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11. 发明申请

US20120022056A1 FUSED TRICYCLIC DERIVATIVES FOR THE TREATMENT OF PSYCHOTIC DISORDERS 审中-公开
标题翻译：用于治疗心理障碍的融合三聚体衍生物
公开(公告)号：US20120022056A1
公开(公告)日：2012-01-26
申请号：US11574450
申请日：2005-08-29
申请人： Jonathan Bentley , Markus Bergauer , Babara Bertani , Matteo Biagetti , Manuela Borriello , Steven Mark Bromidge , Massimo Gianotti , Enrica Granci , Colin Philip Leslie , Alessandra Pasquarello , Valeria Zucchelli
发明人： Jonathan Bentley , Markus Bergauer , Babara Bertani , Matteo Biagetti , Manuela Borriello , Steven Mark Bromidge , Massimo Gianotti , Enrica Granci , Colin Philip Leslie , Alessandra Pasquarello , Valeria Zucchelli
IPC分类号： A61K31/5383 , C07D471/04 , A61K31/496 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/22 , A61P15/00 , C07D498/04 , A61K31/4545
CPC分类号： C07D471/04
摘要： Compounds of formula (I) wherein R1, R2, X, A, Y, B, Z1, Q, p, r and s are defined in the specification for treating inter alia psychotic disorders, depressive disorders, anxiety disorders and sexual dysfunctions.
摘要翻译：在说明书中定义为治疗精神病，抑郁障碍，焦虑障碍和性功能障碍的R1，R2，X，A，Y，B，Z1，Q，p，r和s的式（I）化合物。

12. 发明申请

US20100069416A1 Azabicyclo [3.1.0] Hexyl Derivatives as Modulators of Dopamine D3 Receptors 失效
标题翻译：偶氮二环[3.1.0]己基衍生物作为多巴胺D3受体的调节剂
公开(公告)号：US20100069416A1
公开(公告)日：2010-03-18
申请号：US12295304
申请日：2007-03-30
申请人： Barbara Bertani , Anna Checchia , Romano Di Fabio , Gabriella Gentile , Alessandra Pasquarello , Silvia Terreni
发明人： Barbara Bertani , Anna Checchia , Romano Di Fabio , Gabriella Gentile , Alessandra Pasquarello , Silvia Terreni
IPC分类号： A61K31/506 , C07D403/06 , C07D401/14 , C07D417/14 , A61P25/00 , A61P25/30 , A61P15/12
CPC分类号： C07D401/14 , C07D403/06 , C07D405/14
摘要： The present invention relates to certain azabicyclo compounds of formula (I)′: wherein the various groups are defined herein and that are 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：本发明涉及某些式（I）'的氮杂二环化合物：其中各种基团在本文中定义，并且是多巴胺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。

13. 发明授权

US07329667B2 CRF receptor antagonists 失效
标题翻译： CRF受体拮抗剂
公开(公告)号：US07329667B2
公开(公告)日：2008-02-12
申请号：US10476441
申请日：2002-04-30
申请人： Romano Di Fabio , Fabrizio Micheli , Alessandra Pasquarello , Yves St. Denis
发明人： Romano Di Fabio , Fabrizio Micheli , Alessandra Pasquarello , Yves St. Denis
IPC分类号： A01N43/54 , C07D239/00
CPC分类号： C07D471/06 , C07D487/06
摘要： The present invention relates to tricyclic pyrimidines compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof, to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明涉及式（I）的三环嘧啶化合物，其包括立体异构体，其前药和药学上可接受的盐或溶剂化物，其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放介导的病症因子（CRF）。

