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    3-ARYL-ISOXAZOLE-4-CARBONYL-BENZOFURAN DERIVATIVES
    93.
    发明申请
    3-ARYL-ISOXAZOLE-4-CARBONYL-BENZOFURAN DERIVATIVES 审中-公开
    3-芳基 - 异恶唑-4-羰基苯并呋喃衍生物

    公开(公告)号：WO2007054444A2

    公开(公告)日：2007-05-18

    申请号：PCT/EP2006067879

    申请日：2006-10-27

    Applicant: HOFFMANN LA ROCHE ,  BUETTELMANN BERND ,  HAN BO ,  KNUST HENNER ,  NETTEKOVEN MATTHIAS ,  THOMAS ANDREW

    Inventor： BUETTELMANN BERND ,  HAN BO ,  KNUST HENNER ,  NETTEKOVEN MATTHIAS ,  THOMAS ANDREW

    IPC: C07D413/06 ,  A61K31/42 ,  A61P25/28 ,  C07D413/14

    CPC classification number: C07D413/06 ,  C07D413/14

    Abstract: The present invention is concerned with 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives of formula (I) wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, hydroxy, lower alkoxy, OCF3, -OCH2-R, R3 is hydrogen or lower alkoxy; or R2 and R3 form together with the carbon atom to which they are attached a ring with -CH=CH-CH=-CH-; R is aryl or heteroaryl, optionally substituted by halogen or lower alkyl, or is C(O)NH-lower alkyl, or is -C(O)-heteroaryl, wherein the heteroaryl group is optionally substituted by lower alkyl or phenyl, and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA A cc5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

    Abstract translation: 本发明涉及其中R 1为氢或卤素的式（I）的3-芳基 - 异恶唑-4-羰基 - 苯并呋喃衍生物; R2是氢，卤素，羟基，低级烷氧基，OCF3，-OCH2-R，R3是氢或低级烷氧基; 或者R2和R3与它们所连接的碳原子一起形成具有-CH = CH-CH = -CH-的环; R 2为芳基或杂芳基，任选被卤素或低级烷基取代，或为C（O）NH-低级烷基，或为-C（O） - 杂芳基，其中杂芳基任选被低级烷基或苯基取代， 其药学上可接受的酸加成盐。 已经发现，这类化合物对GABA A cc5受体结合位点显示出高亲和力和选择性，并可用作认知增强剂或用于治疗认知障碍如阿尔茨海默氏病。

    ISOXAZOLE DERIVATIVES
    94.
    发明申请
    ISOXAZOLE DERIVATIVES 审中-公开
    异佛唑衍生物

    公开(公告)号：WO2007042420A1

    公开(公告)日：2007-04-19

    申请号：PCT/EP2006/066959

    申请日：2006-10-02

    Applicant: F. HOFFMANN-LA ROCHE AG ,  BUETTELMANN, Bernd ,  HAN, Bo ,  KNUST, Henner ,  NETTEKOVEN, Matthias ,  THOMAS, Andrew

    Inventor： BUETTELMANN, Bernd ,  HAN, Bo ,  KNUST, Henner ,  NETTEKOVEN, Matthias ,  THOMAS, Andrew

    IPC: C07D413/06 ,  C07D413/14 ,  A61K31/41 ,  A61P25/00

    CPC classification number: C07D413/14

    Abstract: The present invention is concerned with aryl-isoxazole-4-carbonyl-indole-carboxylic acid amide derivatives of formula (I) wherein R 1 is hydrogen, lower alkyl or aryl; R 2 is lower alkyl; R 3 is hydrogen or halogen; R 4 /R 5 is independently from each other hydrogen, lower alkyl, lower alkinyl, -(CH 2 )n-cycloalkyl, -(CH 2 ) n -heteroaryl, -(CH 2 ) n -heterocyclyl or -(CH 2 ) n -OH; n is 0, 1, 2 or 3; and with their pharmaceutically acceptable acid addition salts. It has been found that this class of compounds show high affinity and selectivity for GABA α 5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

