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    Isoxazolecarboxamide derivatives
    4.
    发明授权
    Isoxazolecarboxamide derivatives 失效
    异恶唑甲酰胺衍生物

    公开(公告)号：US06680319B2

    公开(公告)日：2004-01-20

    申请号：US10052325

    申请日：2002-01-17

    申请人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Elena Poggesi

    发明人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Elena Poggesi

    IPC分类号： A61K31422

    CPC分类号： C07D261/18

    摘要： The invention relates to novel N-(substituted phenyl)-N′-[&ohgr;-(3-substituted phenyl-4-isoxazolecarbonylamino)alkyl]piperazines, 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) and neurogenic lower urinary tract dysfunction (NLUTD), and other conditions. The compounds may be administered alone or in combination with an anticholinergic compound.

    摘要翻译： 本发明涉及新的N-（取代的苯基）-N' - （ - （ω-（3-取代的苯基-4-异恶唑氨基）烷基]哌嗪，它们的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）和神经源性下尿路功能障碍（NLUTD）等情况。 化合物可以单独施用或与抗胆碱能化合物组合施用。

    Isoxazolecarboxamide derivatives
    5.
    发明授权
    Isoxazolecarboxamide derivatives 失效
    异恶唑甲酰胺衍生物

    公开(公告)号：US06365591B1

    公开(公告)日：2002-04-02

    申请号：US09691778

    申请日：2000-10-18

    申请人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Elena Poggesi

    发明人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Elena Poggesi

    IPC分类号： C07D41312

    CPC分类号： C07D261/18

    摘要： The invention relates to novel N-(substituted phenyl)-N′-[&ohgr;-(3-substituted phenyl-4-isoxazolecarbonylamino)alkyl]piperazines, 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) and neurogenic lower urinary tract dysfunction (NLUTD), and other conditions.

    摘要翻译： 本发明涉及新的N-（取代的苯基）-N' - （ - （ω-（3-取代的苯基-4-异恶唑氨基）烷基]哌嗪，它们的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）和神经源性下尿路功能障碍（NLUTD）等情况。

    1,4-disubstituted piperazines
    6.
    发明授权
    1,4-disubstituted piperazines 失效
    1,4-二取代的哌嗪

    公开(公告)号：US06271234B1

    公开(公告)日：2001-08-07

    申请号：US09266534

    申请日：1999-03-11

    申请人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Luciano Guarneri ,  Elena Poggesi

    发明人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Luciano Guarneri ,  Elena Poggesi

    IPC分类号： A61K31496

    CPC分类号： C07D213/75

    摘要： Disclosed herein are novel compounds and methods for the treatment of disorders of the lower urinary tract. The novel compounds are 1,4-disubstituted piperazine derivatives. The methods comprise the administration of the novel compounds of the invention, and other compounds that bind to 5HT1A receptors, for treating disorders of the lower urinary tract.

    摘要翻译： 本文公开了用于治疗下尿路疾病的新型化合物和方法。 新化合物是1,4-二取代的哌嗪衍生物。 所述方法包括施用本发明的新化合物和结合5HT1A受体的其它化合物，用于治疗下尿路的疾病。

    HETEROCYCLIC M-GLU5 ANTAGONISTS
    7.
    发明申请
    HETEROCYCLIC M-GLU5 ANTAGONISTS 审中-公开
    杂交M-GLU5拮抗剂

    公开(公告)号：US20120028931A1

    公开(公告)日：2012-02-02

    申请号：US12882169

    申请日：2010-09-14

    申请人： Amedeo Leonardi ,  Carlo Riva ,  Luciano Guarneri ,  Davide Graziani ,  Fabio Marinoni ,  Gianni Motta ,  Ilaria Bettinelli

    发明人： Amedeo Leonardi ,  Carlo Riva ,  Luciano Guarneri ,  Davide Graziani ,  Fabio Marinoni ,  Gianni Motta ,  Ilaria Bettinelli

    IPC分类号： A61K31/616 ,  A61K31/4545 ,  C07D409/14 ,  C07D401/14 ,  C07D417/14 ,  C07D413/14 ,  A61K31/497 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/55 ,  C07D495/04 ,  A61K31/4725 ,  A61K31/46 ,  A61K31/517 ,  A61P13/00 ,  A61P13/10 ,  A61P25/00 ,  A61P25/22 ,  A61P25/30 ,  A61P25/04 ,  A61P43/00 ,  A61P1/04 ,  C07D405/14

    CPC分类号： C07D405/14 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    摘要： Compounds I (R1 is an optionally substituted C1-C13 heteromonocyclic, heterobicyclic or heterotricyclic group containing from 1 to 5 heteroatoms selected from N, O and S; R2 is H, an optionally substituted monocyclic aromatic group, or a C1-C5 heteroaromatic group containing from 1 to 4 heteroatoms selected from N, O and S; R3 is an optionally substituted C1-C13 heteromonocyclic, heterobicyclic or heterotricyclic group containing from 1 to 5 heteroatoms selected from N, O and S; an optionally substituted mono-, bi- or tricyclic C6-C14 aryl group, an optionally substituted C3-C6 cycloalkyl group, or an optionally substituted C3-C6 cycloalkenyl group; each R4, independently for each position capable of substitution, is H or C1-C6 alkyl; R5 is H, halogen or C1-C6 alkyl; m is 0, 1 or 2; n is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, or 6; and is an optional double bond) and their enantiomers, diastereomers, N-oxides and pharmaceutically acceptable salts, and pharmaceutical compositions containing them, are useful for the treatment of neuromuscular dysfunction of the lower urinary tract and also for the treatment of gastrooesophageal reflux disease; anxiety disorder; abuse, substance dependence and substance withdrawal disorders; neuropathic pain disorder, migraine and fragile X syndrome disorders.

    摘要翻译： 化合物I（R1是含有1至5个选自N，O和S的杂原子的任选取代的C 1 -C 13杂单环，杂双环或异三环基团; R 2是H，任选取代的单环芳族基团或含有C 1 -C 5杂芳族基团 1至4个选自N，O和S的杂原子; R 3是任选取代的含有1至5个选自N，O和S的杂原子的C1-C13杂单环，杂双环或异三环;任选取代的单 - ，二 - 三环C 6 -C 14芳基，任选取代的C 3 -C 6环烷基或任选取代的C 3 -C 6环烯基;每个R 4独立地为每个能够取代的位置是H或C 1 -C 6烷基; R 5是H，卤素 或C 1 -C 6烷基; m为0,1或2; n为0,1或2; p为0,1,2,3,4,5或6;并且为任选的双键）及其对映异构体， 非对映异构体，N-氧化物和药学上可接受的盐，以及含有的药物组合物 它们可用于治疗下尿路神经肌肉功能障碍，也可用于治疗胃食管反流病; 焦虑症 滥用，物质依赖和物质戒断障碍; 神经性疼痛障碍，偏头痛和脆弱X综合征障碍。

    Spiroheterocyclic compounds as mGlu5 antagonists
    8.
    发明授权
    Spiroheterocyclic compounds as mGlu5 antagonists 有权
    螺杂环化合物作为mGlu5拮抗剂

    公开(公告)号：US08580962B2

    公开(公告)日：2013-11-12

    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： A61K31/44 ,  C07D213/00

    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。

    NOVEL SPIROHETEROCYCLIC COMPOUNDS AS MGLU5 ANTAGONISTS
    9.
    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。