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    PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE
    2.
    发明申请
    PIPERAZINE THIAZOLE DERIVATIVES USEFUL IN THE TREATMENT OF TAUOPATHIES SUCH AS ALZHEIMER'S DISEASE 审中-公开
    用于治疗诸如阿尔茨海默病的TAUOPATHIES的哌嗪衍生物

    公开(公告)号：WO2013024168A1

    公开(公告)日：2013-02-21

    申请号：PCT/EP2012/066136

    申请日：2012-08-17

    Applicant: REMYND NV ,  GRIFFIOEN, Gerard ,  CECERE, Giuseppe ,  NETTEKOVEN, Matthias ,  PRINCEN, Katrien ,  RATNI, Hasane ,  ROGERS-EVANS, Mark ,  VIFIAN, Walter

    Inventor： GRIFFIOEN, Gerard ,  CECERE, Giuseppe ,  NETTEKOVEN, Matthias ,  PRINCEN, Katrien ,  RATNI, Hasane ,  ROGERS-EVANS, Mark ,  VIFIAN, Walter

    IPC: C07D285/08 ,  C07D417/04 ,  C07D417/12 ,  A61K31/433 ,  A61P25/28

    CPC classification number: A61K31/496 ,  C07D285/08 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

    Abstract: The present invention relates to a compound of formula (IA), wherein G 1 is lower alkyl; lower alkyl substituted by one or more halogens; cycloalkyl; tetrahydropyran-4-yl; phenethyl; phenethyl substituted by one or more halogens; phenoxymethyl; phenoxymethyl substituted by one or more halogens; benzyloxyethyl; benzyloxy-ethyl substituted by one or more halogens; or is -NR 2 R 3 ; R 2 is hydrogen or lower alkyl; R 3 is lower alkyl; tetrahydropyran-4-yl; -CH 2 -cycloalkyl; or cycloalkyl optionally substituted by lower alkyl substituted by one or more halogens; or R 2 and R 3 form together with the N-atom to which they are attached a heterocycloalkyl group with 4 or 5 carbon atoms, which is optionally substituted by one or more substituents selected from halogen; or lower alkyl substituted by one or more halogens; X is -CH 2 - or -(CH 2 ) 2 -; Ar is phenyl or pyridinyl; R 4 is halogen; lower alkyl; lower alkyl substituted by one or more halogens; or lower alkoxy; n is 1 or 2; or to a pharmaceutically active salt thereof, to a stereoisomeric form, including an individual diastereoisomer or enantiomer of the compound of formula (IA) as well as to a racemic or non-racemic mixture thereof. The present invention also relates to the use of a compound of formula (IA) for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.

    Abstract translation: 本发明涉及式（IA）化合物，其中G 1为低级烷基; 被一个或多个卤素取代的低级烷基; 环烷基; 四氢吡喃-4-基; 苯; 被一个或多个卤素取代的苯乙基; 苯氧基; 被一个或多个卤素取代的苯氧基甲基; 苄氧; 由一个或多个卤素取代的苄氧基 - 乙基; 或为-NR2R3; R2是氢或低级烷基; R3是低级烷基; 四氢吡喃-4-基; -CH 2 - 环烷基; 或任选被被一个或多个卤素取代的低级烷基取代的环烷基; 或R 2和R 3与它们所连接的N-原子一起形成具有4或5个碳原子的杂环烷基，其任选被一个或多个选自卤素的取代基取代; 或被一个或多个卤素取代的低级烷基; X是-CH 2 - 或 - （CH 2）2 - ; Ar是苯基或吡啶基; R4是卤素; 低级烷基 被一个或多个卤素取代的低级烷基; 或低级烷氧基; n为1或2; 或其药物活性盐与立体异构体形式，包括式（IA）化合物的单独非对映异构体或对映异构体以及其外消旋或非外消旋混合物。 本发明还涉及式（IA）化合物用于治疗以细胞毒性TAU错误折叠和/或聚集为特征的某些神经变性疾病的用途。

    PYRROLIDINE DERIVATIVES AS NK3 ANTAGONISTS
    3.
    发明申请
    PYRROLIDINE DERIVATIVES AS NK3 ANTAGONISTS 审中-公开
    吡咯啉衍生物作为NK3拮抗剂

