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    4- (SULFANYL-PYRIMIDIN-4-YLMETHYL) -MORPHOLINE DERIVATIVES AND RELATED COMPOUNDS AS GABA RECEPTOR LIGANDS FOR THE TREATMENT OF ANXIETY, DEPRESSION AND EPILEPSY
    5.
    发明申请
    4- (SULFANYL-PYRIMIDIN-4-YLMETHYL) -MORPHOLINE DERIVATIVES AND RELATED COMPOUNDS AS GABA RECEPTOR LIGANDS FOR THE TREATMENT OF ANXIETY, DEPRESSION AND EPILEPSY 审中-公开
    4-（SULFANYL-吡啶基-4-甲基乙基） - 吗啉衍生物及相关化合物作为GABA受体配体，用于治疗放射性疾病，恶化和恶化

    公开(公告)号：WO2005094828A1

    公开(公告)日：2005-10-13

    申请号：PCT/EP2005/001814

    申请日：2005-02-22

    申请人： F. HOFFMANN-LA ROCHE AG ,  MALHERBE, Pari ,  MASCIADRI, Raffaello ,  PRINSSEN, Eric ,  SPOOREN, Will ,  THOMAS, Andrew, William

    发明人： MALHERBE, Pari ,  MASCIADRI, Raffaello ,  PRINSSEN, Eric ,  SPOOREN, Will ,  THOMAS, Andrew, William

    IPC分类号： A61K31/506

    CPC分类号： C07D239/38 ,  C07D239/42 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D471/14 ,  C07D491/10

    摘要： The present invention relates to compounds of Formula (I) wherein X is -S- or -NH-; R 1 is alkyl, alkenyl, arylalkyl, arylalkenyl or aryl-O-alkyl, wherein the aryl groups are optionally substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen or lower halogen-alkyl; R 2 is hydrogen, lower alkyl or cycloalkyl; R 3 /R 4 may form together with the N-atom to which they are attached a non aromatic5, 6 or 7 membered ring, which may contain in addition to the N-atom one additional heteroatom selected from the group consisting of O, S or N, and wherein the ring is optionally substituted by hydroxy, lower alkyl, lower alkoxy, -NR 2 , -CONR 2 , -CO-lower alkyl or benzyl; or may form together with the N-atom to which they are attached a heterocyclic ring system, containing at least two rings and which may contain one or two additional heretoatoms, selected from the group consisting of N or O; R is hydrogen or lower alkyl; R 5 is hydrogen or lower alkyl; and to pharmaceutically suitable acid addition salts thereof. It has been found that the compounds are active on the GABA B receptor and therefore useful for the treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, psychosis, panic disorder, posttraumatic stress disorders or gastro-intestinal disorders.

    摘要翻译： 本发明涉及其中X为-S-或-NH-的式（I）化合物; R 1是烷基，烯基，芳基烷基，芳基烯基或芳基-O-烷基，其中芳基任选被一个或多个选自下列的取代基取代：低级烷基，低级烷氧基，卤素或低级卤代烷基 ; R 2是氢，低级烷基或环烷基; R 3 / R 4可以与它们所连接的N-原子一起形成非芳族5,6或7元环，除了N-原子外，还可以含有一个另外的杂原子，该杂原子选自 的O，S或N，并且其中所述环任选被羟基，低级烷基，低级烷氧基，-NR 2，-CONR 2，-CO-低级烷基或苄基取代; 或者可以与它们所连接的N-原子一起形成含有至少两个环的杂环体系，并且可以含有一个或两个选自N或O的另外的原子， R是氢或低级烷基; R 5是氢或低级烷基; 和其药学上合适的酸加成盐。 已经发现这些化合物对GABA B受体有活性，因此可用于治疗焦虑，抑郁，癫痫，精神分裂症，认知障碍，痉挛和骨骼肌僵硬，脊髓损伤，多发性硬化，肌萎缩性侧索硬化，脑性麻痹 ，神经性疼痛和与可卡因和尼古丁相关的渴望，精神病，恐慌症，创伤后应激障碍或胃肠疾病。

