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21. 发明授权

US5977136A Tetrahydroquinolines as NMDA antagonists 失效
标题翻译：四氢喹啉作为NMDA拮抗剂
公开(公告)号：US5977136A
公开(公告)日：1999-11-02
申请号：US29860
申请日：1998-03-17
申请人： Romano Di Fabio , Simone Giacobbe , Barbara Bertani , Fabrizio Micheli
发明人： Romano Di Fabio , Simone Giacobbe , Barbara Bertani , Fabrizio Micheli
IPC分类号： A61K20060101 , A61K31/47 , A61K31/4709 , C07D20060101 , C07D215/48
CPC分类号： C07D215/48
摘要： Compounds of formula (I) or a salt, or metabolically labile ester thereof, processes for the preparation thereof and their use as antagonists of excitatory amino acids. ##STR1##
摘要翻译： PCT No.PCT / EP96 / 04206 Sec。 371日期：1998年3月17日 102（e）1998年3月17日PCT 1996年9月26日PCT公布。公开号WO97 / 12870 日期1997年4月10日式（I）化合物或其盐或其代谢不稳定酯的方法用于制备它们及其作为兴奋性氨基酸拮抗剂的用途。

22. 发明授权

US07947683B2 3-(1,2,4-triazol-3-ylalkyl) azabicyclo (3.1.0) hexane derivatives as modulators of dopamine D3 receptors 失效
标题翻译： 3-（1,2,4-三唑-3-基烷基）氮杂双环（3.1.0）己烷衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US07947683B2
公开(公告)日：2011-05-24
申请号：US11911027
申请日：2006-04-12
申请人： Giorgio Bonanomi , Anna Checchia , Elettra Fazzolari , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Silvia Terreni
发明人： Giorgio Bonanomi , Anna Checchia , Elettra Fazzolari , Dieter Hamprecht , Fabrizio Micheli , Luca Tarsi , Silvia Terreni
IPC分类号： C07D249/08 , C07D403/14 , C07D401/14 , C07D263/30 , C07D417/14 , A61K31/4196 , A61K31/501 , A61K31/4439 , A61K31/426 , A61K31/4709 , A61P25/18
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐：其制备方法，用于这些方法的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D3受体的调节剂，例如，治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或认知障碍。

23. 发明授权

US08178549B2 Azabicyclo [3. 1. O] hexyl derivatives as modulators of dopamine D3 receptors 失效
标题翻译：氮杂双环[3。 O]己基衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US08178549B2
公开(公告)日：2012-05-15
申请号：US12680785
申请日：2008-10-01
申请人： Barbara Bertani , Francesca Cardullo , Paolo Dambruoso , Paola Marzorati , Fabrizio Micheli , Alessandra Pasquarello , Catia Seri , Giovanna Tedesco
发明人： Barbara Bertani , Francesca Cardullo , Paolo Dambruoso , Paola Marzorati , Fabrizio Micheli , Alessandra Pasquarello , Catia Seri , Giovanna Tedesco
IPC分类号： C07D403/14 , C07D413/14 , A61K31/513
CPC分类号： C07D413/14 , C07D403/14 , C07D417/14 , C07D491/052
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein R1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkoxy and SF5; and n is 1 or 2; their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中R 1是5元杂芳基，任选地与6元杂或碳环稠合; 这样的5或11元系可以任选被1,2,3或4个选自以下的取代基取代：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基，卤代C 1-4烷基， 4烷氧基和SF5; n为1或2; 它们在治疗中的用途，作为多巴胺D3受体的调节剂，例如。治疗药物依赖性，作为抗精神病药，治疗强迫性强迫性疾病或早泄。

24. 发明申请

US20090326011A1 AZAB I CYCLO [3 . 1 . 0] HEXANE DERIVATIVES AS DOPAMIN D3 RECEPTOR MODULATORS 审中-公开
标题翻译： AZAB I CYCLO [3。 1。 0] HEXANE衍生物作为DOPAMIN D3受体调节剂
公开(公告)号：US20090326011A1
公开(公告)日：2009-12-31
申请号：US11917352
申请日：2006-06-13
申请人： Luca Arista , Francesca Cardullo , Anna Checchia , Dieter Hamprecht , Fabrizio Micheli , Giovanna Tedesco , Silvia Terreni
发明人： Luca Arista , Francesca Cardullo , Anna Checchia , Dieter Hamprecht , Fabrizio Micheli , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61K31/4439 , A61K31/41 , A61K31/427 , A61K31/4164 , A61K31/403 , A61K31/4025 , C07D417/14 , C07D417/12 , C07D403/12 , C07D209/52
CPC分类号： C07D417/14 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Disclosed herein are compounds of formula (I) where G and Q are heteroaromatic groups. These compounds are useful for treating psychosis or a psychotic condition, substance abuse, premature ejaculation or cognition impairment.
摘要翻译：本文公开了式（I）的化合物，其中G和Q是杂芳族基团。这些化合物可用于治疗精神病或精神病状，药物滥用，早泄或认知障碍。