    公开(公告)号：WO2012093109A1

    公开(公告)日：2012-07-12

    申请号：PCT/EP2012/050034

    申请日：2012-01-03

    Applicant: F. HOFFMANN-LA ROCHE AG ,  KNUST, Henner ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  VIFIAN, Walter

    Inventor： KNUST, Henner ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  VIFIAN, Walter

    IPC: C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/10 ,  A61K31/4025 ,  A61P25/00

    CPC classification number: C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D407/06 ,  C07D413/10

    Abstract: The invention relates to compounds of formula (I) wherein R 1 is (A), or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl may optionally be substituted by cyano, lower alkyl, halogen-substituted phenyl, lower alkyl-substituted [1,2,4]oxadiazol-3-yl or by 2-oxo-piperidin-1-yl; X is NR or O; R is C(O)-lower alkyl, -C(O)-cycloalkyl substituted by lower alkyl, cycloalkyl or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl may optionally be substituted by lower alkyl, lower alkoxy, cyano, -C(O)-lower alkyl, halogen or lower alkyl substituted by halogen; R 2 is hydrogen or lower alkyl; R 3 is hydrogen, halogen, cyano, lower alkyl or lower alkyl substituted by halogen; R 4 is hydrogen or lower alkyl; wherein R 2 and R 4 are not simultaneously hydrogen or lower alkyl; R 5 is lower alkyl; R 6 halogen, hydroxy, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S(O) 2 -lower alkyl or cyano; or to a pharmaceutically suitable acid addition salt thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

    Abstract translation: 本发明涉及式（I）化合物，其中R 1为（A），或为苯基，吡啶基或哒嗪基，其中苯基，吡啶基和哒嗪基可任选被氰基，低级烷基，卤素取代的苯基，低级烷基取代 [1,2,4]恶二唑-3-基或2-氧代 - 哌啶-1-基; X是NR或O; R是C（O） - 低级烷基，被低级烷基，环烷基或苯基，吡啶基或哒嗪基取代的-C（O） - 环烷基，其中苯基，吡啶基和哒嗪基可以任选地被低级烷基，低级烷氧基，氰基， -C（O） - 低级烷基，卤素或被卤素取代的低级烷基; R2是氢或低级烷基; R3是氢，卤素，氰基，被卤素取代的低级烷基或低级烷基; R4是氢或低级烷基; 其中R2和R4不同时为氢或低级烷基; R5是低级烷基; R 6卤素，羟基，低级烷基，低级烷氧基，被卤素取代的低级烷基，S（O）2 - 低级烷基或氰基; 或其药学上合适的酸加成盐。 已经发现，本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症，焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

    PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS
    6.
    发明申请
    PIPERIDINE DERIVATIVES AS NK3 RECEPTOR ANTAGONISTS 审中-公开
    作为NK3受体拮抗剂的哌啶衍生物

    公开(公告)号：WO2010086259A1

    公开(公告)日：2010-08-05

    申请号：PCT/EP2010/050591

    申请日：2010-01-19

    Applicant: F. HOFFMANN-LA ROCHE AG ,  KNUST, Henner ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  RIEMER, Claus ,  VIFIAN, Walter

    Inventor： KNUST, Henner ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  RIEMER, Claus ,  VIFIAN, Walter

    IPC: C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  A61K31/454 ,  A61K31/4545 ,  A61P25/24 ,  A61P25/04 ,  A61P25/18 ,  A61P25/16 ,  A61P25/22

    CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14

    Abstract: The present invention relates to a compounds of formula (I) wherein Ar 1 is aryl or a six membered heteroaryl; Ar 2 is aryl or a six membered heteroaryl; R 1 is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R 2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R 3 is hydrogen or lower alkyl; R 4 is hydrogen, lower alkyl, phenyl, optionally substituted by halogen, or is a five membered heteroaryl, optionally substituted by lower alkyl, or is aryl optionally substituted by halogen; is a six membered heterocyclic group, wherein X is -N(SO 2 CH 3 ); R 6 is hydrogen; Y is -N(R 7' )- R 7' is a 6-membered heteroaryl group, optionally substituted by cyano or C(O)-cycloalkyl, wherein the cycloalkyl group is optionally substituted by lower alkyl, n is 1; m is 1; o is1; p is 1; s is 0; t is 1; u is 1; or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. It has been found that the present compounds are high potential NK-3 receptor antagonist for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia anxiety and attention deficit hyperactivity disorder (ADHD).