    N-ACYLAMINOBENZENE DERVATIVES AS SELECTIVE MONOAMINE OXIDASE B INHIBITORS
    6.
    发明申请
    N-ACYLAMINOBENZENE DERVATIVES AS SELECTIVE MONOAMINE OXIDASE B INHIBITORS 审中-公开
    作为选择性单胺氧化酶B抑制剂的N-亚氨基苯甲酸衍生物

    公开(公告)号：WO2003099763A1

    公开(公告)日：2003-12-04

    申请号：PCT/EP2003/005297

    申请日：2003-05-21

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： JOLIDON, Synese ,  RODRIGUEZ SARMIENTO, Rosa, Maria ,  THOMAS, Andrew, William ,  WYLER, Rene

    IPC分类号： C07C233/25

    CPC分类号： C07C259/06 ,  C07C233/15 ,  C07C233/25 ,  C07C233/33 ,  C07C233/60 ,  C07C235/16 ,  C07C237/04 ,  C07C237/22 ,  C07C243/14 ,  C07C243/28 ,  C07C255/19 ,  C07C255/23 ,  C07C255/25 ,  C07C323/41 ,  C07C2601/02

    摘要： This invention relates to N-acylamino aryl derivatives of the general formula (I), wherein R 1 is halogen, halogen-(C 1 -C 6 )-alkyl, cyano, C 1 -C 6 -alkoxy or halogen-(C 1 -C 6 )-alkoxy; R 21 , R 22 , R 23 and R 24 independently from each other are selected from the group consisting of hydrogen, (C 1 -C 6 )-alkyl, halogen, halogen-(C 1 -C 6 )-alkyl, hydroxy, C 1 -C 6 -alkoxy or -CHO; R 3 is hydrogen or C 1 -C 3 -alkyl; R 4 , R 5 independently from each other are selected from the group consisting of hydrogen, C 1- C 6 -alkyl, C 1 -C 6 -alkoxy or -COO(C 1 -C 6 )alkyl; or R 4 and R 5 form together with the C-atom to which they are attach a C 3 -C 7 -cycloalkyl ring; R 6 is -CO-NR 7 R 8 ; -COO(C 1 -C 6 )-alkyl, -CN, -NR 2 or -NHC(O)R; R 7 and R 8 independently from each other are selected from the group consisting of hydrogen, C 1- C 6 -alkyl, NH 2 or hydroxy; R is hydrogen or C 1 -C 6 -alkyl; n is 0, 1, 2 or 3. X is -CHRO, -OCHR, -CH 2 S-, -SCH 2 -, -CH 2 CH 2 -, -CH=CH- or -C≡C-; and to pharmaceutically active acid addition salts thereof. It has been found that the compounds of general formula (I) are selective monoamine oxidase B inhibitors and they are therefore useful in the treatment of diseases mediated by monoamine oxidase B inhibitors, for example for the treatment of Alzheimer’s disease or senile dementia.

    摘要翻译： 本发明涉及通式（I）的N-酰基氨基芳基衍生物，其中R 1是卤素，卤素 - （C 1 -C 6） - 烷基，氰基，C 1 -C 6 - 烷氧基或卤素 - （C 1 -C 6） 烷氧基; R 21，R 22，R 23和R 24彼此独立地选自氢，（C 1 -C 6） - 烷基，卤素，卤素 - （C 1 -C 6） - 烷基，羟基，C 1 -C 6 - 烷氧基或-CHO; R 3是氢或C 1 -C 3 - 烷基; R 4，R 5彼此独立地选自氢，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基或-COO（C 1 -C 6）烷基; 或R 4和R 5与它们所连接的C-C原子一起形成C 3 -C 7 - 环烷基环; R 6是-CO-NR 7 R 8; -COO（C 1 -C 6） - 烷基，-CN，-NR 2或-NHC（O）R; R 7和R 8彼此独立地选自氢，C 1 -C 6 - 烷基，NH 2或羟基; R是氢或C 1 -C 6 - 烷基; n是0,1,2或3.X是-CHRO，-OCHR，-CH 2 S - ， - CH 2 - ， - CH 2 CH 2 - ， - CH = CH-或-C = C-; 及其药物活性的酸加成盐。 已经发现通式（I）的化合物是选择性单胺氧化酶B抑制剂，因此它们可用于治疗由单胺氧化酶B抑制剂介导的疾病，例如用于治疗阿尔茨海默氏病或​​老年痴呆症。