    Abstract translation: 本发明涉及式（I）的芳基 - 异恶唑-4-羰基 - 吲哚 - 羧酸酰胺衍生物，其中R 1是氢，低级烷基或芳基; R 2是低级烷基; R 3是氢或卤素; R 4和R 5彼此独立地为氢，低级烷基，低级炔基， - （CH 2 CH 2）n - 环烷基， - （ （CH 2）n - 杂环基， - （CH 2）n - 杂环基或 - （CH 2）n - 2 ）名词 -OH; n为0,1,2或3; 和其药学上可接受的酸加成盐。 已经发现，这类化合物显示出对GABA 5受体结合位点的高亲和力和选择性，并且可以用作认知增强剂或用于治疗诸如阿尔茨海默病的认知障碍。

    THIAZOLYL PIPERIDINE DERIVATIVES
    96.
    发明申请
    THIAZOLYL PIPERIDINE DERIVATIVES 审中-公开
    噻唑啉哌啶衍生物

    公开(公告)号：WO2007020213A2

    公开(公告)日：2007-02-22

    申请号：PCT/EP2006/065167

    申请日：2006-08-09

    Applicant: F. HOFFMANN-LA ROCHE AG ,  NETTEKOVEN, Matthias Heinrich ,  ROCHE, Olivier

    Inventor： NETTEKOVEN, Matthias Heinrich ,  ROCHE, Olivier

    IPC: C07D417/04 ,  C07D417/14 ,  A61K31/427 ,  A61K31/426

    CPC classification number: C07D417/04 ,  C07D417/14

    Abstract: The present invention relates to compounds of formula (I) wherein R 1 , R 2 and R 3 are as defined in the description and claims. It further relates to pharmaceutically acceptable salts thereof as well as to pharmaceutical compositions comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

    Abstract translation: 本发明涉及其中R 1，R 2和R 3的式（I）化合物如说明书和权利要求中所定义。 它还涉及其药学上可接受的盐以及包含这些化合物的药物组合物及其制备方法。 该化合物可用于治疗和/或预防与H3受体的调节相关的疾病。

    1-BENZOYL-PIPERAZINE DERIVATIVES AS GLYCINE UPTAKE INHIBITORS FOR THE TREATMENT OF PSYCHOSES
    98.
    发明申请
    1-BENZOYL-PIPERAZINE DERIVATIVES AS GLYCINE UPTAKE INHIBITORS FOR THE TREATMENT OF PSYCHOSES 审中-公开
    作为用于治疗心脏病的甘油摄取抑制剂的1-苯甲酰基哌嗪衍生物

    公开(公告)号：WO2005023261A1

    公开(公告)日：2005-03-17

    申请号：PCT/EP2004/009699

    申请日：2004-08-31

    Applicant: F. HOFFMANN-LA ROCHE AG ,  ALBERATI-GIANI, Daniela ,  JOLIDON, Synese ,  NARQUIZIAN, Robert ,  NETTEKOVEN, Matthias, Heinrich ,  NORCROSS, Roger, David ,  PINARD, Emmanuel ,  STALDER, Henri

    Inventor： ALBERATI-GIANI, Daniela ,  JOLIDON, Synese ,  NARQUIZIAN, Robert ,  NETTEKOVEN, Matthias, Heinrich ,  NORCROSS, Roger, David ,  PINARD, Emmanuel ,  STALDER, Henri

    IPC: A61K31/496

    CPC classification number: C07D295/16 ,  A61K31/495 ,  A61K31/496 ,  C07D213/56 ,  C07D213/69 ,  C07D213/74 ,  C07D233/64 ,  C07D239/26 ,  C07D239/42 ,  C07D241/12 ,  C07D251/42 ,  C07D251/48 ,  C07D257/04 ,  C07D263/32 ,  C07D277/30 ,  C07D295/185 ,  C07D309/04 ,  C07D309/20 ,  C07D333/24 ,  C07D409/12

