2-氯-5-叔丁氧羰基氨基-4-吡啶甲酸甲酯 | 305371-42-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 2-氯-5-叔丁氧羰基氨基-4-吡啶甲酸甲酯
• 英文名称: methyl 5-((tert-butoxycarbonyl)amino)-2-chloroisonicotinate
• 英文别名: 5-tert-butoxycarbonylamino-2-chloro-isonicotinic acid, methyl ester；Methyl 5-(boc-amino)-2-chloropyridine-4-carboxylate；methyl 2-chloro-5-[(2-methylpropan-2-yl)oxycarbonylamino]pyridine-4-carboxylate
• CAS: 305371-42-0
• 化学式: C₁₂H₁₅ClN₂O₄
• 分子量: 286.715
• InChiKey: JYUMVTMXTSYJOG-UHFFFAOYSA-N

物化性质

• 沸点：
  357.4±42.0 °C(Predicted)
• 密度：
  1.294±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  77.5
• 氢给体数：
  1
• 氢受体数：
  5

安全信息

• 海关编码：
  2933399090

反应信息

• 作为反应物：
  描述：

  2-氯-5-叔丁氧羰基氨基-4-吡啶甲酸甲酯 在 盐酸 、 N,N-二异丙基乙胺 、 三氯氧磷 作用下， 以 甲醇 、 水 、 乙酸乙酯 为溶剂， 反应 57.58h， 生成 N-(2-(benzylsulfonyl)ethyl)-6-chloro-2-(4-methylpiperazin-1-yl)pyrido[3,4-d]pyrimidin-4-amine
  参考文献：
  名称：

  [EN] PYRIDOPYRIMIDINES AS HISTAMINE H4-RECEPTOR INHIBITORS
  [FR] PYRIDOPYRIMIDINES EN TANT QU'INHIBITEURS DU RÉCEPTEUR H4 DE L'HISTAMINE

  摘要：

  该发明涉及式(I)的化合物或其药用可接受的盐或溶剂，以及包含它们的药物组合物，以及它们在治疗和/或预防由组胺H4受体介导的疾病或疾病中的用途。

  公开号：

  WO2020020939A1
• 作为产物：
  描述：

  5-(N-叔丁氧羰基氨基)-2-氯吡啶 在 正丁基锂 、 四甲基乙二胺 、 三甲基硅烷化重氮甲烷 作用下， 以 四氢呋喃 、 正己烷 、 二氯甲烷 为溶剂， -78.0~20.0 ℃ 、206.85 kPa 条件下， 反应 18.0h， 生成 2-氯-5-叔丁氧羰基氨基-4-吡啶甲酸甲酯
  参考文献：
  名称：

  [EN] 3-CYANO-QUINOLINE DERIVATIVES AND USES THEREOF
  [FR] DÉRIVÉS DE 3-CYANO-QUINOLÉINE ET LEURS UTILISATIONS

  摘要：

  本公开涉及公式（I）的化合物及其药学上可接受的盐和立体异构体，其在治疗与ErbB致癌活性相关的癌症方面具有用途，包括制备化合物的方法，包含化合物的组合物以及使用化合物的方法（例如，用于治疗癌症）。

  公开号：

  WO2022266425A1

文献信息

• Combination therapy with CHK1 inhibitors
  申请人：Gesner G. Thomas

  公开号：US20050256157A1

  公开（公告）日：2005-11-17

  Compounds of Structure I, and salts, tautomers, stereoisomers, and mixtures thereof may be used in methods of inhibiting checkpoint kinase 1 in subjects, in methods for inducing cell cycle progression, and in methods for increasing apoptosis in cells. Such compounds may be used to prepare pharmaceutical compositions and may be used in conjunction with DNA damaging agents.

  结构I的化合物及其盐类、互变异构体、立体异构体和混合物可用于抑制受试者中的检查点激酶1，用于诱导细胞周期进展的方法，以及用于增加细胞凋亡的方法。这些化合物可用于制备药物组合物，并且可以与DNA损伤剂联合使用。
• Inhibition of FGFR3 and treatment of multiple myeloma
  申请人：Cai Shaopei

  公开号：US20050261307A1

  公开（公告）日：2005-11-24

  Methods of inhibiting fibroblast growth factor receptor 3 and treating various conditions mediated by fibroblast growth factor receptor 3 are provided that include administering to a subject a compound of Structure I, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I have the following structure where and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting fibroblast growth factor receptor 3 and for use in treating conditions mediated by fibroblast growth factor receptor 3 such as multiple myeloma.