14. 发明授权

US08030322B2 Spirocompounds useful as modulators for dopamine D3 receptors 失效
标题翻译：螺环化合物可用作多巴胺D3受体的调节剂
公开(公告)号：US08030322B2
公开(公告)日：2011-10-04
申请号：US12297253
申请日：2007-04-24
申请人： Barbara Bertani , Romano Di Fabio , Fabrizio Micheli , Alessandra Pasquarello , Luca Tarsi , Silvia Terreni
发明人： Barbara Bertani , Romano Di Fabio , Fabrizio Micheli , Alessandra Pasquarello , Luca Tarsi , Silvia Terreni
IPC分类号： C07D403/06 , C07D409/14 , A61K31/421 , A61K31/506
CPC分类号： C07D403/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/10
摘要： The present invention relates to compounds of formula (I) or salts thereof wherein A, X, R2, R4 and n are defined herein, 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 to enhance cognition.
摘要翻译：本发明涉及式（I）化合物或其盐，其中A，X，R2，R4和n如本文所定义，其制备方法，在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，如多巴胺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，早泄或增强认知。

15. 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。

16. 发明申请

US20100063097A1 Azabicyclo [3.1.0] Hexane Derivatives as Modulators of Dopamine D3 Receptors 失效
标题翻译：氮杂二环[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：US20100063097A1
公开(公告)日：2010-03-11
申请号：US12295024
申请日：2007-03-30
申请人： Barbara Bertani , Fabrizio Micheli , Alessandra Pasquarello , Silvia Terreni
发明人： Barbara Bertani , Fabrizio Micheli , Alessandra Pasquarello , Silvia Terreni
IPC分类号： A61K31/4439 , C07D401/06 , C07D401/14 , A61P25/00 , A61K31/444 , A61P25/30
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to certain azabicyclic compounds of formula (I)′: wherein the several groups are defined herein and are 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：本发明涉及某些式（I）'的氮杂双环化合物：其中数个基团在本文中定义，并且是多巴胺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。

17. 发明申请

US20100004452A1 5-QUINOLINONE DERIVATIVES AS 5HT1A RECEPTOR MODULATORS FOR TREATING SEXUAL DYSFUNCTION, COGNITION IMPAIRMENT, PSYCHOTIC DISORDERS, ANXIETY, DEPRESSION, ETC. 审中-公开
标题翻译： 5-Quinolinone衍生物作为5HT1A受体调节剂，用于治疗性功能障碍，认知障碍，心理障碍，异常，呕吐等。
公开(公告)号：US20100004452A1
公开(公告)日：2010-01-07
申请号：US12442148
申请日：2007-09-24
申请人： Barbara Bertani , Steven Mark Bromidge , Massimo Gianotti , Alessandra Pasquarello , Valeria Zucchelli
发明人： Barbara Bertani , Steven Mark Bromidge , Massimo Gianotti , Alessandra Pasquarello , Valeria Zucchelli
IPC分类号： C07D401/14
CPC分类号： C07D401/12 , C07D401/14 , C07D487/08
摘要： Disclosed are compounds of formula (I) wherein R1 is C1-6alkyl, halo or haloC1-6alkyl; R2 is hydrogen or C1-6alkyl; is a single or double bond; each R3 and R4, which may be the same or different, are hydrogen, C1-6alkyl or haloC1-6alkyl; wherein i) when is a double bond p and q are 1, and ii) when is a single bond, p and q are 2, and one of R3 and one of R4, together with their interconnecting atoms, forms a cyclopropane ring which may be substituted by one or two halo or methyl groups, which groups may be the same or different; X is CH or N; when present each R5, which may be the same or different, is C1-6alkyl or halo; or two R5 groups may join to form a bridge, which bridge contains one or two atoms; n is 0, 1, 2 or 3; when present each R6 which may be the same or different, is C1-6alkyl or halo; and m is 0, 1, 2 or 3.
摘要翻译：公开了式（I）的化合物，其中R 1是C 1-6烷基，卤素或卤代C 1-6烷基; R2是氢或C1-6烷基; “img id =”CUSTOM-CHARACTER-00001“he =”2.79mm“wi =”6.35mm“file =”US20100004452A1-20100107-P00001.TIF“img-content =”character“img-format =”tif“/> 是单键或双键; 每个R 3和R 4可以相同或不同，是氢，C 1-6烷基或卤代C 1-6烷基; 其中i）当是双键p，q是1，ii）当是单键，p和q是2，R 3和R 4中的一个连同它们的互连原子一起形成环丙烷环，被一个或两个卤素或甲基取代，这些基团可以相同或不同; X是CH或N; 当存在时，每个可以相同或不同的R 5是C 1-6烷基或卤素; 或两个R5基团可以连接形成桥，该桥包含一个或两个原子; n为0,1,2或3; 当存在每个可以相同或不同的R 6是C 1-6烷基或卤素时; m为0,1,2或3。

