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    Novel Medicaments
    41.
    发明申请
    Novel Medicaments 失效
    新药

    公开(公告)号：US20090312309A1

    公开(公告)日：2009-12-17

    申请号：US11917823

    申请日：2006-06-30

    申请人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    发明人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    IPC分类号： A61K31/5513 ,  A61K31/5377 ,  A61K31/501 ,  A61K31/497 ,  C07D413/14 ,  C07D403/04

    CPC分类号： C07D213/74 ,  C07D213/84 ,  C07D213/87 ,  C07D237/20 ,  C07D403/04 ,  C07D403/12 ,  C07D417/10

    摘要： Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.

    摘要翻译： 定义与组胺H3受体相互作用的新型化合物。 这些化合物特别可用于治疗组胺H3相互作用有益的各种疾病或病症。 因此，该化合物可用于例如治疗中枢神经系统，周围神经系统，心血管系统，肺系统，胃肠系统和内分泌系统的疾病。 该新化合物具有由在环中含有至少一个氮原子和两个碳原子的6元芳香环组成的核心，并且在该环的其余位置上有碳原子或氮原子。

    Medicaments
    42.
    发明授权
    Medicaments 有权
    药剂

    公开(公告)号：US08846677B2

    公开(公告)日：2014-09-30

    申请号：US13472090

    申请日：2012-05-15

    申请人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    发明人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    IPC分类号： A61K31/501 ,  C07D401/00 ,  C07D409/00

    CPC分类号： C07D213/74 ,  C07D213/84 ,  C07D213/87 ,  C07D237/20 ,  C07D403/04 ,  C07D403/12 ,  C07D417/10

    摘要： Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.

    摘要翻译： 定义与组胺H3受体相互作用的新型化合物。 这些化合物特别可用于治疗组胺H3相互作用有益的各种疾病或病症。 因此，该化合物可用于例如治疗中枢神经系统，周围神经系统，心血管系统，肺系统，胃肠系统和内分泌系统的疾病。 该新化合物具有由在环中含有至少一个氮原子和两个碳原子的6元芳香环组成的核心，并且在该环的其余位置上有碳原子或氮原子。

    Medicaments
    43.
    发明授权
    Medicaments 失效
    药剂

    公开(公告)号：US08501739B2

    公开(公告)日：2013-08-06

    申请号：US11917823

    申请日：2006-06-30

    申请人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    发明人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    IPC分类号： A61K31/50 ,  C07D401/00

    CPC分类号： C07D213/74 ,  C07D213/84 ,  C07D213/87 ,  C07D237/20 ,  C07D403/04 ,  C07D403/12 ,  C07D417/10

    摘要： Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.

    摘要翻译： 定义与组胺H3受体相互作用的新型化合物。 这些化合物特别可用于治疗组胺H3相互作用有益的各种疾病或病症。 因此，该化合物可用于例如治疗中枢神经系统，周围神经系统，心血管系统，肺系统，胃肠系统和内分泌系统的疾病。 该新化合物具有由在环中含有至少一个氮原子和两个碳原子的6元芳香环组成的核心，并且在该环的其余位置上有碳原子或氮原子。

    Novel Medicaments
    45.
    发明申请
    Novel Medicaments 有权
    新药

    公开(公告)号：US20120232078A1

    公开(公告)日：2012-09-13

    申请号：US13472090

    申请日：2012-05-15

    申请人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    发明人： Rolf Hohlweg ,  Knud Erik Andersen ,  Jan Lindy Sorensen ,  Jane Marie Lundbeck

    IPC分类号： A61K31/506 ,  A61P3/04 ,  A61P25/24 ,  A61K31/5377

    CPC分类号： C07D213/74 ,  C07D213/84 ,  C07D213/87 ,  C07D237/20 ,  C07D403/04 ,  C07D403/12 ,  C07D417/10

    摘要： Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.