    ISOQUINOLINE DERIVATIVES
    7.
    发明申请
    ISOQUINOLINE DERIVATIVES 审中-公开
    异喹啉衍生物

    公开(公告)号：WO2003091219A1

    公开(公告)日：2003-11-06

    申请号：PCT/EP2003/003845

    申请日：2003-04-14

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： CESURA, Andrea ,  RODRIGUEZ SARMIENTO, Rosa Maria ,  SCALONE, Michelangelo ,  THOMAS, Andrew, William ,  WYLER, Rene

    IPC分类号： C07D217/24

    CPC分类号： C07D217/24

    摘要： This invention relates to isoquinolino derivatives of the general Formula (I) wherein Y is >C=O or CH 2 -, Z is >C=O or CH 2 -, and R 1 , R 2 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to medicaments containing these compounds, a process for their preparation as well as their use for preparation of medicaments for the treatment or prevention of diseases in which MAO-B inhibitors might be beneficial.

    摘要翻译： 本发明涉及通式（I）的异喹啉衍生物，其中Y为> C = O或CH 2 - ，Z为> C = O或CH 2 - ，R 1，R 2和m如 说明书及其药学上可接受的盐。 本发明还涉及含有这些化合物的药物，其制备方法及其制备用于治疗或预防MAO-B抑制剂可能有益的疾病的药物的用途。

    IMIDAZO-BENZODIAZEPINE DERIVATIVES
    8.
    发明申请
    IMIDAZO-BENZODIAZEPINE DERIVATIVES 审中-公开
    咪唑 - 苯二酮衍生物

    公开(公告)号：WO2006045430A1

    公开(公告)日：2006-05-04

    申请号：PCT/EP2005/010908

    申请日：2005-10-11

    申请人： F. HOFFMANN-LA ROCHE AG ,  KNUST, Henner ,  THOMAS, Andrew, William

    发明人： KNUST, Henner ,  THOMAS, Andrew, William

    IPC分类号： C07D487/14 ,  A61K31/55

    CPC分类号： C07D487/14

    摘要： The present invention is concerned with substituted imidazo [1,5-a] [1,2,4] triazolo [1,5­d] [1,4]benzodiazepine derivatives of formula (I) wherein R 1 is hydrogen, halogen, lower alkyl, lower alkynyl, cycloalkyl, heterocycloalkyl, benzyl, cyano, lower alkoxy, OCF 3 , -NHR, -NHC(O)R or -NHSO 2 R; R 2 is lower alkyl substituted by halogen; R 3 is hydrogen, methyl or aryl; R is lower alkyl, cycloalkyl or aryl; 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 α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders, anxiety, schizophrenia or Alzheimer's disease.

    摘要翻译： 本发明涉及式（I）的取代的咪唑并[1,5-a] [1,2,4]三唑并[1,5d] [1,4]苯并二氮杂衍生物，其中R 1， 卤素，低级烷基，低级炔基，环烷基，杂环烷基，苄基，氰基，低级烷氧基，OCF 3，-NHR，-NHC（O）R或-NHSO 2， / SUB> R等 R 2是被卤素取代的低级烷基; R 3是氢，甲基或芳基; R是低级烷基，环烷基或芳基; 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 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，焦虑，精神分裂症或阿尔茨海默病。