    Abstract translation: 本发明涉及式（I）的化合物，其中Ar 1是芳基或6元杂芳基; Ar 2是芳基或六元杂芳基; R1是氢，卤素，低级烷基，低级烷氧基或被卤素取代的低级烷基; R2是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; R3是氢或低级烷基; R4是氢，低级烷基，任选被卤素取代的苯基，或是任选被低级烷基取代的五元杂芳基，或者是被卤素任意取代的芳基; 是六元杂环基，其中X是-N（SO 2 CH 3）; R6是氢; Y是-N（R 7'）-R 7'是任选被氰基或C（O） - 环烷基取代的6元杂芳基，其中环烷基任选被低级烷基取代，n是1; m为1; o is1; p为1; s是0; t为1; 你是1 或其药物活性盐，外消旋混合物，对映体，旋光异构体或其互变异构形式。 已经发现，本发明化合物是用于治疗抑郁症，疼痛，精神病，帕金森病，精神分裂症焦虑和注意缺陷多动障碍（ADHD）的高潜力NK-3受体拮抗剂。

    HETEROARYL DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
    8.
    发明申请
    HETEROARYL DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
    异丙肾上腺素衍生物作为OREXIN受体拮抗剂

    公开(公告)号：WO2009080533A1

    公开(公告)日：2009-07-02

    申请号：PCT/EP2008/067273

    申请日：2008-12-11

    Applicant: F. HOFFMANN-LA ROCHE AG ,  KNUST, Henner ,  NETTEKOVEN, Matthias ,  PINARD, Emmanuel ,  ROCHE, Olivier ,  ROGERS-EVANS, Mark

    Inventor： KNUST, Henner ,  NETTEKOVEN, Matthias ,  PINARD, Emmanuel ,  ROCHE, Olivier ,  ROGERS-EVANS, Mark

    IPC: C07D401/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D498/04 ,  A61K31/4025 ,  A61P25/00

    CPC classification number: C07D413/12 ,  C07D401/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D498/04

    Abstract: The present invention relates to compounds of Formula (I), wherein Ar is an unsubstituted or substituted aryl or heteroaryl group, wherein the aryl and the heteroaryl group may be substituted by one or more substituents R 2 ; R 2 is hydroxy, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, C(O)-lower alkyl, nitro, NR , R ,, , cyano, S-lower alkyl, SO 2 -lower alkyl, cycloalkyl, heterocycloalkyl, phenyloxy, benzyloxy, phenyl, NH-phenyl or heteroaryl, wherein the phenyl and heteroaryl group is unsubstituted or substituted by one or more substituents selected from lower alkyl or halogen; R , /R ,, are independently from each other hydrogen or lower alkyl; R 1 is hydrogen or lower alkyl; Het is a heteroaryl group, unsubstituted or substituted by one or more substituents selected from R 3 ; R 3 is hydroxy, halogen, =O, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, phenyl, lower alkoxy substituted by halogen, nitro, cyano, SO 2 -lower alkyl, cycloalkyl or heterocycloalkyl; n is 1 or 2; or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of formula (I) are orexin receptor antagonists and the related compounds may be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.

    Abstract translation: 本发明涉及式（I）化合物，其中Ar为未取代或取代的芳基或杂芳基，其中芳基和杂芳基可被一个或多个取代基R2取代; R 2是羟基，卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素取代的低级烷氧基，C（O） - 低级烷基，硝基，NR，R'，氰基，S-低级烷基，SO 2 - 烷基，环烷基，杂环烷基，苯氧基，苄氧基，苯基，NH-苯基或杂芳基，其中苯基和杂芳基是未取代的或被一个或多个选自低级烷基或卤素的取代基取代; R 1 / R 3彼此独立地为氢或低级烷基; R1是氢或低级烷基; Het是未取代或被一个或多个选自R 3的取代基取代的杂芳基; R 3是羟基，卤素，= O，低级烷基，被卤素取代的低级烷基，低级烷氧基，苯基，被卤素，硝基，氰基，SO 2 - 低级烷基，环烷基或杂环烷基取代的低级烷氧基; n为1或2; 或其药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。 已经发现，式（I）化合物是食欲肽受体拮抗剂，相关化合物可用于治疗睡眠呼吸暂停，发作性睡病，失眠，睡眠，时差综合征，昼夜节律障碍或与神经系统疾病相关的睡眠障碍 。

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