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    PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS
    1.
    发明授权
    PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 有权
    PYRROLIDINARYLETHER AS NK-3受体拮抗剂

    公开(公告)号：EP2185540B1

    公开(公告)日：2011-07-20

    申请号：EP08786547.3

    申请日：2008-07-29

    申请人： F. Hoffmann-La Roche AG

    发明人： JABLONSKI, Philippe ,  KAWASAKI, Kenichi ,  KNUST, Henner ,  LIMBERG, Anja ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  RIEMER, Claus ,  WU, Xihan

    IPC分类号： C07D401/08 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D401/08

    摘要： The invention relates to a compound of general formula (I) wherein Ar1 is aryl or a five or six membered heteroaryl; Ar2 is aryl or a five or six membered heteroaryl; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, -S(O)2-lower alkyl, -S(O)2-di-lower alkyl amino, -(CH2)qR, cyano, amino, mono or di-lower alkyl amino, NHC(O)-lower alkyl, cycloalkyl or is or a five membered heteroaryl, optionally substituted by lower alkyl; wherein R is cyano, di-lower alkyl amino or pyrrolidin-1-yl; R2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R3 is hydrogen or lower alkyl or CH2OH; R4 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; n is 1, 2 or 3; in case n is 2 or 3, R1 may be the same or different; o is 1, 2 or 3; in case o is 2 or 3, R2 may be the same or different; p is 1, 2 or 3; in case p is 2 or 3, R4 may be the same or different; q is 1 or 2; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures 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).

    PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS
    3.
    发明公开
    PYRROLIDINE ARYL-ETHER AS NK3 RECEPTOR ANTAGONISTS 有权
    作为NK3受体拮抗剂的吡咯烷基芳基醚

    公开(公告)号：EP2185540A1

    公开(公告)日：2010-05-19

    申请号：EP08786547.3

    申请日：2008-07-29

    申请人： F. Hoffmann-La Roche AG

    发明人： JABLONSKI, Philippe ,  KAWASAKI, Kenichi ,  KNUST, Henner ,  LIMBERG, Anja ,  NETTEKOVEN, Matthias ,  RATNI, Hasane ,  RIEMER, Claus ,  WU, Xihan

    IPC分类号： C07D401/08 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D401/08

    摘要： The invention relates to a compound of general formula (I) wherein Ar1 is aryl or a five or six membered heteroaryl; Ar2 is aryl or a five or six membered heteroaryl; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, S-lower alkyl, -S(O)2-lower alkyl, -S(O)2-di-lower alkyl amino, -(CH2)qR, cyano, amino, mono or di-lower alkyl amino, NHC(O)-lower alkyl, cycloalkyl or is or a five membered heteroaryl, optionally substituted by lower alkyl; wherein R is cyano, di-lower alkyl amino or pyrrolidin-1-yl; R2 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; R3 is hydrogen or lower alkyl or CH2OH; R4 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen or cyano; n is 1, 2 or 3; in case n is 2 or 3, R1 may be the same or different; o is 1, 2 or 3; in case o is 2 or 3, R2 may be the same or different; p is 1, 2 or 3; in case p is 2 or 3, R4 may be the same or different; q is 1 or 2; or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures 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).

    摘要翻译： 本发明涉及通式（I）的化合物，其中Ar 1是芳基或五元或六元杂芳基; Ar 2是芳基或五元或六元杂芳基; R1是氢，卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，S-低级烷基，-S（O）2 - 低级烷基，-S（O）2 - 二低级烷基 氨基， - （CH 2）q R，氰基，氨基，单或二低级烷基氨基，NHC（O） - 低级烷基，环烷基或任选被低级烷基取代的五元杂芳基; 其中R是氰基，二低级烷基氨基或吡咯烷-1-基; R2是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; R3是氢或低级烷基或CH2OH; R4是氢，卤素，低级烷基，被卤素或氰基取代的低级烷基; n是1,2或3; 在n为2或3的情况下，R1可以相同或不同; o是1,2或3; 在o为2或3的情况下，R2可以相同或不同; p是1,2或3; 在p为2或3的情况下，R 4可以相同或不同; q是1或2; 或其药学活性盐，包括式（I）化合物的所有立体异构形式，单独的非对映异构体和对映异构体以及其外消旋和非外消旋混合物。 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，焦虑和注意力缺陷多动症（ADHD）的高潜力NK-3受体拮抗剂。