  提供了抑制成纤维母细胞生长因子受体3并治疗由纤维母细胞生长因子受体3介导的各种疾病的方法，包括向受试者施用结构I的化合物，其药学上可接受的盐，其互变异构体，或其互变异构体的药学上可接受的盐。具有结构I的化合物具有以下结构，其中具有本文描述的变量。这些化合物可用于制备用于抑制纤维母细胞生长因子受体3和用于治疗由纤维母细胞生长因子受体3介导的疾病，如多发性骨髓瘤的药物。
• Substituted 3-cyano-[1.7],[1.5], and [1.8] naphthyridine inhibitors of tyrosine kinases
  申请人：American Cyanamid Company

  公开号：US06355636B1

  公开（公告）日：2002-03-12

  This invention provides compounds of formula I having the structure useful as inhibitors of protein tyrosine kinase.

  这项发明提供了具有结构的化合物，可作为蛋白酪氨酸激酶抑制剂。
• Benzimidazole quinolinones and uses thereof
  申请人：Chiron Corporation

  公开号：US20040092535A1

  公开（公告）日：2004-05-13

  Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes. 1

  提供了抑制各种酶和治疗各种疾病的方法，包括向受试者给予结构式I或IB的化合物、其药学上可接受的盐、其互变异构体或其药学上可接受的互变异构体盐。具有结构式I和IB的化合物具有以下结构，并具有此处描述的变量。这些化合物可用于制备药物，用于抑制各种酶的使用和用于治疗由这些酶介导的疾病。
• Substituted 3-cyano-[1.7], [1.5], and [1.8] naphthyridine inhibitors of tyrosine kinases
  申请人：American Cyanamid Company

