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    Biaryl derivatives
    2.
    发明授权
    Biaryl derivatives 失效
    双芳基衍生物

    公开(公告)号：US07858800B2

    公开(公告)日：2010-12-28

    申请号：US11629730

    申请日：2005-06-29

    申请人： Hiroshi Kawamoto ,  Satoru Ito ,  Atsushi Satoh ,  Yasushi Nagatomi ,  Yukari Hirata ,  Toshifumi Kimura ,  Gentaroh Suzuki ,  Akio Sato ,  Hisashi Ohta

    发明人： Hiroshi Kawamoto ,  Satoru Ito ,  Atsushi Satoh ,  Yasushi Nagatomi ,  Yukari Hirata ,  Toshifumi Kimura ,  Gentaroh Suzuki ,  Akio Sato ,  Hisashi Ohta

    IPC分类号： C07D401/00 ,  A61K31/44

    CPC分类号： C07D401/14 ,  C07D249/06 ,  C07D271/04 ,  C07D401/04 ,  C07D417/04

    摘要： The present invention relates to a compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 is a linear or branched alkoxy group, a cycloalkoxy group, a linear or branched lower alkyl group, etc.; R2 is halogen atom, a lower alkyl group, etc.; Q1 is carbon atom or nitrogen atom; Q2 is carbon atom which may be substituted with oxo group; the formula (III):   (II) is a single bond or a double bond; A is a group selected from the group consisting of the substitutent group α; and R5 is hydrogen atom, a lower alkyl group, cyano group, an alkoxy group or a trialkylsilyl group; having an mGluR1 inhibiting action and being useful as treatment and/or prevention of convulsion, acute pain, cerebral disturbance such as cerebral infarction or transient cerebral ischemia onset, anxiety, chemical dependency or Parkinson's disease.

    摘要翻译： 本发明涉及由式（I）表示的化合物或其药学上可接受的盐，其中：R1是直链或支链烷氧基，环烷氧基，直链或支链低级烷基等; R2是卤原子，低级烷基等; Q1是碳原子或氮原子; Q2是可以被氧代基取代的碳原子; 式（III）：（II）是单键或双键; A是选自由取代基α组成的组的基团; R5为氢原子，低级烷基，氰基，烷氧基或三烷基甲硅烷基; 具有mGluR1抑制作用，并且可用作治疗和/或预防惊厥，急性疼痛，脑梗塞如脑梗死或暂时性脑缺血发作，焦虑，化学依赖或帕金森病。

    Biaryl derivatives
    3.
    发明申请
    Biaryl derivatives 失效
    双芳基衍生物

    公开(公告)号：US20070191389A1

    公开(公告)日：2007-08-16

    申请号：US11629730

    申请日：2005-06-29

    申请人： Hiroshi Kawamoto ,  Satoru Ito ,  Atsushi Satoh ,  Yasushi Nagatomi ,  Yukari Hirata ,  Toshifumi Kimura ,  Gentaroh Suzuki ,  Akio Sato ,  Hisashi Ohta

    发明人： Hiroshi Kawamoto ,  Satoru Ito ,  Atsushi Satoh ,  Yasushi Nagatomi ,  Yukari Hirata ,  Toshifumi Kimura ,  Gentaroh Suzuki ,  Akio Sato ,  Hisashi Ohta

    IPC分类号： A61K31/496 ,  A61K31/454 ,  A61K31/4439 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D401/14 ,  C07D249/06 ,  C07D271/04 ,  C07D401/04 ,  C07D417/04

    摘要： The present invention relates to a compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 is a linear or branched alkoxy group, a cycloalkoxy group, a linear or branched lower alkyl group, etc.; R2 is halogen atom, a lower alkyl group, etc.; Q1 is carbon atom or nitrogen atom; Q2 is carbon atom which may be substituted with oxo group; the formula (III):   (II) is a single bond or a double bond; A is a group selected from the group consisting of the substitutent group α; and R5 is hydrogen atom, a lower alkyl group, cyano group, an alkoxy group or a trialkylsilyl group; having an mGluR1 inhibiting action and being useful as treatment and/or prevention of convulsion, acute pain, cerebral disturbance such as cerebral infarction or transient cerebral ischemia onset, anxiety, chemical dependency or Parkinson's disease.

