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Quinazoline compounds as sodium channel blockers

机译:喹唑啉化合物作为钠通道阻滞剂

摘要

Compound having Formula I: ** Formula ** or a pharmaceutically acceptable salt or solvate thereof, wherein: R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl , halogen, hydroxy, hydroxyalkyl, haloalkyl, cyano; amino, alkylamino, dialkylamino, alkoxy, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyloxy, carboxy, alkoxycarbonyl, aminosulfonyl, alkylsulfonylamino, (alkylsulfonylamino) alkyl, ureido, (aminocarbonyl) alkylamino and (carboxyalkyl) amino; G is G1, G2, G3 or G4, where G1 is -NR5R6, where R5 is H, alkyl or NH2, R6 is a) H, b) alkyl, c) hydroxyalkyl, d) (aminocarbonyl) alkyl, e) (aminocarbonyl) (hydroxy) alkyl; f) aminoalkyl, g) alkylaminoalkyl, h) dialkylaminoalkyl, i) cycloalkyl, unsubstituted or substituted with one or more substituents, each independently selected from the group consisting of alkyl, alkoxy, halogen, haloalkyl, haloalkoxy, hydroxy, hydroxyalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, aminocarbonyl, carboxy, alkoxycarbonyl and cyano; j) (cycloalkyl) alkyl, wherein the cycloalkyl is unsubstituted or substituted with one or more substituents, each independently selected from the group consisting of alkyl, alkoxy, halogen, haloalkyl, haloalkoxy, hydroxy, hydroxyalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, aminocarbonyl, carboxy, alkoxycarbonyl and cyano; k) aryl, unsubstituted or substituted with one or more substituents, each independently selected from the group consisting of alkyl, alkoxy, halogen, haloalkyl, haloalkoxy, hydroxy, hydroxyalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, aminocarbonyl, carboxy, alkoxycarbonyl and cyano; l) arylalkyl, wherein the aryl group is unsubstituted or substituted with one or more substituents, each independently selected from the group consisting of alkyl, alkoxy, halogen, haloalkyl, haloalkoxy, hydroxy, hydroxyalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, aminocarbonyl, carboxy, alkoxycarbonyl and cyano; m) heteroaryl, unsubstituted or substituted with one or more substituents, each independently selected from the group consisting of alkyl, alkoxy, halogen, haloalkyl, haloalkoxy, hydroxy, hydroxyalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, aminocarbonyl, carboxy, alkoxycarbonyl and cyano; n) heteroarylalkyl, wherein the heteroaryl group is unsubstituted or substituted with one or more substituents, each independently selected from the group consisting of alkyl, alkoxy, halogen, haloalkyl, haloalkoxy, hydroxy, hydroxyalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, aminocarbonyl, carboxy, alkoxycarbonyl and cyano; o) heterocycle, unsubstituted or substituted with one or more substituents, each independently selected from the group consisting of alkyl, alkoxy, halogen, haloalkyl, haloalkoxy, hydroxy, hydroxyalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, aminocarbonyl, carboxy, alkoxycarbonyl and cyano; op) heterocycloalkyl, wherein the heterocycle is unsubstituted or substituted with one or more substituents, each independently selected from the group consisting of alkyl, alkoxy, halogen, haloalkyl, haloalkoxy, hydroxy, hydroxyalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl , aminocarbonyl, carboxy, alkoxycarbonyl and cyano.
机译:具有式I ** **的化合物或其药学上可接受的盐或溶剂化物,其中:R1,R2,R3和R4各自独立地选自氢,烷基,烯基,炔基,卤素,羟基,羟烷基,卤代烷基,氰基;氨基,烷基氨基,二烷基氨基,烷氧基,氨基羰基,烷基氨基羰基,二烷基氨基羰基,烷基羰基氨基,烷基羰基氧基,羧基,烷氧基羰基,氨基磺酰基,烷基磺酰基氨基,(烷基磺酰基氨基)烷基,脲基,(氨基羰基)烷基氨基和(羧基烷基)氨基; G是G1,G2,G3或G4,其中G1是-NR5R6,其中R5是H,烷基或NH2,R6是a)H,b)烷基,c)羟烷基,d)(氨基羰基)烷基,e)(氨基羰基) )(羟基)烷基; f)氨基烷基,g)烷基氨基烷基,h)二烷基氨基烷基,i)未被取代或被一个或多个取代基取代的环烷基,所述取代基各自独立地选自烷基,烷氧基,卤素,卤代烷基,卤代烷氧基,羟基,羟烷基,氨基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,氨基羰基,羧基,烷氧羰基和氰基; j)(环烷基)烷基,其中环烷基未被取代或被一个或多个取代基取代,每个取代基独立地选自烷基,烷氧基,卤素,卤代烷基,卤代烷氧基,羟基,羟烷基,氨基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,氨基羰基,羧基,烷氧基羰基和氰基; k)未被取代或被一个或多个取代基取代的芳基,其各自独立地选自烷基,烷氧基,卤素,卤代烷基,卤代烷氧基,羟基,羟烷基,氨基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,氨基羰基,羧基,烷氧基羰基和氰基; l)芳基烷基,其中芳基未被取代或被一个或多个取代基取代,每个取代基独立地选自烷基,烷氧基,卤素,卤代烷基,卤代烷氧基,羟基,羟烷基,氨基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,氨基羰基,羧基,烷氧羰基和氰基; m)未被取代或被一个或多个取代基取代的杂芳基,其各自独立地选自烷基,烷氧基,卤素,卤代烷基,卤代烷氧基,羟基,羟烷基,氨基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,氨基羰基,羧基,烷氧基羰基和氰基; n)杂芳基烷基,其中杂芳基未被取代或被一个或多个取代基取代,每个取代基独立地选自烷基,烷氧基,卤素,卤代烷基,卤代烷氧基,羟基,羟烷基,氨基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,氨基羰基,羧基,烷氧羰基和氰基; o)未被取代或被一个或多个取代基取代的杂环,所述取代基各自独立地选自烷基,烷氧基,卤素,卤代烷基,卤代烷氧基,羟基,羟烷基,氨基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,氨基羰基,羧基,烷氧基羰基和氰基; op)杂环烷基,其中杂环未被取代或被一个或多个取代基取代,每个取代基独立地选自烷基,烷氧基,卤素,卤代烷基,卤代烷氧基,羟基,羟烷基,氨基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,氨基羰基,羧基,烷氧羰基和氰基。

著录项

  • 公开/公告号ES2540562T3

    专利类型

  • 公开/公告日2015-07-10

    原文格式PDF

  • 申请/专利权人 PURDUE PHARMA L.P.;

    申请/专利号ES20110784766T

  • 发明设计人 GOEHRING R.;TAFESSE LAYKEA;YAO JIANGCHAO;

    申请日2011-10-05

  • 分类号C07D239/74;A61K31/517;A61P9/06;A61P25/02;A61P25/06;A61P25/08;A61P25/14;A61P25/24;A61P25/28;C07D239/84;C07D401/04;C07D401/12;C07D403/12;C07D471/08;

  • 国家 ES

  • 入库时间 2022-08-21 15:11:57

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