首页> 外国专利> Derivatives of imidazo 1,2-a pyridine positive allosteric modulators of mGluR2 Receptors, Pharmaceutical compositions containing them and Uses Thereof in the treatment of Neurological and Psychiatric Disorders.

Derivatives of imidazo 1,2-a pyridine positive allosteric modulators of mGluR2 Receptors, Pharmaceutical compositions containing them and Uses Thereof in the treatment of Neurological and Psychiatric Disorders.

机译:mGluR2受体的咪唑并[1,2-a]吡啶正变构调节剂的衍生物,含有它们的药物组合物及其在神经疾病和精神病治疗中的用途。

摘要

Claim 1: a compound having the formula (1) or one of its forms estereoquu00edmicamente isomeric where R1 is alkyl, cycloalkyl C1 - C3 - 6 6 trifluoromethyl; replaced with trifluoromethyl c1-3 alkyl, cycloalkyl 2,2,2-trifluoroethoxy, C3 - 7 phenyl or substituted phenyl alkyl C1 - 3, 3 - C1 - Oxy alkyl, cyano, haloTrifluoromethyl or trifluoromethoxy substituted phenyl; with 1 or 2; phenyl substituents selected from the group consisting of c1-3 alkyl, alkyl C1 - 3 - Oxy, cyano, trifluoromethyl and Halo, or trifluoromethoxy; 4 - tetrahidropiranilo; R2 is Halo, cyano, trifluoromethyl, c1-3 alkyl or ciclopropilo; R3 is A radical of formula (a) or (b) or (c) or (d); R4 is Hydrogen; hidroxicicloalquilo C3 - 6Pyridinyl substituted pyridinyl; with one or two c1-3 alkyl groups, pirimidinilo; pirimidinilo replaced with one or two alkyl groups C1 3 phenyl substituted with 1 or 2; phenyl substituents selected from the group consisting of c1-3 alkyl, Halo, hidroxialquilo c1-3, mono - or polihaloalquilo C1 - 3, cyano, amino, hydroxyl, carboxyl, c1-3 alkyl - oxialquilo c1-3, c1-3 alkyl - oxiMono - or polihalo c1-3 alkyl - Oxy, c1-3 alkyl carbonyl, mono - and di (c1-3 alkyl or phenyl) amino and morfolinilo; two vicinal substituents which, taken together, form a Bivalent radical formula N = CH - (e) - NH, - ch = CH - NH - (f), or - or - CH2 - ch2-nh - (g); R5 is Hydrogen, fluoro, hydroxyl, Hydro Xialquilo c1-3, hidroxialquil C1 - 3 - Oxy, fluoroalquilo c1-3, fluoroalquil C1 - 3 - oxiMorfolinilo or cyano; X is c or n in which case R5 represents a pair of electrons in the N - X; R4 or R5 represents a radical of formula (H) or (i) or (j) n is 0 OR 1; Q is 1 or 2; R6 c1-3 alkyl, cycloalkyl hidroxialquilo C2 - C3 - 6, 6 - 4 pp. ISBN; cicloalquil c1-3 alkyl or phenyl, phenyl, or pirid pyridinyl; Quot replaced with one or two substituents selected from the group consisting of haloC1-3 alkyl, alkoxy hidroxialquilo C1 C1 - 3 - 3 - trifluoromethyl and (CH2) CO2H m, where M = 0, 1, or 2, or cyclical R6 is a radical of formula (k) where R8 is Hydrogen, alkyl c1-3, c1-3 alkyl - oxi hidroxialquilo c1-3; p is 1 or 2; Z is o or CR9 CH2 (OH), where R0 is Hydrogen or c1-3 alkyl R8 and R9 form; or a radical - CH2 - CH2 - R7 is Hydrogen;Halo or trifluoromethyl, and it is a Covalent Bond, or NH, S, so, SO2, C (OH) (CH3), - CH2 -, - or - CH2 -, CHF or CF2; or R6 - and is morfolinilo, pirrolidinilo or piperidinilo optionally substituted with hydroxyl or hidroxialquilo c1-3; and it is o or NH; or a pharmaceutically acceptable Salt or its solvates.
机译:权利要求1的化合物,具有式(1)或其一种形式的酯季铵化合物,其中R 1为烷基,环烷基C 1 -C 3-6 6三氟甲基。被三氟甲基的C 1-3烷基,环烷基的2,2,2-三氟乙氧基,C3-7苯基或取代的苯基烷基C1-3、3-C1的氧代烷基,氰基,卤代三氟甲基或三氟甲氧基取代的苯基取代; 1或2;选自C 1-3烷基,烷基C 1-3-氧基,氰基,三氟甲基和卤代或三氟甲氧基的苯基取代基; 4-四氢吡喃苯胺; R2是卤代,氰基,三氟甲基,c1-3烷基或环丙基。 R3是式(a)或(b)或(c)或(d)的基团; R4是氢; Hidroxicicloalquilo C3-6吡啶基取代的吡啶基;具有一个或两个c 1-3烷基,吡美胺基; pirimidinilo被一个或两个被1或2个取代的C 1 3苯基烷基取代;选自C 1-3烷基,卤代,羟喹基C 1-3,单-或多卤代甲酰基C 1-3,氰基,氨基,羟基,羧基,C 1-3烷基的基团-草酰基C 1-3,C 1-3烷基-OxiMono-或多卤代C1-3烷基-Oxy,C1-3烷基羰基,单和二(C1-3烷基或苯基)氨基和吗啉代;一起形成二价基团的两个邻位取代基N = CH-(e)-NH,-ch = CH-NH-(f),或-或-CH2-ch2-nh-(g); R5是氢,氟,羟基,Xialquilo c1-3羟基,hidroxialquil C1-3-氧,氟代alquilo c1-3,氟代alC1-3-oxiMorfolinilo或氰基; X是c或n,在这种情况下,R5代表N-X中的一对电子; R4或R5代表式(H)或(i)或(j)的基团,n为0或1; Q是1或2; R6为烷基C1-3的C1-3烷基,环烷基C2-C3-6、6-4pp.ISBN; cicloalquil c1-3烷基或苯基,苯基或吡啶基吡啶基;被一个或两个选自卤素C1-3烷基,烷氧基Hidroxialquilo C1 C1-3-3三氟甲基和(CH2)CO2Hm的取代基取代的取代基,其中M = 0、1,2或环状R6是a式(k)的基团,其中R 8是氢,烷基c 1-3,c 1-3烷基-氧代羟基喹啉c 1-3; p是1或2; Z是o或CR9 CH2(OH),其中R0是氢或C1-3烷基,R8和R9形成;或基团-CH2-CH2-R7是氢;卤代或三氟甲基,并且是共价键,或者是NH,S,SO2,C(OH)(CH3),-CH2-,-或-CH2- CHF或CF2;或R 6-且是被羟基或hidroxialquilo c1-3任选取代的吗啉代,吡咯烷基和哌啶子基;或它是o或NH;或其药学上可接受的盐或其溶剂化物。

著录项

  • 公开/公告号AR069309A1

    专利类型

  • 公开/公告日2010-01-13

    原文格式PDF

  • 申请/专利号AR2008P104955

  • 发明设计人

    申请日2008-11-13

  • 分类号C07D471/04;C07D519/00;A61K31/437;A61K31/4188;A61P25/22;A61P25/18;A61P25/08;A61P25/10;A61P25/24;A61P25/32;A61P25/34;A61P25/36;C07D471/04;C07D221/00;C07D235/00;

  • 国家 AR

  • 入库时间 2022-08-21 18:47:31

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