或C.sub.3-10环烷基，任选地被羟基，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烷酰基，或一起是C.sub.3-6聚亚甲基；C.sub.2-10烯基；或苯，可选择地被卤素，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烷基或C.sub.2-7烷酰基；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R.sub.3是具有芳香环中最多十个原子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，除了含有碱性氮的基团，可选择地被一或两个取代基取代，所述取代基选择自卤素，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.23R.sub.24，其中R.sub.23和R.sub.24独立选择自氢，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.25，其中R.sub.25是羟基，C.sub.1-6烷氧基或NR.sub.26R.sub.27，其中R.sub.26和R.sub.27独立选择自氢或C.sub.1-6烷基；R.sub.4是氢，或C.sub.1-4烷基，苯基或苄基，其中每个在苯环中选择自卤素，CF.sub.3，C.sub.1-4烷氧基或C.sub.1-4烷基并附加在氮原子1或2处；而R.sub.x是C.sub.1-6烷基，卤素，硝基，NR.sub.18R.sub.19，其中R.sub.18和R.sub.19独立选择自氢，C.sub.1-6烷基或C.sub.2-7烷酰基，腈，COOH，CONH.sub.2；苯或苄，可选择地被一或两个卤素，硝基，C.sub.1-6烷氧基，羟基，C.sub.2-7烷酰氧基，NR.sub.18R.sub.19，C.sub.1-6烷基，CF.sub.3，CN取代；噻吩基，呋喃基或吡咯基，可选地N-取代C.sub.1-6烷基，但R.sub.1为氢且R.sub.2和R.sub.x为甲基时，R.sub.0和R.sub.3不能同时为氢，该化合物对于治疗炎症或过敏症状是有用的。