  公开号：US20020165229A1

  公开（公告）日：2002-11-07

  This invention provides compounds of formula I having the structure 1 wherein: X is cycloalkyl of 3 to 7 carbon atoms, which may be optionally substituted with one or more alkyl of 1 to 6 carbon atom groups; or X is pyridinyl, pyrimidinyl, or Ph; or X is a bicyclic aryl or bicyclic heteroaryl ring system of 8 to 12 atoms, where the bicyclic heteroaryl ring contains 1 to 4 heteroatoms selected from N, O, and S; wherein the bicyclic aryl or bicyclic heteroaryl ring may be optionally mono-, di-, tri-, or tetra-substituted with a substituent selected from the group consisting of halogen, oxo, thio, alkyl of 1-6 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, azido, hydroxyalkyl of 1-6 carbon atoms, halomethyl, alkoxymethyl of 2-7 carbon atoms, alkanoyloxymethyl of 2-7 carbon atoms, alkoxy of 1-6 carbon atoms, alkylthio of 1-6 carbon atoms, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy of 2-7 carbon atoms, carboalkyl of 2-7 carbon atoms, phenoxy, phenyl, thiophenoxy, benzoyl, benzyl, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 2 to 12 carbon atoms, phenylamino, benzylamino, alkanoylamino of 1-6 carbon atoms, alkenoylamino of 3-8 carbon atoms, alkynoylamino of 3-8 carbon atoms, carboxyalkyl of 2-7 carbon atoms, carboalkoxyalkyl of 3-8 carbon atoms, aminoalkyl of 1-5 carbon atoms, N-alkylaminoalkyl of 2-9 carbon atoms, N,N-dialkylaminoalkyl of 3-10 carbon atoms, N-alkylaminoalkoxy of 2-9 carbon atoms, N,N-dialkylaminoalkoxy of 3-10 carbon atoms, mercapto, methylmercapto, and benzoylamino; or X is the radical 2 ; E is pyridinyl, pyrimidinyl, or Ph; T is substituted on E at carbon and is —NH(CH 2 ) m —, —O(CH 2 ) m —, —S(CH 2 ) m —, —NR(CH 2 ) m —, —(CH 2 ) m —(CH 2 ) m NH—, —(CH 2 ) m O—, —(CH 2 ) m S—, or —(CH 2 ) m NR—; L is a Ph; or L is a 5- or 6-membered heteroaryl ring where the heteroaryl ring contains 1 to 3 heteroatoms selected from N, O, and S; wherein the heteroaryl ring may be optionally mono- or di-substituted with a substituent selected from the group consisting of halogen, oxo, thio, alkyl of 1-6 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, azido, hydroxyalkyl of 1-6 carbon atoms, halomethyl, alkoxymethyl of 2-7 carbon atoms, alkanoyloxymethyl of 2-7 carbon atoms, alkoxy of 1-6 carbon atoms, alkylthio of 1-6 carbon atoms, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy of 2-7 carbon atoms, carboalkyl of 2-7 carbon atoms, phenoxy, phenyl, thiophenoxy, benzoyl, benzyl, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 2 to 12 carbon atoms, phenylamino, benzylamino, alkanoylamino of 1-6 carbon atoms, alkenoylamino of 3-8 carbon atoms, alkynoylamino of 3-8 carbon atoms, carboxyalkyl of 2-7 carbon atoms, carboalkoxyalkyl of 3-8 carbon atoms, aminoalkyl of 1-5 carbon atoms, N-alkylaminoalkyl of 2-9 carbon atoms, N,N-dialkylaminoalkyl of 3-10 carbon atoms, N-alkylaminoalkoxy of 2-9 carbon atoms, N,N-dialkylaminoalkoxy of 3-10 carbon atoms, mercapto, methylmercapto, and benzoylamino; Pyridinyl, pyrimidinyl, or Ph are pyridinyl, pyrimidinyl, or phenyl radicals, respectively, which