18. 发明授权

US07462622B2 Pyrrolo[2, 3-d] pyrimidine derivatives as corticotropin releasing factor antagonists 失效
标题翻译：吡咯并[2,3-d]嘧啶衍生物作为促肾上腺皮质激素释放因子拮抗剂
公开(公告)号：US07462622B2
公开(公告)日：2008-12-09
申请号：US10480958
申请日：2002-06-11
申请人： Romano Di Fabio , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Bendetta Perini , Yves St-Denis
发明人： Romano Di Fabio , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Bendetta Perini , Yves St-Denis
IPC分类号： A61K31/519 , C07D487/04 , A61P25/24 , A61P25/22
CPC分类号： C07D487/04 , A61K51/0459 , C07B2200/05 , C07D239/70 , C07D239/94 , C07D471/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein R is aryl or heteroaryl and each of the above groups R may be substituted by 1 to 4 groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, —COR4, nitro, —NR3R4 cyano, or a group R5; R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkyl, halo C1-C6 alkoxy, halogen, NR3R4 or cyano; R2 corresponds to a group CHR6R7; R3 is hydrogen, C1-C6 alkyl; R4 independently from R3, has the same meanings; R5 is C3-C7 cycloalkyl, which may contain one or more double bonds; aryl; or a 5-6 membered heterocycle; wherein each of the above groups R5 may be substituted by one or more groups selected from: halogen, C1-C6 alkyl, C1-C6 alkoxy, halo C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo C1-C6 alkoxy, C1-C6 dialkylamino, nitro or cyano; R6 is hydrogen, C2-C6 alkenyl or C1-C6 alkyl, wherein each of the above groups R6 may be substituted by one or more groups selected from: C1-C6 alkoxy and hydroxy; R7 independently from R6, has the same meanings; X is carbon or nitrogen; to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF).
摘要翻译：本发明提供式（I）化合物，其包括立体异构体，前药和药学上可接受的盐或溶剂合物，其中R是芳基或杂芳基，并且上述基团中的每一个R可以被1至4个选自以下的基团取代：卤素，C 1 -C 6 烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷氧基，-COR 4，硝基，-NR 3 R 4氰基或基团R 5; R 1是氢，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，卤代C 1 -C 6烷氧基，卤素，NR 3 R 4或氰基; R2对应于CHR6R7基团; R3是氢，C1-C6烷基; R4独立于R3，具有相同的含义; R5是C3-C7环烷基，其可以含有一个或多个双键; 芳基; 或5-6元杂环; 其中每个上述基团R 5可以被一个或多个选自以下的基团取代：卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，卤代C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6 烷氧基，C1-C6二烷基氨基，硝基或氰基; R 6是氢，C 2 -C 6烯基或C 1 -C 6烷基，其中上述基团R 6可以被一个或多个选自以下的基团取代：C 1 -C 6烷氧基和羟基; R7独立于R6，具有相同的含义; X是碳或氮; 其制备方法，含有它们的药物组合物及其用于治疗由促肾上腺皮质激素释放因子（CRF）介导的病症的用途。

