首页> 外国专利> PIRIDINE DERIVATIVES WITH INHIBITING ACTIVITY OF QUINASA IKB (IKK-BETA).

PIRIDINE DERIVATIVES WITH INHIBITING ACTIVITY OF QUINASA IKB (IKK-BETA).

机译:具有抑制奎那萨菌IKB(IKK-BETA)活性的吡啶衍生物。

摘要

A pyridine derivative of formula (I) in which -R1 represents or in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkyl-sulfonylamino, C1 alkoxy -6-carbonyl, C1-6-alkyl, di (C1-6-alkyl) amino, C1-6-alkanoyl-amino, phenyl-C1-6-amino alkyl, phenylsulfonylamino or -O- (CH2) n-R111, representing n a integer selected from 0 to 6, and R111 is C2-6 alkenyl, benzoyl, diphenylmethyl, di (C1-6 alkyl) amino, C1-6 alkanoyl, C1-6 alkoxycarbonyl, or a saturated or unsaturated ring of 3 to 10 members having 0 to 3 heteroatoms selected from the group consisting of S, O and N as heteroatoms and is optionally substituted with C1-6 alkyl, mono or dihalogen, C1-6 alkyl substituted with halogen, nitro, cyano, C1- alkoxy 6-carbonyl, phenyl, hydroxy, amino, C 1-6 alkyl, di (C 1-6 alkyl) amino, C 1-6 alkanoyl, C 1-6 alkoxy or carbamoyl; R2 represents hydrogen or halogen; R3 represents hydrogen or 1,2,3,6-tetrahydropyridine, -CR31R32R33, wherein R31 is hydrogen or C1-6 alkyl, R32 is hydrogen, a-aminobenzyl, C1-6 alkyl optionally substituted with one or two substituents selected from the group consisting of hydroxy, amino, amino substituted phenyl, phenyl, halogen substituted phenyl and C1-6 alkoxy substituted phenyl, or a 5 to 8 membered saturated ring having 0 to 3 atoms selected from the group consisting of S, O and N as heteroatoms and optionally substituted with C1-6 alkyl, and R33 is hydrogen, amino, C1-6 alkoxycarbonylamino, C2-6 alkenyl-oxycarbonylamino, piperidine-C1-6 alkylcarbonylamino, piperidinyl-C1-6 alkyl -carbonylamino, or R32 and R33 can form, together with the adjacent carbon atom, a saturated ring of 5 to 8 members having 0 to 3 heteroatoms selected from the group consisting of N, O and S as heteroatoms, said ring being optionally substituted with C1-6 phenylalkyl, C1 phenylalkyl -6 substituted with C1-6 alkoxy, C1-6 alkyl, amino, cyano, hydroxy, carbamoyl, carboxy, C1-6-amino alkyl, C1-6 alkoxycarbonyl, di (C1-6 alkyl) amino, benzylamino, alkyl C1-6-sulfonyl, piperidine-C1-6 alkylcarbonyl or optionally condensed with benzene; or -NR34R35, wherein R34 is hydrogen or C1-6 alkyl; or one of its salts.
机译:式(I)的吡啶衍生物,其中-R 1表示或其中R 11为氢,C 1-6烷基,卤素,羟基,C 1-12烷氧基,硝基,氨基,C 1-6烷基磺酰基氨基,C 1烷氧基-6-代表na整数的羰基,C1-6-烷基,二(C1-6-烷基)氨基,C1-6-烷酰基-氨基,苯基-C1-6-氨基烷基,苯磺酰基氨基或-O-(CH2)n-R111 R111选自0至6,且R111为C2-6链烯基,苯甲酰基,二苯甲基,二(C1-6烷基)氨基,C1-6烷酰基,C1-6烷氧羰基或具有0的3至10元的饱和或不饱和环1-3个选自S,O和N的杂原子作为杂原子,并且任选地被C 1-6烷基,单卤素或二卤素,被卤素取代的C 1-6烷基,硝基,氰基,C 1烷氧基6-羰基,苯基取代,羟基,氨基,C 1-6烷基,二(C 1-6烷基)氨基,C 1-6烷酰基,C 1-6烷氧基或氨基甲酰基; R 2代表氢或卤素; R 3代表氢或1,2,3,6-四氢吡啶-CR31R32R33,其中R 31是氢或C 1-6烷基,R 32是氢,α-氨基苄基,任选被一个或两个选自以下基团的取代基取代的C 1-6烷基由羟基,氨基,氨基取代的苯基,苯基,卤素取代的苯基和C1-6烷氧基取代的苯基或具有0至3个选自S,O和N的原子作为杂原子的5至8元饱和环和任选地被C 1-6烷基取代,并且R 33是氢,氨基,C 1-6烷氧羰基氨基,C 2-6烯基-氧羰基氨基,哌啶-C 1-6烷基羰基氨基,哌啶基-C 1-6烷基-羰基氨基或R 32和R 33与相邻的碳原子一起,具有5至8个成员的饱和环,其具有0至3个选自N,O和S的杂原子作为杂原子,所述环任选地被C 1-6苯基烷基,C 1苯基烷基-6取代与C1-6烷氧基,C1-6烷基,氨基,青色o,羟基,氨基甲酰基,羧基,C 1-6-氨基烷基,C 1-6烷氧基羰基,二(C 1-6烷基)氨基,苄氨基,烷基C 1-6-磺酰基,哌啶-C 1-6烷基羰基或任选地与苯缩合;或-NR34R35,其中R34是氢或C1-6烷基;或其一种盐。

著录项

  • 公开/公告号ES2298260T3

    专利类型

  • 公开/公告日2008-05-16

    原文格式PDF

  • 申请/专利权人 BAYER HEALTHCARE AG;

    申请/专利号ES20010969704T

  • 申请日2001-09-10

  • 分类号C07D401/04;A61K31/4353;A61K31/437;A61K31/4375;A61K31/4418;A61K31/4427;A61K31/443;A61K31/4433;A61K31/4545;A61K31/4709;A61K31/496;A61K31/519;A61K31/5365;A61K31/551;A61P1/04;A61P9/10;A61P11/02;A61P11/06;A61P17;A61P17/06;A61P19/02;A61P19/06;A61P21;A61P27/02;A61P29;A61P31;A61P35;A61P37/02;A61P37/06;A61P43;C07D213/08;C07D213/09;C07D213/10;C07D213/73;C07D213/80;C07D213/85;C07D401/06;C07D401/12;C07D401/14;C07D405/14;C07D409/12;C07D409/14;C07D413/14;C07D471/04;C07D471/18;C07D498/04;C07D513/04;C07D521;

  • 国家 ES

  • 入库时间 2022-08-21 20:04:15

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