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    NOVEL SPIROHETEROCYCLIC COMPOUNDS AS MGLU5 ANTAGONISTS
    31.
    发明申请
    NOVEL SPIROHETEROCYCLIC COMPOUNDS AS MGLU5 ANTAGONISTS 有权
    新型螺旋体化合物作为MGLU5拮抗剂

    公开(公告)号：US20120059015A1

    公开(公告)日：2012-03-08

    申请号：US13180166

    申请日：2011-07-11

    申请人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Luciano Guarneri ,  Davide Graziani ,  Carlo De Toma ,  Katia Dimitrova Karamfilova

    发明人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Luciano Guarneri ,  Davide Graziani ,  Carlo De Toma ,  Katia Dimitrova Karamfilova

    IPC分类号： A61K31/423 ,  A61K31/4439 ,  A61P1/04 ,  A61K31/427 ,  A61P13/10 ,  A61P13/00 ,  C07D498/10 ,  A61K31/497

    CPC分类号： C07D498/10 ,  C07D491/10

    摘要： The invention is directed to methods of using antagonists selective for the metabotropic mGlu5 receptor to treat conditions of neuromuscular dysfunction of the lower urinary tract in a mammal. Provided are methods of treating a mammal suffering from a condition of neuromuscular dysfunction of the lower urinary tract by administering a selective mGlu5 antagonist. The selective mGlu5 antagonist may be administered alone or in combination with one or more additional therapeutic agents for treating such a condition. Also provided are methods of identifying selective mGlu5 antagonists that are useful for treating neuromuscular dysfunction of the lower urinary tract in a mammal. Methods for treating migraine and gastroesophageal reflux disease (GERD) using selective mGlu5 antagonists are also disclosed.

    摘要翻译： 本发明涉及使用选择性代谢型mGlu5受体的拮抗剂治疗哺乳动物下泌尿道神经肌肉功能障碍的方法。 提供了通过施用选择性mGlu5拮抗剂治疗患有下尿路神经肌肉功能障碍的哺乳动物的方法。 选择性mGlu5拮抗剂可以单独施用或与一种或多种用于治疗这种病症的其它治疗剂组合施用。 还提供鉴定可用于治疗哺乳动物下泌尿道神经肌肉功能障碍的选择性mGlu5拮抗剂的方法。 还公开了使用选择性mGlu5拮抗剂治疗偏头痛和胃食管反流病（GERD）的方法。

    N,N-disubstituted diazocycloalkanes
    34.
    发明授权
    N,N-disubstituted diazocycloalkanes 失效
    N，N-二取代的二氮杂环烷烃

    公开(公告)号：US07071197B2

    公开(公告)日：2006-07-04

    申请号：US10463222

    申请日：2003-06-16

    申请人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Rodolfo Testa

    发明人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Rodolfo Testa

    IPC分类号： A61K31/495 ,  C07D295/092

    CPC分类号： C07D295/092 ,  C07D243/08

    摘要： N,N-Disubstituted diazocycloalkanes of the formula I (R1=halogen, R2=(C3–C8)-cycloalkyl, R3=(C1–C4)-alkoxy or (C1–C4)-haloalkoxy group, m is 1 or 2 and n is 1 or 2, have affinity for serotonergic receptors. These compounds and their enantiomers, diastereoisomers, N-oxides, polymorphs, solvates and pharmaceutically acceptable salts are useful in the treatment of patients with neuromuscular dysfunction of the lower urinary tract and diseases related to 5-HT1A receptor.