19. 发明授权

US07279474B2 Substituted pyrrolo[2,3-d]pyrimidines as antagonists of the corticotropin releasing factor (CRF) 失效
标题翻译：取代的吡咯并[2,3-d]嘧啶作为促肾上腺皮质激素释放因子（CRF）的拮抗剂
公开(公告)号：US07279474B2
公开(公告)日：2007-10-09
申请号：US10476368
申请日：2002-04-30
申请人： Anna Maria Capelli , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Benedetta Perini , Yves St-Denis , Romano Di Fabio
发明人： Anna Maria Capelli , Chiara Marchionni , Fabrizio Micheli , Alessandra Pasquarello , Benedetta Perini , Yves St-Denis , Romano Di Fabio
IPC分类号： A61K31/5355 , A61K31/519 , C07D487/04 , C07D413/14 , A61P25/24 , A61P25/22
CPC分类号： C07D487/04 , A61K51/0459 , A61K51/0463 , A61K51/0465 , C07D239/70 , C07D239/94 , C07D471/04
摘要： The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein the variables are as defined in the description, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions mediated by corticotropin-releasing factor (CRF)
摘要翻译：本发明提供了式（I）化合物，其包括立体异构体，前药和药学上可接受的盐或溶剂合物，其中变量如本说明书所定义，其制备方法，含有它们的药物组合物及其在治疗由促肾上腺皮质激素释放因子（CRF）

20. 发明授权

US06479488B1 Tetrahydroquinoline derivatives as EAA antagonists 失效
标题翻译：四氢喹啉衍生物作为EAA拮抗剂
公开(公告)号：US06479488B1
公开(公告)日：2002-11-12
申请号：US09147568
申请日：2000-10-30
申请人： Romano Di-Fabio , Alessandra Pasquarello , Fabio Maria Sabbatini
发明人： Romano Di-Fabio , Alessandra Pasquarello , Fabio Maria Sabbatini
IPC分类号： A61K3147
CPC分类号： C07D215/48
摘要： Compounds of formula (I) or salt, or metabolically labile ester thereof wherein R represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethoxy, nitro, cyano, SO2R2 or COR2 wherein R2 represents hydroxy, methoxy, amino, alkylamino or dialkylamino; m is zero or an integer 1 or 2; R1 represents cyano or the group (CH2)nCN, —CH═CHR3, CH2)nNHCOCH2R4 or O(CH2)pNR5R6; R3 represents cyano or the group COR7; R4 represents alkoxy or a group NHCOR8; R5 and R6 each represent independently hydrogen or alkyl, or R5 and R6 together with the nitrogen atom to which they are attached represent a heterocyclic group, or R5 is hydrogen and R6 is the group COR9; R7 represents an alkoxy, amino or hydroxyl group; R8 represents a hydrogen atom or optionally substituted alkyl, alkoxy, aryl, or heterocyclic group; R9 is the group R8 or the group NR10R11 wherein R10 represents hydrogen or alkyl group; R11 represents optionally substituted alkyl, aryl, heterocyclic or cycloalkyl group; n is zero or an integer from 1 to 4, p is an integer from 2 to 4, processes for their preparation and to their use in medicine.
摘要翻译：式（I）化合物或其盐或其代谢不稳定的酯，其中R表示选自卤素，烷基，烷氧基，氨基，烷基氨基，二烷基氨基，羟基，三氟甲氧基，硝基，氰基，SO2R2或COR2的基团，其中R2表示羟基，，氨基，烷基氨基或二烷基氨基; m为零或整数1或2; R1表示氰基或（CH2）nCN基团，-CH = CHR3，CH2）nNHCOCH2R4或O（CH2）pNR5R6; R3代表氰基或基团COR7; R4表示烷氧基或NHCOR8基团; R 5和R 6各自独立地表示氢或烷基，或者R 5和R 6与它们所连接的氮原子一起代表杂环基，或R5是氢，R6是基团COR9; R7表示烷氧基，氨基或羟基; R8表示氢原子或任选取代的烷基，烷氧基，芳基或杂环基; R9为基团R8或基团NR10R11，其中R10表示氢或烷基; R11表示任选取代的烷基，芳基，杂环或环烷基; n为0或1〜4的整数，p为2〜4的整数，其制备方法及其在医学上的应用。

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