1,5-萘啶-3-甲腈 | 1142927-37-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 1,5-萘啶-3-甲腈
• 英文名称: [1,5]naphthyridine-3-carbonitrile
• 英文别名: 3-cyano-1,5-naphthyridine；1,5-Naphthyridine-3-carbonitrile
• CAS: 1142927-37-4
• 化学式: C₉H₅N₃
• 分子量: 155.159
• InChiKey: HVWXIFKFFMJTJB-UHFFFAOYSA-N

物化性质

• 沸点：
  341.4±22.0 °C(Predicted)
• 密度：
  1.29±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  49.6
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 危险等级：
  IRRITANT
• WGK Germany：
  3

反应信息

• 作为产物：
  描述：

  zinc(II) cyanide 、 [1,5]萘啶-3-硼酸频哪醇酯 在 copper(II) nitrate 作用下， 以 甲醇 、 水 、 N,N-二甲基甲酰胺 为溶剂， 以61%的产率得到1,5-萘啶-3-甲腈
  参考文献：
  名称：

  Chemistry informer libraries: a chemoinformatics enabled approach to evaluate and advance synthetic methods

  摘要：

  我们报告了一种标准化的复杂分子诊断方法，使用我们称之为化学信息库的相关类药物分子集合。

  DOI：

  10.1039/c5sc04751j

文献信息

• [EN] BRIDGED BICYCLIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS<br/>[FR] COMPOSÉS BICYCLIQUES PONTÉS POUR LE TRAITEMENT DES INFECTIONS BACTÉRIENNES
  申请人：KYORIN SEIYAKU KK

  公开号：WO2013003383A1

  公开（公告）日：2013-01-03

  Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.

  本文披露了新型桥环双环化合物，以及它们的药用盐、水合物和前药。还披露了包含这些化合物的组合物，制备这些化合物的方法以及将这些化合物用作抗菌剂的方法。所披露的化合物、其药用盐、水合物和前药，以及包含这些化合物、盐、水合物和前药的组合物，可用于治疗细菌感染及相关疾病和症状。
• [EN] DIHYDRONAPHTHYRIDINYL AND RELATED COMPOUNDS FOR USE IN TREATING OPHTHALMOLOGICAL DISORDERS<br/>[FR] DIHYDRONAPHTYRIDINYLE ET COMPOSÉS APPARENTÉS UTILISABLES DANS LE CADRE DU TRAITEMENT DE TROUBLES OPHTALMOLOGIQUES
  申请人：CYTOPATHFINDER INC

  公开号：WO2010129843A1

  公开（公告）日：2010-11-11

  The invention provides methods of using dihydronaphthyridinyl and related compounds to treat ophthalmological disorders, such as, wet age-related macular degeneration, diabetic retinopathy, and high myopia. Pharmaceutical compositions and methods of synthesizing the dihydronaphthyridinyl and related compounds are provided.

  这项发明提供了使用二氢萘啉基和相关化合物治疗眼科疾病的方法，如湿性年龄相关性黄斑变性、糖尿病视网膜病变和高度近视。还提供了制备二氢萘啉基和相关化合物的药物组合物和合成方法。
• [EN] TRICYCLIC PROTEIN KINASE INHIBITORS<br/>[FR] INHIBITEURS TRICYCLIQUES DE PROTEINE KINASE
  申请人：AMERICAN HOME PROD

  公开号：WO2001047892A1

  公开（公告）日：2001-07-05

  This invention provides compounds of formula (1) which are useful as inhibitors of protein tyrosine kinase and are antiproliferative agents.

  本发明提供了一种式子为(1)的化合物，它们可用作蛋白酪氨酸激酶的抑制剂并具有抗增殖作用。
• 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。
• 4,6-diamino-[1,7]naphthyridine-3-carbonitrile inhibitors of Tpl2 kinase and methods of making and using the same
  申请人：Green Jeffrey Neal

  公开号：US20060276498A1

  公开（公告）日：2006-12-07

  The present invention provides compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , m and n are defined as described herein. The invention also provides methods of making the compounds of formula (I), and methods of treating inflammatory diseases, such as rheumatoid arthritis, in a mammal comprising administering a therapeutically effective amount of a compound of formula (I) to the mammal.

  本发明提供了式(I)化合物及其药学上可接受的盐，其中R1、R2、R3、R4、R5、R6、m和n的定义如本文所述。本发明还提供了制备式(I)化合物的方法，以及治疗哺乳动物的炎症性疾病，如类风湿性关节炎的方法，包括向哺乳动物施用式(I)化合物的治疗有效量。