    摘要翻译： 式I的N，N-二取代的二氮杂环烷烃（R 1 =卤素，R 2 =（C 3 -C 8） / - ） - 环烷基，R 3 =（C 1 -C 4 - ） - 烷氧基或（C 1 -C 12） 这些化合物及其对映异构体，非对映异构体，N-氧化物，多晶型物，溶剂合物和/或其衍生物，以及 药学上可接受的盐可用于治疗下尿路神经肌肉功能障碍患者和与5-HT 1A受体相关的疾病。

    Benzopyran derivatives
    36.
    发明授权
    Benzopyran derivatives 失效
    苯并吡喃衍生物

    公开(公告)号：US06403594B1

    公开(公告)日：2002-06-11

    申请号：US09691770

    申请日：2000-10-18

    申请人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Giorgio Sironi

    发明人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Giorgio Sironi

    IPC分类号： A61K31496

    CPC分类号： C07D311/30 ,  C07D311/24

    摘要： The invention relates to novel benzopyran derivatives of formula I, their N-oxides and pharmaceutically acceptable salts thereof. The compounds are endowed with enhanced selectivity for alpha1-adrenergic receptors and a low activity in lowering blood pressure. The compounds are useful in the treatment of obstructive syndromes of the lower urinary tract, including benign prostatic hyperplasia (BPH), and in the treatment of lower urinary tract symptoms (LUTS), neurogenic lower urinary tract dysfunction (NLUTD), and other conditions.

    摘要翻译： 本发明涉及式I的新型苯并吡喃衍生物，其N-氧化物及其药学上可接受的盐。 该化合物具有增强的α1-肾上腺素能受体的选择性和降低血压的低活性。 该化合物可用于治疗下尿路阻塞性综合征，包括良性前列腺增生（BPH），以及治疗下尿路症状（LUTS），神经源性下尿路功能障碍（NLUTD）等情况。

    Thienopyrancecarboxamide derivatives
    37.
    发明授权
    Thienopyrancecarboxamide derivatives 失效

    公开(公告)号：US06306861B1

    公开(公告)日：2001-10-23

    申请号：US09627766

    申请日：2000-07-28

    申请人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Rodolfo Testa

    发明人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Rodolfo Testa

    IPC分类号： C07D40512

    CPC分类号： C07D495/04

    摘要： The invention is directed to compounds of Formula I: wherein R is an aryl, cycloalkyl or polyhaloalkyl group, R1 is chosen from the group consisting of alkyl, alkoxy, polyfluoroalkoxy, hydroxy and trifluoromethanesulfonyloxy; each of R2 and R3 independently is chosen from the group consisting of a hydrogen, halogen, alkoxy and polyfluoroalkoxy group, and n is 0, 1 or 2. The invention further provides pharmaceutical compositions comprising a compound of Formula I or a N-oxide or pharmaceutically acceptable salt of such a compound in admixture with a pharmaceutically acceptable diluent or carrier. In another aspect, the present invention is directed to methods for selectively preventing contractions of the urethra and lower urinary tract, without substantially affecting blood pressure, by administering one or more selected compounds of Formula I to a mammal (including a human) in need of such treatment in an amount or amounts effective for the particular use. In yet another aspect, the invention is directed to methods for blocking &agr;1 receptors, by delivering to the environment of said receptors, e.g., to the extracellular medium, (or by administering to a mammal possessing said receptors) an effective amount of a compound of the invention, in this way relieving diseases associated to overactivity of said receptors. It is also an object of the present invention to provide a method of treating BPH which avoids any undue side effects due to acute hypotension (i.e., limited effects on blood pressure). It is another object of the present invention to provide pharmaceutical compositions comprising 7-oxo-7H-thieno[3,2-b]pyran compounds which are selective &agr;1 adrenoceptor antagonists, which compositions are effective for the treatment of BPH optionally including a carrier or diluent. It is another object of the present invention to provide a method of treating BPH using 7-oxo-7H-thieno[3,2-b]pyran compounds which are selective &agr;1 adrenoceptor antagonists. Other aspects of the invention are the use of new compounds for lowering intraocular pressure, the treatment of cardiac arrhythmia and erectile dysfunction, treatment of sympathetically mediated pain, treatment of NLUTD, and treatment of LUTS in males and females. In another aspect of the invention, compounds of the invention are administered in combination with anticholinergic compounds.