利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

32 条记录 (耗时 0.021 秒)

    DIAZA-SPIROPIPERIDINE DERIVATIVES
    21.
    发明申请
    DIAZA-SPIROPIPERIDINE DERIVATIVES 审中-公开

    公开(公告)号：WO2005068463A1

    公开(公告)日：2005-07-28

    申请号：PCT/EP2004/014841

    申请日：2004-12-30

    申请人： F. HOFFMANN-LA ROCHE AG ,  CECCARELLI, Simona, Maria ,  JOLIDON, Synese ,  PINARD, Emmanuel ,  THOMAS, Andrew, William

    发明人： CECCARELLI, Simona, Maria ,  JOLIDON, Synese ,  PINARD, Emmanuel ,  THOMAS, Andrew, William

    IPC分类号： C07D471/10

    CPC分类号： C07D471/10

    摘要： The present invention relates to compounds of formula (I); wherein A-B is -CH 2 -CH 2 -, -CH 2 -O- or -O-CH 2 -; X is hydrogen or hydroxy; R l is aryl, optionally substituted by one or two substituents, selected from the group consisting of halogen, lower alkyl, cyano, CF 3 , -OCF 3 , lower alkoxy, -SO 2 -lower alkyl or by heteroaryl, R 2 is aryl, optionally substituted by one or two substituents, selected from the group consisting of halogen, lower alkyl, CF 3 or lower alkoxy; R 3 is hydrogen or lower alkyl; n is 0, 1 or 2; and to their pharmaceutically active salts. The compounds of formula I may 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A-B是-CH 2 -CH 2 - ， - CH 2 -O-或-O-CH 2 - ; X是氢或羟基; R 1是任选被一个或两个选自卤素，低级烷基，氰基，CF 3，-OCF 3，低级烷氧基，-SO 2 - 低级烷基或杂芳基的取代基取代的芳基，R 2是 芳基，任选被一个或两个选自卤素，低级烷基，CF 3或低级烷氧基的取代基取代; R 3是氢或低级烷基; n为0,1或2; 和其药物活性盐。 式I化合物可用于治疗神经和神经精神障碍。

    DIAZA-SPIROPIPERIDINE DERIVATIVES AS INHIBITORS OF TRANSPORTER 1 AND GLYCINE TRANSPORTER 2
    22.
    发明申请
    DIAZA-SPIROPIPERIDINE DERIVATIVES AS INHIBITORS OF TRANSPORTER 1 AND GLYCINE TRANSPORTER 2 审中-公开
    作为运输车辆1和糖果运输车辆2的抑制剂的DIAZA-螺旋磷酸二氢吡啶衍生物

    公开(公告)号：WO2005068462A1

    公开(公告)日：2005-07-28

    申请号：PCT/EP2004/014840

    申请日：2004-12-30

    申请人： F. HOFFMANN-LA ROCHE AG ,  JOLIDON, Synese ,  PINARD, Emmanuel ,  THOMAS, Andrew, William

    发明人： JOLIDON, Synese ,  PINARD, Emmanuel ,  THOMAS, Andrew, William

    IPC分类号： C07D471/10

    CPC分类号： C07D471/10

    摘要： The present invention relates to compounds of formula (I) wherein A-B is CH 2 -CH 2 , -CH 2 -O-, O-CH 2 , CH 2 -S, -S-CH 2 -, CH 2 -C(O)-, C(O)-CH 2 -, .-N(R 4 )-CH 2 - or -CH 2 -N(R 4 )-; R 1 is lower alkyl, lower alkenyl, cycloalkyl, or is aryl, optionally substituted by one or two substituents, selected from the group consisting of halogen, cyano, lower alkyl, CF 3 , OCF 3 or lower alkoxy, or is heteroaryl, optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, CF 3 or lower alkoxy; R 2 is lower alkyl, cycloalkyl, or is aryl, optionally substituted by one or two substituents, selected from the group consisting of halogen, lower alkyl, CF 3 , lower alkoxy, or is heteroaryl, optionally substituted by one or two substituents, selected from the group consisting of halogen, lower alkyl, CF 3 , lower alkoxy, or is heteroaryl, optionally substituted by one or two substituents, selected from the group consisting of halogen, lower alkyl, CF 3, or lower alkoxy; R 3 is hydrogen, lower alkyl or benzyl; R 4 is hydrogen or benzyl; n is 0, 1 or 2; and to pharmaceutically available salts thereof. The compounds of formula I may 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AB是CH 2 -CH 2，-CH 2 -O-，O-CH 2，CH 2 -S，-S-CH 2 - ，CH 2 -C（O） - ，C（O） -CH 2 - ， - N（R 4）-CH 2 - 或-CH 2 -N（R 4） - ; R 1是低级烷基，低级烯基，环烷基或芳基，任选地被一个或两个选自卤素，氰基，低级烷基，CF 3，OCF 3或低级烷氧基的取代基取代，或者是杂芳基，任选地 被一个或两个选自卤素，低级烷基，CF 3或低级烷氧基的取代基取代; R 2是低级烷基，环烷基或芳基，任选被一个或两个选自卤素，低级烷基，CF 3，低级烷氧基或被一个或两个取代基取代的杂芳基取代的取代基取代， 选自卤素，低级烷基，CF 3，低级烷氧基或杂芳基，任选被一个或两个选自卤素，低级烷基，CF 3或低级烷氧基的取代基取代; R 3是氢，低级烷基或苄基; R 4是氢或苄基; n为0,1或2; 及其药学上可用的盐。 式I化合物可用于治疗神经和神经精神障碍。

