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    COMPOUNDS WHICH INHIBIT THE GLYCINE TRANSPORTER AND USES THEREOF
    3.
    发明申请
    COMPOUNDS WHICH INHIBIT THE GLYCINE TRANSPORTER AND USES THEREOF 审中-公开
    抑制甘油运输机及其用途的化合物

    公开(公告)号：WO2007113309A3

    公开(公告)日：2008-09-12

    申请号：PCT/EP2007053275

    申请日：2007-04-03

    Applicant: GLAXO GROUP LTD ,  COULTON STEVEN ,  GILPIN MARTIN ,  PORTER RODERICK ALAN

    Inventor： COULTON STEVEN ,  GILPIN MARTIN ,  PORTER RODERICK ALAN

    IPC: C07C211/27 ,  A61K31/166 ,  A61K31/40 ,  A61K31/445 ,  A61P25/28 ,  C07C233/78 ,  C07D213/40 ,  C07D295/13

    CPC classification number: C07C211/27 ,  C07C233/78 ,  C07D213/40 ,  C07D295/13

    Abstract: Compounds of formula (I) and salts and solvates are provided wherein R 2 is selected from phenyl substituted with n R 1 groups, and pyridyl substituted with n R 1 groups; n = 0, 1 or 2; each R 1 is independently selected from the group consisting of halo, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkyl, haloC 1-4 alkoxy and cyano; R 3 is selected from hydrogen and C 1-2 alkyl; R 4 is selected from the group consisting of ethyl, n- propyl, i-propyl, n-butyl, i-butyl and t-butyl; or R 3 and R 4 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocyclic ring optionally substituted with one or more groups X; each X is independently selected from the group consisting of C 1-4 alkyl, and haloC 1-4 alkyl; R 12 is selected from the group consisting of hydrogen, fluoro, chloro, bromo, methyl and methylthio; R 13 is selected from hydrogen, chloro and trifluoromethyl; R 14 is selected from hydrogen, trifluoromethyl and chloro; R 15 is selected from hydrogen, chloro and trifluoromethyl; R 16 is selected from hydrogen, methyl, fluoro and chloro; R 12 , R 13 , R 14 , R 15 and R 16 not all simultaneously being hydrogen. Processes for the preparation and uses of the compounds as medicaments for treating disorders such as psychoses, dementia or attention deficit disorder are also disclosed.

    Abstract translation: 提供式（I）化合物及其盐和溶剂合物，其中R 2选自被n R 1基团取代的苯基，和被n R 1取代的吡啶基 组 n = 0,1或2; 每个R 1独立地选自卤素，C 1-4烷基，C 1-4烷氧基，卤代C 1 -C 4烷基， 1-4个C 1-4烷基，卤代C 1-4烷氧基和氰基; R 3选自氢和C 1-12烷基; R 4选自乙基，正丙基，异丙基，正丁基，异丁基和叔丁基; 或R 3和R 4与它们所连接的氮原子一起形成任选被一个或多个基团X取代的饱和5或6元杂环; 每个X独立地选自C 1-4烷基和卤代C 1-4烷基; R 12选自氢，氟，氯，溴，甲基和甲硫基; R 13选自氢，氯和三氟甲基; R 14选自氢，三氟甲基和氯; R 15选自氢，氯和三氟甲基; R 16选自氢，甲基，氟和氯; R 12，R 13，R 14，R 15和R 16不是 全部同时为氢。 还公开了用于制备和使用化合物作为治疗诸如精神病，痴呆或注意力缺陷障碍之类疾病的药物的方法。

    N-[6-(4-MORPHOLINYL)-3-PYRIDINYL]-2-(TETRAHYDRO-2H-PYRAN-4-YL)-N-[(1-{[PHENYL]METHYL}-4-PIPERIDINYL)METHYL] ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS GLYT1 TRANSPORT INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL DISORDERS SUCH AS SCHIZOPHRENIA
    8.
    发明申请
    N-[6-(4-MORPHOLINYL)-3-PYRIDINYL]-2-(TETRAHYDRO-2H-PYRAN-4-YL)-N-[(1-{[PHENYL]METHYL}-4-PIPERIDINYL)METHYL] ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS GLYT1 TRANSPORT INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL DISORDERS SUCH AS SCHIZOPHRENIA 审中-公开
    N- [6-（4-吗啉基）-3-吡啶基] -2-（四氢-2H-吡喃-4-基）-N - [（1 - {[苯基]甲基} -4-哌啶子基）甲基] 作为GLYT1运输抑制剂治疗神经病变的衍生物和相关化合物，如SCHIZOPHRENIA

    公开(公告)号：WO2005103038A1

    公开(公告)日：2005-11-03

    申请号：PCT/GB2005/001448

    申请日：2005-04-15

    Applicant: GLAXO GROUP LIMITED ,  NASH, David, John ,  PORTER, Roderick, Alan

    Inventor： NASH, David, John ,  PORTER, Roderick, Alan

    IPC: C07D405/14

    CPC classification number: C07D405/14 ,  C07D401/12

    Abstract: The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R 1 is selected from the group consisting of optionally substituted C 1-8 alkyl, optionally substituted C 3-8 cycloalkyl, optionally substituted C 3-8 heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, arylC 1-8 alkyl (wherein both aryl and C 1-8 alkyl are optionally substituted), C 3-8 heterocyclylC 1-8 alkyl (wherein the C 1-8 alkyl is optionally substituted) and heteroarylC 1-8 alkyl (wherein both heteroaryl and C 1-8 alkyl are optionally substituted); R 2 and R 3 , together with the carbon atom to which they are attached, form optionally subtituted C 3-4 cycloalkyl, or R 2 and R 3 are independently hydrogen or C 1-8 alkyl; R 4 and R 5 are both hydrogen, or R 4 and R 5 together form a C 1-4 alkylene bridge across the piperidine ring; Het is an optionally substituted 5- or 6-membered monocyclic heteroaryl group; R 6 and R 7 are independently selected from the group consisting of hydrogen, halogen and C 1-4 alkyl, or R 6 and R 7 together form a C 3-4 cycloalkyl; Ar is an optionally substituted aryl or an optionally substituted heteroaryl; and n is 0, 1, 2 or 3. And uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.

    Abstract translation: 本发明提供式（I）化合物或其盐或溶剂化物：其中R 1选自任选取代的C 1-8烷基，任选取代的C 3-8环烷基，任选取代的C 3-8杂环基，任选取代的 芳基，任选取代的杂芳基，芳基C 1-8烷基（其中芳基和C 1-8烷基任选被取代），C 3-8杂环C 1-6烷基（其中C 1-8烷基任选被取代）和杂芳基C 1-8烷基（其中杂芳基和C 1-8烷基均为 任选取代）; R 2和R 3与它们所连接的碳原子一起形成任选取代的C3-4环烷基，或者R 2和R 3独立地是氢或C 1-8烷基; R 4和R 5都是氢，或者R 4和R 5一起形成穿过哌啶环的C 1-4亚烷基桥; Het是任选取代的5或6元单环杂芳基; R 6和R 7独立地选自氢，卤素和C 1-4烷基，或者R 6和R 7一起形成C 3-4环烷基; Ar是任选取代的芳基或任选取代的杂芳基; 并且n为0,1,2或3.以及这些化合物的用途。 该化合物抑制GlyT1转运蛋白并且可用于治疗某些神经和神经精神障碍，包括精神分裂症。

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