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    Imidazoylalkyl substituted with a five, six or seven membered heterocyclic ring containing one nitrogen atom
    1.
    发明授权
    Imidazoylalkyl substituted with a five, six or seven membered heterocyclic ring containing one nitrogen atom 失效
    被含有一个氮原子的五，六或七元杂环取代的咪唑烷基

    公开(公告)号：US6100279A

    公开(公告)日：2000-08-08

    申请号：US185973

    申请日：1998-11-05

    申请人： Wayne D. Vaccaro ,  Ronald L. Wolin ,  Daniel M. Solomon ,  Robert G. Aslanian ,  John J. Piwinski ,  Stuart B. Rosenblum

    发明人： Wayne D. Vaccaro ,  Ronald L. Wolin ,  Daniel M. Solomon ,  Robert G. Aslanian ,  John J. Piwinski ,  Stuart B. Rosenblum

    IPC分类号： A61K31/415 ,  A61K31/445 ,  A61K31/495 ,  A61K45/06 ,  C07D401/06 ,  C07D403/06

    CPC分类号： C07D401/06 ,  A61K31/415 ,  A61K31/445 ,  A61K31/495 ,  A61K45/06 ,  C07D403/06

    摘要： Disclosed are compounds of Formula I ##STR1## or pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula I. Further disclosed is a method of treating allergy (for example asthma), inflammation, hypotension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimer's, schizophrenia, obesity and migraine) comprising administering an effective amount of a compound of Formula I to a patient in need of such treatment. Also disclosed are methods for treatment of upper airway allergic responses comprising administering a compound, or salt or solvate thereof, of formula I in combination or admixture with a histamine H, receptor antagonist.

    摘要翻译： 公开了式I的化合物或其药学上可接受的盐或溶剂化物。 还公开了包含药学上可接受的载体和有效量的式I化合物的药物组合物。还公开了治疗过敏（例如哮喘），炎症，低血压，升高的眼内压（如青光眼）的方法， 降低眼内压，睡眠障碍，超低运动状态和胃肠道酸性分泌的方法，中枢神经系统的低血压和多动症（例如，激动和抑郁）和其他CNS疾病（例如阿兹海默氏症，精神分裂症 ，肥胖症和偏头痛）包括向需要这种治疗的患者施用有效量的式I化合物。 还公开了治疗上呼吸道过敏反应的方法，包括与组胺H受体拮抗剂组合或混合施用式I化合物或其盐或溶剂合物。

    Imidazole compounds substituted with a six or seven membered heterocyclic ring containing two nitrogen atoms
    6.
    发明授权
    Imidazole compounds substituted with a six or seven membered heterocyclic ring containing two nitrogen atoms 失效
    被含有两个氮原子的六元或七元杂环取代的咪唑化合物

    公开(公告)号：US06211182B1

    公开(公告)日：2001-04-03

    申请号：US09264615

    申请日：1999-03-08

    申请人： Wayne Vaccaro ,  John J. Piwinski ,  Wing C. Tom ,  Daniel M. Solomon ,  Robert G. Aslanian

    发明人： Wayne Vaccaro ,  John J. Piwinski ,  Wing C. Tom ,  Daniel M. Solomon ,  Robert G. Aslanian

    IPC分类号： A61K31496

    CPC分类号： C07D233/64 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14

    摘要： This invention discloses novel imidazoles substituted with a six or seven membered heterocyclic ring which contains two nitrogen atoms as part of the heterocyclic ring structure. These compounds have excellent histamine-H3 receptor antagonist activity. Also disclosed are methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy (for example asthma), inflammation, hypertension, raised intraocular pressure (such as glaucoma)—i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypomotility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimer's Disease, schizophrenia, and migraine). An illustrative inventive imidazole is shown below:

    摘要翻译： 本发明公开了用含有两个氮原子作为杂环结构的一部分的六元或七元杂环取代的新型咪唑。 这些化合物具有优异的组胺H3受体拮抗剂活性。 还公开了制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含这种咪唑的药物组合物以及使用它们治疗过敏（例如哮喘），炎症，高血压，升高的眼内压（如青光眼）的方法，降低眼内压的方法， 睡眠障碍，超低运动性和胃肠道酸性分泌状态，中枢神经系统（例如，激动和抑郁）和其他CNS疾病（如阿尔茨海默病，精神分裂症和偏头痛）的低反应和多动症。 本发明的咪唑如下所示：