    1-BENZOYL-PIPERAZINE DERIVATIVES AS GLYCINE UPTAKE INHIBITORS FOR THE TREATMENT OF PSYCHOSES
    23.
    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

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

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

    IPC分类号： A61K31/496

    CPC分类号： 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

    摘要： 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.

    摘要翻译： 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。

    MODULATORS FOR AMYLOID BETA
    26.
    发明申请
    MODULATORS FOR AMYLOID BETA 审中-公开
    AMYLOID BETA的调节剂

    公开(公告)号：WO2010040661A1

    公开(公告)日：2010-04-15

    申请号：PCT/EP2009/062570

    申请日：2009-09-29

    申请人： F. HOFFMANN-LA ROCHE AG ,  GOETSCHI, Erwin ,  JOLIDON, Synese ,  LUEBBERS, Thomas

    发明人： GOETSCHI, Erwin ,  JOLIDON, Synese ,  LUEBBERS, Thomas

    IPC分类号： C07D401/14 ,  C07D403/12 ,  A61P25/28 ,  A61K31/53

    CPC分类号： C07D413/14 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14

    摘要： The invention relates to compounds of formula (I) wherein R 1 is hydrogen, lower alkyl or is lower alkyl substituted by hydroxy; R 2 is hydrogen, lower alkoxy or lower alkyl; R 3 /R 4 are independently from each other hydrogen, halogen, lower alkyl, C(O)O-lower alkyl, OR', NR''R"', lower alkyl substituted by halogen or hydroxy, or is phenyl or benzyl, optionally substituted by one or two halogen atoms; R' is lower alkyl, or is phenyl, benzyl or pyridinyl, which rings are optionally substituted by one or more halogen, lower alkyl or lower alkyl substituted by fluoro; R'' is hydrogen or lower alkyl; R'" is lower alkyl, lower alkyl substituted by one or two hydroxy groups, CH(CH 2 OH)-phenyl, or is -(CH 2 ) 2 O-lower alkyl, or is phenyl substituted by halogen, or R'' and R''' form together with the N-atom to which they are attached a heterocyclic ring, optionally substituted by one or more lower alkyl, CH 2 C(O)O-lower alkyl, or by CH 2 C(O)OH; Ar is a fϊve-membered heteroaryl group; or to pharmaceutically active acid addition salts. It has been found that the present 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 β-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.

    摘要翻译： 本发明涉及式（I）化合物，其中R 1是氢，低级烷基或被羟基取代的低级烷基; R2是氢，低级烷氧基或低级烷基; R 3 / R 4彼此独立地为氢，卤素，低级烷基，C（O）O-低级烷基，OR'，NR“R”'，被卤素或羟基取代的低级烷基，或为苯基或苄基， R 1为低级烷基，或为苯基，苄基或吡啶基，该环任选被一个或多个卤素，被氟取代的低级烷基或低级烷基取代; R“为氢或低级烷基; R'是低级烷基，被一个或两个羟基取代的低级烷基，CH（CH 2 OH） - 苯基，或是 - （CH 2）2 O-低级烷基，或被卤素取代的苯基，或R“和R” （O）O-低级烷基，或被一个或多个低级烷基取代的杂环，或者被一个或多个低级烷基取代。 Ar是一个五元组杂芳基; 或药用活性酸加成盐。 已经发现，本发明的式（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， 和其他疾病如脑淀粉样血管病，遗传性脑出血伴淀粉样变性，荷兰型（HCHWA-D），多发性梗塞性痴呆，痴呆和唐氏综合征。

