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31. 发明授权

US08153681B2 Method of treating epilepsy by administering 5-(4{[(2-fluorophenyl)methyl]oxy}phenyl)prolinamide 有权
标题翻译：通过施用5-（4 {[（2-氟苯基）甲基]氧基}苯基）脯氨酰胺治疗癫痫的方法
公开(公告)号：US08153681B2
公开(公告)日：2012-04-10
申请号：US12641111
申请日：2009-12-17
申请人： Giuseppe Alvaro , Markus Bergauer , Roberto Profeta , Riccardo Giovannini
发明人： Giuseppe Alvaro , Markus Bergauer , Roberto Profeta , Riccardo Giovannini
IPC分类号： A61K31/401
CPC分类号： C07D207/22
摘要： The invention provides a compound of formula (I), a solvate, a salt or prodrug thereof, useful in the treatment of diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels. Methods of treating epilepsy in a mammal are also provided.
摘要翻译：本发明提供式（I）化合物，其溶剂合物，盐或前药，其可用于治疗通过调节依赖于电压门控钠通道介导的疾病和病症。还提供了治疗哺乳动物癫痫的方法。

32. 发明授权

US07655693B2 Compounds 有权
标题翻译：化合物
公开(公告)号：US07655693B2
公开(公告)日：2010-02-02
申请号：US11570560
申请日：2006-10-06
申请人： Giuseppe Alvaro , Markus Bergauer , Roberto Profeta , Riccardo Giovannini
发明人： Giuseppe Alvaro , Markus Bergauer , Roberto Profeta , Riccardo Giovannini
IPC分类号： A61K31/401
CPC分类号： C07D207/22
摘要： The invention provides a compound of formula (I), pharmaceutical compositions thereof, and methods of treatment using the same.
摘要翻译：本发明提供了式（I）化合物，其药物组合物及其使用方法。

33. 发明申请

US20080262041A1 Beta-Lactams for Treatment of Cns Disorders 审中-公开
标题翻译：用于治疗Cns病的β-内酰胺类
公开(公告)号：US20080262041A1
公开(公告)日：2008-10-23
申请号：US10595662
申请日：2004-11-10
申请人： Giuseppe Alvaro , Romano Di Fabio , Riccardo Giovannini , Alfredo Paio , Maria Elvira Tranquillini , Lucia Mattioli
发明人： Giuseppe Alvaro , Romano Di Fabio , Riccardo Giovannini , Alfredo Paio , Maria Elvira Tranquillini , Lucia Mattioli
IPC分类号： A61K31/4439 , A61K31/4025 , C07D401/04 , A61P25/18 , A61P25/24 , A61P19/02 , C07D403/04
CPC分类号： C07D401/04
摘要： The present invention relates to novel compounds of formula (I): wherein — represents a single or a double bond; R is a radical selected from: in which R1 is halogen, cyano, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy and p is zero or an integer from 1 to 3; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen, hydroxy or C1-4 alkyl; R4 is hydrogen or R4 together with R3 represents ═O or ═CH2; R5 is phenyl, naphthyl, a 9 to 10 membered fused bicyclic heterocyclic group or a 5 or 6 membered heteroaryl group, wherein said groups are optionally substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, hydroxy, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or S(O)qC1-4 alkyl; R6 and R7 independently are hydrogen, cyano, C1-4 alkyl; R8 is (CH2)rR10; R9 is hydrogen, halogen, C3-7 cycloalkyl, hydroxy, nitro, cyano or C1-4 alkyl optionally substituted by one or two groups selected from halogen, cyano, hydroxy or C1-4 alkoxy; R10 is hydrogen or C3-7 cycloalkyl; n is 1 or 2; q is 0, 1 or 2; r is 0 or an integer from 1 to 4; or a pharmaceutically acceptable salt or a solvate thereof, process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of the serotonin reuptake transporter protein
摘要翻译：本发明涉及新的式（I）化合物：其中 - 表示单键或双键; R是选自以下的基团：其中R 1是卤素，氰基，C 1-4烷基，C 1-4烷氧基，三氟甲基或三氟甲氧基，p为0或1至3的整数; R 2是氢或C 1-4烷基; R 3是氢，羟基或C 1-4烷基; R 4是氢或R 4与R 3一起代表-O或-CH 2; R 5是苯基，萘基，9至10元稠合双环杂环基或5或6元杂芳基，其中所述基团任选被1至3个独立地选自三氟甲基，烷基，羟基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或S（O）q C 1-4烷基; R 6和R 7独立地是氢，氰基，C 1-4烷基; R 8是（CH 2 2）r R 10; R 9是氢，卤素，C 3-7环烷基，羟基，硝基，氰基或C 1-4烷基，任选被一个或多个两个选自卤素，氰基，羟基或C 1-4烷氧基的基团; R 10是氢或C 3-7环烷基; n为1或2; q是0,1或2; r为0或1至4的整数; 或其药学上可接受的盐或溶剂合物，其制备方法及其用于治疗由粘蛋白介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白

