中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

305 records (took 0.026 seconds)

    3-ARYL-ISOXAZOLE-4-CARBONYL-BENZOFURAN DERIVATIVES
    1.
    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-IMIDAZOLE DERIVATIVES
    2.
    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。

    PIPERIDINE DERIVATIVES
    3.
    发明申请
    PIPERIDINE DERIVATIVES 审中-公开
    哌啶衍生物

    公开(公告)号：WO2011101304A3

    公开(公告)日：2011-10-20

    申请号：PCT/EP2011052101

    申请日：2011-02-14

    Applicant: HOFFMANN LA ROCHE ,  BAUMANN KARLHEINZ ,  FLOHR ALEXANDER ,  GOETSCHI ERWIN ,  GREEN LUKE ,  JOLIDON SYNESE ,  KNUST HENNER ,  LIMBERG ANJA ,  LUEBBERS THOMAS ,  THOMAS ANDREW

    Inventor： BAUMANN KARLHEINZ ,  FLOHR ALEXANDER ,  GOETSCHI ERWIN ,  GREEN LUKE ,  JOLIDON SYNESE ,  KNUST HENNER ,  LIMBERG ANJA ,  LUEBBERS THOMAS ,  THOMAS ANDREW

    IPC: C07D401/14 ,  A61K31/4523 ,  A61P25/28 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

    CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D498/04

    Abstract: The invention relates to compounds of formula (I). Hetaryl I is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; hetaryl II is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N, or is a two membered ring system containing 1 to 4 heteroatoms selected from S, O or N, wherein at least one ring is aromatic in nature; R1 is lower alkyl, lower alkoxy, lower alkyl substituted by halogen, or halogen; R2 is halogen, lower alkyl, lower alkoxy, hydroxy, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy or benzo[1,3]dioxolyl, or is -(CHR)p-phenyl, optionally substituted by halogen, lower alkyl, lower alkoxy, S(O)2-lower alkyl, cyano, nitro, lower alkoxy substituted by halogen, dimethylamino, -(CH2)P-NHC(O)O-Iower alkyl, or lower alkyl substituted by halogen, and R is hydrogen, halogen, hydroxy or lower alkoxy, or is cycloalkenyl or cycloalkyl, optionally substituted by hydroxy or lower alkyl substituted by halogen, or is a five or six membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N, which is optionally substituted by halogen, lower alkyl, lower alkoxy or dimethylamino, or is O-phenyl, optionally substituted by halogen, or is heterocycloalkyl, optionally substituted by halogen, hydroxy, lower alkyl substituted by halogen or C(O)O-lower alkyl; R3 is hydrogen, lower alkyl, cyano or phenyl; R4 is lower alkoxy, lower alkyl or halogen; p is 0 or 1; n is 0, 1 or 2; if n is 2 then R4 may be the same or different; m is 0, 1 or 2; if m is 2 then R1 may be the same or different; o is 0, 1, 2 or 3, if o is 2 or 3 then R2 may be the same or different; or to pharmaceutically active acid addition salts thereof. The compounds of formula (I) are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ß-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

    Abstract translation: 本发明涉及式（I）化合物。 芳基I是含有1至3个选自O，S或N的杂原子的五或六元杂芳基; 杂芳基II是含有1至3个选自O，S或N的杂原子的五或六元杂芳基，或是含有1至4个选自S，O或N的杂原子的二元环体系，其中至少一个环 本质上是芳香的 R1是低级烷基，低级烷氧基，被卤素取代的低级烷基或卤素; R 2为卤素，低级烷基，低级烷氧基，羟基，被卤素取代的低级烷基，被羟基或苯并[1,3]二氧杂环戊烯取代的低级烷基，或为 - （CHR）对 - 苯基，任选被卤素，低级烷基， 低级烷氧基，S（O）2-低级烷基，氰基，硝基，被卤素取代的低级烷氧基，二甲基氨基， - （CH2）P-NHC（O）O-低级烷基或被卤素取代的低级烷基，R是氢 ，卤素，羟基或低级烷氧基，或是任选被羟基或被卤素取代的低级烷基取代的环烯基或环烷基，或是含有1至3个选自O，S或N的杂原子的五或六元杂芳基，其中 或任选被卤素取代的O-苯基，或任选被卤素取代的杂环烷基，羟基，被卤素或C（O）O-低级烷基取代的低级烷基， ; R3是氢，低级烷基，氰基或苯基; R4是低级烷氧基，低级烷基或卤素; p为0或1; n为0,1或2; 如果n为2，则R4可以相同或不同; m为0,1或2; 如果m为2，则R1可以相同或不同; o为0,1,2或3，如果o为2或3，则R2可以相同或不同; 或其药物活性的酸加成盐。 式（I）化合物是淀粉样蛋白β的调节剂，因此它们可用于治疗或预防与脑中β-淀粉样蛋白沉积相关的疾病，特别是阿尔茨海默病，以及其他疾病如脑 淀粉样血管病，淀粉样变性遗传性脑出血，荷兰型（HCHWA-D），多发性梗死性痴呆，痴呆和唐氏综合征。

Patent Agency Ranking