    DI-AROMATIC SUBSTITUTED AMIDES AS INHIBITORS FOR GLYT1
    28.
    发明申请
    DI-AROMATIC SUBSTITUTED AMIDES AS INHIBITORS FOR GLYT1 审中-公开
    作为GLYT1抑制剂的DI-AROMATIC取代的氨基酸

    公开(公告)号：WO2008022938A1

    公开(公告)日：2008-02-28

    申请号：PCT/EP2007/058350

    申请日：2007-08-13

    申请人： F. HOFFMANN-LA ROCHE AG ,  JOLIDON, Synese ,  NARQUIZIAN, Robert ,  PINARD, Emmanuel

    发明人： JOLIDON, Synese ,  NARQUIZIAN, Robert ,  PINARD, Emmanuel

    IPC分类号： C07C237/22 ,  C07C255/57 ,  C07C271/22 ,  C07C275/24 ,  C07D213/40 ,  C07D213/81 ,  C07D261/18 ,  C07D275/02 ,  C07D279/02 ,  C07D307/79 ,  C07D333/20 ,  C07D333/38 ,  C07D333/44 ,  C07D335/18 ,  A61K31/16

    CPC分类号： C07C237/22 ,  C07C255/57 ,  C07C271/22 ,  C07C275/24 ,  C07C2601/14 ,  C07D213/40 ,  C07D213/81 ,  C07D261/18 ,  C07D275/02 ,  C07D279/02 ,  C07D307/79 ,  C07D333/20 ,  C07D333/38 ,  C07D333/44 ,  C07D335/18

    摘要： The present invention relates to compounds of the general Formula (I) wherein (A) is a 5 or 6-membered aromatic or heteroaromatic ring; R 1 is cycloalkyl or is aryl or heteroaryl, wherein at least one ring is aromatic in nature, unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, -C(O) -lower alkyl, -S(O) 2 -lower alkyl, nitro or cyano; R 2 is hydrogen or lower alkyl; R 3 is hydrogen or lower alkyl; R 4 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or nitro; R 5 is hydrogen, halogen, lower alkyl or lower alkyl substituted by halogen; X is a bond, -(CH 2 ) m -, -CH 2 O- or -CH 2 NH-; The dotted line denotes a bond or not; n is 1 or 2; m is 1, 2 or 3; and pharmaceutically acceptable acid addition salts thereof and their use in the treatment of neurological and neuropsychiatric disorders.

    摘要翻译： 本发明涉及通式（I）的化合物，其中（A）是5或6元芳族或杂芳族环; R 1是环烷基或芳基或杂芳基，其中至少一个环在本质上是芳族的，未被取代或被1至3个选自以下的取代基取代：卤素，低级烷基，被 卤素，低级烷氧基，被卤素取代的低级烷氧基，-C（O） - 低级烷基，-S（O）2 - 低级烷基，硝基或氰基; R 2是氢或低级烷基; R 3是氢或低级烷基; R 4是卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素或硝基取代的低级烷氧基; R 5是氢，卤素，被卤素取代的低级烷基或低级烷基; X是一个键， - （CH 2）2 - ， - CH 2 O-或-CH 2 - NH-; 虚线表示不是键; n为1或2; m为1,2或3; 及其药学上可接受的酸加成盐及其在治疗神经和神经精神障碍中的用途。

    SUBSTITUTED PHENYL METHANONE DERIVATIVES
    29.
    发明申请
    SUBSTITUTED PHENYL METHANONE DERIVATIVES 审中-公开

    公开(公告)号：WO2007147770A3

    公开(公告)日：2007-12-27

    申请号：PCT/EP2007/055871

    申请日：2007-06-14

    申请人： F. HOFFMANN-LA ROCHE AG ,  JOLIDON, Synese ,  NARQUIZIAN, Robert ,  NORCROSS, Roger ,  PINARD, Emmanuel

    发明人： JOLIDON, Synese ,  NARQUIZIAN, Robert ,  NORCROSS, Roger ,  PINARD, Emmanuel