25. 发明授权

US07776904B2 Azabicyclo [3.1.0] hexylphenyl derivatives as modulators of dopamine D3 receptors 失效
标题翻译：氮杂双环[3.1.0]己基苯基衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US07776904B2
公开(公告)日：2010-08-17
申请号：US12064121
申请日：2006-08-18
申请人： Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Adolfo Prandi , Silvia Terreni
发明人： Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Adolfo Prandi , Silvia Terreni
IPC分类号： A61K31/403 , C07D209/52
CPC分类号： C07D209/52
摘要： The present invention relates to novel compounds of formula (IA) or a salt thereof: wherein: A is attached to the phenyl group at the meta position or the para position relative to the cyclopropyl group, and is selected from the group consisting of: —SO2NR5—, —SO2CR2R3—, —CR2R3SO2— and —NR5SO2—; R1 is hydrogen, C1-6alkyl, haloC1-6alkyl or C2-6alkylene; R2 and R3 are independently hydrogen or C1-6alkyl; R4 is hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; R5 is hydrogen, C1-6alkyl, or a phenyl optionally substituted by R4; and R6 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（IA）化合物或其盐：其中：A相对于环丙基在间位或对位与苯基连接，并且选自： - SO 2 NR 5 - ， - SO 2 CR 2 R 3 - ， - CR 2 R 3 SO 2 - 和-NR 5 SO 2 - ; R1是氢，C1-6烷基，卤代C 1-6烷基或C 2-6亚烷基; R2和R3独立地是氢或C1-6烷基; R 4是氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; R5是氢，C1-6烷基或任选被R4取代的苯基; 并且R 6是氢，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D3受体的调节剂。治疗物质相关疾病，作为抗精神病药物早泄或认知障碍。

26. 发明申请

US20100016287A1 COMPOUNDS HAVING AFFINITY FOR DOPAMINE D3 RECEPTOR AND USES THEREOF" 失效
标题翻译：具有DOPAMINE D3受体的亲和性的化合物及其用途“
公开(公告)号：US20100016287A1
公开(公告)日：2010-01-21
申请号：US11569880
申请日：2005-05-31
申请人： Giorgio Bonanomi , Federica Damiani , Gabriella Gentile , Dieter Wolfgang Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
发明人： Giorgio Bonanomi , Federica Damiani , Gabriella Gentile , Dieter Wolfgang Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61K31/55 , C07D498/04 , A61P25/00
CPC分类号： C07D513/04 , C07D487/04
摘要： Compounds of formula (I) wherein A is a 5 or 6 membered heteroaromatic ring or a 5 or 6 membered heterocyclic ring, and which are useful for treating mental disorders such as schizophrenia are set out herein.
摘要翻译：本文列出了其中A为5或6元杂芳环或5或6元杂环，可用于治疗精神障碍如精神分裂症的式（I）化合物。

27. 发明申请

US20090030062A1 AZABICYCLO [3.1.0] HEXYLPHENYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 失效
标题翻译：亚氨基胆碱[3.1.0]作为DOPAMINE D3受体的调节剂的HEXYLPHENYL衍生物
公开(公告)号：US20090030062A1
公开(公告)日：2009-01-29
申请号：US12064121
申请日：2006-08-18
申请人： Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Adolfo Prandi , Silvia Terreni
发明人： Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli , Adolfo Prandi , Silvia Terreni
IPC分类号： A61K31/403 , C07D209/52
CPC分类号： C07D209/52
摘要： The present invention relates to novel compounds of formula (IA) or a salt thereof: wherein: A is attached to the phenyl group at the meta position or the para position relative to the cyclopropyl group, and is selected from the group consisting of: —SO2NR5—, —SO2CR2R3—, —CR2R3SO2— and —NR5SO2—; R1 is hydrogen, C1-6alkyl, haloC1-6alkyl or C2-6alkylene; R2 and R3 are independently hydrogen or C1-6alkyl; R4 is hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; R5 is hydrogen, C1-6alkyl, or a phenyl optionally substituted by R4; and R6 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
摘要翻译：本发明涉及式（IA）的新化合物或其盐：其中：A相对于环丙基在间位或对位与苯基连接，并且选自： - SO 2 NR 5 - ， - SO 2 CR 2 R 3 - ， - CR 2 R 3 SO 2 - 和-NR 5 SO 2 - ; R1是氢，C1-6烷基，卤代C 1-6烷基或C 2-6亚烷基; R2和R3独立地是氢或C1-6烷基; R 4是氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; R5是氢，C1-6烷基或任选被R4取代的苯基; 并且R 6是氢，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D3受体的调节剂。治疗物质相关疾病，作为抗精神病药物早泄或认知障碍。