34. 发明授权

US07345041B2 Chemical compounds 有权
标题翻译：化合物
公开(公告)号：US07345041B2
公开(公告)日：2008-03-18
申请号：US11334267
申请日：2006-01-18
申请人： Giuseppe Alvaro , Romano Di Fabio , Riccardo Giovannini , Giuseppe Guercio , Yves St-Denis , Antonella Ursini
发明人： Giuseppe Alvaro , Romano Di Fabio , Riccardo Giovannini , Giuseppe Guercio , Yves St-Denis , Antonella Ursini
IPC分类号： A61K31/495 , A61K31/50
CPC分类号： C07D401/06 , A61K31/135 , A61K31/196 , A61K31/495 , A61K31/496 , C07D241/04 , C07D403/06 , A61K2300/00
摘要： The invention relates to methods for the treatment of a sleep disorder comprising administering a compound of formula (I): wherein all variables are as defined herein.
摘要翻译：本发明涉及治疗睡眠障碍的方法，包括给予式（I）化合物：其中所有变量如本文所定义。

35. 发明授权

US09079905B2 Compounds for the treatment of CNS disorders 有权
标题翻译：用于治疗CNS疾病的化合物
公开(公告)号：US09079905B2
公开(公告)日：2015-07-14
申请号：US13062625
申请日：2009-09-04
申请人： Klaus Fuchs , Cornelia Dorner-Ciossek , Christian Eickmeier , Dennis Fiegen , Thomas Fox , Riccardo Giovannini , Niklas Heine , Martin Hendrix , Holger Rosenbrock , Gerhard Schaenzle
发明人： Klaus Fuchs , Cornelia Dorner-Ciossek , Christian Eickmeier , Dennis Fiegen , Thomas Fox , Riccardo Giovannini , Niklas Heine , Martin Hendrix , Holger Rosenbrock , Gerhard Schaenzle
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04
摘要： The invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones of formula (I). wherein A, R1-R5 and x are as defined herein, and their use as medicaments for improving perception, concentration, learning and/or memory in patients in need thereof.
摘要翻译：本发明涉及式（I）的新型环烷基 - 或环烯基取代的吡唑并嘧啶酮。其中A，R1-R5和x如本文所定义，并且它们作为用于改善有需要的患者的感知，浓度，学习和/或记忆的药物的用途。

36. 发明授权

US08623901B2 Compounds for the treatment of CNS disorders 有权
标题翻译：用于治疗CNS疾病的化合物
公开(公告)号：US08623901B2
公开(公告)日：2014-01-07
申请号：US12749904
申请日：2010-03-30
申请人： Riccardo Giovannini , Cornelia Dorner-Ciossek , Christian Eickmeier , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Niklas Heine , Holger Rosenbrock , Gerhard Schaenzle
发明人： Riccardo Giovannini , Cornelia Dorner-Ciossek , Christian Eickmeier , Dennis Fiegen , Thomas Fox , Klaus Fuchs , Niklas Heine , Holger Rosenbrock , Gerhard Schaenzle
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04 , A61K31/519
摘要： The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), in which Hc is a tetrahydropyranyl-group and R1 is the group V−W−*, whereby V and W independently of each other may be an aryl group or an heteroaryl group, which independently of each other may optionally be substituted. According to one aspect of the invention the new compounds are for use as medicaments or for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments and/or for use in the treatment of e.g. Alzheimer's disease, in particular for cognitive impairment associated with Alzheimer's disease.
摘要翻译：本发明涉及式（I）的新颖的1,6-二取代吡唑并嘧啶酮，其中Hc是四氢吡喃基，R1是VW- *基团，其中V和W彼此独立地可以是芳基或杂芳基基团彼此独立地可以任选地被取代。根据本发明的一个方面，新化合物用作药物或用于制备药物，特别是用于治疗有关感知，集中，学习或记忆缺陷的病症的药物。新化合物也用于制备药物和/或用于治疗例如药物。阿尔茨海默病，特别是与阿尔茨海默病相关的认知障碍。

