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    QUINOLIZIDINE AND INDOLIZIDINE DERIVATIVES
    1.
    发明申请
    QUINOLIZIDINE AND INDOLIZIDINE DERIVATIVES 有权
    喹诺酮和吲哚来啶衍生物

    公开(公告)号：US20110313165A1

    公开(公告)日：2011-12-22

    申请号：US13161534

    申请日：2011-06-16

    申请人： Sabine Kolczewski ,  Emmanuel Pinard

    发明人： Sabine Kolczewski ,  Emmanuel Pinard

    IPC分类号： C07D471/04 ,  C07D455/00

    CPC分类号： C07D455/02 ,  C07D471/04

    摘要： The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. The compounds of formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.

    摘要翻译： 本发明涉及式I-A或I-B化合物，其中X，R 1，R 2和R 3在本文中定义; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体。 式I-A和I-B的化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，并且对甘氨酸转运蛋白2（GlyT-2）抑制剂具有良好的选择性，适用于治疗神经和神经精神障碍。

    Quinolizidine and indolizidine derivatives
    2.
    发明授权
    Quinolizidine and indolizidine derivatives 有权
    喹诺啶和吲哚来啶衍生物

    公开(公告)号：US08143273B2

    公开(公告)日：2012-03-27

    申请号：US13161534

    申请日：2011-06-16

    申请人： Sabine Kolczewski ,  Emmanuel Pinard

    发明人： Sabine Kolczewski ,  Emmanuel Pinard

    IPC分类号： A61K31/44 ,  C07D217/02

    CPC分类号： C07D455/02 ,  C07D471/04

    摘要： The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. The compounds of formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.

    摘要翻译： 本发明涉及式I-A或I-B化合物，其中X，R 1，R 2和R 3在本文中定义; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体。 式I-A和I-B的化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，并且对甘氨酸转运蛋白2（GlyT-2）抑制剂具有良好的选择性，适用于治疗神经和神经精神障碍。

    AMIDO-TROPANE DERIVATIVES
    3.
    发明申请
    AMIDO-TROPANE DERIVATIVES 有权
    AMIDO-TROPANE衍生物

    公开(公告)号：US20110312993A1

    公开(公告)日：2011-12-22

    申请号：US13160559

    申请日：2011-06-15

    申请人： Sabine Kolczewski ,  Emmanuel Pinard

    发明人： Sabine Kolczewski ,  Emmanuel Pinard

    IPC分类号： A61K31/46 ,  A61P25/00 ,  A61P25/18 ,  C07D451/02 ,  A61P25/28

    CPC分类号： C07D451/02 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4858 ,  A61K9/4866

    摘要： The present invention relates to a compound of formula I wherein R1, R2 and R3 are each independently hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, racemic mixture, or corresponding enantiomer and/or optical isomer thereof. The compounds of formula I are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. The compounds can be used in the treatment of neurological and neuropsychiatric disorders.

    摘要翻译： 本发明涉及式I化合物，其中R 1，R 2和R 3各自独立地为氢，低级烷基，低级烷氧基，环烷基，被卤素或S-低级烷基取代的低级烷基; 或其药学上可接受的酸加成盐，外消旋混合物或其相应的对映异构体和/或其光学异构体。 式I化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，对甘氨酸转运蛋白2（GlyT-2）抑制剂具有良好的选择性。 该化合物可用于治疗神经和神经精神障碍。

    Tetrahydro-pyran derivatives
    9.
    发明授权
    Tetrahydro-pyran derivatives 有权
    四氢吡喃衍生物

    公开(公告)号：US08524909B2

    公开(公告)日：2013-09-03

    申请号：US13010864

    申请日：2011-01-21

    申请人： Sabine Kolczewski ,  Emmanuel Pinard

    发明人： Sabine Kolczewski ,  Emmanuel Pinard

    IPC分类号： C07D401/04 ,  C07D209/52 ,  C07D405/04 ,  C07D309/14 ,  A61K31/4453 ,  A61K31/403 ,  A61K31/4025 ,  A61K31/351

    CPC分类号： A61K31/351 ,  A61K9/2018 ,  A61K9/4858 ,  A61K31/4025 ,  A61K31/439 ,  A61K31/4412 ,  A61K31/4433 ,  C07D309/14 ,  C07D405/04

    摘要： The present invention relates to a compound of formula I wherein R1/R2 are independently from each other hydrogen, (CR2)o-cycloalkyl, optionally substituted by lower alkyl or hydroxy, or are lower alkyl or heterocycloalkyl, and o is 0 or 1; and R may be the same or different and is hydrogen or lower alkyl; or R1 and R2 may form together with the N atom to which they are attached a heterocycloalkyl group, selected from the group consisting of pyrrolidinyl, piperidinyl, 3-aza-bicyclo[3.1.0]hex-3-yl or 2-aza-bicyclo[3.1.0]hex-2-yl, which are optionally substituted by hydroxy; R3 is S-lower alkyl, lower alkyl, lower alkoxy or cycloalkyl; R3′ is hydrogen, lower alkyl substituted by halogen, lower alkyl or lower alkoxy R4 is lower alkyl substituted by halogen, lower alkyl or lower alkoxy; X is —O— or —CH2—; X′ is —O— or —CH2—; with the proviso that one of X or X′ is always —O— and the other is —CH2—; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. It has been found that the compounds of formula I are good inhibitors of the glycine transporter 1 (GlyT-1) and therefore they may be used for the treatment of schizophrenia.

    摘要翻译： 本发明涉及式I化合物，其中R 1 / R 2彼此独立地为氢，（CR 2）o - 环烷基，任选被低级烷基或羟基取代，或为低级烷基或杂环烷基，o为0或1; 并且R可以相同或不同，为氢或低级烷基; 或者R 1和R 2可以与它们所连接的N原子一起形成杂环烷基，该杂环烷基选自吡咯烷基，哌啶基，3-氮杂 - 双环[3.1.0]己-3-基或2-氮杂 - 双环[3.1.0]己-2-基，其任选被羟基取代; R3是S-低级烷基，低级烷基，低级烷氧基或环烷基; R3'是氢，被卤素取代的低级烷基，低级烷基或低级烷氧基R4是被卤素，低级烷基或低级烷氧基取代的低级烷基; X是-O-或-CH 2 - ; X'是-O-或-CH 2 - ; 条件是X或X'中的一个总是-O-，另一个是-CH 2 - ; 或其药学上可接受的酸加成盐，或其相应的对映异构体和/或其旋光异构体。 已经发现，式I化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂，因此它们可用于治疗精神分裂症。