28. 发明授权

US07989444B2 Compounds having affinity for dopamine D3 receptor and uses thereof 失效
标题翻译：对多巴胺D3受体具有亲和性的化合物及其用途
公开(公告)号：US07989444B2
公开(公告)日：2011-08-02
申请号：US11569880
申请日：2005-05-31
申请人： Giorgio Bonanomi , Federica Damiani , Gabriella Gentile , Dieter Wolfgang Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
发明人： Giorgio Bonanomi , Federica Damiani , Gabriella Gentile , Dieter Wolfgang Hamprecht , Fabrizio Micheli , Luca Tarsi , Giovanna Tedesco , Silvia Terreni
IPC分类号： A61P25/18 , A61K31/55 , C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D513/04 , C07D487/04
摘要： Compounds of formula (I) wherein A is a 5 or 6 membered heteroaromatic ring or a 5 or 6 membered heterocyclic ring, and which are useful for treating mental disorders such as schizophrenia are set out herein.
摘要翻译：本文列出了其中A为5或6元杂芳环或5或6元杂环，可用于治疗精神障碍如精神分裂症的式（I）化合物。

29. 发明申请

US20100210672A1 AZABICYCLO [3. 1. O] HEXYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 失效
标题翻译： AZABICYCLO [3。作为DOPAMINE D3受体的调节剂的HEXYL衍生物
公开(公告)号：US20100210672A1
公开(公告)日：2010-08-19
申请号：US12680785
申请日：2008-10-01
申请人： Barbara Bertani , Francesca Cardullo , Paolo Dambruoso , Paola Marzorati , Fabrizio Micheli , Alessandra Pasquarello , Catia Seri , Giovanna Tedesco
发明人： Barbara Bertani , Francesca Cardullo , Paolo Dambruoso , Paola Marzorati , Fabrizio Micheli , Alessandra Pasquarello , Catia Seri , Giovanna Tedesco
IPC分类号： A61K31/506 , C07D403/14 , A61P25/18 , A61P25/30
CPC分类号： C07D413/14 , C07D403/14 , C07D417/14 , C07D491/052
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: whereinR1 is a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkoxy and SF5; and n is 1 or 2; their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中R 1是5元杂芳基，任选地与6元杂或碳环稠合; 这样的5或11元系可以任选被1,2,3或4个选自以下的取代基取代：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基，卤代C 1-4烷基， 4烷氧基和SF5; n为1或2; 它们在治疗中的用途，作为多巴胺D3受体的调节剂，例如。治疗药物依赖性，作为抗精神病药，治疗强迫性强迫性疾病或早泄。

30. 发明授权

US07745458B2 Azabicyclo (3, 1, 0) hexan derivatives useful as modulators of dopamine D3 receptors 失效
标题翻译：可用作多巴胺D3受体调节剂的氮杂双环（3,1,0）己烷衍生物
公开(公告)号：US07745458B2
公开(公告)日：2010-06-29
申请号：US12064123
申请日：2006-08-18
申请人： Luca Arista , Anna Checchia , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli
发明人： Luca Arista , Anna Checchia , Gabriella Gentile , Dieter Hamprecht , Fabrizio Micheli
IPC分类号： A01N43/42 , A61K31/44 , C07D239/00 , C07D239/02 , C07D261/04 , C07D261/14 , C07D233/00 , C07D233/14 , C07D233/60
CPC分类号： C07D403/06 , C07D403/12
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中：p为0,1,2,3,4或5; R 1独立地选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; n为3或4; R2是氢或C1-4烷基; n为2或3; X是-CH 2 - ， - O-或-S-; Z可以是-CH-或N; A是P或P1基团，其中P是和P1是且Y是氢，-OH，C 1-4烷基，卤代C 1-4烷基，苯基或杂芳基，其中苯基和杂芳基任选被一个或两个选自C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基和卤代C 1-4烷氧基的取代基; 它们的制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D3受体的调节剂。治疗物质相关疾病，作为抗精神病药物早泄或认知障碍。

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