may be optionally mono- di-, or tri-substituted with a substituent selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, azido, hydroxyalkyl of 1-6 carbon atoms, halomethyl, alkoxymethyl of 2-7 carbon atoms, alkanoyloxymethyl of 2-7 carbon atoms, alkoxy of 1-6 carbon atoms, alkylthio of 1-6 carbon atoms, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy of 2-7 carbon atoms, carboalkyl of 2-7 carbon atoms, benzoyl, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 2 to 12 carbon atoms, alkanoylamino of 1-6 carbon atoms, alkenoylamino of 3-8 carbon atoms, alkynoylamino of 3-8 carbon atoms, carboxyalkyl of 2-7 carbon atoms, carboalkoxyalkyl of 3-8 carbon atoms, aminoalkyl of 1-5 carbon atoms, N-alkylaminoalkyl of 2-9 carbon atoms, N,N-dialkylaminoalkyl of 3-10 carbon atoms, N-alkylaminoalkoxy of 2-9 carbon atoms, N,N-dialkylaminoalkoxy of 3-10 carbon atoms, mercapto, methylmercapto, and benzoylamino; Z is —NH—, —O—, —S—, or —NR—; R is alkyl of 1-6 carbon atoms, or carboalkyl of 2-7 carbon atoms; A″ is a diavalent moiety selected from the group 3 G 1 , G 2 , G 3 , and G 4 are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, alkenyloxy of 2-6 carbon atoms, alkynyloxy of 2-6 carbon atoms, hydroxymethyl, halomethyl, alkanoyloxy of 2-6 carbon atoms, alkenoyloxy of 3-8 carbon atoms, alkynoyloxy of 3-8 carbon atoms, alkanoyloxymethyl of 2-7 carbon atoms, alkenoyloxymethyl of 49 carbon atoms, alkynoyloxymethyl of 49 carbon atoms, alkoxymethyl of 2-7 carbon atoms, alkoxy of 1-6 carbon atoms, alkylthio of 1-6 carbon atoms, alkylsulphinyl of 1-6 carbon atoms, alkylsulphonyl of 1-6 carbon atoms, alkylsulfonamido of 1-6 carbon atoms, alkenylsulfonamido of 2-6 carbon atoms, alkynylsulfonamido of 2-6 carbon atoms, hydroxy, trifluoromethyl, trifluoromethoxy, cyano, nitro, carboxy, carboalkoxy of 2-7 carbon atoms, carboalkyl of 2-7 carbon atoms, phenoxy, phenyl, thiophenoxy, benzyl, amino, hydroxyamino, alkoxyamino of 1-4 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 2 to 12 carbon atoms, N-alkylcarbamoyl, N,N-dialkylcarbamoyl, N-alkyl-N-alkenylamino of 4 to 12 carbon atoms, N,N-dialkenylamino of 6-12 carbon atoms, phenylamino, benzylamino, R 2 NH, 4 R 7 —(C(R 6 ) 2 ) g —Y—, R 7 —(C(R 6 ) 2 ) p —M—(C(R 6 ) 2 ) k —Y—, Het-(C(R 6 ) 2 ) q —W—(C(R 6 ) 2 ) k —Y—, with the proviso that G 3 and G 4 are not R 2 NH; Y is a divalent radical selected from the group consisting of 5 R 7 is —NR 6 R 6 , —OR 6 , —J, —N(R 6 ) 3 + , or —NR 6 (OR 6 ); M is >NR 6 , —O—, >N—(C(R 6 ) 2 ) p NR 6 R 6 , or >N—(C(R 6 ) 2 ) p —OR 6 ; W is >NR 6 , —O— or is a bond; Het is a heterocyclic radical selected from the group consisting of morpholine, thiomorpholine, thiomorpholine S-oxide, thiomorpholine S,S-dioxide, piperidine, pyrrolidine, aziridine, pyridine, imidazole, 1,2,3-triazole, 1,2,4-triazole, thiazole, thiazolidine, tetrazole, piperazine, furan, thiophene, tetrahydrothiophene, tetrahydrofuran, dioxane, 1,3-dioxolane, tetrahydropyran, and 6 which may be optionally mono- or di-substituted on carbon with R 6 , hydroxy, —N(R 6 ) 2 , —OR 6 —(C(R 6 ) 2 ) s OR 6 or —(C(R 6 ) 