    摘要翻译： 定义与组胺H3受体相互作用的新型化合物。 这些化合物特别可用于治疗组胺H3相互作用有益的各种疾病或病症。 因此，该化合物可用于例如治疗中枢神经系统，周围神经系统，心血管系统，肺系统，胃肠系统和内分泌系统的疾病。 该新化合物具有由在环中含有至少一个氮原子和两个碳原子的6元芳香环组成的核心，并且在该环的其余位置上有碳原子或氮原子。

    Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines
    47.
    发明授权
    Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines 失效
    取代的六氢吡咯并[1,2-a]吡嗪，八氢吡啶并[1,2-a] - 吡嗪和十氢吡嗪并[1,2-a]吖庚因

    公开(公告)号：US07186721B2

    公开(公告)日：2007-03-06

    申请号：US11115564

    申请日：2005-04-27

    申请人： Bernd Peschke ,  Rolf Hohlweg

    发明人： Bernd Peschke ,  Rolf Hohlweg

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D241/36

    CPC分类号： C07D471/04 ,  A61K31/519 ,  C07D487/04

    摘要： Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

    摘要翻译： 新型取代六氢吡咯并[1,2-a]吡嗪，八氢吡啶并[1,2-a] - 吡嗪和十氢吡嗪并[1,2-a]吖庚因，这些化合物用作药物组合物，包含该化合物的药物组合物， 使用这些化合物和组合物的治疗。 化合物对组胺H3受体表现出高且选择性的结合亲和力，表明组胺H3受体拮抗，反向激动或激动活性。 结果，这些化合物可用于治疗与组胺H3受体相关的疾病和病症。

    1,4-disubstituted piperazines
    48.
    发明授权
    1,4-disubstituted piperazines 失效
    1,4-二取代的哌嗪

    公开(公告)号：US5276035A

    公开(公告)日：1994-01-04

    申请号：US879518

    申请日：1992-05-04

    申请人： Rolf Hohlweg ,  Erling Guddal ,  Erik B. Nielsen

    发明人： Rolf Hohlweg ,  Erling Guddal ,  Erik B. Nielsen

    IPC分类号： C07D261/08 ,  C07D263/10 ,  C07D271/06 ,  C07D295/084 ,  C07D295/088 ,  C07D295/15 ,  C07D333/20 ,  C07D333/22 ,  C07F9/6509 ,  A61K31/495 ,  A61K33/42 ,  C07D409/06

    CPC分类号： C07D263/10 ,  C07D261/08 ,  C07D271/06 ,  C07D295/084 ,  C07D295/088 ,  C07D295/15 ,  C07D333/20 ,  C07D333/22 ,  C07F9/650958

    摘要： A disubstituted piperazine compound having the formula ##STR1## wherein R.sup.1 is halogen, methoxy, C.sub.1-6 -alkyl or trifluoromethyl, and R.sup.2 is methyl or substituted C.sub.1-8 -alkyl, C.sub.3-8 -alkenyl or C.sub.3-8 -cycloalkyl, where substituents may be hydroxy-, keto- or oximino-groups in any position leading to a stable tertiary amine; or R.sup.2 is a straight or branched C.sub.1-8 -alkyl or C.sub.3-8 -alkenyl, which in any position may be substituted as above, but is terminally substituted with one of the following groups: cyano, optionally C.sub.1-4 -alkoxy-substituted C.sub.1-4 -alkoxy, dimethoxy, optiontionally substituted phenoxy, phosphonic acid, thienyl, furyl, oxazoline, isoxazole, oxadiazole, where the optional substitution is represented by C.sub.1-6 -alkyl or phenyl, provided that when cyano is the only substituent in R.sup.2, R.sup.2 must contain at least four carbon atoms, and pharmaceutically acceptable acid addition salts thereof.The compounds are useful in the treatment of mental disorders in which a dopaminergic deficit is implicated.

    摘要翻译： 具有式（I）的二取代哌嗪化合物，其中R 1是卤素，甲氧基，C 1-6 - 烷基或三氟甲基，R 2是甲基或取代的C 1-8 - 烷基，C 3-8 - 烯基或C 3-8 - 环烷基，其中取代基可以是导致稳定叔胺的任何位置的羟基，酮基或肟基; 或R 2是直链或支链C 1-8 - 烷基或C 3-8 - 烯基，其在任何位置可以如上所述被取代，但被下列基团之一末端取代：氰基，任选地C 1-4 - 烷氧基取代 C 1-4 - 烷氧基，二甲氧基，选择性取代的苯氧基，膦酸，噻吩基，呋喃基，恶唑啉，异恶唑，恶二唑，其中任选的取代由C 1-6 - 烷基或苯基表示，条件是当氰基是R 2中的唯一取代基 ，R2必须含有至少四个碳原子，及其药学上可接受的酸加成盐。 这些化合物可用于治疗涉及多巴胺能缺乏症的精神障碍。