    BRIDGED PIPERIDINE DERIVATIVES
    8.
    发明公开
    BRIDGED PIPERIDINE DERIVATIVES 审中-公开

    公开(公告)号：EP3347363A1

    公开(公告)日：2018-07-18

    申请号：EP16763491.4

    申请日：2016-09-05

    申请人： F. Hoffmann-La Roche AG

    发明人： BAUMANN, Karlheinz ,  GALLEY, Guido ,  JAKOB-ROETNE, Roland ,  LIMBERG, Anja ,  NEIDHART, Werner ,  RODRIGUEZ SARMIENTO, Rosa Maria ,  BARTELS, Bjoern ,  RATNI, Hasane

    IPC分类号： C07D519/00 ,  A61K31/4375 ,  A61P25/28

    摘要： The present invention relates to compounds of formula (I); hetaryl is a five membered heteroaryl group, containing 1 to 3 heteroatoms, selected from O, S or N; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S-lower alkyl substituted by halogen or lower alkoxy substituted by halogen, or two neighboring carbon atoms may form on phenyl an additional ring containing -O-CH2-O-; n is 1 to 5; R2 is hydrogen or lower alkyl substituted by halogen; R3 is hydrogen or lower alkyl substituted by halogen; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers or optical isomers or stereoisomers thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.

    INDOLIN-2-ONE AND 1,3-DIHYDRO-PYRROLO[3,2-c]PYRIDIN-2-ONE DERIVATIVES
    9.
    发明公开
    INDOLIN-2-ONE AND 1,3-DIHYDRO-PYRROLO[3,2-c]PYRIDIN-2-ONE DERIVATIVES 审中-公开
    茚满-2-酮在1,3-二羟基吡咯并[3,2-C]吡啶-2-酮衍生物

    公开(公告)号：EP3145923A1

    公开(公告)日：2017-03-29

    申请号：EP15723917.9

    申请日：2015-05-19

    申请人： F. Hoffmann-La Roche AG

    发明人： HILPERT, Hans ,  KOLCZEWSKI, Sabine ,  LIMBERG, Anja ,  STOLL, Theodor

    IPC分类号： C07D401/14 ,  C07D413/14 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  C07D403/04 ,  C07D403/14 ,  C07D411/12 ,  C07D417/14 ,  C07D471/04 ,  A61P25/32 ,  A61P25/34 ,  A61P25/24 ,  A61P25/36

    CPC分类号： C07D471/04 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D411/12 ,  C07D413/14 ,  C07D417/14

    摘要： The present invention is concerned with indolin-2-one and l,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula (I) wherein Ar1 is phenyl, pyridinyl or pyrimidinyl; Ar2 is a 5 or 6 membered heteroaryl group, containing 2 or 3 heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, halogen or lower alkoxy; R2 is hydrogen or lower alkyl; R3 is hydrogen, lower alkyl, lower alkyl substituted by hydroxy, cycloalkyl, oxetan-3-yl, pyridinyl, imidazolyl, pyrazolyl, pyrimidinyl, which rings may optionally substituted by lower alkyl, or is -(CH2)3-S(O)2-cyclopropyl; X is CH or N; n is 1 or 2; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof, for use in the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.

    摘要翻译： 本发明涉及通式（I）的二氢吲哚-2-酮和1,3-二氢 - 吡咯并[3,2-c]吡啶-2-酮衍生物，其中Ar 1是苯基，吡啶基或嘧啶基; Ar 2是5或6元杂芳基，含有2或3个选自N，O或S的杂原子; R1是氢，低级烷基，卤素或低级烷氧基; R2是氢或低级烷基; 或R 3为氢，低级烷基，被羟基取代的低级烷基，环烷基，氧杂环丁烷-3-基，吡啶基，咪唑基，吡唑基，嘧啶基，该环可任选被低级烷基取代，或为 - （CH 2）3 -S（O） 2-环丙基; X是CH或N; n为1或2; 以及其药学上可接受的盐与外消旋混合物或其相应的对映异构体和/或其光学异构体和/或立体异构体一起用于治疗某些中性神经系统疾病，其为正（精神病）和阴性 精神分裂症，药物滥用，酒精和药物成瘾，强迫症，认知障碍，双相情感障碍，情绪障碍，重症抑郁症，耐药性抑郁症，焦虑症，阿尔茨海默病，孤独症，帕金森病，慢性疼痛，边缘人格障碍 ，睡眠障碍，慢性疲劳综合征，僵硬，关节炎中的抗炎作用和平衡问题。