首页> 外国专利> Metabotropic glutamate receptor (mGluR4) modulators having 5- or 6-membered N-heteroaryl ring substituted by both N-cyclylamino amp; 5-membered N-heteroaryl ring

Metabotropic glutamate receptor (mGluR4) modulators having 5- or 6-membered N-heteroaryl ring substituted by both N-cyclylamino amp; 5-membered N-heteroaryl ring

机译:代谢型谷氨酸受体(mGluR4)调节剂,具有被N-环氨基和5-元N-杂芳基环取代的5-或6-元N-杂芳基环

摘要

Compounds of formula (I): ```wherein: DL TSIZE=18 COMPACT=COMPACT DTX1, X2, X3 and X4DDare C, N, O, S or C=C, such that the ring is a 5- or 6-membered heteroaryl ring which is further substituted by 1 to 3 radicals Am; DTAmDDis H, a substituent as defined in the specification, or any two radicals Am taken together may form an optionally substituted 3- to 10-membered carbocyclic or heterocyclic ring; DTY1, Y2, Y3 and Y4DDare C or N, such that the ring is a 5-membered heteroaryl ring which is further substituted by 1 to 3 radicals Bm; DTBmDDis H, a substituent as defined in the specification, or any two radicals Bm taken together may form an optionally substituted 3- to 10-membered carbocyclic or heterocyclic ring; DTM1DDis an optionally substituted 3- to 10-membered ring selected from aryl, heteroaryl, heterocyclic and cycloalkyl; DTM2DDis H or a substituent as defined in the specification; DTM3DDis H or ```an optionally substituted radical selected from: ```-C0-6-alkyl-CO-R11, ```-C2-6-alkyl-S(O)R11, ```-C0-6-alkyl-CO-NR11R12, and ```-C0-6-alkyl-SO2-R11, DTR11 and R12DDand H or an optionally substituted radical selected from: ```-C1-6-alkylhalo, ```-C1-6-alkyl, ```-C1-6-alkylcyano, ```-C3-7-cycloalkyl ```-C4-10-alkyl-cycloalkyl, heteroaryl, ```-C1-6-alkylheteroaryl, aryl, ```-C1-6-alkylaryl, and heterocycle; /DL and stereoisomers, acid/base addition salts, and N-oxides thereof are modulators of metabotropic glutamate receptors - subtype 4 (mGluR4) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluRA4 receptors. Such compounds may also be used to prepare a tracer for imaging an metabotropic glutamate receptor. They may also be used as a taste agent, a flavour (or flavour enhancing) agent, or a food or beverage additive.
机译:式(I)的化合物:其中:
X1,X2,X3和X4
是C,N,O,S或C = C,使得环是5或6元杂芳基环,其进一步被1-3个Am基团取代;
Am
是H,如说明书中所定义的取代基,或两个基团Am一起可形成任选取代的3至10元碳环或杂环; Y 1,Y 2,Y 3和Y 4 DD为C或N,使得该环为5元杂芳基环,其进一步被1-3个基团Bm取代; DT Bm DD为H,如说明书中所定义的取代基,或任意两个基团B m一起可形成任选取代的3至10元碳环或杂环; M 1 DD是任选取代的3至10元环,其选自芳基,杂芳基,杂环和环烷基;
M2
是H或说明书中定义的取代基;
M3
是H或选自以下的任选取代的基团:-C0-6-烷基-CO-R11,-C2-6-烷基-S(O)R11, -C0-6-烷基-CO-NR11R12和-C0-6-烷基-SO2-R11, R11和R12
和H或选自以下的任选取代的基团: -C1-6-烷基卤代,-C1-6-烷基,-C1-6-烷基氰基,-C3-7-环烷基,-C4-10-烷基-环烷基,杂芳基,-C 1-6-烷基杂芳基,芳基,-C 1-6-烷基芳基和杂环; 和立体异构体,酸/碱加成盐及其N-氧化物是促代谢型谷氨酸受体-亚型4(mGluR4)的调节剂,可用于治疗或预防中枢神经系统疾病以及其他由MHC调节的疾病mGluRA4受体。这样的化合物也可用于制备示踪剂以使代谢型谷氨酸受体成像。它们也可以用作调味剂,增香剂(或增香剂)或食品或饮料添加剂。

著录项

  • 公开/公告号GB2455111A

    专利类型

  • 公开/公告日2009-06-03

    原文格式PDF

  • 申请/专利权人 ADDEX PHARMA S.A;

    申请/专利号GB20070023342

  • 发明设计人 CHRISTELLE BOLEA;

    申请日2007-11-28

  • 分类号C07D417/04;A61K31/4245;A61K31/427;A61K31/433;A61K31/4439;A61K49;A61P1;A61P1/04;A61P1/06;A61P3/10;A61P5;A61P5/14;A61P5/50;A61P9/10;A61P17;A61P19/02;A61P25;A61P25/06;A61P25/08;A61P25/14;A61P25/16;A61P25/18;A61P25/22;A61P25/24;A61P25/28;A61P25/30;A61P27/02;A61P29;A61P31/18;A61P35;A61P37/02;A61P37/04;A61P37/06;A61P43;C07D413/04;C07D417/14;

  • 国家 GB

  • 入库时间 2022-08-21 19:06:36

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