37. 发明授权

US08143306B2 Methods of treating bipolar disorders 有权
标题翻译：治疗双相性精神障碍的方法
公开(公告)号：US08143306B2
公开(公告)日：2012-03-27
申请号：US12984318
申请日：2011-01-04
申请人： Giuseppe Alvaro , Markus Bergauer , Roberto Profeta , Riccardo Giovannini
发明人： Giuseppe Alvaro , Markus Bergauer , Roberto Profeta , Riccardo Giovannini
IPC分类号： A61K31/401
CPC分类号： A61K31/401
摘要： The invention provides a compound of formula (I), a solvate, a salt or prodrug thereof, useful in the treatment of diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels. Methods of treating and moderating one or more bipolar disorders in a mammal are also provided.
摘要翻译：本发明提供式（I）化合物，其溶剂合物，盐或前药，其可用于治疗通过调节依赖于电压门控钠通道介导的疾病和病症。还提供了治疗和调节哺乳动物中的一种或多种双相性精神障碍的方法。

38. 发明申请

US20100105754A1 5-(4PHENYL)PROLINAMIDE FOR TREATMENT OF EPILEPSY 有权
标题翻译： 5-（4PHENYL）丙酰胺用于治疗EPILEPSY
公开(公告)号：US20100105754A1
公开(公告)日：2010-04-29
申请号：US12641111
申请日：2009-12-17
申请人： Giuseppe Alvaro , Markus Bergauer , Roberto Profeta , Riccardo Giovannini
发明人： Giuseppe Alvaro , Markus Bergauer , Roberto Profeta , Riccardo Giovannini
IPC分类号： A61K31/40 , A61P25/08
CPC分类号： C07D207/22
摘要： The invention provides a compound of formula (I), a solvate, a salt or prodrug thereof, useful in the treatment of diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels.
摘要翻译：本发明提供式（I）化合物，其溶剂合物，盐或前药，其可用于治疗通过调节依赖于电压门控钠通道介导的疾病和病症。

39. 再颁专利

USRE39921E1 Chemical compounds 有权
标题翻译：化合物
公开(公告)号：USRE39921E1
公开(公告)日：2007-11-13
申请号：US10958744
申请日：2004-10-05
申请人： Giuseppe Alvaro , Romano DiFabio , Riccardo Giovannini , Giuseppe Guercio , Yves St-Denis , Antonella Ursini
发明人： Giuseppe Alvaro , Romano DiFabio , Riccardo Giovannini , Giuseppe Guercio , Yves St-Denis , Antonella Ursini
IPC分类号： A61K31/4965
CPC分类号： C07D401/06 , A61K31/496 , C07D241/04 , C07D403/06
摘要： The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.
摘要翻译：本发明涉及哌嗪衍生物，其制备方法，含有它们的药物组合物及其医疗用途。新化合物是速激肽的拮抗剂，包括物质P和其他神经激肽。

40. 发明授权

US09328120B2 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders 有权
标题翻译： 6-环烷基 - 吡唑并嘧啶酮用于治疗CNS疾病
公开(公告)号：US09328120B2
公开(公告)日：2016-05-03
申请号：US14511238
申请日：2014-10-10
申请人： Niklas Heine , Christian Eickmeier , Marco Ferrera , Riccardo Giovannini , Holger Rosenbrock , Gerhard Schaenzle
发明人： Niklas Heine , Christian Eickmeier , Marco Ferrera , Riccardo Giovannini , Holger Rosenbrock , Gerhard Schaenzle
IPC分类号： A61K31/519 , C07D487/04 , A61K45/06 , A61P25/28 , A61P25/18
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61K2300/00
摘要： The invention relates to novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I). wherein R1 is a 5 or 6 membered aromatic heteroaryl-group, R2 is an optional substituent, D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3- or 4-pyridyl, m=1 or 2 and n is 0, 1 or 2. The new compounds are for use as the active entity of medicaments or for the manufacture of medicaments respectively, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. Such conditions may for example be associated with Alzheimer's disease, schizophrenia and other diseases. The new compounds are also for example for the manufacture of medicaments and/or for use in the treatment of these diseases, in particular for cognitive impairment associated with such disease. The compounds of the invention show PDE9 inhibiting properties.
摘要翻译：本发明涉及式（I）的新型6-环烷基 - 吡唑并嘧啶酮。其中R1是5或6元芳族杂芳基，R2是任选的取代基，D是任选取代的环戊基，环己基，四氢呋喃基，四氢吡喃基或2-，3-或4-吡啶基，m = 1或2，n是0 ，1或2.新化合物分别用作药物的活性成分或用于制造药物，特别是用于治疗感知，集中，学习或记忆缺陷的病症的药物。这种情况可能例如与阿尔茨海默病，精神分裂症和其他疾病相关。新化合物还例如用于制备药物和/或用于治疗这些疾病，特别是与这种疾病相关的认知障碍。本发明化合物显示PDE9抑制性质。

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