2 ) s N(R 6 ) 2 ; optionally mono-substituted on nitrogen with R 6 ; and optionally mono or di-substituted on a saturated carbon with divalent radicals —O— or —O(C(R 6 ) 2 ) s O—; R 6 is hydrogen, alkyl of 1-6 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, cycloalkyl of 1-6 carbon atoms, carboalkyl of 2-7 carbon atoms, carboxyalkyl 2-7 carbon atoms, phenyl, or phenyl optionally substituted with one or more halogen, alkoxy of 1-6 carbon atoms, trifluoromethyl, amino, alkylamino of 1-3 carbon atoms, dialkylamino of 2-6 carbon atoms, nitro, cyano, azido, halomethyl, alkoxymethyl of 2-7 carbon atoms, alkanoyloxymethyl of 2-7 carbon atoms, alkylthio of 1-6 carbon atoms, hydroxy, carboxyl, carboalkoxy of 2-7 carbon atoms, phenoxy, phenyl, thiophenoxy, benzoyl, benzyl, phenylamino, benzylamino, alkanoylamino of 1-6 carbon atoms, or alkyl of 1-6 carbon atoms; with the proviso that the alkenyl or alkynyl moiety is bound to a nitrogen or oxygen atom through a saturated carbon atom; R 2 , is selected from the group consisting of 7 R 3 is hydrogen, alkyl of 1-6 carbon atoms, carboxy, carboalkoxy of 1-6 carbon atoms, phenyl, carboalkyl of 2-7 carbon atoms, 8 , R 7 —(C(R) 2 ) s —, R 7 —(C(R 6 ) 2 ) p —M—(C(R 6 ) 2 ) r —, R 8 R 9 —CH—M(C(R 6 ) 2 ) r —, or Het-(C(R 6 ) 2 ) q —W—C(R 6 ) 2 ) r —; R 5 is hydrogen, alkyl of 1-6 carbon atoms, carboxy, carboalkoxy of 1-6 carbon atoms, phenyl, carboalkyl of 2-7 carbon atoms, 9 , R 7 —(C(R 6 ) 2 ) s —, R 7 —(C(R 6 ) 2 ) p —M—(C(R 6 ) 2 ) r —, R 8 R 9 —CH—M—(C(R 6 ) 2 ) r —, or Het-(C(R 6 ) 2 ) q —W—(C(R 6 ) 2 ) r —; R 8 , and R 9 are each, independently, —(C(R 6 ) 2 ) r NR 6 R 6 , or —(C(R 6 ) 2 ) r OR 6 ; J is independently hydrogen, chlorine, fluorine, or bromine; Q is alkyl of 1-6 carbon atoms or hydrogen; a=0-1; g=1-6; k=0-4; n is 0-1; m is 0-3; p=2-4; q=0-4; r=1-4; s=1-6; u=0-4 and v=0-4, wherein the sum of u+v is 2-4; or a pharmaceutically acceptable salt thereof, provided that when R 6 is alkenyl of 2-7 carbon atoms or alynyl of 2-7 carbon atoms, such alkenyl or alynyl moiety is bound to a nitrogen or oxygen atom through a saturated carbon atom; and provided that when R 3 is bound to sulfur, it cannot be hydrogen, carboxy, carboalkoxy, or carboalkyl; and provided that when Y is —NR 6 — and R 7 is —NR 6 R 6 , —N(R 6 ) 3 + , or —NR 6 (OR 6 ), then g=2-6; when M is —O— and R 7 is —OR 6 then p=1-4; when Y is —NR 6 — then k=2-4; when Y is —O— and M or W is —O— then k=1-4 when W is not a bond with Het bonded through a nitrogen atom then q=2-4 and when W is a bond with Het bonded through a nitrogen atom and Y is —O— or —NR6— then k=2-4; and finally provided that when A″ is the moiety 10 n=0, Z is NH, G 1 is hydrogen, halogen, alkyl, alkoxy, hydroxy, alkanoyloxy of 2-6 carbon atoms, or phenoxy, and G 2 is hydrogen, halogen, alkyl, hydroxy, carboxyalkyl, carboalkoxyalkyl, hydroxyalkyl, alkoxy,halomethyl, carboxyl, carboalkoxy, alkanoylamino, or alkenoylamino, then X can not be a pyridinyl, pyrimidinyl, or phenyl ring that is substituted with a hydroxy or alkoxy group, which are useful as inhibitors of protein tyrosine kinase.

