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    HETEROCYCLIC M-GLU5 ANTAGONISTS
    1.
    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。

    QUINOLINE-4-CARBOXAMIDE AS NK-2 AND NK-3 RECEPTOR ANTAGONISTS
    2.
    发明申请
    QUINOLINE-4-CARBOXAMIDE AS NK-2 AND NK-3 RECEPTOR ANTAGONISTS 审中-公开

    公开(公告)号：US20070197546A1

    公开(公告)日：2007-08-23

    申请号：US11691899

    申请日：2007-03-27

    申请人： Giuseppe Giardina ,  Mario Grugni ,  Davide Graziani ,  Luca Raveglia

    发明人： Giuseppe Giardina ,  Mario Grugni ,  Davide Graziani ,  Luca Raveglia

    IPC分类号： A61K31/4709 ,  A61K31/496 ,  C07D401/02

    CPC分类号： C07D401/06 ,  C07D215/50 ,  C07D215/52 ,  C07D251/52 ,  C07D491/10 ,  C07D491/113

    摘要： A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or a C5-7 cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group,; R is C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, optionally substituted phenyl or phenyl C1-6 alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or R is a group —(CH2)p— wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C1-6 alkylamino; R2 represents a moiety —(CH2)n—NY1Y2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from hydrogen; C1-6-alkyl; C1-6 alkyl substituted with hydroxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or C1-6 alkyl; a pharmaceutical composition comprising such a compound, process for preparing such a compound and the use of such a compound in medicine.

    Quinoline-4-carboxamide as NK-2 and NK-3 receptor antagonists
    3.
    发明申请
    Quinoline-4-carboxamide as NK-2 and NK-3 receptor antagonists 审中-公开

    公开(公告)号：US20060205735A1

    公开(公告)日：2006-09-14

    申请号：US11418274

    申请日：2006-05-04

    申请人： Giuseppe Maria Glardina ,  Mario Grugni ,  Davide Graziani ,  Luca Raveglia

    发明人： Giuseppe Maria Glardina ,  Mario Grugni ,  Davide Graziani ,  Luca Raveglia

    IPC分类号： A61K31/496 ,  A61K31/4709 ,  C07D403/02 ,  C07D401/02

    CPC分类号： C07D401/06 ,  C07D215/50 ,  C07D215/52 ,  C07D251/52 ,  C07D491/10 ,  C07D491/113

    摘要： A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or a C5-7 cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group; R is C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, optionally substituted phenyl or phenyl C1-6 alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or R is a group —(CH2)p— wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C1-6 alkylamino; R2 represents a moiety —(CH2)n—NY1Y2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from hydrogen; C1-6-alkyl; C1-6 alkyl substituted with hydroxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or C1-6 alkyl; a pharmaceutical composition comprising such a compound, process for preparing such a compound and the use of such a compound in medicine.

    Quinoline-4-carboxamide derivatives asNK-2 and NK-3 receptor antagonists
    4.
    发明申请
    Quinoline-4-carboxamide derivatives asNK-2 and NK-3 receptor antagonists 审中-公开

    公开(公告)号：US20050159428A1

    公开(公告)日：2005-07-21

    申请号：US11085028

    申请日：2005-03-14

    申请人： Giuseppe Maria Giardina ,  Mario Grugni ,  Davide Graziani ,  Luca Raveglia

    发明人： Giuseppe Maria Giardina ,  Mario Grugni ,  Davide Graziani ,  Luca Raveglia

    IPC分类号： C07D251/52 ,  C07D401/06 ,  C07D491/10 ,  C07D43/02 ,  A61K31/4709 ,  A61K31/496 ,  C07D41/02

    CPC分类号： C07D401/06 ,  C07D215/50 ,  C07D215/52 ,  C07D251/52 ,  C07D491/10 ,  C07D491/113

    摘要： A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or a C5-7 cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group; R is C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, optionally substituted phenyl or phenyl C1-6 alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or R is a group —(CH2)p— wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C1-6 alkylamino; R2 represents a moiety —(CH2)n—NY1Y2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from hydrogen; C1-6-alkyl; C1-6 alkyl substituted with hydroxy, C1-6 alkylamino or bis(C1-6 alkyl)amino; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or C1-6 alkyl; a pharmaceutical composition comprising such a compound, process for preparing such a compound and the use of such a compound in medicine.

    NOVEL SPIROHETEROCYCLIC COMPOUNDS AS MGLU5 ANTAGONISTS
    7.
    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。

    Spiroheterocyclic compounds as mGlu5 antagonists
    10.
    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。