首页> 外国专利> Derivatives - 1,2,4 triazolo 4,3-a pyridine positive allosteric modulators of mGluR2 Receptors, Pharmaceutical compositions containing them and their use in the treatment of Neurological and Psychiatric Disorders.

Derivatives - 1,2,4 triazolo 4,3-a pyridine positive allosteric modulators of mGluR2 Receptors, Pharmaceutical compositions containing them and their use in the treatment of Neurological and Psychiatric Disorders.

机译:衍生物-mGluR2受体的1,2,4三唑并[4,3-a]吡啶正构构调节剂,含有它们的药物组合物及其在治疗神经和精神疾病中的用途。

摘要

Claim 1: A compound having the formula (1) or a stereochemically isomeric form thereof, wherein the bond drawn into the ring indicates that the bond can be attached to any atom of the carbon ring; R1 is selected from the group consisting of hydrogen; C1-6 alkyl, (C1-3 alkyloxy) C1-3 alkyl, [(C1-3 alkyloxy) -C1-3alkyloxy] C1-3 alkyl; C1-3 alkyl substituted with one or more independently selected halo substituents; unsubstituted benzyl; benzyl substituted with one or more substituents each independently selected from the group consisting of halo, C1-3 alkyl, C1-3 alkyloxy C1-3 alkyl, C1-3 alkyloxy, C1-3 hydroxyalkyl, cyano,Hydroxy, amino, C (= O) r ',it is life.C (3DO) NR Rmono- or di- (C1-3 alkyl) amino, morpholinyl, (C3-7 cycloalkyl) C1-3 alkyloxy, trifluoromethyl and trifluoromethoxy, where R 'and Rö are independently selected from hydrogen and C1-6 alkyl, (benzyloxy) alkyl C1-3; unsubstituted C3-7 cycloalkyl; C3-7 cycloalkyl substituted with one or more independently selected C1-3 alkyl substituted with one or more independently selected halo substituents; (C3-7 cycloalkyl) C1-3 alkyl; 4- (2,3,4,5-tetrahydro-benzo [f] [1,4] oxazepin) methyl; Het1; Het1 C1-3alkyl, Het2 and Het2 C1-3alkyl; R2 is selected from the group consisting of cyano; halo; C1-3 alkyl substituted with one or more independently selected halo substituents;C1-3 tar is replaced by one or more independently selected halogen substitutes; c1-3 tar; c3-7 cyclopentadiene; c1-3 tar (cyclopentadiene c3-7); a-d-forms a radical form in (a),(b)(c)(d) And (E);The links drawn in (a) indicate that R4 can be connected to any atom in carbon rings 2 and 3; each R3 should be independent of the hydrogen group; C1-6 is not replaced; C1-6 is replaced by one or more substitutes, independent of the halogen group, Hydrogen Xi, alcoxi c1-3 and trifluoromethane; unsubstituted cyclopentanediol c3-7; unsubstituted cyclopentanediol c3-7; cyclopentanediol c3-7 substituted by one or more substitutes, independent of halogen, c1-3 hydrocarbon, hydroxyl, c1-3 and trifluoromethane groups; cyclopentanediol c3-7-c1-3 tar; unsubstituted phenyl;One or more alternatives are used to replace phenyl, independent of the substances of halogen, c1-3 tar, c1oxy c1-3 and trifluoromethyl, hett3 and hett3 tar c1-3 groups, or R8 is selected from c1-3 tar respectively from a cyclic equation excimer (f), C1-3 hydrocarbon and c1-3 hydroxyhydrazide; q is 1 or 2; X is selected from O, CH2 and CR9 (OH).R9 is selected from hydrogen, c1-3 hydrocarbon and cyclo-7; or X is a periodic equation radical (g), where R and s are independently selected between 0, 1 and 