    Abstract: The invention relates to compounds of formula (I) wherein Ar is substituted aryl or unsubstituted or substituted 6-membered heteroaryl, containing one, two or three nitrogen atoms, and wherein the aryl and the heteroaryl groups may be substituted by one or more substituents selected from the group consisting of hydroxy, halogen, CN, (C 1 ­C 6 )-alkyl, (C 1 -C 6 )-alkyl substituted by halogen, (C 1 -C 6 )-alkoxy, (C 1 -C 6 )-alkoxy substituted by halogen, NR 7 R 8 , C(O)R 9 or SO 2 R 10 ; R 1 is hydrogen or (C 1 -C 6 )-alkyl; R 2 is halogen, (C 1 -C 6 ) -alkyl, (C 2 -C 6 ) -alkenyl, wherein a hydrogen atom may be replaced by CN, C(O)-R 9 or (C 1 -C 6 )-alkyl, or is (C 2 -C 6 )­alkynyl, (C 1 -C 6 )-alkyl substituted by halogen, -(CH 2 ) n -(C 3 -C 7 )-cycloalkyl, -(CH 2 ) n -heterocycloalkyl, -C(O)-R 9 , -(CH 2 ) n -aryl or -(CH 2 ) n -5 or -6­membered heteroaryl containing one, two or three heteroatoms, selected from the group consisting of oxygen, sulphur or nitrogen wherein aryl, cycloalkyl, heterocycloalkyl and heteroaryl are unsubstituted or substituted by one or more substituents selected from the group consisting of hydroxy, halogen, (C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkyl substituted by halogen or (C 1 -C 6 ) alkoxy; R 3 , R 4 and R 6 independently from each other are hydrogen, hydroxy, halogen, (C 1 -C 6 )-alkyl or (C 1 -C 6 )-alkoxy; R 5 is NO 2 , CN, C(O)R 9 , SO 2 R 10 or NR 11 R 12 ; R 7 and R 8 independently from each other are hydrogen or (C 1 -C 6 )-alkyl; the other substituents are defined in the claims; and to pharmaceutically acceptable acid addition salts thereof for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.

    Abstract translation: 本发明涉及式（I）化合物，其中Ar是含有一个，两个或三个氮原子的取代的芳基或未取代或取代的6元杂芳基，其中芳基和杂芳基可以被一个或多个选自 由羟基，卤素，CN，（C 1 -C 6） - 烷基，被卤素取代的（C 1 -C 6） - 烷基，（C 1 -C 6） - 烷氧基，被卤素取代的（C 1 -C 6） - 烷氧基，NR 7 R 8，C（O）R 9或SO 2 R 10; R 1是氢或（C 1 -C 6） - 烷基; R 2是卤素，（C 1 -C 6） - 烷基，（C 2 -C 6） - 烯基，其中氢原子可以被CN，C（O）-R 9或（C 1 -C 6） - 烷基 或（C 2 -C 6）炔基，被卤素， - （CH 2）n - （C 3 -C 7） - 环烷基， - （CH 2）n - 杂环烷基，-C（O）-R 含有一个，两个或三个选自氧，硫或氮的杂原子的（CH 2）n - 芳基或 - （CH 2）n-5或 - （CH 2）n-5或-6元杂芳基，其中芳基，环烷基，杂环烷基和 杂芳基是未取代的或被一个或多个选自羟基，卤素，（C 1 -C 6） - 烷基，被卤素或（C 1 -C 6）烷氧基取代的（C 1 -C 6） R 3，R 4和R 6彼此独立地是氢，羟基，卤素，（C 1 -C 6） - 烷基或（C 1 -C 6） - 烷氧基; R 5是NO 2，CN，C（O）R 9，SO 2 R 10或NR 11 R 12; R 7和R 8彼此独立地是氢或（C 1 -C 6） - 烷基; 其它取代基在权利要求中限定; 以及其药学上可接受的酸加成盐，用于治疗精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆和其他认知过程受损的其他疾病，如注意力缺陷障碍或阿尔茨海默病。

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