  本发明提供了具有以下结构的公式I的化合物：其中：X是3到7个碳原子的环烷基，可以选择地用1到6个碳原子的烷基取代；或者X是吡啶基、嘧啶基或苯基；或者X是8到12个原子的双环芳基或双环杂芳基环系，其中双环杂芳基环含有1到4个从N、O和S中选择的杂原子；其中双环芳基或双环杂芳基环可以选择地单、双、三或四取代，取代基选择自卤素、氧代、硫代、1-6个碳原子的烷基、2-6个碳原子的烯基、2-6个碳原子的炔基、偶氮基、1-6个碳原子的羟基烷基、卤代甲基、2-7个碳原子的烷氧甲基、2-7个碳原子的烷酰氧甲基、1-6个碳原子的烷氧基、1-6个碳原子的烷硫基、羟基、三氟甲基、氰基、硝基、羧基、2-7个碳原子的羧酸酯基、2-7个碳原子的羧基烷基、苯氧基、苯基、噻吩氧基、苯甲酰基、苄基、氨基、1-6个碳原子的烷基氨基、2到12个碳原子的二烷基氨基、苯基氨基、苄基氨基、1-6个碳原子的烷酰氨基、3-8个碳原子的烯酰氨基、3-8个碳原子的炔酰氨基、2-7个碳原子的羧基烷基、3-8个碳原子的羧酸酯基烷基、1-5个碳原子的氨基烷基、2-9个碳原子的N-烷基氨基烷基、3-10个碳原子的N,N-二烷基氨基烷基、2-9个碳原子的N-烷基氨基烷氧基、3-10个碳原子的N,N-二烷基氨基烷氧基、巯基、甲硫基和苯甲酰氨基；或者X是基团2；E是吡啶基、嘧啶基或苯基；T在碳上被取代，为—NH(CH2)m—、—O(CH2)m—、—S(CH2)m—、—NR(CH2)m—、—(CH2)m—(CH2)mNH—、—(CH2)mO—、—(CH2)mS—或—(CH2)mNR—；L是苯基；或者L是一个5或6元杂芳基环，其中杂芳基环含有1到3个从N、O和S中选择的杂原子；其中杂芳基环可以选择地单取代或双取代，取代基选择自卤素、氧代、硫代、1-6个碳原子的烷基、2-6个碳原子的烯基、2-6个碳原子的炔基、偶氮基、1-6个碳原子的羟基烷基、卤代甲基、2-7个碳原子的烷氧甲基、2-7个碳原子的烷酰氧甲基、1-6个碳原子的烷氧基、1-6个碳原子的烷硫基、羟基、三氟甲基、氰基、硝基、羧基、2-7个碳原子的羧酸酯基、2-7个碳原子的羧基烷基、苯氧基、苯基、噻吩氧基、苯甲酰基、苄基、氨基、1-6个碳原子的烷基氨基、2到12个碳原子的二烷基氨基、苯基氨基、苄基氨基、1-6个碳原子的烷酰氨基、3-8个碳原子的烯酰氨基、3-8个碳原子的炔酰氨基、2-7个碳原子的羧基烷基、3-8个碳原子的羧酸酯基烷基、1-5个碳原子的氨基烷基、2-9个碳原子的N-烷基氨基烷基、3-10个碳原子的N,N-二烷基氨基烷基、2-9个碳原子的N-烷基氨基烷氧基、3-10个碳原子的N,N-二烷基氨基烷氧基、巯基、甲硫基和苯甲酰氨基；Pyridinyl、pyrimidinyl或Ph分别是吡啶基、嘧啶基或苯基基团，可以选择地单、双或三取代，取代基选择自卤素、1-6个碳原子的烷基、2-6个碳原子的烯基、2-6个碳原子的炔基、偶氮基、1-6个碳原子的羟基烷基、卤代甲基、2-7个碳原子的烷氧甲基、2-7个碳原子的烷酰氧甲基、1-6个碳原子的烷氧基、1-6个碳原子的烷硫基、羟基、三氟甲基、氰基、硝基、羧基、2-7个碳原子的羧酸酯基、2-7个碳原子的羧基烷基、苯甲酰基、氨基、1-6个碳原子的烷基氨基、2到12个碳原子的二烷基氨基、1-6个碳原子的烷酰氨基、3-8个碳原子的烯酰氨基、3-8个碳原子的炔酰氨基、2-7个碳原子的羧基烷基、3-8个碳原子的羧酸酯基烷基、1-5个碳原子的氨基烷基、2-9个碳原子的N-烷基氨基烷基、3-10个碳原子的N,N-二烷基氨基烷基、2-9个碳原子的N-烷基氨基烷氧基、3-10个碳原子的N,N-二烷基氨基烷氧基、巯基、甲硫基和苯甲酰氨基；Z是—NH—、—O—、—S—或—NR—；R是1-6个碳原子的烷基或2-7个碳原子的羧基烷基；A″是从群体3中选择的二价基团，G1、G2、G3和G4分别独立地是氢、卤素、1-6个碳原子的烷基、2-6个碳原子的烯基、2-6个碳原子的炔基、2-6个碳原子的烯氧基、2-6个碳原子的炔氧基、羟甲基、卤代甲基、2-6个碳原子的烷酰氧基、3-8个碳原子的烯酰氧基、3-8个碳原子的炔酰氧基、2-7个碳原子的烷酰氧甲基、3-8个碳原子的烯酰氧甲基、3-8个碳原子的炔酰氧甲基、2-7个碳原子的烷氧甲基、1-6个碳原子的烷氧基、1-6个碳原子的烷硫基、1-6个碳原子的烷磺酰基、1-6个碳原子的烷磺酰胺基、2-6个碳原子的烯磺酰胺基、2-6个碳原子的炔磺酰胺基、羟基、三氟甲基、三氟甲氧基、氰基、硝基、羧基、2-7个碳原子的羧酸酯基、2-7个碳原子的羧基烷基、苯氧基、苯基、噻吩氧基、苄基、氨基、1-4个碳原子的烷氧基、1-6个碳原子的烷基氨基、2到12个碳原子的二烷基氨基、N-烷基氨基烷基、N,N-二烷基氨基烷基、4到12个碳原子的N-烷基-N-烯基氨基、6-12个碳原子的N,N-二烯基氨基、苯基氨基、苄基氨基、R2NH、R7—(C(R6)2)g—Y—、R7—(C(R6)2)p—M—(C(R6)2)k—Y—、Het-(C(R6)2)q—W—(C(R6)2)k—；但是当R6为2-7个碳原子的烯基或炔基时，该烯基或炔基通过饱和碳原子与氮或氧原子结合；当R3与硫结合时，它不能是氢、羧基、羧酸酯基或羧基烷基；当Y是—NR6—且R7是—NR6R6、—N(R6)3+或—NR6(OR6)时，g=2-6；当M是—O—且R7是—OR6时，p=1-4；当Y是—NR6—时，k=2-4；当Y是—O—且M或W是—O—时，k=1-4；当W不是与Het通过氮原子结合的键时，q=2-4；当W是与Het通过氮原子结合的键且Y是—O—或—NR6—时，k=2-4；最后，当A″是基团10时，n=0，Z是NH，G1是氢、卤素、烷基、烷氧基、羟基、2-6个碳原子的烷酰氧基或苯氧基，G2是氢、卤素、烷基、羟基、烷基羧酸、烷氧基、卤代甲基、羧基、羧酸酯基、1-6个碳原子的烷基酰胺基或3-8个碳原子的烯基酰胺基时，X不能是带有氢氧基或烷氧基取代的吡啶基、嘧啶基或苯基环，这些化合物可用作蛋白酪氨酸激酶的抑制剂。