2, provided that R + S = 2; per R4, R6 and R7 are independently selected from c1-3 and c1-3 tar replaced by one or more independently selected halogenated substitutes; each R5 is a group of hydrogen, c1-3 tar and c1-3 tar replaced by one or more independently selected halogenated substitutes; N, M While P is selected from 0, 1 and 2 respectively; V equals 0 or 1;T and u are independently selected from 1 and 2, W from N and CR10, R10 from hydrogen, halogen and methyl trifluoride, and each het1 is a saturated heterocyclic radical selected from pyridine, pyridyldi, pyridyldi, pyridine and morphine, each of which can be replaced by one or more alternatives. Plus each individual C1-6 tar group, monkey group,Di-y tri halogequile c1-3; unsubstituted phenyl; and phenyl substituted by 1, 2 or 3 substitutes independently selected from the halogenated, trifluoromethyl, and trifluoromethyl compound groups; each het2 is pyridine or pyridine; each het3 is a different heterocycle selected from the tetrahydropyridine, pyridan, and pyridinediol groups. Choose to replace each selected alternative with one or more alternatives, regardless of the categories consisting of halogen, c1-3 tar, alcoxi c1-3 and trifluoromethyl; and choose halogen from fluorine, chlorine, bromine and iodine or from salt or solution acceptable to the same agent.
机译:权利要求1:具有式(1)或其立体化学异构体形式的化合物,其中拉入环的键表示该键可以连接至碳环的任何原子; R1选自氢; C 1-6烷基,(C 1-3烷氧基)C 1-3烷基,[(C 1-3烷氧基)-C 1-3烷氧基] C 1-3烷基;被一个或多个独立选择的卤素取代基取代的C 1-3烷基;未取代的苄基;被一个或多个取代基取代的苄基,每个取代基独立地选自卤素,C1-3烷基,C1-3烷氧基C1-3烷基,C1-3烷氧基,C1-3羟烷基,氰基,羟基,氨基,C(= C(3DO)NR R单或二(C1-3烷基)氨基,吗啉基,(C3-7环烷基)C1-3烷氧基,三氟甲基和三氟甲氧基,其中R'和Rö独立地选自氢和C 1-6烷基,(苄氧基)烷基C 1-3;未取代的C3-7环烷基; C3-7环烷基被一个或多个独立选择的C1-3烷基取代,所述C1-3烷基被一个或多个独立选择的卤素取代基取代; (C3-7环烷基)C1-3烷基; 4-(2,3,4,5-四氢-苯并[f] [1,4]草氮杂)甲基; Het1; Het1 C1-3烷基,Het2和Het2 C1-3烷基; R 2选自氰基;光环;被一个或多个独立选择的卤素取代基取代的C1-3烷基; C1-3的焦油被一个或多个独立选择的卤素取代基取代; c1-3焦油; c3-7环戊二烯; c1-3 tar(环戊二烯c3-7); a-d在(a),(b)(c)(d)和(E)中形成自由基形式;在(a)中绘制的连接表明R 4可以连接至碳环2和3中的任何原子;每个R 3应独立于氢基团; C1-6未更换; C 1-6被一个或多个取代基取代,独立于卤素基团,氢xi,alcoxi c1-3和三氟甲烷;未取代的环戊二醇c3-7;未取代的环戊二醇c3-7;被一个或多个取代基取代的环戊二醇c3-7,独立于卤素,c1-3烃基,羟基,c1-3和三氟甲烷基团;环戊二醇c3-7-c1-3焦油;未取代的苯基;一个或多个替代取代苯的物质,与卤素,c1-3 tar,c1oxy c1-3和三氟甲基,hett3和hett3 tar的c1-3基团无关,或R8选自c1-3 tar分别从循环方程准分子(f),C 1-3烃和c 1-3羟基酰肼得到。 q是1或2; X选自O,CH 2和CR 9(OH)。R9选自氢,c 1-3烃和环-7;或X是周期方程根(g),其中R和s独立地在0、1和2之间选择,只要R + S> 0,则R = 1。 = 2;根据R4,R6和R7独立地选自c1-3和c1-3焦油,被一个或多个独立选择的卤代取代基取代;每个R 5是被一个或多个独立选择的卤代取代基取代的氢,c 1-3 tar和c 1-3 tar的基团; N,M,而P分别从0、1和2中选择; V等于0或1; T和u独立地选自1和2,W选自N和CR 10,R 10选自氢,卤素和三氟甲基,并且每个het1是选自吡啶,吡啶基二,吡啶基二,吡啶和吗啡,每个都可以被一个或多个替代品替代。加上每个单独的C1-6焦油组,猴子组,Di-y tri halogequile c1-3;未取代的苯基被1、2或3个独立地选自卤代,三氟甲基和三氟甲基化合物基团的取代基取代的苯基;每个het2是吡啶或吡啶;每个het3是选自四氢吡啶,吡啶和吡啶二醇基团的不同杂环。选择用一个或多个替代物替代每个选择的替代物,而不必考虑卤素,c1-3焦油,alcoxi c1-3和三氟甲基的类别;并从氟,氯,溴和碘中选择卤素,或从同一试剂可接受的盐或溶液中选择卤素。

著录项

  • 公开/公告号AR076859A1

    专利类型

  • 公开/公告日2011-07-13

    原文格式PDF

  • 申请/专利号AR2010P101611

  • 发明设计人

    申请日2010-05-11

  • 分类号C07D471/04;C07D519/00;A61K31/437;A61K31/4196;A61K31/407;A61P25/22;A61P25/18;A61P25/24;A61P25/06;A61P25/08;A61P25/28;

  • 国家 AR

  • 入库时间 2022-08-21 18:07:26

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