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    ARYL-ISOXAZOL-4-YL-IMIDAZOLE DERIVATIVES
    1.
    发明申请
    ARYL-ISOXAZOL-4-YL-IMIDAZOLE DERIVATIVES 审中-公开
    ARYL-ISOXAZOL-4-Y-IMIDAZOLE DERIVATIVES

    公开(公告)号：WO2007074078A2

    公开(公告)日：2007-07-05

    申请号：PCT/EP2006069722

    申请日：2006-12-14

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

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

    CPC classification number: C07D413/04

    Abstract: The present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula (I), wherein R 1 to R 3 are each independently hydrogen or halogen; R 4 is hydrogen, lower alkyl, cycloalkyl, -(CH 2 ) n -O-lower alkyl or lower alkyl substituted by hydroxy; R 5 is -(CH 2 ) m -aryl or -(CH 2 ) m -heteroaryl which are optionally substituted by one or more substituents selected from the group consisting of halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkylsulfanyl, lower alkyl substituted by halogen, -C(O)-lower alkyl, -C(O)-O-lower alkyl, -NH-C(O)-O-lower alkyl or -C(O)-NH-R', wherein R' is lower alkynyl or lower alkyl substituted by halogen, or is -(CH 2 ) n -cycloalkyl, -(CH 2 ) n -heterocyclyl, -(CH 2 ) n -heteroaryl or -(CH 2 ) n -aryl, optionally substituted by halogen; R 6 is hydrogen, -C(O)H, -(CH 2 ) n -O-lower alkyl, -C(O)O-lower alkyl, lower alkyl substituted by hydroxy or halogen, or is cycloalkyl, aryl, or is -(CH 2 ) n -O-CH 2 -aryl, optionally substituted by halogen or lower alkyl, or is -(CH 2 ) n -O-CH 2 -heteroaryl, optionally substituted by halogen, lower alkyl or lower alkyl substituted by halogen, or is -(CH 2 ) n -NH-(CH 2 ) o -heterocyclyl; n is 0, 1, 2 or 3 m is 0 or 1; o is 1, 2 or 3; as well as with pharmaceutically acceptable acid addition salts thereof. It has been found that this class of compounds show high affinity and selectivity for GABA A a5 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-基 - 咪唑衍生物，其中R 1至R 3各自独立地为氢或卤素; R 4是氢，低级烷基，环烷基， - （CH 2）n -O- -O-低级烷基或被羟基取代的低级烷基; R 5是 - （CH 2）2 - 或 - （CH 2 CH 2）m - 任选地被一个或多个选自卤素，氰基，硝基，低级烷基，低级烷氧基，低级烷基硫烷基，被卤素取代的低级烷基，-C（O） - 低级烷基， -C（O）-O-低级烷基，-NH-C（O）-O-低级烷基或-C（O）-NH-R'，其中R'为低级炔基或被卤素取代的低级烷基， - （CH 2）n - 环烷基， - （CH 2）n - 杂环基， - （CH 2 CH 2） - （CH 2）n - 芳基，任选被卤素取代; - （CH 2）n - R 6是氢，-C（O）H， - （CH 2）n -O-低级烷基，-C（O） O-低级烷基，被羟基或卤素取代的低级烷基，或是环烷基，芳基或 - （CH 2）n -O-CH 2， 或任选被卤素或低级烷基取代的芳基，或为 - （CH 2）n -O-CH 2 - 杂芳基 任选被卤素取代的低级烷基或被卤素取代的低级烷基，或者是 - （CH 2 CH 2）n -NH-（CH 2） ） 0 - 杂环基; n为0,1,2或3m为0或1; o是1,2或3; 以及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 A a5受体结合位点的高亲和力和选择性，并且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。

    3-ARYL-ISOXAZOLE-4-CARBONYL-BENZOFURAN DERIVATIVES
    2.
    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。

    Aryl-isoxazol-4-yl-imidazo[1, 5-a]pyridine derivatives
    3.
    发明专利
    Aryl-isoxazol-4-yl-imidazo[1, 5-a]pyridine derivatives 未知

    公开(公告)号：AU2006331363B2

    公开(公告)日：2012-07-05

    申请号：AU2006331363

    申请日：2006-12-18

    Applicant: HOFFMANN LA ROCHE

    Inventor： HAN BO ,  BUETTELMANN BERND ,  THOMAS ANDREW ,  KNUST HENNER ,  DONG JIAQIANG

    IPC: C07D471/04 ,  A61K31/4188 ,  A61K31/437 ,  A61P25/28

    Abstract: The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives of formula (I) wherein: R is hydrogen, halogen, hydroxy, lower alkyl, benzyloxy or -O-(CH)-(CO)-5 or 6 membered heteroaryl optionally substituted by aryl and lower alkyl; R is hydrogen, lower alkyl, or -(CO)-R; R is hydrogen, halogen, cyano, lower alkyl, or -(CO)-R; R is hydroxy, lower alkoxy, NR'R'', wherein R' and R'' are each independently hydrogen, cycloalkyl, 5 or 6-membered heterocycloalkyl or lower alkyl optionally substituted by cycloalkyl, cyano, 5 or 6-membered heterocycloalkyl or 5 or 6-membered heteroaryl; as well as pharmaceutically acceptable acid addition salts thereof. It has been found that this class of compounds show high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

    7.
    发明专利
    未知

    公开(公告)号：BRPI0616184A2

    公开(公告)日：2011-06-07

    申请号：BRPI0616184

    申请日：2006-09-07

    Applicant: HOFFMANN LA ROCHE

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

    IPC: C07D413/14 ,  A61K31/42 ,  A61P25/28 ,  C07D413/06 ,  C07D451/06

    Abstract: The present invention is concerned with aryl-isoxazole-4-carbonyl-pyrrole-2-carboxylic acid amide derivatives of formula wherein R1, R2, R3, R4, and R5, and m are as defined herein and with their pharmaceutically acceptable acid addition salts. This class of compounds have high affinity and selectivity for GABA A alpha5 receptor binding sites and therefore may be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

    10.
    发明专利
    未知

    公开(公告)号：AT466858T

    公开(公告)日：2010-05-15

    申请号：AT06819173

    申请日：2006-10-27

    Applicant: HOFFMANN LA ROCHE

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

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

    Abstract: The present invention is concerned with 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives of formula I wherein R 1 , R 2 , and R 3 are as defined in the specification and claims and with their pharmaceutically acceptable acid addition salts. These compounds have a high affinity and selectivity for GABA A alpha5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.

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