    摘要翻译： 本发明涉及由式（I）表示的化合物或其药学上可接受的盐，其中：R 1是直链或支链烷氧基，环烷氧基，直链或支链低级 烷基等; R 2是卤素原子，低级烷基等; Q 1是碳原子或氮原子; Q 2是可以被氧代基取代的碳原子; 公式（III）：<？in-line-formula description =“In-line Formulas”end =“lead”？> （II）<？in-line-formula description =”In-line 公式“end =”tail“？>是单键或双键; A是选自由取代基组α组成的组的组; R 5是氢原子，低级烷基，氰基，烷氧基或三烷基甲硅烷基; 具有mGluR1抑制作用，并且可用作治疗和/或预防惊厥，急性疼痛，脑梗塞如脑梗死或暂时性脑缺血发作，焦虑，化学依赖或帕金森病。

    N-dihydroxyalkyl-substituted 2-oxo-imidazole derivatives
    7.
    发明申请
    N-dihydroxyalkyl-substituted 2-oxo-imidazole derivatives 有权
    N-二羟基烷基取代的2-氧代 - 咪唑衍生物

    公开(公告)号：US20070015792A1

    公开(公告)日：2007-01-18

    申请号：US11484203

    申请日：2006-07-11

    申请人： Masaya Hashimoto ,  Yoshikazu Iwasawa ,  Hiroshi Kawamoto ,  Hisashi Ohta ,  Satoshi Ozaki ,  Takeshi Sagara ,  Hiroki Sakoh ,  Atsushi Satoh

    发明人： Masaya Hashimoto ,  Yoshikazu Iwasawa ,  Hiroshi Kawamoto ,  Hisashi Ohta ,  Satoshi Ozaki ,  Takeshi Sagara ,  Hiroki Sakoh ,  Atsushi Satoh

    IPC分类号： A61K31/454 ,  C07D403/04

    CPC分类号： C07D403/04

    摘要： The invention provides the compounds represented by the formula (I) in which, R stands for a dihydroxy-substituted C1-C6 alkyl group, and Cy stands for an optionally substituted C6-C10 bi- or tri-cyclic aliphatic carbocyclic group. These compounds act as nociceptin receptor antagonist, and are useful, for example, as relievers against tolerance to narcotic analgesic, dependence on narcotic analgesic or addiction; analgesic enhancers; antiobestic or appetite suppressors; treating or prophylactic agents for cognitive impairment and dementia/amnesia; agents for treating developmental cognitive abnormality; remedy for schizophrenia; agents for treating neurodegenerative diseases; anti-depressant or treating agents for affective disorder; treating or prophylactic agents for diabetes insipidus; treating or prophylactic agents for polyuria; and remedy for hypotension and the like.

    摘要翻译： 本发明提供由式（I）表示的化合物，其中R代表二羟基取代的C 1 -C 6烷基，Cy代表任选地 取代的C 6 -C 10 - 二环或三环脂族碳环基团。 这些化合物作为伤害感受肽受体拮抗剂起作用，例如可用作对麻醉止痛药的耐受性，对麻醉性镇痛药或成瘾的依赖; 镇痛增强剂; 抗生素或食欲抑制剂; 认知障碍和痴呆/遗忘症的治疗或预防剂; 治疗发育性认知异常的药剂; 精神分裂症补救措施 治疗神经变性疾病的药剂; 用于情感障碍的抗抑郁药或治疗剂; 尿崩症的治疗或预防剂; 多尿症的治疗或预防剂; 并补救低血压等。

    N-dihydroxyalkyl-substituted 2-oxo-imidazole derivatives
    8.
    发明申请
    N-dihydroxyalkyl-substituted 2-oxo-imidazole derivatives 审中-公开
    N-二羟基烷基取代的2-氧代 - 咪唑衍生物

    公开(公告)号：US20080103178A1

    公开(公告)日：2008-05-01

    申请号：US11974130

    申请日：2007-10-11

    申请人： Masaya Hashimoto ,  Yoshikazu Iwasawa ,  Hiroshi Kawamoto ,  Hisashi Ohta ,  Satoshi Ozaki ,  Takeshi Sagara ,  Hiroki Sakoh ,  Atsushi Satoh