    IPC分类号： C07D205/04 ,  C07D207/06 ,  C07D211/16 ,  C07D407/10 ,  A61K31/445 ,  A61P25/18

    摘要： The present invention relates to compounds of the general formula (i), wherein R 1 is -OR 1 ' , heterocycloalkyl, aryl or heteroaryl, which are unsubstituted or substituted by lower alkyl or halogen; R1' is lower alkyl, lower alkyl substituted by halogen, or is -(CH 2 ) o -cycloalkyl; R 2 is -S(O) 2 -lower alkyl, -S(O) 2 NH-lower alkyl, NO 2 or CN; R 3 is aryl or heteroaryl, which are unsubstituted or substituted by one to three substituents, selected from the group consisting of lower alkyl, lower alkoxy, CN, NO 2 , halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, aryl or sulfonamide; X is a bond, -CH 2 -, -NH-, -CH 2 O- or -OCH 2 -; n is 1 or 2; m is 1 or 2; o is 0 or 1; to pharmaceutically acceptable acid addition salts thereof, to pharmaceutical compositions containing them and their use in the treatment of neurological and neuropsychiatric disorders. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1).

    [4-(HETEROARYL) PIPERAZIN-1-YL]-(2,5-SUBSTITUTED -PHENYL)METHANONE DERIVATIVES AS GLYCINE TRANSPORTER 1 (GLYT-1) INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS
    30.
    发明申请
    [4-(HETEROARYL) PIPERAZIN-1-YL]-(2,5-SUBSTITUTED -PHENYL)METHANONE DERIVATIVES AS GLYCINE TRANSPORTER 1 (GLYT-1) INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS 审中-公开
    作为用于治疗神经病学和神经病学疾病的甘氨酸运输1（GLYT-1）抑制剂的[4-（异丁基）哌嗪-1-基] - （2,5-取代的苯基）甲酮衍生物

    公开(公告)号：WO2006072436A1

    公开(公告)日：2006-07-13

    申请号：PCT/EP2005/014082

    申请日：2005-12-28

    申请人： F. HOFFMANN-LA ROCHE AG ,  JOLIDON, Synese ,  NARQUIZIAN, Robert ,  NORCROSS, Roger, David ,  PINARD, Emmanuel

    发明人： JOLIDON, Synese ,  NARQUIZIAN, Robert ,  NORCROSS, Roger, David ,  PINARD, Emmanuel

    IPC分类号： A61K31/427 ,  A61K31/433 ,  A61P25/28 ,  C07D277/42 ,  C07D277/56 ,  C07D417/12 ,  C07D285/12 ,  C07D285/08

    CPC分类号： C07D285/08 ,  C07D277/42 ,  C07D277/56 ,  C07D285/135 ,  C07D417/12

    摘要： The present invention relates to compounds of the general formula (I) wherein R 1 is-OR 1’ ,-SR 1’ or is a heterocycloalkyl group; R 1’ is lower alkyl, lower alkyl substituted by halogen or is -(CH 2 ) n -cycloalkyl; R 2 is-S(O) 2 -lower alkyl, -S(O) 2 NH-lower alkyl, NO 2 or CN; X 1 is CR 3 or N; X 2 is CR 3’ or N; R 3 /R 3’ are independently from each other hydrogen, halogen, lower alkyl, CN, NO 2 ,-S(O) 2 -phenyl, -S(O) 2 -lower alkyl, -S(O) 2 -pyridin-2, 3 or 4-yl, phenyl, optionnally substituted by one or two substituents selected from the group consisting of NO 2 or halogen, or is lower alkyl substituted by halogen or is -C(O)-lower alkyl; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1). They may be used in the treatment of schizophrenia.

    摘要翻译： 本发明涉及通式（I）的化合物，其中R 1是 - 或 - 1'， - SR 1'或其是 杂环烷基 R 1是低级烷基，被卤素取代的低级烷基或是 - （CH 2 CH 2）n - 环烷基; R 2是-S（O）2 - 低级烷基，-S（O）2 NH-低级烷基，NO 2 或CN; X 1是CR 3或N; X 2是CR 3或N; R 3和R 3彼此独立地为氢，卤素，低级烷基，CN，NO 2，-S（O） -S（O）2 - 低级烷基，-S（O）2 - 吡啶基-2,3或4-基 - ，苯基，其选自一个或两个选自NO 2或卤素的取代基，或被卤素取代的低级烷基或-C（O） - 低级烷基; n为0,1或2; 及其药学上可接受的酸加成盐。 已经发现通式（I）的化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂。 它们可用于治疗精神分裂症。