    发明人： Masaya Hashimoto ,  Yoshikazu Iwasawa ,  Hiroshi Kawamoto ,  Hisashi Ohta ,  Satoshi Ozaki ,  Takeshi Sagara ,  Hiroki Sakoh ,  Atsushi Satoh

    IPC分类号： A61K31/454 ,  A61P25/00

    CPC分类号： C07D403/04

    摘要： The invention provides the compounds represented by the formula (I) in which, R stands for a dihydroxy-substituted C1-C6 alkyl group, and Cy stands for an optionally substituted C6-C10 bi- or tri-cyclic aliphatic carbocyclic group. These compounds act as nociceptin receptor antagonist, and are useful, for example, as relievers against tolerance to narcotic analgesic, dependence on narcotic analgesic or addiction; analgesic enhancers; antiobestic or appetite suppressors; treating or prophylactic agents for cognitive impairment and dementia/amnesia; agents for treating developmental cognitive abnormality; remedy for schizophrenia; agents for treating neurodegenerative diseases; anti-depressant or treating agents for affective disorder; treating or prophylactic agents for diabetes insipidus; treating or prophylactic agents for polyuria; and remedy for hypotension and the like.

    摘要翻译： 本发明提供由式（I）表示的化合物，其中R代表二羟基取代的C 1 -C 6烷基，Cy代表任选地 取代的C 6 -C 10 - 二环或三环脂族碳环基团。 这些化合物作为伤害感受肽受体拮抗剂起作用，例如可用作对麻醉止痛药的耐受性，对麻醉性镇痛药或成瘾的依赖; 镇痛增强剂; 抗生素或食欲抑制剂; 认知障碍和痴呆/遗忘症的治疗或预防剂; 治疗发育性认知异常的药剂; 精神分裂症补救措施 治疗神经变性疾病的药剂; 用于情感障碍的抗抑郁药或治疗剂; 尿崩症的治疗或预防剂; 多尿症的治疗或预防剂; 并补救低血压等。

    4-oxoimidazolidine-2-spiropiperidine derivatives
    10.
    发明授权
    4-oxoimidazolidine-2-spiropiperidine derivatives 失效
    4-氧代咪唑烷-2-螺哌啶衍生物

    公开(公告)号：US07557117B2

    公开(公告)日：2009-07-07

    申请号：US11603147

    申请日：2006-11-22

    申请人： Masaya Hashimoto ,  Osamu Okamoto ,  Satoshi Ozaki ,  Hisashi Ohta

    发明人： Masaya Hashimoto ,  Osamu Okamoto ,  Satoshi Ozaki ,  Hisashi Ohta

    IPC分类号： A61K31/438 ,  C07D401/04

    CPC分类号： C07D471/10

    摘要： The invention relates to 4-oxoimidazolidine-2-spiropiperidine derivatives represented by a general formula [I] [in which A1, A2, A3, A4 and A5 stand for optionally halogen-substituted methine, or nitrogen atom; R1 and R2 stand for lower alkyl or the like; R3 stands for hydrogen or lower alkyl; R4 and R5 stand for hydrogen, or lower alkyl which is optionally substituted with hydroxy, or the like]or salts thereof. These compounds act as nociceptin receptor agonist, and are useful as analgesic, reliever from tolerance to narcotic analgesic, reliever from dependence on narcotic analgesic, analgesic enhancer, antiobestic, drug for ameliorating brain function, remedy for schizophrenia, drug for treating regressive neurodegenerative diseases, antianxiety agent or antidepressant and remedy for diabetes insipidus and polyuria; and the like.

    摘要翻译： 本发明涉及由通式[I]表示的4-氧代咪唑烷-2-螺哌啶衍生物[其中A1，A2，A3，A4和A5代表任选卤素取代的次甲基或氮原子; R1和R2代表低级烷基等; R3代表氢或低级烷基; R4和R5代表氢，或任选被羟基取代的低级烷基，或其盐。 这些化合物作为伤害感受肽受体激动剂起作用，可用作镇痛药，缓解麻醉止痛药耐受性，缓解依赖麻醉止痛药，镇痛增强剂，抗胆固醇药，改善脑功能药物，精神分裂症药物治疗，治疗退行性神经退行性疾病药物， 抗焦虑药或抗抑郁药及其治疗尿崩症及多尿症; 等等。